Guanethidine

This MedLibrary.org supplementary page on Guanethidine is provided directly from the open source Wikipedia as a service to our readers. Please see the note below on authorship of this content, as well as the Wikipedia usage guidelines. To search for other content from our encyclopedia supplement, please use the form below:

Related Sponsors

BM Pharmacy Generic pharmaceuticals at unbeatable prices. Insomnia, men's health, hair health, pain control. bmpharmacy.com
Online Pharmacy Carisoprodol, tadalafil, sildenafil, vardenafil and more... xlpharmacy.com
MedBasket.com Discreet. Inexpensive. Fast shipping. Great selection. What more can we say? medbasket.com
Frugalmed 2000 reasons to shop with us first. frugalmed.com
Ads by Tiva

Guanethidine
Systematic (IUPAC) name
2-(2-azocan-1-ylethyl)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
Bioavailability  ?
Metabolism  ?
Half life 1.5 days
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?
Legal status
Routes  ?

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

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. 
v • d • e
Adrenergic antagonists
α
Non-selective α
reversible (Phentolamine) · irreversible (Phenoxybenzamine)
Ungrouped
β
β1 selective
(cardioselective)
Mixed α1/β
Indirect
tyrosine hydroxylase inhibitor (Metirosine) · vesicle storage inhibitor (Reserpine) · neurotransmitter release blocker (Guanethidine, Bretylium)
v • d • e
Adrenergic agonists (models/most important in small caps)
α
β
Nonselective β
α and β
Epinephrine (α1+2, β1+2) · Norepinephrine (α1+2, β1) · Cirazoline · Etilefrine · Ephedrine · Pseudoephedrine
Indirect
v • d • e
Antihypertensives, not including diuretics (C02)
Sympatholytics
Central
Clonidine • Guanfacine • Methyldopa
Guanidine derivatives: Betanidine • Guanethidine • Guanoxan • Debrisoquine • Guanoclor • Guanazodine • Guanoxabenz
Peripheral
Indirect
Direct
Non-selective α blocker
Other
v • d • e
Ophthalmologicals: antiglaucoma preparations and miotics (S01E)
Sympathomimetics
Parasympathomimetics
Carbonic anhydrase inhibitors
Beta blocking agents
Prostaglandin analogues
Other agents
Dapiprazole • Guanethidine
Structure of captopril, the first clinically successful ACE inhibitor  This antihypertensive-related article is a stub. You can help Wikipedia by expanding it.

Wikipedia content modification information:

  • This page was last modified on 3 October 2008, at 13:17.

Wikipedia Authorship and Review

Wikipedia content provided here is not reviewed directly by MedLibrary.org. Wikipedia content is authored by an open community of volunteers and is not produced by or in any way affiliated with MedLibrary.org.

Wikipedia Usage Guidelines

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article on "Guanethidine".

The URL for this specific entry is:

All Wikipedia text is available under the terms of the GNU Free Documentation License. (See Copyrights for details). Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc.