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Loperamide - Acre - antidiarrheal drug. Reduces the tone and motility of the smooth muscles of the intestine, apparently due to binding to opioid receptors in the intestinal wall. Inhibits the release of acetylcholine and prostaglandins, reducing peristalsis and increasing the time it takes for the contents to pass through the intestines.
Increases the tone of the anal sphincter. The action comes quickly and lasts 4-6 hours.
After ingestion, absorption of loperamide is about 40%, and is extensively metabolized during the "first pass" through the liver. A small amount of unchanged loperamide enters the systemic circulation. Does not penetrate the BBB.
Metabolized in the liver.
T1 / 2 is 9-14 hours. It is excreted through bile with feces in the form of conjugated metabolites, an insignificant part is excreted with urine.
Symptomatic treatment of acute and chronic diarrhea of various origins (including allergic, emotional, medicinal, radiation; when changing the diet and the qualitative composition of food, in violation of metabolism and absorption; as an adjunct in infectious genesis diarrhea). Regulation of stools in patients with ileostomy.
1 capsule contains:
Active substance: loperamide hydrochloride 2 mg;
Excipients: corn starch; milk sugar; talc; aerosil; magnesium stearate.
Loperamide is marketed under different brands and generic names, and comes in different dosage forms:
|Brand name||Manufacturer||Country||Dosage form|
|Imodium||Catalent UK Swindon Zaydis Limited/Janssen-Cilag||UK||pills|
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Dosage and Administration
For oral use.
Acute diarrhea. Adults: the initial dose is 4 mg, then 2 mg after each bowel movement with liquid stools.Children over 5 years: The initial dose is 2 mg, then 2 mg after each bowel movement with liquid stool.
Chronic diarrhea. Adults: the initial dose is 4 mg, then 2 mg 1–6 times a day.Children over 5 years: 2 mg 1–5 times a day.
Allergic reactions (skin rash), drowsiness or insomnia, dizziness, hypovolemia, electrolyte disturbances; dry oral mucosa, intestinal colic, gastralgia, abdominal pain or discomfort, nausea, vomiting, flatulence.
Seldom - urinary retention, extremely rarely - intestinal obstruction.
- Hypersensitivity, intestinal obstruction, diverticulosis, acute ulcerative colitis, pseudomembranous colitis caused by taking broad-spectrum antibiotics;
- other conditions in which the inhibition of intestinal peristalsis is unacceptable;
- acute dysentery (especially with the presence of blood in the stool and accompanied by increased body temperature);
- children's age (up to 2 years).
Opioid analgesics increase the risk of developing severe constipation.
Pregnancy and Lactation
Loperamide-Acre is contraindicated in the first trimester of pregnancy. At the time of treatment should stop breastfeeding.
In the absence of effect after 2 days of loperamide use, you should consult a doctor.
If constipation or bloating develop during treatment, loperamide should be withdrawn. In patients with impaired liver function, careful monitoring of toxic signs of CNS damage is necessary.
During the treatment of diarrhea, it is necessary to compensate for the loss of fluid and electrolytes.
During the period of treatment, care must be taken when driving and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions.
Symptoms: depression of the central nervous system (stupor, incoordination, drowsiness, miosis, muscle hypertension, respiratory depression), intestinal obstruction.
Treatment: antidote - naloxone; Considering that the duration of loperamide is longer than that of naloxone, it is possible to reintroduce the latter.
Symptomatic treatment:Activated charcoal, gastric lavage, artificial lung ventilation.
Medical supervision is required for at least 48 hours.
- Brand name: Loperamide Akrikhin
- Active ingredient: Loperamide
- Dosage form: Capsules
- Manufacturer: Akrikhin
- Country of Origin: Russia
- Misuse of loperamide in anxiety disorder patients
- Metabolites of loperamide in rats
- Further studies on the interaction of loperamide with capacitative calcium entry in Leukemic HL-60 cells
- Pharmacology and antidiarrheal effect of loperamide
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- Inhibition of pancreaticobiliary secretion by loperamide in humans
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- The effect of loperamide on the thermal behavior of dimyristoylphosphatidylcholine large unilamellar vesicles
- Effect of finite doses of propylene glycol on enhancement of in vitro percutaneous permeation of loperamide hydrochloride
- Spectrofluorimetric and derivative absorption spectrophotometric techniques for the determination of loperamide hydrochloride in pharmaceutical formulations
- Characterization of P-glycoprotein inhibition at the blood brain barrier by ketoconazole and quinidine using the central pharmacodynamics of loperamide as an indicator of brain distribution
- Liquid chromatography–tandem mass spectrometry determination of loperamide and its main metabolite desmethylloperamide in biological specimens and application to forensic cases
- Validation of a liquid chromatographic-tandem mass spectrometric method for the determination of loperamide in human plasma
- LC–MS determination and bioavailability study of loperamide hydrochloride after oral administration of loperamide capsule in human volunteers
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- Loperamide causes respiratory depression when P-gp is inhibited
- Symptomatic treatment of acute infectious diarrhoea: Loperamide versus placebo in a double-blind trial
- Characterization of the antidiarrhoeal loperamide by gas chromatography-mass spectrometry and application of the Hofmann degradation and Cope elimination reaction
- Spectrophotometric determination of loperamide hydrochloride by acid-dye and charge-transfer complexation methods in the presence of its degradation products
- Determination of loperamide in rat plasma and bovine serum albumin by LC
- Effect of Loperamide on Mucosal Guanylyl Cyclase Activity in Rat Jejunum Following Escherichia coli Heat-Stable Toxin-Induced Fluid Accumulation