Zolmitriptan

Zolmitriptan binds with high affinity to human recombinant 5-HT 1D and 5-HT 1B receptors, and moderate affinity for 5-HT 1A receptors. The N-desmethyl metabolite also has high affinity for 5-HT 1B/1D and moderate affinity for 5-HT1A receptors.

• ZOLMITRIPTAN NASAL SPRAY is indicated for the acute treatment of migraine with or without aura in adults and pediatric patients 12 years of age and older. Limitations of Use Only use ZOLMITRIPTAN NASAL SPRAY if a clear diagnosis of migraine has been established.ICD-10: G43.909

• Zolmitriptan is contraindicated in patients with: Ischemic coronary artery disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), other significant underlying cardiovascular disease, or coronary artery vasospasm including Prinzmetal's angina [see Warnings and Precautions (5.1) ] Wolff-Parkinson-White Syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [see Warnings and Precautions (5.2) ] History of stroke, transient ischemic attack (TIA) or history of hemiplegic or basilar migraine because these patients are at higher risk of stroke [see Warnings and Precautions (5.4) ] Peripheral vascular disease (PVD) [see Warnings and Precautions (5.5) ] Ischemic bowel disease [see Warnings and Precautions (5.5) ] Uncontrolled hypertension [see Warnings and Precautions (5.8) ] Recent use (i.e., within 24 hours) of another 5-HT 1 agonist, ergotamine-containing medication, or ergot-type medication (such as dihydroergotamine or methysergide) [see Drug Interactions (7.1 , 7.3) ] Concurrent administration of an MAO-A inhibitor or recent discontinuation of a MAO-A inhibitor (that is within 2 weeks) [see Drug Interactions (7…contraindicated

Recommended starting dose: 2.5 mg (2.1) Maximum single dose: 5 mg (2.1) May repeat dose after 2 hours if needed; not to exceed 10 mg in any 24-hour period (2.1) 2.1 Dosing Information The recommended starting dose for ZOLMITRIPTAN NASAL SPRAY in adult and pediatric patients 12 years of age and older is 2.5 mg. As the individual response to ZOLMITRIPTAN NASAL SPRAY may vary, the dose should be adjusted on an individual basis. The maximum recommended single dose of ZOLMITRIPTAN NASAL SPRAY is 5 mg. If the migraine has not resolved by 2 hours after taking ZOLMITRIPTAN NASAL SPRAY, or returns after a transient improvement, another dose may be administered at least 2 hours after the previous dose. The maximum daily dose should not exceed 10 mg in any 24-hour period. The safety of ZOLMITRIPTAN NASAL SPRAY in the treatment of an average of more than four headaches in a 30-day period has not been established. 2.2 Dosing in Patients with Hepatic Impairment ZOLMITRIPTAN NASAL SPRAY is not recommended in patients with moderate to severe hepatic impairment because of increased zolmitriptan blood levels in these patients and elevation of blood pressure in some of these patients. The recommended dosage of ZOLMITRIPTAN NASAL SPRAY in patients with mild hepatic impairment is the same as for patients with normal hepatic function [see Dosage and Administration (2.1) , Warnings and Precautions (5.8) , Use in Specific Populations (8.6) and Clinical Pharmacology (12.3) ] .

Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina: Perform cardiac evaluation in patients with multiple cardiovascular risk factors (5.1) Arrhythmias: Discontinue dosing if occurs (5.2) Chest/throat/neck/jaw pain, tightness, pressure, or heaviness: Generally not associated with myocardial ischemia; evaluate for coronary artery disease in patients at high risk (5.3) Cerebral hemorrhage, subarachnoid hemorrhage, and stroke: Discontinue dosing if occurs (5.4) Gastrointestinal ischemic events, peripheral vasospastic reactions: Discontinue dosing if occurs (5.5) Medication Overuse Headache: Detoxification may be necessary (5.6) Serotonin syndrome: Discontinue dosing if occurs (5.7 , 7.5) Increase in blood pressure: very rarely associated with significant events (5.8) 5.1 Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina Zolmitriptan is contraindicated in patients with ischemic or vasospastic coronary artery disease (CAD). There have been rare reports of serious cardiac adverse reactions, including acute myocardial infarction, occurring within a few hours following administration of zolmitriptan. Some of these reactions occurred in patients without known CAD. 5-HT 1 agonists including zolmitriptan may cause coronary artery vasospasm (Prinzmetal's Angina), even in patients without a history of CAD. Perform a cardiovascular evaluation in triptan-naïve patients who have multiple cardiovascular risk factors (e.g., increased age, diabetes, hypertension, smoking, obesity, strong family history of CAD) prior to receiving zolmitriptan.

The following adverse reactions are discussed in more detail in other sections of labeling: Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina [see Warnings and Precautions (5.1) ] Arrhythmias [see Warnings and Precautions (5.2) ] Chest, Throat, Neck and/or Jaw Pain/Tightness/Pressure [see Warnings and Precautions (5.3)] Cerebrovascular Events [see Warnings and Precautions (5.4)] Other Vasospasm Reactions [see Warnings and Precautions (5.5)] Medication Overuse Headache [see Warnings and Precautions (5.6) ] Serotonin Syndrome [see Warnings and Precautions (5.7) ] Increase in Blood Pressure [see Warnings and Precautions (5.8) ] The most common adverse reactions (≥ 5% and > placebo) were: Adults: unusual taste, paresthesia, dizziness, and hyperesthesia (6.1) Pediatrics: unusual taste (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Amneal Pharmaceuticals at 1-877-835-5472 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice. Adults Among 460 patients treating 1180 single attacks with zolmitriptan nasal spray in a blinded placebo controlled trial (Study 1), there was a low withdrawal rate related to adverse reactions: 5 mg (1.3%), 2.5 mg (0%), and placebo (0.4%). None of the withdrawals were due to a serious event.

Pregnancy: Based on animal data, may cause fetal harm (8.1) 8.1 Pregnancy Risk Summary There are no adequate data on the developmental risk associated with the use of zolmitriptan in pregnant women. In reproductive toxicity studies in rats and rabbits, oral administration of zolmitriptan to pregnant animals resulted in embryolethality and fetal abnormalities (malformations and variations) at clinically relevant exposures. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. The estimated rates of major birth defects (2.2%-2.9%) and miscarriage (17%) among deliveries to women with migraine are similar to rates reported in women without migraine. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Published data have suggested that women with migraine may be at increased risk of preeclampsia during pregnancy. Data Animal Data When zolmitriptan was administered to pregnant rats during the period of organogenesis at oral doses of 100, 400, and 1200 mg/kg/day (plasma exposures (AUCs) ≈280, 1100, and 5000 times the human AUC at the maximum recommended human dose (MRHD) of 10 mg/day), there was a dose-related increase in embryolethality. A no-effect dose for embryolethality was not established.

Metabolism

Absorption, Distribution, Metabolism, and Excretion Absorption Zolmitriptan nasal spray is rapidly absorbed via the nasopharynx as detected in a Photon Emission Tomography (PET) study using 11 C zolmitriptan. The mean relative bioavailability of the nasal spray formulation is 102%, compared with the oral tablet.

There is no experience with acute overdose. Clinical study subjects receiving single 50 mg oral doses of zolmitriptan commonly experienced sedation. The elimination half-life of zolmitriptan is 3 hours [see Clinical Pharmacology (12.1) ] and therefore monitoring of patients after overdose with zolmitriptan should continue for at least 15 hours or while symptoms or signs persist. There is no specific antidote to zolmitriptan. In cases of severe intoxication, intensive care procedures are recommended, including establishing and maintaining a patent airway, ensuring adequate oxygenation and ventilation, and monitoring and support of the cardiovascular system. It is unknown what effect hemodialysis or peritoneal dialysis has on the plasma concentrations of zolmitriptan.

• Sep 30, 2003NDANDA021450Amneal
• May 14, 2013ANDAANDA202560Glenmark Pharms Ltd
• May 14, 2013ANDAANDA201779Glenmark Pharms Ltd
• May 15, 2013ANDAANDA202890Zydus Pharms Usa Inc
• Apr 9, 2014ANDAANDA204284Invagen Pharms
• Sep 17, 2015ANDAANDA202956Jubilant Generics
• Sep 30, 2015ANDAANDA204232Alembic
• May 11, 2016ANDAANDA207021Aurobindo Pharma

1. 1Migraine1,01414%
2. 2Headache90313%
3. 3Drug Ineffective72810%
4. 4Nausea5497.8%
5. 5Off Label Use5047.2%
6. 6Fatigue4726.7%
7. 7Pain4306.1%
8. 8Vomiting3404.8%
9. 9Drug Intolerance3264.6%
10. 10Dizziness3244.6%
11. 11Malaise2954.2%
12. 12Dyspnoea2894.1%
13. 13Drug Dose Omission2844.0%
14. 14Insomnia2533.6%
15. 15Diarrhoea2463.5%

The 10 most recently updated of 28 ClinicalTrials.gov registrations naming Zolmitriptan as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Pharmacokinetics in Oral and Intranasal Formulations of Zolmitriptan.
  Completed · Phase 1 · Interventional · 8 enrolled · Parc de Salut Mar
  NCT06074016updated 2026-05-05
• Quality Improvement and Practice Based Research in Neurology Using the EMR
  Enrolling by invitation · Phase 4 · Interventional · 3,300 enrolled · Endeavor Health
  NCT02670161updated 2025-08-24
• Cocaine and Zolmitriptan
  Completed · Early phase 1 · Interventional · 12 enrolled · William Stoops
  NCT05019430updated 2025-08-05
• Treatments of Migraine with Triptans in Individuals with Elevated Cardiovascular Risk and in Pregnant Women
  Completed · Observational · 68,419 enrolled · Mayo Clinic
  NCT05854992updated 2024-12-02
• Efficacy of Zolmitriptan (Zomig) in the Treatment of Migraines in Adolescents
  Completed · Phase 3 · Interventional · 247 enrolled · Impax Laboratories, LLC
  NCT00617695updated 2024-10-02
• Double-Blind Comparison of the Efficacy and Safety of C213 to Placebo for the Acute Treatment of Cluster Headaches
  Completed · Phase 2 · Phase 3 · Interventional · 42 enrolled · Zosano Pharma Corporation
  NCT04066023updated 2022-06-14
• A Four-way Crossover Study of 3 Formulations of M207 With Intranasal Zolmitriptan in Healthy Volunteers
  Completed · Phase 1 · Interventional · 24 enrolled · Zosano Pharma Corporation
  NCT03978403updated 2021-11-18
• Study of PK, Safety, and Tolerability of 2 Lots of M207 & Intranasal Zolmitriptan in Healthy Volunteers
  Completed · Phase 1 · Interventional · 48 enrolled · Zosano Pharma Corporation
  NCT04969497updated 2021-09-17
• Efficacy & Safety Of Zomig Nasal Spray For Acute Migraine Treatment In Subjects 6 To 11 Years, With OLE
  Completed · Phase 3 · Interventional · 374 enrolled · Impax Laboratories, LLC
  NCT03275922updated 2021-01-11
• A Study to Evaluate the Long-Term Safety of M207 in the Acute Treatment of Migraine
  Completed · Phase 3 · Interventional · 342 enrolled · Zosano Pharma Corporation
  NCT03282227updated 2020-08-19

Frequently asked questions

How does Zolmitriptan work?

Zolmitriptan binds with high affinity to human recombinant 5-HT 1D and 5-HT 1B receptors, and moderate affinity for 5-HT 1A receptors. The N-desmethyl metabolite also has high affinity for 5-HT 1B/1D and moderate affinity for 5-HT1A receptors.

What is Zolmitriptan used for?

According to FDA labeling, Zolmitriptan carries indications including: ZOLMITRIPTAN NASAL SPRAY is indicated for the acute treatment of migraine with or without aura in adults and pediatric patients 12 years of age and older. Limitations of Use Only use ZOLMITRIPTAN NASAL SPRAY if a clear diagnosis of migraine has been established.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Zolmitriptan?

Zolmitriptan is classified as Selective serotonin (5HT1) agonists, Serotonin-1b and Serotonin-1d Receptor Agonist, Monoamine Oxidase Inhibitors, Serotonin 1b Receptor Agonists, Serotonin 1d Receptor Agonists, Serotonin Agonists, Cerebral Arterial Vasoconstriction, Increased Central Nervous System Serotonin Activity.

What are the brand names for Zolmitriptan?

Zolmitriptan is marketed under brand names including Zomig.

What are the contraindications for Zolmitriptan?

Zolmitriptan labeling lists contraindications including: Zolmitriptan is contraindicated in patients with: Ischemic coronary artery disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), other significant underlying cardiovascular disease, or coronary artery vasospasm including Prinzmetal's angina [see Warnings and Precautions (5.1) ] Wolff-Parkinson-White Syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [see Warnings and Precautions (5.2) ] History of stroke, transient ischemic attack (TIA) or history of hemiplegic or basilar migraine because these patients are at higher risk of stroke [see Warnings and Precautions (5.4) ] Peripheral vascular disease (PVD) [see Warnings and Precautions (5.5) ] Ischemic bowel disease [see Warnings and Precautions (5.5) ] Uncontrolled hypertension [see Warnings and Precautions (5.8) ] Recent use (i.e., within 24 hours) of another 5-HT 1 agonist, ergotamine-containing medication, or ergot-type medication (such as dihydroergotamine or methysergide) [see Drug Interactions (7.1 , 7.3) ] Concurrent administration of an MAO-A inhibitor or recent discontinuation of a MAO-A inhibitor (that is within 2 weeks) [see Drug Interactions (7…. Always consult the full prescribing information and a clinician.