Guanethidine

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Guanethidine chemical structure Guanethidine
2-[2-(azocan-1-yl)ethyl]guanidine IUPAC name
CAS number 645-43-2	ATC code C02CC02 .
PubChem 3518	DrugBank APRD01007
Chemical formula	{{{chemical_formula}}}
Molecular weight	198.309 g/mol
Bioavailability
Metabolism
Elimination half-life	1.5 days
Excretion	{{{excretion}}}
Pregnancy category
Legal status
Routes of administration

Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as noradrenaline. Its mechanism is inhibition of the Na+ATPase dependent pump.

Side effects

Side effects include orthostatic and exercise hypotension, sexual dysfunction (delayed or retrograde ejaculation), and diarrhea.

Pharmacology

Guanethidine is transported by uptake 1 into the presynaptic terminal. (In this it competes with noradrenaline so can potentiate exogenously applied noradrenaline). Once inside the terminal it blocks the release of noradrenaline in response to arrival of an action potential. Spontaneous release is not affected.

Uses

Guanethidine was once a mainstay for hypertension resistant to other agents, but it is now rarely used in the US due to side effects and because substantially better drugs are available. It is still licensed in some countries, e.g. UK, for the rapid control of blood pressure in a hypertensive emergency.

Intravenous nerve block (Bier block) using guanethidine has been used to treat chronic pain caused by complex regional pain syndrome.

See also

• Norepinephrine