Rizatriptan

Rizatriptan
MAXALT® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
Clinical Trials on Rizatriptan
ClinicalTrials.gov

Rizatriptan

Clinical data
Trade names	Maxalt
AHFS/Drugs.com	Monograph
MedlinePlus	a601109
Pregnancy category	B1 (Au), C (U.S.)
Routes of administration	Oral
ATC code	N02CC04 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	45%
Protein binding	14%
Metabolism	by monoamine oxidase
Elimination half-life	2–3 hours
Excretion	82% urine; 12% faeces
Identifiers
IUPAC name N,N-dimethyl-2-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethanamine
CAS Number	145202-66-0 Y
PubChem CID	5078
IUPHAR/BPS	51
DrugBank	DB00953 Y
ChemSpider	4900 Y
UNII	WR978S7QHH
KEGG	D00675 N
ChEBI	CHEBI:48273 Y
ChEMBL	ChEMBL905 Y
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C15H19N5
Molar mass	269.345 g/mol
3D model (JSmol)	Interactive image
SMILES n1cn(nc1)Cc2cc3c(cc2)ncc3CCN(C)C
InChI InChI=1S/C15H19N5/c1-19(2)6-5-13-8-17-15-4-3-12(7-14(13)15)9-20-11-16-10-18-20/h3-4,7-8,10-11,17H,5-6,9H2,1-2H3 Y Key:ULFRLSNUDGIQQP-UHFFFAOYSA-N Y
NY (what is this?)  (verify)

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

For patient information about Rizatriptan, click here.

Synonyms / Brand Names: MAXALT

Overview

Rizatriptan (trade name Maxalt) is a 5-HT1 agonist triptan drug developed by Merck & Co. for the treatment of migraine headaches. It is available in strengths of 5 and 10 mg as tablets and orally disintegrating tablets (Maxalt-MLT).

Maxalt obtained approval by the United States Food and Drug Administration (FDA) on June 29, 1998. It is a second-generation triptan.

Rizatriptan is available only by prescription in Australia, Finland, the United States, Canada and New Zealand. Similarly, it is classed as a POM (Prescription Only Medicine) in the United Kingdom, Italy (as Rizaliv), Israel (as Rizalt), The Netherlands, Croatia and Spain (as Maxalt).

Category

Antimigraine Drugs, Triptans

FDA Package Insert

MAXALT (rizatriptan benzoate) tablet

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Use

Rizatriptan is used to treat acute migraine attacks with or without aura. It does not prevent future migraine attacks.

Contraindications

• coronary artery disease
• use of monoamine oxidase inhibitors

Adverse effects

Severe:

• serotonin syndrome when used with MAOIs
• coronary artery vasospasm
• transient myocardial ischemia Template:Nb10
• myocardial infarction
• ventricular tachycardia
• ventricular fibrillation
• hypertensive crisis

Atypical sensations:

• paresthesia

Cardiovascular:

• palpitations
• syncope
• hypertension
• hypotension

Ear, nose, and throat:

• tinnitus
• sinusitis
• allergic rhinitis
• upper respiratory tract inflammation

Gastrointestinal:

• diarrhea

Muscular:

• myalgia

Neurological:

• phonophobia
• photophobia

Respiratory:

• dyspnea

Skin:

• sweating

Miscellaneous:

• hypersensitivity

Mechanism of Action

Rizatriptan binds with high affinity to human cloned 5-HT1B/1D receptors. Rizatriptan presumably exerts its therapeutic effects in the treatment of migraine headache by binding to 5-HT1B/1D receptors located on intracranial blood vessels and sensory nerves of the trigeminal system.