ORAP pimozide tablet

Krajina: Spojené štáty

Jazyk: angličtina

Zdroj: NLM (National Library of Medicine)

Aktívna zložka:

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

Dostupné z:

Teva Select Brands

INN (Medzinárodný Name):

PIMOZIDE

Zloženie:

PIMOZIDE 2 mg

Typ predpisu:

PRESCRIPTION DRUG

Stav Autorizácia:

New Drug Application

Súhrn charakteristických

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-(4-piperid