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Selegiline information from DrugsUpdate  

See Available Brands of Selegiline in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation

Selegiline (l-deprenyl, Eldepryl) is a drug used for the treatment of early-stage Parkinson's disease, depression and senile dementia. In normal clinical doses it is a selective irreversible MAO-B inhibitor, however in larger doses it loses its specificity and also inhibits MAO-A. Dietary restrictions are common for MAOI treatments, but special dietary restrictions for lower doses have been found to be unnecessary, and dietary restrictions appear to be unnecessary at any dose when selegiline is taken as Emsam, the transdermal patch form, as no adverse events due to diet have ever been reported with Emsam. The drug was researched by Jozsef Knoll et al. (Hungary). Selegiline belongs to a class of drugs called phenethylamines. Selegiline consists of a l-desoxyephedrine (levomethamphetamine) skeleton with a propargyl group attached to the nitrogen atom.

Pharmacodynamics

Pharmacokinetics

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 hours.

Selegiline Indications / Selegiline Uses

Information Not Available

Selegiline Adverse Reactions / Selegiline Side Effects

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.

Precautions

Some patients given Selegiline may experience an exacerbation of levodopa associated side effects, presumably due to the increased amounts of dopamine reaction with super sensitive post-synaptic receptors. These effects may often be mitigated by reducing the dose of levodopa/carbidopa by approximately 10 to 30%.

The decision to prescribe Selegiline should take into consideration that the MAO system of enzymes is complex and incompletely understood and there is only a limited amount of carefully documented clinical experience with Selegiline. Consequently, the full spectrum of possible responses to Selegiline may not have been observed in pre-marketing evaluation of the drug. It is advisable, therefore, to observe patients closely for atypical responses.

Overdosage
Symptoms may include dizziness, irritability, hyperactivity, agitation, hallucinations, convulsions and coma. Immediate hospitalisation, with continuous observation and monitoring is strongly recommended.

Special Precautions

History of peptic ulcer, uncontrolled hypertension, arrhythmias, angina, psychosis. Severe liver or kidney dysfunction.

Other 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.

Other Interactions

Information Not Available

Dosage

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 weeks if needed.
Elderly: Initially, 2.5 mg daily.

Transdermal
Depression
Adult: Initially, 6 mg/24 hours, dose may be increased in steps of 3 mg/24 hours at intervals of not <2 weeks. Patients on doses ≥9 mg/24 hours should restrict intake of tyramine-rich foods during and for 2 weeks after discontinuing the treatment. Patches should be changed every 24 hours and the new patch is applied to a different site. Max: 12 mg/24 hours.

Food(before/after)

Should be taken with food

List of Contraindications

Selegiline and Pregnancy

Contraindicated in pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Selegiline and Lactation

Contraindicated in lactation

Selegiline and Children

Information Not Available

Selegiline and Geriatic

Information Not Available

Selegiline and Other Contraindications

Active ulceration. Pregnancy and lactation

Storage

Oral
Store at 15-30°C

Transdermal

Store at 15-30°C

Lab interference

Oral
Store at 15-30°C

Transdermal

Store at 15-30°C

Selegiline brands in India:

Eldepryl Elegelin Jumax Jumex Selerin Selgin

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