Drug Guide
Rizatriptan Benzoate
Classification
Therapeutic: Antimigraine agent
Pharmacological: Selective 5-HT1B/1D receptor agonist (triptan)
FDA Approved Indications
- Acute treatment of migraine attacks with or without aura
Mechanism of Action
Rizatriptan selectively binds to serotonin 5-HT1B and 5-HT1D receptors, leading to vasoconstriction of intracranial blood vessels, inhibition of neuropeptide release, and diminution of transmission in pain pathways within the central nervous system.
Dosage and Administration
Adult: Initial dose typically 5 mg orally; can repeat after 2 hours if needed, not exceeding 30 mg in 24 hours.
Pediatric: Not recommended for children under 6 years. For ages 6-17, dosing should be guided by a healthcare provider.
Geriatric: Use with caution; start at the lower end of dosing range due to potential increased sensitivity.
Renal Impairment: Adjust dose based on severity; use caution.
Hepatic Impairment: Use with caution; start at lower doses due to increased systemic exposure.
Pharmacokinetics
Absorption: Rapidly absorbed after oral administration with peak plasma levels in approximately 1-1.5 hours.
Distribution: Widely distributed with a volume of distribution of about 2-4 L/kg.
Metabolism: Extensively metabolized by monoamine oxidase-A (MAO-A) with minimal cytochrome P450 involvement.
Excretion: Primarily eliminated via renal route; metabolites are excreted in urine.
Half Life: Approximately 2-3 hours.
Contraindications
- History of ischemic cardiac disease, coronary artery vasospasm or angina pectoris
- History of cerebrovascular accident or transient ischemic attack
- Uncontrolled hypertension
- Ischemic bowel disease
Precautions
- Use with caution in patients with risk factors for cardiovascular disease, including hypertension, hyperlipidemia, smoking, or family history of cardiac disease.
- Potential for cardiac ischemia; consider cardiac evaluation if indicated.
Adverse Reactions - Common
- Dizziness (Common)
- Drowsiness (Common)
- Throat/neck heaviness or pressure (Common)
Adverse Reactions - Serious
- Myocardial infarction (Rare)
- Serotonin syndrome (when combined with other serotonergic drugs) (Rare)
- Allergic reactions including angioedema, rash (Rare)
Drug-Drug Interactions
- Selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), MAO inhibitors (MAOIs). Use together may increase risk of serotonin syndrome.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Assess for cardiovascular disease history before administering.
Diagnoses:
- Risk for ineffective cerebral/cardiac tissue perfusion.
- Imbalanced nutrition: less than body requirements.
Implementation: Administer at onset of migraine symptoms. Monitor blood pressure and for cardiac symptoms.
Evaluation: Assess effectiveness by reduction in migraine severity and duration.
Patient/Family Teaching
- Take at first sign of migraine.
- Do not exceed recommended dose.
- Report chest pain, tightness, dizziness, or signs of allergic reaction immediately.
- Avoid concomitant use with other serotonergic agents unless instructed by a healthcare provider.
Special Considerations
Black Box Warnings:
- Cardiovascular risk: contraindicated in patients with ischemic heart disease or uncontrolled hypertension.
Genetic Factors: Genetic variations in CYP1A2 enzyme may affect metabolism.
Lab Test Interference: May affect some cardiac enzyme tests due to vasoconstrictive properties.
Overdose Management
Signs/Symptoms: Signs may include dizziness, tightness in chest, vomiting, altered consciousness.
Treatment: Supportive care, activated charcoal if ingestion was recent, and cardiovascular monitoring.
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F).
Stability: Stable for 24 months when stored properly.