MAXALT-MLT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MAXALT-MLT (MAXALT-MLT).
Selective 5-HT1B/1D receptor agonist; causes vasoconstriction of intracranial arteries and inhibits trigeminal nerve activation.
| Metabolism | Primarily metabolized by monoamine oxidase A (MAO-A) to an indoleacetic acid metabolite; minor CYP450 involvement. |
| Excretion | Primarily hepatic metabolism; ~14% excreted unchanged in urine, ~76% as metabolites in feces via bile, total renal excretion of parent and metabolites ~40%. |
| Half-life | Terminal elimination half-life of approximately 2-3 hours; clinical context: short half-life supports acute migraine treatment with rapid offset. |
| Protein binding | ~14% bound to plasma proteins (mainly albumin). |
| Volume of Distribution | Volume of distribution ~3 L/kg; indicates extensive tissue distribution beyond plasma. |
| Bioavailability | Oral bioavailability of rizatriptan (including MAXALT-MLT) is approximately 45% due to first-pass metabolism; comparable to standard tablet. |
| Onset of Action | Orally disintegrating tablet: onset within 30 minutes, peak plasma concentration at 1-1.5 hours. |
| Duration of Action | Clinical effect duration of 2-4 hours; migraine recurrence may occur, requiring a second dose after at least 2 hours. |
10 mg orally as a single dose; maximum 30 mg in 24 hours. Administer at onset of migraine; do not use for prophylaxis.
| Dosage form | TABLET, ORALLY DISINTEGRATING |
| Renal impairment | No dose adjustment for mild to moderate renal impairment. Contraindicated in severe renal impairment (CrCl < 10 mL/min) due to lack of data. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh C). For mild to moderate impairment, use with caution; no specific dose adjustment recommended but may consider starting at 5 mg. |
| Pediatric use | Children 12 years and older: 10 mg orally as a single dose. Safety and efficacy not established under 12 years. |
| Geriatric use | No specific dose adjustment recommended; use with caution due to increased sensitivity and potential for adverse events in elderly patients. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for MAXALT-MLT (MAXALT-MLT).
| Breastfeeding | Rizatriptan is excreted in human breast milk at low concentrations (estimated infant dose <3% of maternal weight-adjusted dose). M/P ratio not established. Caution is advised; consider alternative treatments or temporarily discontinue breastfeeding during therapy. |
| Teratogenic Risk | First trimester: Limited human data; animal studies show no evidence of teratogenicity at clinically relevant doses. Second and third trimesters: No increased risk of major malformations reported; potential for uterine hypertonicity and reduced placental blood flow with use near term. Avoid use in pregnancy unless clearly needed. |
■ FDA Black Box Warning
Maxalt-MLT should not be given to patients with ischemic heart disease or coronary artery vasospasm, including Prinzmetal's angina; cases of serious cardiac adverse reactions, including acute myocardial infarction, have been reported within a few hours following administration of 5-HT1 agonists.
| Serious Effects |
["Ischemic heart disease (e.g., angina pectoris, history of MI, documented silent ischemia)","Coronary artery vasospasm (including Prinzmetal's angina)","History of stroke or transient ischemic attack","Peripheral vascular disease","Uncontrolled hypertension","Concomitant use or within 24 hours of MAO-A inhibitors","Severe hepatic impairment","Hypersensitivity to rizatriptan or any component of the formulation","Hemiplegic or basilar migraine"]
| Precautions | ["Risk of myocardial ischemia and/or infarction, coronary artery vasospasm, and other cardiac events","Cerebrovascular events including stroke and subarachnoid hemorrhage","Serotonin syndrome (particularly with concomitant serotonergic drugs)","Increase in blood pressure (including hypertensive crisis)","Severe hepatic impairment (use contraindicated; for patients with moderate hepatic impairment, use with caution and consider lower dose)"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal blood pressure and heart rate during administration. Fetal heart rate monitoring recommended if used during third trimester due to potential for uterine hypertonicity. Assess for signs of serotonin syndrome if concomitant serotonergic drugs used. |
| Fertility Effects | No significant effects on fertility observed in animal studies. Human data insufficient to determine impact on fertility. |