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Abbey pharm shelf/step > pharmacology: cholinergic drugs > Flashcards

pharmacology: cholinergic drugs Flashcards

1
Q

where are M2 receptors? what is their mechanism?

A

SA and AV node

Gi coupled; decreased cAMP

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2
Q

where are the M1 receptors? M3 receptors? what is their mechanism?

A

M1: glands in the GI tract
M3: everywhere else essentially
Gq coupled: increased phospholipase C –> increased IP3, DAG, and Ca2+

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3
Q

botulinum toxin mechanism

A

interacts with synpatobrevin and other proteins to prevent ACh release - used in blepharospasm, strabismus/hyperhydrosis, dystonia, cosmetics

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4
Q

what has no innervation but has M3 receptors? what are the implications of this?

A

blood vessels - M3 leads to NO release (vasodilation)

means there will be no effects of indirect agonists

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5
Q

what are the muscarinic agonists?

A

Ach, bethanechol, methacholine, pilocarpine

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6
Q

Ach clinical uses

A

short half-life so no clinical use

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7
Q

bethanechol clnical use

A

ileus (postop/neurogenic), urinary retention

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8
Q

methacholine clinical uses

A

diagnositic procedure - bronchial hyperreactivity

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9
Q

pilocarpine use

A

topically used for glaucoma, xerostomia

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10
Q

what receptors can cause flaccid paralysis?

A

NN and NM because desensitized very quickly

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11
Q

NN and NM mechanisms

A

activation (opening) of Na/K channels

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12
Q

what are the indirect-acting cholinomimetics?

A

acetylcholinesterase inhibitors:
edrophonium, physostigmine, neostigmine, pyridostigmine, donepezil, organophosphates (echothiphate, malathion, parathion)

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13
Q

edrophonium: characteristics and clinical uses

A

characteristics : short acting

clinical uses: diagnose myasthenia and used to differentiate myasthenia from cholinergic crisis (desensitization)

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14
Q

physostigmine: characteristics and clinical uses

A

characteristics: tertiary amine (enters CNS)

clinical uses: glaucoma, antidote in atropine overdose

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15
Q

neostigmine and pyridostigmine: characteristics and clinical uses

A

characteristics: quaternary amines (no CNS entry)

clinical uses: ileus, urinary retention, myasthenia, reversal of nondepolarizing NM blockers

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16
Q

donepezil: characteristics and clinical uses

A

characteristics: lipid soluble (CNS entry) - oral form!!

clinical uses: alzheimer’s

17
Q

organophosphates (echothiophate, malathion, parathion, sarin): characteristics and clinical uses

A

characteristics: lipid-soluble, IRREVERSIBLE INHIBITORS (non competitive)
clinical uses: glaucoma (echothiophate eyedrops)
insecticides (malathion, parathion), nerve gas (sarin)

18
Q

where can acetylcholinesterase inhibitors NOT be used?

A

blood vessels

19
Q

acute toxicity of AChE inhibitors

A

excessive muscarinic and nicotinic stimulations
muscarinic effects: diarrhea, urination, miosis (pinpoint pupil), bradycardia, bronchoconstriction, lacrimation, salivation, sweating, CNS stimulation
nicotinic effects: skeletal muscle excitation followed by paralysis (cholinergic crisis), CNS stimulation

20
Q

management of AChE inhibitors

A

atropine (muscarinic blocker); regeneration of AChE: pralidoxime (2-PAM)

21
Q

chronic toxicity of AChE inhibitors

A

peripheral neuropathy causing muscle weakness and sensory loss d/t demyelination not due to AChE inhibitors (no treatment)

22
Q

what are the muscarinic receptor antagonists?

A

atropine, tropicamide, ipratropium, triotropium, scopolamine, benztropine, trihexyphenidyl

23
Q

atropine: characteristics and clinical uses

A

characteristics: tertiary amine (enters CNS)
clinical uses: antispasmodic, antisecretory, management of AChE inhibitors overdose, antidiarrheal, ophthalmology (long action)

24
Q

pharmacologic effects of atropine

A

decreased secretions, mydriasis, cycloplegia, hyperthermia, tachycardia, sedation, urinary retention and constipation, excitation and hallucinations (mimics alzheimer’s)

25
Q

what are classes of drugs with antimuscarinic pharmacology

A

antihistamines, tricyclic antidepressants, antipsychotics, quinidine, amantadine, meperidine

26
Q

what is used for treatment of acute intoxication of antimuscarinics

A

physostigmine

27
Q

tropicamide clinical uses

A

ophthalmology (topical)

28
Q

ipratropium and tiotropium clinical uses

A

asthma and COPD (inhalational) - no CNS entry, no change in mucus viscosity (decreased secretions)

29
Q

scopolamine clinical uses

A

used in motion sickness, causes sedation and short-term memory block (affects CN8 most)

30
Q

benztropine and trihexyphenidyl clinical uses

A

lipid-soluble (CNS entry) used in parkinsonism and in acute extrapyramidal symptoms induced by antipsychotics

31
Q

what are the ganglion blocking agents (nicotinic recptor antagonists)

A

hexamethonium and mecamylamine (preduce the predominant autonomic tone) –> prevent baroreceptor reflex changes

Abbey pharm shelf/step (23 decks)

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