soo-ma-TRIP-tan

Therapeutic Classification: vascular headache suppressants

Pharmacologic Classification: five ht1 agonists

• SC, PO, Intranasal: Acute treatment of migraine attacks.
• SC: Acute treatment of cluster headache episodes.

• Acts as a selective agonist of 5-HT₁ at specific vascular serotonin receptor sites, causing vasoconstriction in large intracranial arteries.

• Relief of acute attacks of migraine.

Absorption: Well absorbed (97%) after SUBQ administration. Absorption after oral administration is incomplete and significant amounts undergo substantial hepatic metabolism, resulting in poor bioavailability (14%). Well absorbed after intranasal administration.

Distribution: Well distributed to tissues.

Metabolism/Excretion: Mostly metabolized (80%) by the liver.

Half-life: 2 hr.

(relief of migraine)

Contraindicated in:

• Hypersensitivity to sumatriptan or latex (needle shield of prefilled syringe contains rubber [latex derivative])
• Ischemic heart disease or signs and symptoms of ischemic heart disease, Prinzmetal's angina, or uncontrolled hypertension
• Stroke or transient ischemic attack
• Peripheral vascular disease (including, but not limited to, ischemic bowel disease)
• Concurrent MAO inhibitor therapy
• Hemiplegic or basilar migraine
• Concurrent use of (within 24 hr) ergotamine-containing or ergot-type drugs or other 5HT₁ agonists
• Severe hepatic impairment.

Use Cautiously in:

• OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
• Women of reproductive potential
• Pedi: Safety and effectiveness not established in children
• Geri: ↑risk of cardiovascular complications in older adults.

Exercise Extreme Caution in:

• Cardiovascular risk factors (hypertension, hypercholesterolemia, smoking, obesity, diabetes, family history, menopausal women or men >40 yr); use only if cardiovascular status has been evaluated and determined to be safe and 1st dose is administered under supervision.

CV: angina, chest pressure, chest tightness, coronary vasospasm, ECG changes, MI, transient hypertension.

Derm: tingling, warm sensation, burning sensation, cool sensation, flushing.

EENT: alterations in vision, nasal sinus discomfort, throat discomfort.

GI: abdominal discomfort, dysphagia.

Local: injection site reaction.

MS: jaw discomfort, muscle cramps, myalgia, neck pain, neck stiffness.

Neuro: dizziness, vertigo, anxiety, drowsiness, fatigue, feeling of heaviness, feeling of tightness, headache, malaise, numbness, tight feeling in head, weakness.
Misc: (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)HYPERSENSITIVITY REACTIONS .

Drug-Drug:

• The risk of vasospastic reactions may be ↑ by concurrent use of ergotamine or dihydroergotamine (avoid within 24 hr of each other).
• Avoid concurrent use with other 5HT₁ agonists.
• MAO inhibitors may ↑ levels; do not use within 2 wk of discontinuing MAO inhibitor.
• ↑risk of serotonin syndrome with SSRIs, SNRIs, TCAs, meperidine, bupropion, or buspirone; avoid concurrent use.

Drug-Natural Products:

• ↑risk of serotonergic side effects including serotonin syndrome with St. John’s wort and SAMe.

• PO (Adults): 25 mg initially; if response is inadequate at 2 hr, up to 100 mg may be given (initial doses of 25–50 mg may be more effective than 25 mg). If headache recurs, doses may be repeated every 2 hr (not to exceed 300 mg/day). If PO therapy is to follow SUBQ injection, additional PO sumatriptan may be taken every 2 hr (not to exceed 200 mg/day).
• SC (Adults): 6 mg; may repeat after 1 hr (not to exceed 12 mg in 24 hr); Zembrace SymTouch: 3 mg; may repeat after 1 hr (not to exceed 12 mg/24 hr).
• Intranasal (Adults): Nasal spray (Imitrex): Single dose of 5, 10, or 20 mg in 1 nostril; may be repeated in 2 hr (not to exceed 40 mg/24 hr or treatment of >5 episodes/mo); Nasal spray (Tosymra): Single dose of 10 mg in 1 nostril; may be repeated in 1 hr (not to exceed 30 mg/24 hr); Nasal powder: 11 mg in each nostril; may be repeated in 2 hr (not to exceed 44 mg/24 hr or treatment of >4 episodes/mo).

(Generic available)

• Nasal powder capsules (Onzetra Xsail): 11 mg;
• Nasal spray (Imitrex, Tosymra): 5 mg/spray; 10 mg/spray; 20 mg/spray;
• Solution for injection (autoinjectors): 3 mg/0.5 mL; 4 mg/0.5 mL; 6 mg/0.5 mL;
• Tablets: 25 mg; 50 mg; 100 mg;
• In combination with: naproxen (Treximet); see Appendix [not included in this PDA edition].

• Assess pain location, intensity, duration, and associated symptoms (photophobia, phonophobia, nausea, vomiting) during migraine attack.
• Give initial SUBQ dose under observation to patients with potential for coronary artery disease including postmenopausal women, men >40 yr, patients with risk factors for coronary artery disease such as hypertension, hypercholesterolemia, obesity, diabetes, smoking, or family history. Monitor BP before and for 1 hr after initial injection. If angina occurs, monitor ECG for ischemic changes.
• Monitor for serotonin syndrome in patients taking SSRIs or SNRIs concurrently with sumatriptan.

• Do not confuse sumatriptan with sitagliptin or zolmitriptan.
• PO: Tablets should be swallowed whole; DNC: do not crush, break, or chew. Tablets are film-coated to prevent contact with tablet contents, which have an unpleasant taste and may cause nausea and vomiting.
• SC: Administer as a single injection. Solution is clear and colorless or pale yellow; do not use if dark-colored or cloudy or if beyond expiration date.
• Intranasal: 10-mg dose may be administered as 2 sprays of 5 mg in 1 nostril or 1 spray in each nostril.
  • Nasal Powder: Remove clear device cap from the reusable delivery device, then remove a disposable nosepiece from foil pouch and click nosepiece into device body. Press fully and promptly release white piercing button on device body to pierce capsule inside nosepiece. White piercing button should only be pressed once and released prior to administration to each nostril. Insert nosepiece into nostril making a tight seal. Rotate device to place mouthpiece into the mouth. Patient blows forcefully through mouthpiece to deliver the sumatriptan powder into nasal cavity. Vibration (e.g., a rattling noise) may occur, and indicates that patient is blowing forcefully, as directed. Once medication in the first nosepiece has been administered, remove and discard nosepiece.

• Inform patient that sumatriptan should be used only during a migraine attack. It is meant to be used for relief of migraine attacks but not to prevent or reduce the number of attacks.
  • Instruct patient to administer sumatriptan as soon as symptoms of a migraine attack appear, but it may be administered at any time during an attack. If migraine symptoms return, a 2nd injection may be used. Allow at least 1 hr between doses, and do not use more than 2 injections in any 24-hr period. Additional sumatriptan doses are not likely to be effective, and alternative medications may be used. If no relief from 1st dose, unlikely 2nd dose will provide relief. Advise patient to read Patient Information prior to using and with each Rx refill; new information may be available.
  • Advise patient that lying down in a darkened room after sumatriptan administration may further help relieve headache.
  • Advise patient that overuse (use more than 10 days/mo) may lead to exacerbation of headache (migraine-like daily headaches, or as a marked increase in frequency of migraine attacks). May require gradual withdrawal of sumatriptan and treatment of symptoms (transient worsening of headache).
  • Advise patient to notify health care professional before next dose of sumatriptan if pain or tightness in chest occurs during use. If pain is severe or does not subside, notify health care professional immediately. If wheezing; heart throbbing; swelling of eyelids, face, or lips; skin rash; skin lumps; or hives occur, notify health care professional immediately, and do not take more sumatriptan without approval of health care professional. If usual dose fails to relieve 3 consecutive headaches, or if frequency and/or severity increases, notify health care professional. If feelings of tingling, heat, flushing, heaviness, pressure, drowsiness, dizziness, tiredness, or sickness develop, discuss with health care professional at next visit.
  • Sumatriptan may cause dizziness or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
  • Advise patient to avoid alcohol, which aggravates headaches, during sumatriptan use.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications. Patients concurrently taking SSRI or SNRI antidepressants should notify health care professional promptly if signs of serotonin syndrome (mental status changes: agitation, hallucinations, coma; autonomic instability: tachycardia, labile BP, hyperthermia; neuromuscular aberrations: hyper-reflexia, incoordination; and/or gastrointestinal symptoms: nausea, vomiting, diarrhea) occur.
• Caution patient not to use sumatriptan if pregnancy is planned or suspected or if breastfeeding. Adequate contraception should be used during therapy.
• SC: Instruct patient on the proper technique for loading, administering, and discarding the Imitrex STATdose pen autoinjector. Patient information pamphlet is provided. Instructional video is available from the manufacturer.
  • Inform patient that pain or redness at the injection site usually lasts less than 1 hr.
• Intranasal: Instruct patient in proper technique for intranasal administration. Usual dose is a single spray in 1 nostril. If headache returns, a 2nd dose may be administered in 2 hr. Do not administer 2nd dose if no relief was provided by 1st dose without consulting health care professional.

• Relief of migraine attack.

Imitrex, Imitrex STATdose, Onzetra Xsail, Tosymra, Zembrace SymTouch

Imitrex DF