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Pharmacology > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

1
Q

Phenylephrine

A

Adrenergic Agonist: Direct Acting: Alpha1 Selective
Activates alpha adrenergic receptors in vascular sm: increases BP & TPR (reflex bradycardia)
Activates beta receptors only at much higher conc.
Clinical Indications: antihypotensive (orthostatic hypotension & shock), paroxysmal atrial tachycardia, nasal decongestant, mydriatic

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2
Q

Clonidine

A

Adrenergic Agonist: Direct Acting: Alpha2 Selective
Activates central alpha2 receptors (located on presynaptic nerve terminals) which decrease NT release & NE synthesis: decreases central sympathetic outflow: BP decreases. Also decreases aqueous humor production: decreased intraocular pressure
Uses: systemic hypertension and glaucoma
Adverse Effects: dry mouth, sedation, hypotension

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3
Q

Terbutaline

A

Adrenergic Agonist: Direct Acting: Beta2 Selective
Relax bronchial sm and decrease airway resistance, suppress release of leukotrienes & histamine from mast cells in lungs, enhance mucociliary function, decrease microvascular permeability, inhibit phospholipase A2
Not a substrate for methylation by COMT
Used for long-term tx of obstructive airway diseases, acute bronchospasm, emergyency tx of status asthmaticus (IV)

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4
Q

Fenoldopam

A

Adrenergic Agonist: Direct Acting: D1 Selective
D1»D2 Some stimulation of alpha2: feedback inhibition of NE release
Renal, mesenteric, peripheral, coronary vasodilation
RBF maintained & natriuresis promoted
Used during Hypertensive Crisis Side effect: hypotension

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5
Q

Isoproterenol

A

Adrenergic Agonist: Direct Acting: Non-Selective
Powerful Beta1&2 agonist, no effect on alpha
Decrease TPR, Increase HR, arrhythmias, myocardial contractility
Uses: bradycardia or complete heart block, particularly in torsade de pointes, CHF: as an inotropic agent, can be used in MI as an inotropic agent, high dose can cause myocardial necrosis

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6
Q

Dobutamine

A

Adrenergic Agonist: Direct Acting: Non-Selective
Stimulates alpha1, beta1&2, mainly acts on beta1 at therapeutic doses (considered selective)
Does not affect release of NE from nerve endings, does not affect dopaminergic receptors.
beta1 = +inotropic effect (>isoproterenol), +chronotropic effect: SA node automaticity, AV conduction
Does not change TPR b/c balance b/t alpha1&beta2
Used for: short-term tx of cardiac failure (post-cardiac surgery, CHF, MI) Stress Test: used in pts w/ coronary artery disease to assess exercise tolerance
Adverse Effects: Excessive increases in BP&HR, increased ventricular response rate in pts w/ AFib, entricular ectopic activity, my increase size of MI, tolerance may develop

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7
Q

Low Dose Epinephrine IV

A

Adrenergic Agonist: Direct Acting: Non-Selective
Epi stimulates everything: alpha1&2 beta1&2
In low dose IV: effects on beta1&2 predominate:
Beta1: increase pulse pressure, HR, SV, CO
Beta2: Decrease TPR, slight decrease in MAP, reflex tachycardia

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8
Q

Moderate Dose Epinephrine IV

A

Adrenergic Agonist: Direct Acting: Non-Selective
Epi stimulates everything: alpha1&2 beta1&2
In med dose IV: effects on beta1&2 and alpha1
Beta1: increase pulse pressure, HR, SV, CO
Beta2: Decrease TPR, slight decrease in MAP, reflex tachycardia
Alpha1: Increased TPR & BP
Final Effects = BP increased

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9
Q

High Dose Epinephrine IV

A

Adrenergic Agonist: Direct Acting: Non-Selective
Epi stimulates everything: alpha1&2 beta1&2
In high dose IV: predominant actions on alpha1 receptor causing an increase in TPR and BP w/ reflex bradycardia
Lesser effects on beta1&2 at high doses

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10
Q

Norepinephrine

A

Adrenergic Agonist: Direct Acting: Non-Selective
alpha1»beta1»»»beta2 (so no vasodilation)
Increase sBP, dBP, pulse pressure, coronary blood flow (coronary dilation and increased BP)
Unchanged or decreased CO d/t reflex bradycarida
Increase TPR, decrease renal, splanchnic hepatic blood flow
Limited therapeutic value. Can tx hypotension but dose titration usually required

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11
Q

Dopamine

A

Adrenergic Agonist: Direct Acting: Non-Selective
D1, D2, Beta1, Alpha1
Dose dependent (low dose is most common)
Diuretic effect: D2 receptors: increased Na+ filtration and decerased reabsorption = Na+ diuresis
Presynaptic D2 receptors: decrease NE release: vasodilation
Precaution: hypovolemia should aloways be corrected before dopamine use
Used in tx of severe CHF, particulary in pts w/ oliguria and low or normal peripheral vascular resistance. Cardiogenic/septic shock.

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12
Q

Ephedrine

A

Adrenergic Agonist: Mixed Acting
Directly activates adrenoceptors & indirectly releases NE
First orally active sypathomimetic drug, ma-huang, ↑bioavailability, long duration of action, mild CNS stimulant, decongestant (pseudoephedrine)

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13
Q

Amphetamine

A

Adrenergic Agonist: Indirect-Acting
CNS effects: releases biogenic amines from storage sties in nerve terminals, ↑medullary resp center, ↑cortex&reticular activating system which prevents fatigue and delays need for sleep. Decrease need for food.
CV effects: activates peripheral alpha/beta receptors, ↑s&dBP, HR, cardiac arrhythmias may occur, ↑bladder sphincter cx: used to tx enuresis/incontinence

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14
Q

Tyramine

A

Adrenergic Agonist: Indirect-Acting
Can be used to make NE & epi using indirect pathway
Destroyed by MAO in intestinal wall and liver
In pts using MAOIs, ingestion of fermented cheese (high tyramine levels) can cause dangerous ↑BP
Tyramine does not cross BBB = peripheral effects

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15
Q

Phenoxybenzamine

A

Alpha Adrenoceptor Antagonist (Alpha Blocker)
Irreversibly blocks alpha1&2, lowers BP, HR raises d/t indirect baroreflex activation
Tx: pheochromocytoma, high catecholamine states
T1/2>1day: orthostatic hypotension, tachycardia, MI

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16
Q

Prazosin (Terazosin, Doxazosin)

A

Alpha Adrenoceptor Antagonist (Alpha Blocker)
Blocks only alpha1, NOT alpha2
Lowers BP
Tx: HTN, BPH
Larger depressor effect w/ first dose may cause orthostatic hypotension (notable side effect)

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17
Q

Tamsulosin

A

Alpha Adrenoceptor Antagonist (Alpha Blocker)
slightly selectve for alpha1A, blockade may relax prostatic sm more than vascular sm
Used to tx: BPH, orthostatic hypotension may be less common than with prazosin

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18
Q

Propranolol (Nadolol, Timolol, Pindolol - has ISA, less bradycardia)

A

Beta Adrenoceptor Antagonist (beta blocker)
1st gen beta blocker - nonselective (blocks b1 = b2)
Effects: lower HR, BP, reduce renin
Tx: HTN, angina pectoris, arrhythmias, migrane, hyperthyroidism
Toxic: Bradycardia, worsened asthma, fatigue, vivid dreams, cold hands

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19
Q

Metoprolol (Atenolol, Esmolol, Alprenolol, Betaxolol, Acebutolol - has ISA, less bradycardia)

A

Beta Adrenoceptor Antagonist (beta blocker)
2nd gen beta blocker - selective (blocks b1»>b2)
Effects: lower HR, BP, reduce renin, may be safer in asthma pts d/t less b2 effects
Tx: angina pectoris, HTN, arrhythmias
Toxic: bradycardia, fatigue, vivid dreams, cold hands

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20
Q

Labetalol

A

Beta Adrenoceptor Antagonist (beta blocker)
3rd gen beta blocker - vasodilatory (b1=b2>=a1>a2)
Effects: lowers blood pressure w/ limited HR increase
Tx: HTN
This drug is commonly used like it’s one of the alpha blockers - it can lower BP with less reflex tachycardia than the other alpha blockers.

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21
Q

Alpha-Methyldopa

A

Alpha2 Adrenoceptor Agonist

Decrease BP in pregnency

22
Q

Apraclonidine & Brimonidine

A

Alpha2 Adrenoceptor Agonist

Lover intraocular pressure only

23
Q

Metaproterenol

A

Beta2 Adrenoceptor Agonist
Asthma, COPD, bronchospasm
Less used than albuterol & terbutaline

24
Q

Albuterol

A

Beta2 Adrenoceptor agonist

For asthma

25
Q

Ritodrine

A

Beta2 Adrenoceptor agonist
uterine relaxant
stop preterm labor

26
Q

Cocaine

A

Reuptake Inhibitor

Indirect Adrenergic Agonist

27
Q

Pargyline & Entacapone

A

MAO/COMT inhibitor

Indirecet Adrenergic Agonist

28
Q

Phentolamine

A

Alpha1 & Alpha 2 Adrenoceptor Antagonist
Give to pts on MAOI who eat tyramine
Can cause orthostatic hypotension & tachycardia

29
Q

Yohimbine (Rauwoscine, Torazoline)

A

Alpha 2 > Alpha 1 Adrenoceptor Antagonist
Increase NE release, Increase BP & HR
Use in male erectile dysfunction & hypotension

30
Q

Carvedilol

A

Beta Adrenoceptor Antagonist (beta blocker)
3rd gen beta blocker - vasodilatory (b1=b2>=a1>a2)
Effects: lowers blood pressure w/ limited HR increase
Use to Tx Heart Failure

31
Q

Acetylcholine

A

Prototype direct acting cholinoceptor agonist

Rapid destruction, not usually clinically used

32
Q

Methacholine

A

Direct Acting Muscarinic Cholinoceptor Agonist

Dx asthma

33
Q

Carbachol

A

Direct Acting Muscarinic Cholinoceptor agonist
Lower intraocular pressure
Use to tx glaucoma

34
Q

Bethanechol

A

Muscarinic cholinoceptor agonist
Increase GI motility & bladder
Tx ileus & unobstructed urinary retention

35
Q

Pilocarpine

A

Muscarinic cholinoceptor agonist
Miosis, glaucoma, xerostomia
test PANS dysfunction

36
Q

Nicotine

A

Nicotinic cholinoceptor agonist
Muscle spasms, increased HR, peripheral vasoconstriction, increased gut motility & secretion, increased RR, nausea/vomiting
Tx smoking cessation

37
Q

Edrophonium

A 
Cholinesterase inhibitor (indirect agonist)
Dx myasthenia gravis
38
Q

Neostigmine & Pyridostigmine

A

Cholinesterase inhibitor (indirect agonist)
Doesn’t cross BBB
Tx ileus, myasthenia gravis, urinary retention, reverse depolarizing NM blockers

39
Q

Physositmine

A 
Cholinesterase inhibitor (indirect agonist)
Crosses BBB
Use in atropine overdose
40
Q

Donepezil

A

Cholinesterase inhibitor (indirect agonist)
Crosses BBB
Tx Alzheimers

41
Q

Organophosphates

A

Irreversible cholinesterase inhibitors
used in insecticides (malathion, prathion, sarin, echothiophate)
Cause Diarrhea, Urination, Miosis, Bradycardia, Bronchospasm, Excitation of skeletal muscles & CNS, Lacrimation, Sweating, Salivation (DUMBBELSS)
Treat with atropine

42
Q

Atropine

A

Muscarinic receptor antagonist
Treat ACh intoxication (except E symptom)
Antisecratory (can lead to dry mouth, increased temperature, flushing, disorientation), causes mydrisasis & cycloplegia

43
Q

Ipratropium

A

Muscarinic receptor antagonist
Decreases bronchoconstriction & bronchial secretions
Tx asthma & COPD

44
Q

Benztropine

A

Muscarinic receptor antagonist
Tx Parkinson’s
Causes decreased GI motility & Increased HR

45
Q

Hexamethonium & Mecamylamine

A

Nicotinic Receptor Antagonist (ganglion)
Decrease autonomic tone, prevent baroreceptor change in HR
Cause vasodilation, decreased BP, increased HR, mydriasis, cycloplegia, decreased GI motility, decreased sweat/saliva (xerostomia, anhidrosis), constipation & urinary retention

46
Q

D-tubocurarine

A

Non-depolarizing Neuromuscular (Nm) blocker
Prevent chanel opening & decrease ACh release
Anesthesia, tracheal intubation, convulsions
Can cause hypotention, increased gastric & intraocular pressure, muscle pain, & hyperkalemia

47
Q

Succinylcholine

A

Depolarizing Neuromuscular Blocking Drug
Causes depolarizing paralysis & later desensitization of chanels to depolarization
Anesthesia, tracheal intubation, convulsions
Can cause hypotention, increased gastric & intraocular pressure, muscle pain, & hyperkalemia

48
Q

Muscarinic Antagonists

A

Atropine, Ipratropium, Benztropine

49
Q

Direct Acting Cholinoceptor Agonists

A

Methacholine, Carbachol, Bethanechol, Pilocarpine

50
Q

Indirect Acting (reversible) Cholinoceptor Agonists

A

Edrophonium, Neostigmine, Pyridostigmine, Physostigmine, Donepezil

51
Q

Alpha receptor Antagonists

A

Prazosin, Phenoxybenzamine, Tamsulosin, Phentolamine, Yohimibine

52
Q

Beta Receptor Antagonists

A

Propranolol, Metoprolol, Labetalol, Carvedilol

Pharmacology (8 decks)

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