Actibine - General Information
A plant alkaloid with alpha-2-adrenergic blocking activity. Actibine has been used as a mydriatic and in the treatment of impotence. It is also alleged to be an aphrodisiac.
Pharmacology of Actibine
Actibine is an indolalkylamine alkaloid with chemical similarity to reserpine. Actibine blocks presynaptic alpha-2 adrenergic receptors. Its action on peripheral blood vessels resembles that of reserpine, though it is weaker and of short duration. Actibine's peripheral autonomic nervous system effect is to increase parasympathetic (cholinergic) and decrease sympathetic (adrenergic) activity. It is to be noted that in male sexual performance, erection is linked to cholinergic activity and to alpha-2 adrenergic blockade which may theoretically result in increased penile inflow, decreased penile outflow or both. Actibine exerts a stimulating action on the mood and may increase anxiety. Such actions have not been adequately studied or related to dosage although they appear to require high doses of the drug. Actibine has a mild anti-diuretic action, probably via stimulation of hypothalmic center and release of posterior pituitary hormone. Reportedly Actibine exerts no significant influence on cardiac stimulation and other effects mediated by (beta)-adrenergic receptors. Its effect on blood pressure, if any, would be to lower it; however, no adequate studies are at hand to quantitate this effect in terms of Actibine dosage.
Actibine for patients
Renal diseases, and patients sensitive to the drug. In view of the limited and inadequate information at hand, no precise tabulation can be offered of additional contraindications.
Additional information about Actibine
Actibine Indication: Indicated as a sympatholytic and mydriatic. Impotence has been successfully treated with yohimbine in male patients with vascular or diabetic origins and psychogenic origins.
Mechanism Of Action: Actibine is a pre-synaptic alpha 2-adrenergic blocking agent. The exact mechanism for its use in impotence has not been fully elucidated. However, yohimbine may exert its beneficial effect on erectile ability through blockade of central alpha 2-adrenergic receptors producing an increase in sympathetic drive secondary to an increase in norepinephrine release and in firing rate of cells in the brain noradrenergic nuclei. Actibine-mediated norepinephrine release at the level of the corporeal tissues may also be involved. In addition, beneficial effects may involve other neurotransmitters such as dopamine and serotonin and cholinergic receptors.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Yohimbine
Drug Category: Adrenergic alpha-Antagonists; Mydriatics
Drug Type: Small Molecule; Approved
Other Brand Names containing Yohimbine: Yocon; Yohimar; Yohimex; Yoman; Yovital; Thybine; Actibine; Baron-X; Dayto himbin; Aphrodyne;
Absorption: Rapidly absorbed following oral administration. Bioavailability is highly variable, ranging from 7 to 87% (mean 33%).
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Yohimbine appears to undergo extensive metabolism in an organ of high flow such as the liver or kidney, however, the precise metabolic fate of yohimbine has not been fully determined.
Half Life: Elimination half-life is approximately 36 minutes.
Dosage Forms of Actibine: Tablet Oral
Chemical IUPAC Name: Not Available
Chemical Formula: C21H26N2O3
Yohimbine on Wikipedia: http://en.wikipedia.org/wiki/Yohimbine
Organisms Affected: Humans and other mammals