Drug intelligence / Profile preview

trimethaphan

Development stage
Phase 1
Modality
Small Molecules
Administration
Intravenous
01

Overview

Trimethaphan is a ganglionic blocking agent and nicotinic acetylcholine receptor antagonist used primarily for the rapid reduction of blood pressure in hypertensive emergencies, controlled hypotension during surgery, and emergency treatment of pulmonary edema associated with systemic hypertension. It acts as a non-depolarizing competitive antagonist at nicotinic acetylcholine receptors in autonomic ganglia, thereby inhibiting both sympathetic and parasympathetic neurotransmission. This results in vasodilation, decreased vascular tone, reduced cardiac output, and lowered blood pressure. Trimethaphan does not cross the blood-brain barrier due to its charged sulfonium structure and thus has no central nervous system effects. Its use is now rare due to severe side effects from nonselective autonomic blockade and the availability of safer alternatives[1][2][3][4][6].

Brand names
Arfonad
Other names
trimetaphanthimethaphantrimetaphanumtrimethaphan camsylate
02

Targets

Nicotinic Acetylcholine Receptor

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