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

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

Flashcards in Cholinoceptor-activating & Cholinesterase-inhibiting Drugs (Cholinomimetics) Deck (13):
1

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

BETANECHOL

2

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

PILOCARPINE

3

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

NICOTINE

4

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

EDROPHONIUM

5

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

NEOSTIGMINE

6

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

RIVASTIGMINE

7

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

ATROPINE

8

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

PRALIDOXIME

9

The autoimmune destruction of NICOTINIC ACh receptors, characterized by:
- fluctuating muscle weakness
- ocular symptoms
- bulbar symptoms
- proximal muscle weakness

myasthenia gravis

10

Myasthenic crisis or cholinergic crisis?
- acute worsening of muscle weakness symptoms due to infection, stress, or UNDERmedication
- IMPROVES with EDROPHONIUM

myasthenic crisis

11

Myasthenic crisis or cholinergic crisis?
- excessive activation of cholinoceptors causing skeletal muscle weakness and parasympathetic signs due to OVERmedication
- WORSENS with EDROPHONIUM

cholinergic crisis

12

Muscarinic toxicity or nicotinic toxicity?
- diarrhea
- urination
- miosis
- bronchospasm, bronchorrhea
- bradycardia
- emesis
- lacrimation
- salivation
- sweating
- excitation (skeletal muscle and CNS)

muscarinic toxicity (also organophosphate poisoning)

mnemonic: DUMBBELSS

13

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

nicotinic toxicity