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:

American Health Packaging

INN (International Name):

LOPERAMIDE HYDROCHLORIDE

Composition:

LOPERAMIDE HYDROCHLORIDE 2 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Loperamide hydrochloride is 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 difficile ) 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 coadministration 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.

Product summary:

Loperamide hydrochloride capsules USP, 2 mg are available as: A light brown opaque body and dark brown opaque capsule, imprinted "TEVA" on the cap and "0311" on the body and packaged in unit dose packages of 100 (10 x 10) NDC 60687-229-01. Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. FOR YOUR PROTECTION: Do not use if blister is torn or broken. KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN. PACKAGING INFORMATION American Health Packaging unit dose blisters (see How Supplied section) contain drug product from Teva Pharmaceuticals USA, Inc. as follows: (2 mg / 100 UD) NDC 60687-229-01 packaged from NDC 0093-0311 Distributed by: American Health Packaging Columbus, OH 43217 8422901/0717

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

LOPERAMIDE HYDROCHLORIDE- LOPERAMIDE HYDROCHLORIDE CAPSULE
AMERICAN HEALTH PACKAGING
----------
LOPERAMIDE HYDROCHLORIDE CAPSULES USP
8422901/0717
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 (SEE WARNINGS AND OVERDOSAGE).
LOPERAMIDE HYDROCHLORIDE IS CONTRAINDICATED IN PEDIATRIC PATIENTS LESS
THAN 2 YEARS OF AGE (SEE CONTRAINDICATIONS).
AVOID LOPERAMIDE HYDROCHLORIDE 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 is a white to slightly yellow powder and is
freely soluble in
methanol, isopropyl alcohol, chloroform and slightly soluble in water.
Loperamide hydrochloride,
4-(p-chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-
piperidinebutyramide monohydrochloride, is a synthetic antidiarrheal
for oral use. Its
structural formula is:
C
H
ClN
O
•HCl           M.W. 513.51
Loperamide hydrochloride is available in 2 mg capsules.
The inactive ingredients: dimethylpolysiloxane, gelatin, iron oxide
black, iron oxide red,
iron oxide yellow, lactose monohydrate, pregelatinized corn starch,
magnesium stearate,
shellac, and titanium dioxide.
29
33
2
2
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 peristalsis, and
increasing intestinal
transit time. Loperamide increases the tone of the anal sphincter,
thereby reducing
incontinence and urgency.
Pharmacodynamics
Loperamide prolongs the transit time of the intestinal contents. It
reduces daily fecal
volume, increases the visc