DRUG SUMMARY TABLE: Cholinoceptor-Activating & Cholinesterase-Inhibiting Drugs.

Clinical and Other

Subclass Mechanism of Action Applications Pharmacokinetics Toxicities, Interactions

Direct-acting, muscarinic agonists

Bethanechol Activates muscarinic (M) receptors Bladder and bowel atony, for Oral, IM activity All parasympathomimetic effects: cyclo-
3 and DAG example, after surgery or spinal Poor lipid solubility: does not spasm, diarrhea, urinary urgency, plus
cord injury enter CNS vasodilation, reflex tachycardia, and
Duration: 0.3–2 h sweating
Pilocarpine - Sjögren’s syndrome (increases Oral, IM activity Similar to bethanechol but may cause
vate EPSP via M receptors in ganglia Good lipid solubility, topical vasoconstriction via ganglionic effect
(causes miosis, cyclospasm) activity in eye
Muscarine Same as bethanechol Alkaloid found in mushrooms Low lipid solubility but readily Mushroom poisoning of fast-onset type
absorbed from gut

Direct-acting, nicotinic agonists

Nicotine Smoking cessation (also used as High lipid solubility, absorbed by Generalized ganglionic stimulation: hyper-
opens Na+-K+ channels in ganglia and insecticide) all routes tension, tachycardia, nausea, vomiting,
neuromuscular end plates diarrhea
Major overdose: convulsions, paralysis,
used as gum or transdermal patch coma
Duration: 4–6 h
Varenicline A partial agonist at N receptors Smoking cessation High lipid solubility, oral activity Hypertension, sweating, sensory dis-
turbance, diarrhea, polyuria, menstrual
disturbance
Succinylcholine N-receptor agonist, moderately Muscle relaxation Highly polar, used IV Initial muscle spasms and postoperative pain
selective for neuromuscular end (see Chapter 27)
plate (NM receptors) butyrylcholinesterase

Indirect-acting, alcohol
Edrophonium Reversal of NM block by nondepo- Increased parasympathetic effects, espe-
of endogenously released Ach - 5–10 min cially nausea, vomiting, diarrhea, urinary
thenia gravis urgency

Indirect-acting, carbamates
Neostigmine Like edrophonium plus small direct Reversal of NM block, treatment of Moderately polar but orally active Like edrophonium but longer duration
nicotinic agonist action myasthenia
Pyridostigmine Like edrophonium Treatment of myasthenia Moderately polar but orally active Like edrophonium but longer duration

Physostigmine Like edrophonium Reversal of severe atropine poison- - Like edrophonium but longer duration
plus CNS effects: seizures
glaucoma (topical)

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DRUG SUMMARY TABLE: Cholinoceptor-Activating & Cholinesterase-Inhibiting Drugs. (Continued )

Clinical and Other
Subclass Mechanism of Action Applications Pharmacokinetics Toxicities, Interactions

Indirect-acting, organophosphates
Parathion Like edrophonium Insecticide only Highly lipid-soluble
Duration: days to weeks all parasympathetic effects plus muscle
paralysis and coma
Malathion Like edrophonium Insecticide and scabicide (topical) Highly lipid-soluble but metabo- Much safer insecticide than parathion
Duration: days lized to inactive products in mam-
mals and birds
Sarin, tabun, others Like parathion Like parathion but more rapid Rapidly lethal
action

Indirect-acting, for Alzheimer’s disease

Rivastigmine, Cholinesterase inhibition plus vari- Alzheimer’s disease Nausea, vomiting
galantamine, done- able other poorly understood effects 1.5–70 h
pezil; tacrine is
obsolete

ACh, acetylcholine; DAG, diacylglycerol; EPSP, excitatory postsynaptic potential; IP 3 , inositol-1,4,5-trisphosphate.

② Med Notes (www.mednotes.in)

* Revision Notes med notes site
company
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