Cholinomimetics Flashcards

1
Q

Pilocarpine (Salagen) Class

A

Direct Acting non-ester

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2
Q

Pilocarpine MOA

A

Direct acting muscarinic cholinomimetic

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3
Q

Pilocarpine (Salagen) Treatments

A

Glaucoma

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

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4
Q

Pilocarpine (Salagen) Side Effects

A

SLUDGE

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5
Q

Cevimeline (Evoxac) Class

A

Direct Acting non-ester

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6
Q

Cevimeline (Evoxac) MOA

A

Direct acting muscarinic cholinomimetic

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7
Q

Cevimeline (Evoxac) Treatments

A

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

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8
Q

Nicotine (NRT) Class

A

Direct Acting non-ester

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9
Q

Nicotine (NRT) MOA

A

Direct acting nicotinic cholinomimetic, reduces cravings

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10
Q

Nicotine (NRT) Treatment

A

Smoking cessation

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11
Q

Cevimeline (Evoxac) Side effects

A

SLUDGE

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12
Q

Neostigmine Class

A

Indirect Acting

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13
Q

Neostigmine MOA

A

AChE Inhibitor (Short Acting)

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14
Q

Neostigmine Treatment

A

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

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15
Q

Donepezil (Aricept) Class

A

Indirect Acting non-ester

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16
Q

Donepezil (Aricept) MOA

A

AChE Inhibitor

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17
Q

Donepezil (Aricept) Treatment

A

Alzheimer’s (amplifies endogenous ACh in brain)

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18
Q

Edrophonium (Enlon) Class

A

Indirect acting non-ester

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19
Q

Edrophonium (Enlon) MOA

A

AChE inhibitor

20
Q

Edrophonium (Enlon) Treatment

A

Myasthenia gravis

21
Q

Direct Acting Cholinergic Agonists MOA

A

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

22
Q

Physiologic effects of direct acting Cholinergic agonists

A

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

23
Q

Primary clinical uses of direct acting cholinergic agonists

A
  1. Diseases of the eye (Glaucoma)
  2. Decreased secretions
  3. GI and urinary tract disorders esp. post operative
24
Q

Indirect Acting Cholinergic Agonists MOA

A

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

25
Q

Pralidoxime PAM (Protopam) Class

A

Strong nucleophile

26
Q

Pralidoxime PAM (Protopam) MOA

A

Regenerates phosphorylated AChE

27
Q

Pralidoxime Treatment

A

Antidote to poisoning by nerve gas or insecticide

28
Q

Sarin Class

A

Indirect acting organophosphate

29
Q

Sarin MOA

A

AChE inhibitor

30
Q

Sarin Treatment

A

Volatile nerve gas

31
Q

Antidote to indirect acting cholinergic agonists

A

PAM and atropine

32
Q

Toxic effects of cholinergic receptor activating drugs

A
SLUDGE
Salivation
Lacrimation
Urination
Defecation
GI Distress
Emesis
33
Q

Antidote to direct acting cholinergic agonists

A

Atropine

34
Q

Muscarinic receptors that lead to excitation

A

M1, M3, M5

35
Q

Muscarinic receptors that lead to inhibition

A

M2, M4

36
Q

Location of M1 receptors

A

Gastric parietal cells

37
Q

Location of M2 receptors

A

Cardiac cells and smooth muscle

38
Q

Location of M3 receptors

A

bladder, exocrine glands, smooth muscle

39
Q

Location of nicotinic receptors

A

CNS, adrenal medulla, autonomic ganglia, NMJ

40
Q

Physostigmine (Esterine) Class

A

Indirect acting carbamate

41
Q

Physostigmine (Esterine) MOA

A

AChE inhibitor (short acting)

42
Q

Physostigmine (Esterine) Therapeutics

A

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

43
Q

Physostigmine (Esterine) SE

A

SLUDGE and general increase in cholinergic neurtotransmission, paralysis

44
Q

Direct acting cholimimetics MOA

A

Bind directly to cholinergic receptors

45
Q

Indirect acting cholimimetics MOA

A

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