Rimegepant

Patients taking moderate CYP3A4 inhibitors (e.g. erythromycin, diltiazem, fluconazole) or potent P-gp inhibitors (e.g. amiodarone, ciclosporin, lapatinib, quinidine, ranolazine, verapamil): Avoid taking another dose of rimegepant within 48 hours.

ESRD: Not recommended.

CrCl (mL/min)	Dosage
<15	Not recommended.

Severe (Child-Pugh class C): Not recommended.

Rimegepant May be taken with or without food. Place on the tongue & allow to dissolve.

Pregnancy.

Concomitant use with strong CYP3A4 and P-gp inhibitors. Severe renal (ESRD, CrCl <15 mL/min) and hepatic (Child-Pugh class C) impairment. Lactation.

Significant: Hypersensitivity reactions (e.g. rash, dyspnoea, delayed serious reactions).
Gastrointestinal disorders: Nausea, abdominal pain, dyspepsia.

PO: Z (Avoid)

Monitor for medication overuse headache (MOH) in patients who have frequent or daily headaches despite (or because of) the regular use of medicines for headache. Assess for signs and symptoms of hypersensitivity reactions.

Significantly increased serum concentrations with strong CYP3A4 inhibitors (e.g. clarithromycin, itraconazole, ritonavir). Potential increase in exposure with moderate CYP3A4 inhibitors (e.g. erythromycin, diltiazem, fluconazole). Significantly decreased serum concentrations with strong CYP3A4 inducers (e.g. rifampicin, phenobarbital) or moderate CYP3A4 inducers (e.g. bosentan, efavirenz, modafinil). Increased plasma concentration with BCRP or P-gp inhibitors (e.g. amiodarone, ciclosporin, lapatinib, quinidine, ranolazine, verapamil).

Decreased serum concentrations with St. John’s wort.

Description:
Mechanism of Action: Rimegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist. It selectively binds with high affinity to the CGRP receptor and subsequently inhibits the activity of CGRP, a pain-signalling neuropeptide and a potent vasodilator involved in the pathophysiology of migraine.
Onset: Migraine: Treatment: ≤2 hours. Prevention: ≤4 weeks.
Duration: Migraine: Treatment: Up to 48 hours.
Pharmacokinetics:
Absorption: Food, specifically high- or low-fat meal, reduces rate and extent of absorption. Absolute bioavailability: Approx 64%. Time to peak plasma concentration: 1.5 hours; 1 hour delayed following a high-fat meal.
Distribution: Enters breast milk. Plasma protein binding: Approx 96%.
Metabolism: Metabolised in the liver mainly by CYP3A4 and CYP2C9 (lesser extent).
Excretion: Via urine (51% as unchanged drug); faeces (42% as unchanged drug). Elimination half-life: Approx 11 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 51049968, Rimegepant. https://pubchem.ncbi.nlm.nih.gov/compound/Rimegepant. Accessed July 26, 2024.

Store between 15-30°C. Protect from moisture.

Antimigraine Preparations

N02CD06 - rimegepant ; Belongs to the class of calcitonin gene-related peptide (CGRP) antagonists preparations. Used to relieve migraine.

Anon. Rimegepant. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 03/07/2024.

Brayfield A, Cadart C (eds). Rimegepant. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/07/2024.

Joint Formulary Committee. Rimegepant. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/07/2024.

Nurtec 75 mg Oral Lyophilisate (Pfizer [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 03/07/2024.

Nurtec ODT - Tablet, Orally Disintegrating (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 03/07/2024.

Rimegepant. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 03/07/2024.

Vydura 75 mg Oral Lyophilisate (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 03/07/2024.