Cholinomimetics

Question 1

Pilocarpine (Salagen) Class

Answer 1

Direct Acting non-ester

Question 2

Pilocarpine MOA

Answer 2

Direct acting muscarinic cholinomimetic

Question 3

Pilocarpine (Salagen) Treatments

Answer 3

Glaucoma

ACh activates sphincter and ciliary muscle constriction to increase drainage of aqueous humor and decrease IO pressure

Question 4

Pilocarpine (Salagen) Side Effects

Answer 4

SLUDGE

Question 5

Cevimeline (Evoxac) Class

Answer 5

Direct Acting non-ester

Question 6

Cevimeline (Evoxac) MOA

Answer 6

Direct acting muscarinic cholinomimetic

Question 7

Cevimeline (Evoxac) Treatments

Answer 7

Dry mouth (ex. Sjogen’s, post radiation therapy; via increased salivation)

Question 8

Nicotine (NRT) Class

Answer 8

Direct Acting non-ester

Question 9

Nicotine (NRT) MOA

Answer 9

Direct acting nicotinic cholinomimetic, reduces cravings

Question 10

Nicotine (NRT) Treatment

Answer 10

Smoking cessation

Question 11

Cevimeline (Evoxac) Side effects

Answer 11

SLUDGE

Question 12

Neostigmine Class

Answer 12

Indirect Acting

Question 13

Neostigmine MOA

Answer 13

AChE Inhibitor (Short Acting)

Question 14

Neostigmine Treatment

Answer 14

Post-operative and neurogenic ileus, urinary retention, myasthenia gravis (increasesmuscle strength for 0.5-2 hrs), reversal of neuromuscular blockade

Question 15

Donepezil (Aricept) Class

Answer 15

Indirect Acting non-ester

Question 16

Donepezil (Aricept) MOA

Answer 16

AChE Inhibitor

Question 17

Donepezil (Aricept) Treatment

Answer 17

Alzheimer’s (amplifies endogenous ACh in brain)

Question 18

Edrophonium (Enlon) Class

Answer 18

Indirect acting non-ester

Question 19

Edrophonium (Enlon) MOA

Answer 19

AChE inhibitor

Question 20

Edrophonium (Enlon) Treatment

Answer 20

Myasthenia gravis

Question 21

Direct Acting Cholinergic Agonists MOA

Answer 21

Bind directly to nicotinic or muscarinic cholinoreceptors. May be esters or non-esters of choline

Question 22

Physiologic effects of direct acting Cholinergic agonists

Answer 22

Decrease HR and CO
Decrease BP via vasodilation
Increase salivation, sweat, and lacrimal production
Stimulate intestinal secretions and motility
Increase bronchial secretions
Contract detrussor muscle of bladder
Pupilary constriction

Question 23

Primary clinical uses of direct acting cholinergic agonists

Answer 23

1. Diseases of the eye (Glaucoma)
2. Decreased secretions
3. GI and urinary tract disorders esp. post operative

Question 24

Indirect Acting Cholinergic Agonists MOA

Answer 24

Prolong the life of ACh in synapse by inhibiting ACHesterase. This increases the effect of ACh

Question 25

Pralidoxime PAM (Protopam) Class

Answer 25

Strong nucleophile

Question 26

Pralidoxime PAM (Protopam) MOA

Answer 26

Regenerates phosphorylated AChE

Question 27

Pralidoxime Treatment

Answer 27

Antidote to poisoning by nerve gas or insecticide

Question 28

Sarin Class

Answer 28

Indirect acting organophosphate

Question 29

Sarin MOA

Answer 29

AChE inhibitor

Question 30

Sarin Treatment

Answer 30

Volatile nerve gas

Question 31

Antidote to indirect acting cholinergic agonists

Answer 31

PAM and atropine

Question 32

Toxic effects of cholinergic receptor activating drugs

Answer 32

``` SLUDGE Salivation Lacrimation Urination Defecation GI Distress Emesis ```

Question 33

Antidote to direct acting cholinergic agonists

Answer 33

Atropine

Question 34

Muscarinic receptors that lead to excitation

Answer 34

M1, M3, M5

Question 35

Muscarinic receptors that lead to inhibition

Answer 35

M2, M4

Question 36

Location of M1 receptors

Answer 36

Gastric parietal cells

Question 37

Location of M2 receptors

Answer 37

Cardiac cells and smooth muscle

Question 38

Location of M3 receptors

Answer 38

bladder, exocrine glands, smooth muscle

Question 39

Location of nicotinic receptors

Answer 39

CNS, adrenal medulla, autonomic ganglia, NMJ

Question 40

Physostigmine (Esterine) Class

Answer 40

Indirect acting carbamate

Question 41

Physostigmine (Esterine) MOA

Answer 41

AChE inhibitor (short acting)

Question 42

Physostigmine (Esterine) Therapeutics

Answer 42

Glaucoma (ACh activates papillary sphincter and ciliary muscles of the eyes)

Question 43

Physostigmine (Esterine) SE

Answer 43

SLUDGE and general increase in cholinergic neurtotransmission, paralysis

Question 44

Direct acting cholimimetics MOA

Answer 44

Bind directly to cholinergic receptors

Question 45

Indirect acting cholimimetics MOA

Answer 45

Inhibit acetylchloinesterase, therefore ACh is not broken down in the synaptic cleft and more is available to send signals