ZECUITY

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ZECUITY (ZECUITY).

How it works

Selegiline is a selective, irreversible inhibitor of monoamine oxidase type B (MAO-B). It inhibits the breakdown of dopamine by MAO-B, increasing dopaminergic activity in the brain.

What the body does with it

Metabolism	Hepatic metabolism primarily via MAO-B inhibition and further metabolism to N-desmethylselegiline, amphetamine, and methamphetamine. CYP450 enzymes not significantly involved.
Excretion	Sumatriptan is primarily eliminated by metabolism followed by renal excretion of metabolites. Approximately 60% of a dose is recovered in urine (22% as unchanged sumatriptan, 38% as metabolites) and 40% in feces (primarily metabolites).
Half-life	The terminal elimination half-life of sumatriptan is approximately 2 hours (range 1–4 hours). Due to this short half-life, a second dose may be considered if migraine recurs after initial relief, but no more than two doses in 24 hours via the same route.
Protein binding	Sumatriptan is approximately 14–21% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	The volume of distribution is approximately 2.4–3.0 L/kg, indicating extensive distribution into tissues beyond plasma.
Bioavailability	Iontophoretic transdermal system (Zecuity): Absolute bioavailability is approximately 99% of the delivered dose, as sumatriptan is delivered directly into the systemic circulation. The system delivers 6.5 mg of sumatriptan over 4 hours.
Onset of Action	Iontophoretic transdermal system (Zecuity): Onset of relief typically occurs within 30–60 minutes after application; the system delivers 6.5 mg over 4 hours.
Duration of Action	Duration of effect is typically 4–6 hours, consistent with the infusion profile of the patch. Patients may experience recurrence after this period and may need a second dose (if allowed).

Classification & Brands

Dosing & administration

Apply one 1.3 mg/24 hour transdermal system to a clean, dry, hairless area of the upper arm or thigh for 24 hours; can be repeated at 24-hour intervals for up to 12 weeks.

Dosage form	SYSTEM
Renal impairment	No specific dose adjustment recommended for GFR ≥30 mL/min; contraindicated in end-stage renal disease (GFR <15 mL/min) and in patients requiring dialysis.
Liver impairment	Contraindicated in Child-Pugh Class C (severe hepatic impairment); use with caution in Child-Pugh Class A or B, with no specific dose adjustment recommended in mild to moderate impairment.
Pediatric use	Not approved for use in pediatric patients (safety and effectiveness not established).
Geriatric use	No specific dose adjustment recommended; however, elderly patients may be more sensitive to anticholinergic effects; use with caution and monitor for adverse effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for ZECUITY (ZECUITY).

Breastfeeding	No human data on transfer into breast milk; M/P ratio unknown. Avoid breastfeeding due to potential for sumatriptan-related adverse effects (e.g., diarrhea, poor feeding) and treximet metabolites. Consider pump and discard during therapy.
Teratogenic Risk	Pregnancy Category C. First trimester: Animal studies show fetal resorption and skeletal abnormalities; human data limited. Second/third trimester: Risk of neonatal withdrawal (irritability, hypertonia, tremors) and persistent pulmonary hypertension of the newborn (PPHN) with late use. Consider risks vs benefits.

Warnings & precautions

■ FDA Black Box Warning

Increased risk of suicidal thinking and behavior in children, adolescents, and young adults taking antidepressants. ZECUITY is not approved for use in pediatric patients.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Concomitant use with other MAOIs or within 14 days of stopping therapy","Concomitant use with SSRIs, SNRIs, tricyclic antidepressants, bupropion, meperidine, tramadol, dextromethorphan, or St. John's Wort","Pheochromocytoma","Tyramine-rich diet (for doses >6 mg/24 hours or when using oral formulation)","Severe renal impairment (eGFR <15 mL/min/1.73 m²)"]

Clinical Precautions

Precautions

["Serotonin syndrome when used with other serotonergic drugs","Tyramine-induced hypertensive crisis if dietary tyramine restrictions are not followed (especially with higher doses)","Activation of mania/hypomania in bipolar disorder","Seizures in patients with history of seizure disorders","Suicidality monitoring in young adults and children"]

Clinical Tips & Counseling

Drug interactions

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ZECUITY

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ZECUITY (ZECUITY).

How it works

Selegiline is a selective, irreversible inhibitor of monoamine oxidase type B (MAO-B). It inhibits the breakdown of dopamine by MAO-B, increasing dopaminergic activity in the brain.

What the body does with it

Metabolism	Hepatic metabolism primarily via MAO-B inhibition and further metabolism to N-desmethylselegiline, amphetamine, and methamphetamine. CYP450 enzymes not significantly involved.
Excretion	Sumatriptan is primarily eliminated by metabolism followed by renal excretion of metabolites. Approximately 60% of a dose is recovered in urine (22% as unchanged sumatriptan, 38% as metabolites) and 40% in feces (primarily metabolites).
Half-life	The terminal elimination half-life of sumatriptan is approximately 2 hours (range 1–4 hours). Due to this short half-life, a second dose may be considered if migraine recurs after initial relief, but no more than two doses in 24 hours via the same route.
Protein binding	Sumatriptan is approximately 14–21% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	The volume of distribution is approximately 2.4–3.0 L/kg, indicating extensive distribution into tissues beyond plasma.
Bioavailability	Iontophoretic transdermal system (Zecuity): Absolute bioavailability is approximately 99% of the delivered dose, as sumatriptan is delivered directly into the systemic circulation. The system delivers 6.5 mg of sumatriptan over 4 hours.
Onset of Action	Iontophoretic transdermal system (Zecuity): Onset of relief typically occurs within 30–60 minutes after application; the system delivers 6.5 mg over 4 hours.
Duration of Action	Duration of effect is typically 4–6 hours, consistent with the infusion profile of the patch. Patients may experience recurrence after this period and may need a second dose (if allowed).

Classification & Brands

Dosing & administration

Apply one 1.3 mg/24 hour transdermal system to a clean, dry, hairless area of the upper arm or thigh for 24 hours; can be repeated at 24-hour intervals for up to 12 weeks.

Dosage form	SYSTEM
Renal impairment	No specific dose adjustment recommended for GFR ≥30 mL/min; contraindicated in end-stage renal disease (GFR <15 mL/min) and in patients requiring dialysis.
Liver impairment	Contraindicated in Child-Pugh Class C (severe hepatic impairment); use with caution in Child-Pugh Class A or B, with no specific dose adjustment recommended in mild to moderate impairment.
Pediatric use	Not approved for use in pediatric patients (safety and effectiveness not established).
Geriatric use	No specific dose adjustment recommended; however, elderly patients may be more sensitive to anticholinergic effects; use with caution and monitor for adverse effects.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for ZECUITY (ZECUITY).

Breastfeeding	No human data on transfer into breast milk; M/P ratio unknown. Avoid breastfeeding due to potential for sumatriptan-related adverse effects (e.g., diarrhea, poor feeding) and treximet metabolites. Consider pump and discard during therapy.
Teratogenic Risk	Pregnancy Category C. First trimester: Animal studies show fetal resorption and skeletal abnormalities; human data limited. Second/third trimester: Risk of neonatal withdrawal (irritability, hypertonia, tremors) and persistent pulmonary hypertension of the newborn (PPHN) with late use. Consider risks vs benefits.

Warnings & precautions

■ FDA Black Box Warning

Increased risk of suicidal thinking and behavior in children, adolescents, and young adults taking antidepressants. ZECUITY is not approved for use in pediatric patients.