Drug Groups

approved; investigational

Description

Zolmitriptan is a synthetic tryptamine derivative and appears as a white powder that is readily soluble in water. [Wikipedia]

Indication

For the acute treatment of adult migraine with or without auras.

Pharmacology

Zolmitriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists, and has only a weak affinity for 5-HT_1A, 5-HT_5A, and 5-HT₇ receptors and no significant affinity or pharmacological activity at 5-HT₂, 5-HT₃ or 5-HT₄ receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Zolmitriptan also activates 5-HT₁ receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Zolmitriptan in humans.

Affected Organisms

Biotransformation

Hepatic. There have been three metabolites identified: indole acetic acid, N -oxide, and N-desmethyl metabolites. However, the N-desmethyl is the only active metabolite.

Absorption

Mean absolute oral bioavailability is approximately 40%. Food has no affect on the rate and extent of absorption.

Half Life

The mean elimination half-life of zolmitriptan and of the active N-desmethyl metabolite is 3 hours.

Protein Binding

25%

Distribution

* 8.4±3.3 L/kg

Clearance

* 25.9 mL/min/kg

References

External Links