治療腹瀉 Diarrhea, acute.
Diarrhea, chronic - Irritable bowel syndrome.
High output ileostomy.
Traveler's diarrhea.

Loperamide hydrochloride exerts antidiarrheal action by prolonging gastrointestinal transit time. Additionally, loperamide reduces fecal volume, increases viscosity and bulk density, and decreases fluid and electrolyte volume depletion. In vitro studies suggest a direct effect on the gastrointestinal wall by local interactions with cholinergic and noncholinergic (eg, opiate receptor) mechanisms.

[Absorption]
Bioavailability: 0.3%

[Metabolism]
Metabolism: Oxidative N-demethylation, Major
Major Substrate of CYP2C8 and CYP3A4

[Excretion]
Renal: 2%
Feces: Extensive, 33% unchanged

[Elimination Half Life]
9 to 10.8 hours

abdominal pain in the absence of diarrhea;
bacterial enterocolitis, caused by invasive organisms including Salmonella, Shigella, and Campylobacter; do not use as primary therapy;
acute dysentery, do not use as primary therapy;
hypersensitivity to loperamide or to any of the excipients;
infants below 24 months of age;
pseudomembranous colitis, associated with the use of broad spectrum antibiotics, do not use as primary therapy;
ulcerative colitis, acute, do not use as primary therapy

C [FDA]

Infant risk cannot be ruled out. [MDX]

[Central nervous system] Dizziness (1%)
[Gastrointestinal] Constipation (2% to 5%), abdominal cramps (?3%), nausea (?3%)

[Diarrhea, acute]
4 mg PO followed by 2 mg after each loose stool up to MAX 16 mg/day

[Diarrhea, chronic - Irritable bowel syndrome]
(initial) 4 mg PO followed by 2 mg after each loose stool up to MAX 16 mg/day
(maintenance) titrate to individual's need, average daily dosage 4-8 mg PO up to MAX 16 mg/day, may be taken as a single dose or in divided doses

[High output ileostomy]
dose used in some trials: 4 mg BID for 4 days, may then be increased to 12 mg daily for the remaining 3 days (total duration of therapy studied: 7 days)

[Traveler's diarrhea]
4 mg PO followed by 2 mg after each loose stool up to MAX 8 mg/day

[Diarrhea, acute]
(first day dosage, 2 to 5 y/o, 13 to 20 kg) 1 mg PO TID;
(first day dosage, 6 to 8 y/o, 20 to 30 kg) 2 mg PO BID;
(first day dosage, 8 to 12y/o, greater than 30 kg) 2 mg PO TID;
(subsequent daily dosage, 2 to 12 y/o) 1 mg/10 kg of body weight PO only after a loose stool, total daily dose should not exceed dosages for the first day

[Diarrhea, chronic - Irritable bowel syndrome]
therapeutic dose in children has not been established; 0.08 to 0.24 milligram/kilogram/day in 2 to 3 divided doses have been used

[Traveler's diarrhea]
(2 to 5 y/o, 11 to 21.9 kg) 1 mg PO followed by 1 mg after each loose stool up to MAX 3 mg/day
(6 to 8 y/o, 22 to 26.9 kg) 2 mg PO followed by 1 mg after each loose stool up to MAX 4 mg/day
(9 to 11y/o, 27 to 43 kg) 2 mg PO followed by 1 mg after each loose stool up to MAX 6 mg/day
(12 y/o and older) 4 mg PO followed by 2 mg after each loose stool up to MAX 8 mg/day

No dosing adjustments are necessary.

Nil.

Store at 15 to 25 degrees Celsius.