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:

Mylan Pharmaceuticals Inc.

INN (International Name):

LOPERAMIDE HYDROCHLORIDE

Composition:

LOPERAMIDE HYDROCHLORIDE 2 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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: 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 are available containing 2 mg of loperamide hydrochloride, USP. The capsules are hard-shell gelatin capsules with a light brown opaque cap and a light brown opaque body filled with white to off-white powder blend. The capsules are axially printed with MYLAN over 2100 in black ink on both the cap and the body. They are available as follows: NDC 0378-2100-01 bottles of 100 capsules NDC 0378-2100-05 bottles of 500 capsules Store at 20° to 25°C (68° 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. Manufactured for: Mylan Pharmaceuticals Inc. Morgantown, WV 26505 U.S.A. Revised: 9/2022 VPL:LOP:R1

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

LOPERAMIDE HYDROCHLORIDE- LOPERAMIDE HYDROCHLORIDE CAPSULE
MYLAN PHARMACEUTICALS INC.
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WARNING: TORSADES DE POINTES AND SUDDEN DEATH
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: black
iron oxide, colloidal silicon dioxide, gelatin, lactose monohydrate,
magnesium stearate,
microcrystalline cellulose, red iron oxide, sodium lauryl sulfate,
sodium starch glycolate,
titanium dioxide, and yellow iron oxide. In addition, the black
imprinting ink also contains
black iron oxide, D&C Yellow No. 10 Aluminum Lake, FD&C Blue No. 1
Aluminum Lake,
FD&C Blue No. 2 Aluminum Lake, FD&C Red No. 40 Aluminum Lake,
propylene glycol,
and shellac glaze.
● CASES OF TORSADES DE POINTES, CARDIAC ARREST, AND DEATH HAVE
BEEN REPORTED WITH THE USE OF A HIGHER THAN RECOMMENDED DOSAGE
OF LOPERAMIDE HYDROCHLORIDE CAPSULES (SEE WARNINGS AND
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 ).
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
_In vitro _and animal studies show that loperamide hydrochloride
capsules act 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.
PHARMACODYNAMICS
Loperamide prolongs the transi