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Pharmacology > VII - Cholinergic Pharmacology > Flashcards

VII - Cholinergic Pharmacology Flashcards

1
Q

Primary neurotransmitter in all autonomic ganglia and at the synapses between parasympathetic post-ganglionic neurons and their effector cells

A

acetylcholine

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2
Q

Primary neurotransmitter at the somatic (voluntary) skeletal muscle neuromuscular junction

A

acetylcholine

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3
Q

Steps in Cholinergic Stimulation

A

synthesis, storage, release, termination

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4
Q

Cholinergic Stimulation: Step 1

A

SYNTHESIS - ACh is synthesized from acetyl CoA and choline by the enzyme choline acyltransferase (ChAT)

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5
Q

Cholinergic Stimulation: choline transport is inhibited by

A

hemicholinium

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6
Q

Cholinergic Stimulation: Step 2

A

STORAGE - ACh is actively transported into vesicles for storage by vesicle-associated transporter (VAT)

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7
Q

Cholinergic Stimulation: ACh vesicle storage is inhibited by

A

vesamicol

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8
Q

Cholinergic Stimulation: Step 3

A

RELEASE - entry of Ca triggers interaction among SNARE proteins (VAMPs, SNAPs)

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9
Q

Cholinergic Stimulation: alters synaptobrevins to prevent release of ACh

A

botulinum toxin

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10
Q

Cholinergic Stimulation: Step 4

A

TERMINATION - degradation of ACh into choline and acetate by acetylcholinesterase

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11
Q

Cholinergic Stimulation: inhibits acetylcholinesterase

A

Indirect-Acting Cholinomimetics: neostigmine, carbamates, organophosphates

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12
Q

Cholinergic drugs are not very useful for systemic therapy because

A

their effects are not sufficiently selective

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13
Q

Cholinoreceptors: nerve endings, Gq-coupled, increase IP3, DAG cascade

A

M1

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14
Q

Cholinoreceptors: heart, some nerve endings, Gi-coupled, decrease cAMP, activates K+ channels

A

M2

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15
Q

Cholinoreceptors: effector cells of smooth muscles, glands and endothelium, Gq-coupled, increase IP3, DAG cascade

A

M3

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16
Q

Cholinoreceptors: ANS ganglia, ion channel, depolarizes, action potential

A

Nn

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17
Q

Cholinoreceptors: neuromuscular end-plate, ion channel, depolarizes, action potential

A

Nm

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18
Q

Betanechol: Class

A

cholinomimetic - direct-acting, muscarinic

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19
Q

Betanechol: MOA

A

activates M3

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20
Q

Betanechol: Uses

A

bladder and bowel atony (post-op, spinal cord injury)

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21
Q

Betanechol: Side Effects

A

cyclospasm, diarrhea, urinary urgency, vasodilation, reflex tachycardia, sweating

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22
Q

Pilocarpine: Class

A

cholinomimetic - direct-acting, muscarinic

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23
Q

Pilocarpine: MOA

A

activates M3 in ciliary muscle (inc. aqueous humor outflow) and salivary glands (inc. salivation)

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24
Q

Pilocarpine: Uses

A

glaucoma, Sjorgen syndrome, Sicca syndrome

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25
Q

Pilocarpine: Side Effects

A

miosis, BOV (cyclospasm)

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26
Q

Nicotine: Similar Drug

A

Varenicline

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27
Q

Nicotine: Class

A

cholinomimetic - direct-acting, nicotinic

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28
Q

Nicotine: MOA

A

activates Nn and Nm

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29
Q

Nicotine: Uses

A

smoking cessation

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30
Q

Nicotine: Side Effects

A

generalized ganglionic stimulation: hypertension, tachycardia, nausea, vomiting, diarrhea

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31
Q

Nicotine: Overdose

A

convulsions, paralysis, coma

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32
Q

CNS stimulation, miosis, spasm of accomodation, bronchocostriction, excessive GIT/GUT smooth muscle activity, increased secretory activity, vasodilation

A

Muscarinic Toxicity

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33
Q

Muscarine and similar alkaloids are found in these mushrooms

A

Inocybe, Amanita muscaria

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34
Q

Symptoms of Mushroom Poisoning

A

nausea, vomiting, diarrhea

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35
Q

ganglionic stimulation, blockade of neuromuscular end-plate depolarization (fasciculations, paralysis), CNS toxicity (convulsions, CNS depression)

A

Nicotinic Toxicity

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36
Q

Bind to cholinesterase and undergo hydrolysis releasing the alcohol portion

A

Indirect-Acting Cholinomimetics

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37
Q

The _____ portion of indirect-acting cholinomimetics is retained and slowly released to prevent binding and hydrolysis of endogenous acetylcholine which amplifies ACh effects.

A

acidic portion

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38
Q

Edrophonium: Class

A

cholinomimetic - indirect-acting

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39
Q

Edrophonium: MOA

A

inhibits acetylcholinesterase, amplifies endogenously released ACh

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40
Q

Edrophonium: Uses

A

diagnosis of Myasthenia Gravis (Tensilon Test), differentiation of cholinergic crisis and myasthenic crisis

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41
Q

Side Effects: miosis, salivation, nausea, vomiting, diarrhea, bradycardia

A

Edrophonium, Neostigmine, Rivastigmine

42
Q

Edrophonium: IV

A

very short-acting

43
Q

Neostigmine: Similar Drugs

A

pyridostigmine, physostigmine

44
Q

Neostigmine: Class

A

cholinomimetic - indirect-acting

45
Q

Neostigmine: MOA

A

inhibits acetylcholinesterase, amplifies endogenously released ACh

46
Q

Neostigmine: Uses

A

treatment of Myasthenia Gravis, reversal of non-depolarizing neuromuscular blockade, Ogilvie syndrome, glaucoma (physostigmine)

47
Q

Side Effects: miosis, salivation, nausea, vomiting, diarrhea, bradycardia

A

Edrophonium, Neostigmine, Rivastigmine

48
Q

Neostigmine: muscarinic effects are blocked by

A

Atropine

49
Q

Autoimmune destruction of nicotinic ACh receptors, fluctuating muscle, weakness, ocular symptoms, bulbar symptoms, proximal muscle weakness

A

Myasthenia Gravis

50
Q

Myasthenia Gravis: acute worsening of symptoms due to infection, stress or undermedication

A

myasthenic crisis

51
Q

Myasthenia Gravis: excessive activation of cholinoreceptors, skeletal muscle weakness, parasympathetic signs due to overmedication

A

cholinergic crisis

52
Q

Edrophonium _____ muscle strength in myasthenic crisis.

A

improves

53
Q

Edrophonium _____ muscle strength in cholinergic crisis.

A

weakens

54
Q

Rivastigmine: Similar Drugs

A

galantamine, donepezil, tacrine

55
Q

Rivastigmine: Class

A

cholinomimetic - indirect-acting

56
Q

Rivastigmine: MOA

A

inhibits acetylcholinesterase, amplifies endogenously released ACh

57
Q

Rivastigmine: Uses

A

Alzheimer’s Disease

58
Q

Side Effects: miosis, salivation, nausea, vomiting, diarrhea, bradycardia

A

Edrophonium, Neostigmine, Rivastigmine

59
Q

Organophosphate Poisoning Symptoms

A

diarrhea, urination, miosis, bronchospasm, bradycardia, excitation (skeletal muscle, CNS), lacrimation, sweating, salivation

60
Q

Atropine: Class

A

cholinergic antagonist - muscarinic

61
Q

Atropine: MOA

A

competitively blocks all muscarinic receptors

62
Q

Atropine: Uses

A

antidote for organophosphate poisoning (first choice), mydriatic, cycloplegic, bradycardia, hypersalivation

63
Q

Side Effects: tachycardia, mydriasis, cycloplegia, skin flushing, delirium, hallucinations

A

Atropine

64
Q

Atropine: No effect on _____ of organophosphate toxicity

A

nicotinic signs

65
Q

Pralidoxime: Class

A

cholinesterase regenerator, antidote

66
Q

Pralidoxime: MOA

A

binds with phosphorus of organophosphate, breaks organophosphate bond with cholinesterase

67
Q

Pralidoxime: Uses

A

antidote for organophosphate poisoning and nerve gas poisoning (sarin, tabun)

68
Q

Pralidoxime: Side Effects

A

muscle weakness

69
Q

Pralidoxime: Administration

A

must be administered before 6-8 hours of organophasphate bond with cholinesterase occurs

70
Q

Prototype non-selective muscarinic blocker, found in Atropa belladonna, tertiary amine that readily crosses membrane barriers

A

Atropine

71
Q

Atropine: Similar Drugs

A

homatropine, cyclopentolate, tropicamide

72
Q

Benztropine: Similar Drugs

A

biperiden, trihexyphenidyl

73
Q

Benztropine: Class

A

cholinergic antagonist - muscarinic

74
Q

Benztropine: MOA

A

competitively blocks all muscarinic receptors, restores neurotransmitter balance in the basal ganglia

75
Q

Benztropine: Uses

A

Parkinson’s Disease

76
Q

Benztropine: Side Effects

A

BOV, dry eyes, constipation, dry mouth, urinary retention

77
Q

Benztropine: Reduces _____ more than bradykinesis or rigidity

A

tremors

78
Q

Muscarinic Antagonists for Parkinsonism

A

trihexyphenidyl, benztropine, biperiden

79
Q

Ipratropium: Similar Drugs

A

tiotropium

80
Q

Ipratropium: Class

A

cholinergic antagonist - muscarinic

81
Q

Ipratropium: MOA

A

blocks muscarinic receptors in bronchial smooth muscle, prevents vagal-stimulated bronchoconstriction

82
Q

Ipratropium: Uses

A

asthma, COPD

83
Q

Ipratropium: Side Effects

A

dry mouth, cough, nasal dryness

84
Q

Ipratropium: More effective and less toxic than _____ in patients with COPD and heart disease

A

beta-agonists

85
Q

Preferred bronchodilator in patients with COPD and heart disease, less likely to cause tachycardia and cardiac arrythmias

A

Ipratropium

86
Q

Scopolamine: Class

A

cholinergic antagonist - muscarinic

87
Q

Scopolamine: MOA

A

competitively blocks all muscarinic receptors, antagonizes histamine and serotonin

88
Q

Scopolamine: Uses

A

motion sickness

89
Q

Scopolamine: Side Effects

A

drowsiness, BOV, dry eyes, constipation, dry mouth, urinary retention

90
Q

Scopolamine: Application

A

transdermal patch

91
Q

Hyperthermia, cutaneous vasodilation, decreased secretions, tachycardia, intraventricular conduction block, constipation, BOV, CNS toxicity

A

Atropine Toxicity - HOT as a hare, DRY as a bone, RED as a beet, BLIND as a bat, MAD as a hatter

92
Q

Contraindications for Muscarine Blockers

A

infants, hyperthermia (decreased sweating), acute angle closure glaucoma, benign prostatic hyperplasia

93
Q

Competitive pharmacologic antagonists at nicotinic ACh receptors, first successful agents for HPN, adverse blockade

A

Ganglion Blockers

94
Q

Hexamethonium: Similar Drugs

A

trimethaphan

95
Q

Hexamethonium: Class

A

cholinergic antagonist - nicotinic

96
Q

Hexamethonium: MOA

A

competitively blocks Nn nicotinic ACh receptors

97
Q

Hexamethonium: Uses

A

hypertension (obsolete), hypertensive emergencies

98
Q

Hexamethonium: Side Effects

A

postural hypotension, dry mouth, BOV, constipation, sexual dysfunction

99
Q

Important for producing complete skeletal muscle relaxation in surgery

A

Neuromuscular Blockers

100
Q

Neuromuscular Blockers: Non-Depolarizing

A

tubocurarine, pancuronium, atracurium, vecuronium

101
Q

Neuromuscular Blockers: Depolarizing

A

succinylcholine

Pharmacology (34 decks)

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