국가: 미국
언어: 영어
출처: NLM (National Library of Medicine)
PIMOZIDE (UNII: 1HIZ4DL86F) (PIMOZIDE - UNII:1HIZ4DL86F)
Avera McKennan Hospital
PIMOZIDE
PIMOZIDE 2 mg
PRESCRIPTION DRUG
Abbreviated New Drug Application
PIMOZIDE- PIMOZIDE TABLET AVERA MCKENNAN HOSPITAL ---------- 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 전체 문서 읽기