zolmitriptan 5 mg Spray, 6 bottles
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Serotonin-1b and Serotonin-1d Receptor Agonist class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 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:
Where does this data come from?
Ask a licensed pharmacist directly — free, answered by our team.
🧪 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.
Where does this data come from?
IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
💲 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 ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $41.292 | $247.75 / 6 spray |
| Medicaid paysCMS SDUD · 12 mo | $51.97 | $311.84 / 6 spray |
| Medicare drug plans payPart D · Q2 2026 | $67.78 | $406.69 / 6 spray |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| zolmitriptan 5 mgthis 45802-0711-91 | Padagis | 6 bottles | $41.292 | AB | Availability likely | — |
| Zolmitriptan 5 mg 69238-2352-06 | Amneal | 6 bottles | $41.292 | AB | Availability likely | — |
| Zomig 5 mg 64896-0084-12 | Amneal | 6 bottles | $108.943 | AB | Discontinued | +164% |
| zolmitriptan 5 mg 63629-9575-01 | Bryant | 6 bottles | — | AB | FDA listed | — |
| zolmitriptan 5 mg 71335-2947-01 | Bryant | 6 bottles | — | AB | FDA listed | — |
| zolmitriptan 5 mg 72162-1425-02 | Bryant | 6 bottles | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 45802-0711-91 You're viewing this | 6 BOTTLE, SPRAY in 1 CARTON (45802-711-91) / 1 SPRAY in 1 BOTTLE, SPRAY (45802-711-00) | 2021-11-16 | Active |
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE 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 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. • Not recommended in patients with moderate or severe hepatic impairment [ see Dosage and Administration ( 2.2 ) ]. • Zolmitriptan Nasal Spray is a serotonin (5-HT) 1B/1D receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults and pediatric patients 12 years and older ( 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 ) • Not recommended in patients with moderate to severe hepatic impairment ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION • 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 )
2.1Dosing 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 is 5 mg.
If the migraine has not resolved by 2 hours after taking zolmitriptan, 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 in the treatment of an average of more than four headaches in a 30-day period has not been established.
2.2Dosing 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 ) ].
2.3Dosing 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 ( 7.4 ) and Clinical Pharmacology ( 12.3 ) ].
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Nasal Spray 2.5 mg and 5 mg. Nasal Spray: 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 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 ( 7.2 ) and Clinical Pharmacology ( 12.3 ) ] • Known hypersensitivity to zolmitriptan (angioedema and anaphylaxis seen) [ see Adverse Reactions ( 6.2 ) ] • History of ischemic heart disease or coronary artery 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 of an ergot-type medication ( 4 ) • MAO-A inhibitor used in past 2 weeks ( 4 ) • Hypersensitivity to zolmitriptan ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • 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 )
5.1Myocardial 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. 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. Patients with Wolff-Parkinson-White Syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders should not receive zolmitriptan [ see Contraindications ( 4 ) ].
5.3Chest, Throat, Neck, and/or Jaw Pain/Tightness/Pressure As with other 5-HT 1 agonists, sensations of tightness, pain, pressure, and heaviness in the precordium, throat, neck, and jaw commonly occur after treatment with zolmitriptan and is usually non-cardiac in origin. However, if a cardiac origin is suspected, patients should be evaluated. Patients shown to have CAD and those with Prinzmetal’s variant angina should not receive 5-HT 1 agonists [ 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. Discontinue zolmitriptan if a cerebrovascular event occurs.
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, other potentially serious neurological conditions should be excluded. Zolmitriptan should not be administered to patients with a history of stroke or transient ischemic attack [ see Contraindications ( 4 ) ].
5.5 Oth…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS 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 Padagis at 1-866-634-9120 or 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. 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. One patient was withdrawn due to abnormal ECG changes from baseline that were incidentally found 23 days after the last dose of zolmitriptan nasal spray. The most common adverse reactions (≥ 5% and > placebo) in any dosage strength in clinical trials for zolmitriptan nasal spray were: unusual taste, paresthesia, hyperesthesia, and dizziness.
The incidence of adverse reactions was generally dose-related. Table 1 lists the adverse reactions from the controlled clinical trial (Study 1) that occurred in ≥ 2% of patients in either the 2.5 or 5 mg zolmitriptan nasal spray dose groups and with an incidence greater than placebo. Table 1: Adverse reactions in a Placebo-Controlled Study in Adult Patients with Migraine (Study 1) Body System Adverse Reaction Placebo (N=228) Zolmitriptan 2.5 mg (N=224) Zolmitriptan 5 mg (N=236) Atypical Sensations Hyperesthesia 0% 1% 5% Paraesthesia 6% 5% 10% Warm Sensation 2% 4% 0% Ear/Nose/Throat Disorder/Discomfort of nasal cavity 2% 1% 3% Pain and Pressure Sensations Pain Location Specified 1% 2% 4% Throat Pain 1% 4% 4% Throat Tightness 1% <1% 2% Digestive Dry Mouth <1% 3% 2% Nausea 1% 1% 4% Neurological Dizziness 4% 6% 3% Somnolence 2% 1% 4% Other Unusual Taste 3% 17% 21% Asthenia 1% 3% 3% In Study 1, adverse reactions occurring in ≥ 1% and < 2% of patients in all attacks in either zolmitriptan nasal spray dose group and with incidence greater than that of placebo were: abdominal pain, chills, throat pressure, facial edema, chest pressure, palpitation, dysphagia, arthralgia, myalgia, and depersonalization.
The incidence of adverse reactions in controlled clinical trials was not affected by gender, weight, or age of the patients (18-39 vs. 40-65 years of age), or presence of aura. There were insufficient data to assess the impact of race on the incidence of adverse reactions.
Local Adverse Reactions: Among 460 patients using zolmitriptan 2.5 mg or 5 mg in the controlled clinical trial, approximately 3% noted local irritation or soreness at the site of administration. Adverse reactions of any kind, perceived in the nasopharynx (which may include systemic effects of triptans) were severe in about 1% of patients and approximately 57% resolved in 1 hour. Nasopharyngeal examinations, in a subset of patients participating in two long term trials of up to one-year duration, failed to demonstrate any clinically significant changes with repe…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS If co-administered with cimetidine: Maximum single dose of 2.5 mg, not to exceed 5 mg in any 24-hour period. ( 2.3 , 7.4 )
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. Therefore, the use of zolmitriptan in patients receiving MAO-A inhibitors is contraindicated [ see Contraindications ( 4 ) and Clinical Pharmacology ( 12.3 ) ]. 7.3 5-HT 1B/1D agonists (e.g. triptans) 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 ) ].
7.4Cimetidine Following administration of cimetidine, the half-life and AUC of zolmitriptan and its active metabolites 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 ( 2.3 ) and Clinical Pharmacology ( 12.3 ) ].
7.5Selective Serotonin Reuptake Inhibitors/Serotonin Norepinephrine Reuptake Inhibitors and Serotonin Syndrome Cases of life-threatening serotonin syndrome have been reported during combined use of selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs) and triptans [ see Warnings and Precautions ( 5.7 ) ].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Pregnancy: Based on animal data, may cause fetal harm. ( 8.1 )
8.1Pregnancy 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 (see Data) . 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. 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.
8.2Lactation Risk Summary There are no data on the presence of zolmitriptan or its metabolites in human milk, the effects on the breastfed infant, or the effects of zolmitriptan and its metabolites on milk production. In rats, oral dosing with zolmitriptan resulted in levels in milk up to 4 times that in maternal plasma. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for zolmitriptan and any potential adverse effects on the breastfed infant from zolmitriptan or from the underlying maternal condition.
8.4Pediatric Use Safety and effectiveness of zolmitriptan in pediatric patients under 12 years of age have not been established. The efficacy of zolmitriptan nasal spray in the acute treatment of migraine in pediatric patients 12 to 17 years of age was established in a placebo-controlled study with a total of 81 pediatric patients receiving zolmitriptan 2.5 mg and 229 pediatric patients receiving zolmitriptan 5 mg [ see Clinical Studies ( 14.2 ) ]. In an earlier study with a different design, zolmitriptan 5 mg nasal spray was evaluated in the acute treatment of migraine headache in 171 pediatric patients 12 to 17 years of age.
In that study, the efficacy of zolmitriptan nasal spray was not established. The safety of zolmitriptan nasal spray in the acute treatment of migraine in pediatric patients 12 to 17 years of age was established in two placebo-controlled studies with a total of 81 pediatric patients receiving zolmitriptan 2.5 mg and 431 pediatric patients receiving zolmitriptan 5 mg [ see Adverse Reactions ( 6.1 ) ]. The safety profile of zolmitriptan nasal spray in pediatric patients 12 to 17 years of age is similar to the profile observed in adults [ see Adverse Reactions ( 6.1 ) ].
In the postmarketing experience with trip…
🤰 Pregnancy ▾
8.1Pregnancy 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 (see Data) . 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. 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 Safety and effectiveness of zolmitriptan in pediatric patients under 12 years of age have not been established. The efficacy of zolmitriptan nasal spray in the acute treatment of migraine in pediatric patients 12 to 17 years of age was established in a placebo-controlled study with a total of 81 pediatric patients receiving zolmitriptan 2.5 mg and 229 pediatric patients receiving zolmitriptan 5 mg [ see Clinical Studies ( 14.2 ) ]. In an earlier study with a different design, zolmitriptan 5 mg nasal spray was evaluated in the acute treatment of migraine headache in 171 pediatric patients 12 to 17 years of age.
In that study, the efficacy of zolmitriptan nasal spray was not established. The safety of zolmitriptan nasal spray in the acute treatment of migraine in pediatric patients 12 to 17 years of age was established in two placebo-controlled studies with a total of 81 pediatric patients receiving zolmitriptan 2.5 mg and 431 pediatric patients receiving zolmitriptan 5 mg [ see Adverse Reactions ( 6.1 ) ]. The safety profile of zolmitriptan nasal spray in pediatric patients 12 to 17 years of age is similar to the profile observed in adults [ see Adverse Reactions ( 6.1 ) ].
In the postmarketing experience with triptans, including zolmitriptan, there is a limited number of reports that describe pediatric patients who have experienced clinically serious adverse events; those that were reported are similar in nature to those reported rarely 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.
Geriatric patients who have other cardiovascular risk factors (e.g., diabetes, hypertension, smoking, obesity, strong family history of coronary artery disease) should have a cardiovascular evaluation 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. 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.
🧬 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. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are 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 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. Zolmitriptan was detected in plasma by 5 minutes and peak plasma concentration generally was achieved by 3 hours.
The time at which maximum plasma concentrations were observed was similar after single (1 day) or multiple (4 days) nasal dosing. Plasma concentrations of zolmitriptan are sustained for 4 to 6 hours after dosing. Zolmitriptan and its active N-desmethyl metabolite display linear kinetics after single or multiple doses of zolmitriptan nasal spray over the dose range of 0.1 to 10 mg.
The pharmacokinetics of the N-desmethyl metabolite are similar to that of zolmitriptan for all nasal spray dosages. The N-desmethyl metabolite is detected in plasma by 15 minutes and peak plasma concentration is generally achieved by 3 hours after administration. Food has no significant effect on the bioavailability of zolmitriptan.
Distribution Plasma protein binding of zolmitriptan is 25% over the concentration range of 10-1000 ng/mL. The mean apparent volume of distribution for zolmitriptan nasal spray formulation is
8.4L/kg. Metabolism Zolmitriptan is converted to an active N-desmethyl metabolite such that 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 The mean elimination half-life for zolmitriptan and N-desmethyl metabolite following single or multiple nasal spray administration are approximately 3 hours, similar to the half-life values seen after oral tablet administration. In a study with orally administered zolmitriptan, total radioactivity recovered in urine and feces was 65% and 30% of the administered dose, respectively. In urine, unchanged zolmitriptan and N-desmethyl metabolite accounted for 8% and 4% of the dose, respectively, whereas the inactive indole acetic acid and N-oxide metabolites accounted for 31% and 7% of the dose, respectively.
Mean total plasma clearance for zolmitriptan nasal spray is 25.9 mL/min/kg, of which one-sixth is renal clearance. The renal clearance is greater than the glomerular filtration rate suggesting renal tubular secretion. Specific Populations Age: The pharmacokinetics of orally administered zolmitriptan in healthy elderly non-migraineur volunteers (age 65-76 yrs) was similar to those in younger non-migraineur volunteers (age 18-39 yrs).
Sex: Mean plasma concentrations of orally administered zolmitriptan were up to 1.5-fold higher in females than males. Race: There are no significant differences in the pharmacokinetics of orally administered zolmitriptan in Japanese and Cau…
🧬 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. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are 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 The Zolmitriptan Nasal Spray device is a white plastic device, labeled to indicate the nominal dose. Each Zolmitriptan Nasal Spray device administers a single dose of zolmitriptan. Zolmitriptan Nasal Spray, USP is supplied as a clear to pale yellow solution of zolmitriptan, buffered to a pH 5.0.
Each Zolmitriptan Nasal Spray device contains 2.5 mg or 5 mg of zolmitriptan in a 100 μL unit dose aqueous buffered solution containing citric acid, anhydrous, USP, disodium phosphate dodecahydrate USP, benzalkonium chloride solution NF and purified water USP. 2.5 mg Zolmitriptan Nasal Spray is supplied in boxes of 6 single-use nasal spray units. (NDC 45802-606-91) 5 mg Zolmitriptan Nasal Spray is supplied in boxes of 6 single-use nasal spray units.
(NDC 45802-711-91) Each Zolmitriptan Nasal Spray single dose unit spray supplies 2.5 and 5 mg, respectively, of zolmitriptan. The Zolmitriptan Nasal Spray unit must be discarded after use. Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].
📋 Description ▾
11 DESCRIPTION Zolmitriptan Nasal Spray, USP contains 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 almost white powder that is readily soluble in water.
Zolmitriptan Nasal Spray is supplied as a clear to pale yellow solution of zolmitriptan, buffered to a pH 5.0. Each Zolmitriptan Nasal Spray contains 2.5 mg or 5 mg of zolmitriptan in a 100-μL unit dose aqueous buffered solution containing citric acid, anhydrous, USP, disodium phosphate dodecahydrate USP, benzalkonium chloride solution NF and purified water USP. Zolmitriptan Nasal Spray is hypertonic.
The osmolarity of Zolmitriptan Nasal Spray for 2.5 mg is 358 to 396 mOsmol, and for 5 mg is 411 to 455 mOsmol. chemical-structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Risk of Myocardial Ischemia and/or Infarction, Prinzmetal’s angina, Other Vasospasm-related Events, and Cerebrovascular Events Inform patients that zolmitriptan may cause serious cardiovascular side effects such as myocardial infarction or stroke, which may result in hospitalization and even death. Although serious cardiovascular events can occur without warning symptoms, patients should be alert for the signs and symptoms of chest pain, shortness of breath, weakness, slurring of speech, and should ask for medical advice when observing any indicative sign or symptoms [ see Warnings and Precautions ( 5.1 , 5.2 , 5.4 , 5.5 ) ].
Medication Overuse Headache Inform patients that use of acute migraine drugs 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 Advise patients to notify their healthcare provider if they are pregnant or plan to become pregnant. Lactation Advise patients to notify their healthcare provider if they are breastfeeding or plan to breastfeed [ see Use in Specific Populations ( 8.2 ) ]. Handling of Zolmitriptan Nasal Spray device The Zolmitriptan Nasal Spray device is a white plastic device, labeled to indicate the nominal dose.
The device is packaged in individual plastic packs and supplied in boxes of 6 single-use nasal spray devices. Caution patients to not remove the device from the plastic pack prior to dosing. The Zolmitriptan Nasal Spray device is placed in a nostril and actuated to deliver a single dose.
Caution patients to avoid spraying the contents of the device in their eyes. Manufactured By Padagis Yeruham, Israel Distributed By Padagis TM Allegan, MI 49010 www.padagis.com Rev 11-22