PIMOZIDE tablet

Země: Spojené státy

Jazyk: angličtina

Zdroj: NLM (National Library of Medicine)

Aktivní složka:

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

Dostupné s:

Avera McKennan Hospital

INN (Mezinárodní Name):

PIMOZIDE

Složení:

PIMOZIDE 2 mg

Druh předpisu:

PRESCRIPTION DRUG

Stav Autorizace:

Abbreviated New Drug Application

Charakteristika produktu

PIMOZIDE- PIMOZIDE TABLET
AVERA MCKENNAN HOSPITAL
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PIMOZIDE TABLETS, USP
DESCRIPTION
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]-4piperidinyl]-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 Pimozide 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
Pimozide tablets, USP 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 tablets, USP 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 to 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