Zolmitriptan 5 mg Tablet, Orally Disintegrating
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Serotonin-1b and Serotonin-1d Receptor Agonist class.
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🏭 Manufacturer & labeler
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🩺 Clinical
- Zolmitriptan is designed to treat a migraine that's already started, not just dull the pain a little. It works on specific receptors in the brain to help narrow the widened blood v...
- What exactly does zolmitriptan do — will it stop my migraine or just take the edge off?
- Yes — if your migraine hasn't fully gone away after 2 hours, or if it comes back after initially getting better, you can take a second dose. You just need to wait at least 2 hours...
- Can I take it again if my headache comes back a few hours later?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Zolmitriptan — tap one for details:
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💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII Z0H242BBR1
Aspartame is an artificial sweetener made from amino acids. It's added to medicines to improve taste, making bitter or unpleasant-tasting drugs easier to take.
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UNII 68401960MK
Crospovidone is a synthetic polymer made from polyvinylpyrrolidone. It acts as a disintegrant, helping tablets break apart quickly in the stomach so the medicine dissolves and absorbs into the body.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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UNII 3OWL53L36A
A natural sugar alcohol derived from seaweed or synthesized in the lab. It's used as a filler to add bulk, a sweetener in sugar-free formulas, and a disintegrant to help tablets break apart in the stomach.
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UNII OP1R32D61U
Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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UNII 5EVU04N5QU
A natural or synthetic colorant that gives the medicine an orange hue. It helps identify the medication and may improve appearance.
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UNII ETJ7Z6XBU4
Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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UNII 7CV7WJK4UI
Sodium stearyl fumarate is a synthetic compound made from stearyl alcohol and fumaric acid. It acts as a lubricant and glidant in tablets and capsules, helping ingredients flow smoothly during manufacturing and preventing sticking.
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UNII XHX3C3X673
Triacetin is a clear, oily liquid made from glycerin and acetic acid. It works as a plasticizer and solvent in medicines, helping soften coatings and improve how liquids mix together in formulations.
9 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Zolmitriptan OD 5 mg 59746-0462-13 | Jubilant | 3 tablets | $3.045 | AB | Availability likely | — |
| zolmiptriptan 5 mg 68462-0500-33 | Glenmark | 3 tablets | $3.045 | AB | Availability likely | — |
| Zolmitriptan OD 5 mg 42291-0999-03 | AvKARE | 3 tablets | — | AB | FDA listed | — |
| Zolmitriptan 5 mgthis 46708-0182-13 | Alembic | 3 tablets | — | AB | FDA listed | — |
| Zolmitriptan 5 mg 62332-0182-13 | Alembic | 3 tablets | — | AB | FDA listed | — |
| Zolmitriptan 5 mg 65841-0768-01 | Zydus | 100 tablets | — | AB | FDA listed | — |
| Zolmitriptan 5 mg 68382-0717-01 | Zydus | 100 tablets | — | AB | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 46708-0182-13 You're viewing this | 3 BLISTER PACK in 1 CARTON (46708-182-13) / 3 TABLET, ORALLY DISINTEGRATING in 1 BLISTER PACK | 2016-12-01 | Active |
| 46708-0182-03 | 3 BLISTER PACK in 1 CARTON (46708-182-03) / 3 TABLET, ORALLY DISINTEGRATING in 1 BLISTER PACK | 2016-12-01 | Active |
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🧭 About this NDC listing & data coverage
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Zolmitriptan is indicated for the acute treatment of migraine with or without aura in adults. Limitations of Use Only use zolmitriptan if a clear diagnosis of migraine has been established. If a patient has no response to zolmitriptan treatment for the first migraine attack, reconsider the diagnosis of migraine before zolmitriptan is administered to treat any subsequent attacks.
Zolmitriptan is not indicated for the prevention of migraine attacks. Safety and effectiveness of zolmitriptan have not been established for cluster headache. Zolmitriptan is a serotonin (5-HT) 1B/1D receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults (1) Limitations of Use : Use only after a clear diagnosis of migraine has been established (1) Not indicated for the prophylactic therapy of migraine (1) Not indicated for the treatment of cluster headache (1)
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Recommended starting dose: 1.25 mg or 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) Do not break zolmitriptan orally disintegrating tablets (2.2) Moderate or Severe Hepatic Impairment: 1.25 mg recommended (2.3, 8.6)
2.1Dosing Information The recommended starting dose of zolmitriptan tablet is 1.25 mg or 2.5 mg. The 1.25 mg dose can be achieved by manually breaking the functionally-scored 2.5 mg tablet in half. The maximum recommended single dose of zolmitriptan tablet is 5 mg.
In controlled clinical trials, a greater proportion of patients had headache response following a 2.5 mg or 5 mg dose than following a 1 mg dose. There was little added benefit from the 5 mg dose compared to the 2.5 mg dose, but adverse reactions were more frequent with the 5 mg dose. If the migraine has not resolved by 2 hours after taking zolmitriptan, or returns after a transient improvement, a second dose may be administered at least 2 hours after the first dose.
The maximum daily dose is 10 mg in any 24-hour period. The safety of zolmitriptan in the treatment of an average of more than three migraines in a 30-day period has not been established.
2.2Administration of Zolmitriptan Orally Disintegrating Tablets Instruct patients not to break zolmitriptan orally disintegrating tablets because they are not functionally-scored. Administration with liquid is not necessary. Orally disintegrating tablets are packaged in a blister pack.
Instruct patients not to remove the tablet from the blister until just prior to dosing. Subsequently, instruct patients to peel the blister pack open, and to place the orally disintegrating tablet on the tongue, where it will dissolve and it will be swallowed with the saliva.
2.3Dosing in Patients with Hepatic Impairment The recommended dose of zolmitriptan tablet in patients with moderate to severe hepatic impairment is 1.25 mg (one-half of one 2.5 mg zolmitriptan tablet) because of increased zolmitriptan blood levels in these patients and elevation of blood pressure in some of these patients. Limit the total daily dose in patients with severe hepatic impairment to no more than 5 mg per day. The use of zolmitriptan orally disintegrating tablets is not recommended in patients with moderate or severe hepatic impairment because these orally disintegrating tablets should not be broken in half [see Use in Specific Populations (8.6), and Clinical Pharmacology (12.3) ].
2.4Dosing in Patients taking Cimetidine If zolmitriptan is co-administered with cimetidine, limit the maximum single dose of zolmitriptan to 2.5 mg, not to exceed 5 mg in any 24-hour period [ see Drug Interactions (7.5), Clinical Pharmacology (12.3) ].
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS 2.5 mg Orally Disintegrating Tablets : White to off-white, round, flat faced bevelled edge tablets debossed with '359' on one side and 'L' on other side. 5 mg Orally Disintegrating Tablets : White to off-white, round, flat faced bevelled edge tablets debossed with '360' on one side and 'L' on other side. Orally Disintegrating Tablets: 2.5 mg and 5 mg (3)
⛔ Contraindications ▾
4 CONTRAINDICATIONS 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 a 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 a monoamine oxidase (MAO)-A inhibitor or recent use of a MAO-A inhibitor (that is within 2 weeks) [ see Drug Interactions (7.2) and Clinical Pharmacology (12.3) ] Known hypersensitivity to zolmitriptan (angioedema and anaphylaxis seen) [ see Adverse Reactions (6.2) ] History of coronary artery disease (CAD)or coronary vasospasm (4) Symptomatic Wolff-Parkinson-White syndrome or other cardiac accessory conduction pathway disorders (4) History of stroke, transient ischemic attack, or hemiplegic or basilar migraine (4) Peripheral vascular disease (4) Ischemic bowel disease (4) Uncontrolled hypertension (4) Recent (within 24 hours) use of another 5-HT 1 agonist (e.g., another triptan), or an ergotamine-containing medication (4) Monamine oxidase (MAO)-A inhibitor used in past 2 weeks (4) Known hypersensitivity to zolmitriptan (4)
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Myocardial Ischemia/Infarction, and Prinzmetal Angina : Perform cardiac evaluation in patients with multiple cardiovascular risk factors (5.1) Arrhythmias : Discontinue zolmitriptan if occurs (5.2) Chest/Throat/Neck/Jaw Pain, Tightness, and Pressure : Generally not associated with myocardial ischemia; evaluate for CAD in patients at high risk (5.3) Cerebral Hemorrhage, Subarachnoid Hemorrhage, and Stroke : Discontinue zolmitriptan if occurs (5.4) Gastrointestinal Ischemic Reactions and Peripheral Vasospastic Reactions : Discontinue zolmitriptan if occurs (5.5) Medication Overuse Headache : Detoxification may be necessary (5.6) Serotonin Syndrome : Discontinue zolmitriptanif occurs (5.7, 7.4) Patients with Phenylketonuria : Zolmitriptan orally disintegrating tablet contains phenylalanine (5.9)
5.1Myocardial Ischemia, Myocardial Infarction, and Prinzmetal 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 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. Do not administer zolmitriptan if there is evidence of CAD or coronary artery vasospasm [ see Contraindications (4) ].
For patients with multiple cardiovascular risk factors who have a negative cardiovascular evaluation, consider administrating the first zolmitriptan dose in a medically-supervised setting and performing an electrocardiogram (ECG) immediately following zolmitriptan administration. For such patients, consider periodic cardiovascular evaluation in intermittent long-term users of zolmitriptan.
5.2Arrhythmias Life-threatening disturbances of cardiac rhythm including ventricular tachycardia and ventricular fibrillation leading to death have been reported within a few hours following the administration of 5-HT 1 agonists. Discontinue zolmitriptan if these disturbances occur. Zolmitriptan is contraindicated in patients with Wolff-Parkinson-White Syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [ see Contraindications (4) ] .
5.3Chest, Throat, Neck and Jaw Pain/Tightness/Pressure As with other 5-HT 1 agonists, sensations of tightness, pain, and pressure in the chest, throat, neck, and jaw commonly occur after treatment with zolmitriptan and is usually non-cardiac in origin. However, perform a cardiac evaluation if these patients are at high cardiac risk. 5-HT 1 agonists including zolmitriptan are contraindicated in patients with CAD or Prinzmetal’s variant angina [ see Contraindications (4) ].
5.4Cerebrovascular Events Cerebral hemorrhage, subarachnoid hemorrhage, and stroke have occurred in patients treated with 5-HT 1 agonists, and some have resulted in fatalities. In a number of cases, it appears possible that the cerebrovascular events were primary, the 5-HT 1 agonist having been administered in the incorrect belief that the symptoms experienced were a consequence of migraine, when they were not. As with other acute migraine therapies, before treating headaches in patients not previously diagnosed as migraineurs, and in migraineurs who present with symptoms atypical for migraine, exclude other potentially serious neurological conditions.
Zolmitriptan is contraindicated in patients with a history of stroke or transient ischemic attack [ see Contraindications (4) ].
5.5Other Vasospasm Reactions 5-HT 1 agonists, including zolmitriptan, may cause non-coronary vasospastic reactions,…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in other sections of the prescribing information: Myocardial Ischemia, Myocardial Infarction, and Prinzmetal Angina [ see Warnings and Precautions (5.1) ]. Arrthymias [ see Warnings and Precautions (5.2) ]. Chest and or Throat, Neck and 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) ]. Risks in Patients with Phenylketonuria [ see Warnings and Precautions (5.9) ].
Most common adverse reactions (≥5% and >placebo) were neck/throat/ jaw pain/tightness/pressure, dizziness, paresthesia, asthenia, somnolence, warm/cold sensation, nausea, heaviness sensation, and dry mouth (6.1) To report SUSPECTED ADVERSE REACTIONS, contact FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical 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. In a long-term, open-label study where patients were allowed to treat multiple migraine attacks for up to 1 year, 8% (167 out of 2,058) withdrew from the trial because of adverse reaction. The most common adverse reactions (≥5% and >placebo) in these trials were neck/throat/jaw pain, dizziness, paresthesia, asthenia, somnolence, warm/cold sensation, nausea, heaviness sensation, and dry mouth.
Table 1 lists the adverse reactions that occurred in ≥2% of the 2,074 patients in any one of the zolmitriptan 1 mg, 2.5 mg, or 5 mg dose groups in the controlled clinical trials of zolmitriptan in patients with migraines (Studies 1, 2, 3, 4, and 5) [ see Clinical Studies (14) ]. Only adverse reactions that were at least 2% more frequent in a zolmitriptan group compared to the placebo group are included. Several of the adverse reactions appear dose related, notably paresthesia, sensation of heaviness or tightness in chest, neck, jaw, and throat, dizziness, somnolence and possibly asthenia and nausea.
Table 1: Adverse Reaction Incidence in Five Pooled Placebo-Controlled Migraine Clinical Trials 1 Placebo Zolmitriptan Zolmitriptan Zolmitriptan 1 mg 2.5 mg 5 mg (n=401) (n=163) (n=498) (n=1012) ATYPICAL SENSATIONS 6% 12% 12% 18% Paresthesia (all types) 2% 5% 7% 9% Warm/cold sensation 4% 6% 5% 7% PAIN AND PRESSURE SENSATIONS 7% 13% 14% 22% Chest - pain/tightness/pressure and/or heaviness 1% 2% 3% 4% Neck/throat/jaw - pain/tightness/pressure 3% 4% 7% 10% Heaviness other than chest or neck 1% 1% 2% 5% Other-Pressure/tightness/heaviness 0% 2% 2% 2% DIGESTIVE 8% 11% 16% 14% Dry mouth 2% 5% 3% 3% Dyspepsia 1% 3% 2% 1% Dysphagia 0% 0% 0% 2% Nausea 4% 4% 9% 6% NEUROLOGICAL 10% 11% 17% 21% Dizziness 4% 6% 8% 10% Somnolence 3% 5% 6% 8% Vertigo 0% 0% 0% 2% OTHER Asthenia 3% 5% 3% 9% Sweating 1% 0% 2% 3% 1 Only adverse reactions that were at least 2% more frequent in a zolmitriptan group compared to the placebo group are included.
There were no differences in the incidence of adverse reactions in controlled clinical trials in the following subgroups: gender, weight, age, use of prophylactic medications, or presence of aura. There were insufficient data to assess the impact of race on the incidence of adverse reactions. Less Common Adverse Reactions with Z olmitriptan Tablets: In the paragraphs that follow, the frequencies of less commonly reported adverse clinical reactions are presented.
Because the reports include reactions observed in open and uncontrolled studies, the role of zolmitriptan in their causation cannot be reliably determined. Furthermore, variability associated with adverse reac…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS
7.1Ergot-containing Drugs Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and zolmitriptan within 24 hours of each other is contraindicated [ see Contraindications (4) ].
7.2MAO-A Inhibitors MAO-A inhibitors increase the systemic exposure of zolmitriptan and its active N-desmethyl metabolite. Therefore, the use of zolmitriptan in patients receiving MAO-A inhibitors is contraindicated [ see Contraindications (4) and Clinical Pharmacology (12.3) ] . 7.3 5-HT1B/1D Agonists Concomitant use of other 5-HT 1B/1D agonists (including triptans) within 24 hours of zolmitriptan treatment is contraindicated because the risk of vasospastic reactions may be additive [ see Contraindications (4) ].
7.4Selective Serotonin Reuptake Inhibitors and Serotonin Norepinephrine Reuptake Inhibitors Cases of life-threatening serotonin syndrome have been reported during co-administration of triptans and selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs) [ see Warnings and Precautions (5.7) ].
7.5Cimetidine Following administration of cimetidine, the half-life and blood levels of zolmitriptan and its active N-desmethyl metabolite were approximately doubled [ see Clinical Pharmacology (12.3) ] . If cimetidine and zolmitriptan are used concomitantly, limit the maximum single dose of zolmitriptan to 2.5 mg, not to exceed 5 mg in any 24-hour period [ see Dosage and Administration, (2.4) and Clinical Pharmacology (12.3) ].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Pregnancy: Based on animal data, may cause fetal harm (8.1)
8.1Pregnancy Pregnancy Category C: There are no adequate and well-controlled studies in pregnant women; therefore, zolmitriptan should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. 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. 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. When zolmitriptan was administered to pregnant rabbits during the period of organogenesis at oral doses of 3, 10, and 30 mg/kg/day (plasma AUCs ≈1, 11, and 42 times the human AUC at the MRHD), there were increases in embryolethality and in fetal malformations and variations. The no-effect dose for adverse effects on embryo-fetal development was associated with a plasma AUC similar to that in humans at the MRHD.
When female rats were given zolmitriptan during gestation, parturition, and lactation at oral doses of 25, 100, and 400 mg/kg/day (plasma AUCs ≈70, 280, and 1100 times that in human at the MRHD), an increased incidence of hydronephrosis was found in the offspring. The no-effect dose was associated with a plasma AUC ≈280 times that in humans at the MRHD.
8.3Nursing Mothers It is not known whether zolmitriptan is excreted in human milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants from zolmitriptan, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. In rats, oral dosing with zolmitriptan resulted in levels in milk up to 4 times higher than in plasma.
8.4Pediatric Use The safety and effectiveness in pediatric patients have not been established. Therefore, zolmitriptan is not recommended for use in patients under 18 years of age. One randomized, placebo-controlled clinical trial of zolmitriptan (2.5, 5 and 10 mg) evaluated 696 pediatric patients (aged 12 to 17 years) with migraines.
This study did not demonstrate the efficacy of zolmitriptan compared to placebo in the treatment of migraine in adolescents. Adverse reactions in the adolescent patients treated with zolmitriptan were similar in nature and frequency to those reported in clinical trials in adults treated with zolmitriptan. Zolmitriptan has not been studied in pediatric patients less than 12 years old.
In the postmarketing experience with triptans, including zolmitriptan, there were no additional adverse reactions seen in pediatric patients that were not seen in adults.
8.5Geriatric Use Clinical studies of zolmitriptan did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
A cardiovascular evaluation is recommended for geriatric patients who have other cardiovascular risk factors (e.g., diabetes, hypertension, smoking, obesity, strong family history of coronary artery disease) prior to receiving zolmitriptan [ see Warnings and Precautions (5.1) ]. The pharmacokinetics of zolmitriptan were similar in geriatric patients (aged >65 years) com…
🤰 Pregnancy ▾
8.1Pregnancy Pregnancy Category C: There are no adequate and well-controlled studies in pregnant women; therefore, zolmitriptan should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. 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. 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. When zolmitriptan was administered to pregnant rabbits during the period of organogenesis at oral doses of 3, 10, and 30 mg/kg/day (plasma AUCs ≈1, 11, and 42 times the human AUC at the MRHD), there were increases in embryolethality and in fetal malformations and variations. The no-effect dose for adverse effects on embryo-fetal development was associated with a plasma AUC similar to that in humans at the MRHD.
When female rats were given zolmitriptan during gestation, parturition, and lactation at oral doses of 25, 100, and 400 mg/kg/day (plasma AUCs ≈70, 280, and 1100 times that in human at the MRHD), an increased incidence of hydronephrosis was found in the offspring. The no-effect dose was associated with a plasma AUC ≈280 times that in humans at the MRHD.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness in pediatric patients have not been established. Therefore, zolmitriptan is not recommended for use in patients under 18 years of age. One randomized, placebo-controlled clinical trial of zolmitriptan (2.5, 5 and 10 mg) evaluated 696 pediatric patients (aged 12 to 17 years) with migraines.
This study did not demonstrate the efficacy of zolmitriptan compared to placebo in the treatment of migraine in adolescents. Adverse reactions in the adolescent patients treated with zolmitriptan were similar in nature and frequency to those reported in clinical trials in adults treated with zolmitriptan. Zolmitriptan has not been studied in pediatric patients less than 12 years old.
In the postmarketing experience with triptans, including zolmitriptan, there were no additional adverse reactions seen in pediatric patients that were not seen in adults.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical studies of zolmitriptan did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
A cardiovascular evaluation is recommended for geriatric patients who have other cardiovascular risk factors (e.g., diabetes, hypertension, smoking, obesity, strong family history of coronary artery disease) prior to receiving zolmitriptan [ see Warnings and Precautions (5.1) ]. The pharmacokinetics of zolmitriptan were similar in geriatric patients (aged >65 years) compared to younger patients [ see Clinical Pharmacology (12.3) ].
🆘 Overdosage ▾
10 OVERDOSAGE There is no experience with acute overdose of zolmitriptan. Clinical study subjects who received single 50 mg oral doses of zolmitriptan commonly experienced sedation. 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. The elimination half-life of zolmitriptan is 3 hours [ see Clinical Pharmacology (12.1) ]; therefore, monitor patients after overdose with zolmitriptan for at least 15 hours or until symptoms or signs resolve. It is unknown what effect hemodialysis or peritoneal dialysis has on the plasma concentrations of zolmitriptan.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action 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-HT 1A receptors. Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system.
The therapeutic activity of zolmitriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT 1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
12.3Pharmacokinetics Absorption, Distribution, Metabolism, and Excretion Absorption Zolmitriptan is well absorbed after oral administration for zolmitriptan orally disintegrating tablets. Zolmitriptan displays linear kinetics over the dose range of 2.5 to 50 mg. The AUC and C max of zolmitriptan are similar following administration of zolmitriptan tablets and zolmitriptan orally disintegrating tablets, but the T max is somewhat later with zolmitriptan orally disintegrating tablets, with a median T max of 3 hours for zolmitriptan orally disintegrating tablet compared with 1.5 hours for the zolmitriptan tablet.
The AUC, C max , and T max for the active N-desmethyl metabolite are similar for the two formulations. During a moderate to severe migraine attack, mean AUC 0-4 and C max for zolmitriptan, dosed as a zolmitriptan tablet, were decreased by 40% and 25%, respectively, and mean T max was delayed by one-half hour compared to the same patients during a migraine free period. Food has no significant effect on the bioavailability of zolmitriptan.
No accumulation occurred on multiple dosing. Distribution Mean absolute bioavailability is approximately 40%. The mean apparent volume of distribution is 7 L/kg.
Plasma protein binding of zolmitriptan is 25% over the concentration range of 10 to 1000 ng/mL. Metabolism Zolmitriptan is converted to an active N-desmethyl metabolite; the metabolite concentrations are about two-thirds that of zolmitriptan. Because the 5HT 1B/1D potency of the metabolite is 2 to 6 times that of the parent compound, the metabolite may contribute a substantial portion of the overall effect after zolmitriptan administration.
Excretion Total radioactivity recovered in urine and feces was 65% and 30% of the administered dose, respectively. About 8% of the dose was recovered in the urine as unchanged zolmitriptan. Indole acetic acid metabolite accounted for 31% of the dose, followed by N-oxide (7%) and N-desmethyl (4%) metabolites.
The indole acetic acid and N-oxide metabolites are inactive. Mean total plasma clearance is 31.5 mL/min/kg, of which one-sixth is renal clearance. The renal clearance is greater than the glomerular filtration rate suggesting renal tubular secretion.
Special Populations Hepatic Impairment In patients with severe hepatic impairment, the mean C max , T max , and AUC 0-∞ of zolmitriptan were increased 1.5-fold, 2-fold (2 vs. 4 hours), and 3-fold, respectively, compared to subjects with normal hepatic function. Seven out of 27 patients experienced 20 to 80 mm Hg elevations in systolic and/or diastolic blood pressure after a 10 mg zolmitriptan dose.
Adjust the zolmitriptan dose in patients with moderate or severe hepatic impairment [see Dosage and Administration (2.3) and Use in Specific Populations (8.6) ]. Renal Impairment Clearance of zolmitriptan was reduced by 25% in patients with severe renal impairment (Clcr ≥ 5 ≤ 25 mL/min) compared to subjects with normal renal function (Clcr > = 70 mL/min); no significant change in clearance was observed in patients with moderate renal impairment (Clcr ≥ 26 ≤ 50 mL/min).…
🧬 Mechanism of Action ▾
12.1Mechanism of Action 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-HT 1A receptors. Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system.
The therapeutic activity of zolmitriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT 1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING 2.5 mg Orally Disintegrating Tablets - White to off-white, round, flat faced bevelled edge tablets debossed with ‘359’ on one side and ‘L’ on other side. NDC 46708-181-06 Carton of 1 blister of 6 tablets 5 mg Orally Disintegrating Tablets - White to off-white, round, flat faced bevelled edge tablets debossed with ‘360’ on one side and ‘L’ on other side. NDC 46708-182-03 Carton of 1 blister of 3 tablets Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].
Protect from light and moisture.
📋 Description ▾
11 DESCRIPTION Zolmitriptan orally disintegrating tablets contain zolmitriptan, which is a selective 5-hydroxytryptamine 1B/1D (5-HT 1B/1D ) receptor agonist. Zolmitriptan is chemically designated as (S)-4-[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]-2-oxazolidinone and has the following chemical structure: The empirical formula is C 16 H 21 N 3 O 2 , representing a molecular weight of 287.36. Zolmitriptan is a white to off-white crystalline powder that is freely soluble in N,N-dimethyl formamide, dimethyl sulfoxide and practically insoluble in water.
Zolmitriptan orally disintegrating tablets are available as 2.5 mg and 5 mg white to off-white uncoated tablets. The orally disintegrating tablets contain mannitol, microcrystalline cellulose, crospovidone, aspartame [ see Warnings and Precautions (5.9) ], sodium stearyl fumarate, colloidal silicon dioxide, magnesium stearate, orange flavor, modified food starch and triacetin.
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION See FDA Approved Patient Labeling (Patient Information). Myocardial Ischemia and/or Infarction, Prinzmetal’s angina, Other Vasospastic Reactions, and Cerebrovascular Events Inform patients that zolmitriptan may cause serious cardiovascular adverse reactions such as myocardial infarction or stroke, which may result in hospitalization and even death. Although serious cardiovascular reactions can occur without warning symptoms, instruct patients to be alert for the signs and symptoms of chest pain, shortness of breath, weakness, slurring of speech, and instruct them to ask for medical advice when observing any indicative sign or symptoms.
Instruct patients to seek medical advice if they have symptoms of other vasospastic reactions [ see Warnings and Precautions (5.1, 5.2, 5.4, 5.5) ]. Medication Overuse Headache Inform patients that use of drugs to treat acute migraines for 10 or more days per month may lead to an exacerbation of headache, and encourage patients to record headache frequency and drug use (e.g., by keeping a headache diary) [ see Warnings and Precautions (5.6) ]. Serotonin Syndrome Inform patients about the risk of serotonin syndrome with the use of zolmitriptan or other triptans,-particularly during combined use with selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs) [ see Warnings and Precautions (5.7) ].
Pregnancy Inform patients that zolmitriptan should not be used during pregnancy unless the potential benefit justifies the potential risk to the fetus [ see Use in Specific Populations (8.1) ]. Nursing Mothers Advise patients to notify their healthcare provider if they are breastfeeding or plan to breastfeed [ see Use in Specific Populations (8.3) ]. Handling of zolmitriptan orally Disintegrating Tablets Inform patients not to break zolmitriptan oral disintegrating tablets.
Inform patients that the orally disintegrating tablet is packaged in a blister. Instruct patients not to remove the oral disintegrating tablet from the blister until just prior to dosing. Instruct patients that prior to dosing, peel open the blister pack and place the orally disintegrating tablet on the tongue, where it will dissolve and be swallowed with the saliva [ see Dosage and Administration (2.2) ].
Patients with Phenylketonuria Inform patients with phenylketonuria (PKU) that zolmitriptan orally disintegrating tablet contains phenylalanine (a component of aspartame) [ see Warnings and Precautions (5.9) ].