Selegiline indications

In the United States, the three MAOIS available for the treatment of psychiatric conditions are phenelzine (Nardil), tranylcypromine (Parnate), and isocarboxazid (Marplan). All three agents have indications for adult major depression (>16 years old) and, more specifically, atypical depression (anergia, hypersomnia, hy-perphagia, somatization, and anxiety symptoms). Although not indicated for anxiety, the MAOIs can also be particularly helpful in treatment of these disorders. Selegiline or L-deprenyl (Eldepryl) is also available in the United States and indicated for symptoms of Parkinson s disease and depression. 

A comparison of the pharmacokinetics of selegiline in 14 male patients (18 to 30 years of age) with 6 elderly male patients (age > 60 years) indicated that the Cmm and the AUC remains unaltered between the young and the elderly patients. The tm of selegiline in the elderly patients was almost twofold longer than in the young patients (3.2 h in the elderly patients vs. 1.5 h in the young) however, because of the small sample size and high variability in tm p, this difference may not be a real difference and may not have any clinical impact. 

The effects of treatment with selegiline, an MAO-B inhibitor, on plasma levels of insulin-like growth factor I (IGF-I) (as indicator of GH secretion), levels of monoamines and their metabolites, and the activity and content of tyrosine hydroxylase — the rate-limiting enzyme in the biosynthesis of catecholamines — in the hypothalamus and hypophysis of old animals have been studied. It is believed that the antiaging effects of selegiline are due to restoration of hypothalamic hormones. 

The neuroprotection of SH-SY54 cells from apoptosis caused by NOR-4 and SIN-1 is not related to inhibition of MAO-B, because SH-SY54 contains only MAO-A. Selegiline is able to protect dopaminergic neurons from the toxicity of MPTP and also of MPP an oxidized product of MPTP by MAO-B. This indicates that the neuroprotection by selegiline does not require blockage of the conversion of MPTP to MPP+. 

Trade names Apo-Selegiline Carbex Eldeprine Eldepryl (Somerset) Emsam Jumex Movergan Novo-Selegiline Plurimen Indications Parkinsonism... 

FIGURE 87 Monoamine oxidase B preferentially uses dopamine and is inhibited by selegiline. Clinical evidence indicates that 10 mg of selegiline in combination with levodopa and carbidopa is superior to levodopa-carbidopa therapy alone. There are indications that selegiline alone can slow the progression of Parkinson s disease, when taken in the early stages of the disease. 

Selegiline [(/ )(-)-W,a-dimethyl-W-(2-propynyl)benzeneethanamine, Elde-pryl. Deprenyl, 1] is a phenethylamine derivative which is pharmacologically active in the levo form. It is indicated as adjuvant treatment with levo-dopa in Parkinson s disease, and is supplied as a 5 mg tablet of selegiline hydrochloride. It belongs to the class of type B inhibitors of monoamine oxidase (MAOI-B). At high doses (>40 mg/day in man), selegiline loses its MAOI-B specificity and also inhibits MAO-A. 

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