<unk>  is a selective 5-hydroxytryptamine 1B/1D receptor agonist with a weak affinity for the 5-HT 1A receptor subtypes. Its action on 5-HT 1B/1D receptors causes vasoconstriction in intracranial blood vessels; as well it can inhibit the release of pro-inflammatory neuropeptides from trigeminal perivascular nerve endings. It crosses the blood-brain-barrier as evidenced by the presence of radioactive 3H-zolmitriptan labels within the cells of the trigeminal nucleus caudalis and nucleus tractus solitaries. Pharmacokinetics<unk>  has a rapid onset of action and has been detected in the brain as early as within 5 minutes of intranasal administration. On average,<unk>  has an oral bioavailability of 40%, a mean volume of distribution of 8.3 L/kg after oral administration, and 2.4L/kg after intravenous administration.<unk>  is metabolized into three major metabolites by the human hepatic cytochrome P450 enzymes—primarily CYP1A2. Two-thirds of the parent compound breaks down into the active metabolite N-desmethyl-zolmitriptan (183C91), while the remaining one-third separates into the other two inactive metabolites:<unk>  N-oxide and an indole acetic acid derivative. It has an elimination half-life of about three hours before it undergoes renal elimination; its clearance is greater than the glomerular filtration rate suggesting that there is some renal tubular secretion of the compound.
Zolmitriptan
Sumatriptan
Eletriptan
Rizatriptan
Frovatriptan
Almotriptan
Naratriptan
Triptan