Selegiline; Mechanism, Uses, Contraindications, Dosage, Side effects, Interaction

Selegiline
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Selegiline is a selective, irreversible inhibitor of Type B monoamine oxidase. It is used in newly diagnosed patients with Parkinson’s disease. It may slow the progression of the clinical disease and delay the requirement for levodopa therapy. It also may be given with levodopa upon the onset of disability. (From AMA Drug Evaluations Annual, 1994, p385) The compound without isomeric designation is Deprenyl.

Selegiline is a Monoamine Oxidase Inhibitor and Monoamine Oxidase Type B Inhibitor. The mechanism of action of selegiline is as a Monoamine Oxidase Inhibitor and Monoamine Oxidase-B Inhibitor.
Selegiline is an inhibitor of monoamine oxidase used in the treatment of depression and as adjunctive therapy in combination with levodopa and carbidopa in the therapy of Parkinson disease. Selegiline has been associated with a low rate of serum enzyme elevations during treatment but has not been linked to instances of clinically apparent acute liver injury.

Mechanism of action of Selegiline

Although the mechanisms for selegiline’s beneficial action in the treatment of Parkinson’s disease are not fully understood, the selective, irreversible inhibition of monoamine oxidase type B (MAO-B) is thought to be of primary importance. MAO-B is involved in the oxidative deamination of dopamine in the brain. Selegiline binds to MAO-B within the nigrostriatal pathways in the central nervous system, thus blocking microsomal metabolism of dopamine and enhancing the dopaminergic activity in the substantial nigra. Selegiline may also increase dopaminergic activity through mechanisms other than inhibition of MAO-B. At higher doses, selegiline can also inhibit monoamine oxidase type A (MAO-A), allowing it to be used for the treatment of depression.

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or

The action of selegiline is thought to be related to its irreversible inhibition of monoamine oxidase type B (MAO B), the major form of the enzyme in the human brain. MAO B, which is involved in the oxidative deamination of dopamine in the brain, is inhibited when selegiline binds covalently and stoichiometrically to the isoalloxazine flavin adenine dinucleotide (FAD) at its active center. Administration of 10 mg of selegiline a day produces almost complete inhibition of MAO B in the brain. Selegiline becomes a nonselective inhibitor of all monoamine oxidase (MAO) at higher doses, possibly at 20 to 40 mg a day. At these doses, tyramine-mediated hypertensive reaction with MAO-A blockade (“cheese reactions”) may occur.

Indications of Selegiline

Contra-Indications of Selegiline

Side Effects of Selegiline

The most common

More common

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Rare

Drug Interactions of Selegiline

Selegiline may interact with the following drug, supplements, & may change the efficacy of the drugs

Pregnancy Catagory

FDA Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Lactation

It is not known if selegiline passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children.

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Referances

Selegiline

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