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QuickView for Guanethidine (compound)


PubChem
Name: Guanethidine
PubChem Compound ID: 3518
Description: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.
Molecular formula: C10H22N4
Molecular weight: 198.309 g/mol
Synonyms:
NSC29863; Octadin; CAS-60-02-6; Guanetidina [INN-Spanish]; Sanotensin; Guanidine, N-[2-(hexahydro-1(2H)-azocinyl)ethyl]-;; AIDS-155922; Octatensine; KBio2_006453; EINECS 200-241-3.
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DrugBank
Identification
Name: Guanethidine
Name (isomeric): DB01170
Drug Type: small molecule
Description: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.
Synonyms:
Guanethidine Sulphae; Guanethidine Monosulfate
Brand: Oktadin, Apo-Guanethidine, Abapresin, Ismelin, Eutensol
Category: Sympatholytics, Adrenergic Agents, Antihypertensive Agents
CAS number: 645-43-2
Pharmacology
Indication: For the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension.
Pharmacology:
High blood pressure can cause the heart and arteries to not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled. Guane...
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Mechanism of Action:
Guanethidine acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine, rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles...
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Absorption: 3-30% of oral dose (poor and highly variable)
Biotransformation: Guanethidine is converted by the liver to three metabolites, which are excreted in the urine. The metabolites are pharmacologically less active than the parent compound.
Route of elimination: Ismelin is converted by the liver to three metabolites, which are excreted in the urine.
Half Life: 1.5 days
Clearance: Renal cl=56 ml/min
Toxicity: Side effects include drowsiness, dizziness, tiredness or confusion. LD50=1000 mg/kg (mouse, oral)
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take without regard to meals.
Drug interaction:
BenzphetamineBenzphetamine may decrease the effect of guanethidine.
MethylphenidateMethylphenidate may decrease the effect of guanethidine.
EphedrineEphedrine may decrease the effect of guanethidine.
ChlorpromazineChlorpromazine may decrease the effect of guanethidine.
ProchlorperazineProchlorperazine may decrease the effect of guanethidine.
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