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Guanethidine: Wikis

  

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Guanethidine
Systematic (IUPAC) name
2-[2-(azocan-1-yl)ethyl]guanidine
Identifiers
CAS number 645-43-2
ATC code C02CC02 S01EX01
PubChem 3518
DrugBank APRD01007
Chemical data
Formula C10H22N4 
Mol. mass 198.309 g/mol
Pharmacokinetic data
Half life 1.5 days
Therapeutic considerations
Pregnancy cat.  ?
Legal status
 Yes check.svgY(what is this?)  (verify)

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

Contents

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.[1]

References

  1. ^ Joyce PI, Rizzi D, Caló G, Rowbotham DJ, Lambert DG (November 2002). "The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens". Anesth. Analg. 95 (5): 1339–43, table of contents. PMID 12401623. http://www.anesthesia-analgesia.org/cgi/pmidlookup?view=long&pmid=12401623. 







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