Rizatriptan
Medication used for the treatment of migraine headaches
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Through Medication, Pregnancy and Metabolite
Common side effects include chest pain, dizziness, dry mouth, and tingling. Other side effects may include myocardial infarction, stroke, high blood pressure, serotonin syndrome, and anaphylaxis. Excessive use may result in medication overuse headaches. Use is not recommended during pregnancy and breastfeeding is not recommended within 24 hours after taking a dose. Rizatriptan is in the triptan class and is believed to work by activating the 5-HT1 receptor.
Rizatriptan was patented in 1991 and came into medical use in 1998. It is available as a generic medication. In 2023, it was the 208th most commonly prescribed medication in the United States, with more than 2 million prescriptions. Rizatriptan is available in combination with meloxicam as meloxicam/rizatriptan.
Medical uses
Rizatriptan is indicated to treat acute migraine attacks with or without aura. It does not prevent future migraine attacks. A 2010 review found rizatriptan to be more efficacious and tolerable than sumatriptan.
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Contraindications
Rizatriptan and other triptans can cause vasoconstriction, they are contraindicated in people with cardiovascular conditions.
Adverse effects
Frequent adverse effects (incidence less than 10%) are dizziness, drowsiness, asthenia/fatigue, and nausea. Clinical adverse experiences were typically mild and short-lasting (2–3 hours).
Interactions
Rizatriptan has an important but complex interaction with a metabolite of the beta blocker propranolol. This interaction involves the enzyme monoamine oxidase A (MAO-A). Due to the interaction, the dose of rizatriptan should be reduced to 5 mg when it is combined with propranolol.
Pharmacology
Mechanism of action
Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors. Like the other triptans sumatriptan and zolmitriptan, rizatriptan induces vasoconstriction—possibly by inhibiting the release of calcitonin gene-related peptide from sensory neurons in the trigeminal nerve.
Chemistry
Rizatriptan, also known as 5-(1H-1,2,4-triazol-1-ylmethyl)-N,N-dimethyltryptamine, is a tryptamine derivative and a 5-substituted derivative of the psychedelic drug dimethyltryptamine (DMT).
The experimental log P of rizatriptan is 1.4 and its predicted log P is 1.67 to 1.77.
History
Rizatriptan was patented in 1991 and was introduced for medical use in 1998.
Society and culture
Brand names
Brand names include Rizalt, Rizalt RPD, Rizact (India), Rizafilm, Maxalt, and Maxalt-MLT.