IMITREX sumatriptan 4 mg/.5mL Injection, 2 syringes — NDC 0173-0739-00 (Billing 00173-0739-00)
This is a package of 2 syringes of IMITREX sumatriptan 4 mg/.5mL Injection from GlaxoSmithKline LLC, marketed since Apr 2006 and currently FDA-listed; retail pharmacies pay about $463.07 per mL (NADAC). It is the main listing for this product, which comes in 2 package sizes.
Identity & classification
Regulatory identifiers FDA, NLM and CMS codes for this package
Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification
- GSN (GCN sequence number): 060499
- GCN: 26666
- HICL (First Databank): 006587
- AHFS class code: 28:32.28.00
- RxCUI (RxNorm): 758523
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
- RxNorm (NLM RxNav) · catalog refreshed Oct 1, 2026
- Medi-Span GPI (licensed)
- First Databank (licensed) · refreshed Oct 1, 2026
RxNorm drug class
This medicine belongs to the Serotonin-1b and Serotonin-1d Receptor Agonist class.
Where does this data come from?
- RxClass (NLM) · catalog refreshed Oct 1, 2026
Clinical
Sumatriptan injection is used to treat the symptoms of migraine headaches (severe, throbbing headaches that sometimes come with nausea and a strong reaction to sound and light). Sumatriptan injection is also used to treat the symptoms of cluster headaches (severe headaches usually on one side of the head or around one eye). Sumatriptan is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and stops the release of certain natural substances that cause pain, nausea, and othe...
Read the full MedlinePlus article ↗- Sumatriptan injection treats a migraine or cluster headache that's already started — it's designed to stop an attack, not prevent future ones. It works by narrowing certain blood v...
- What exactly does sumatriptan injection do — will it prevent my migraines from coming back?
- You inject it subcutaneously — meaning just under the skin, not into a vein or muscle. Studies show it works whether you inject it in the arm or thigh, and whether you use a manual...
- How do I use the injection, and does it matter where on my body I inject it?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Sumatriptan — tap one for details:
Where does this data come from?
- MedlinePlus (NLM) · refreshed Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
Ask a licensed pharmacist directly — free, answered by our team.
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 mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $463.073 | $463.07 / 1 ml |
| Medicaid paysCMS SDUD · 12 mo | $490.94 | $490.94 / 1 ml |
| Medicare drug plans payPart D · Q2 2026 | $474.76 | $474.76 / 1 ml |
| Medicare Part B allowsASP · J3030 | No ASP payment limit on file for J3030 this quarter. | |
Where does this data come from?
- CMS NADAC weekly file · file of Sep 30, 2026
- CMS ASP pricing files · refreshed Sep 20, 2026
- CMS Medicaid State Drug Utilization Data · through Q1 2026
- CMS Part D plan pricing files · refreshed Sep 24, 2026
- VA National Acquisition Center price file
Billing & reimbursement
Where does this data come from?
- CMS ASP NDC-HCPCS crosswalk · refreshed Sep 22, 2026
- DMEPDAC NDC-HCPCS crosswalk
- openFDA NSDE billing units · refreshed Sep 7, 2026
Packaging — all sizes for this product
| Package NDC | Description | Per unit | Per pack | Marketing start | Marketing end | Status |
|---|---|---|---|---|---|---|
| 00173-0739-00 You're viewing this Main listing | 2 SYRINGE in 1 PACKAGE / .5 mL in 1 SYRINGE | $463.07 / mL | $463.07 | 2006-04-06 | — | Active |
| 00173-0739-02 0173-0739-02 | 2 SYRINGE in 1 CARTON / .5 mL in 1 SYRINGE | — | — | 2006-04-06 | — | Active |
Pack size FAQ
What quantity is in this package?
How does this package differ from NDC 00173-0739-02?
What NDC number is used to bill for this package of IMITREX sumatriptan 4 mg/.5mL Injection?
Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.
Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Imitrex 4 mg/.5mLthis 00173-0739-00 | GlaxoSmithKline | 2 syringes | $463.073 | AB | Availability likely | — |
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA Orange Book · refreshed Oct 3, 2026
- CMS NADAC weekly file · file of Sep 30, 2026
Availability & generic status
FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.
Where does this data come from?
- FDA Orange Book · refreshed Oct 3, 2026
What it looks like
Where does this data come from?
- FDA label on DailyMed · label index refreshed Oct 1, 2026
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.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
-
3.8 mg / 0.5 mL
UNII 451W47IQ8X
Sodium chloride is common table salt. It's used in medicines as a buffer to maintain proper pH, as a filler to add bulk, or to adjust the osmotic balance in liquid formulations.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
2 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
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.- FDA label on DailyMed · label index refreshed Oct 1, 2026
- FDA openFDA NDC Directory · synced Oct 1, 2026
Inactive ingredient FAQ
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Manufacturer & labeler
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- Drugs@FDA
Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE IMITREX injection is indicated in adults for (1) the acute treatment of migraine, with or without aura, and (2) the acute treatment of cluster headache. Limitations of Use • Use only if a clear diagnosis of migraine or cluster headache has been established. If a patient has no response to the first migraine or cluster headache attack treated with IMITREX injection, reconsider the diagnosis before IMITREX injection is administered to treat any subsequent attacks. • IMITREX injection is not indicated for the prevention of migraine or cluster headache attacks.
IMITREX injection is a serotonin (5-HT 1B/1D ) receptor agonist (triptan) indicated for: • Acute treatment of migraine with or without aura in adults. ( 1 ) • Acute treatment of cluster headache in adults. ( 1 ) Limitations of Use • Use only if a clear diagnosis of migraine or cluster headache has been established.
( 1 ) • Not indicated for the prophylactic therapy of migraine or cluster headache attacks. ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION • For subcutaneous use only. ( 2.1 ) • Acute treatment of migraine: single dose of 4 mg or 6 mg. ( 2.1 ) • Acute treatment of cluster headache: single dose of 6 mg. ( 2.1 ) • Maximum dose in a 24-hour period: 12 mg, separate doses by at least 1 hour. ( 2.1 ) • The needle shield of the prefilled syringe contains dry natural rubber (a latex derivative) which may cause allergic reactions in latex-sensitive patients. ( 2.2 )
2.1Dosing Information The maximum single recommended adult dose of IMITREX injection for the acute treatment of migraine or cluster headache is 6 mg injected subcutaneously. For the treatment of migraine, if side effects are dose limiting, the lower dose of 4 mg may be used [see Clinical Studies ( 14.1 )] . For the treatment of cluster headache, the efficacy of lower doses has not been established.
The maximum cumulative dose that may be given in 24 hours is 12 mg, two 6-mg injections separated by at least 1 hour. A second 6-mg dose should only be considered if some response to a first injection was observed.
2.2Administration Using the IMITREX STATdose Pen An autoinjector device (IMITREX STATdose Pen) is available for use with 4-mg and 6-mg prefilled syringe cartridges. With this device, the needle penetrates approximately 1/4 inch (5 to 6 mm). The injection is intended to be given subcutaneously, and intramuscular or intravascular delivery must be avoided.
Instruct patients on the proper use of IMITREX STATdose Pen and direct them to use injection sites with an adequate skin and subcutaneous thickness to accommodate the length of the needle. The needle shield of the prefilled syringe contains dry natural rubber (a latex derivative) [see Warnings and Precautions (5.9)] .
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Injection: 4-mg and 6-mg single-dose prefilled syringe cartridges for use with the IMITREX STATdose Pen. Each 0.5 mL injection contains 5.6 mg or 8.4 mg of sumatriptan succinate equivalent to 4 mg or 6 mg of sumatriptan, respectively. Injection: 4- and 6-mg single-dose prefilled syringe cartridges for use with IMITREX STATdose Pen. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS IMITREX injection is contraindicated in patients with: • Ischemic coronary artery disease (CAD) (angina pectoris, history of myocardial infarction, or documented silent ischemia) 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 or transient ischemic attack (TIA) or history of hemiplegic or basilar migraine because these patients are at a higher risk of stroke [s ee Warnings and Precautions ( 5.4 )] . • Peripheral vascular disease [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 ergotamine-containing medication, ergot-type medication (such as dihydroergotamine or methysergide), or another 5-hydroxytryptamine 1 (5-HT 1 ) agonist [see Drug Interactions ( 7.1 , 7.3 )] . • Concurrent administration of a monoamine oxidase (MAO)-A inhibitor or recent (within 2 weeks) use of an MAO-A inhibitor [see Drug Interactions ( 7.2 ), Clinical Pharmacology ( 12.3 )]. • Hypersensitivity to IMITREX (angioedema and anaphylaxis seen) [see Warnings and Precautions ( 5.9 )] . • Severe hepatic impairment [see Clinical Pharmacology ( 12.3 )] . • History of coronary artery disease or coronary artery vasospasm.
( 4 ) • 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 ergotamine-containing medication.
( 4 ) • Concurrent or recent (past 2 weeks) use of monoamine oxidase-A inhibitor. ( 4 ) • Hypersensitivity to IMITREX (angioedema and anaphylaxis seen). ( 4 ) • Severe hepatic impairment.
( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Myocardial ischemia/infarction and Prinzmetal’s angina: Perform cardiac evaluation in patients with multiple cardiovascular risk factors. ( 5.1 ) • Arrhythmias: Discontinue IMITREX 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 IMITREX if occurs. ( 5.4 ) • Gastrointestinal ischemic reactions and peripheral vasospastic reactions: Discontinue IMITREX if occurs. ( 5.5 ) • Medication overuse headache: Detoxification may be necessary.
( 5.6 ) • Serotonin syndrome: Discontinue IMITREX if occurs. ( 5.7 ) • Seizures: Use with caution in patients with epilepsy or a lowered seizure threshold. ( 5.10 )
5.1Myocardial Ischemia, Myocardial Infarction, and Prinzmetal’s Angina The use of IMITREX injection is contraindicated in patients with ischemic or vasospastic CAD. There have been rare reports of serious cardiac adverse reactions, including acute myocardial infarction, occurring within a few hours following administration of IMITREX injection. Some of these reactions occurred in patients without known CAD.
IMITREX injection may cause coronary artery vasospasm (Prinzmetal’s angina), even in patients without a history of CAD. Perform a cardiovascular evaluation in triptan-naive patients who have multiple cardiovascular risk factors (e.g., increased age, diabetes, hypertension, smoking, obesity, strong family history of CAD) prior to receiving IMITREX injection. If there is evidence of CAD or coronary artery vasospasm, IMITREX injection is contraindicated.
For patients with multiple cardiovascular risk factors who have a negative cardiovascular evaluation, consider administering the first dose of IMITREX injection in a medically supervised setting and performing an electrocardiogram (ECG) immediately following administration of IMITREX injection. For such patients, consider periodic cardiovascular evaluation in intermittent long‑term users of IMITREX injection.
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 IMITREX injection if these disturbances occur. IMITREX injection is contraindicated in patients with Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders.
5.3Chest, Throat, Neck, and/or Jaw Pain/Tightness/Pressure Sensations of tightness, pain, pressure, and heaviness in the precordium, throat, neck, and jaw commonly occur after treatment with IMITREX injection and are usually non-cardiac in origin. However, perform a cardiac evaluation if these patients are at high cardiac risk. The use of IMITREX injection is contraindicated in patients with CAD and those with Prinzmetal’s variant angina.
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. Also, patients with migraine may be at increased risk of certain cerebrovascular events (e.g., stroke, hemorrhage, TIA).
Discontinue IMITREX injection if a cerebrovascular event occurs. Before treating headaches in patients not previously diagnosed with migraine or cluster headache or in patients who present with atypical symptoms, exclude other potentially serious neurological conditions. IMITREX injection is contraindicated in patients with a history of stroke or TIA.
5.5Other Vasospasm Reactions IMITREX injection may cause non-co… [Excerpted — this section continues on DailyMed.]
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following serious adverse reactions are described below and elsewhere in the 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 )] • Hypersensitivity reactions [see Contraindications ( 4 ), Warnings and Precautions ( 5.9 )] • Seizures [see Warnings and Precautions ( 5.10 )] Most common adverse reactions (≥5% and >placebo) were injection site reactions, tingling, dizziness/vertigo, warm/hot sensation, burning sensation, feeling of heaviness, pressure sensation, flushing, feeling of tightness, and numbness.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact GlaxoSmithKline at 1-888-825-5249 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. Migraine Headache Table 1 lists adverse reactions that occurred in 2 U.S. placebo‑controlled clinical trials in patients with migraines (Studies 2 and 3) following either a single 6‑mg dose of IMITREX injection or placebo. Only reactions that occurred at a frequency of 2% or more in groups treated with IMITREX injection 6 mg and that occurred at a frequency greater than the placebo group are included in Table 1 .
Table 1. Adverse Reactions in Pooled Placebo-Controlled Trials in Patients with Migraine (Studies 2 and 3) Adverse Reaction IMITREX Injection 6 mg Subcutaneous (n = 547) % Placebo (n = 370) % Atypical sensations 42 9 Tingling 14 3 Warm/hot sensation 11 4 Burning sensation 7 <1 Feeling of heaviness 7 1 Pressure sensation 7 2 Feeling of tightness 5 <1 Numbness 5 2 Feeling strange 2 <1 Tight feeling in head 2 <1 Cardiovascular Flushing 7 2 Chest discomfort 5 1 Tightness in chest 3 <1 Pressure in chest 2 <1 Ear, nose, and throat Throat discomfort 3 <1 Discomfort: nasal cavity/sinuses 2 <1 Injection site reaction a 59 24 Miscellaneous Jaw discomfort 2 0 Musculoskeletal Weakness 5 <1 Neck pain/stiffness 5 <1 Myalgia 2 <1 Neurological Dizziness/vertigo 12 4 Drowsiness/sedation 3 2 Headache 2 <1 Skin Sweating 2 1 a Includes injection site pain, stinging/burning, swelling, erythema, bruising, bleeding.
The incidence of adverse reactions in controlled clinical trials was not affected by gender or age of the patients. There were insufficient data to assess the impact of race on the incidence of adverse reactions. Cluster Headache In the controlled clinical trials assessing the efficacy of IMITREX injection as a treatment for cluster headache (Studies 4 and 5), no new significant adverse reactions were detected that had not already been identified in trials of IMITREX in patients with migraine.
Overall, the frequency of adverse reactions reported in the trials of cluster headache was generally lower than in the migraine trials. Exceptions include reports of paresthesia (5% IMITREX injection, 0% placebo), nausea and vomiting (4% IMITREX injection, 0% placebo), and bronchospasm (1% IMITREX injection, 0% placebo).
6.2Postmarketing Experience The following adverse reactions have been identified during postapproval use of IMITREX tablets, IMITREX nasal spray, and IMITREX injection. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causa… [Excerpted — this section continues on DailyMed.]
🔄 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 IMITREX injection within 24 hours of each other is contraindicated.
7.2Monoamine Oxidase-A Inhibitors MAO-A inhibitors increase systemic exposure by 2-fold. Therefore, the use of IMITREX injection in patients receiving MAO-A inhibitors is contraindicated [see Clinical Pharmacology ( 12.3 )] .
7.3Other 5-HT 1 Agonists Because their vasospastic effects may be additive, coadministration of IMITREX injection and other 5-HT 1 agonists (e.g., triptans) within 24 hours of each other is contraindicated.
7.4Selective Serotonin Reuptake Inhibitors/Serotonin Norepinephrine Reuptake Inhibitors and Serotonin Syndrome Cases of serotonin syndrome have been reported during coadministration of triptans and SSRIs, SNRIs, TCAs, and MAO inhibitors [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 Data from a prospective pregnancy exposure registry and epidemiological studies of pregnant women have not detected an increased frequency of birth defects or a consistent pattern of birth defects among women exposed to sumatriptan compared with the general population (see Data) . In developmental toxicity studies in rats and rabbits, oral administration of sumatriptan to pregnant animals was associated with embryolethality, fetal abnormalities, and pup mortality. When administered by the intravenous route to pregnant rabbits, sumatriptan was embryolethal (see Data) .
In the U.S. general population, the estimated background risk of major birth defects and of miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. The reported rate of major birth defects among deliveries to women with migraine ranged from 2.2% to 2.9% and the reported rate of miscarriage was 17%, which were similar to rates reported in women without migraine. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk: Several studies have suggested that women with migraine may be at increased risk of preeclampsia during pregnancy.
Data Human Data: The Sumatriptan/Naratriptan/TREXIMET (sumatriptan and naproxen sodium) Pregnancy Registry, a population-based international prospective study, collected data for sumatriptan from January 1996 to September 2012. The Registry documented outcomes of 626 infants and fetuses exposed to sumatriptan during pregnancy (528 with earliest exposure during the first trimester, 78 during the second trimester, 16 during the third trimester, and 4 unknown). The occurrence of major birth defects (excluding fetal deaths and induced abortions without reported defects and all spontaneous pregnancy losses) during first-trimester exposure to sumatriptan was 4.2% (20/478 [95% CI: 2.6% to 6.5%]) and during any trimester of exposure was 4.2% (24/576 [95% CI: 2.7% to 6.2%]).
The sample size in this study had 80% power to detect at least a 1.73- to 1.91-fold increase in the rate of major malformations. The number of exposed pregnancy outcomes accumulated during the registry was insufficient to support definitive conclusions about overall malformation risk or for making comparisons of the frequencies of specific birth defects. Of the 20 infants with reported birth defects after exposure to sumatriptan in the first trimester, 4 infants had ventricular septal defects, including one infant who was exposed to both sumatriptan and naratriptan, and 3 infants had pyloric stenosis.
No other birth defect was reported for more than 2 infants in this group. In a study using data from the Swedish Medical Birth Register, live births to women who reported using triptans or ergots during pregnancy were compared with those of women who did not. Of the 2,257 births with first-trimester exposure to sumatriptan, 107 infants were born with malformations (relative risk 0.99 [95% CI: 0.91 to 1.21]).
A study using linked data from the Medical Birth Registry of Norway to the Norwegian Prescription Database compared pregnancy outcomes in women who redeemed prescriptions for triptans during pregnancy, as well as a migraine disease comparison group who redeemed prescriptions for sumatriptan before pregnancy only, compared with a population control group. Of the 415 women who redeemed prescriptions for sumatriptan during the first trimester, 15 had infants with major congenital malformations (OR 1.16 [95% CI: 0.69 to 1.94]) while for the 364 women who redeemed prescriptions for sumatriptan before, but not during, pregnancy, 20 had infants with major congenital malformations (OR 1.83 [95% CI: 1.17 to 2.88]), each compared with the population comparison group.
Additional smaller observational studies evaluating use of sumatriptan during pregnancy have not suggested an increased risk of teratogenicity. Ani… [Excerpted — this section continues on DailyMed.]
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Data from a prospective pregnancy exposure registry and epidemiological studies of pregnant women have not detected an increased frequency of birth defects or a consistent pattern of birth defects among women exposed to sumatriptan compared with the general population (see Data) . In developmental toxicity studies in rats and rabbits, oral administration of sumatriptan to pregnant animals was associated with embryolethality, fetal abnormalities, and pup mortality. When administered by the intravenous route to pregnant rabbits, sumatriptan was embryolethal (see Data) .
In the U.S. general population, the estimated background risk of major birth defects and of miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. The reported rate of major birth defects among deliveries to women with migraine ranged from 2.2% to 2.9% and the reported rate of miscarriage was 17%, which were similar to rates reported in women without migraine. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk: Several studies have suggested that women with migraine may be at increased risk of preeclampsia during pregnancy.
Data Human Data: The Sumatriptan/Naratriptan/TREXIMET (sumatriptan and naproxen sodium) Pregnancy Registry, a population-based international prospective study, collected data for sumatriptan from January 1996 to September 2012. The Registry documented outcomes of 626 infants and fetuses exposed to sumatriptan during pregnancy (528 with earliest exposure during the first trimester, 78 during the second trimester, 16 during the third trimester, and 4 unknown). The occurrence of major birth defects (excluding fetal deaths and induced abortions without reported defects and all spontaneous pregnancy losses) during first-trimester exposure to sumatriptan was 4.2% (20/478 [95% CI: 2.6% to 6.5%]) and during any trimester of exposure was 4.2% (24/576 [95% CI: 2.7% to 6.2%]).
The sample size in this study had 80% power to detect at least a 1.73- to 1.91-fold increase in the rate of major malformations. The number of exposed pregnancy outcomes accumulated during the registry was insufficient to support definitive conclusions about overall malformation risk or for making comparisons of the frequencies of specific birth defects. Of the 20 infants with reported birth defects after exposure to sumatriptan in the first trimester, 4 infants had ventricular septal defects, including one infant who was exposed to both sumatriptan and naratriptan, and 3 infants had pyloric stenosis.
No other birth defect was reported for more than 2 infants in this group. In a study using data from the Swedish Medical Birth Register, live births to women who reported using triptans or ergots during pregnancy were compared with those of women who did not. Of the 2,257 births with first-trimester exposure to sumatriptan, 107 infants were born with malformations (relative risk 0.99 [95% CI: 0.91 to 1.21]).
A study using linked data from the Medical Birth Registry of Norway to the Norwegian Prescription Database compared pregnancy outcomes in women who redeemed prescriptions for triptans during pregnancy, as well as a migraine disease comparison group who redeemed prescriptions for sumatriptan before pregnancy only, compared with a population control group. Of the 415 women who redeemed prescriptions for sumatriptan during the first trimester, 15 had infants with major congenital malformations (OR 1.16 [95% CI: 0.69 to 1.94]) while for the 364 women who redeemed prescriptions for sumatriptan before, but not during, pregnancy, 20 had infants with major congenital malformations (OR 1.83 [95% CI: 1.17 to 2.88]), each compared with the population comparison group.
Additional smaller observational studies evaluating use of sumatriptan during pregnancy have not suggested an increased risk of teratogenicity. Animal Data: Oral administration of sumatriptan to pregnant rats during the period of organogene… [Excerpted — this section continues on DailyMed.]
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and effectiveness in pediatric patients have not been established. IMITREX injection is not recommended for use in patients younger than 18 years of age. Two controlled clinical trials evaluated IMITREX nasal spray (5 to 20 mg) in 1,248 pediatric migraineurs aged 12 to 17 years who treated a single attack.
The trials did not establish the efficacy of IMITREX nasal spray compared with placebo in the treatment of migraine in pediatric patients. Adverse reactions observed in these clinical trials were similar in nature to those reported in clinical trials in adults. Five controlled clinical trials (2 single-attack trials, 3 multiple-attack trials) evaluating oral IMITREX (25 to 100 mg) in pediatric patients aged 12 to 17 years enrolled a total of 701 pediatric migraineurs.
These trials did not establish the efficacy of oral IMITREX compared with placebo in the treatment of migraine in pediatric patients. Adverse reactions observed in these clinical trials were similar in nature to those reported in clinical trials in adults. The frequency of all adverse reactions in these patients appeared to be both dose- and age‑dependent, with younger patients reporting reactions more commonly than older pediatric patients.
Postmarketing experience documents that serious adverse reactions have occurred in the pediatric population after use of subcutaneous, oral, and/or intranasal IMITREX. These reports include reactions similar in nature to those reported rarely in adults, including stroke, visual loss, and death. A myocardial infarction has been reported in a 14-year-old male following the use of oral IMITREX; clinical signs occurred within 1 day of drug administration.
Clinical data to determine the frequency of serious adverse reactions in pediatric patients who might receive subcutaneous, oral, or intranasal IMITREX are not presently available.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical trials of IMITREX injection did not include sufficient numbers of patients aged 65 years and older to determine whether they respond differently from younger patients. 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 CAD) prior to receiving IMITREX injection [see Warnings and Precautions ( 5.1 )] .
🆘 Overdosage ▾
10 OVERDOSAGE Coronary vasospasm was observed after intravenous administration of IMITREX injection [see Contraindications ( 4 )] . Overdoses would be expected from animal data (dogs at 0.1 g/kg, rats at 2 g/kg) to possibly cause convulsions, tremor, inactivity, erythema of the extremities, reduced respiratory rate, cyanosis, ataxia, mydriasis, injection site reactions (desquamation, hair loss, and scab formation), and paralysis. The elimination half-life of sumatriptan is about 2 hours [see Clinical Pharmacology ( 12.3 )] ; therefore, monitoring of patients after overdose with IMITREX injection should continue for at least 10 hours or while symptoms or signs persist.
It is unknown what effect hemodialysis or peritoneal dialysis has on the serum concentrations of sumatriptan.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Sumatriptan binds with high affinity to human cloned 5-HT 1B / 1D receptors. Sumatriptan presumably exerts its therapeutic effects in the treatment of migraine and cluster headaches through agonist effects at the 5-HT 1B / 1D receptors on intracranial blood vessels and sensory nerves of the trigeminal system, which result in cranial vessel constriction and inhibition of pro‑inflammatory neuropeptide release.
12.2Pharmacodynamics Blood Pressure Significant elevation in blood pressure, including hypertensive crisis, has been reported in patients with and without a history of hypertension [see Warnings and Precautions ( 5.8 )] . Peripheral (Small) Arteries In healthy volunteers (N = 18), a trial evaluating the effects of sumatriptan on peripheral (small vessel) arterial reactivity failed to detect a clinically significant increase in peripheral resistance. Heart Rate Transient increases in blood pressure observed in some patients in clinical trials carried out during sumatriptan’s development as a treatment for migraine were not accompanied by any clinically significant changes in heart rate.
12.3Pharmacokinetics Absorption The bioavailability of sumatriptan via subcutaneous site injection to 18 healthy male subjects was 97% ± 16% of that obtained following intravenous injection. After a single 6-mg subcutaneous manual injection into the deltoid area of the arm in 18 healthy males (age: 24 ± 6 years, weight: 70 kg), the maximum serum concentration (C max ) of sumatriptan was (mean ± standard deviation) 74 ± 15 ng/mL and the time to peak concentration (T max ) was 12 minutes after injection (range: 5 to 20 minutes) .
In this trial, the same dose injected subcutaneously in the thigh gave a C max of 61 ± 15 ng/mL by manual injection versus 52 ± 15 ng/mL by autoinjector techniques. The T max or amount absorbed was not significantly altered by either the site or technique of injection. Distribution Protein binding, determined by equilibrium dialysis over the concentration range of 10 to 1,000 ng/mL is low, approximately 14% to 21%.
The effect of sumatriptan on the protein binding of other drugs has not been evaluated. Following a 6-mg subcutaneous injection into the deltoid area of the arm in 9 males (mean age: 33 years, mean weight: 77 kg) the volume of distribution central compartment of sumatriptan was 50 ± 8 liters and the distribution half‑life was 15 ± 2 minutes . Metabolism In vitro studies with human microsomes suggest that sumatriptan is metabolized by MAO, predominantly the A isoenzyme.
Most of a radiolabeled dose of sumatriptan excreted in the urine is the major metabolite indole acetic acid (IAA) or the IAA glucuronide, both of which are inactive. Elimination After a single 6-mg subcutaneous dose, 22% ± 4% was excreted in the urine as unchanged sumatriptan and 38% ± 7% as the IAA metabolite. Following a 6-mg subcutaneous injection into the deltoid area of the arm, the systemic clearance of sumatriptan was 1,194 ± 149 mL/min and the terminal half-life was 115 ± 19 minutes.
Specific Populations Age: The pharmacokinetics of sumatriptan in the elderly (mean age: 72 years, 2 males and 4 females) and in subjects with migraine (mean age: 38 years, 25 males and 155 females) were similar to that in healthy male subjects (mean age: 30 years). Patients with Hepatic Impairment: The effect of mild to moderate hepatic disease on the pharmacokinetics of subcutaneously administered sumatriptan has been evaluated. There were no significant differences in the pharmacokinetics of subcutaneously administered sumatriptan in moderately hepatically impaired subjects compared with healthy controls.
The pharmacokinetics of subcutaneously administered sumatriptan in patients with severe hepatic impairment has not been studied. The use of IMITREX injection in this population is contraindicated [see Contraindications ( 4 )] . Racial Groups: The systemic clearance and C max of subcutaneous sumatripta… [Excerpted — this section continues on DailyMed.]
🧬 Mechanism of Action ▾
12.1Mechanism of Action Sumatriptan binds with high affinity to human cloned 5-HT 1B / 1D receptors. Sumatriptan presumably exerts its therapeutic effects in the treatment of migraine and cluster headaches through agonist effects at the 5-HT 1B / 1D receptors on intracranial blood vessels 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 IMITREX injection contains sumatriptan (base) as the succinate salt and is supplied as a clear, colorless to pale yellow, sterile, nonpyrogenic solution as follows: Prefilled Syringe and/or Autoinjector Pen: The needle shield of the prefilled syringe contains dry natural rubber (a latex derivative) that has the potential to cause allergic reactions in latex-sensitive individuals. Each pack contains a Patient Information and Instructions for Use leaflet. • IMITREX STATdose System, 4 mg, containing 1 IMITREX STATdose Pen, 2 prefilled single-dose syringe cartridges, and 1 carrying case (NDC 0173-0739-00). • IMITREX STATdose System, 6 mg, containing 1 IMITREX STATdose Pen, 2 prefilled single-dose syringe cartridges, and 1 carrying case (NDC 0173-0479-00). • Two 4-mg single-dose prefilled syringe cartridges for use with IMITREX STATdose System (NDC 0173-0739-02). • Two 6-mg single-dose prefilled syringe cartridges for use with IMITREX STATdose System (NDC 0173-0478-00).
Store between 2° and 30°C (36° and 86°F). Protect from light.
📋 Description ▾
11 DESCRIPTION IMITREX injection contains sumatriptan succinate, a selective 5-HT 1B/1D receptor agonist. Sumatriptan succinate is chemically designated as 3-[2-(dimethylamino)ethyl]-N-methyl-indole-5-methanesulfonamide succinate (1:1), and it has the following structure: The empirical formula is C 14 H 21 N 3 O 2 S•C 4 H 6 O 4 , representing a molecular weight of 413.5. Sumatriptan succinate is a white to off-white powder that is readily soluble in water and in saline.
IMITREX injection is a clear, colorless to pale yellow, sterile, nonpyrogenic solution for subcutaneous injection. Each 0.5 mL of IMITREX injection 8-mg/mL solution contains 5.6 mg of sumatriptan succinate equivalent to 4 mg of sumatriptan and 3.8 mg of sodium chloride, USP in Water for Injection, USP. Each 0.5 mL of IMITREX injection 12-mg/mL solution contains 8.4 mg of sumatriptan succinate equivalent to 6 mg of sumatriptan and 3.5 mg of sodium chloride, USP in Water for Injection, USP.
The pH range of both solutions is approximately 4.2 to 5.3. The osmolality of both injections is 291 mOsmol. Sumatriptan Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information and Instructions for Use). Risk of Myocardial Ischemia and/or Infarction, Prinzmetal’s Angina, Other Vasospasm-Related Events, Arrhythmias, and Cerebrovascular Events Inform patients that IMITREX injection may cause serious cardiovascular side effects such as myocardial infarction or stroke. Although serious cardiovascular events can occur without warning symptoms, patients should be alert for the signs and symptoms of chest pain, shortness of breath, irregular heartbeat, significant rise in blood pressure, weakness, and slurring of speech, and should ask for medical advice if any indicative sign or symptoms are observed.
Apprise patients of the importance of this follow-up [see Warnings and Precautions ( 5.1 , 5.2 , 5.4 , 5.5 , 5.8 )] . Hypersensitivity Reactions Inform patients that anaphylactic reactions have occurred in patients receiving IMITREX injection. Such reactions can be life-threatening or fatal.
In general, anaphylactic reactions to drugs are more likely to occur in individuals with a history of sensitivity to multiple allergens [see Contraindications ( 4 ), Warnings and Precautions ( 5.9 )] . Inform latex-sensitive patients that the needle shield of the IMITREX prefilled syringe contains dry natural rubber (a derivative of latex) that may cause allergic reactions in individuals sensitive to latex. Concomitant Use with Other Triptans or Ergot Medications Inform patients that use of IMITREX injection within 24 hours of another triptan or an ergot-type medication (including dihydroergotamine or methysergide) is contraindicated [see Contraindications ( 4 ), Drug Interactions ( 7.1 , 7.3 )] .
Serotonin Syndrome Caution patients about the risk of serotonin syndrome with the use of IMITREX injection or other triptans, particularly during combined use with SSRIs, SNRIs, TCAs, and MAO inhibitors [see Warnings and Precautions ( 5.7 ), Drug Interactions ( 7.4 )] . 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 )] .
Pregnancy Advise patients to notify their healthcare provider if they become pregnant during treatment or plan to become pregnant [see Use in Specific Populations ( 8.1 )] . Lactation Advise breastfeeding women that they may develop transient breast pain when taking IMITREX. Advise breastfeeding women that avoiding breastfeeding for 12 hours after treatment with IMITREX can minimize their infant’s exposure to sumatriptan [see Use in Specific Populations ( 8.2 )] .
Ability to Perform Complex Tasks Treatment with IMITREX injection may cause somnolence and dizziness; instruct patients to evaluate their ability to perform complex tasks after administration of IMITREX injection. How to Use IMITREX injection Instruct patients to read the Instructions for Use before starting therapy. Provide patients instruction on the proper use of IMITREX injection if they are able to self-administer IMITREX injection in medically unsupervised situations.
Instruct patients on storage and disposal of the pen [see How Supplied/Storage and Handling ( 16 )] . Inform patients that the needle in the IMITREX STATdose Pen penetrates approximately 1/4 of an inch (5 to 6 mm). Inform patients that the injection is intended to be given subcutaneously and intramuscular or intravascular delivery should be avoided.
Instruct patients to use injection sites with an adequate skin and subcutaneous thickness to accommodate the length of the needle. IMITREX, IMITREX STATdose System and IMITREX STATdose Pen are trademarks owned by or licensed to the GSK group of companies. The other brand listed is a trademark owned by or licensed to its owner and is not owned by or licensed to the GSK group of companies.
The… [Excerpted — this section continues on DailyMed.]
🧬 Pharmacokinetics ▾
12.3Pharmacokinetics Absorption The bioavailability of sumatriptan via subcutaneous site injection to 18 healthy male subjects was 97% ± 16% of that obtained following intravenous injection. After a single 6-mg subcutaneous manual injection into the deltoid area of the arm in 18 healthy males (age: 24 ± 6 years, weight: 70 kg), the maximum serum concentration (C max ) of sumatriptan was (mean ± standard deviation) 74 ± 15 ng/mL and the time to peak concentration (T max ) was 12 minutes after injection (range: 5 to 20 minutes) .
In this trial, the same dose injected subcutaneously in the thigh gave a C max of 61 ± 15 ng/mL by manual injection versus 52 ± 15 ng/mL by autoinjector techniques. The T max or amount absorbed was not significantly altered by either the site or technique of injection. Distribution Protein binding, determined by equilibrium dialysis over the concentration range of 10 to 1,000 ng/mL is low, approximately 14% to 21%.
The effect of sumatriptan on the protein binding of other drugs has not been evaluated. Following a 6-mg subcutaneous injection into the deltoid area of the arm in 9 males (mean age: 33 years, mean weight: 77 kg) the volume of distribution central compartment of sumatriptan was 50 ± 8 liters and the distribution half‑life was 15 ± 2 minutes . Metabolism In vitro studies with human microsomes suggest that sumatriptan is metabolized by MAO, predominantly the A isoenzyme.
Most of a radiolabeled dose of sumatriptan excreted in the urine is the major metabolite indole acetic acid (IAA) or the IAA glucuronide, both of which are inactive. Elimination After a single 6-mg subcutaneous dose, 22% ± 4% was excreted in the urine as unchanged sumatriptan and 38% ± 7% as the IAA metabolite. Following a 6-mg subcutaneous injection into the deltoid area of the arm, the systemic clearance of sumatriptan was 1,194 ± 149 mL/min and the terminal half-life was 115 ± 19 minutes.
Specific Populations Age: The pharmacokinetics of sumatriptan in the elderly (mean age: 72 years, 2 males and 4 females) and in subjects with migraine (mean age: 38 years, 25 males and 155 females) were similar to that in healthy male subjects (mean age: 30 years). Patients with Hepatic Impairment: The effect of mild to moderate hepatic disease on the pharmacokinetics of subcutaneously administered sumatriptan has been evaluated. There were no significant differences in the pharmacokinetics of subcutaneously administered sumatriptan in moderately hepatically impaired subjects compared with healthy controls.
The pharmacokinetics of subcutaneously administered sumatriptan in patients with severe hepatic impairment has not been studied. The use of IMITREX injection in this population is contraindicated [see Contraindications ( 4 )] . Racial Groups: The systemic clearance and C max of subcutaneous sumatriptan were similar in black (n = 34) and Caucasian (n = 38) healthy male subjects.
Drug Interaction Studies Monoamine Oxidase-A Inhibitors: In a trial of 14 healthy females, pretreatment with an MAO-A inhibitor decreased the clearance of subcutaneous sumatriptan, resulting in a 2-fold increase in the area under the sumatriptan plasma concentration-time curve (AUC), corresponding to a 40% increase in elimination half-life.
🧬 Pharmacodynamics ▾
12.2Pharmacodynamics Blood Pressure Significant elevation in blood pressure, including hypertensive crisis, has been reported in patients with and without a history of hypertension [see Warnings and Precautions ( 5.8 )] . Peripheral (Small) Arteries In healthy volunteers (N = 18), a trial evaluating the effects of sumatriptan on peripheral (small vessel) arterial reactivity failed to detect a clinically significant increase in peripheral resistance. Heart Rate Transient increases in blood pressure observed in some patients in clinical trials carried out during sumatriptan’s development as a treatment for migraine were not accompanied by any clinically significant changes in heart rate.
🔬 Clinical Studies ▾
14 CLINICAL STUDIES
14.1Migraine In controlled clinical trials enrolling more than 1,000 patients during migraine attacks who were experiencing moderate or severe pain and 1 or more of the symptoms enumerated in Table 3, onset of relief began as early as 10 minutes following a 6-mg IMITREX injection. Lower doses of IMITREX injection may also prove effective, although the proportion of patients obtaining adequate relief was decreased and the latency to that relief is greater with lower doses. In Study 1, 6 different doses of IMITREX injection (n = 30 each group) were compared with placebo (n = 62) in a single-attack, parallel-group design; the dose-response relationship was found to be as shown in Table 2 .
Table 2. Proportion of Patients with Migraine Relief and Incidence of Adverse Reactions by Time and by Dose of IMITREX in Study 1 Dose of IMITREX Injection Percent Patients with Relief a Adverse Reactions Incidence (%) at 10 Minutes at 30 Minutes at 1 Hour at 2 Hours Placebo 5 15 24 21 55 1 mg 10 40 43 40 63 2 mg 7 23 57 43 63 3 mg 17 47 57 60 77 4 mg 13 37 50 57 80 6 mg 10 63 73 70 83 8 mg 23 57 80 83 93 a Relief is defined as the reduction of moderate or severe pain to no or mild pain after dosing without use of rescue medication.
In 2 randomized, placebo-controlled clinical trials of IMITREX injection 6 mg in 1,104 patients with moderate or severe migraine pain (Studies 2 and 3), the onset of relief was less than 10 minutes. Headache relief, as defined by a reduction in pain from severe or moderately severe to mild or no headache, was achieved in 70% of the patients within 1 hour of a single 6-mg subcutaneous dose of IMITREX injection. Approximately 82% and 65% of patients treated with IMITREX 6 mg had headache relief and were pain free within 2 hours, respectively.
Table 3 shows the 1- and 2-hour efficacy results for IMITREX injection 6 mg in Studies 2 and 3. Table 3. Proportion of Patients with Pain Relief and Relief of Migraine Symptoms after 1 and 2 Hours of Treatment in Studies 2 and 3 1-Hour Data Study 2 Study 3 Placebo (n = 190) IMITREX 6 mg (n = 384) Placebo (n = 180) IMITREX 6 mg (n = 350) Patients with pain relief (Grade 0/1) 18% 70% a 26% 70% a Patients with no pain 5% 48% a 13% 49% a Patients without nausea 48% 73% a 50% 73% a Patients without photophobia 23% 56% a 25% 58% a Patients with little or no clinical disability b 34% 76% a 34% 76% a 2-Hour Data Study 2 Study 3 Placebo c IMITREX 6 mg d Placebo c IMITREX 6 mg d Patients with pain relief (Grade 0/1) 31% 81% a 39% 82% a Patients with no pain 11% 63% a 19% 65% a Patients without nausea 56% 82% a 63% 81% a Patients without photophobia 31% 72% a 35% 71% a Patients with little or no clinical disability b 42% 85% a 49% 84% a a P <0.05 versus placebo. b A successful outcome in terms of clinical disability was defined prospectively as ability to work mildly impaired or ability to work and function normally. c Includes patients that may have received an additional placebo injection 1 hour after the initial injection. d Includes patients that may have received an additional 6 mg of IMITREX injection 1 hour after the initial injection.
IMITREX injection also relieved photophobia, phonophobia (sound sensitivity), nausea, and vomiting associated with migraine attacks. Similar efficacy was seen when patients self-administered IMITREX injection using the IMITREX STATdose Pen. The efficacy of IMITREX injection was unaffected by whether or not the migraine was associated with aura, duration of attack, gender or age of the patient, or concomitant use of common migraine prophylactic drugs (e.g., beta-blockers).
14.2Cluster Headache The efficacy of IMITREX injection in the acute treatment of cluster headache was demonstrated in 2 randomized, double-blind, placebo-controlled, 2-period crossover trials (Studies 4 and 5). Patients aged 21 to 65 years were enrolled and were instructed to treat a moderate to very severe headache within 10 minutes of onset. Headache relief was… [Excerpted — this section continues on DailyMed.]
🧪 Nonclinical Toxicology ▾
13 NONCLINICAL TOXICOLOGY
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis In carcinogenicity studies in mouse and rat, sumatriptan was administered orally for 78 weeks and 104 weeks, respectively, at doses up to 160 mg/kg/day (the high dose in rat was reduced from 360 mg/kg/day during Week 21). The highest dose to mice and rats was approximately 130 and 260 times the single maximum recommended human dose (MRHD) of 6 mg administered subcutaneously on a mg/m 2 basis. There was no evidence in either species of an increase in tumors related to sumatriptan administration.
Mutagenesis Sumatriptan was negative in in vitro (bacterial reverse mutation [Ames], gene cell mutation in Chinese hamster V79/HGPRT, chromosomal aberration in human lymphocytes) and in vivo (rat micronucleus) assays. Impairment of Fertility When sumatriptan (5, 50, 500 mg/kg/day) was administered orally to male and female rats prior to and throughout the mating period, there was a treatment-related decrease in fertility secondary to a decrease in mating in animals treated with doses greater than 5 mg/kg/day. It is not clear whether this finding was due to an effect on males or females or both.
When sumatriptan was administered by subcutaneous injection to male and female rats prior to and throughout the mating period, there was no evidence of impaired fertility at doses up to 60 mg/kg/day.
13.2Animal Toxicology and/or Pharmacology Corneal Opacities Dogs receiving oral sumatriptan developed corneal opacities and defects in the corneal epithelium. Corneal opacities were seen at the lowest dose tested, 2 mg/kg/day, and were present after 1 month of treatment. Defects in the corneal epithelium were noted in a 60-week study.
Earlier examinations for these toxicities were not conducted and no-effect doses were not established; however, the relative plasma exposure at the lowest dose tested was approximately 3 times the human exposure after a 6-mg subcutaneous dose.
📄 Carcinogenesis, Mutagenesis, Impairment of Fertility ▾
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis In carcinogenicity studies in mouse and rat, sumatriptan was administered orally for 78 weeks and 104 weeks, respectively, at doses up to 160 mg/kg/day (the high dose in rat was reduced from 360 mg/kg/day during Week 21). The highest dose to mice and rats was approximately 130 and 260 times the single maximum recommended human dose (MRHD) of 6 mg administered subcutaneously on a mg/m 2 basis. There was no evidence in either species of an increase in tumors related to sumatriptan administration.
Mutagenesis Sumatriptan was negative in in vitro (bacterial reverse mutation [Ames], gene cell mutation in Chinese hamster V79/HGPRT, chromosomal aberration in human lymphocytes) and in vivo (rat micronucleus) assays. Impairment of Fertility When sumatriptan (5, 50, 500 mg/kg/day) was administered orally to male and female rats prior to and throughout the mating period, there was a treatment-related decrease in fertility secondary to a decrease in mating in animals treated with doses greater than 5 mg/kg/day. It is not clear whether this finding was due to an effect on males or females or both.
When sumatriptan was administered by subcutaneous injection to male and female rats prior to and throughout the mating period, there was no evidence of impaired fertility at doses up to 60 mg/kg/day.
📄 Patient Package Insert ▾
PATIENT INFORMATION IMITREX (IM-i-trex) (sumatriptan) injection What is the most important information I should know about IMITREX? IMITREX can cause serious side effects, including: Heart attack and other heart problems. Heart problems may lead to death.
Stop taking IMITREX and get emergency medical help right away if you have any of the following symptoms of a heart attack: • discomfort in the center of your chest that lasts for more than a few minutes, or that goes away and comes back • severe tightness, pain, pressure, or heaviness in your chest, throat, neck, or jaw • pain or discomfort in your arms, back, neck, jaw, or stomach • shortness of breath with or without chest discomfort • breaking out in a cold sweat • nausea or vomiting • feeling lightheaded IMITREX is not for people with risk factors for heart disease unless a heart exam is done and shows no problem.
You have a higher risk for heart disease if you: • have high blood pressure • have high cholesterol levels • smoke • are overweight • have diabetes • have a family history of heart disease What is IMITREX? IMITREX injection is a prescription medicine used to treat acute migraine headaches with or without aura and acute cluster headaches in adults who have been diagnosed with migraine or cluster headaches. IMITREX is not used to treat other types of headaches such as hemiplegic (that make you unable to move on one side of your body) or basilar (rare form of migraine with aura) migraines.
IMITREX is not used to prevent or decrease the number of migraine or cluster headaches you have. It is not known if IMITREX is safe and effective in children under 18 years of age. Do not take IMITREX if you have: • heart problems or a history of heart problems. • narrowing of blood vessels to your legs, arms, stomach, or kidneys (peripheral vascular disease). • uncontrolled high blood pressure. • severe liver problems. • hemiplegic migraines or basilar migraines.
If you are not sure if you have these types of migraines, ask your healthcare provider. • had a stroke, transient ischemic attacks (TIAs), or problems with your blood circulation. • taken any of the following medicines in the last 24 hours: o almotriptan (AXERT) o frovatriptan (FROVA) o rizatriptan (MAXALT, MAXALT-MLT) o ergotamines (CAFERGOT, ERGOMAR, MIGERGOT) o eletriptan (RELPAX) o naratriptan (AMERGE) o sumatriptan and naproxen (TREXIMET) o dihydroergotamine (D.H.E. 45, MIGRANAL) Ask your healthcare provider if you are not sure if your medicine is listed above. • an allergy to sumatriptan or any of the ingredients in IMITREX.
See the end of this leaflet for a complete list of ingredients in IMITREX. Before taking IMITREX, tell your healthcare provider about all of your medical conditions, including if you: • have high blood pressure • have high cholesterol • have diabetes • smoke • are overweight • have heart problems or family history of heart problems or stroke • have kidney problems • have liver problems • are allergic to latex • have had epilepsy or seizures • are not using effective birth control • are pregnant or plan to become pregnant.
It is not known if IMITREX can harm your unborn baby. • are breastfeeding or plan to breastfeed. IMITREX passes into your breast milk. It is not known if this can harm your baby.
Talk with your healthcare provider about the best way to feed your baby if you take IMITREX. Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. IMITREX and certain other medicines can affect each other, causing serious side effects.
Especially tell your healthcare provider if you take antidepressant medicines called: • selective serotonin reuptake inhibitors (SSRIs) • serotonin norepinephrine reuptake inhibitors (SNRIs) • tricyclic antidepressants (TCAs) • monoamine oxidase inhibitors (MAOIs) Ask your healthcare provider or pharmacist for a list of these medicines if you are not sure. Know the medici… [Excerpted — this section continues on DailyMed.]
📄 Package Label / Principal Display Panel ▾
PRINCIPAL DISPLAY PANEL NDC 0173-0739-02 IMITREX (SUMATRIPTAN) INJECTION 4 mg 0.5 mL For subcutaneous injection only. 2 Single-Dose Syringe Cartridges R x only 62000000090054 Rev. 10/23 Imitrex Injection 4 mg cartridge label
PRINCIPAL DISPLAY PANEL NDC 0173-0478-00 IMITREX (SUMATRIPTAN) INJECTION 6 mg 0.5 mL For subcutaneous injection only. R x only 2 Single-Dose Syringe Cartridges 62000000090057 Rev. 10/23 Imitrex Injection 6 mg cartridge label
PRINCIPAL DISPLAY PANEL NDC 0173-0479-00 IMITREX STATdose SYSTEM 6 mg This carton contains: • Imitrex (sumatriptan) Injection 2 prefilled 0.5-mL syringe cartridges, each containing 6 mg of sumatriptan for subcutaneous injection only • 1 Imitrex STATdose Pen • 1 Carrying Case • Instructions for Use/Information for the Patient • Prescribing Information This Product Contains Dry Natural Rubber R x only Do not accept if security seal is missing or broken. Made in India ©2023 the GSK group of companies or its licensor 62000000090058 Rev.
10/23 Imitrex 6mg Statdose carton