Not available in the U.S.

Moxonidine

PHYSIOTENS

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Moxonidine ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Moxonidine ballicule

What it isCentrally acting antihypertensive that works mainly at the I1 imidazoline receptor rather than at alpha-2, and is not marketed in the United States.

Why this oneThe I1 selectivity is the point: it lowers sympathetic outflow with much less of the sedation and dry mouth that limit clonidine.

What limits itRenally cleared with a short half-life. The MOXCON heart-failure trial was stopped early for excess mortality, so it is not used in systolic heart failure.

Moxonidine molecular structure (skeletal formula) — Molecular structure: Moxonidine

Off-label

hypertension (approved outside the US)

NO BOXED WARNINGS

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability1 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Defining liabilityBradycardia, conduction block, hypotension and somnolence

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Self-check

What receptor preference distinguishes moxonidine from clonidine?
I1 imidazoline rather than alpha-2.
Why is moxonidine not used in systolic heart failure?
Excess mortality in MOXCON.