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Rizatriptan

( 5-ht1b Agonists )

Medical uses
Contraindications
Adverse effects
Interactions
Pharmacology

Mechanism of action

Chemistry
History
Society and culture

Brand names

References

C O N T E N T S

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Rizatriptan, sold under the brand name Maxalt among others, is a medication used for the treatment of migraine headaches. It is taken by mouth. It can also be applied on the tongue. It is a serotonin (5-HT) 1B/1D receptor agonist (triptan).

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.

(2025). 9783527607495, John Wiley & Sons. . ISBN 9783527607495

It is available as a generic medication.

(2025). 9780857113382, Pharmaceutical Press. ISBN 9780857113382

In 2023, it was the 208th most commonly prescribed medication in the United States, with more than 2million 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.

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 drug 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 5mg when it is combined with propranolol.

Pharmacology

Mechanism of action

+
48–500 (K_i) >10,000 () 40% ()
3–138 (K_i) 1.4–234 () 74–99% ()
1.5–138 (K_i) 1.6–16 () 83–105% ()
87–316 (K_i) 6.8–870 () 107% ()
138–5,370 (K_i) 4.2–2,540 () 93% ()
>10,000 (K_i) >10,000 ()
257–3,090 (K_i) 3,240 ()
>3,160 (K_i) ()
>3,160 (mouse)
>3,160 (guinea pig)
5,500 (rat)
>3,160
1,860–>10,000 (K_i) >10,000 ()












Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified. Refs: (2025). 9780128233573 ISBN 9780128233573

Rizatriptan acts as an agonist at serotonin 5-HT_1B and 5-HT_1D 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-(1 H-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 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.