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Clinical Pharmacology > Autonomic Drugs > Flashcards

Autonomic Drugs Flashcards

Test receptor target and basic function of drugs.

1
Q

Muscarine

A

Muscarinic Receptor Agonist

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2
Q

Carbachol

A

Muscarinic Receptor Agonist, also Nicotinic, local use for glaucoma

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3
Q

Bethanechol

A

Muscarinic Receptor Agonist, resistant to cholinesteraes, increases GI and urinary motility

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4
Q

Methacholine

A

Muscarinic Receptor Agonist, better duration and selectivity, CV adverse fx, for asthma, methacholin challenge.

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5
Q

Pilocarpine

A

Muscarinic Receptor Agonist, increases salivation and sweating, used locally for glaucoma.

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6
Q

Physostigmine

A

Reversible Cholinesterase Inhibitor, treat anticholingergic overdose by decreasing Ach destruction, for glaucoma, too.

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7
Q

Neostigmine

A

Reversible Cholinesterase Inhibitor, treat myasthenia gravis, has direct nicotinic agonist action in skeletal muscle

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8
Q

Edrophonium

A

Reversible choline stress inhibitor. Short acting (2-10 minutes), distinguish myasthenia gravis from cholinergic crisis.

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9
Q

Pralidoxime

A

Irreversible cholinesterase inhibitor, reactivates phosphorylated AChesterases

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10
Q

Pyridostigmine

A

Reversible Cholinesterase Inhibitor, treat myasthenia gravis

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11
Q

Nicotine

A

Nicotinic agonist

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12
Q

Lobeline

A

Nicotinic agonist, used for nicotinic withdrawal

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13
Q

Arecoline

A

Nicotinic agonist from betel nut, peripheral like methacholine

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14
Q

Succinylcholine

A

Nicotinic agonist, used for paralysis during surgery b/c depolarizing blockade, resists AChE

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15
Q

Atropine

A

Muscarinic Receptor Antagonist, from deadly nightshade, decreases secretion, dilates pupil, increases HR, decreases voiding, use to treat severe bradycardia, bladder spasms, antidote to cholinergic poisoning.

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16
Q

Scopolamine

A

Muscarinic Receptor Antagonist, tertiary amine, prevents and treats motion sickness/antiemetic

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17
Q

Glycopyrrolate

A

Muscarinic Receptor Antagonist, Quaternary amine (less CNS & BBB crossing), decreases oral secretions, treat peptic ulcer disease, decrease GI spasms, decrease bradycardia during surgery. Delayed but measurable CNS & cog anticholinergic fx.

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18
Q

Imatropium/Tiotropium

A

Muscarinic Receptor Antagonist, quat. ammonium compounds, fx on resp system – helps COPD, local if inhaled.

19
Q

Oxybutynin, fesoterodine, propantheline, tolterodine, trospium

A

Nonspecific muscarinic antagonists used for incontinence and overactive bladder syndrome.

20
Q

Pancuronium

A

nicotinic receptor antagonist, Long acting

21
Q

Rocuronium

A

nicotinic receptor antagonist, Rapid/intermediate onset

22
Q

Norepinephrine

A

Direct acting sympathomimetic - acts on alpha 1,2, beta 1,2,3, alpha fx predominate. Intense vasoconstriction, increase MAP and PVR, increase HR, but reflex bradycardia due to baroreceptors

23
Q

Epinephrine

A

Direct acting sympathomimetic, synthesized in adrenal medulla, acts on A1/2, B1/2/3, low doses B dominates (vasodilation), higher doses A dominates (vasoconstriction). vasoconstriction (A1) increases inotropy, chronotropy (B1), bronchodilation (B2), lipolysis (B3), decreased PVR (B2) leading to decrease in diastolic BP and increased systolic BP.

24
Q

Dopamine

A

Direct acting sympathomimetic, vasodilation in peripheral renal, mesenteric & coronary/vascular beds b/c D1 receptors AC –> cAMP –> vasodilation, inhibits NE release. @higher doses, B1 cardiac fx predominate, even higher doses, A1AR activated - treat shock via vasoconstriction, increase BP.

25
Q

Phenylephrine

A

A1 selective adrenergic agonist, longer acting, intense vasoconstriction, increase PVR, increase MAP, pot. reflex bradycardia if parenteral, topically for mydriasis. Via GqA, IP3, Ca, MLCK

26
Q

Clonidine

A

A2 selective adrenergic agonist. CNS: postsynaptic A2R on CV regulatory centre, Peripherally: presynaptic A2R blocks catecholamine release from post ganglionic sympathetic neurons.

27
Q

Dobutamine

A

B1 selective adrenergic agonists, racemic mixture, l-isomer is A1 agonist and weak B1 agonist, d-isomer is A1 antagonist, strong B1 agonist, inotropic&raquo_space; chronotropic fx, used to treat urgent heart failure

28
Q

Salbutamol/terbutalene

A

B2 selective adrenergic agonists, short acting (3-4 hrs), via AC, cAMP, PKA blocking MLCK

29
Q

Salmeterol, formoterol

A

B2 selective adrenergic agonists, long acting (12 hrs), via AC, cAMP, PKA blocking MLCK

30
Q

Isoproterenol

A

Non-selective B agonist, peripheral vasodilation, tachycardia (B1), myocardial stimulation (B2) , bronchial relaxation (B2). RARELY USED.

31
Q

Amphetamines, tyramine

A

Indirect adrenergic agonist, increases NE release, leads to vasoconstriction, increase MAP (A-AR), increased inotropy (B), adverse fx: HTN, cerebral hemorrhage, coma, confusion, anxiety, hallucinations, tremor

32
Q

Cocaine, TCA

A

Decrease NE reuptake

33
Q

Ephedrine/pseudoephedrine

A

Mixed sympathomimetic, release stored NE, stim A1, B1, and B2 AR, similar to epi, less potent

34
Q

Phenoxybenzamine

A

Nonselective A-AR antagonist/sympatholytic, irreversible, inhibits A1/A2, decrease PVR, reflex tachycardia, increase NE release from A2 blockade, not useful HTN treatment

35
Q

Phentolamine

A

Nonselective A-AR antagonist/sympatholytic, inhibits A1/A2, decrease PVR, reflex tachycardia, increase NE release from A2 blockade, not useful HTN treatment

36
Q

Prazosin/terazosin/doxazosin

A

A1 selective adrenergic antagonists, useful in HTN treatment, relaxation of arterial and venous smooth muscle

37
Q

Tamsulosin

A

A1A selective adrenergic antagonist, treat BPH, vasodilation of smooth muscle.

38
Q

Propanolol

A

Non-selective B-AR antagonist (sympatholytic), blocks B1 & B2 equally –> resp problems. Decreases inotropy and chronotropy, decrease CO, SA & AV activity, peripheral vasoconstriction, bronchoconstriction

39
Q

Timolol

A

Non-selective B-AR antagonist (sympatholytic), reduce aqueous humour production in eye.

40
Q

Nadolol

A

Non-selective B-AR antagonist (sympatholytic), longer duration of action.

41
Q

Labetalol

A

3rd gen Non-selective B-AR antagonist (sympatholytic), decrease BP w/out reflex tachycardia, use to treat pheochromocytoma/HTN emergencies, 8 hour half life.

42
Q

Metoprolol

A

B1 Selective AR Antagonist, no bronchoconstriction b/c no B2 antagonist activity, useful in db HTN patient

43
Q

Atenolol

A

B1 Selective AR Antagonist, no bronchoconstriction b/c no B2 antagonist activity, useful in db HTN patient

44
Q

Bisoprolol

A

B1 Selective AR Antagonist, no bronchoconstriction b/c no B2 antagonist activity, useful in db HTN patient

Clinical Pharmacology (3 decks)

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