Cholinergic Agonists and Antagonists

Question 1

Acetycholine

Answer 1

Direct acting cholinomimetic

Question 2

Bethanechol

Answer 2

direct acting cholinomimetic

Question 3

Carbachol

Answer 3

direct acting cholinomimetic

Question 4

Civemeline

Answer 4

direct acting cholinomimetic

Question 5

Methacholine

Answer 5

direct acting cholinomimetic

Question 6

Pliocarpine

Answer 6

direct acting cholinomimetic

Question 7

Varenicline (Chantix)

Answer 7

direct acting cholinomimetic

Question 8

Ambenonium

Answer 8

Cholinisterase inhibitor

Question 9

Donepezil

Answer 9

Cholinesterase inhibitor

Question 10

Echothiophate

Answer 10

Cholinesterase inhibitor

Question 11

Edrophonium

Answer 11

Cholinesterase inhibitor

Question 12

Galantamine

Answer 12

Cholinesterase inhibitor

Question 13

Neostimine

Answer 13

Cholinesterase inhibitor

Question 14

Physostigmine

Answer 14

Cholinesterase inhibitor

Question 15

Pyridostigmine

Answer 15

Cholinesterase inhibitor

Question 16

Rivastimine

Answer 16

Cholinesterase inhibitor

Question 17

Tacrine

Answer 17

Cholinesterase inhibitor

Question 18

Pralidoxime

Answer 18

Cholinesterase regenerator

Question 19

Antimuscarinic drugs used for motion sickness

Answer 19

Scopolamine

Question 20

Antimuscarinic drugs for GI disorders

Answer 20

Atropine
Dicyclomine
Glycopyrrolate
Hyoscyamine

Question 21

Antimuscarinic drugs used in ophthamology

Answer 21

Atropine
Cyclopentolate
Homatopine
Scopolamine
Tropicamide

Question 22

Antimuscarinic drugs used for respiratory disorders (asthma, COPD)

Answer 22

Ipratropium

Tiotropium

Question 23

Antimuscarinic drugs used for urinary disorders

Answer 23

Darifenacin
Fesoterodine
Oxybutynin
SOlifenacin
Tolterodine
Trospium

Question 24

Antimuscarinic drugs used for cholinergic poisoning

Answer 24

Atropine (+ pralidoxime)

Question 25

Antimuscarinic Drugs used for movement disorders

Answer 25

``` Benztropine Biperiden Orphenadrine Procyclidine Trihexyphenidyl ```

Question 26

Ganglion blockers

Answer 26

Mecamylamine

Question 27

Choline esters and alkaloids are what type of drugs

Answer 27

Direct acting cholinergic agonists

Question 28

Choline esters MOA

Answer 28

Act as agonists on cholinergic receptors

Question 29

Choline esters eg

Answer 29

acetylcholine | carbachol, bethanechol

Question 30

Choline esters absorption, distribution and metabolism

Answer 30

permanently charged quartenary ammonium groups that result in poor absorption and distribution into the CNS Hydrolyzed in the GI tract, less active when given by mouth Hydrolysed by cholinesterase but at different rates --> varrying durations of action

Question 31

Alkaloid MOA

Answer 31

acts as agonist on cholinergic receptors

Question 32

Alkaloids eg

Answer 32

muscarine, nicotine, pliocarpine

Question 33

Hydrolyzation speeds of choline esters by cholinesterase

Answer 33

most rapid: acetylcholine > methacholine> carbachol=bethanechol : least rapid

Question 34

Alkaloids absorption, distribution and metabolism

Answer 34

uncharge tertiary amines (muscarine is an exception). well absorbed from most sites of administration muscarine is a quartenary amine, is highly toxic when ingested, and can enter the brain (musrooms) Cheifly excreted by the kidneys; acidification of the urine accelerates clearance.

Question 35

M1, M3, M5

Answer 35

Gq, stimulatory, Ip3 DAG cascade Nerves (M1) Glands, smooth muscle, endothelium, (M3) CNS (M5)

Question 36

M2, M4

Answer 36

Gi, inhibitory, inhibition of cAMP production (activation of K+ch in M2) M2 - heart, nerves, smooth muscle M4 - CNS

Question 37

Nicotinic receptors

Answer 37

Nm - skeletal NMJ Nn - postganglionic cell body, dendrites, cns Na, K depolarizing ion channel

Question 38

``` Organ system effects of the direct acting cholinergic agonists Skeletal muscle (somatic effects) ```

Answer 38

only nACHRs ar on skeletal muscle, so only those agents that activate nACHR will produce any effect (muscle contraction) Prolonged agonist occupancy of the nACHr abolishes the effector response: the postganglionic neuron stops firing and the skeletal muscle cell relaxes (similar to succiylcholine) Eventually a state of depolarizing blockade is produced (flaccid paralysis) Nicotine itself has a greater affinity for neuronal nACHRs than skeltal muscle nACHRs

Question 39

Organ system effects of the direct acting cholinergic agonists Eye

Answer 39

Contraction of iris sphincter and ciliary muscle --> increased aqueous humor outflow into canal of Schlemm

Question 40

Organ system effects of the direct acting cholinergic agonists Cardiovascular system

Answer 40

M2 mACHR | reduction in peripheral vascular resistance and changes in HR