RIZAFILM

Clinical safety rating: caution

Comprehensive clinical and safety monograph for RIZAFILM (RIZAFILM).

How it works

N-methyl-D-aspartate (NMDA) receptor antagonist; inhibits glutamate binding and reduces excitatory neurotransmission.

What the body does with it

Metabolism	Hepatic via CYP2B6, CYP3A4, and CYP2C9; also undergoes N-glucuronidation and hydroxylation.
Excretion	Renal: 20% unchanged; Fecal: 60% (as metabolites); Biliary: 10% (as metabolites).
Half-life	Terminal half-life: 12-15 hours; allows once-daily dosing; prolonged in hepatic impairment.
Protein binding	99% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.3 L/kg (low Vd, distribution mainly in plasma and interstitial fluid).
Bioavailability	Oral: 80% (high first-pass metabolism, but active metabolites contribute to effect).
Onset of Action	Oral: 30-60 minutes (peak plasma concentration at 1-2 hours).
Duration of Action	12-24 hours; clinical effect persists beyond half-life due to high protein binding and active metabolites.

Classification & Brands

Dosing & administration

10 mg sublingually as needed for migraine, with a maximum of 2 doses in 24 hours (minimum interval 2 hours).

Dosage form	FILM
Renal impairment	No dose adjustment required for GFR ≥15 mL/min. Insufficient data for GFR <15 mL/min or dialysis; use with caution.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 5 mg. Child-Pugh C: Avoid use (not recommended).
Pediatric use	Not approved for pediatric patients under 18 years. Safety and efficacy not established.
Geriatric use	No specific dose adjustment recommended; use with caution due to increased sensitivity and potential for adverse effects (e.g., somnolence, dizziness).

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for RIZAFILM (RIZAFILM).

Breastfeeding	No human data on excretion in breast milk. M/P ratio unknown. Theoretical risk of infant toxicity. Manufacturer advises discontinue breastfeeding or drug.
Teratogenic Risk	Pregnancy Category C. First trimester: Increased risk of major congenital malformations (cardiac, neural tube defects) based on animal studies and limited human data. Second and third trimesters: Potential for fetal growth restriction and preterm birth. Avoid in pregnancy unless benefit > risk.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

WARNING: SEDATION AND DISSOCIATION, RISK OF ABUSE AND MISUSE, and SUICIDAL THOUGHTS AND BEHAVIORS. See full prescribing information for complete boxed warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to rizatriptan or any component of the formulation; concurrent use of monoamine oxidase inhibitors (MAOIs) or within 2 weeks of discontinuation; use within 24 hours of other 5-HT1 receptor agonists; hemiplegic or basilar migraine; history of ischemic heart disease or cerebrovascular disease; uncontrolled hypertension; severe hepatic impairment.

Clinical Precautions

Precautions

Sedation and dissociation; risk of abuse and misuse; suicidal thoughts and behaviors; increased blood pressure and heart rate; cognitive impairment; urinary tract symptoms; hypersensitivity reactions; need for patient monitoring during administration.

Clinical Tips & Counseling

Drug interactions

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RIZAFILM

Clinical safety rating: caution

Comprehensive clinical and safety monograph for RIZAFILM (RIZAFILM).

How it works

N-methyl-D-aspartate (NMDA) receptor antagonist; inhibits glutamate binding and reduces excitatory neurotransmission.

What the body does with it

Metabolism	Hepatic via CYP2B6, CYP3A4, and CYP2C9; also undergoes N-glucuronidation and hydroxylation.
Excretion	Renal: 20% unchanged; Fecal: 60% (as metabolites); Biliary: 10% (as metabolites).
Half-life	Terminal half-life: 12-15 hours; allows once-daily dosing; prolonged in hepatic impairment.
Protein binding	99% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.3 L/kg (low Vd, distribution mainly in plasma and interstitial fluid).
Bioavailability	Oral: 80% (high first-pass metabolism, but active metabolites contribute to effect).
Onset of Action	Oral: 30-60 minutes (peak plasma concentration at 1-2 hours).
Duration of Action	12-24 hours; clinical effect persists beyond half-life due to high protein binding and active metabolites.

Classification & Brands

Dosing & administration

10 mg sublingually as needed for migraine, with a maximum of 2 doses in 24 hours (minimum interval 2 hours).

Dosage form	FILM
Renal impairment	No dose adjustment required for GFR ≥15 mL/min. Insufficient data for GFR <15 mL/min or dialysis; use with caution.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 5 mg. Child-Pugh C: Avoid use (not recommended).
Pediatric use	Not approved for pediatric patients under 18 years. Safety and efficacy not established.
Geriatric use	No specific dose adjustment recommended; use with caution due to increased sensitivity and potential for adverse effects (e.g., somnolence, dizziness).

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for RIZAFILM (RIZAFILM).

Breastfeeding	No human data on excretion in breast milk. M/P ratio unknown. Theoretical risk of infant toxicity. Manufacturer advises discontinue breastfeeding or drug.
Teratogenic Risk	Pregnancy Category C. First trimester: Increased risk of major congenital malformations (cardiac, neural tube defects) based on animal studies and limited human data. Second and third trimesters: Potential for fetal growth restriction and preterm birth. Avoid in pregnancy unless benefit > risk.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

WARNING: SEDATION AND DISSOCIATION, RISK OF ABUSE AND MISUSE, and SUICIDAL THOUGHTS AND BEHAVIORS. See full prescribing information for complete boxed warning.