Cholinergic Agonists · Pharmacology

Why is Acetylcholine itself rarely used as a systemic therapeutic agent?

  1. It produces excessive stimulation of nicotinic receptors in skeletal muscle
  2. It has a very short half-life due to rapid hydrolysis by cholinesterases
  3. It binds only to nicotinic receptors and not to muscarinic ones
  4. It is destroyed by gastric acid before absorption occurs
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Correct answer: It has a very short half-life due to rapid hydrolysis by cholinesterases

Acetylcholine is rapidly degraded by both acetylcholinesterase and pseudocholinesterase in the blood. Consequently, its duration of action is measured in seconds, and it lacks the selectivity required for systemic therapy.

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