Zolmitriptan

Serotonin-1b and Serotonin-1d Receptor Agonist — NERVOUS SYSTEM

Key facts

Zolmitriptan is an ofp drug in the Serotonin-1b and Serotonin-1d Receptor Agonist class catalogued in DrugCentral. It was first approved by the FDA in 1997. Its mechanism of action is classified as Serotonin 1b Receptor Agonists and Serotonin 1d Receptor Agonists. DrugCentral lists 8 molecular targets, including Drd2, Drd1 and HTR1D. Recorded indications include Migraine.

• Approval status: ofp (first approved 1997 by the FDA).
• Drug class: Serotonin-1b and Serotonin-1d Receptor Agonist.
• Mechanism of action: Serotonin 1b Receptor Agonists; Serotonin 1d Receptor Agonists.
• Molecular targets: Drd2, Drd1, HTR1D and Adra2b|Adra2c|Adra2a (8 listed in DrugCentral).
• Indications: Migraine.
• ATC code: N02CC03 (Selective serotonin (5HT1) agonists).
• Molecular formula: C16H21N3O2; molecular weight 287.36 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Migraine

Contraindications (19)

• Angina pectoris
• Cardiovascular event risk
• Cerebral arteriosclerosis
• Cerebral ischemia
• Cerebrovascular accident
• Disease of liver
• Disorder of coronary artery
• Hemiplegic migraine
• Hypertensive disorder
• Hypertensive urgency
• Kidney disease
• Myocardial infarction
• Myocardial ischemia
• Peripheral vascular disease
• Prinzmetal angina
• Raynaud's phenomenon
• Transient ischemic attack
• Vascular insufficiency of intestine
• Wolff-Parkinson-White pattern

Mechanism & targets

• Mechanism of action (MoA): Serotonin 1b Receptor Agonists; Serotonin 1d Receptor Agonists
• Established pharmacologic class: Serotonin-1b and Serotonin-1d Receptor Agonist

Molecular targets (8)

Target	Gene	Action	Activity
D(2) dopamine receptor	Drd2	unknown	Kd 10.40
D(1A) dopamine receptor	Drd1	unknown	Kd 9.52
5-hydroxytryptamine receptor 1D	HTR1D	agonist	Ki 8.90
Adrenergic receptor alpha-2	Adra2b|Adra2c|Adra2a	unknown	Kd 8.15
5-hydroxytryptamine receptor 1E	HTR1E	unknown	Ki 7.70
5-hydroxytryptamine receptor 1B	HTR1B	agonist	Ki 7.70
5-hydroxytryptamine receptor 1F	HTR1F	unknown	Ki 7.45
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 6.60

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1997-11-25	FDA	—	IPR

ATC classification

ATC code	Therapeutic hierarchy
N02CC03	NERVOUS SYSTEM › ANALGESICS › ANTIMIGRAINE PREPARATIONS › Selective serotonin (5HT1) agonists

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Swollen tongue	330.2
Dysphonia	295.3
Swelling face	276.5
Angioedema	271.6
Drug ineffective for unapproved indication	253.5
Headache	221.7
Migraine	194.4
Drug intolerance	148.4
Medication overuse headache	140.4
Paranasal cyst	122.4
Vascular malformation	120.6
Mastoiditis	112.8

Chemical structure

• Molecular formula: C₁₆H₂₁N₃O₂
• Molecular weight: 287.36 g/mol
• CAS number: —
• InChIKey: ULSDMUVEXKOYBU-ZDUSSCGKSA-N
• PubChem CID: 60857

CN(C)CCC1=CNC2=C1C=C(C[C@H]1COC(=O)N1)C=C2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Zolmitriptan used for?

DrugCentral lists the following indications for Zolmitriptan: Migraine.

How does Zolmitriptan work?

Zolmitriptan is classified as Serotonin 1b Receptor Agonists and Serotonin 1d Receptor Agonists; its molecular targets in DrugCentral include Drd2, Drd1, HTR1D (agonist) and Adra2b|Adra2c|Adra2a.

When was Zolmitriptan first approved?

Zolmitriptan was first approved by the FDA in 1997.

What drug class does Zolmitriptan belong to?

Zolmitriptan is in the Serotonin-1b and Serotonin-1d Receptor Agonist class.

What is the chemical formula of Zolmitriptan?

Zolmitriptan has the molecular formula C16H21N3O2 and a molecular weight of 287.36 g/mol.

Sources

• DrugCentral drug card 2869 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1185 — compound record and bioactivity
• PubChem CID 60857 — chemical identifiers
• DrugBank DB00315 — drug record
• FDA UNII 2FS66TH3YW — substance identity
• DailyMed: FDA labels for Zolmitriptan — current prescribing information (label search)
• UniProt P28221 (HTR1D) — target protein
• UniProt P28566 (HTR1E) — target protein
• UniProt P28222 (HTR1B) — target protein
• UniProt P30939 (HTR1F) — target protein
• UniProt P08908 (HTR1A) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.