Zolmitriptan

Category: pharmacological

Aliases: Zomig

Pharmacological Mechanism

Selective 5-HT1B/1D receptor agonist (triptan) for acute migraine — cranial vasoconstriction and trigeminal inhibition; also binds 5-HT1F. Active N-desmethyl metabolite.

Half-Life (t½)

PO: 3h

Dosing Guidelines

• PO: Typical 2.5 mg (Range: 1.25–5 mg)

Target Organ Systems

• nervous

Notes

PK from FDA prescribing information (DailyMed setid 333caafc-2e63-49f8-a0c6-534e528d228d): mean absolute bioavailability ~40% (F 0.4), apparent Vd 7 L/kg (~490 L), elimination t½ ~3 h, Tmax ~1.5 h (tablet). ka_hr 1.5 derived from Tmax 1.5 h (ke from t½ 3 h).

Chemical Identifiers

• PubChem CID: 60857
• Formula: C16H21N3O2
• Molecular weight: 287.36 g/mol
• InChIKey: ULSDMUVEXKOYBU-ZDUSSCGKSA-N
• SMILES: CN(C)CCC1=CNC2=C1C=C(C=C2)C[C@H]3COC(=O)N3

References

• PMID 10193663
• PMID 15900510