LOPERAMIDE HYDROCHLORIDE capsule

Pays: États-Unis

Langue: anglais

Source: NLM (National Library of Medicine)

Ingrédients actifs:

LOPERAMIDE HYDROCHLORIDE (UNII: 77TI35393C) (LOPERAMIDE - UNII:6X9OC3H4II)

Disponible depuis:

McKesson Contract Packaging

DCI (Dénomination commune internationale):

LOPERAMIDE HYDROCHLORIDE

Composition:

LOPERAMIDE HYDROCHLORIDE 2 mg

Type d'ordonnance:

PRESCRIPTION DRUG

Statut de autorisation:

Abbreviated New Drug Application

Résumé des caractéristiques du produit

LOPERAMIDE HYDROCHLORIDE- LOPERAMIDE HYDROCHLORIDE CAPSULE
MCKESSON CONTRACT PACKAGING
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DESCRIPTION
Loperamide hydrochloride, 4-(p-chlorophenyl)-4-hydroxy-N,
N-dimethyl-α,α-diphenyl-1-
piperidinebutyramide monohydrochloride, is a synthetic antidiarrheal
for oral use.
Loperamide hydrochloride is available in 2 mg capsules.
Loperamide hydrochloride capsules, USP contain the following inactive
ingredients: colloidal silicon
dioxide, gelatin, iron oxides, lactose (hydrous), magnesium stearate,
microcrystalline cellulose, sodium
starch glycolate and titanium dioxide.
CLINICAL PHARMACOLOGY
_In vitro_ and animal studies show that loperamide hydrochloride acts
by slowing intestinal motility and by
affecting water and electrolyte movement through the bowel. Loperamide
binds to the opiate receptor in
the gut wall. Consequently, it inhibits the release of acetylcholine
and prostaglandins, thereby reducing
peristalsis, and increasing intestinal transit time. Loperamide
increases the tone of the anal sphincter,
thereby reducing incontinence and urgency.
In man, loperamide hydrochloride prolongs the transit time of the
intestinal contents. It reduces the daily
fecal volume, increases the viscosity and bulk density, and diminishes
the loss of fluid and electrolytes.
Tolerance to the antidiarrheal effect has not been observed. Clinical
studies have indicated that the
apparent elimination half-life of loperamide in man is 10.8 hours with
a range of 9.1 to 14.4 hours.
Plasma levels of unchanged drug remain below 2 nanograms per mL after
the intake of a 2 mg capsule of
loperamide hydrochloride. Plasma levels are highest approximately 5
hours after administration of the
capsule and 2.5 hours after the liquid. The peak plasma levels of
loperamide were similar for both
formulations. Elimination of loperamide mainly occurs by oxidative
N-demethylation. Cytochrome P450
(CYP450) isozymes, CYP2C8 and CYP3A4, are thought to play an important
role in loperamide N-
demethylation process since quercetin (CYP2C8 inhibitor) and
keto