Loperamide is a synthetic piperidine derivative, is an opioid drug used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. In most countries it is available generically and under brand names such as Lopex, Imodium, Dimor, Fortasec, Lopedium, and Pepto Diarrhea Control. It was developed at Janssen Pharmaceutica
Loperamide slows the rhythm of digestion so that the small intestines have more time to absorb fluid and nutrients from the foods you eat.
Loperamide is used to treat diarrhea. Loperamide is also used to reduce the amount of stool in people who have an ileostomy (re-routing of the bowel through a surgical opening in the stomach).
It is an opioid-receptor agonist and acts on the μ-opioid receptors in the myenteric plexus of the large intestine; by itself it does not affect the central nervous system.
It works by decreasing the activity of the myenteric plexus, which, like morphine, decreases the tone of the longitudinal smooth muscles but increases the tone of circular smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.
IUPAC NAME - 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]- N,N-dimethyl-2,2-diphenylbutanamide.
IMPORTENT
You should not use this medication if you are allergic to loperamide, or if you have:
stools that are bloody, black, or tarry; or
if you have diarrhea that is caused by taking an antibiotic.
Ask a doctor or pharmacist if it is safe for you to take this medicine if you have:
a fever;
mucus in your stools;
a history of liver disease; or
if you are taking an antibiotic.
FDA pregnancy category C. It is not known whether loperamide will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.
Loperamide can pass into breast milk and may harm a nursing baby. You should not breast-feed while you are using loperamide.
Do not give this medicine to a child without medical advice.
IF YOU FORGET A DOSE -
If you are taking scheduled doses of loperamide, take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
Loperamide Dosing Information
Usual Adult Dose for Diarrhea -- Acute:
Tablets, capsules, and liquid:
Initial: 4 mg orally after the first loose stool, then
Maintenance: 2 mg after each loose stool, not to exceed 16 mg in any 24-hour period. Clinical improvement is usually observed within 48 hours.
Chewable tablets:
Initial: 4 mg after the first loose stool, then
Maintenance: 2 mg after each subsequent loose stool, but not exceeding 8 mg in 24 hours.
Usual Adult Dose for Diarrhea -- Chronic:
Tablets, capsules, and liquid:
Initial: 4 mg orally once followed by 2 mg orally after each loose stool, not to exceed 16 mg in any 24-hour period.
Maintenance: The average daily maintenance dosage is 4 to 8 mg. Clinical improvement is usually observed within 10 days. If clinical improvement is not observed at a maximum dosage of 16 mg for duration of 10 days, symptoms are unlikely to be controlled by further administration.
Usual Pediatric Dose for Diarrhea -- Acute:
2 to 6 years (13 to 20 kg):
Liquid formulation only to be used in this age group.
Initial: 1 mg orally 3 times a day for the first day, then
Maintenance: 0.1 mg/kg/dose after each loose stool, but not exceeding initial dose.
6 to 8 years (20 to 30 kg):
Tablets, capsules, and liquid:
Initial: 2 mg orally twice a day for the first day, then
Maintenance: 0.1 mg/kg/dose after each loose stool, but not exceeding initial dose.
Chewable tablets:
Initial: 2 mg orally after the first loose stool, then
Maintenance: 1 mg orally after each subsequent loose stool, but not exceeding 4 mg in 24 hours.
8 to 12 years (greater than 30 kg):
Tablets, capsules, and liquid:
Initial: 2 mg orally 3 times a day for the first day, then
Maintenance: 0.1 mg/kg/dose after each loose stool, but not exceeding initial dose.
Chewable tablets:
Initial: 2 mg orally after the first loose stool, then
Maintenance: 1 mg orally after each subsequent loose stool, but not exceeding 6 mg in 24 hours.
12 to 18 years:
Tablets, chewable tablets, capsules, and liquid:
Initial: 4 mg after the first loose stool, then
Maintenance: 2 mg after each subsequent loose stool, but not exceeding 8 mg in 24 hours.
Usual Pediatric Dose for Diarrhea -- Chronic:
less than 2 years:
Therapeutic dose for the treatment of chronic diarrhea has not been established for this patient population.
IMPORTENT
You should not use this medication if you are allergic to loperamide, or if you have:
stools that are bloody, black, or tarry; or
if you have diarrhea that is caused by taking an antibiotic.
Ask a doctor or pharmacist if it is safe for you to take this medicine if you have:
a fever; mucus in your stools; a history of liver disease; or
if you are taking an antibiotic.
FDA pregnancy category C. It is not known whether loperamide will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.
Loperamide can pass into breast milk and may harm a nursing baby. You should not breast-feed while you are using loperamide.
Do not give this medicine to a child without medical advice.
IF YOU FORGET A DOSE -
If you are taking scheduled doses of loperamide, take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
SIDE EFFECTS
Loperamide may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away: dry mouth, dizziness, drowsiness, vomiting, stomach pain, discomfort, or distention (enlargement) , constipation, fatigue,
If you experience any of the following symptoms, call your doctor immediately: skin rash, hives, itching, wheezing, difficulty breathing
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online [at http://www.fda.gov/Safety/MedWatch] or by phone [1-800-332-1088].
AVAILABLE BRANDS - LOPAMIDE TAB , IMODIUM CAP , ANDIAL
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