CNS - Cholinergics A ntagonists - INTRO - Ganglionic Blockers

9 important questions on CNS - Cholinergics A ntagonists - INTRO - Ganglionic Blockers

What are examples of non-depolarizing competitive receptor blockers?

Examples include Tetra-ethyl ammonium, (Etamon), Trimethaphan camsylate (Arfonad), Mecamylamine, and Pentolinium. These are types of ganglionic blockers.

What do presynaptic ganglion blockers do?

Presynaptic ganglion blockers block the synthesis and/or release of Ach. Drugs like Hemicholine and Tri-ethylcholine block the synthesis of Ach and compete with the choline uptake process.

What type of drugs are Methonium compounds and Hexamethonium?

Methonium compounds and Hexamethonium are non-depolarizing non-competitive ion channel blocking drugs that block receptors associated ion channels.
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What do they block in therapeutic uses?

Cholinergic responses mediated by nicotinic acetylcholine receptors (nAchRs) are blocked. Nicotinic acetylcholine receptors are found on skeletal muscle. Used less frequently now due to antihypertensive drugs.

What is the mechanism of action for postsynaptic ganglion blockers?

Postsynaptic ganglion blockers are nicotinic receptor antagonists. They cause rapid desensitization of nicotinic ACh receptors and spontaneous closure of Na+ channels in sympathetic and parasympathetic ganglia.

Why are ganglionic blockers not used in clinical practice?

They are not used in clinical practice because of non-specificity resulting in side effects. This limits their practical application.

Where are nicotinic acetylcholine receptors found?

Nicotinic acetylcholine receptors are found on skeletal muscle. Used less frequently now compared to the past because of availability of antihypertensive drugs with fewer side effects.

In what situations are some of these drugs still used?

Some are still used in emergency situations e.g. aortic dissection or autonomic dysreflexia. Mecamylamine, pentolinium, and trimethaphan are used for controlled hypotension during surgery.

What are examples of drugs used for controlled hypotension during surgery?

Mecamylamine, pentolinium, and trimethaphan are therapeutically used for controlled hypotension during surgery to reduce bleeding and for rapid reduction of BP in emergencies like acute dissecting aneurysm.

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