Selegiline

Indications
 Oral
Early parkinsonism
Adult: As conventional preparations: 10 mg daily either as a single dose in the morning or in 2 divided doses of 5 mg at breakfast and lunchtime. As oral lyophilisate tablets: Initially, 1.25 mg daily, may increase to 2.5 mg once daily after at least 6 wk if needed.
Elderly: Initially, 2.5 mg daily.
Transdermal
Depression
Adult: Initially, 6 mg/24 hr, dose may be increased in steps of 3 mg/24 hr at intervals of not <2 wk. Patients on doses ≥9 mg/24 hr should restrict intake of tyramine-rich foods during and for 2 wk after discontinuing the treatment. Patches should be changed every 24 hr and the new patch is applied to a different site. Max: 12 mg/24 hr.
Contraindications
 Active ulceration. Pregnancy and lactation.
Warnings / Precautions
 History of peptic ulcer, uncontrolled hypertension, arrhythmias, angina, psychosis. Severe liver or kidney dysfunction.
Adverse Reactions
 Hallucinations, dizziness, confusion, anxiety, dreams, palpitations, syncope, irritability, restlessness, nausea, dry mouth, sexual dysfunction, hypotension, arrhythmia, angina, tachycardia. Orthostatic hypotension, chest pain, insomnia, abnormal dreams. Transient elevations in liver enzymes.
Overdose Reactions
 Symptoms may include dizziness, irritability, hyperactivity, agitation, hallucinations, convulsions and coma. Immediate hospitalisation, with continuous observation and monitoring is strongly recommended.
Drug Interactions
 Amantadine may increase BP when used together. Risk of hypertensive effect when used with dopamine. Concurrent use with dextromethorphan increases the risk of adverse effects.
Potentially Fatal: Risk of muscular rigidity, severe agitation and elevated temperature when used with meperidine. Increased risk of toxicity when used with TCAs or SSRIs. Risk of orthostatic hypotension when used with bupropion.
See Below for More selegiline Drug Interactions
Mechanism of Actions
 Selegiline increases dopaminergic activity by intervening with the re-uptake of dopamine at the synapse. It also irreversibly inhibits the MAO-B which is involved in the metabolism of dopamine.
Absorption: Readily absorbed from the GI tract (oral). Bioavailability is about 10%.
Distribution: Rapidly distributed throughout the body and crosses the blood-brain barrier.
Metabolism: Extensive hepatic first-pass effect; converted to L-(-)-desmethylselegiline, L-(-)-N-methylamfetamine and L-(-)-amfetamine.
Excretion: Mainly as metabolites in the urine; about 15% is excreted via faeces. Elimination half-life: about 10 hr.
Administration
 Should be taken with food.
Storage Conditions
 Oral: Store at 15-30°C. Transdermal: Store at 15-30°C.
ATC Classification
 N04BD01 - selegiline ; Belongs to the class of dopaminergic agents, monoamine oxidase B inhibitors. Used in the management of Parkinson's disease.
Storage
 Oral: Store at 15-30°C. Transdermal: Store at 15-30°C.
Available As
  • Selegiline 10 mg
  • Selegiline 5 mg

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