Loperamide + Simethicone (Loperamidum + Simethiconum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antidiarrhoeic agents

Included in the formulation
  • Imodium Plus
    pills inwards 
    Johnson & Johnson, LLC     Russia
    • АТХ:

    A.07.D.A.53   Loperamide in combination with other drugs

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

    Pharmacodynamics:

    Loperamide binds to opioid receptors in the intestinal wall, which leads to inhibition of propulsive peristalsis, increased resorption of water and electrolytes. Loperamide does not change the physiological microflora of the intestine and increases the tone of the anal sphincter.

    Simethicone is an inert surface-active compound. Has a defoaming effect, and therefore facilitates the symptoms associated with diarrhea (flatulence, abdominal discomfort, spastic pain).

    Does not have a central action.

    Pharmacokinetics:

    Loperamide: 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). The half-life is 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).

    Simethicone: Not absorbed. Elimination in unchanged form with feces.

    Indications:

    - Diarrhea of ​​any etiology and associated symptoms (flatulence, abdominal discomfort, spastic pain).

    ICD-10

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

    XI.K55-K63.K59.1   Functional diarrhea

    Contraindications:

    Hypersensitivity to loperamide, simethicone.

    Ulcerative colitis (possibly development of toxic megacolon), diverticular disease.

    Diarrhea due to Clostridium difficile, developed against the background of the use of broad-spectrum antibiotics.

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

    Pregnancy (I trimester), breast-feeding, children's age (less than 12 years).

    Carefully:

    Dehydration, infectious diarrhea, impaired liver function.

    Pregnancy and lactation:

    Controlled studies in humans have not been conducted. In rats and rabbits in doses exceeding the recommended for humans up to 30 times, is not teratogenic and does not negatively affect the offspring. In higher doses, the survival of the mother and newborns is reduced. There is no information on the penetration of breast milk, but in lactating rats at a dose of 40 mg / kg reduces the survival of offspring.

    The category of FDA recommendations is not defined.

    Dosing and Administration:

    The drug is prescribed for adults and children over 12 years in the initial dose of 2 tablets, then - 1 tablet after each liquid stool. The maximum daily dose is 4 tablets. Duration of reception - no more than 2 days.

    When using the drug in elderly patients, dose adjustment is not required.

    When using the drug in patients with impaired renal function, a dose reduction is not required.

    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.

    Strengthens the effect of other antidiarrhoeic agents with a similar mechanism of action.

    Special instructions:

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

    Inhibition of peristalsis of the intestine 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.

    With ulcerative colitis, treatment with loperamide should be discontinued if 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.

    Distinctive features:

    Patients in old age should be administered with caution, since loperamide can mask dehydration and electrolyte disturbances. In addition, dehydration can influence the subsequent response to loperamide.

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