LOPERAMIDE HYDROCHLORIDE capsule

Šalis: Jungtinės Valstijos

kalba: anglų

Šaltinis: NLM (National Library of Medicine)

Veiklioji medžiaga:

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

Prieinama:

Bionpharma Inc.

Vartojimo būdas:

ORAL

Recepto tipas:

PRESCRIPTION DRUG

Terapinės indikacijos:

Loperamide hydrochloride capsules are indicated for the control and symptomatic relief of acute nonspecific diarrhea in patients 2 years of age and older and of chronic diarrhea in adults associated with inflammatory bowel disease. Loperamide hydrochloride capsules are also indicated for reducing the volume of discharge from ileostomies. Loperamide hydrochloride capsules are contraindicated in: - pediatric patients less than 2 years of age due to the risks of respiratory depression and serious cardiac adverse reactions (see WARNINGS ). - patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients. - patients with abdominal pain in the absence of diarrhea. - patients with acute dysentery, which is characterized by blood in stools and high fever. - patients with acute ulcerative colitis. - patients with bacterial enterocolitis caused by invasive organisms including Salmonella , Shigella , and Campylobacter . - patients with pseudomembranous colitis (e.g., Clostridium difficle ) associated with the use of broad-spectrum antibiotics. Loperamide is not a controlled substance. Loperamide is a mu-opioid agonist. A human abuse potential study of loperamide hydrochloride at single doses up to 60 mg (3.75 times the recommended maximum adult dosage of 16 mg per day) was compared, in a double-blind cross-over design using nine subjects who had been active opiate users, to a threshold dose of codeine sulfate at 120 mg (96 mg base) or placebo. This resulted in one subject (11%) feeling a drug on placebo and identifying it as "dope" (heroin) and liking it slightly. Codeine was felt by 56% of subjects and identified as "dope" by 44%. Loperamide was felt by 44% of subjects and identified as "dope" by 11% and possibly dope mixed with some other kind of drug by another 22%. Loperamide abuse and misuse have been reported, especially at doses of 60 mg or greater. Loperamide can have greater CNS opioid effects at higher doses or with co-administration of drugs that increase systemic exposure and/or increase CNS penetration of loperamide (through inhibition of the CYP450 enzyme system or inhibition of P-glycoprotein). Loperamide is primarily being misused for relief from opioid withdrawal, and abused by a few users who obtain some (reportedly mild-moderate) level of euphoria. In animals, parenteral administration of loperamide hydrochloride can cause physical dependence, cross-tolerance to opioids, and all the other pharmacologic effects typical of mu-opioid agonists. Studies in morphine-dependent monkeys demonstrated that loperamide hydrochloride at doses above those recommended for humans prevented signs of morphine withdrawal.

Produkto santrauka:

Loperamide hydrochloride capsules, USP are available containing 2 mg of loperamide hydrochloride, USP. The capsules have a hard-shell gelatin capsule with a white opaque cap and a white opaque body filled with white to off-white powder blend. The capsule is printed with “ LM1 ” in black ink on the body. Loperamide hydrochloride capsules, USP are supplied in bottles of 100 (NDC 69452-271-20) and bottles of 500 (NDC 69452-271-30). Store at 20°C to 25°C (68°F to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure. Distributed by: Bionpharma Inc. Princeton, NJ 08540 MADE IN INDIA Revised: 9/2023 948026802 FDA-04

Autorizacija statusas:

Abbreviated New Drug Application

Prekės savybės

LOPERAMIDE HYDROCHLORIDE- LOPERAMIDE HYDROCHLORIDE CAPSULE
BIONPHARMA INC.
----------
LOPERAMIDE HYDROCHLORIDE CAPSULES, USP
RX ONLY
WARNING: TORSADES DE POINTES AND SUDDEN DEATH
CASES OF TORSADES DE POINTES, CARDIAC ARREST, AND DEATH HAVE BEEN
REPORTED WITH THE USE OF A HIGHER THAN RECOMMENDED DOSAGES OF
LOPERAMIDE HYDROCHLORIDE CAPSULES (SEE WARNINGSAND
OVERDOSAGE).
LOPERAMIDE HYDROCHLORIDE CAPSULES ARE CONTRAINDICATED IN PEDIATRIC
PATIENTS LESS THAN 2 YEARS OF AGE (SEE CONTRAINDICATIONS).
AVOID LOPERAMIDE HYDROCHLORIDE CAPSULES DOSAGES HIGHER THAN
RECOMMENDED IN ADULTS AND PEDIATRIC PATIENTS 2 YEARS OF AGE AND
OLDER DUE TO THE RISK OF SERIOUS CARDIAC ADVERSE REACTIONS (SEE
DOSAGE AND ADMINISTRATION).
DESCRIPTION
Loperamide hydrochloride,
4-(p-chlorophenyl)-4-hydroxy-N,N-dimethyl-a,adiphenyl-1-
piperidinebutyramide monohydrochloride, is a synthetic antidiarrheal
for oral use.
The molecular formula for loperamide hydrochloride, USP is C
H
ClN
O
HCl, with a
molecular weight of 513.50. The structural formula is:
Loperamide hydrochloride, USP is available in 2 mg capsules.
Loperamide hydrochloride capsules, USP contain the following inactive
ingredients:
colloidal silicon dioxide, lactose monohydrate, microcrystalline
cellulose, magnesium
29
33
2
2
stearate, and sodium starch glycolate. The hard-capsule shell is
composed of gelatin,
sodium lauryl sulfate, and titanium dioxide. The capsules are printed
with black ink
composed of black iron oxide, potassium hydroxide, propylene glycol,
and shellac.
CLINICAL PHARMACOLOGY
Mechanism of Action
_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 propulsive
peristalsis, and increasing
intestinal transit time. Loperamide increases the tone of the anal
sphincter, thereby
reducing incontinence and urgency.
Pharmacody