Autonomic Drugs

Question 1

Muscarine

Answer 1

Muscarinic Receptor Agonist

Question 2

Carbachol

Answer 2

Muscarinic Receptor Agonist, also Nicotinic, local use for glaucoma

Question 3

Bethanechol

Answer 3

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

Question 4

Methacholine

Answer 4

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

Question 5

Pilocarpine

Answer 5

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

Question 6

Physostigmine

Answer 6

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

Question 7

Neostigmine

Answer 7

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

Question 8

Edrophonium

Answer 8

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

Question 9

Pralidoxime

Answer 9

Irreversible cholinesterase inhibitor, reactivates phosphorylated AChesterases

Question 10

Pyridostigmine

Answer 10

Reversible Cholinesterase Inhibitor, treat myasthenia gravis

Question 11

Nicotine

Answer 11

Nicotinic agonist

Question 12

Lobeline

Answer 12

Nicotinic agonist, used for nicotinic withdrawal

Question 13

Arecoline

Answer 13

Nicotinic agonist from betel nut, peripheral like methacholine

Question 14

Succinylcholine

Answer 14

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

Question 15

Atropine

Answer 15

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.

Question 16

Scopolamine

Answer 16

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

Question 17

Glycopyrrolate

Answer 17

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.

Question 18

Imatropium/Tiotropium

Answer 18

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

Question 19

Oxybutynin, fesoterodine, propantheline, tolterodine, trospium

Answer 19

Nonspecific muscarinic antagonists used for incontinence and overactive bladder syndrome.

Question 20

Pancuronium

Answer 20

nicotinic receptor antagonist, Long acting

Question 21

Rocuronium

Answer 21

nicotinic receptor antagonist, Rapid/intermediate onset

Question 22

Norepinephrine

Answer 22

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

Question 23

Epinephrine

Answer 23

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.

Question 24

Dopamine

Answer 24

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.

Question 25

Phenylephrine

Answer 25

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

Question 26

Clonidine

Answer 26

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

Question 27

Dobutamine

Answer 27

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

Question 28

Salbutamol/terbutalene

Answer 28

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

Question 29

Salmeterol, formoterol

Answer 29

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

Question 30

Isoproterenol

Answer 30

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

Question 31

Amphetamines, tyramine

Answer 31

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

Question 32

Cocaine, TCA

Answer 32

Decrease NE reuptake

Question 33

Ephedrine/pseudoephedrine

Answer 33

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

Question 34

Phenoxybenzamine

Answer 34

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

Question 35

Phentolamine

Answer 35

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

Question 36

Prazosin/terazosin/doxazosin

Answer 36

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

Question 37

Tamsulosin

Answer 37

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

Question 38

Propanolol

Answer 38

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

Question 39

Timolol

Answer 39

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

Question 40

Nadolol

Answer 40

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

Question 41

Labetalol

Answer 41

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

Question 42

Metoprolol

Answer 42

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

Question 43

Atenolol

Answer 43

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

Question 44

Bisoprolol

Answer 44

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