EMSAM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EMSAM (EMSAM).
Irreversible inhibitor of monoamine oxidase type B (MAO-B); increases synaptic concentrations of monoamines (e.g., dopamine) in the CNS.
| Metabolism | Hepatic, primarily via CYP2C19 and CYP3A4; also metabolized by MAO-A and MAO-B. |
| Excretion | Renal: 70-80% (as metabolites, primarily 5-(2-aminopropyl)-7-methyl-5,6,7,8-tetrahydro-1H-[1,3]oxazolo[3,4-d]pyridazine and other metabolites); Fecal: 10-15% |
| Half-life | Terminal half-life: 1.9-3.7 hours for the transdermal system due to continuous absorption, but effective half-life of MAO-B inhibition is 24-36 hours due to irreversible binding |
| Protein binding | Plasma protein binding: approximately 90% (primarily to albumin) |
| Volume of Distribution | Vd: 1.3-2.5 L/kg (indicates extensive tissue distribution) |
| Bioavailability | Transdermal: approximately 74% (systemic absorption rate); avoid oral administration due to extensive first-pass metabolism and high risk of tyramine reaction |
| Onset of Action | Transdermal: 2-3 days for initial antidepressant effect; full therapeutic benefit may require 2-4 weeks |
| Duration of Action | Transdermal: MAO-B inhibition persists for 2-4 weeks after discontinuation due to irreversible inhibition; clinical effect lasts while system is applied (change daily) |
6 mg/24 hours transdermally once daily; may increase to 9 mg/24 hours or 12 mg/24 hours after at least 2 weeks if needed.
| Dosage form | FILM, EXTENDED RELEASE |
| Renal impairment | No specific dose adjustment recommended; use caution in severe renal impairment (CrCl <30 mL/min) due to limited data. |
| Liver impairment | Contraindicated in patients with Child-Pugh Class C; for Class A or B, reduce dose to 6 mg/24 hours and avoid dose escalation. |
| Pediatric use | Safety and efficacy not established; use not recommended in patients under 18 years. |
| Geriatric use | Initiate at 6 mg/24 hours; consider lower doses due to increased risk of adverse effects; no specific maximum dose differs from adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EMSAM (EMSAM).
| Breastfeeding | Not recommended; no data on excretion in human milk. M/P ratio unknown. |
| Teratogenic Risk | Pregnancy Category C. First trimester: Risk cannot be ruled out; no adequate studies in pregnant women. Second and third trimesters: Potential for hypertensive crises and serotonin syndrome; use only if benefit justifies risk. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and signs of serotonin syndrome. Fetal monitoring for growth and well-being due to potential vasoconstrictive effects. |
■ FDA Black Box Warning
Increased risk of suicidal thoughts and behavior in children, adolescents, and young adults taking antidepressants. Monitor for clinical worsening, suicidality, or unusual changes in behavior. Not approved for pediatric use.
| Serious Effects |
["Concomitant use of other MAOIs, SSRIs, SNRIs, bupropion, or other serotonergic drugs.","Use within 14 days of other MAOIs or serotonergic drugs.","Pheochromocytoma or uncontrolled hypertension.","Known hypersensitivity to selegiline or components of the patch.","Use with tyramine-containing foods or beverages (e.g., aged cheese, cured meats, red wine)."]
| Precautions | ["Hypertensive crisis with tyramine-rich foods or sympathomimetic drugs; dietary restrictions required.","Serotonin syndrome when used with other serotonergic drugs (e.g., SSRIs, SNRIs).","Potential for elevated blood pressure; monitor blood pressure regularly.","Risk of serotonin syndrome with concomitant use of other MAOIs or within 14 days of discontinuation.","Avoid use in patients with pheochromocytoma, uncontrolled hypertension, or thyroid disease."] |
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| Fertility Effects | No specific human data; animal studies show no impairment of fertility. |