Autonomic Cholinergics I

Question 1

Neostigmine

Answer 1

Anticholinesterase inhibitor reversible; charged can’t get in CNS

Question 2

Phyostigmine

Answer 2

anticholinesterase inhibitor reversible; rx glaucoma for increase intraocular pressure; can cross BBB

Question 3

Pilocarpine

Answer 3

Muscarinic Antagonists

Question 4

Atropine

Answer 4

Muscarinic Antagonist; antidote to sarin; all M receptors

Question 5

Hyoscine

Answer 5

Muscarinic Antagonists

Question 6

Tubocarine

Answer 6

NMJ (nm) competitive antagonists, non depolarizing

Question 7

Pancuronium

Answer 7

NMJ (nicotinic) competitive anatagonists, non depolarizing

Question 8

Suxamethonium

Answer 8

NMJ blocking agent, not reversed by anticholinesterase Depolarizing agent

Question 9

M1 receptor

Answer 9

Location: nerves; Gq IP3 DAG

Question 10

M2 receptor

Answer 10

“cardiac M2” heart, nerves, smooth muscle; Gi inhibit cAMP, activate K+ channels (GIRK inward rectifying); inhibit funny current (if = funny pacemaker channel responsible for earliest part of phase 4 diastolic depolarization. decrease cAMP, decrease slope phase 4, decrease heart rate M2 receptor activation. increase camp, increase slope phase 4, increase heart rate (ie NE B1 receptor activation). AcH also acts on AV node to slow conduction velocity and prolong refractory period

Question 11

Methacholine

Answer 11

ACH agonist, choline ester slightly susceptible to ACHE (direct acting) Muscarinic Action,

Question 12

Carbachol

Answer 12

Direct acting ACH agonist, not susceptible to ACHE, muscarinic slight activity, more nicotinic

Question 13

Bethanechol

Answer 13

direct acting ACH agonist to muscaranic (slight) not to nictoninc, not susceptible to ACHE

Question 14

Pilocarpine

Answer 14

muscaranic agonist, not suscpetible to ACHE (it is an alkaloid)

Question 15

Lobeline

Answer 15

Nicotinic agonist, not susceptible to ACHE (it is an alkaloid)

Question 16

Sphincter muscle of iris stimulated by ACH

Answer 16

contraction for miosis

Question 17

Ciliary muscle of eye stim by ACH

Answer 17

contraction for near vision,

Question 18

M3 receptors

Answer 18

Gq receptor in endothelium, not innervated, stim by AcH to produce NO synthase which diffuses to vascular smooth muscle and relaxes via cGMP. glands, smooth muscle (but not vasculature), endothelium

Question 19

Atropine

Answer 19

Muscarinic antagonist; alpha 1 agonist; mydriasis, increase TPR

Question 20

Echothiophate

Answer 20

Irreversible anticholinersterase inhibitor (organophosphate) rx glaucoma; can rescue within a couple of hours with 2PAM antidote which can remove inhibitor of enzyme

Question 21

Soman

Answer 21

Irreversible Anticholinesterase Inhibitor (organophosphate) chemical warfare

Question 22

Sarin

Answer 22

irreversible Anticholinesterase inhibitor warfare

Question 23

Parathion

Answer 23

organophosphate prodrug to Paraoxon (active insecticide)

Question 24

Malathion

Answer 24

organophosphate prodrug to malaoxon active insecticide

Question 25

Scopolamine

Answer 25

muscarinic antagonist, like atropine, works via competitive inhibition at receptor; also works for motion sickness

Question 26

Homatropine

Answer 26

muscarinnic antagonist in opthalmology

Question 27

Cyclopentolate

Answer 27

muscarinic antagonist in opthalmology

Question 28

Tropicamide

Answer 28

muscarinic antagonist in opthalmology

Question 29

Dycyclomine

Answer 29

competitive antagonism at M3; reduces smooth muscle and secretory activity of gut (irritable bowel, minor diarrhea)

Question 30

Ipratropium

Answer 30

competitive non selective antagonist at M receptor, reduces prevents bronchospasm

Question 31

Oxybutynin

Answer 31

slightly M 3 selective muscarinic antagonist; reduce detrusor smooth muscle tone, spasms

Question 32

Hexamethonium

Answer 32

Antagonise Nicotinic (ach) receptors so preganglionic in symp and para and symp to adrenal medulla

Question 33

Tetraethylammonium

Answer 33

antagonize Nn receptors

Question 34

Mecamylamine

Answer 34

antagonize Nn receptors, can cross BBB