Clinical and pharmacological group: & nbsp

Antidiarrhoeic agents

Included in the formulation
  • Vero-Loperamide
    pills inwards 
    VEROPHARM SA     Russia
  • Dyara
    pills inwards 
  • Diara®
    capsules inwards 
  • Imodium®
    pills inwards 
  • Imodium®
    capsules inwards 
  • Lopedium®
    capsules inwards 
    Sandoz d.     Slovenia
  • Lopedium®
    pills inwards 
    Sandoz d.     Slovenia
  • Loperamide
    capsules inwards 
    BIOKOM, CJSC     Russia
  • Loperamide
    pills inwards 
    PHARMACY 36.6, CJSC     Russia
  • Loperamide
    capsules inwards 
  • Loperamide
    pills inwards 
  • Loperamide
    pills inwards 
    BIOKOM, CJSC     Russia
  • Loperamide
    capsules inwards 
    NORTH STAR, CJSC     Russia
  • Loperamide
    pills inwards 
    OZONE, LLC     Russia
  • Loperamide
    pills inwards 
    LEKHIM-KHARKOV, CJSC     Ukraine
  • Loperamide Grindeks
    capsules inwards 
    GRINDEX, JSC     Latvia
  • Loperamide STADA
    capsules inwards 
    NIZHFARM, JSC     Russia
  • Loperamide-Akrihin
    capsules inwards 
    AKRIKHIN HFK, JSC     Russia
  • Sperilop
    capsules inwards 
  • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    Minimal chemist's assortment

    АТХ:

    A.07.D.A   Drugs that reduce the peristalsis of the digestive tract

    A.07.D.A.03   Loperamide

    Pharmacodynamics:

    Affects opioid receptors in the small intestine (stimulates choline and adrenergic neurons through guanine nucleotides), reduces the activity of circular and longitudinal muscle fibers (inhibits the release of acetylcholine and prostaglandins), slows the passage of contents through the intestine, lengthens the time of contact of the contents with the wall and, directly inhibits the secretion of fluid and electrolytes and / or the simultaneous absorption of salts and water. Increases the tone of the anal sphincter, promotes retention of fecal masses and reduced urge to defecate.

    Pharmacokinetics:

    Absorbed from the gastrointestinal tract by 40%. Communication with plasma proteins is 97% (mainly with albumins). Does not penetrate the blood-brain barrier. Exposed to intensive metabolism in the process of oxidative N-demethylation at the first passage through the liver. Biotransformation in the liver (by conjugation). Half-life - 9.1-14.4 hours (an average of 10.8 hours). TCmax - 5 hours (when taking capsules), 2.5 hours (when taking a solution). Elimination with feces (mainly) and kidneys (insignificant part, in the form of conjugated metabolites).

    Indications:Symptomatic treatment of acute and chronic diarrhea of ​​various genesis (including allergic, emotional, drug, radiation, with a change in diet and quality of food, in violation of metabolism and absorption, as an aid for diarrhea of ​​infectious genesis). Regulation of stool in patients with ileostomy.

    XI.K50-K52.K52   Other non-infectious gastroenteritis and colitis

    XI.K55-K63.K59.1   Functional diarrhea

    XI.K90-K93.K91.4   Dysfunction after colostomy and enterostomy

    Contraindications:

    Hypersensitivity (possible development of toxic megacolon).

    Diarrhea due to Clostridium difficile, developed against the background of the use of broad-spectrum antibiotics (possibly lengthening and / or weighting diarrhea).

    Acute shigellosis with an increase in body temperature and an admixture of blood in the feces.

    Intestinal obstruction, ulcerative colitis (the possibility of developing a toxic megacolon), diverticular disease.

    Pregnancy (I trimester), breast-feeding.

    Carefully:

    Dehydration, infectious diarrhea, impaired liver function.

    Pregnancy and lactation:

    Contraindicated in the first trimester of pregnancy, in the II and III trimesters of pregnancy loperamide can be prescribed in cases where the expected benefit of therapy for the mother exceeds the potential risk to the fetus.

    A small amount penetrates into breast milk, reception during lactation is not recommended.

    The FDA recommendation category is B.

    Dosing and Administration:

    Adults with acute diarrhea first dose - 4 mg, then - 2 mg after each act of defecation in the case of a loose stool. In chronic diarrhea, the first dose is 2 mg, the maintenance dose is selected so that the stool frequency is 1-2 times a day (2-12 mg per day).

    The maximum daily intake for adults is 16 mg.

    Children aged 4-8 years - 1 mg 3-4 times a day for 3 days; 9-12 years - 2 mg 4 times a day for 5 days.

    Side effects:

    In some cases, it is difficult to differentiate the side effects of loperamide and the manifestation of diarrheal syndrome; usually stopping spontaneously.

    From the digestive tract: toxic megacolon, dry mouth, intestinal colic, gastralgia, intestinal obstruction, burning sensation or tingling of the tongue (when taking tablets for resorption).

    From the urinary system: retention of urine.

    From the nervous system: dizziness, confusion.

    Hypersensitivity: allergic reactions (skin rashes).

    On the part of the reproductive system: in rats and rabbits in doses exceeding the recommended for humans up to 30 times, does not affect fertility.

    Carcinogenicity: in rats at doses exceeding the maximum recommended for humans up to 133 times, does not show carcinogenicity.

    Other: hypovolemia, electrolyte disturbances.

    Overdose:

    Clinical picture: the person is not described; in animals leads to CNS depression (stupor, impaired coordination of movements, drowsiness, miosis, muscle hypertension, respiratory depression), constipation and irritation of the gastrointestinal tract.

    Treatment (similar to an overdose of opiates): in order to reduce absorption - Activated carbon (as soon as possible after an overdose inside); when vomiting - a suspension of 100 g of activated carbon immediately when it is possible to hold the liquid in the stomach; in the absence of vomiting - gastric lavage. Specific therapy: if necessary - the introduction of antagonists of narcotic drugs (for example, naloxone). Since the duration of action of loperamide is greater than that of naloxone, it is possible to re-administer the latter.Supportive therapy: respiratory support. Monitoring: long and thorough.

    Interaction:

    Opioid (narcotic) analgesics - may increase the risk of severe constipation when combined with loperamide.

    Special instructions:

    The effectiveness of any antidiarrheal agents in the treatment of nonspecific diarrhea is questionable. Preferably therapy, including correction of water-electrolyte balance, nutritional support and, if possible, elimination of the cause of diarrhea.

    Loperamide is not recommended in children younger than 6 years, except for a special doctor. It is also not recommended as a routine therapy for diarrhea of ​​the first line in infections or food allergies in older children who do not have concomitant pathology.

    Can not use loperamide with diarrhea accompanied by fever or an admixture of blood or mucus in the feces.

    Maximum doses: in the form of capsules - 16 mg per day (8 mg per day for self-administration without doctor's appointment); in the form of a solution for oral administration or tablets - 8 mg per day (30 drops of 0.002% solution) for 2 days.

    The maximum duration of therapy in children: 4-8 years - 3 days; 8-12 years - 5 days; over 12 years old - similar to that for adults.

    Inhibition of intestinal peristalsis can lead to fluid retention, enhancing and masking dehydration, and electrolyte disturbances, especially in young children. With the development of dehydration or electrolyte disorders, discontinuation of loperamide therapy and the initiation of adequate corrective therapy are necessary.

    In acute ulcerative colitis, treatment with loperamide should be discontinued when there is an increase in the abdomen or other signs of a toxic megacolon.

    Addiction or physical dependence on loperamide in humans is not described, but morphine-like dependence is described in monkeys when taking high doses of loperamide.

    In acute diarrhea, treatment with loperamide should be discontinued if there is no improvement within 48 hours. In chronic diarrhea, if there is no response to the maximum dose within 10 days, a further answer is unlikely.

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