SELEGILINE HYDROCHLORIDE- selegiline hydrochloride tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

SELEGILINE HYDROCHLORIDE (UNII: 6W731X367Q) (SELEGILINE - UNII:2K1V7GP655)

Available from:

Mayne Pharma

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Selegiline Hydrochloride Tablets USP is indicated as an adjunct in the management of Parkinsonian patients being treated with levodopa/carbidopa who exhibit deterioration in the quality of their response to this therapy. There is no evidence from controlled studies that selegiline has any beneficial effect in the absence of concurrent levodopa therapy. Evidence supporting this claim was obtained in randomized controlled clinical investigations that compared the effects of added selegiline or placebo in patients receiving levodopa/carbidopa. Selegiline was significantly superior to placebo on all three principal outcome measures employed: change from baseline in daily levodopa/carbidopa dose, the amount of 'off' time, and patient self-rating of treatment success. Beneficial effects were also observed on other measures of treatment success (e.g., measures of reduced end of dose akinesia, decreased tremor and sialorrhea, improved speech and dressing ability and improved overall disability as assessed by walking

Product summary:

Selegiline Hydrchloride Tablets USP 5 mg are available for oral administration as white, round, convex face tablet debossed on one side with "1020" and blank on the other side. They are supplied as bottles of 60 (NDC 51862-146-06).

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

SELEGILINE HYDROCHLORIDE- SELEGILINE HYDROCHLORIDE TABLET
MAYNE PHARMA
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SELEGILINE HYDROCHLORIDE TABLETS USP 5 MG
RX ONLY
DESCRIPTION
Selegiline hydrochloride is a levorotatory acetylenic derivative of
phenethylamine. It is commonly
referred to in the clinical and pharmacological literature as
l-deprenyl.
The chemical name is:
(R)-(-)-_N_,2-dimethyl-_N_-2-propynylphenethylamine hydrochloride. It
is a white to
near white crystalline powder, freely soluble in water, chloroform,
and methanol, and has a molecular
weight of 223.75. The molecular formula is C
H •HCl. The structural formula is as follows:
Each tablet, for oral administration, contains 5 mg selegiline
hydrochloride. Inactive ingredients are
microcrystalline cellulose, lactose monohydrate, and stearic acid.
CLINICAL PHARMACOLOGY
The mechanisms accounting for selegiline's beneficial adjunctive
action in the treatment of Parkinson's
disease are not fully understood. Inhibition of monoamine oxidase,
type B, activity is generally
considered to be of primary importance; in addition, there is evidence
that selegiline may act through
other mechanisms to increase dopaminergic activity.
Selegiline is best known as an irreversible inhibitor of monoamine
oxidase (MAO), an intracellular
enzyme associated with the outer membrane of mitochondria. Selegiline
inhibits MAO by acting as a
'suicide' substrate for the enzyme; that is, it is converted by MAO to
an active moiety which combines
irreversibly with the active site and/or the enzymes essential FAD
cofactor. Because selegiline has
greater affinity for type B rather than for type A active sites, it
can serve as a selective inhibitor of
MAO type B if it is administered at the recommended dose.
MAOs are widely distributed throughout the body; their concentration
is especially high in liver,
kidney, stomach, intestinal wall, and brain. MAOs are currently
subclassified into two types, A and B,
which differ in their substrate specificity and tissue distribution.
In humans, intestinal MAO is
predominantly type