Overview
11 DESCRIPTION MAXALT contains rizatriptan benzoate, a selective 5-hydroxytryptamine 1B/1D (5-HT 1B/1D ) receptor agonist. Rizatriptan benzoate is described chemically as: N,N -dimethyl-5-(1 H -1,2,4-triazol-1-ylmethyl)-1 H -indole-3-ethanamine monobenzoate and its structural formula is: Its empirical formula is C 15 H 19 N 5 •C 7 H 6 O 2 , representing a molecular weight of the free base of 269.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Rizatriptan binds with high affinity to human cloned 5-HT 1B/1D receptors. MAXALT presumably exerts its therapeutic effects in the treatment of migraine headache by binding to 5-HT 1B/1D receptors located on intracranial blood vessels and sensory nerves of the trigeminal system. 12.3 Pharmacokinetics Absorption Rizatriptan is completely absorbed following oral administration. The mean oral absolute bioavailability of the MAXALT Tablet is about 45%, and mean peak plasma concentrations (C max ) are reached in approximately 1-1.5 hours (T max ). The presence of a migraine headache did not appear to affect the absorption or pharmacokinetics of rizatriptan.
Indications
- 1 INDICATIONS AND USAGE MAXALT ® and MAXALT-MLT ® are indicated for the acute treatment of migraine with or without aura in adults and in pediatric patients 6 to 17 years old. Limitations of Use MAXALT should only be used where a clear diagnosis of migraine has been established. If a patient has no response for the first migraine attack treated with MAXALT, the diagnosis of migraine should be reconsidered before MAXALT is administered to treat any subsequent attacks. MAXALT is not indicated for use in the management of hemiplegic or basilar migraine [see Contraindications (4) ] .
Common Doses
- 5 mg
- 10 mg
- 30 mg
- 15 mg
Dosage
2 DOSAGE AND ADMINISTRATION Although rizatriptan benzoate 5 mg tablets and orally disintegrating tablets are available in the marketplace, MAXALT Tablets and MAXALT-MLT Orally Disintegrating Tablets are no longer marketed in the 5 mg strength. Adults: 5 or 10 mg single dose; separate repeat doses by at least two hours; maximum dose in a 24-hour period: 30 mg ( 2.1 ) Pediatric patients 6 to 17 years: 5 mg single dose in patients less than 40 kg (88 lb); 10 mg single dose in patients 40 kg (88 lb) or more ( 2.2 ) Adjust dose if co-administered with propranolol ( 2.4 ) 2.
Contraindications
- 4 CONTRAINDICATIONS MAXALT is contraindicated in patients with: Ischemic coronary artery disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), or other significant underlying cardiovascular disease [see Warnings and Precautions (5.1) ] . Coronary artery vasospasm including Prinzmetal's angina [see Warnings and Precautions (5.1) ] . History of stroke or transient ischemic attack (TIA) [see Warnings and Precautions (5.4) ] . Peripheral vascular disease (PVD) [see Warnings and Precautions (5.5) ] . Ischemic bowel disease [see Warnings and Precautions (5.
Side Effects
- 6 ADVERSE REACTIONS The following adverse reactions are discussed in more detail in other sections of the labeling: Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina [see Warnings and Precautions (5.1) ] . Arrhythmias [see Warnings and Precautions (5.2) ]. Chest, Throat, Neck and/or Jaw Pain/Tightness/Pressure [see Warnings and Precautions (5.3) ] . Cerebrovascular Events [see Warnings and Precautions (5.4) ] . Other Vasospasm Reactions [see Warnings and Precautions (5.5) ] . Medication Overuse Headache [see Warnings and Precautions (5.6) ] .
Interactions
- 7 DRUG INTERACTIONS 7.1 Propranolol The dose of MAXALT should be adjusted in propranolol-treated patients, as propranolol has been shown to increase the plasma AUC of rizatriptan by 70% [see Dosage and Administration (2.4) and Clinical Pharmacology (12.3) ] . 7.2 Ergot-Containing Drugs Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and MAXALT within 24 hours is contraindicated [see Contraindications (4) ] . 7.