Products
Rizatriptan is commercially available in tablet and lingual (melting) tablet form (Maxalt, generics). It has been approved in many countries since 2000. Generic versions went on sale in 2015.
Structure and properties
Ritatriptan (C15H19N5, Mr = 269.3 g/mol) is present in drugs as rizatriptan benzoate, a white crystalline powder that is soluble in water. It is an indole and triazole derivative structurally related to serotonin.
Effects
Rizatriptan (ATC N02CC04) has vasoconstrictive, analgesic, and anti-inflammatory properties. The effects are due to selective agonism at 5-HT1B/1D serotonin receptors. The half-life is short, lasting two to three hours.
Indications
For acute treatment of migraine with or without aura.
Dosage
According to the SmPC. The drug should not be used as a preventive, but exclusively for treatment. The low maximum daily doses (30 mg) and the dosing interval (at least two hours) must be observed. Lingual tablets can be taken without water.
Contraindications
- Hypersensitivity
- Basilar migraine
- Hemiplegic migraine
- Certain cardiovascular diseases
- Combination with MAO inhibitors
Full precautions can be found in the drug label.
Interactions
Rizatriptan is metabolized primarily by monoamine oxidase-A. Drug-drug interactions are possible with MAO inhibitors, beta-blockers (propranolol), and drugs with serotonergic effects (risk for serotonin syndrome).
Adverse effects
The most common possible adverse effects include fatigue, drowsiness, pain, tightness, dizziness, diarrhea, vomiting, respiratory disturbances, flushing, flushing, palpitations, hypesthesia, decreased acuity of consciousness, euphoria, tremor, and warm/cold sensations.
