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Drug Information
Pharmacokinetics
| Indication
& Dosage | Action
| Interactions|Adverse
Effects & Precautions |
Brands available in Market
Pharmacokinetics.
Selegiline is readily absorbed from the gastrointestinal tract from
conventional preparations and crosses the blood-brain barrier. It
undergoes extensive first-pass metabolism in the liver to produce at
least 5 metabolites, including l-(-)-desmethylselegiline (norselegiline),
l-(-)-N-methylamphetamine and l-(-)-amphetamine. Concentrations of
selegiline metabolites are greatly reduced following administration of
the oral lyophilisate preparation, the majority of which undergoes
absorption through the buccal mucosa. It is excreted as metabolites
mainly in the urine and approximately 15% appears in the faeces.
Indication
& Dosage
Oral
ADJUCT IN PARKINSON PATIENTS ON LEVADOPA/CARBIDOPA
THERAPY: 10mg/day administered as divided doses of 5mg each taken at
breakfast and lunch. There is no evidence that higher doses offer
additional benefits.
Action
Selegiline’s beneficial adjunctive action in the treatment of
parkinson’ disease is, in part, due to inhibition of MAO-B. In addition
there is eveidence that this may act through other mechanisms to
increase dopaminergic activity.
Meperidine:
Contraindicated for use with meperidine since reports of fatal
interactions related to its MAO inhibiting activity.
Analgesic: Hyperpyrexia and CNS toxicity with pethidine.
Antidepressants: Hypertension and CNS excitation with fluoxetine.
Adverse Effect &
Precautions
Nausea, confusion, involuntary
movement, skin rash and psycholosis.
Precaution: Children cardiac arrhythmias, psychosis.
Pregnancy: Safety not established.
Breast Feeding: Use with caution
Man: May be given in reduced dose.
