Selegiline Hydrochloride CAS 14611-52-0

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Selegiline Hydrochloride is a synthetic derivative of phenethylamine and a selective, irreversible inhibitor of monoamine oxidase type B (MAO-B). It is primarily used as an adjunct therapy for Parkinson's disease and is also prescribed for certain types of depression in some regions.

Below is a concise English overview of its key properties, uses, and pharmacological profile:

1. Chemical and Physical Characteristics

IUPAC Name: (R)-(-)-N,α-Dimethyl-N-2-propynylphenethylamine Hydrochloride.

Molecular Formula: C13H17N·HCl.

Molecular Weight: 223.75 g/mol.

Physical Form: White to near-white crystalline powder, freely soluble in water, chloroform, and methanol.

2. Pharmacological Mechanism

MAO-B Inhibition: Selegiline selectively and irreversibly inhibits MAO-B, an enzyme responsible for the breakdown of dopamine in the brain. By inhibiting this enzyme, it increases the availability of dopamine, which is beneficial for managing Parkinsonian symptoms.

Dose-Dependent Selectivity: At recommended therapeutic doses (typically ≤10 mg/day), it selectively inhibits MAO-B. However, at higher doses, its selectivity may diminish, potentially leading to non-selective MAO inhibition and associated risks.

Metabolites: Selegiline is metabolized in the liver to several compounds, including L-amphetamine and L-methamphetamine, which may contribute to its pharmacological effects.

3. Therapeutic Uses

Parkinson's Disease (Adjunct Therapy):

Indication: Used as an adjunct to levodopa/carbidopa therapy in patients experiencing motor fluctuations (e.g., “wearing-off” phenomena). It helps to enhance and prolong the effects of levodopa.

Dosage: Typically administered in 5 mg or 10 mg tablets, taken twice daily (5 mg each time) for a total of 10 mg per day.

Depression: In some countries, transdermal patches of Selegiline (e.g., 6 mg/24h or 12 mg/24h) are approved for treating major depressive disorder. The transdermal route bypasses first-pass metabolism, reducing the formation of amphetamine-like metabolites.

4. Clinical Considerations

Contraindications:

Not recommended for patients with known hypersensitivity to Selegiline or any of its components.

Contraindicated with meperidine (Demerol) and other opioids due to the risk of severe reactions.

Potential Side Effects: Common adverse effects may include nausea, dizziness, insomnia, and orthostatic hypotension. At higher doses, there is a risk of hypertensive crisis due to potential non-selective MAO inhibition.

Special Populations: Caution is advised in patients with hepatic impairment, as the drug is extensively metabolized in the liver. Renal impairment does not significantly affect its clearance.