Apo-Selegiline - General Information
A selective, irreversible inhibitor of Type B monoamine oxidase. It is used in newly diagnosed patients with Parkinson&
Pharmacology of Apo-Selegiline
Dopamine is an essential chemical that occurs in many parts of the body. It is the premature degradation of dopamine that results in the symptoms of Parkinson's disease. Monoamine oxidase (MAO) is an enzyme which accelerates the breakdown of dopamine. Apo-Selegiline can prolong the effects of dopamine in the brain by preventing its breakdown through seletively blocking MAO. It also may prevent the removal of dopamine between nerve endings and enhance release of dopamine from nerve cells.
Apo-Selegiline for patients
Patients should be advised of the possible need to reduce levodopa dosage after the initiation of ELDEPRYL therapy.
Patients (or their families if the patient is incompetent) should be advised not to exceed the daily recommended dose of 10 mg. The risk of using higher daily doses of selegiline should be explained, and a brief description of the 'cheese reaction' provided. Rare hypertensive reactions with selegiline at recommended doses associated with dietary influences have been reported.
Consequently, it may be useful to inform patients (or their families) about the signs and symptoms associated with MAOI induced hypertensive reactions. In particular, patients should be urged to report, immediately, any severe headache or other atypical or unusual symptoms not previously experienced.
The occurrence of stupor, muscular rigidity, severe agitation, and elevated temperature has been reported in some patients receiving the combination of selegiline and meperidine. Symptoms usually resolve over days when the combination is discontinued. This is typical of the interaction of meperidine and MAOIs. Other serious reactions (including severe agitation, hallucinations, and death) have been reported in patients receiving this combination. Severe toxicity has also been reported in patients receiving the combination of tricyclic antidepressants and ELDEPRYL and selective serotonin reuptake inhibitors and ELDEPRYL. One case of hypertensive crisis has been reported in a patient taking the recommended doses of selegiline and a sympathomimetic medication (ephedrine).
ELDEPRYL is contraindicated in patients with a known hypersensitivity to this drug.
ELDEPRYL is contraindicated for use with meperidine (DEMEROL & other trade names). This contraindication is often extended to other opioids.
Additional information about Apo-Selegiline
Apo-Selegiline Indication: For the adjunct treatment for Parkinson's disease and depression.
Mechanism Of Action: Although the mechanisms for selegiline's beneficial action in the treatment of Parkinson's disease are not fully understood, the 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. Apo-Selegiline is best known as an irreversible inhibitor of MAO. MAO's activity is inhibited when selegiline binds to the isoalloxazine flavin adenine dinucleotide (FAD) at its active center. In addition, there is evidence that selegiline may increase dopaminergic activity through other mechanisms.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Selegiline
Synonyms: L-Deprenalin; Selegeline Hcl; Selegilina [Inn-Spanish]; Selegilinum [Inn-Latin]
Drug Category: Dopaminergics; Neuroprotective Agents; Antiparkinson Agents; Antidyskinetics; Central Nervous System Agents; Monoamine Oxidase Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Selegiline: Apo-Selegiline; Carbex; Eldepryl; Gen-Selegiline; Jumex; Novo-Selegiline; Nu-Selegiline; Sd Deprenyl;
Absorption: Rapidly absorbed from the gastrointestinal tract.
Toxicity (Overdose): LD50=63 mg/kg (rats, IV)
Protein Binding: > 99.5%
Biotransformation: Not Available
Half Life: 2 hours
Dosage Forms of Apo-Selegiline: Tablet Oral
Chemical IUPAC Name: N-methyl-N-[(2R)-1-phenylpropan-2-yl]prop-2-yn-1-amine
Chemical Formula: C13H17N
Selegiline on Wikipedia: http://en.wikipedia.org/wiki/Selegiline
Organisms Affected: Humans and other mammals