Generic Name

Ubrogepant

Mechanism

• Ubrogepant is a selective, non‑peptide calcitonin gene‑related peptide (CGRP) receptor antagonist.
• By competitively binding to the CGRP receptor located on trigeminal neuronal cells, it blocks CGRP‑mediated vasodilation, neurogenic inflammation, and pain transmission.
• Consequently, it dampens the trigeminovascular activation that underlies migraine attack initiation.

Pharmacokinetics

• Absorption – Oral tablet; peak serum concentration (Tmax) ≈ 1–1.5 h; oral bioavailability ≈ 70–80 %.
• Distribution – Volume of distribution ≈ 35 L; highly protein‑bound (~94 %).
• Metabolism – Hepatic via CYP2C19, CYP3A4, and CYP1A2; negligible renal excretion of unchanged drug.
• Elimination half‑life – ~5 h (dose‑dependent but < 10 h).
• Drug‑drug interactions – Strong CYP2C19 inhibitors (e.g., fluconazole) raise exposure; strong CYP3A4 inducers (e.g., rifampin) lower it.

Indications

• Acute migraine without aura in adults.
• Considered when patients have failed or are intolerant to triptans or NSAIDs.

Contraindications

• Contraindications – Hypersensitivity to ubrogepant or any excipient; active liver disease (ALT/AST > 3× upper limit of normal).
• Warnings
• *Potential hepatotoxicity* – monitor liver enzymes if treatment > 1 month.
• *Drug interactions* – co‑administration with potent CYP3A4 inhibitors may increase hypersensitivity risk.
• *Pregnancy* – Category B; use only if benefit outweighs risk.

Dosing

• Standard dose: 50 mg orally once per migraine attack.
• Repeat dose: Up to 50 mg can be taken 24 h after the initial dose if pain remains.
• Administration: Take with or without food; avoid concurrent alcohol.

Adverse Effects

• Immediate reaction: Seek care if rash, swelling, or breathing trouble appears within the first few days.
• Liver monitoring: Report any increase in transaminases early.

Monitoring

• Baseline LFTs before initiating therapy; repeat at 4–6 weeks if > 8 weeks of treatment.
• CYP2C19 inhibitor/inductor status – adjust dosing or avoid concomitant use.
• Pregnancy test for women of childbearing potential before first dose.

Clinical Pearls

1. Rapid Onset: Tmax of ~1 h makes *ubrogepant* ideal for patients needing early relief when traditional triptans are contraindicated.

2. Non‑triptan Alternative: Effective for patients intolerant to serotonin agonists or with cardiovascular comorbidities.

3. Hepatic Caution: Metabolism via CYP enzymes necessitates careful use in hepatic impairment; dose reduction or alternative therapy may be required.

4. Avoid Duplication: Do not combine with other CGRP‑targeted acute therapies to prevent overlapping adverse events.

5. Patient Education: Instruct patients to monitor for signs of liver dysfunction, rash, swelling, or dyspnea and to seek help promptly.

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• *This drug card is intended for educational and reference purposes. Always consult prescribing information and clinical guidelines for patient‑specific decision making.*