Term
|
Definition
| Inhibits metabolism of levodopa, reducing the needed dosage of l-dopa, and prevents l-dopa toxicity |
|
|
Term
| Carbidopa clinical indications |
|
Definition
| Used in combination with levodopa for the treatment of Parkinson's |
|
|
Term
|
Definition
|
|
Term
|
Definition
| topically applied local anesthetic and vasoconstrictor for ENT procedures |
|
|
Term
|
Definition
| Alpha 1 agonist (a direct-acting sympathomimetic). Has longer duration of activity than catecholamines |
|
|
Term
|
Definition
Alpha 1 receptor stimulant with little effect on beta-receptors in the heart. Works on vascular smooth muscle to increase peripheral vascular resistance due to vasoconstriction and elevates blood pressure. Marked reflex bradycardia
occurs |
|
|
Term
| Phenylephrine Clinical Indications |
|
Definition
| Effective mydriatic (dilates pupils) and decongestant; also used to raise blood pressure. Approved for used in paroxysmal SVT |
|
|
Term
|
Definition
| Muscarinic agonist. It has increased activity at muscarinic sites, because it is a direct agonist |
|
|
Term
|
Definition
| Activates M1-M3 receptors in all peripheral tissues. It causes increased secretion, smooth muscle contraction (except vascular smooth muscle relaxes), and changes in heart rate |
|
|
Term
| Bethanechol Clinical Application |
|
Definition
| Postoperative and neurogenic ileus and urinary retention. It causes contraction of the detrusor muscle and relaxation of the trigone and sphincter to promote voiding |
|
|
Term
|
Definition
| Increased cholinergic activity, increase gastric acid secretion, increased GI & GU muscle tone(therapeutic effect), bronchoconstriction, hypotenstion, bradycardia, increased tearing of the eye |
|
|
Term
| Atropine is the prototype for which drug class? |
|
Definition
|
|
Term
| How many amines does atropine have? |
|
Definition
|
|
Term
|
Definition
| Atropine causes reversible blockade of cholinomimetic actions at muscarinic receptors. Atropine is highly selective for muscarinic receptors. |
|
|
Term
|
Definition
| Cardio- Increased heart rate d/t blockade of vagal slowing. Eye- Pupil dilation. Respiratory- Bronchodilation and reduced secretions. GI-Reduced motility. GU- Reduces bladder spasms. Suppresses sweating. |
|
|
Term
| Atropine Adverse Effects in Children |
|
Definition
| Children and especially infants are very sensitive to the hyperthermic effects of atropine. Deaths have occurs with as small of a dose as 2mg. |
|
|
Term
|
Definition
| Treatment with atropine for one organ system almost always produces undesirable effects in other organ systems. ADR dry mouth, mydriasis, tachycardia, hot and flushed skin, agitation, and delirium are common ADR. “Dry as a bone, blind as a bat, red as a beet, mad as a hatter” |
|
|
Term
|
Definition
| Antiparkinsonian: Transported into the CNS and converted to dopamine; also converted to dopamine in the periphery |
|
|
Term
| Levodopa Pharmacokinetics |
|
Definition
| Rapidly absorbed from the small intestine (depends on gastric emptying and pH); delayed by food ingestion. Only 1-3% of drug enters the brain unaltered so given in large amounts if used alone |
|
|
Term
| Clinical Uses of Levodopa |
|
Definition
| Parkinson's Disease: Most efficacious therapy (best restuls seen in first few years of Tx, likely because daily dose must be decreased over time to avoid adverse effects). Does not stop progression of parkinsonism but early use decreases mortality |
|
|
Term
|
Definition
| Generally given in combination with levodopa - decreases required dosage of levodopa |
|
|
Term
|
Definition
| GI upset (monitor patients with peptic ulcers carefully); arrhythmias, postural hypotension, HTN; dyskinesias, on-off and wearing-off phenomena; behavioral disturbances; mydriasis. Use with care in patients with skin cancer or lesions |
|
|
Term
| Levodopa Drug Interactions |
|
Definition
| 1) Vitamin B6 may prevent its therapeutic effect; 2) MAO-I may lead to hypertensive crisis |
|
|
Term
| Levodopa Contraindictaions |
|
Definition
| 1) Psychoses 2) Angle-closure glaucoma |
|
|
Term
|
Definition
| Non-selective agonist of all adrenergic receptors. Agonist at both the alpha and beta receptors. |
|
|
Term
|
Definition
| Potent vasoconstrictor and cardiac stimulant. Positive inotropic and chronotropic actions on the heart cause a rise in systolic blood pressure. |
|
|
Term
| Epinephrine classification |
|
Definition
Catecholamines and component of flight-or-flight response within the
sympathetic nervous system |
|
|
Term
| Epinephrine Most Common Uses |
|
Definition
| Cardiac arrest, anaphylaxis, asthma attacks |
|
|
Term
|
Definition
| Palpitations, Tachycardia, Arrhythmias, Anxiety, HA, Tremors, HTN, Acute Pulmonary Edema. Can lead to loss of intravascular fluid volume and hypotension during anaphylactic reactions |
|
|
Term
| Epinephrine Contraindications |
|
Definition
| Use within administration of MAOI, Non anaphylactic shock, requires additional cardiac monitoring |
|
|
Term
|
Definition
| is a sympathomimetic amine that has both alpha-adrenergic activity resulting in peripheral vasoconstriction, and beta-adrenergic activity leading to inotropic stimulation of the heart and coronary artery vasodilation |
|
|
Term
|
Definition
| Acetylcholine, norepinephrine, dopamine, epinephrine, others |
|
|
Term
|
Definition
| Cardiac arrest, cardiac dysrythmia, HTN, bradyarrhythmia, urinary retention |
|
|
Term
| Acetylchone (ACh) is released by which part of the ANS? |
|
Definition
|
|
Term
| Norepinephrine Contraindications |
|
Definition
| hypotension related to blood volume deficiency |
|
|
Term
| Where is acetylcholine (ACh) produced? |
|
Definition
| In the cytoplasm of the cell |
|
|
Term
| 2 components of acetylcholine (ACh) and where they originate |
|
Definition
| 1) Acetyl-CoA is produced in the mitochondria of the nerve ending, 2) choline is transported into the cell from extracellular fluid via a sodium-dependent transporter |
|
|
Term
| Norepinephrine Classification |
|
Definition
| Adrenergic, Sympathomimetic, Vasopressor |
|
|
Term
|
Definition
| Intravenous = 1-2 minutes |
|
|
Term
| Acetylcholinesterase (AChE) |
|
Definition
| Enzyme that usually terminates the action of Acetylcholine (ACh) by splitting it into Acetyl-CoA and choline |
|
|
Term
|
Definition
| Neurotransmitter released by cholinergic fibers |
|
|
Term
| Norepinephrine Interactions |
|
Definition
| Amitriptyline, Chlorpromazine, Digoxin, Doxepin, Linezolid, Trimipramine |
|
|
Term
| Acetylcholine (ACh) probable roles |
|
Definition
| 1) The primary transmitter at ANS ganglia, at the somatic neuromuscular junction, and at parasympathetic postganglionic nerve ending. 2) A primary excitatory transmitter to smooth muscles & secretory cells in the ENS (enteric nervous system). 3) Probably also the major neuron-to-neuron (ganglionic) transmitter in the ENS |
|
|
Term
| Acetylcholine (ACh)- a choline ester- kinetics |
|
Definition
| Insoluble in lipids- poorly absorbed & poorly distributed into CNS because hydrophilic- rapidly hydrolyzed in GI tract by cholinesterase- must by IV in large amounts- IV bolus has brief effect (5-20 seconds)- IM & SQ have only local effects |
|
|
Term
|
Definition
| modifies organ function via 2 mechanisms: 1) Direct- ACh released from parasympathetic nerves activates muscarinic receptors on receptor cells, 2) Indirect- Ach interacts with muscarinic receptors on nerve terminals to inhibit release of their neurotranmitter to modulate effects of parasympathetic & sympathetic nervous systems |
|
|
Term
|
Definition
| Tertiary antimuscarinic drug, intestinal antispasmodic/anticholinergic: Inhibits muscarinic cholinergic receptors in the enteric plexus & on smooth muscle (antagonist at M1) |
|
|
Term
| Dicyclomine ADR and clinical cautions |
|
Definition
| At low doses, minimal autonomic effects. At high doses, anticholinergic effects include dry mouth, visual disturbances, urinary retention, constipation, dry eyes, nausea. Contraindicated in glaucoma, use caution in males with prostatic hyperplasia, contraindicated in pregnancy, breastfeeding, < 6 mo old, GI obstruction, MG, obstructive uropathy, reflux esophagitis, severe ulcerative colitis, unstable CV status w/ acute hemorrhage |
|
|
Term
| Dicyclomine clinical uses |
|
Definition
| Peptic disease, hypermotility, IBS |
|
|
Term
|
Definition
| a nonergot dopamine agonist, exact mechanism of action is unknown |
|
|
Term
|
Definition
| Well absorbed from gut & conjuctiva, widely distributed, significant levels in CNS within 30 minutes to 1 hour; Bioavailability twice as high with IM over PO, Do not administer IV since may cause thrombosis; Eliminated mostly renally- caution in elderly, T1/2=1.8h |
|
|
Term
|
Definition
| its action is believed to be related to its ability to stimulate dopamine receptors in the striatum. |
|
|
Term
|
Definition
| Has intrinsic activity at the D(2) subfamily of dopamine receptors, and a higher affinity to the D(3) receptors than the D(2) or D(4) receptors |
|
|
Term
|
Definition
| Parkinson's Disease & Restless Leg Syndrome |
|
|
Term
|
Definition
| Heart Failure, Sleep attack, Malignant Melanoma, Orthostatic hypotension, EPS movements, hallucinations |
|
|
Term
|
Definition
| increased half-life for elderly patients (12 hours) |
|
|
Term
|
Definition
| A Sympathomimetic, non-catecholamine |
|
|
Term
| Albuterol Beta agonist MOA: |
|
Definition
| MOA: Causes bronchodilation in lungs through Beta-2 receptor stimulation. Also stimulates Beta receptors in heart to increase contractional force and heart rate. |
|
|
Term
| Albuterol Beta agonist ADR: |
|
Definition
| Tachycardia, A-Fib, SVT, angina, palpitations, tremors, dizziness |
|
|
Term
Midodrine Alpha-one-receptor agonist
A prodrug |
|
Definition
| A direct-acting, Sympathomimetic |
|
|
Term
Midodrine Alpha-one-receptor agonist
A prodrug MOA: |
|
Definition
| Enzymatically hydrolized to desglymidodrine , a selective alpha-one-receptor agonist to increase blood pressure for those with orthostatic hypotension. Works on the arteriolar and venous alpha-one-receptors. |
|
|
Term
Midodrine Alpha-one-receptor agonist
A prodrug ADR: |
|
Definition
| Can cause hypertension in supine. May cause bradycardia due to vagal stimulation. |
|
|
Term
| Acetylcholine (ACh) Clinical indications |
|
Definition
| Miosis induction, eye surgery |
|
|
Term
|
Definition
| naturally occurring neurohormone, interferes w/ transmission of nerve impluses at all cholinergic sites involving somatic & autonomic nerves, causes pupil constriction when directly applied to iris |
|
|
Term
|
Definition
| A combination of two synthetic isomers which offset each other- the outcome is a primarily β-receptor agonist in cardiac muscle; causes increased cardiac contractility (+ inotrope) through β1 stimulation and a second effect of vasodilation through slight β2 stimulation |
|
|
Term
|
Definition
| Increased myocardial oxygen demand leading to angina or arrhythmias in patients with coronary artery disease. Other signif. ADR’s include hypokalemia and platelet inhibition. |
|
|
Term
|
Definition
| Acute heart failure, cardiogenic shock |
|
|
Term
|
Definition
| Antagonist of muscarinic receptors in basal ganglia (anticholinergic) |
|
|
Term
|
Definition
| Anticholinergics antagonize the effect of acetylcholine. This decreases the imbalance between the neurotransmitters acetylcholine and dopamine, which may improve the symptoms of early Parkinson's disease. |
|
|
Term
|
Definition
| Fever, hyperthermia, heat stroke, tachy/bradyarrhythmias, constipation, muscle weakness, tardive dyskinesia, confusion and depression |
|
|
Term
| Benztropine: Special considerations |
|
Definition
| On Beer’s Criteria list as not recommended in older adults for prevention of antipsychotic induced extra-pyramidal symptoms. It is also not recommended for the treatment of Parkinson's disease in older adults as more effective agents are available. Avoid use in patients with dementia and cognitive impairment due to the risk of adverse CNS effects. |
|
|
Term
|
Definition
| Muscarinic partial agonist, activates M1-M3 receptors in tissues - results in increased secretion and smooth muscle contraction, except vascular smooth muscle relaxes |
|
|
Term
|
Definition
| Glaucoma; Sjogren's syndrome |
|
|
Term
| Pilocarpine Pharmacokinetics |
|
Definition
| Oral lozenge and topical application |
|
|
Term
|
Definition
| Excessive parasympathomimetic effects |
|
|
Term
|
Definition
| Inhibits monoamine oxidase (MAO) B |
|
|
Term
|
Definition
| Used in addition to levodopa to help prolong its effects to help reduce Parkinson's symptoms |
|
|
Term
| Rasagiline Administration and Toxicity |
|
Definition
| Given orally, may cause serotonin syndrome when used with meperidine or SSRIs |
|
|
Term
|
Definition
| Used in the treatment of cognitive dysfunction in Alzheimer's patients |
|
|
Term
|
Definition
| It reversibly and noncompetitively inhibits centrally-active acetylcholinesterase, the enzyme responsible for hydrolysis of acetylcholine which results in increased concentrations of acetylcholine that are available for synaptic transmission |
|
|
Term
|
Definition
| May be given once daily because of its long half-life. Comes in 5, 10, & 23 mg tablets |
|
|
Term
| Donepezil Pharmocokinetics |
|
Definition
| Peak: 3-4 hours, Half-life: 70 hours and 104 hours in subject >55 years old. Metabolized in the liver and >50% is excreted in urine. |
|
|
Term
|
Definition
| This drug is a newer drug and is more selective acetylcholinesterase inhibitors and lacks the hepatotoxic effects as older versions |
|
|
Term
|
Definition
| This drug is an Antiparkinsonian Catechol-O-Methyltransferase Inhibitor, which prolong the action of levodopa by diminishing its peripheral metabolism |
|
|
Term
|
Definition
| This drug is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT), an enzyme with highest activity in the liver, intestinal tract, and kidney, is responsible for catalyzing O-methylation of levodopa to 3-O-methyldopa |
|
|
Term
| Entacapone Pharmocokinetics |
|
Definition
| Half-life is approximately 2 hours and needs to be taken (200mg) with each dose of levodopa, up to 5 times daily. This medication is preferred as it isn't hepatotoxic |
|
|
Term
| Entacapone adverse effects |
|
Definition
| Relate to increased levodopa exposure and include dyskinesias, nausea, confusion, abdominal pain, orthostatic hypotension, sleep disturbances and an orange discoloration of the urine. |
|
|
Term
| Entacapone considerations |
|
Definition
| It is often necessary to lower the daily dose of levodopa by about 30% in the first 48 hours to avoid or reverse some complications |
|
|
Term
|
Definition
| Inhibits acetylcholine's muscarinic actions at postganglionic parasympathetic receptors in smooth muscles, secretory glands, and the CNS. Decreases GI motility. |
|
|
Term
| Dicyclomine (Clinical Uses) |
|
Definition
| Irritable Bowel Syndrome, other functional GI disorders |
|
|
Term
| Dicyclomine (Side Effects) |
|
Definition
| Headache, palpitations, dizziness, blurred vision, constipation, urinary retention |
|
|
Term
|
Definition
| interferes with transmission of nerve impulses at all cholinergic sites involving somatic and autonomic nerves. Aceteylcholine released from parasymphathic nerve: 1. Activates Muscarini receptors on effector cells to directly alter organ function 2. interacts with muscarinic receptors on nerve terminals to inhibit the release of neurotransmiters |
|
|
Term
| Acetylcholine (Clinical Uses) |
|
Definition
| pupil constriction in eye surgeries, glaucoma treatment |
|
|
Term
| Acetylcholine (Pharmacokinetics) |
|
Definition
| Rapidly hydrolyzed (high dose/concentration of IV must be infused to achieve desired effects), poorly absorbed and distributed into CNS, |
|
|
Term
| Acetylcholine (Side Effects) |
|
Definition
| cataract, corneal decompensation and edema, optic atrophy |
|
|
Term
|
Definition
| Stimulates beta1 adrenergic receptors causing increased contraction of heart |
|
|
Term
| Dobutamine (Clinical Use) |
|
Definition
| Short term management of cardiac decompensation. |
|
|
Term
| Dobutamine (Side Effects) |
|
Definition
| Increased HR, BP, PVC's, chest pain, palpitations |
|
|
Term
|
Definition
| Anticholinergic and antihistaminic drug. Inhibits reuptake of dopamine therby prolonging actions of dopamine |
|
|
Term
| Benztropine (Clinical Use) |
|
Definition
| Adjuctive treatment for Parkinsons |
|
|
Term
| Benztropine (Side Effects) |
|
Definition
| Tachycardia, confusion, hyperthermia |
|
|
Term
Acetylcholinesterase
(AChE) |
|
Definition
| Enzyme that hydolizes acetylcholine into choline & acetic acid |
|
|
Term
|
Definition
REVERSIBLE Acetylcholinesterase (AChE) Inhibitor (aka-partial Acetylcholine agonist)
Blocks AChE from breaking down Acetylcholine
-Crosses BBB
-Metabolized in Liver
-Excreted mostly in Kidney
-Can be given daily
-100% biovailability (administer drug PO) |
|
|
Term
Donepezil (Aricept)
(Clinical Use) |
|
Definition
| Used to treat Alzheimers Disease |
|
|
Term
Donepezil (Aricept)
(Side Effects) |
|
Definition
| S/E: dizziness, lacrimation, incr. salivation, incr. secretions iin GI/resp tract, bronchospasm, bradycardia, abd cramping |
|
|
Term
Acetylcholinesterase
(AChE) Inhibitors |
|
Definition
Two Types:
1. Irreversible- bind to enzyme (AChE) & render it inactive permanently (ie: insecticides)
2. Reversible- bind to enzyme (AChE) for short time then diffuse away (ie: Donepezil-"Aricept") |
|
|
Term
Cholinergic Agonist
S/EAcronym:
"DUMBBELLS" |
|
Definition
D- diarrhea
U-urination
M-miosis (pupil constriction)
B-bradycardia
B-brochoconstriction
E-emesis
L-lacrimation (tearing of eyes)
L-lethargy
S-salivation |
|
|
Term
Catechol-O-Methyltransferase
(COMT) |
|
Definition
| COMT= enzyme that metabolizes levodopa |
|
|
Term
|
Definition
Catechol-O-Methyltransferase (COMT) Inhibitor:
Drug blocks COMT so peripheral metabolism of levodopa is decreased
(This drug effects peripheral tissue only- not brain)
More levodopa is avail. to cross BBB
**should be given in combination with Levodopa & a dopadecarboxylase inhibitor (ie: Carbodopa) |
|
|
Term
|
Definition
| Used in combination with Levodopa and Carbidopa (dopa decarboylase inhibitor) to treat Parkinson's Disease |
|
|
Term
|
Definition
Drug increases Levodopa exposure & can lead to -dyskinesias, nausea & confusion
*Decrease daily dose of Levodopa by 30% in 1st 48 hrs of using Enacapone to avoid above S/E
Other S/E:
-diarrhea
-abd pain
-ortho hypotension
-sleep disturbances
-orange colored urine |
|
|
Term
|
Definition
Selective alpha 1 agonist
Activates phospholipase C - causing increased intracellular Ca+ and vasoconstriction |
|
|
Term
|
Definition
Orthostatic hypotension
Causes contraction vascular smooth muscle = Increase BP |
|
|
Term
|
Definition
HTN when in supine
Goose bumps (piloerection)
urinary retention |
|
|
Term
|
Definition
|
|
Term
|
Definition
Bronchodilation
Used: Asthma, CODP, or acute bronchospasms
Available in Aerosol inhaler, nebs, and PO tab/syrup |
|
|
Term
|
Definition
Tremors
Tachycardia
Overdose: Arrhythmias |
|
|
Term
|
Definition
a parasympathomimetic agent that works directly on muscarinic alkaloids or sythentics to increase secreations, increased smooth muscle contraction and changes in heart rate.
It is used primarily for glaucoma (eye drops/topical), in which the medications causes pupli constriction, ciliary muscle contraction and a decrease in the intraocular pressure.
It can also be used to treat Sjorns syndrome (oral) by increasing secretions of the exocrine glands. |
|
|
Term
|
Definition
| hypertension, hypotension, decrease heart rate and potiental for cardiac arrhythmias |
|
|
Term
|
Definition
Blocks monoamine oxidase B. Monamine oxidase B selectively metabolizes dopamine, therefore the medication will selectively block metabolism of dopamine.
It is used for treating early onset Parkinson's disease and used in conjunction with carbidopa/levodopa pharmacotherapy to prolong the effect of the carbidopa/levodopa in those with advanced Parkinson's disease. |
|
|
Term
|
Definition
| A direct cholinergic agonist which stimulates the release of acetylcholine, activating the parasympathetic nervous system. It is muscarinic specific. |
|
|
Term
| Bethanechol (Clinical Use) |
|
Definition
| Causes contraction of the detrusor muscle and relaxation of the trigone and sphincter to promote voiding. It is used post-op to promote voiding. Also used for post-op and neurogenic ileus. |
|
|
Term
|
Definition
| Increased cholinergic activity causing: Increased gastric acid secretion, increased GI and GU muscle tone, abdominal cramps, diarrhea, increased tearing of the eye, bronchoconstriction, hypotension, bradycardia. |
|
|
Term
|
Definition
| An anticholinergic, muscarinic antagonist, that blocks the effect of parasympathetic autonomic discharge. It is a tertiary amine alkaloid esters of tropic acid. It increases firing of the SA node and increases conduction through the AV node. Opposes the action of the vagus nerve, blocks acetylcholine receptor sites and decreases bronchial secretions. |
|
|
Term
|
Definition
| Prototype of the muscarinic receptor-blocking drugs |
|
|
Term
|
Definition
| It is used to transiently increase heart rate without a change in blood pressure or cardiac output. Used for parasympathomimetic drug poisoning. |
|
|
Term
|
Definition
| Mydriasis , cycloplegia, tachycardia, agitation. Remarkably safe in adults. Children, especially infants are very sensitive to the hyperthermic effects. Highly dangerous when overdose occurs in infants or children. |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| Dopamine agonist: Once administered, Levodopa is decarboxylated into dopamine. Dopamine does not cross the BBB but Levodopa, the metabolic precursur of dopamine, does |
|
|
Term
| Levodopa administration considerations |
|
Definition
| Absorbed rapidly from the small intestine, depends on rate of gastric emptying and pH of gastric contents. Administered with food delays Levodopa getting into the plasma. Has much higher plasma levels when given with a dopa decarboxylase inhibitior (carbidopa) |
|
|
Term
|
Definition
| GI: anorexia, N/V when not given with decarboxylase inhibitor. Cardiovascular: Arrythmias, tachycardia, postural hypotension. Behavior: depression, anxiety, agitation, changes in personality (more common in people taking Levodopa/decarboxylase inhibitor). Dyskinesias: Occur in 80% of patients taking Levodopa for more than 10 years |
|
|
Term
| Levodopa on/off phenomenon |
|
Definition
| Fluctuations in clinical response that are unrelated to the timing of the dose. Off periods of marked akinesia alternate with on periods of improved mobility but often more dyskinesia |
|
|
Term
| Levodopa-avoid administration |
|
Definition
| Patients taking MOAI's or within 2 weeks of discontinuing them due to potential for hypertensive crisis |
|
|
Term
| Levodopa contraindications/precautions |
|
Definition
| Psychotic patients: may exacerbate mental disturbances. Administer carefully and with monitoring in patients with open angle glaucoma, active peptic ulcer, patietns with history of melanoma |
|
|
Term
|
Definition
| Sympathomimetic, relatively pure alpha agonist |
|
|
Term
|
Definition
| Short term management of acute hypotension (IV) and intranasally as a decongestant to produce local vasoconstriction, also used as a mydriatic agent (dilate pupils) when examining the retina |
|
|
Term
| Epinephrine (EPI) / Norepinephrine (NE) |
|
Definition
| Sympathomimetic & Endogenous Catecholamines; Agonists at α1, α2, & β1; EPI also acts on β2; ↑BP, ↑ vasoconstriction, ↑ blood flow, ↑ contractility |
|
|
Term
|
Definition
| Dopamine (D3) agonsit; treats mild parkinsonism or acts as adjunct to levodopa |
|
|
Term
|
Definition
| Desglymidodrine (a metabolite of medodrine) is a selective alpha1 receptor agonist. It activates phospholipase C and causes an increase in intracellular calcium vasoconstriction. |
|
|
Term
|
Definition
| Amatine, ProAmatine, Gutron |
|
|
Term
|
Definition
| Treatment of orthostatic hypotension that is caused from impaired autonomic nervous system function |
|
|
Term
| Midodrine Adverse Effects |
|
Definition
| Hypertension (especially while in supine position) and bradycardia |
|
|
Term
| Midodrine Pharmacokinetics |
|
Definition
|
|
Term
|
Definition
| Beta 2 selective adrenoceptor agonist. It activates adenylyl cyclase. |
|
|
Term
|
Definition
| Bronchodilation. Symptomatic treatment of asthma and COPD |
|
|
Term
| Albuterol Edverse Effects |
|
Definition
| Tremors, Tachycardia, arrythmias |
|
|
Term
|
Definition
| Anticholinergic, Antispasmodic - Inhibits the muscarinic of acetylcholine on smooth muscle that relaxes the bladder smooth muscle thus maximizing urinary capacity & volume decreasing urgency, frequency, & incontinence |
|
|
Term
| Oxybutynin adverse effects |
|
Definition
| diarrhea, UTI, constipation, pruritis, angioedema, |
|
|
Term
| Oxybutynin Pharmacokinetics - |
|
Definition
| Metabolized - Liver (bypasses 1st pass-effect), Excreted - Kidneys |
|
|
Term
|
Definition
| (Catapres) - (Antihypertensive) - Stimulates alpha 2adrenergic receptors in the brain reducing sympathetic CNS outflow, decreased peripheral resistance, renal vascular resistance, heart rate, & blood pressure |
|
|
Term
| Clonidine Pharmacokinetics |
|
Definition
| Distribution - 20-40% protein binding, Metabolism - Liver, Excreted -Renal, not dialyzable, |
|
|
Term
| Clonidine Adverse Effects |
|
Definition
| Headache, dizziness,somnolence, erythema, pruritis, fatigue, xerostoma |
|
|
Term
|
Definition
| Immediate metabolic precursor of dopamine, enters the brain, where it is decarboxylated to dopamine |
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Term
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Definition
| immediate- N/V in 80% of patients, hypotension. Long-term-dyskinesia, motor fluctuation, psychiatric SE (vivid dreams, depression, anxiety, agitation, confusion, psychosis), insomnia |
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Term
| Levodopa pharmacokinetics |
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Definition
| rapidly absorbed by the small intestine, but its absorption depends on the rate of gastric emptying and the pH of the gastric contents. Only 1-3% of administered levadopa enters brain unaltered, the remainder is metabolized to dopamine which does not cross the BBB, so it must be given in large doses when given alone. |
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Term
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Definition
| Does not stop progression of parkinsonism, its early initiation lowers the mortality rate. It is particularily effective in relieving bradykinesia and any disabilities resulting from it. Generally given in combination with with carbidopa. |
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Term
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Definition
| alpha 1 receptor agonist, it constricts blood vessels by stimulating alpha-adrenergic receptors. Not a catechol derivative, it is not inactivated by COMT and has a longer duration of action than the catecholamines. Increase peripheral vascular resistance and blood pressure. It is an effective mydriatic and decongestant and can be used to raise the blood pressure. ADR- arrhythmias, CNS effects (anxiety, HA, insomnia). |
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Term
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Definition
| Affects the parasympathetic nervous system. Muscarinic agonist. |
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Term
| Bethanechol Pharmacokinetics |
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Definition
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Term
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Definition
| Has muscarinic action but no nicotinic action. Both directly and indirectly affects organ function: acetylcholine released from parasympathetic nerves activates the muscarinic receptor on the effector cells to alter organ functions directly; interacts with muscarinic receptors on nerve terminals to inhibit release of neurotransmitters which changes the effects of the parasympathetic nervous system and alters organ function. |
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Term
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Definition
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Term
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Definition
| Postoperative and neurogenic ileus, urinary retention |
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Term
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Definition
| Excessive parasympathomimetic effects, especially bronchospasm in asthmatics |
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Term
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Definition
| Additive with other parasympathomimetics |
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Term
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Definition
| Affects the parasympathetic nervous system. Muscarinic agonist. |
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Term
| Atropine Pharmacokinetics |
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Definition
| Well absorbed in gut and conjunctival membranes |
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Term
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Definition
| Competative antagonism (reversible blockade) of cholinomimetic actions at muscarinic receptors - effectiveness depends on tissue (most sensative: salivary, bronchial, and sweat glands) and source of agonist (exogenously administered cholinoceptor agonists better than endogenously released acetylcholine) |
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Term
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Definition
| CNS: minimal effects, slower, longer-lasting sedative effect on brain, decreases tremor in Parkinson's |
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Term
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Definition
| Retinal examination, prevention of synechiae after surgery |
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Term
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Definition
| Increase intraocular pressure in closed-angle glaucoma |
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Term
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Definition
| Antagonist at M receptors in the basal ganglia |
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Term
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Definition
| reduces tremor and rigidity in those with Parkinson's Disease but have little effect on bradykinesia |
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Term
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Definition
| Widely distributed in the body, usually within 30 minutes to one hour. Taken orally. Helps decrease the relatively access of acetylcholine in the body that occurs there is a deficiency of dopaminergic activity in the basal ganglia-striatum system. Daily dose is 1-6mg. |
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Term
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Definition
| sedation, mydriasis, urinary retention, constipation, confusion, dry mouth |
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Term
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Definition
| initially considered a relatively beta one selective agonist, but more complex than that. Actions are mostly activation of alpha and beta receptors. |
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Term
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Definition
| Activates adenylyl cyclase, increasing myocardical contractility. Has a positive inotropic effect |
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Term
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Definition
| Used in cardiac shock, acute heart failure, results in increased cardiac output with less reflex tachycardia, requires dose titration to desired effect |
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Term
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Definition
| increased blood pressure and allergic reactions |
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Term
| Pramipexole has preferential affinity for what recptors |
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Definition
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Term
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Definition
| A dopamine recepter agonist used in monotherapy for mild and advanced parkinsonism, allowing the dose of levodopa to be reduced and smooths out response fluctuations |
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Term
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Definition
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Term
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Definition
| Primary neuro transmitter at most sympathetic post ganlionic nerve endings |
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Term
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Definition
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Term
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Definition
| Agonist at both Alpha and Beta receptors |
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Term
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Definition
| Selective inhibitor of catechol-O-methyltransferase (COMT) used in the treatment of Parkinsons disease. Typically given with levodopa because it reduces metabolism of levodopa and prolongs its action. |
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Term
| Entacapone Pharmacologic Effects |
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Definition
| Rapidly absorbed, bound to plasma proteins, and metabolized before excretion |
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Term
| Entacapone Adverse Reactions |
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Definition
| Dyskinesias, nausea, confusion, diarrhea, abdominal pain, orthostatic hypotension, sleep disturbances, and orange discoloration of the urine. |
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Term
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Definition
| Cholinesterase inhibitor. Inhibits the enzyme acetylcholinesterase which breaks down acetylcholine. Used in the treatment for Alzheimer's disease. |
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Term
| Donepezil Adverse Reactions |
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Definition
| Cause significant adverse effects, including nausea and vomiting, and other peripheral cholinomimetic effects. Use in caution in patients receiving other drugs that inhibit cytochrome P450 enzymes. |
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Term
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Definition
| primary excitatory nuerotransmitter released by cholinergic fibers in the autonomic nervous system (ANS) There are two main cholinergic receptors muscarinic and nicotinic |
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Term
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Definition
| drug with anticholinergic action used for GI disorders such as IBS and minor diarrhea- reduces smooth muscle and secretory activity of the gut |
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Term
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Definition
| competative antagonism at M3 receptors |
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Term
| Dicyclomine Pharmacokinetics |
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Definition
| short 1/2 life, but action lasts up to 6 hours |
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Term
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Definition
| tachycardia, confusion, urinary retention, increased intraoccular pressure |
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Term
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Definition
| Parasympathomimetic; acts as a partial agonist for activation of muscarinic receptors. |
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Term
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Definition
| Excessive parasympathomimetic effects such as bronchospasm, bradycardia, excessive sweating |
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Term
| Pilocarpine Clinical Uses |
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Definition
| Glaucoma; Sjogren’s syndrome |
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Term
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Definition
| Selectively inhibits MAO-B; also inhibits MAO-A at higher doses. Increases dopamine stores in neurons. |
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Term
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Definition
| May causes serotonin syndrome with meperidine, SSRIs, and tricyclic antidepressants. Avoid all OTC cold preparations. |
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Term
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Definition
| Parkinson’s disease, used either alone or as an adjunct to prolong the effects of levodopa-carbidopa |
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Term
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Definition
| Primary clinical use is for topical anesthesia for ear, nose, and throat procedures where it also serves as a potent vasoconstrictor to reduce bleeding. Being replaced by newly developed drugs due to concerns for systemic toxicity and the regulation involved with dispensing and handling |
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Term
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Definition
| MOA = Blocks the uptake of dopamine, noradrenaline, and serotonin, through their respective receptors; inhibits voltage-gated sodium channels, which blocks the conduction of action potentials. |
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Term
| Cocain - Nursing Considerations |
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Definition
| Nursing considerations = Highly addictive; increases arterial pressure, produces tachycardia and often produces ventricular arrhythmias. Causes loss of appetite, hyperactivity, and insomnia. Increases risk of intracranial hemorrhage, ischemic stroke, MI, and/or seizures. Overdose can lead to hyperthermia, coma, and death. |
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Term
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Definition
| A decarboxylase inhibitor; increases the efficacy of levodopa. Doubles the amount of levodopa that gets to the blood, and triples the amount that gets to the brain. |
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Term
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Definition
| Acetylcholinesterase inhibitor (prevents acetylcholinesterase from breaking down acetylcholine to choline and acetate, thereby increasing cholinergic tone). ADR: related to increased acetylcholine (dizziness, salivation, lacrimation, excessive secretions, bronchospasm) |
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Term
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Definition
| Selective alpha 1 agonist. |
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Term
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Definition
| locally for nasal decongestion or systemically (IV) to raise blood pressure. Constricts alpha receptor vessels. |
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Term
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Definition
| used for parkinsons disease as an oral agent that is rapidly absorbed in GI when taken on empty stomach. |
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Term
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Definition
| crosses BBB, dopamine does not. Used often as first line defense then used in combination with carbidopa to combat decreased effects after 3-4 years. |
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Term
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Definition
| ADR- take in divided small doses to prevent anorexia and nausea. Fewer GI effects when combination drug Sinimet (carbidopa/levodopa) is used. Asymptomatic postural hypotension, do not use with MOAI's. |
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Term
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Definition
| Dyskinesias in 80% of people- twitching movements or face or distal extremities. |
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Term
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Definition
| Behavioral responses of dellusion, hallucination depression or anxiety with administration of sinimet but decreased when levodopa alone. Do NOT use in psychotic pts or thos with angle-closure glaucoma. Use care with peptic ulcers, hx of melanoma. |
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Term
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Definition
| Within the parasympathetic nervous system, bethanechol stimulates muscarinic receptors as a direct agonist in cholinergic transmission. More specific use , negligible to nicotine receptors. |
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Term
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Definition
| Increased gastric acid secretions, increased GI and GU muscle tone, bronchoconstriction, hypotension, bradycardia, increased tearing of the eye. Often given to promote urination after surgery. |
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Term
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Definition
| Prototype for antimuscarinics, tertiary amine, causes reversible blockade, antagonist of cholinomimetic actions at muscarinic receptors with parasympathetic system. Used to treat bradycardia and organophosphate poisoning. |
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Term
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Definition
| Decreased GI motility, decreased urinary function, decrease in secretions, prevents bronchoconstriction, dilates pupils, confusion, sleepy, and increased heart rate as a reflux from vasodilation. Blocks action of vegus nerve. |
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Term
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Definition
| Dopamine receptor agonist. MOA: Direct agonist at D3 receptors, nonergot. Reduces the symptoms of parkinsonism and smoothes out fluctuations in levodopa response. |
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Term
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Definition
| Stimulates cholinergic receptors by acting as a direct acting muscarinic (an agononist to the PNS) Has little to no effect at the nicotinic receptors. Activates all 3 "M" receptors causing increased secreation, decreased heart rate, increases GI motility by smooth muscle contraction. Used for glaucoma and Sjogren's syndrome. Can be administered PO or topically. ADR include those associated with increased PNS actions: dizziness, HA, N/V (d/t increased GI motility), urinary frequency, bronchospasm, increased lacrimation, and pupil constriction. Contraindicated in Angle-closure glaucoma. Renal excretion. |
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Term
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Definition
| Adverse Effects: Nausea and vomiting, postural hypotension, dyskinesias, confusion, impulse control disorders and sleepiness |
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Term
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Definition
| Specific sympathomimetic drug. Both alpha and beta receptor agonist. Very potent vasoconstrictor and cardiac stimulant. |
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Term
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Definition
| Both alpha-1 and alpha-2 receptor agonist. Also activates beta-1 receptors with similar potency as epinephrine. Little effect on beta-2 receptors. Increases peripheral resistance and both diastolic and systolic BP. Baroreflex activation tends to overcome the direct positive chronotropic effects of norepi, but the positive inotropic effects of the heart are maintained. |
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Term
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Definition
| Causes a rise in SBP due to positive inotropic and chronotropic actions on the heart-mainly beta-1 receptors. Also activates beta-2 receptors which can cause dilation in some vessels. This drug functions largely as a hormone, it acts on distant cells. |
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Term
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Definition
| An indirect agonist by acting as an irreversible monoamine oxidase B inhibitor to treat Parkinsonism. This inactivation of MAO leads to increased amounts of dopamine in the CNS. Is used for early symptomatic treatment and as adjunctive therapy to increase the effects of sinemet. ADR include: dizziness, hallucinations, rhinitis, anorexia, N/V, arthralgia, dyskinesia (d/t increased levodopa). Metabolized through the liver, modify in hepatic impairment. |
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Term
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Definition
| Direct parasympathetic stimulation at muscarinic and nicotinic receptors. Hydophilic molecules- poorly absorbed and distributed in CNS. Hydrolysed in the GI tract. |
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Term
| Acetylcholine organ system effects and ADRs |
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Definition
| Eye: miosis; CV: vasodilation, decreased peripheral vascular resistance; Resp: bronchoconstriction, increased secretions; GI: increased peristalsis, stimulates saliva and gastric glands, relaxes spincters; GU: relaxes sphincters/ muscles, promotes voiding; CNS: alertness- coma, tremors, convulsions. ADRs: nausea/vomiting, urinary urgency, salivation, sweating, vasodilation, bronchconstriction. When targeting one organ system, will have side effects in others. |
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Term
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Definition
| Anticholinergic drug used for irritable bowel syndrome and diarrhea. Competitive antagonist at M3 receptors. Reduces smooth muscle activity and decreases GI secretions. ADRs: tachycardia, confusion, urinary retention, increased intraocular pressure |
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Term
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Definition
| Alpha 1 selective agonist. Causes an increase in PVR; increases arteriolar and venous tone which causes a rise in blood pressure. Used to help patients with orthostatic hypotension. Midodrine (Prodrug) is converted to Desglymidodrine (active agent). ADR: Supine HTN, urinary urgency or retention, paresthesias, piloerection, and pruritis. |
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Term
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Definition
| Sympathomimetic agent. Beta-2 agonist as well as some Beta-1 activity. Used for bronchodilation. Comes in inhilation and oral form. ADR: Tremor, irritability, insomnia, irregular heartbeat. |
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Term
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Definition
| Antimuscarinic drug somewhat selective for M3 receptors used in treatment of over active bladder. |
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Term
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Definition
| alpha2 selective agonist used to treat hypertension |
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Term
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Definition
| Local anesthetic with peripheral sympathomimetic action resulted from transmitter reuptake inhibition at nonadrenergic synapses.At CNS produces short lasting but more intense .amphetamine like psychologycal effect. |
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Term
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Definition
| Restricted to topical anesthesia(ear,nose and throat procedures) to reduce bleeding.Other anesthesics combined with vasoconstrictor are preferred to avoid Cocaine systemic toxicity and handling this controlled substance. |
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