rizatriptan
Brand: Maxalt, Maxalt-MLT
Prototype: sumatriptan
Drug Class: triptan (serotonin 5-HT1B/1D agonist)
Drug Family: antimigraine
Subclass: second-generation triptan
Organ Systems: cns
Mechanism of Action
Selective agonist at 5-HT1B (causes cranial vasoconstriction) and 5-HT1D (inhibits trigeminal nerve neuropeptide release) receptors, aborting migraine through dual vasoconstriction and neuronal inhibition mechanisms.
5-HT1B receptor5-HT1D receptor
Indications
- acute migraine (with or without aura)
Contraindications
- ischemic heart disease
- coronary artery vasospasm
- cerebrovascular disease
- peripheral vascular disease
- concurrent MAOI use (within 14 days)
- hemiplegic or basilar migraine
- concurrent other triptans or ergotamine within 24 hours
Adverse Effects
Common
- pain/pressure/tightness in chest, neck, jaw (non-cardiac in most cases)
- somnolence
- dizziness
- nausea
- paresthesias
Serious
- coronary artery vasospasm
- myocardial infarction
- serotonin syndrome (with MAOIs)
- stroke
Pharmacokinetics (ADME)
| Absorption | oral bioavailability ~45%; food delays but does not reduce absorption |
| Distribution | protein binding ~14%; Vd ~140 L |
| Metabolism | primarily MAO-A oxidative deamination; CYP3A4 minor |
| Excretion | renal (82%) and fecal (12%) |
| Half-life | 2-3 hours |
| Onset | 30-60 minutes |
| Peak | 1-1.5 hours |
| Duration | 2-12 hours per dose |
| Protein Binding | 14% |
| Vd | 140 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| MAO inhibitors | decreased rizatriptan metabolism; increased levels; serotonin syndrome | contraindicated |
| propranolol | inhibits MAO-A; increases rizatriptan levels 70%; reduce dose to 5 mg | major |
| other triptans/ergotamine | additive vasospasm; 24-hour separation required | contraindicated |
Nursing Considerations
- Cardiac risk assessment before prescribing; first dose should be administered in monitored setting for patients with cardiac risk factors.
- Propranolol interaction: reduce rizatriptan dose to 5 mg (maximum 10 mg/day) in patients on propranolol due to 70% increased AUC.
- Do not use for hemiplegic migraine or migraine with brainstem aura (basilar migraine) due to vasospasm risk in posterior circulation.
- Not a preventive treatment; for acute treatment only; do not use >10 days/month to avoid medication overuse headache.
Clinical Pearls
- Rizatriptan has a faster onset than sumatriptan tablets and comparable efficacy to zolmitriptan, making it one of the most commonly prescribed oral triptans for acute migraine.
- The orally-disintegrating tablet (MLT) does not require water and offers the same pharmacokinetics as the conventional tablet; useful for patients with migraine-associated nausea who find swallowing difficult.
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
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