Term
| sympathetic nervous system |
|
Definition
-Important regulator of activities of organs
-Especially in responses to stress
-Regulator of heart and peripheral vasculature |
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Term
|
Definition
| Drugs that mimic stimulation of sympathetic nervous system |
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Term
|
Definition
|
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Term
|
Definition
| drug acts directly on the receptor |
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Term
| example of direct activation |
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Definition
|
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Term
|
Definition
| Drug actions depend on release of endogenous catecholamines |
|
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Term
| mechanisms of indirect activation |
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Definition
1. displacement
2. reuptake inhibition
3. blockade of metabolism |
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Term
|
Definition
| Drug causes displacement (dumping) of stored catecholamines |
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Term
|
Definition
|
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Term
|
Definition
| Drugs can inhibit reuptake of catecholamines already released |
|
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Term
| examples of re-uptake inhibition |
|
Definition
| cocaine and tricyclic antidepressants |
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Term
| Blockade of metabolism occurs via |
|
Definition
Catechol-O-methyltransferase (COMT)
Monoamine oxidase (MAO) |
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Term
| blockade or inhibition enzymes |
|
Definition
Increases stores of catecholamines
Indirectly potentiates sympathomimetic actions
Example: MAO Inhibitors (Parnate, Nardil, Marplan) |
|
|
Term
| examples of MAO inhibitors |
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Definition
|
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Term
|
Definition
| Drugs can be classified by the receptors they activate |
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Term
| example of spectrum of action |
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Definition
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Term
|
Definition
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Term
|
Definition
| derived from amino acid-tyrosine |
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Term
| availability of catecholamines |
|
Definition
Endogenously (released from adrenal glands during stress)
and As a drug |
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Term
|
Definition
| Not given orally- Rapidly metabolized by COMT and MAO |
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Term
|
Definition
Given parentally- Short duration of action
Does not significantly enter CNS through IV route |
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|
Term
| examples of Phenylisopropylamines |
|
Definition
|
|
Term
|
Definition
Are NOT catecholamines
NOT metabolized by COMT and MAO
Given orally
Enter CNS readily
Effects last longer than catecholamines |
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Term
|
Definition
Sympathomimetic found in foods
Not a phenylisopropylamine
Is rapidly metabolized by MAO
MAO Inhibitor drugs can cause tyramine toxicity |
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|
Term
| Mechanism of Action of Sympathomimetics |
|
Definition
Act via principal receptors
α – receptors
ß – receptors
DA – receptors |
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Term
|
Definition
|
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Term
|
Definition
|
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Term
|
Definition
| Response to drugs differs in various tissues |
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Term
| Beta adrenoreceptors subtypes |
|
Definition
- ß1 and ß2 (ß3 novel)
- defined by affinity for EPI and NE |
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Term
|
Definition
| EPI = NE (equal affinity) |
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Term
|
Definition
|
|
Term
|
Definition
Distinct from α and ß receptors
Mainly important in brain and splanchnic and renal vasculature
Highly relevant to behavior and Parkinson’s Disease |
|
|
Term
| dopamine receptors main subtypes |
|
Definition
|
|
Term
| dopamine receptors subtypes within subtypes |
|
Definition
D1 like- D1 , D5
D2 like- D2 , D3 , D4
AE and efficacy of antipsychotic drugs vary between subtypes |
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Term
|
Definition
Drug may prefer to bind to one subgroup over another at low concentrations
Not absolute (“specificity” is nearly absolute)
Numeric subclass is important for drugs with selectivity |
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Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| prostate drugs α1 blocker |
|
Definition
Hytrin (terazosin)
Lowers BP and relaxes neck of bladder |
|
|
Term
| prostate drugs α1A blocker |
|
Definition
Flomax (tamsulosin) developed
α1A selective, found mostly in prostate & neck bladder
Results in bladder relaxation without so much BP lowering
more selective |
|
|
Term
| Effects of catecholamines |
|
Definition
| are mediated by cell surface receptors |
|
|
Term
|
Definition
| are coupled by G (guanine) proteins to produce their effects |
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Term
|
Definition
| is changing intracellular calcium concentration |
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|
Term
| Stimulation of α1 receptors leads to |
|
Definition
-activation of Gq-coupling protein
-This leads to release of IP3 and DAG
-IP3 stimulates release of sequestered stores of Ca++
-Increase in intracellular Ca++ causes contraction/constriction |
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|
Term
|
Definition
Phenylephrine
Effects: increase IP3, DAG |
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Term
|
Definition
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|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| Stimulation of β receptors |
|
Definition
-activate Gs coupling protein
-Results in activation of adenylyl cyclase
-Catalyzes conversion of ATP to cAMP
-Leads to Ca++ influx and release of sequestered Ca++
-Cardiac tissue=heart contractility
-SA node=increased HR
-Smooth muscle=muscle relaxation |
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|
Term
|
Definition
|
|
Term
| beta 1 receptor antagonist |
|
Definition
|
|
Term
|
Definition
|
|
Term
| beta 2 receptor antagonist |
|
Definition
|
|
Term
| beta 1 and 2 receptor agonist |
|
Definition
| isoproterenol -increase CAMP |
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|
Term
|
Definition
|
|
Term
|
Definition
| Stimulates adenylyl cyclase = ↑ cAMP in smooth muscle = relaxation of smooth muscle (vasodilator) |
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Term
|
Definition
| Inhibit adenylyl cyclase = ↓ cAMP, open K channels and ↓ Ca influx |
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|
Term
|
Definition
Fenoldopam (used for severe HTN)
Effect: increase cAMP |
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Term
|
Definition
Bromocriptine - many uses, Infertility, Parkinson‘s, prevent lactation
Effect: decrease cAMP |
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Term
|
Definition
|
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Term
|
Definition
| Clozapine- Effect: decrease cAMP |
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Term
|
Definition
|
|
Term
|
Definition
tissue becomes less responsive with repeated exposure by agonist
a.k.a-tolerance, refractoriness and tachyphylaxis |
|
|
Term
| Homologous desensitization |
|
Definition
| – loss of responsiveness exclusively only to directly exposed receptors |
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|
Term
| Heterologous desensitization |
|
Definition
| loss of responsiveness to exposed and some non-exposed receptors |
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Term
|
Definition
| most vascular smooth muscle- constriction |
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Term
|
Definition
| pupillary dilator muscle- contraction= dilation of pupil |
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Term
|
Definition
| pilomotor smooth muscle- erects hair |
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Term
|
Definition
|
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Term
|
Definition
| heart- increases force of contraction |
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Term
|
Definition
| postsynaptic CNS adrenoceptors- multiple effects |
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Term
|
Definition
|
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Term
|
Definition
| adrenergic nerve terminals- inhibition of transmitter release |
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Term
|
Definition
| cholinergic nerve terminals- inhibition of transmitter release |
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Term
|
Definition
| some vascular smooth muscle- contraction |
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Term
|
Definition
| fat cells- inhibition of lipolysis |
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Term
|
Definition
| pancreatic B cells- inhibits insulin release |
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Term
|
Definition
| heart- increase force and rate of contraction |
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Term
|
Definition
| kidney (juxtaglomerular cells)- increase renin release |
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Term
|
Definition
| respiratory muscle- promote smooth muscle relaxation |
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Term
|
Definition
| uterine muscle- promote smooth muscle relaxation |
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Term
|
Definition
| vascular smooth muscle- promote smooth muscle relaxation |
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Term
|
Definition
| skeletal muscle- promotes potassium uptake= tremor |
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Term
|
Definition
| pancreatic B cells- increase insulin release |
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Term
|
Definition
| liver- activates glycogenolysis= increase glucose |
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Term
|
Definition
| fat cells- stimulates lipolysis |
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Term
|
Definition
| renal blood vessels- dilates renal blood vessels |
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Term
|
Definition
| splanchnic blood vessels- dilates renal blood vessels |
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Term
|
Definition
| nerve endings- modulates transmitter release |
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Term
|
Definition
| control peripheral vascular resistance |
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Term
|
Definition
| increase arterial resistance |
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Term
|
Definition
| promote smooth muscle relaxation |
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Term
|
Definition
| promote vasodilation of kidneys playing a role in natriuresis |
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Term
|
Definition
| effect depending on anatomical site |
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Term
|
Definition
| Largely determined by β1 receptors |
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Term
|
Definition
-Activation results in Ca++ influx
-SA node & purkinje fibers increase – positive chronotropic effect
-AV node – conduction velocity ↑ & refractory period ↓
-Intrinsic contractility is increased – positive inotropic effect and relaxation is accelerated
-Ejection time is decreased |
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Term
|
Definition
-Produces peripheral vasoconstriction and resistance
-↑ SBP and DBP |
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Term
|
Definition
| Increases cardiac output (↑ HR and contractility) |
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Term
|
Definition
| Vasodilatation and ↓ peripheral vascular resistance |
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Term
|
Definition
|
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Term
|
Definition
| increases outflow of aqueous humor from the eye – reduces IOP |
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Term
|
Definition
| decrease production of aqueous humor |
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Term
|
Definition
| decrease in accommodation- ciliary muscle |
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Term
|
Definition
| relaxation- bronchodilation |
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Term
|
Definition
| vasoconstriction- Blood vessels of upper respiratory tract mucosa (sinuses) |
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|
Term
| a receptors mostly (b also) |
|
Definition
| GI smooth muscle relaxation |
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Term
|
Definition
| decrease salt and water flux into the lumen of the intestine |
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|
Term
| a and b receptors contained? |
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Definition
|
|
Term
|
Definition
| mediate contraction – promotes urinary incontinence |
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Term
|
Definition
|
|
Term
|
Definition
| Ejaculation- (ductus deferens, seminal vesicles & prostate) |
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|
Term
| Many symphathomimetic drugs causes what? |
|
Definition
|
|
Term
| apocrine sweat glands is stimulated by? |
|
Definition
| adrenoceptor stimulants that causes sweaty palms |
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|
Term
| b3 in fat cells causes what? (metabolic) |
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Definition
|
|
Term
| increase in glycogenolysis in liver cause an increase in? |
|
Definition
| glucose (sympathomimetic drugs) |
|
|
Term
| insulin secretion is stimulated by this receptor? |
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Definition
|
|
Term
| insulin secretion is inhibited by this receptor? |
|
Definition
|
|
Term
| renin secretion is stimulated by this receptors? |
|
Definition
|
|
Term
| renin secretion is inhibited by this receptors? |
|
Definition
|
|
Term
| beta blockers can lower what? |
|
Definition
|
|
Term
| leukocytosis or an increase in WBC can be caused by what? |
|
Definition
|
|
Term
|
Definition
Actions vary dramatically
Depending on ability to cross BBB
Usually cross in high rates of infusion
Nervousness, tachycardia, tremor
Elevation of mood, insomnia, anorexia |
|
|
Term
|
Definition
Epinephrine
Norepinephrine
Isoproterenol
Fenoldopam |
|
|
Term
|
Definition
Dopamine
Dopamine agonist
Dobutamine |
|
|
Term
| Epinephrine (adrenaline) is a potent agonist at all? |
|
Definition
|
|
Term
|
Definition
| increases BP and vasoconstriction |
|
|
Term
|
Definition
| increase HR and increase contractility= cardiac stimulation |
|
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Term
|
Definition
| blood vessel dilation in skeletal muscle= bronchodilation |
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|
Term
|
Definition
| levarterenol and noradrenaline |
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Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| a1 is greater than b1 and little effect on b2 |
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Term
|
Definition
| increase PVR and both SBP and DBP |
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Term
|
Definition
| increase BP = vasoconstriction |
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|
Term
|
Definition
| increase HR and increase contractility= cardiac stimulation |
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Term
|
Definition
| isoproterenol or isoprenaline |
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|
Term
| Isoproterenol (isoprenaline) |
|
Definition
| Potent β- agonist (little α- effect) |
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Term
| Isoproterenol (isoprenaline) |
|
Definition
| Positive chronotropic & inotropic actions= ↑ cardiac output |
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Term
| Isoproterenol (isoprenaline) |
|
Definition
|
|
Term
| Isoproterenol (isoprenaline) |
|
Definition
| ↓ in diastolic & mean arterial pressure |
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|
Term
| Isoproterenol (isoprenaline) b1 agonist |
|
Definition
| increase HR and increase contractility= cardiac stimulation |
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|
Term
| Isoproterenol (isoprenaline) b2 agonist |
|
Definition
| blood vessel dilation in skeletal muscle= bronchodilation |
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Term
|
Definition
|
|
Term
|
Definition
| Activates presynaptic D2=↓ EPI release |
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Term
|
Definition
| Activates D1 and β2 = vasodilation (↓ PVR) |
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Term
|
Definition
| Activates β1 in the heart = some ↑ in HR |
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Term
|
Definition
|
|
Term
|
Definition
| High doses = activates α; mimics EPI |
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Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| IV treatment of severe HTN |
|
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Term
|
Definition
| Bromocriptine-dopamine 2 agonist |
|
|
Term
| Bromocriptine-dopamine 2 agonist |
|
Definition
| Tx of Parkinson’s disease |
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|
Term
| Bromocriptine-dopamine 2 agonist |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| Phenylephrine (Neo-synephrine) is an? |
|
Definition
|
|
Term
| Phenylephrine (Neo-synephrine) is used for? |
|
Definition
| decongestant and to increase BP |
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Term
|
Definition
|
|
Term
| midodrine is used for treating? |
|
Definition
|
|
Term
| Ephedrine (ma-huang) is a stimulant that releases? |
|
Definition
| catecholamines (never studied) |
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|
Term
| Oxymetazoline (Afrin, Visine) is a? |
|
Definition
|
|
Term
| Oxymetazoline (Afrin, Visine) is a vasoconstrictor used for? |
|
Definition
| decongestant and decrease eye redness |
|
|
Term
| Oxymetazoline (Afrin, Visine) is a type of drug? |
|
Definition
|
|
Term
| Amphetamine is misused as a? |
|
Definition
| CNS stimulant (anorexiant and alertness) |
|
|
Term
| Amphetamine is a stimulant that releases? |
|
Definition
|
|
Term
| Methamphetamine is similar to what? |
|
Definition
| amphetamine but more CNS effect |
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Term
| Methylphenidate (Ritalin) is stimulant used for? |
|
Definition
|
|
Term
| pemoline is a stimulant used for? |
|
Definition
| ADHD but no longer available due to hepatic failure |
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Term
| modafinil or provigil is a stimulant used for? |
|
Definition
|
|
Term
| a2 agonists are used for? |
|
Definition
|
|
Term
| give examples of a2 agonists? |
|
Definition
| clonidine, methyldopa, guanfacine, guanabenz |
|
|
Term
|
Definition
|
|
Term
| an example of a beta 1 selective agonist is? |
|
Definition
-dobutamine
- Less vasodilation (less β2) = increase CO w/less tachycardia |
|
|
Term
| beta 2 selective agents are? |
|
Definition
-Albuterol -used for asthma
-Terbutaline -used for uterine relaxation (premature labor) |
|
|
Term
| an example of a special sympathomimetics is? |
|
Definition
|
|
Term
|
Definition
nerve permeability to Na=↓nerve impulse conduction
Topical anesthetic (oral and nasal membranes) |
|
|
Term
| cocaine stimulates the release of? |
|
Definition
|
|
Term
|
Definition
| reuptake - stimulant/sympathomimetic |
|
|
Term
| cocaine stimulates the release of ? |
|
Definition
| DA and inhibits reuptake that causes significant euphoria = addiction |
|
|
Term
| an example of a special sympathomimetic drug? |
|
Definition
|
|
Term
|
Definition
Natural occurring in body
Also found in some fermented foods
Not a drug, but interacts with drugs |
|
|
Term
|
Definition
Rapidly degraded by MAO in gut and liver
When MAO is not available to degrade tyramine = high amounts of tyramine = release of catecholamines
MAO inhibitors (Nardil, Marplan, Parnate)
Results in sympathomimetic effects
Increase in BP |
|
|
Term
| examples of MAO inhibitors are ? |
|
Definition
|
|
Term
| Foods that contain tyramine? |
|
Definition
Beer
Broad beans/fava beans
Cheese
Chicken liver
Chocolate |
|
|
Term
| Foods that contain tyramine ? |
|
Definition
sausage
Salami
Pepperoni
Pickled herring
Snails
Red wine |
|
|
Term
| medications that are needed to enhance blood flow and pressure? |
|
Definition
Norepinepherine
Phenylephrine
Methoxamine
Ephedrine
Midodrine |
|
|
Term
| shock is a reduction in ? |
|
Definition
| perfusion of vital tissues |
|
|
Term
| 3 major mechanisms responsible for shock |
|
Definition
Hypovolemia
Cardiac insufficiency
Altered vascular resistance |
|
|
Term
|
Definition
| One of the mainstays of treatment of shock |
|
|
Term
| volume replacement is an ? |
|
Definition
| Efficacy of sympathomimetic drugs are used but efficacy unclear |
|
|
Term
| medications for treating cardiogenic shock? |
|
Definition
|
|
Term
| cardiogenic shock is usually due to ? |
|
Definition
|
|
Term
| cardiogenic shock have poor ? |
|
Definition
|
|
Term
|
Definition
| positive inotropic agents with little peripheral vasoconstriction |
|
|
Term
| Conditions in which reduction of local or regional blood is needed |
|
Definition
Achieving hemostasis in surgery
Reducing diffusion of anesthetics away from site of administration
Reducing mucous membrane congestions
α receptor activation usually desired |
|
|
Term
| EPI (cardiovascular applications) |
|
Definition
topical nasal packs for epistaxis
In gingival string for gingivectomy
Combined with local anesthetics prolongs effects and reduces toxicity |
|
|
Term
| cocaine (cardiovascular applications) |
|
Definition
Used for nasopharyngeal surgery
Has combination hemostatic and local anesthetic effect |
|
|
Term
| phenylphrine (cardiovascular applications) |
|
Definition
Used for nasal decongestant
Prolonged use can cause rebound congestions due to ischemic changes |
|
|
Term
| isoproterenol (cardiovascular application) is used for? |
|
Definition
| Emergency management of complete heart block and cardiac arrest |
|
|
Term
| EPI (cardiovascular application) is used for ? |
|
Definition
| Emergency management of complete heart block and cardiac arrest |
|
|
Term
| dobutamine (cardiovascular application) is used for ? |
|
Definition
|
|
Term
| type of b2 selective agents ? |
|
Definition
| metaproterenol, terbutaline, and albuterol |
|
|
Term
| metaproterenol is used for ? |
|
Definition
|
|
Term
| terbutaline is used for ? |
|
Definition
|
|
Term
|
Definition
|
|
Term
| anaphylaxis affect both ? |
|
Definition
| respiratory and CV system |
|
|
Term
|
Definition
Bronchospasm
Mucous membrane congestion
Angioedema
Severe hypotension |
|
|
Term
| what is the treatment of anaphylaxis ? |
|
Definition
|
|
Term
| phenylephrine is what type of medication? |
|
Definition
|
|
Term
|
Definition
| mydriatic agent to facilitate examination of the retina |
|
|
Term
| apraclonidine and brimonidine (a2 agonist) is what type of medication ? and what are they used for ? |
|
Definition
| ophthalmic medication and are used to lower IOP (glaucoma) |
|
|
Term
| ritodrine and terbutaline are medications of the ? |
|
Definition
|
|
Term
| ritodrine and terbutaline are b2 agonists that are used to what? |
|
Definition
| relaxes the uterus and suppress premature labor |
|
|
Term
| amphetamines are medication used for the ? |
|
Definition
|
|
Term
| amphetamines are used for the following effects? |
|
Definition
mood elevating (euphoria) causing abuse
Increases alertness (modafinil for narcolepsy)
Improved attention (ADHD)
Appetite suppressant |
|
|
Term
| toxicity effects of sympathomimetic drugs on CV system? |
|
Definition
| increase BP, increased cardiac work which precipitates cardiac ischemia and failure |
|
|
Term
| toxicity effects of sympathomimetic drugs on CNS ? |
|
Definition
| restlessness, tremor, insomnia, anxiety and induced paranoid state |
|
|
Term
| cocaine toxicity of sympathomimetic drugs ? |
|
Definition
| convulsions, cerebral hemorrhage, arrhythmias, MI |
|
|
Term
| alpha receptor antagonists can be ? |
|
Definition
| reversible or irreversible |
|
|
Term
| alpha receptor antagonist (reversible) |
|
Definition
Dissociate from receptors & can be surmounted by high agonist concentrations
Duration of action depends on t1/2 and rate of dissociation from receptor |
|
|
Term
| examples of apha receptor antagonist (reversible)? |
|
Definition
| prazosin and phentolamine |
|
|
Term
| alpha receptor antagonists (irreversible) |
|
Definition
Do not dissociate & can’t be surmounted
Effects of drug may persist after drug has cleared plasma |
|
|
Term
| an example of alpha receptor antagonist ? |
|
Definition
| Phenoxybenzamine- restoration of tissue responsiveness is dependent on synthesis of new receptors which takes several days |
|
|
Term
| cardiovascular effects of alpha receptor antagonists can ? |
|
Definition
| Cause lowering of peripheral vascular resistance and blood pressure |
|
|
Term
| often causes of alpha receptor antagonist are ? |
|
Definition
Postural hypotension
Reflex tachycardia
More selective to alpha-1 the less tachycardia |
|
|
Term
| other effects of alpha receptor antagonists are ? |
|
Definition
Miosis (constriction of pupil)
Nasal stuffiness
Decrease resistance in urine flow |
|
|
Term
| an example of a specific alpha blocking agents is ? |
|
Definition
|
|
Term
|
Definition
-Antagonist at alpha 1 & 2
-Causes reduction in peripheral resistance
-Has limited absorption after oral administration
-Half life is 5-7 hrs
-Adverse effect: HA, nasal congestion, severe tachycardia, arrhythmias & myocardial ischemia |
|
|
Term
| phentolamine is used for treating ? |
|
Definition
| pheochromocytoma and erectile dysfunction |
|
|
Term
| an example of specific alpha blocking agents is ? |
|
Definition
|
|
Term
| Phenoxybenzamine is used for treating ? |
|
Definition
|
|
Term
|
Definition
Irreversible blockade
Long duration of action:14-48 h or longer
Somewhat selective for alpha-1
Also blocks H1, acetylcholine and serotonin
Adverse effects: postural hypotension, tachycardia, nasal stuffiness, inhibition of ejaculation
Other effects: fatigue, sedation & nausea |
|
|
Term
| an example of a specific alpha blocking agent is? |
|
Definition
|
|
Term
| prazosin is used for treating ? |
|
Definition
|
|
Term
| prazosin (minipress) is ? |
|
Definition
Highly selective for alpha-1
Significantly less tachycardia because less blocking of α-2
Relaxation of both arterial & venous vascular smooth muscle and smooth muscle of prostate
Metabolized by the liver
Half life: 3 hrs |
|
|
Term
| an example of a specific alpha blocking agents is ? |
|
Definition
|
|
Term
| terazosin (hytrin) is used for treating ? |
|
Definition
|
|
Term
|
Definition
Alpha-1 selective
Metabolized in the liver
Half life: 9-12 hrs |
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Term
| an example of a specific alpha blocking agent is ? |
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Definition
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Term
| doxazosin is used for treating ? |
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Definition
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Term
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Definition
Half life: 22 hrs
longer than prazosin and terazosin |
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Term
| an example of a specific alpha blocking agent is ? |
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Definition
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Term
| Tamsulosin (Flomax) used for treating ? |
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Definition
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Term
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Definition
Selective to alpha-1A subtype
Greater potency in inhibiting contraction in prostate smooth muscle than vascular smooth muscle compared to other alpha blockers
Half life: 9-15 hrs |
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Term
| examples of other alpha antagonists are |
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Definition
| alfuzosin (uroxatrol), indoramin, urapidil (european drug), labetalol, yohimbine |
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Term
| alfuzosin (uroxatrol) is used for treating ? |
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Definition
BPH
Selective alpha-1 antagonist
Half life: 5 hrs |
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Term
| indoramin is used for treating ? |
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Definition
HTN
selective alpha 1 antagonist |
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Term
| urapidil is used for treating ? |
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Definition
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Term
| labetalol is used for treating ? |
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Definition
HTN
both a1 and beta blocker |
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Term
| examples of neuroleptic drugs ? |
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Definition
| chlorpromazine and haloperidol |
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Term
| chlorpromazine and haloperidol are ? |
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Definition
potent DA receptro antagonists
also alpha antagonists
contributes to AE of hypotension |
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Term
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Definition
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Term
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Definition
abruptly reverse the antihypertensive effects of alpha 2 agonist (clonidine)
Serious drug interaction |
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Term
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Definition
| alpha 2 selective antagonist |
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Term
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Definition
Tumor usually found on the adrenal medulla
Typically releases EPI & NE in excess
Sx: HTN, HA, palpitations & ↑ sweating
Unavoidable release of catecholamines can occur during surgery |
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Term
| pheochromocytoma can be pretreated by this medication to control HTN before surgery ? |
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Definition
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Term
| can use this medication for hypertensive emergency ? |
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Definition
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Term
| this medication can be use for treating mild to moderate hypertension ? |
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Definition
| member of prazosin family |
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Term
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Definition
Interesting side effect of α-1 selective blockers
Occurs within 1-3 hours of 1st dose or increased dose
Transient dizziness or faintness
Palpitations
Orthostatic hypotension
Helps to have patient take 1st or 1st increase dose at bedtime |
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Term
| drugs that are used for peripheral vascular disease ? |
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Definition
phentolamine, prazosin, or phenoxybenzamine
May be used in Raynaud’s phenomenon or other conditions involving excessive reversible vasospasms |
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Term
| phentolamine is used to ? |
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Definition
| reverse intense local vasoconstriction caused by inadvertent infiltration of catecholamines into subcutaneous tissue that was intended to be IV |
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Term
| preferred drug for urinary obstruction (BPH) ? |
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Definition
tamsulosin- Relieving symptoms involves reversal of smooth muscle contraction of neck of bladder and enlarged prostate
prazosin, doxazosin, & terazosin considered if HTN as well |
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Term
| drugs that are used to treat erectile dysfunction ? |
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Definition
phentolamine with nonspecific smooth muscle relaxant papaverine
phentolamine with nonspecific smooth muscle relaxant papaverine
Helps with ED when directly injected into penis
Longterm use can cause fibrotic changes
Other AE: priapism, orthostatic hypotension |
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Term
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Definition
little clinical usefulness
Research looking into
Raynaud’s phenomenon-inhibit smooth muscle contraction
Type 2 DM (alpha 2 inhibits insulin secretion)
Psychiatric depression |
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Term
| common features of beta blockers ? |
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Definition
Occupy & block catecholamines effects at β receptors
End in –olol or –alol |
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Term
| differences of beta blockers ? |
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Definition
Cardioselectivity
Partial agonist activity/ISA
Lipid solubility |
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Term
| receptors that are all over the body but predominate in certain tissues and organs ? |
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Definition
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Term
| receptors that are in teh heart and kidney ? |
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Definition
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Term
| the stimulation of b1 receptors causes ? |
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Definition
| ↑HR, ↑contractility, ↑renin release= increase BP |
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Term
| receptors that are located in the lungs, liver, pancreas, and arteriolar smooth muscle ? |
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Definition
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Term
| the stimulation of b2 receptors causes ? |
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Definition
bronchodilation and vasodilation
Pancreas = ↑ insulin secretion
Liver = ↑ glycogenolysis |
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Term
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Definition
Blocks increase HR, contractility and renin
Without blocking broncho and vasodilation of β2 receptors in lungs, glucose and arteriolar smooth muscle |
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Term
| Cardioselective beta blockers are preferred in ? |
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Definition
asthma, COPD, DM and PVD
At higher doses cardioselectivity is less |
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Term
| examples of cardioselective beta blockers ? |
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Definition
Acebutolol
Atenolol
Betaxolol
Bisoprolol |
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Term
| examples of cardioselective beta blockers ? |
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Definition
Celiprolol
Esmolol
Metoprolol
Nebivolol |
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Term
| examples of non-selective beta blockers ? |
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Definition
Carteolol
Carvedilol
Labetolol
Nadolol |
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Term
| examples of non-selective beta blockers ? |
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Definition
penbutol
Pindolol
Propranolol
Sotalol
Timolol |
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Term
| partial β-agonist activity |
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Definition
Block effects of excessive sympathetic activity
Moderately activate receptors when sympathetic tone low
Therefore at rest, HR, CO and peripheral blood flow not reduced
Ideally for borderline HF, sinus bradycardia
aka: Intrinsic Sympathomimetic Activity (ISA) |
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Term
| examples of beta blockers with ISA ? |
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Definition
Acebutolol
Carteolol
Celiprolol |
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Term
| examples of beta blockers with ISA ? |
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Definition
Labetalol
Penbutolol
Pindolol |
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Term
| more lipophilic the more ? |
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Definition
CNS penetration
Increase in side effects
Depression
Sedation |
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Term
| beta blockers and high lipid solubility ? |
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Definition
Carvedilol
Penbutolol
Propranolol |
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Term
| beta blockers and moderate lipid solubility ? |
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Definition
Labetolol
Metoprolol
Pindolol
Timolol |
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Term
| beta blockers and low lipid solubility ? |
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Definition
Acebutolol
Atenolol
Betaxolol
Bisoprolol
Carteolol
Celiprolol
Esmolol
Nadolol
Sotalol |
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Term
| labetolol and carvedilol are ? |
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Definition
Non selective BB
Alpha 1 blocker |
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Term
| nebivolol (bystlic) are ? |
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Definition
Newest BB (approved 12/07)
Cardioselective BB
Nitric oxide mediated vasodilation |
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Term
| blocking b1 can make the heart have a ? |
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Definition
| negative chronotropic and inotropic effects |
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Term
| blocking b1 can make the kidney ? |
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Definition
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Term
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Definition
| Decrease in SA and AV node conduction |
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Term
| blocking b2 (non cardioselective BB) leads to ? |
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Definition
increased airway constriction and bronchospasms
Use in caution w/ asthma or COPD
Pts with COPD tolerate the drugs better
Select cardioselective BB in these pts |
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Term
| Can increase or decrease glucose (B2) |
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Definition
decrease insulin
decrease glycogenolysis
use with caution in diabetics |
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Term
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Definition
Chronic use can reduce HDL
ISA BB’s have less altered lipid effects |
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Term
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Definition
| propranolol, metoprolol, atenolol, nadolol, timolol, levobunolol, betaxolol, and esmolol |
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Term
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Definition
1st BB approved for clinical use
Half life: 3.5-6hrs
Selectivity: none
Partial agonist activity: no
Highly lipid soluble |
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Term
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Definition
Cardioselective
Preferred in respiratory diseases and PVD |
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Term
|
Definition
Longest durations of action
Half life: 14-24 hrs |
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Term
| timolol, levobunolol, and betaxolol |
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Definition
Non selective
Excellent ocular hypotensive effects with opthalmic use
Used in glaucoma |
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Term
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Definition
Ultra short acting
Half life: 10 min
Given as continuous IV infusion
Selectivity: Beta 1
Useful in tx supraventricular arrhythmias |
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Term
| the use of BB can effectively treatment this disease ? |
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Definition
hypertension
Proven to be effective & well tolerated
Less effective in elderly & African-Americans |
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Term
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Definition
Ischemic Heart Disease
Reduce frequency of anginal episodes & improve exercise tolerance
Reduces oxygen demand
Relative contraindications: bradycardia, hypotension, left ventricular failure, shock, heart block, active airway disease |
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Term
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Definition
Cardiac Arrhythmias
Effective in tx supraventricular & ventricular arrhythmias
Slows ventricular response rates in AFib & AFlutter |
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Term
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Definition
Heart Failure
Can worsen acute CHF
Chronic use can prolong life
MOA uncertain
Proven efficacy
metoprolol, bisoprolol or carvedilol |
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Term
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Definition
Chronic Glaucoma (open angle glaucoma)
Leading cause of Blindness
As eyes age increase in IOP can occur by
Over production of aqueous fluid and build up
Drainage system clogging
Increase in pressure causes damage to optic nerve and retina |
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Term
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Definition
| Pressure is due to overproduction or blocked drainage of fluid despite open space between iris and cornea |
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Term
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Definition
| Pressure is due to outflow of fluid being blocked due to structural abnormality |
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Term
| Narrow Angle or closed angle is usually ? |
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Definition
acute & causes pain (unlike open)
Usually treated urgently with surgery or drugs |
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Term
| Pre-op drugs limited to ? (narrow angle or closed angle) |
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Definition
Cholinomimetics
Acetazolamide
Osmotic agents
Onset of action of others too slow |
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Term
| 5 General Drug Classes used for glaucoma ? |
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Definition
Cholinomimetics
α agonists
BB
Prostaglandin analogs
Diuretics |
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Term
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Definition
Parasympathomimetic
Directly stimulates cholinergic receptors
Produces contraction of iris sphincter muscle
pupillary constriction (miosis)
constriction of the ciliary muscle
resulting in increased accommodation
reduction in intraocular pressure
associated with an increase in the outflow and a decrease in the inflow of aqueous humor |
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Term
| examples of cholinomimetic drugs ? |
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Definition
Pilocarpine
Carbachol
Physostigmine
Echothiophate
Demecarium |
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Term
| unselective alpha agonists ? |
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Definition
Epinephrine and dipivefrin
Mechanism: increase outflow |
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Term
| alpha 2 selective alpha agonists ? |
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Definition
Apraclonidine and brimonidine
Mechanism: decrease aqueous secretion |
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Term
| examples of beta blockers? |
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Definition
Timolol, betaxolol, carteolol, levobunolol, metipranolol
Mechanism: decrease aqueous secretion from the epithelium
Timolol drops can be systemically absorbed
Heart rate and airway effects
Can interact with other oral drugs like verapamil |
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Term
| Carbonic anhydrase inhibitors (diurectics) |
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Definition
Carbonic anhydrase enzyme is responsible for productions of forming hydrogen and bicarb ions from carbon dioxide and water
Inhibiting this enzyme causes decrease HCO3- resulting in diuretic effect
Also causes decrease aqueous secretion |
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Term
| examples of carbonic anhydrase inhibitors (diuretics) ? |
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Definition
| Dorzolamide, brinzolamide, acetazolamide, dichlorphenamide, methazolamide |
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Term
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Definition
Selective agonists for FP prostaglandin receptor
Results in increase outflow of aqueous humor |
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Term
| examples of Prostaglandin F2α ? |
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Definition
| Latanoprost, bimatoprost, travoprost, unoprostone |
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Term
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Definition
Hyperthyroidism
Inhibition of thyroxine (T4) conversion to triiodothyronine (T3)
Tx: thyroid storm w/ propranolol
Controls supraventricular tachycardias that often precipitate heart failure |
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Term
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Definition
Neurologic Disease
Migraines: propranolol reduces frequency & intensity
“Stage fright”: propranolol
Alcohol withdrawal in some pts |
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Term
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Definition
Esophageal varicies
BB reduce portal vein pressure in cirrhosis pts
Propranolol and nadolol can also prevent bleeding and decrease mortality |
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Term
| BB and Clinical Toxicology |
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Definition
Rash, fever, sedation, sleep disturbances, depression
More lipid soluble = more CNS side effects
Nadolol and atenolol are most water soluble |
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Term
| BB and Clinical Toxicology |
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Definition
Major Side Effects
Worsening or respiratory diseases
Life saving CVD benefits likely outweigh risk
Worsening of PVD
Worsening or heart failure
Hypotension
Bradycardia |
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Term
| BB and Clinical Toxicology |
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Definition
Can produce a syndrome of sympathetic over activity
agitation, headache, sweating, and nausea
Can provoke rapid upswings in blood pressure |
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Term
| BB and Clinical Toxicology |
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Definition
May mask symptoms of hypoglycemia in diabetics
Except sweating
Important counseling point |
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Term
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Definition
Performance anxiety
Mitral valve prolapse
Post-MI
HTN
Open angle glaucoma
Cardiac dysrythmias
Thyroid storm |
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Term
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Definition
Angina
Migraine prophylaxis
CHF
Aggressive behavior
Pheochromocytoma
GI hemorrhage
Essential tremors
Drug overdose??? |
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Term
| Cocaine Overdose Management |
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Definition
| Avoid beta-blockers to treat HTN |
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Term
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Definition
Thoracolumbar
“fight or flight” |
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Term
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Definition
| Collection of neurons in the walls of the gastrointestinal system |
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Term
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Definition
“rest and digest”
Craniosacral |
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Term
| Afferent (sensory) fibers |
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Definition
Run from periphery to integrating centers
Enteric plexus in gut |
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Term
| Cholinergic fibers release |
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Definition
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Term
| Noradrenergic (adrenergic) fibers releases |
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Definition
| Norepinephrine (noradrenaline) |
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Term
| is an important vasodilator transmitter in renal blood vessels |
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Definition
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Term
| cells that release Epi & NE? |
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Definition
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Term
| Most autonomic nerves also releases ? |
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Definition
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Term
| In most sympathetic postganglionic neurons, this is the primary transmitter ? |
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Definition
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Term
| examples of transmitters ? |
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Definition
ATP
CGRP
CCK
Dopamine
Enkephalin
Galanin
GABA
GRP |
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Term
| examples of transmitters ? |
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Definition
Neuropeptide Y
Nitric oxide
NE
Serotonin (5-HT)
Substance P
Vasoactive intestinal peptide |
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Term
| cholinergic receptors are affected by ? |
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Definition
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Term
| subtypes of cholinergic receptors are |
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Definition
muscarinic receptors
nicotinic receptors |
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Term
| CNS, sympathetic postganglionic neurons, some presynaptic sites |
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Definition
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Term
| Myocardium, smooth muscle, some presynaptic sites, CNS |
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Definition
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Term
| Exocrine glands, vessels (smooth muscle & endothelium), CNS neurons |
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Definition
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Term
| CNS, possibly vagal nerve endings |
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Definition
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Term
| Vascular endothelium, esp. cerebral vessels, CNS |
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Definition
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Term
| cholinoceptors are from ? |
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Definition
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Term
| Postganglionic neurons, some presynaptic cholinergic terminals |
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Definition
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Term
| Skeletal muscle neuromuscular end plates |
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Definition
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Term
| adrenergic receptors are affected by ? |
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Definition
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Term
| examples of catecholamine are ? |
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Definition
Norepinephrine (NE)
Epinephrine (EPI)
Dopamine (DA) |
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Term
| subtypes of adrenergic receptors are |
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Definition
α-adrenoceptors
β-adrenoceptors
Dopaminergic |
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Term
| types of adrenoceptors are ? |
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Definition
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Term
| Postsynaptic effector cells, esp. smooth muscle |
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Definition
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Term
| Presynaptic adrenergic nerve terminals, platelets, lipocytes, smooth muscle |
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Definition
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Term
| Post-synaptic effector cells, esp. heart, lipocytes, brain |
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Definition
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Term
| Post-synaptic effector cells, esp. smooth muscle and cardiac muscle |
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Definition
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Term
| Post-synaptic effector cells, esp. lipocytes and heart |
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Definition
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Term
| autonomic receptors (dopamine receptors) |
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Definition
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Term
| Brain, effector tissue, esp. smooth muscle of the renal vascular bed |
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Definition
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Term
| Brain, effector tissues, esp. smooth muscle, presynaptic nerve terminals |
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Definition
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Term
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Definition
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Term
| Brain, cardiovascular system |
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Definition
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Term
| Iris radial muscle – alpha 1 (SA) |
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Definition
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Term
| Ciliary muscle – beta – (SA) |
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Definition
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Term
| Iris circular muscle – M3 – (PA) |
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Definition
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Term
| Ciliary muscle – M3 - (PA) |
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Definition
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Term
| SA node – Beta1/Beta2 – (SA) |
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Definition
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Term
| Ectopic pacemakers – Beta1/Beta2 – (SA) |
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Definition
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Term
| Contractility – Beta 1/Beta2 – (SA) |
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Definition
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Term
|
Definition
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Term
| Contractility – M2 – (PA) |
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Definition
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Term
| Skin, splanchnic vessels – alpha (SA) |
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Definition
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Term
| Skeletal muscle vessels – Beta2 – (SA) |
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Definition
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Term
| Skeletal muscle vessels – alpha (SA) |
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Definition
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Term
| Skeletal muscle vessels – M3 – (SA) |
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Definition
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Term
|
Definition
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Term
| Bronchiolar Smooth Muscle- Beta2 (SA) |
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Definition
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Term
| Bronchiolar Smooth Muscle-M3- (PA) |
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Definition
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Term
| Gastrointestinal Tract-Smooth muscle of wall – alpha 2/Beta 2 – (SA) |
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Definition
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Term
| Gastrointestinal Tract- Smooth muscles of sphincters – alpha 1 – (SA) |
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Definition
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Term
| Gastrointestinal Tract- Smooth muscle of wall – M3 – (SA) |
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Definition
|
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Term
| Gastrointestinal Tract- Smooth muscles of sphincters – M3 – (SA) |
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Definition
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Term
| Gastrointestinal Tract- Secretion – M3 – (SA) |
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Definition
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Term
| Genitourinary Smooth Muscle- Bladder wall – Beta 2 – (SA) |
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Definition
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Term
| Genitourinary Smooth Muscle- Sphincter – alpha 1 – (SA) |
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Definition
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Term
| Genitourinary Smooth Muscle- Uterus, pregnant – Beta 2 (SA) |
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Definition
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Term
| Genitourinary Smooth Muscle- Uterus, pregnant – alpha – (SA) |
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Definition
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Term
| Genitourinary Smooth Muscle- Penis, seminal vesicle – alpha – (SA) |
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Definition
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Term
| Genitourinary Smooth Muscle- Bladder wall – M3 – (PA) |
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Definition
|
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Term
| Genitourinary Smooth Muscle- Sphincter – M3 – (PA) |
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Definition
|
|
Term
| Genitourinary Smooth Muscle- Uterus, pregnant – M3 (PA) |
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Definition
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|
Term
| Genitourinary Smooth Muscle- Penis, seminal vesicle – M3- (PA) |
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Definition
|
|
Term
| Pilomotor smooth muscle – alpha -(SA) |
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Definition
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|
Term
| Sweat glands – thermoregulatory – M (SA) |
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Definition
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|
Term
| Sweat glands – apocrine (stress) – alpha (SA) |
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Definition
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|
Term
|
Definition
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|
Term
|
Definition
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Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| central integration occurs in ? |
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Definition
Occurs in midbrain and medulla
ANS fully integrated |
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Term
| Cooperative interactions in ANS Occur in ? |
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Definition
brain stem, medulla, spinal cord
Baroreceptor in glossopharyngeal nerve
Sensory fibers in the urinary bladder wall |
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Term
| Example: slow infusion of NE |
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Definition
| Powerful vasoconstriction: ↑ peripheral vascular resistance → ↑ MAP |
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Term
| Example: slow infusion of NE (cardiac) |
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Definition
| Negative feedback baroreceptor responds to ↑ MAP |
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Term
| NET effect of ↑ peripheral vascular resistance, ↑ MAP, and a ? |
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Definition
|
|
Term
| autoreceptors respond to ? |
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Definition
|
|
Term
| autoreceptors modulate release of ? |
|
Definition
NT by the nerve
Usually inhibitory |
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Term
| Heteroreceptors May be activated by ? |
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Definition
| NTs released by other nerve terminals that synapse with the nerve ending |
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Term
| example of heteroreceptor action |
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Definition
| Vagal fibers in myocardium synapse on sympathetic adrenergic nerve terminals and inhibit NE release. |
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Term
| Modulation by history of activity (postsynaptic regulation) |
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Definition
| Up-regulation or down-regulation of receptor |
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Term
| example of Modulation by history of activity (postsynaptic regulation) |
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Definition
Denervation supersensitivity
Reserpine |
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Term
| Potential Pharmacologic Targets |
|
Definition
Synthesis
Storage
Release
Termination of action
Function of receptor |
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Term
| Action potential propagation |
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Definition
-Examples: local anesthetics, tetrodotoxin (toxin of puffer fish), saxitoxin (toxin of gonyaulax – red tide organism)
-Site: nerve axons
-Action: blocks sodium channel, blocks conduction |
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Term
|
Definition
-Example: hemicholinium
-Site: membrane of cholinergic nerve terminals
-Action: blocks uptake of choline and slows synthesis |
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Term
|
Definition
-Example: alpha-methyltyrosine (metyrosine)
-Site: cytoplasm of adrenergic nerve terminals and adrenal medulla
-Action: blocks synthesis |
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Term
|
Definition
-Example: vesamicol
-Site: cholinergic terminal vesicles
-Action: prevents storage, depletes ACh |
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Term
|
Definition
-Example: reserpine
-Site: adrenergic terminal vesicles
-Action: prevents storage, depletes NE and dopamine |
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Term
|
Definition
-Example: NE, DA, ACh, angiotensin II, various prostaglandins
-Site: nerve terminal membrane receptor
-Action: modulates release |
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Term
|
Definition
-Example: omega-conotoxin GVIA (toxin of marine snails)
-Site: nerve terminal calcium channel
-Action: reduces transmitter release |
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Term
|
Definition
-Example: Botulinum toxin
-Site: cholinergic vesicles
-Action: prevents release |
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Term
|
Definition
-Example: alpha latrotoxin (black widow spider venom)
-Site: cholinergic and adrenergic vesicles
-Action: causes explosive transmitter release |
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Term
|
Definition
-Example: tyramine, amphetamine
-Site: adrenergic nerve terminals
-Action: promote transmitter release |
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Term
| Transmitter uptake after release |
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Definition
-Example: cocaine, tricyclic antidepressants
-Site: adrenergic nerve terminals
-Action: inhibit uptake, increase transmitter effect on postsynaptic receptors |
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Term
| Receptor activation or blockade |
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Definition
-Example: norepinephrine
-Site: receptors at adrenergic junctions
-Action: binds alpha receptors, causes contraction |
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Term
| Receptor activation or blockade |
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Definition
-Example: phentolamine
-Site: receptors at adrenergic junctions
-Action: binds alpha receptors, prevents activation |
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Term
| Receptor activation or blockade |
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Definition
-Example: isoproterenol
-Site: receptors at adrenergic junctions
-Action: binds beta receptors |
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Term
| Receptor activation or blockade |
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Definition
-Example: propranolol
-Site: receptors at adrenergic junctions
-Action: binds beta receptors, prevents activation |
|
|
Term
| Receptor activation or blockade |
|
Definition
-Example: nicotine
-Site: receptors at nicotinic cholinergic junctions (autonomic ganglion, neuromuscular end plates)
-Action: binds nicotinic receptors, opens ion channel in postsynaptic membrane |
|
|
Term
| Receptor activation or blockade |
|
Definition
-Example: bethanechol
-Site: receptors, parasympathetic effector cells (smooth muscle, glands)
-Action: binds and activates muscarinic receptors |
|
|
Term
| Receptor activation or blockade |
|
Definition
-Example: atropine
-Site: receptors, parasympathetic effector cells
-Action: binds muscarinic receptors, prevents activation |
|
|
Term
| Enzymatic inactivation of transmitter |
|
Definition
-Example: neostigmine
-Site: cholinergic synapses (acetylcholinesterase)
-Action: inhibits enzyme which prolongs and intensifies transmitter action |
|
|
Term
| Enzymatic inactivation of transmitter |
|
Definition
-Example: tranylcypromine
-Site: adrenergic nerve terminals (monoamine oxidase)
-Action: inhibits enzyme which increases stored transmitter pool |
|
|
Term
| types of cholinomimetics drugs ? |
|
Definition
| ACh agonists, achE inhibitors, muscarinic, and nicotinic |
|
|
Term
| drugs that mimic ACH action? |
|
Definition
| ach agonists and ACHE inhibitors |
|
|
Term
|
Definition
|
|
Term
| tissues that are effected by muscarinic |
|
Definition
| smooth muscle, heart, & exocrine glands |
|
|
Term
| tissue that are effected by nicotinic |
|
Definition
| Skeletal muscle & autonomic ganglia |
|
|
Term
| muscarinic receptors (cholinoceptors) |
|
Definition
|
|
Term
| nicotinic (cholinoceptors) |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| seven transmembrane segments, Gq/11 protein linked |
|
|
Term
| M1 Postreceptor Mechanism: |
|
Definition
|
|
Term
|
Definition
| heart, nerves, smooth muscle |
|
|
Term
| M2 (cardiac M2) Structural features: |
|
Definition
| seven transmembrane segments, Gi/0 protein linked |
|
|
Term
| M2 (cardiac M2) Postreceptor Mechanism: |
|
Definition
| inhibition of cAMP production, activation of K+ channels |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Glands, smooth muscle, endothelium |
|
|
Term
|
Definition
| seven transmembrane segments, Gq/11 protein linked |
|
|
Term
| M4 Postreceptor Mechanism: |
|
Definition
|
|
Term
|
Definition
| Structural Features: seven transmembrane segments, Gi/0 protein linked |
|
|
Term
| M4 Postreceptor Mechanism: |
|
Definition
| inhibition of cAMP production |
|
|
Term
|
Definition
|
|
Term
|
Definition
| seven transmembrane segments, Gq/11 protein linked |
|
|
Term
| M5 Postreceptor Mechanism: |
|
Definition
|
|
Term
NM (muscle type, end plate receptor)
Location: |
|
Definition
| Skeletal muscle neuromuscular junction) |
|
|
Term
| NM (muscle type, end plate receptor) Structural Features: |
|
Definition
|
|
Term
| NM (muscle type, end plate receptor) Postreceptor Mechanism: |
|
Definition
| Na+, K+ depolarizing ion channel |
|
|
Term
NN (neuronal type, ganglion receptor)
Location: |
|
Definition
| postganglionic cell body, dendrites |
|
|
Term
| NN (neuronal type, ganglion receptor) Structural Features: |
|
Definition
|
|
Term
| NN (neuronal type, ganglion receptor) Postreceptor Mechanism: |
|
Definition
| Na+, K+ depolarizing ion channel |
|
|
Term
Direct acting cholinomimetic agents
Bind M receptors and/or N receptors |
|
Definition
|
|
Term
|
Definition
“reversible”
“irreversible” |
|
|
Term
| are Poorly absorbed and distributed into CNS |
|
Definition
|
|
Term
| Choline Ester Characteristics |
|
Definition
-Hydrophilic
Poorly absorbed and distributed into CNS
-Hydrolyzed in GI tract
-Differing susceptibility to hydrolysis
ACh is rapidly hydrolyzed
A large IV bolus lasts 5-20 seconds
-Methacholine → Carbachol, bethanechol |
|
|
Term
|
Definition
-Well absorbed from most sites of administration
-Nicotine can be absorbed through the skin
-Mainly excreted by the kidneys
-Acidifying the urine increases clearance |
|
|
Term
| Direct agonist: action on Cholinoceptor |
|
Definition
| muscarinic, and nicotinic |
|
|
Term
| Muscarinic (ACh released from PNS) |
|
Definition
Directly alters effector organ function
Binds muscarinic receptors on neurons which inhibits release of neurotransmitters |
|
|
Term
|
Definition
|
|
Term
| Eye Receptor: muscarinic Sphincter muscle of iris |
|
Definition
|
|
Term
Eye Receptor: muscarinic
Ciliary muscle |
|
Definition
| contraction -accommodation |
|
|
Term
Cardiovascular
Receptors: muscarinic
SA Node |
|
Definition
|
|
Term
Cardiovascular
Receptors: muscarinic
atria |
|
Definition
| Decrease in contractile strength & refractory period |
|
|
Term
Cardiovascular
Receptors: muscarinic
AV node |
|
Definition
Decrease in conduction velocity
Increase in refractory period |
|
|
Term
Cardiovascular
Receptors: muscarinic
ventricles |
|
Definition
| Small decrease in contractile strength |
|
|
Term
Cardiovascular
Receptors: muscarinic
net effect: |
|
Definition
| reduction in peripheral vascular resistance and change in heart rate |
|
|
Term
Blood Vessels
muscarinic
Arteries |
|
Definition
Dilation (via EDRF)
High dose direct effector response - constriction |
|
|
Term
Blood Vessels
muscarinic
veins |
|
Definition
Dilation (via EDRF)
High dose direct effector response - constriction |
|
|
Term
Respiratory System (Lungs)
Receptor: Muscarinic
bronchial muscle |
|
Definition
| constriction (bronchoconstriction) |
|
|
Term
Respiratory System (Lungs)
Receptor: Muscarinic
bronchial glands |
|
Definition
|
|
Term
Gastrointestinal Tract
Receptor: muscarinic
Motility |
|
Definition
|
|
Term
Gastrointestinal Tract
Receptor: muscarinic
sphincters |
|
Definition
|
|
Term
Gastrointestinal Tract
Receptor: muscarinic
secretion |
|
Definition
|
|
Term
Genitourinary tract (urinary bladder)
Receptors: muscarinic
Detrusor |
|
Definition
|
|
Term
Genitourinary tract (urinary bladder)
Receptors: muscarinic
trigone and sphincter |
|
Definition
|
|
Term
Secretory Glands
Receptors: muscarinic
Sweat |
|
Definition
|
|
Term
Secretory Glands
Receptors: muscarinic
salivary |
|
Definition
|
|
Term
Secretory Glands
Receptors: muscarinic
lacrimal |
|
Definition
|
|
Term
Secretory Glands
Receptors: muscarinic
nasopharyngeal |
|
Definition
|
|
Term
|
Definition
|
|
Term
| brain is richer in what receptors? |
|
Definition
|
|
Term
| spinal cord is richer in what receptors ? |
|
Definition
|
|
Term
| nicotinic receptors in high levels causes ? |
|
Definition
| tremor, emesis, and stimulation of the respiratory system |
|
|
Term
| nicotinic receptors in higher levels causes ? |
|
Definition
| convulsions which can lead to fatal coma |
|
|
Term
|
Definition
Nicotine has greater affinity for neuronal nicotinic receptors
hypertension
nausea
vomiting
diarrhea
Voiding of urine |
|
|
Term
Neuromuscular junction
Receptor: |
|
Definition
| nicotinic on the neuromuscular end plate |
|
|
Term
| nicotinic on the neuromuscular end plate result in ? |
|
Definition
| immediate depolarization of the end-plates |
|
|
Term
|
Definition
ACHE
note:Butyrylcholinesterase – also inhibited |
|
|
Term
| examples of cholinesterase inhibitors ? |
|
Definition
edrophonium
carbamates
neostigmine
organophosphates
echothiophate |
|
|
Term
| types of direct-acting cholinomimetics ? |
|
Definition
| MOA and cholinesterase inhibitors |
|
|
Term
|
Definition
-Relatively insoluble due to permanent charge
-Poor absorption from conjunctiva, skin, and lungs
-Larger oral doses required
-Negligible distribution to CNS
-Physostigmine is well absorbed though
Duration determined by stability of inhibitor-enzyme complex |
|
|
Term
|
Definition
-Well absorbed from skin, lung, gut, and conjunctiva
-Effective insecticides but dangerous to humans
-Distributed to all parts of the body
Exception is echothiophate
-CNS toxicity |
|
|
Term
| (Alcohols) Edrophonium Uses for ? |
|
Definition
Myasthenia gravis
Ileus
2-10 minutes |
|
|
Term
| (Carbamates and related agents) Neostigmine Uses for ? |
|
Definition
Myasthenia gravis
Ileus
1/2 hour to 2 hours |
|
|
Term
| (Carbamates and related agents) pyridostigmine uses for ? |
|
Definition
myasthenia gravis
3 to 6 hours |
|
|
Term
| (Carbamates and related agents) Physostigmine Uses for ? |
|
Definition
glaucoma
1/2 hour to 2 hours |
|
|
Term
| (Carbamates and related agents) ambenonium uses for ? |
|
Definition
myasthenia gravis
4 to 8 hours |
|
|
Term
| (Organophosphates) Echothiophate Uses for ? |
|
Definition
|
|
Term
| (Organophosphates) malathion and parathion are ? |
|
Definition
Highly lipid soluble
Thiophosphate prodrugs
Insecticides |
|
|
Term
| Indirect Pharmacodynamics- AGING! |
|
Definition
-Involves the breaking down of one oxygen-phosphorus bond of the inhibitor
-Further strengthens the phosphorus enzyme bond
-“Cholinesterase regenerators” can break the phosphorus enzyme bond if given before aging
-More difficult to break if aging has occurred |
|
|
Term
| Indirect – Organ System Effects - most prominent effects are seen in ? |
|
Definition
CV system
GI system
Eye
Skeletal muscle neuromuscular junction |
|
|
Term
| CNS in Low concentrations (Indirect – Organ System Effects) |
|
Definition
| diffuse activation on electroencephalogram and subjective alerting response |
|
|
Term
| CNS in higher concentration (indirect-organ system effects) |
|
Definition
| generalized convulsions that can lead to coma and respiratory arrest |
|
|
Term
| EYE- sphincter muscle of iris (indirect organ system effect |
|
Definition
|
|
Term
| EYE- ciliary muscle (indirect organ system effect |
|
Definition
| contraction for near vision |
|
|
Term
| RESPIRATORY- bronchial muscle (indirect organ system effect |
|
Definition
| constriction (bronchoconstriction) |
|
|
Term
| RESPIRATORY -bronchial glands (indirect organ system effect |
|
Definition
|
|
Term
| Gastrointestinal tract -Motility (Indirect – Organ System Effect) |
|
Definition
|
|
Term
| Gastrointestinal tract- sphincters (Indirect – Organ System Effects) |
|
Definition
|
|
Term
| Gastrointestinal tract-secretion (Indirect – Organ System Effects) |
|
Definition
|
|
Term
| Urinary Tract-Detrusor (Indirect – Organ System Effects) |
|
Definition
|
|
Term
| Urinary Tract- trigone and sphincter (Indirect – Organ System Effects) |
|
Definition
|
|
Term
| Cardiovascular System (Indirect – Organ System Effects) |
|
Definition
Increases activity in both sympathetic and parasympathetic ganglia
Fall in cardiac output due to bradycardia
Decrease in atrial contractility
Reduction in ventricular contractility |
|
|
Term
| Vascular smooth muscle – minimal effect (Indirect – Organ System Effects) |
|
Definition
| Vascular resistance may be increased |
|
|
Term
| Neuromuscular junction- Low (therapeutic) concentrations (Indirect – Organ System Effects) |
|
Definition
Moderately prolong and intensify actions of ACh
Increases strength of muscle contraction |
|
|
Term
Neuromuscular junction- Higher concentrations
(Indirect – Organ System Effects) |
|
Definition
Accumulation of ACh
Fibrillation of muscle fibers
Fasciculations of entire motor unit |
|
|
Term
| Eye diseases (Cholinomimetics – Clinical Use) |
|
Definition
Glaucoma
Accommodative esotropia |
|
|
Term
| GI/GU (Cholinomimetics – Clinical Use) |
|
Definition
| Post operative atony, neurogenic bladder |
|
|
Term
| Neuromuscular junction (Cholinomimetics – Clinical Use) |
|
Definition
|
|
Term
| heart (Cholinomimetics – Clinical Use) |
|
Definition
| certain atrial arrhythmias |
|
|
Term
| Bethanechol- Cholinomimetics – Clinical Use for ? |
|
Definition
| Post-op and Neurogenic Ileus and Urinary Retention |
|
|
Term
| Carbachol- Cholinomimetics – Clinical Use for ? |
|
Definition
|
|
Term
| Pilocarpine- Cholinomimetics – Clinical Use for ? |
|
Definition
| Glaucoma, Sjogren’s Syndrome |
|
|
Term
| Nicotine- Cholinomimetics – Clinical Use for ? |
|
Definition
|
|
Term
|
Definition
| increased intraocular pressure |
|
|
Term
| Muscarinic stimulants and AChE inhibitors reduces ? |
|
Definition
intraocular pressure
Contraction of ciliary body
Facilitate outflow of aqueous humor
Decrease rate of secretion of aqueous humor |
|
|
Term
| Glaucoma Treatment (direct agonist) medications ? |
|
Definition
| pilocarpine, methacholine, carbachol |
|
|
Term
| Glaucoma Treatment (cholinesterase inhibitors) |
|
Definition
| physostigmine, echothiophate |
|
|
Term
|
Definition
| Topical Beta Blockers and Prostaglandin derivatives |
|
|
Term
Acute angle-closure glaucoma is a medical emergency
and treated initially with ? |
|
Definition
direct muscarinic agonist and a cholinesterase inhibitor (pilocarpine plus physostigmine)
Once intraocular pressure is controlled and danger of vision loss is diminished – surgery (iridectomy) |
|
|
Term
| Postoperative ileus w/o obstruction and Increase tone of LES (pts w/ reflux esophagitis/GERD/reflux) can be treated with ? |
|
Definition
Bethanechol 10-25 mg PO TID or QID
Neostigmine 15 mg PO |
|
|
Term
| Sjogren’s syndrome is treated with ? |
|
Definition
| pilocarpine to increase salivary secretions |
|
|
Term
Urinary retention – postoperative or postpartum
and Neurogenic bladder (secondary to spinal cord injury or disease) can be treated with ? |
|
Definition
Bethanechol 5mg subcutaneously, may be repeated in 30 min if necessary
Neostigmine 0.5 to 1 mg subcutaneously
Neostigmine 15 mg PO |
|
|
Term
| Myasthenia gravis is disease ? |
|
Definition
| affecting skeletal muscle neuromuscular junction (autoimmune process) |
|
|
Term
| Neuromuscular Junction is ? |
|
Definition
| Extremely sensitive to actions of drugs that interfere with neuromuscular junction – aminoglycoside antibiotics |
|
|
Term
| are valuable in treating myasthenia gravis ? |
|
Definition
| cholinesterase inhibitors |
|
|
Term
| is used in diagnosing myasthenia gravis ? |
|
Definition
|
|
Term
| long term treatment myasthenia gravis ? |
|
Definition
pyridostigmine with neostigmine or ambenonium as alternatives
Doses titrated based on changes in muscle strength
Require frequent dosing |
|
|
Term
| treatment for Supraventricular tachyarrhythmias ? |
|
Definition
adenosine and calcium channel blockers
Edrophonium was once used |
|
|
Term
| is amodest efficacy and significant hepatic toxicity in treatment of Alzheimer’s ? (CNS) |
|
Definition
|
|
Term
| is a modest clinical benefit in treatment of Alzheimer’s ? (CNS) |
|
Definition
|
|
Term
| is a direct acting nicotinic agonist used in smoking cessation ? (CNS) |
|
Definition
varenicline
Toxicity includes nausea, headache, and sleep disturbance |
|
|
Term
| Direct acting Muscarinic (toxicity)- pilocarpine |
|
Definition
| nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation, and bronchial constriction |
|
|
Term
|
Definition
nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, cutaneous vasodilation and bronchial constriction
symptoms within 15-30 minutes of ingestion
Treatment: Atropine 1-2 mg parenterally |
|
|
Term
| Direct acting Nicotinic (toxicity) |
|
Definition
Fatal dose of nicotine 40 mg or 1 drop of pure liquid (same amount of nicotine in 2 regular cigarettes)
CNS stimulation: convulsions, coma, respiratory arrest
Skeletal muscle end plate depolarization leading to respiratory paralysis
Hypertension and cardiac arrhythmias |
|
|
Term
| Direct acting Nicotinic (toxicity) |
|
Definition
Acute toxicity treatment: directed towards symptoms
Muscarinic – atropine
Central stimulation – anticonvulsants (diazepam)
Neuromuscular – does not respond to drugs so mechanical respiration required
Nicotine is metabolized and excreted rapidly – pt may survive and recover completely if hypoxia and brain damage hasn’t occurred in the first 4 hrs |
|
|
Term
| Cholinesterase Inhibitors (toxicity) |
|
Definition
Usually from pesticides in agriculture or home use
Signs of muscarinic excess: diarrhea, urination, miosis, bronchoconstriction, excitation (of skeletal muscle and CNS), lacrimation, and salivation and sweating → “DUMBELS” |
|
|
Term
| treatment of cholinesterase inhibitors toxicity ? |
|
Definition
Maintenance of vital signs
Decontamination
Atropine parenterally as needed to control signs of muscarinic excess |
|
|
Term
| examples of Direct acting Cholinomimetics ? |
|
Definition
ACh (Miochol-E)
Bethanechol (Urecholine)
Carbachol (Miostat)
Cevimeline (Evoxac)
Pilocarpine (Isopto Carpine)
Varenicline (Chantix) |
|
|
Term
| examples of Cholinesterase Inhibitors ? |
|
Definition
Ambenonium (Mytelase)
Donepezil (Aricept)
Echothiophate (Phospholine)
Edrophonium (Tensilon)
Galantamine (Reminyl) |
|
|
Term
|
Definition
Neostigmine (Prostigmin)
Physostigmine
Pyridostigmine (Mestinon, Regonol)
Rivastigmine (Exelon)
Tacrine (Cognex) |
|
|
Term
| Cholinoceptor blocking agents block the effect of ? |
|
Definition
| parasympathetic activation |
|
|
Term
| examples of Antinicotinic drugs (Cholinoceptor blocking agents)? |
|
Definition
Ganglion Blockers
Neuromuscular Blockers |
|
|
Term
example of Antimuscarinic (anticholinergic)
/ Cholinoceptor blocking agents |
|
Definition
| atropine is the prototype |
|
|
Term
| examples of Muscarinic antagonists (Antimuscarinic Agents) ? |
|
Definition
|
|
Term
|
Definition
Naturally occurring tertiary amine alkaloid esters
Atropa belladonna and Datura stramonium
Absorbed well from the gut and conjunctival membrane |
|
|
Term
|
Definition
Hyoscyamus niger
Absorbed across the skin |
|
|
Term
| antimuscarinic agents -structure - tertiary amines ? |
|
Definition
Useful in eye and CNS conditions
Similar structures
Antihistamines, antipsychotics, antidepressants |
|
|
Term
| antimuscarinic agents -structure - quaternary amines |
|
Definition
More peripheral effects
Less CNS penetration |
|
|
Term
| atropine (Pharmacokinetics) |
|
Definition
Distribution: CNS within 30 min to 1 hour
Metabolism: plasma half life of 2 hours
Excretion: 60% excreted unchanged
Effects on the iris and ciliary muscle persist for more than 72 hours |
|
|
Term
|
Definition
Atropine causes reversible blockade
Binds to muscarinic receptor and prevents release of IP3 and inhibits adenylyl cyclase
Effect varies by tissue
Tissues most affected: salivary, bronchial, and sweat glands |
|
|
Term
|
Definition
Highly selective for muscarinic receptors
Lower potency at nicotinic receptors
Does not distinguish between M1 - M3
Other antimuscarinics are moderately selective for one of the receptor subgroups |
|
|
Term
| order of effects of increased dose of atropine |
|
Definition
Decreased salivary and bronchial secretions
Decreased sweating
Pupil dilation and tachycardia
Inhibition of voiding
Decreased GI motility
Decreased gastric secretions |
|
|
Term
| CNS (atropine)- organ system effects |
|
Definition
Minimal stimulant effects
Longer lasting sedative effect on the brain
One of the 1st drugs used for tremor of Parkinson’s |
|
|
Term
| CNS-scopolamine -organ system effects (atropine) |
|
Definition
Prevents motion sickness of vestibular disturbances
Drowsiness and amnesia
Toxic doses – excitement, agitation, hallucinations, and coma |
|
|
Term
| Eye - Topical atropine -organ system effects (atropine) |
|
Definition
blocks activation in pupillary constrictor muscle
Leads to unopposed sympathetic dilator activity and mydriasis
Weakens contraction of the ciliary muscle (cycloplegia)
Loss of ability to focus for near vision
Reduces lacrimal secretion |
|
|
Term
Cardiovascular
SA node (organ system effects) (atropine) |
|
Definition
very sensitive to blockade
Moderate to high doses of atropine cause tachycardia
Lower doses initially cause bradycardia |
|
|
Term
| cardiovascular- AV node- organ system effects (atropine) |
|
Definition
| blockade can reduce PR interval |
|
|
Term
| cardiovascular- ventricles- organ system effects (atropine) |
|
Definition
| intraventricular conduction block in toxic concentrations |
|
|
Term
| cardiovascular- blood vessels- organ system effects (atropine) |
|
Definition
| vasodilation can be blocked |
|
|
Term
Respiratory System- organ system effects
(atropine) |
|
Definition
Atropine can cause some bronchodilation and reduce secretion
Limited effectiveness in treating chronic obstructive pulmonary disease (COPD)
May be valuable in some asthma patients
Often used before administration of inhalant anesthetics to reduce the accumulation of secretions and the possibility of laryngospasm |
|
|
Term
| Gastrointestinal tract (organ system effects) (atropine) |
|
Definition
Blocks motility (from stomach to colon) and some secretory functions
Blocks parasympathetic vagal nerve input
But GI function also controlled by local hormones and noncholinergic neurons
Blocks salivary gland leading to dry mouth
Reduction in gastric secretions
Little effect on pancreatic and intestinal secretions |
|
|
Term
| Genitourinary tract (organ system effects) (atropine) |
|
Definition
Relaxes smooth muscle of ureters and bladder wall which slows voiding
Useful in treatment of spasm due to mild inflammation, surgery, and certain neurologic conditions
Urinary retention in males with prostatic hyperplasia
No significant effect on the uterus |
|
|
Term
| Sweat Glands- organ system effects -atropine |
|
Definition
Atropine suppresses thermoregulatory sweating
Adults only affected when large doses used
Infants and children are more affected – “atropine fever” |
|
|
Term
| CNS Disorders (Therapeutic Applications) Parkinson’s disease |
|
Definition
| Adjunctive therapy in some patients |
|
|
Term
| CNS Disorders-Therapeutic Applications-Motion sickness |
|
Definition
Vestibular disorders
Scopolamine for seasickness
Scopolamine patch can last 48-72 hrs but can cause sedation and dry mouth |
|
|
Term
| Ophthalmologic Disorders- Therapeutic Applications- Antimuscarinics useful in eye examinations |
|
Definition
Help examine the retina
Use shorter acting drugs in adults and older children
Younger children may require atropine but the possibility of antimuscarinic poisoning is increased
Antimuscarinics should never be used for dilation unless cycloplegia or prolonged action is required
Prevent synechia formation in uveitis & iritis
Longer lasting agents are useful |
|
|
Term
| Ophthalmologic Disorders (atropine) |
|
Definition
Atropine effects last 7-10 days
Cyclopentolate effects last 1 day
Tropicamide effects last 6 hours |
|
|
Term
| Atropine or scopolamine used preoperatively to decrease |
|
Definition
| airway secretions and decrease laryngospasms |
|
|
Term
| Scopolamine produced a postoperative ? |
|
Definition
amnesia of the events
However they increased urinary retention & intestinal hypomotility |
|
|
Term
| is useful in asthma & COPD ? |
|
Definition
|
|
Term
| is useful to reduced incidence of COPD exacerbations ? |
|
Definition
tiotropium
Longer bronchodilator action than ipratropium |
|
|
Term
| Cardiovascular Disorders- info! |
|
Definition
Can overcome the depression of SA or AV node function that is due to reflex vagal discharge in an MI
Useful in blocking the parasympathetic actions in some people with idiopathic dilated cardiomyopathy
Due to antibody formation |
|
|
Term
| Gastrointestinal Disorders (Therapeutic Applications) |
|
Definition
Used to treat traveler’s diarrhea and other mild self limited hypermotility conditions
Often combined with an opioid antidiarrheal drug
The antimuscarinic drug is mainly present to discourage abuse of the opioid agent |
|
|
Term
| Is Used to relieve bladder spasms after urologic surgery and Used to reduce involuntary voiding ? |
|
Definition
|
|
Term
| Darifenacin & solifenacin |
|
Definition
Greater selectivity for M3
Once daily dosing
Reduced incidence of xerostomia & constipation |
|
|
Term
| Is Used in adults with urinary incontinence and Reduced incidence of dry mouth ? |
|
Definition
|
|
Term
| IS Used to reduce urinary incontinence in institutionalized elderly patients and Causes significant CNS toxicity ? |
|
Definition
Imipramine
Tricyclic antidepressant with antimuscarinic actions |
|
|
Term
| Cholinergic Poisoning (antimuscarinic therapy) |
|
Definition
Both nicotinic & muscarinic effects of cholinesterase inhibitors can be life threatening
To reverse muscarinic effects a tertiary amine must be used – atropine preferably
Use atropine for effects of organophosphate inhibitors, parathion, & chemical warfare nerve gas
Atropine sulfate 1-2 mg IV every 5-15 min until signs of reversal |
|
|
Term
| Cholinergic Poisoning (Cholinesterase regenerator compound) |
|
Definition
Pralidoxime (PAM) & diacetylmonoxime (DAM) used for organophosphorus poisoning
Can hydrolyze the phosphorylated enzyme if the complex has not aged
Pralidoxime 1-2 g IV infusion over 15-30 min
Diacetylmonoxime crosses the BBB |
|
|
Term
| Cholinergic Poisoning (Mushroom poisoning) |
|
Definition
Rapid onset within 15-30 min – nausea, vomiting, diarrhea, urinary urgency, vasodilation, reflex tachycardia (sometimes bradycardia), sweating, salivation, bronchoconstriction
Parenteral Atropine 1-2 mg
Delayed onset within 6-12 hrs – nausea, vomiting, hepatic injury, renal injury
Atropine has no value |
|
|
Term
|
Definition
Directed at one organ almost always induces undesirable effects in other organs
Atropine poisoning – dry mouth, mydriasis, tachycardia, hot & flushed skin, agitation, & delirium
“Dry as a bone, blind as a bat, red as a beet, and mad as a hatter”
Children and infants are very sensitive to the hyperthermic effects of atropine – death in doses as low as 2 mg |
|
|
Term
| Contraindications of Antimuscarinic drugs |
|
Definition
contraindicated in pts with glaucoma
Elderly male pts use caution & avoid if pt has prostatic hyperplasia
Slows gastric emptying – increase gastric ulcer symptoms |
|
|
Term
Ganglionic Blockade:
Non-depolarizing |
|
Definition
| Blockade can be overcome by increasing the concentration of an agonist |
|
|
Term
Ganglionic Blockade:
depolarizing |
|
Definition
| Can be produced by nicotine and even ACh |
|
|
Term
CNS
Mecamylamine (Ganglion Blocking Organ System Effect) |
|
Definition
crosses BBB
Can cause sedation, tremor, choreiform movements, mental aberrations |
|
|
Term
Eye
Ciliary muscle (Ganglion Blocking Organ System Effect) |
|
Definition
| cycloplegia with the loss of accommodation |
|
|
Term
| eye- pupil (Ganglion Blocking Organ System Effect) |
|
Definition
hard to predict
Sympathetic innervation – pupillary dilation
Parasympathetic innervation – pupillary constriction
Ganglionic blockade often causes moderate dilation
Ganglionic blockade often causes moderate dilation |
|
|
Term
CV
Blood vessels
(Ganglion Blocking Organ System Effect) |
|
Definition
Decrease in arteriolar and venomotor tone leading to a fall in blood pressure
Hypotension in the upright position (orthostatic hypotension) |
|
|
Term
| CV- cardiac (Ganglion Blocking Organ System Effect) |
|
Definition
Diminished contractility
Moderate tachycardia |
|
|
Term
| GI tract (Ganglion Blocking Organ System Effect) |
|
Definition
Reduced secretions
Motility inhibited
Constipation |
|
|
Term
| GU (Ganglion Blocking Organ System Effect) |
|
Definition
Urinary hesitancy
Urinary retention
Impaired erection
Impaired ejaculation |
|
|
Term
| Thermoregulatory sweating reduced (Ganglion Blocking Organ System Effect) |
|
Definition
| Hyperthermia usually not a concern due to cutaneous vasodilation |
|
|
Term
| examples of Antimuscarinic Anticholinergic Drugs ? |
|
Definition
Atropine
Belladonna alkaloids
Dicyclomine (Bentyl) |
|
|
Term
| examples of Antimuscarinic Anticholinergic Drugs ? |
|
Definition
Flavoxate (Urispas)
Glycopyrrolate (Robinul)
I-Hyoscyamine
Ipratropium (Atrovent) |
|
|
Term
| examples of Antimuscarinic Anticholinergic Drugs ? |
|
Definition
Methscopolamine (Pamine)
Oxybutynin (Ditropan)
Scopolamine
Solifenacin (Vesicare) |
|
|
Term
| examples of Antimuscarinic Anticholinergic Drugs ? |
|
Definition
Tiotropium (Spiriva)
Tolterodine (Detrol)
Trospium (Spasmex) |
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