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Apo-Guanethidine

Apo-Guanethidine - General Information

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.

 

Pharmacology of Apo-Guanethidine

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. Apo-Guanethidine works by decreasing the heart rate and relaxing the blood vessels so that blood can flow more easily through the body, thereby reducing these risks. It is a postganglionic sympathetic nerve terminal blocker that prevents the release of norepinephrine from nerve terminals.

 

Apo-Guanethidine for patients

 

Apo-Guanethidine Interactions

http://www.rxlist.com/cgi/generic3/guanethidine_od.htm

 

Apo-Guanethidine Contraindications

Known or suspected pheochromocytoma; hypersensitivity; frank congestive heart failure not due to hypertension; use of monoamine oxidase (MAO) inhibitors.

 

Additional information about Apo-Guanethidine

Apo-Guanethidine Indication: For the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension.
Mechanism Of Action: Apo-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. In contrast to ganglionic blocking agents, Apo-Guanethidine suppresses equally the responses mediated by alpha-and beta-adrenergic receptors but does not produce parasympathetic blockade. Since sympathetic blockade results in modest decreases in peripheral resistance and cardiac output, Apo-Guanethidine lowers blood pressure in the supine position. It further reduces blood pressure by decreasing the degree of vasoconstriction that normally results from reflex sympathetic nervous activity upon assumption of the upright posture, thus reducing venous return and cardiac output more.
Drug Interactions: Acetophenazine The agent decreases the effect of guanethidine
Amitriptyline The tricyclic decreases the effect of guanethidine
Amphetamine The agent decreases the effect of guanethidine
Benzphetamine The agent decreases the effect of guanethidine
Chlorpromazine The agent decreases the effect of guanethidine
Chlorprothixene The agent decreases the effect of guanethidine
Dexfenfluramine The agent decreases the effect of guanethidine
Dextroamphetamine The agent decreases the effect of guanethidine
Diethylpropion The agent decreases the effect of guanethidine
Dobutamine The agent decreases the effect of guanethidine
Dopamine The agent decreases the effect of guanethidine
Ephedra The agent decreases the effect of guanethidine
Ephedrine The agent decreases the effect of guanethidine
Epinephrine The agent decreases the effect of guanethidine
Ethopropazine The agent decreases the effect of guanethidine
Fenfluramine The agent decreases the effect of guanethidine
Fluphenazine The agent decreases the effect of guanethidine
Haloperidol The agent decreases the effect of guanethidine
Isocarboxazid The agent decreases the effect of guanethidine
Methotrimeprazine The agent decreases the effect of guanethidine
Mazindol The agent decreases the effect of guanethidine
Mesoridazine The agent decreases the effect of guanethidine
Metaraminol The agent decreases the effect of guanethidine
Methamphetamine The agent decreases the effect of guanethidine
Methdilazine The agent decreases the effect of guanethidine
Methoxamine The agent decreases the effect of guanethidine
Methylphenidate The agent decreases the effect of guanethidine
Norepinephrine The agent decreases the effect of guanethidine
Pargyline The agent decreases the effect of guanethidine
Propericiazine The agent decreases the effect of guanethidine
Perphenazine The agent decreases the effect of guanethidine
Phendimetrazine The agent decreases the effect of guanethidine
Phenelzine The agent decreases the effect of guanethidine
Phenmetrazine The agent decreases the effect of guanethidine
Phentermine The agent decreases the effect of guanethidine
Phenylephrine The agent decreases the effect of guanethidine
Phenylpropanolamine The agent decreases the effect of guanethidine
Prochlorperazine The agent decreases the effect of guanethidine
Promazine The agent decreases the effect of guanethidine
Promethazine The agent decreases the effect of guanethidine
Propiomazine The agent decreases the effect of guanethidine
Pseudoephedrine The agent decreases the effect of guanethidine
Thiethylperazine The agent decreases the effect of guanethidine
Thioridazine The agent decreases the effect of guanethidine
Thiothixene The agent decreases the effect of guanethidine
Tranylcypromine The agent decreases the effect of guanethidine
Trifluoperazine The agent decreases the effect of guanethidine
Triflupromazine The agent decreases the effect of guanethidine
Trimeprazine The agent decreases the effect of guanethidine
Amoxapine The tricyclic decreases the effect of guanethidine
Clomipramine The tricyclic decreases the effect of guanethidine
Desipramine The tricyclic decreases the effect of guanethidine
Doxepin The tricyclic decreases the effect of guanethidine
Imipramine The tricyclic decreases the effect of guanethidine
Nortriptyline The tricyclic decreases the effect of guanethidine
Trimipramine The tricyclic decreases the effect of guanethidine
Protriptyline The tricyclic decreases the effect of guanethidine
Food Interactions: Take without regard to meals.
Generic Name: Guanethidine
Synonyms: Guanethidine Monosulfate; Guanethidine Sulphae
Drug Category: Adrenergic Agents; Antihypertensive Agents; Sympatholytics
Drug Type: Small Molecule; Approved
Other Brand Names containing Guanethidine: Apo-Guanethidine; Ismelin; Eutensol; Abapresin; Oktadin;
Absorption: 3-30% of oral dose (poor and highly variable)
Toxicity (Overdose): Side effects include drowsiness, dizziness, tiredness or confusion. LD50=1000 mg/kg (mouse, oral)
Protein Binding: Not Available
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.
Half Life: 1.5 days
Dosage Forms of Apo-Guanethidine: Tablet Oral
Chemical IUPAC Name: 2-[2-(azocan-1-yl)ethyl]guanidine
Chemical Formula: C10H22N4
Guanethidine on Wikipedia: http://en.wikipedia.org/wiki/Guanethidine
Organisms Affected: Humans and other mammals