ORAP- pimozide tablet

Страна: США

мова: англійська

Джерело: NLM (National Library of Medicine)

Активний інгредієнт:

PIMOZIDE (UNII: 1HIZ4DL86F) (PIMOZIDE - UNII:1HIZ4DL86F)

Доступна з:

Teva Select Brands

Адміністрація маршрут:

ORAL

Тип рецепту:

PRESCRIPTION DRUG

Терапевтичні свідчення:

ORAP (pimozide) is indicated for the suppression of motor and phonic tics in patients with Tourette’s Disorder who have failed to respond satisfactorily to standard treatment. ORAP is not intended as a treatment of first choice nor is it intended for the treatment of tics that are merely annoying or cosmetically troublesome. ORAP should be reserved for use in Tourette’s Disorder patients whose development and/or daily life function is severely compromised by the presence of motor and phonic tics. Evidence supporting approval of pimozide for use in Tourette’s Disorder was obtained in two controlled clinical investigations which enrolled patients between the ages of 8 and 53 years. Most subjects in the two trials were 12 or older. - ORAP (pimozide) is contraindicated in the treatment of simple tics or tics other than those associated with Tourette’s Disorder. - ORAP should not be used in patients taking drugs that may, themselves, cause motor and phonic tics (e.g., pemoline, methylphenidate and amphetamines) un

Огляд продуктів:

ORAP (pimozide) 1 mg tablets are white, oval tablets, debossed “ORAP 1”, partially scored on one side and scored on the other. They are available in bottles of 100 (NDC 57844-151-01). ORAP (pimozide) 2 mg tablets are white, oval tablets, debossed “ORAP 2”, partially scored on one side and scored on the other. They are available in bottles of 100 (NDC 57844-198-01). Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) [see USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the official compendium. Pharmacist: Dispense in child-resistant container. Manufactured in Croatia by: PLIVA HRVATSKA d.o.o. Zagreb, Croatia Manufactured for: Teva Select Brands, Horsham, PA 19044 Division of Teva Pharmaceuticals USA Rev. 4/2018 ORA-001

Статус Авторизація:

New Drug Application

Характеристики продукта

ORAP- PIMOZIDE TABLET
TEVA SELECT BRANDS
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ORAP (PIMOZIDE)
TABLETS
DESCRIPTION
ORAP (pimozide) is an orally active antipsychotic agent of the
diphenyl-butylpiperidine series. The
structural formula of pimozide,
1-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2H-
benzimidazole-2-one is:
The solubility of pimozide in water is less than 0.01 mg/mL; it is
slightly soluble in most organic
solvents.
Each white ORAP tablet contains either 1 mg or 2 mg of pimozide and
the following inactive
ingredients: calcium stearate, microcrystalline cellulose, lactose
anhydrous and corn starch.
CLINICAL PHARMACOLOGY
PHARMACODYNAMIC ACTIONS
ORAP (pimozide) is an orally active antipsychotic drug product which
shares with other antipsychotics
the ability to blockade dopaminergic receptors on neurons in the
central nervous system. Although its
exact mode of action has not been established, the ability of pimozide
to suppress motor and phonic tics
in Tourette’s Disorder is thought to be a function of its
dopaminergic blocking activity. However,
receptor blockade is often accompanied by a series of secondary
alterations in central dopamine
metabolism and function which may contribute to both pimozide’s
therapeutic and untoward effects. In
addition, pimozide, in common with other antipsychotic drugs, has
various effects on other central
nervous system receptor systems which are not fully characterized.
METABOLISM AND PHARMACOKINETICS
More than 50% of a dose of pimozide is absorbed after oral
administration. Based on the
pharmacokinetic and metabolic profile, pimozide appears to undergo
significant first pass metabolism.
Peak serum levels occur generally six to eight hours (range 4-12
hours) after dosing.
Pimozide is extensively metabolized, primarily by N-dealkylation in
the liver. This metabolism is
®
®
catalyzed mainly by the cytochrome P450 3A4 (CYP 3A4) enzymatic system
and to a lesser extent, by
cytochrome P450 1A2 (CYP 1A2) and cytochrome P450 2D6 (CYP 2D6). Two
major metabolites have
been identified, 1-