Generic Name

sumatriptan

Mechanism

Sumatriptan selectively activates 5‑HT1B and 5‑HT1D serotonin receptors:
• 5‑HT1B activation constricts cranial vasculature, decreasing pain‑mediated vasodilatation.
• 5‑HT1D activation inhibits trigeminal neuropeptide release (e.g., CGRP, substance P), reducing neurogenic inflammation.
• Combined effects reduce migraine pain and associated autonomic symptoms (nausea, photophobia).

Pharmacokinetics

• Onset: Dissolves within 1–2 min; Tmax ≈ 1 h (oral).
• Absorption: Rapid, unaffected by food or gastric motility changes.
• Metabolism: Minimal hepatic metabolism; primarily excreted unchanged.
• Half‑life: 2–3 h.
• Renal clearance: 80–90 % renal; no dose adjustment for mild to moderate CKD, but caution in severe renal impairment.

Indications

• Acute treatment of migraine with or without aura in adults, including patients with orthostatic intolerance who require a rapid‑acting formulation.

Contraindications

• Contraindications
• Known hypersensitivity to sumatriptan or any excipient.
• Uncontrolled systemic hypertension.
• Recent cerebrovascular accident or coronary artery disease.
• Severe hepatic disease (Child‑Pugh B/C).
• Severe renal impairment (dialysis patients).
• Warnings
• Cerebrovascular and cardiovascular: Avoid in patients with ischemic heart disease, uncontrolled HTN, diabetes with vascular disease, or significant peripheral arterial disease.
• MAO inhibitor interaction: Contraindicated if MAOIs were used within 14 days (or 4 days for non‑selective).
• Medication interactions: Avoid concurrent use with other serotoninergic drugs (e.g., ergot derivatives, ergotamine, selective serotonin reuptake inhibitors) due to risk of serotonin syndrome.
• Pregnancy: Category B; use only if benefit outweighs risk.

Dosing

• First dose: 20 mg ODT.
• Repeat dose: 40 mg ODT after 2–3 h only if migraine persists.
• Maximum: 60 mg in a 24‑h period; not to exceed 120 mg per week.
• Administration: Place under the tongue; may swallow the tablet.
• Special instructions: Avoid taking with opioids, CNS depressants, or other migraine therapies that already lower platelet function.

Adverse Effects

• Common (≥10 %)
• Tingling/numbness
• Chest discomfort (benign vasospasm)
• Dizziness, fatigue, headache
• Nausea, vomiting, abdominal discomfort
• Serious (≤1 %)
• Chest pain indicating myocardial ischemia; seek emergent care.
• Severe allergic reactions (anaphylaxis).
• Seizures – rarely reported in predisposed patients.
• TRALI in patients with transfusion history (rare).
• Patient counsel: Use with caution in those with cardiovascular risk factors; advise to remit any chest pain promptly.

Monitoring

• Baseline: Blood pressure and heart rate; assess cardiovascular risk profile.
• During treatment:
• Monitor for chest symptoms or dizziness.
• Evaluate headache relief after 2 hr; reassess dose if needed.
• In patients with mild renal impairment, monitor creatinine clearance if repeated use.
• Follow‑up: Document frequency/severity of migraine attacks; check for medication overuse headaches (≥10 days/month).

Clinical Pearls

• Rapid onset: Nurtec ODT’s dissolution makes it ideal for patients who cannot swallow tablets or who need relief within minutes.
• Safe coexistence: It can be safely combined with NSAIDs or acetaminophen for enhanced pain control, provided the patient has no contraindications.
• Avoid with nitroglycerin: Both cause vasodilation; combination may blunt efficacy and increase adverse effects.
• Use in pregnancy cautiously: While Category B, data are limited; consider if migraine control is essential.
• Maximize benefit: Administer at the earliest stage of the migraine (symptom onset) to reduce risk of transformation into a persistent attack.
• Do not exceed dose: Over‑treatment can result in vaso‑spastic episodes; stick to the 60 mg/24 h limit.
• Patient education: Instruct patients to keep a headache diary, especially if using sumatriptan >2–3 times/month, to identify medication‑overuse risk.

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• Key Takeaway: Nurtec ODT offers a fast‑acting, precision dose of sumatriptan for migraine sufferers, bridging the gap when quick relief is essential. With careful patient selection, avoidance of drug interactions, and vigilant monitoring, it remains a cornerstone acute migraine therapy.