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PLE Reviewer - PHARMACOLOGY > Cholinoceptor-activating & Cholinesterase-inhibiting Drugs (Cholinomimetics) > Flashcards

Cholinoceptor-activating & Cholinesterase-inhibiting Drugs (Cholinomimetics) Flashcards

1
Q

Class: cholinomimemtic, direct-acting, muscarinic

MOA: activates M1-M3 receptors only

Uses: bower/bladder atony (post-surgical/post-SCI)

SE: cyclospasm (false-nearsightedness), diarrhea, urinary urgency, vasodilaion, reflex tachycardia, sweating, cholinergic symptoms

Similar:
CARBACHOL - acts on BOTH M and N receptors

A

BETANECHOL

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2
Q

Class: cholinomimemtic, direct-acting, muscarinic

MOA: activates M3 receptor only - in ciliary muscle (increasing aqueous outflow) and salivary glands (increasing salivation)

Uses: glaucoma, Sjogren syndrome, sicca syndrome

SE: miosis (pupillary constriction), cyclospasm (false-nearsightedness)

Similar:
CEVIMELINE - M3-selective

A

PILOCARPINE

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3
Q

Class: cholinomimemtic, direct-acting, nicotinic

MOA: activates Nn and Nm receptors

Uses: smoking cessation

SE: generalized ganglionic stimulation - hypertension, tachycardia, nausea, vomiting, diarrhea; overdose leads to convulsions, paralysis, coma

Similar:
VARENICLINE

A

NICOTINE

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4
Q

Class: cholinomimemtic, indirect-acting, alcohol

MOA: inhibits acetylcholinesterase, amplifies endogenously-released Ach

Uses: myasthenia gravis (diagnostic via Tensilon test), differentiation of cholinergic crisis and myasthenic crisis (weakens muscle strength in cholinergic, strengthens muscle in myasthenic)

SE: miosis, salivation, nausea, vomiting, diarrhea, bradycardia; VERY SHORT-ACTING via IV

A

EDROPHONIUM

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5
Q

Class: cholinomimemtic, indirect-acting, carbamate

MOA: inhibits acetylcholinesterase, amplifies endogenously-released Ach

Uses: myasthenia gravis (treatment), reversal of non-depolarizing neuromuscular blockade

SE: miosis, salivation, nausea, vomiting, diarrhea, bradycardia; muscarinic effects blocked by ATROPINE

Similar:
PYRIDOSTIGMINE- carbamate
PHYSOSTIGMINE - carbamate, glaucoma Tx
AMBENONIUM - carbamate
DEMECARIUM - carbamate, glaucoma Tx
ECHOTHIOPHATE - organophosphate, glaucoma Tx
MALATHION - organophosphate, insecticide
PARATHION - organophosphate, insecticide
SARIN - organophosphate, nerve gas
TABUN - organophosphate, nerve gas
SOMAN - organophosphate, nerve gas
A

NEOSTIGMINE

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6
Q

Class: cholinomimemtic, indirect-acting, carbamate

MOA: inhibits acetylcholinesterase, amplifies endogenously-released Ach

Uses: Alzheimer’s disease (TRANSDERMAL PATCH)

SE: miosis, salivation, nausea, vomiting, diarrhea, bradycardia

Similar:
GALANTAMINE
DONEPEZIL
TACRINE

A

RIVASTIGMINE

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7
Q

Class: cholinergic antagonist (antimuscarinic) (prototype)

MOA: completely blocks all M receptors

Uses: FIRST CHOICE antidote for organophosphate poisoning, mydriatic, cyclopegic, bradycardia, hypersalivation (decrease airway secretion during anesthesia)

SE: tachycardia, mydriasis, cyclopegia, skin flushing, delirium, hallucinations, urinary retention, constipation; NO EFFECT on nicotinic toxicity, notorious for causing hyperthermia

Similar:
HOMATROPINE
CYCLOPENTOLATE
TROPICAMIDE

A

ATROPINE

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8
Q

Class: cholinesterase regenerator

MOA: binds P or organophosphate, breaks organophosphate bond with cholinesterase

Uses: antidote for organophosphate poisoning (including nerve gas poisoning - SARIN, TABUN)

SE: muscle weakness, MUST BE ADMINISTERED 6-8 HOURS BEFORE organophosphate bond with cholinesterase

A

PRALIDOXIME

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9
Q

The autoimmune destruction of NICOTINIC ACh receptors, characterized by:

  • fluctuating muscle weakness
  • ocular symptoms
  • bulbar symptoms
  • proximal muscle weakness
A

myasthenia gravis

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10
Q

Myasthenic crisis or cholinergic crisis?

  • acute worsening of muscle weakness symptoms due to infection, stress, or UNDERmedication
  • IMPROVES with EDROPHONIUM
A

myasthenic crisis

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11
Q

Myasthenic crisis or cholinergic crisis?

  • excessive activation of cholinoceptors causing skeletal muscle weakness and parasympathetic signs due to OVERmedication
  • WORSENS with EDROPHONIUM
A

cholinergic crisis

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12
Q

Muscarinic toxicity or nicotinic toxicity?

  • diarrhea
  • urination
  • miosis
  • bronchospasm, bronchorrhea
  • bradycardia
  • emesis
  • lacrimation
  • salivation
  • sweating
  • excitation (skeletal muscle and CNS)
A

muscarinic toxicity (also organophosphate poisoning)

mnemonic: DUMBBELSS

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13
Q

Muscarinic toxicity or nicotinic toxicity?

  • ganglionic stimulation (hypertension, tachycardia, nausea, vomiting, diarrhea)
  • neuromuscular end-plate depolarization block (fasciculations, paralysis)
  • CNS toxicity (convulsions) followed by CNS depression
A

nicotinic toxicity

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PLE Reviewer - PHARMACOLOGY (6 decks)

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