Term
| Effects of alpha 1 on smooth muscle |
|
Definition
|
|
Term
| Effects of alpha 1 on pupillary dilator muscle |
|
Definition
| contraction (dilates pupil) |
|
|
Term
| effects of alpha 1 on pilomotor smooth muscle |
|
Definition
|
|
Term
| effects of alpha 1 on prostate |
|
Definition
|
|
Term
| effects of alpha 1 on heart |
|
Definition
| increases force of contraction |
|
|
Term
| effects of alpha 2 on platelets |
|
Definition
|
|
Term
| Effects of alpha 2 on adrenergic and cholinergic nerve terminals |
|
Definition
| inhibition of transmitter release |
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|
Term
| Effects of alpha 2 on some vascular smooth muscle |
|
Definition
|
|
Term
| Effects of alpha 2 on fat cells |
|
Definition
|
|
Term
| Effects of beta 2 on respiratory, uterine, and vascular smooth muscle |
|
Definition
| promotes smooth muscle relaxation |
|
|
Term
| effects of beta 2 on skeletal muscle |
|
Definition
| promotes potassium uptake |
|
|
Term
| effects of beta 2 on human liver |
|
Definition
|
|
Term
| effects of D1 receptor on smooth muscle |
|
Definition
| dilates renal blood vessels |
|
|
Term
| effects of D2 on nerve endings |
|
Definition
| modulates transmitter release |
|
|
Term
| Direct-acting sympathomimetics |
|
Definition
| Bind to adrenergic receptors |
|
|
Term
| Indirect-acting sympathomimetics |
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Definition
| Cause release of NE from nerve endings, All indirect-acting drugs are substrates for uptake-1 |
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|
Term
| Examples of indirect-acting sympathomimetics |
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Definition
| Amphetamine, Methamphetamine, Methylphenidate, Tyramine |
|
|
Term
| Positive response after reserpine treatment |
|
Definition
|
|
Term
| no effect after reserpine treatment |
|
Definition
|
|
Term
| partial effect after reserpine treatment |
|
Definition
|
|
Term
| Effects of beta 2 and alpha 1 on the bladder |
|
Definition
| Beta 2 - relaxation, Alpha 1 - tightens sphincter to prevent urination |
|
|
Term
| effects of skin if Alpha 1 agonist binds to alpha 1 receptor |
|
Definition
| vasoconstriction in blood vessels in skin |
|
|
Term
| Effect of blood flow in skeletal muscle by activating beta 2 and alpha 1 receptors in physiological doses |
|
Definition
| Beta 2 is activated first, vasodilation, blood flow in skeletal muscles in high |
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|
Term
| Effects of blood flow in skeletal muscle when activating alpha 1 and beta 2 receptors under higher doses |
|
Definition
| Activate alpha 1 and cause vasoconstriction. |
|
|
Term
| Effects of high doses of epinephrine on blood pressure |
|
Definition
|
|
Term
|
Definition
| Degrade catecholamines (catechol, phenylethylamine,norepinephrine, epinephrine, isoproterenol, dopamine) |
|
|
Term
| Effects of epinephrine administered orally |
|
Definition
| not effective- cannot cross gut |
|
|
Term
| Effects of epinephrine administered subcutaneously |
|
Definition
| slow absorption- vasoconstriction in skin by alpha receptor (lower blood flow) |
|
|
Term
| effects of epinephrine administered intramuscularly |
|
Definition
| more rapid- causes vasodilation increasing flow |
|
|
Term
| effects of inhaled epinephrine |
|
Definition
| localized- lipophobic nature of epinephrine |
|
|
Term
| Cardiac output x Peripheral vascular resistance |
|
Definition
|
|
Term
| Cardiac effects of epinephrine |
|
Definition
| + inotropic effects, + chronotropic effects (beta 1) |
|
|
Term
| vascular effects of epinephrine |
|
Definition
redistribution of blood flow, cutaneous vasoconstriction, blood flow in skeletal muscles
(physiological dose= dilate blood vessels, high dose= constrict vessels) |
|
|
Term
|
Definition
| Reversal of blood pressure caused by prior administration of an alpha-adrenergic antagonist |
|
|
Term
| Use of beta 2 agonist on uterine smooth muscle |
|
Definition
| can be used to delay delivery of the baby |
|
|
Term
| effects of beta 2 receptor on bladder smooth muscle |
|
Definition
|
|
Term
| effects of alpha 1 receptor on bladder smooth muscle |
|
Definition
| contracts trigone and sphincter muscles |
|
|
Term
| Respiratory effects of beta 2 and alpha 1 activation |
|
Definition
Beta 2- bronchodilation and inhibition of Ag-induced release of inflammatory mediators from mast cells
Alpha 1- decreases bronchial secretion |
|
|
Term
| insulin effects of alpha 2 receptor in pancreas activation |
|
Definition
| inhibits insulin release --> blood glucose increases |
|
|
Term
| insulin effects of beta 2 receptor in pancreas |
|
Definition
| enhances insulin release --> blood glucose decreases |
|
|
Term
| dominating receptor in pancreas |
|
Definition
|
|
Term
| Beta 2 receptor in pancreas effects on glucagon secretion |
|
Definition
| increase in glucagon secretion, increase in blood glucose |
|
|
Term
| metabolic effect of epinephrine in glucose uptake by peripheral tissues |
|
Definition
| glucose uptake is decreased |
|
|
Term
| epinephrine metabolic effect on glycogenolysis |
|
Definition
| increases glycogenolysis (breaks down glycogen into glucose) - beta 2 |
|
|
Term
| effects of epinephrine on lipolysis |
|
Definition
| increased lipolysis- increases fatty acids, beta 3 receptor activation |
|
|
Term
| serious side effects (toxicities) of epinephrine |
|
Definition
| cerebral hemorrhage (caused by elevated blood pressure), cardiac arrhythmia (caused by beta 1 receptor) |
|
|
Term
| effects of administering epinephrine to someone taking a nonselective beta blocker |
|
Definition
| exaggerated response- shoots up response (patient may die from cerebral hemorrhage) |
|
|
Term
| epinephrine effects on local anesthetics |
|
Definition
| prolongs actions of local anesthetics- alpha 1 receptor |
|
|
Term
| epinephrine effects on cardiac rhythm |
|
Definition
| can restore cardiac rhythm (beta 1 receptor) |
|
|
Term
| epinephrine effects on bleeding surfaces |
|
Definition
| topical hemostatic agent on bleeding surfaces (alpha 1 causing vasoconstriction) |
|
|
Term
| epinephrine effects on open-angle glaucoma |
|
Definition
| treatment of open-angle glaucoma (alpha 2 decreases aqueous formation, alpha 1 increases aqueous outflow) |
|
|
Term
|
Definition
| prodrug put on eyeball, gets metabolized into epinephrine after crossing cell membrane |
|
|
Term
| effects on someone on an MAO inhibitor |
|
Definition
| prolonged effects of catecholamines because they will not be metabolized as quickly |
|
|
Term
| Receptors activated by Norepinephrine |
|
Definition
|
|
Term
| Epinephrine vs. Norepinephrine (which has greater alpha activation) |
|
Definition
| Epinephrine is more potent activator at alpha receptor than NE |
|
|
Term
| Renin effects by epinephrine and norepinephrine |
|
Definition
| both stimulate renin release |
|
|
Term
| blood pressure and pulse pressure effects from norepinephrine |
|
Definition
| systolic and diastolic pressure are increased, pulse pressure usually increased -- involve activation of beta 1 cardiac receptor |
|
|
Term
| TPR effect from norepinephrine |
|
Definition
| TPR is increased -- alpha 1 receptor activated |
|
|
Term
| Norepinephrine metabolic effects |
|
Definition
| hyperglycemia, similar to EPI. (no beta 2 so you cannot increase insulin, you do not get the stimulation of glucagon release-- also do not increase glycogenolysis) |
|
|
Term
| Uterine effects from norepinephrine |
|
Definition
| increased frequency of contraction of pregnant human uterus |
|
|
Term
|
Definition
similar to EPI but less pronounced and less frequent.
most common- anxiety, respiratory difficulty, awareness of a slow forceful heart beat, transient headache
overdoses- severe hypertension, violent headache, photophobia, stabbing retrosternal pain, pallor, intense sweating, vomiting |
|
|
Term
| Therapeutic uses of NE (Levophed) |
|
Definition
|
|
Term
| Effects of MAO inhibitor on dopamine |
|
Definition
| will be prolonged because it is not metabolized as quickly |
|
|
Term
| dopamine effect on kidney |
|
Definition
| vasodilation- improve kidney function. important in patients who are renally compromised |
|
|
Term
| high doses of dopamine effects on heart |
|
Definition
| tend to stimulate beta 1 receptors, increase strength of contraction of heart, positive inotropic effect |
|
|
Term
| Mixed acting effects of dopamine |
|
Definition
causes release of NE from nerve terminals
(therefore these effects can be blocked by tricyclic antidepressant or cocaine) |
|
|
Term
|
Definition
| half life is short- effects quickly disappear |
|
|
Term
| therapeutic use of dopamine |
|
Definition
| treatment of shock (hypotension) |
|
|
Term
| clinical roles of Beta adrenergic sympathomimetic |
|
Definition
treatment of bronchoconstriction- beta 2
cardiac stimulants- beta 1 |
|
|
Term
|
Definition
nonselective beta sympathomimetic
(can activate beta 1, 2 and 3)
much stronger agonist than epi at beta 1 and 2 receptors.
no alpha activity |
|
|
Term
|
Definition
has catelcholamine in its structure- not an endogenous catelcholamine.
(effects will be prolonged by an MAO inhibitor) |
|
|
Term
| cardiovascular effects of nonselective beta sympathomimetic |
|
Definition
decrease TPR - beta 2
increase HR- beta 1
increase CO- beta 1
net effect: decrease blood pressure |
|
|
Term
| Drug toxicities of nonselective beta sympathomimetic |
|
Definition
| palpitations, tachycardia, arrythmias, myocardial necrosis, flushed skin |
|
|
Term
| smooth muscle effects of nonselective beta sympathomimetic |
|
Definition
bronchial relaxation- beta 2
GI smooth muscle relaxation- beta 2 |
|
|
Term
| insulin effects of nonselective beta sympathomimetic |
|
Definition
| insulin secretion increases- beta 2 (blood glucose decreases) |
|
|
Term
| fatty acid effect of nonselective beta adrenergic sympathomimetic |
|
Definition
| free fatty acid release increases because of beta 3 |
|
|
Term
| energy production effect of nonselective beta adrenergic sympathomimetic |
|
Definition
increased energy production- beta 2
(increased glycogenolysis, increased glucagon release, increased blood glucose) |
|
|
Term
| therapeutic uses of nonselective beta adrenergic sympathomimetic |
|
Definition
stimulate HR in patients with bradycardia- beta 1
treatment of asthma- beta 2
treatment of shock -beta 1 |
|
|
Term
|
Definition
| beta 1 selective sympathomimetic |
|
|
Term
|
Definition
| resembled dopamine structurally (dobutamine and dopamine are the 2 most widely used beta 1 agonists, but their use is limited to emergency i.v. therapy) |
|
|
Term
| Cardiovascular effects of Dobutamine |
|
Definition
Dose related-
low doses- selective beta 1 agonist
high doses- acts on beta 2 receptors with mild effects on alpha receptors
less peripheral vasoconstriction produced than if EPI is administered |
|
|
Term
| A person with an enlarged heart that is not functioning properly to provide the body with enough blood- what is the best drug to use? |
|
Definition
| Dobutamine- helps with congestive heart failure because it doesn't increase heart rate much but increases CO. |
|
|
Term
| therapeutic uses of Dobutamine |
|
Definition
| Treatment of cardiac decompensation that may occur after cardiac surgery or in patients with congestive heart failure or acute myocardial infarction |
|
|
Term
| Major use of Beta 2 selective adrenergic sympathomimetic |
|
Definition
treatment of asthma
(bronchodilation, decreased release of leukotrienes and histamine from mast cells, increased mucociliary function, decreased microvascular permeability, inhibition of phospholipase A2, decreased arachidonic acid metabolism) |
|
|
Term
| Examples of Beta 2 selective adrenergic sympathomimetics |
|
Definition
| metaproterenol, terbutaline, albuterol,levalbuterol, pirbuterol, salmeterol, formoterol, arformoterol,indacaterol,ritodrine |
|
|
Term
| Toxicities of beta 2 selective adrenergic sympathomimetics |
|
Definition
Skeletal muscle tremor (beta 2)
feelings of restlessness, apprehension, anxiety, tachycardia and arrythmias
increase glycogenolysis (beta 2 outsider of lungs) |
|
|
Term
| Cardiovascular toxicity effects from MAO inhibitors and tricyclic antidepressants |
|
Definition
| Toxicities are increased because of the enhanced NE effects |
|
|
Term
| general effects of alpha 1 selective adrenergic agonists |
|
Definition
| vasoconstriction, increased TPR, BP is maintained or increased |
|
|
Term
| General clinical uses of alpha 1 selective adrenergic sympathomimetics |
|
Definition
| treatment of hypotension, treatment of shock. |
|
|
Term
| Phenylephrine and Methoxamine |
|
Definition
| Direct-acting alpha 1 selective adrenergic agonists |
|
|
Term
| Mephentermine and Metaraminol |
|
Definition
| Mixed-acting alpha 1 selective adrenergic agonist |
|
|
Term
| Primary use of selective alpha 2 agonists |
|
Definition
hypertension (they activate alpha 2 receptors in CNS that can cross the blood brain barrier. Suppresses sympathetic outflow from CNS)
Still causes vasoconstriction in smooth muscles. |
|
|
Term
| Examples of alpha 2 selective agonists |
|
Definition
Clonidine, Apraclonidine, Guanfacine, Guanabenz, Methyldopa, Dexmedetomidine
(inhibit or paralyze sympathetic nervous system) |
|
|
Term
| Pharmocological effects of Clonidine |
|
Definition
| Decreased blood pressure, decreased heart rate |
|
|
Term
|
Definition
| Dry mouth, sedation, sexual dysfunction, marked bardycardia, contact dermatitis |
|
|
Term
| Therapeutic uses of Clonidine |
|
Definition
FDA approved = treatment of hypertension and ADHD
non-FDA approved= decrease GI motility, treatment of withdrawal symptoms in narcotic and nicotine addicts, relieve menopausal hot flashes, treatment of neuropathic pain, anaesthetic uses, treatment of insomnia |
|
|
Term
|
Definition
Amphetamine (oral), Dextroamphetamine (oral), hydroxyamphetamine (ophthalamic)
= miscedllaneous adrenergic agonist |
|
|
Term
| pharmacological effects of amphetamines |
|
Definition
indirect-acting sympathomimetic + CNS effects
(main effects on CNS, mainly cardiovascular effects because of CNS effects) |
|
|
Term
| cardiovascular effects of amphetamines |
|
Definition
| increased BP, heart rate reflexly slowed, cardiac arrythmias w/ large doses, cardiac output is generally not increased with therapeutic doses, cerebral blood flow does not change w/ therapeutic doses |
|
|
Term
| Amphetamines effect on appetite |
|
Definition
| decreased appetite (used to treat obesity) |
|
|
Term
| Toxicities of Amphetamines |
|
Definition
| psychotic effects, fatigue and depression, cardiovascular effects, excessive sweating, GI symptoms, fatal poisoning: convulsions and coma |
|
|
Term
| Treatment of obesity, narcolepsy, and ADHD |
|
Definition
|
|
Term
| classified as a schedule II drug under federal regulations |
|
Definition
| Methamphetamine (Desoxyn) |
|
|
Term
|
Definition
| Miscellaneous adrenergic agonist. Mixed-acting sympathomimetic + CNS effects |
|
|
Term
| Pharmacological effects of Ephedrine |
|
Definition
Increased HR and CO, Increased TPR, Increased BP, Urinary Retention, Bronchodilation, Potent CNS stimulant
(can activate all 4 receptors) |
|
|
Term
|
Definition
| Risk of hypertension and cardiac arrhythmias, insomnia, tachyphylaxis (tolerance) with repetitive doses |
|
|
Term
| Therapeutic uses of Ephedrine |
|
Definition
| bronchodilators in patients with asthma, promotion of urinary continence, treatment of hypotension associated with spinal anesthesia, nasal degonestant, past uses as CNS stimulant (narcolepsy and depression) |
|
|
Term
| Methylphenidate (Ritalin) |
|
Definition
| used in treatment of narcolepsy and ADHD |
|
|
Term
|
Definition
| Drugs that are competitive antagonists at alpha or beta adrenergic receptors |
|
|
Term
| Direct-acting sympatholytics |
|
Definition
| act peripherally on adrenergic neurotransmission at pre- or postsynaptic sites |
|
|
Term
| Indirect-acting sympatholytics |
|
Definition
|
|
Term
| Pharmacological effects of alpha 1- adrenergic antagonists |
|
Definition
| inhibit CV effects of endogenous catecholamines and exogenous sympathomimetics, vasodilation, decreased TPR, decreased BP, baroreceptor reflex increased in HR and CO |
|
|
Term
| Alpha 2 adrenergic antagonists CV pharmacological effects |
|
Definition
| increased release of NE from nerve endings, increased sympathetic outflow from CNS |
|
|
Term
| Actions of alpha adrenergic antagonists (in addition to CV effects) |
|
Definition
| decreased resistance to urinary outflow, inhibit contraction of bronchial smooth muscle, inhibit platelet aggregation, decreased glycogenolysis, increased insulin release from pancreas, decreased blood glucose |
|
|
Term
|
Definition
| nonselective, irreversible alpha blocker |
|
|
Term
| pharmacological effects of phenoxybenzmine |
|
Definition
| vasodilation, decreased TPR, increased CO, orthostatic hypotension, ability to respond to hypovolemia and anesthetic-induced vasodilation is impaired |
|
|
Term
| Therapeutic uses of Phenoxybenzamine |
|
Definition
| treatment of pheochromocytoma, management of benign prostatic obstruction, management of autonomic hyperreflexia in patients with spinal cord transection |
|
|
Term
| Adverse side effects of Phenoxybenzamine |
|
Definition
| orthostatic or postural hypotension, reflex tachycardia |
|
|
Term
| similar agent of Pheoxybenzamine |
|
Definition
|
|
Term
|
Definition
Selective alpha 1 blocker
Potent inhibitor of cyclic nucleotide phosphodiesterases (increases cAMP) |
|
|
Term
| Examples of related agents to Prazosin (Minipress) |
|
Definition
| Terazosin, Doxazosin, Tamsulosin, Alfuzosin |
|
|
Term
| Pharmacological effects of Prazosin |
|
Definition
| decreased TPR, increased vasodilation, decreased VR, decreased cardiac preload (little tendency to increase CO and HR) |
|
|
Term
| Therapeutic uses of Prazosin |
|
Definition
Major use: treatment of hypertension
Treatment of congestive heart failure
treatment of benign prostate hyperplasia |
|
|
Term
|
Definition
| Selective alpha 2 blocker |
|
|
Term
|
Definition
| Little clinical usefulness (limited benefit in treating male erectile dysfunction), potention for treating orthostatic hypotension (promotes NE release via blockade of presynaptic alpha2 receptors |
|
|
Term
| cardiovascular effects of beta adrenergic receptor antagonists |
|
Definition
| decreased HR, negative inotropic effects, short term use - decreased CO, increased TPR, long term use- TPR returns to initial values |
|
|
Term
| pulmonary system effects of beta adrenergic receptor antagonists |
|
Definition
| in patients with asthma or COPD, blockade of beta 2 receptors in bronchial smooth muscle can lead to life threatening bronchoconstriction |
|
|
Term
| metabolic effects of beta adrenergic receptor antagonists |
|
Definition
| changes in metabolism of carbohydrates and lipids, potentially decrease pancreatic insulin release, increase blood glucose, may adversely affect recovery from hypoglycemia in insulin-dependence diabetics, decrease release of fatty acids from adipose tissue |
|
|
Term
|
Definition
beta adrenergic receptor antagonist
prototype- used in the treatment of hypertension and angina |
|
|
Term
| examples of beta adrenergic antagonists |
|
Definition
| nadolol, timolol, pindolol, sotalol, carteolol |
|
|
Term
| examples of beta 1 selective receptor antagonists |
|
Definition
| metprolol, atenolol, esmolol, acebutolol, betaxolol, bisoprolol, nebivolol |
|
|
Term
|
Definition
| beta 2 selective adrenergic receptor antagonist |
|
|
Term
| CV toxic side effects of beta antagonists |
|
Definition
| may induce CHF in susceptible individuals, may cause or exacerate heart failure in compromised individuals, may cause bradycardia and life threatening radyarrhythmias, cold extremeties- worsening of PVD, development of Raynaud's phenomenon, Consequences of abrupt discontinuation after long term use- exacerbation of angina, increased risk of sudden death |
|
|
Term
| toxic side effects of pulmonary function- beta antagonists |
|
Definition
| life threatening increase in airway resistance |
|
|
Term
| toxic side effects of central nervous system- beta antagonists |
|
Definition
| fatigue, sleep disturbances (insomnia, nightmares) depression |
|
|
Term
| toxic side effects of metabolism -- beta antagonists |
|
Definition
| blunt recognition of hypoglycemia by patients, delay recovery from insulin-induced hypoglycemia, increased plasma triglycerides |
|
|
Term
| CV diseases therapeutic uses- beta antagonists |
|
Definition
| treatment of hypertension, treatment of ventricular arrhythmias, treatment of acute myocardial infarction and prevention of recurrences |
|
|
Term
| non-CV therapeutic uses of beta blockers |
|
Definition
| treatment of symptoms of hyperthroidism, prophylaxis of migraine headaches, control of acute pain, treatment of glaucoma, treatment of alcohol withdrawal |
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|
