TOSYMRA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TOSYMRA (TOSYMRA).

How it works

Sumatriptan is a selective agonist of serotonin (5-HT1B/1D) receptors, leading to vasoconstriction of intracranial blood vessels and inhibition of trigeminal nerve transmission.

What the body does with it

Metabolism	Metabolized primarily by monoamine oxidase A (MAO-A); undergoes first-pass metabolism.
Excretion	Renal excretion of unchanged drug and metabolites; 70% recovered in urine as parent and metabolites, 30% in feces.
Half-life	Terminal elimination half-life approximately 2.5 hours; clinically relevant for dosing every 4-6 hours.
Protein binding	Low (<20%); primarily albumin.
Volume of Distribution	Approximately 1.0 L/kg; suggests distribution into total body water.
Bioavailability	Intranasal: approximately 30% relative to intravenous administration.
Onset of Action	Intranasal: 15-30 minutes.
Duration of Action	4-6 hours; analgesic effect correlating with plasma concentration.

Classification & Brands

Dosing & administration

10 mg intranasally as a single dose, may repeat once after 24 hours if needed. Maximum 2 doses in 7 days.

Dosage form	SPRAY
Renal impairment	No specific dose adjustment recommended. Use with caution in severe renal impairment (CrCl <30 mL/min) due to potential for increased exposure.
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh class C). No specific dose adjustment recommended for mild to moderate impairment.
Pediatric use	Not recommended for use in patients under 18 years due to potential adverse effects on cardiovascular system.
Geriatric use	Caution in patients >65 years due to increased risk of cardiovascular events; use lowest effective dose and monitor closely.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for TOSYMRA (TOSYMRA).

Breastfeeding	Excreted in breast milk; M/P ratio unknown. Due to potential adverse effects on infant cardiovascular and renal systems, not recommended during breastfeeding.
Teratogenic Risk	Pregnancy Category C: Inadequate human data; animal studies show fetal harm at high doses. Risk in first trimester unknown; avoid in second and third trimester as NSAIDs may cause premature closure of ductus arteriosus and oligohydramnios.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Nasal spray formulation contains sumatriptan, which is contraindicated in patients with coronary artery disease or risk factors due to risk of myocardial ischemia/infarction and other cardiac events.

Side Effect Profile

Serious Effects

Absolute Contraindications

["History of coronary artery disease, myocardial infarction, or ischemic heart disease","Wolff-Parkinson-White syndrome or other cardiac accessory pathway disorders","Uncontrolled hypertension","Hemiplegic or basilar migraine","Use within 24 hours of ergotamine derivatives or another 5-HT1 agonist","Concurrent use or within 2 weeks of MAO-A inhibitors","Known hypersensitivity to sumatriptan"]

Clinical Precautions

Precautions

["Risk of myocardial ischemia/infarction and other cardiac events","Cerebral hemorrhage, subarachnoid hemorrhage, and stroke","Serotonin syndrome","Increase in blood pressure","Medication overuse headache"]

Clinical Tips & Counseling

Drug interactions

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TOSYMRA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TOSYMRA (TOSYMRA).

How it works

Sumatriptan is a selective agonist of serotonin (5-HT1B/1D) receptors, leading to vasoconstriction of intracranial blood vessels and inhibition of trigeminal nerve transmission.

What the body does with it

Metabolism	Metabolized primarily by monoamine oxidase A (MAO-A); undergoes first-pass metabolism.
Excretion	Renal excretion of unchanged drug and metabolites; 70% recovered in urine as parent and metabolites, 30% in feces.
Half-life	Terminal elimination half-life approximately 2.5 hours; clinically relevant for dosing every 4-6 hours.
Protein binding	Low (<20%); primarily albumin.
Volume of Distribution	Approximately 1.0 L/kg; suggests distribution into total body water.
Bioavailability	Intranasal: approximately 30% relative to intravenous administration.
Onset of Action	Intranasal: 15-30 minutes.
Duration of Action	4-6 hours; analgesic effect correlating with plasma concentration.

Classification & Brands

Dosing & administration

10 mg intranasally as a single dose, may repeat once after 24 hours if needed. Maximum 2 doses in 7 days.

Dosage form	SPRAY
Renal impairment	No specific dose adjustment recommended. Use with caution in severe renal impairment (CrCl <30 mL/min) due to potential for increased exposure.
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh class C). No specific dose adjustment recommended for mild to moderate impairment.
Pediatric use	Not recommended for use in patients under 18 years due to potential adverse effects on cardiovascular system.
Geriatric use	Caution in patients >65 years due to increased risk of cardiovascular events; use lowest effective dose and monitor closely.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for TOSYMRA (TOSYMRA).

Breastfeeding	Excreted in breast milk; M/P ratio unknown. Due to potential adverse effects on infant cardiovascular and renal systems, not recommended during breastfeeding.
Teratogenic Risk	Pregnancy Category C: Inadequate human data; animal studies show fetal harm at high doses. Risk in first trimester unknown; avoid in second and third trimester as NSAIDs may cause premature closure of ductus arteriosus and oligohydramnios.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Nasal spray formulation contains sumatriptan, which is contraindicated in patients with coronary artery disease or risk factors due to risk of myocardial ischemia/infarction and other cardiac events.