imodium- Loperamide Hydrochloride capsule

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Loperamide Hydrochloride (UNII: 77TI35393C) (Loperamide - UNII:6X9OC3H4II)

Available from:

McNeil Consumer Healthcare

INN (International Name):

Loperamide Hydrochloride

Pharmaceutical form:

CAPSULE

Composition:

2 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

IMODIUM® (loperamide hydrochloride) is indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. IMODIUM® is also indicated for reducing the volume of discharge from ileostomies. IMODIUM is contraindicated in patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients. IMODIUM is contraindicated in patients with abdominal pain in the absence of diarrhea. IMODIUM is not recommended in infants below 24 months of age. IMODIUM should not be used as the primary therapy: A specific clinical study designed to assess the abuse potential of loperamide at high doses resulted in a finding of extremely low abuse potential. Studies in morphine-dependent monkeys demonstrated that loperamide hydrochloride at doses above those recommended for humans prevented signs of morphine withdrawal. However, in humans, the naloxone challenge pupil test, which when positive indicates opiate-like effects, performed

Product summary:

Capsules - each capsule contains 2 mg of loperamide hydrochloride. The capsules have a light green body and a dark green cap with "JANSSEN" imprinted on one segment and "IMODIUM" on the other segment. IMODIUM® capsules are supplied in bottles of 100. NDC 50458-400-10 (100 CAPSULES) Store at 15°-25°C (59°-77°F).

Summary of Product characteristics

IMODIUM- LOPERAMIDE HYDROCHLORIDE CAPSULE
MCNEIL CONSUMER HEALTHCARE
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IMODIUM CAPSULES
DESCRIPTION
IMODIUM® (loperamide hydrochloride),
4-(p-chlorophenyl)-4-hydroxy-N,N-dimethyl-_a,a_-diphenyl-
1-piperidinebutyramide monohydrochloride, is a synthetic antidiarrheal
for oral use.
IMODIUM® is available in 2mg capsules.
The inactive ingredients are: Lactose, cornstarch, talc, and magnesium
stearate. IMODIUM® capsules
contain FD&C Yellow No. 6.
CLINICAL PHARMACOLOGY
_IN VITRO_ and animal studies show that IMODIUM® (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, IMODIUM® prolongs the transit time of the intestinal
contents. It reduces 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 - 14.4 hours. Plasma levels
of unchanged drug remain below 2 nanograms per mL after the intake of
a 2mg capsule of IMODIUM®.
Plasma levels are highest approximately five 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 ketoconazole (CYP3A4 inhibitor)
significantly inhibited the N-
demethylation process _in vitro_ by 40% and 90%, respectively. In
addition, CYP2B6 and