Loperamide hydrochloride
Loperamide hydrochloride: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Loperamide
ATX code: A07DA03
Active ingredient: loperamide (Loperamide)
Manufacturer: JSC "Borisov Plant of Medical Products" (JSC "BZMP") (Republic of Belarus)
Description and photo update: 2019-09-07
Loperamide hydrochloride is an antidiarrheal agent.
Release form and composition
Dosage form - capsules: cylindrical with hemispherical ends, solid, gelatinous, white or white with a yellowish tinge; content - granules of white or white with a yellowish tinge color (in a cardboard box 1–2 cell contour packaging of 10 capsules and instructions for use of Loperamide hydrochloride).
Composition of 1 capsule:
- active substance: loperamide hydrochloride - 2 mg;
- auxiliary components: magnesium stearate, corn starch, lactose monohydrate;
- composition of the capsule shell: gelatin, sodium lauryl sulfate, glycerin, propyl parahydroxybenzoate E 216, methyl parahydroxybenzoate E 218, titanium dioxide E 171, purified water.
Pharmacological properties
Pharmacodynamics
Loperamide is a peripheral opioid receptor agonist. Its antagonist is naloxone.
The mechanism of action of loperamide hydrochloride is due to the ability to suppress the release of acetylcholine and prostaglandins, reduce propulsive peristalsis, reduce the time it takes for contents to pass through the intestine, and enhance the ability of the intestinal wall to absorb fluid.
By increasing the tone of the anal sphincter, the drug reduces the urge to defecate and fecal incontinence.
Loperamide is highly specific for the intestinal wall. Systemic circulation reaches a limited amount. Practically does not penetrate the blood-brain barrier.
The maximum dose of loperamide hydrochloride exhibiting an antidiarrheal effect is well below the central action threshold.
Pharmacokinetics
Once in the intestine, most of the loperamide hydrochloride is absorbed. The drug undergoes intensive metabolism during the first passage through the liver, therefore, the systemic bioavailability is about 0.3%, and the plasma concentration is very low.
In studies on rats, it was found that loperamide has a high affinity for the intestinal wall and binds mainly to the receptors of the longitudinal muscle layer. According to preclinical data, loperamide is a substrate for P-glycoprotein.
Plasma proteins (mainly albumin) bind about 95% of the dose. Loperamide does not penetrate through the BBB (blood-brain barrier).
Loperamide hydrochloride is almost completely metabolized in the liver by conjugation, then excreted in the bile. The main metabolic pathway is oxidative N-demethylation with the participation of mainly CYPZA4 and CYP2C8 isoenzymes.
Loperamide and its metabolites are excreted mainly in the feces. The half-life is 9-14 hours.
The pharmacokinetic parameters of loperamide in children have not been studied. It is expected that the characteristics of loperamide, including when interacting with other drugs, will be similar to those in adults.
Indications for use
Loperamide hydrochloride is indicated for the symptomatic treatment of diarrhea (acute, chronic of various etiologies and travelers' diarrhea).
Contraindications
- diarrhea with blood in the stool and high fever;
- acute ulcerative colitis;
- intestinal obstruction;
- conditions in which suppression of peristalsis is contraindicated;
- diverticulosis;
- pseudomembranous enterocolitis (diarrhea caused by taking antibiotics);
- acute dysentery and other infections of the gastrointestinal tract (including those caused by Campylobacter spp., Salmonella spp. and Shigella spp.);
- rare congenital galactose intolerance, lactase deficiency, glucose / galactose malabsorption syndrome;
- children under 6 years old;
- I trimester of pregnancy;
- lactation period;
- hypersensitivity to any component of the drug.
With caution, Loperamide hydrochloride in capsules should be used in liver failure, in the II and III trimesters of pregnancy.
Loperamide hydrochloride, instructions for use: method and dosage
Loperamide hydrochloride capsules are taken orally, swallowed whole and washed down with water.
Recommended doses for adults:
- acute diarrhea: first dose - 2 capsules, then - 1 capsule after each bowel movement in case of loose stools;
- chronic diarrhea: the initial dose is 2 capsules, then the dose is selected so that the stool frequency is 1–2 times a day, this requires taking Loperamide hydrochloride 1–6 capsules a day.
The maximum daily dose for adults with acute and chronic diarrhea is 8 capsules.
Recommended doses of Loperamide hydrochloride for children 6-17 years old:
- acute diarrhea: initial dose - 1 capsule, then - 1 capsule after each bowel movement in case of loose stools;
- chronic diarrhea: 1 capsule 1 time per day.
The maximum dose for children with acute and chronic diarrhea is calculated by body weight: 6 mg (3 capsules) per 20 kg of body weight, but it should not exceed 16 mg (8 capsules) per day.
The therapy ends after the appearance of normal stool or in the absence of stool for more than 12 hours.
If with acute diarrhea after 48 hours the condition does not improve, Loperamide hydrochloride should be discontinued and a doctor should be consulted.
Fluid and electrolyte replenishment is an important prerequisite for treatment, especially in children.
Side effects
Adverse reactions according to the frequency of development are classified as follows: very often -> 10%, often - from> 1% to 0.1% to 0.01% to <0.1%, very rarely - <0.01%, including single cases.
Side effects for both acute and chronic diarrhea:
- from the immune system: rarely - hypersensitivity reactions, anaphylactic reactions (including anaphylactic shock);
- from the nervous system: often - headache, dizziness; infrequently - drowsiness; rarely - loss of consciousness, stupor, depression of consciousness, impaired coordination, increased muscle tone;
- on the part of the organ of vision: rarely - miosis;
- from the gastrointestinal tract: often - flatulence, nausea, constipation; infrequently - dry mouth, discomfort and abdominal pain, vomiting, dyspepsia; rarely - bloating, glossalgia, intestinal obstruction (including paralytic ileus), megacolon (including toxic);
- from the kidneys and urinary system: rarely - urinary retention;
- from the skin and subcutaneous tissues: infrequently - rash; rarely - itching, urticaria, angioedema, bullous rash (including erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome);
- others: rarely - fatigue.
Overdose
An overdose of loperamide causes urinary retention, intestinal obstruction and depression of the central nervous system (CNS), which is manifested by drowsiness, impaired coordination of movements, stupor, muscle hypertension, miosis, and respiratory depression.
First aid measures (no later than 3 hours after taking an excessive dose of Loperamide hydrochloride): gastric lavage, taking activated charcoal. Further treatment is symptomatic. With respiratory depression, artificial ventilation is performed. The antidote to loperamide is naloxone, which has a shorter duration of action than loperamide and may require re-administration. For at least 48 hours, the patient should be under medical supervision to identify possible depression of the central nervous system.
special instructions
If constipation, abdominal distention or intestinal obstruction appears while taking loperamide, the drug should be discontinued immediately.
If after 48 hours in patients with acute diarrhea there is no improvement in their condition, it is necessary to stop taking Loperamide hydrochloride and consult a doctor. An additional examination is required to exclude the infectious genesis of diarrhea.
Treatment with the drug is symptomatic, therefore, it is simultaneously recommended to use etiotropic agents to eliminate the cause of the disorder.
Diarrhea, especially in children, can cause hypovolemia and decreased electrolyte levels. As a consequence, fluid and electrolyte replenishment is an important treatment. Diet is recommended.
Patients with acquired immunodeficiency syndrome (AIDS) should stop treatment immediately at the first sign of bloating. In infectious and bacterial colitis in such patients, in some cases, toxic expansion of the colon may develop.
Influence on the ability to drive vehicles and complex mechanisms
Loperamide hydrochloride can cause side effects from the central nervous system (including drowsiness and dizziness), so it is recommended to refrain from potentially hazardous activities during the period of treatment.
Application during pregnancy and lactation
In the first trimester of pregnancy, Loperamide hydrochloride is contraindicated. Despite the lack of data on teratogenic and embryotoxic effects, in the II and III trimesters, the drug can be used only in cases where the expected benefit is higher than the possible risks.
Loperamide passes into breast milk. If treatment is required during lactation, breastfeeding should be interrupted.
Pediatric use
Loperamide hydrochloride is contraindicated in children under 6 years of age due to the high content of the active substance and the characteristics of the dosage form.
With impaired renal function
No dose adjustment of Loperamide hydrochloride is required.
For violations of liver function
Loperamide hydrochloride should be used with caution in liver failure, since such patients may have a decrease in the presystemic metabolism of loperamide, which is why there is a risk of relative overdose and, as a result, the development of toxic effects from the central nervous system.
Use in the elderly
No dose adjustment is required.
Drug interactions
It is expected that with the simultaneous use of drugs with similar pharmacological properties, it is possible to increase the effect of loperamide hydrochloride, and drugs that enhance the motility of the gastrointestinal tract - a decrease in its effect.
Co-administration of quinidine or ritonavir, which are inhibitors of P-glycoprotein, increases the plasma concentration of loperamide, used in a single dose of 16 mg, by 2–3 times. When the drug is taken in recommended doses, the clinical significance of this interaction is unknown.
With the simultaneous use of loperamide hydrochloride in a single dose of 16 mg and ketoconazole, which is an inhibitor of the enzyme CYP3A4 and P-glycoprotein, there was a 5-fold increase in the plasma concentration of loperamide, but this was not accompanied by an increase in its pharmacodynamic effects.
With the simultaneous use of loperamide in a single dose of 4 mg and itraconazole, which is an inhibitor of the CYP3A4 enzyme and P-glycoprotein, there was a 3-4-fold increase in the plasma concentration of loperamide. In the same study, gemfibrozil (an inhibitor of CYP2C8) increased plasma levels of loperamide by about 2 times. With the simultaneous use of itraconazole and gemfibrozil, the maximum plasma concentrations of loperamide increased 4 times, and the total plasma exposure increased 13 times. However, the results of psychomotor tests (test of substitution of digital symbols and test of subjective feeling of sleepiness) did not show an increase in the effect of the combination of these substances on the central nervous system.
Loperamide hydrochloride, when used together, increases the plasma content of desmopressin by 3 times (probably due to inhibition of gastrointestinal motility).
Loperamide should not be used in children in combination with drugs that can depress the central nervous system.
Analogs
Loperamide hydrochloride analogues are Vero-loperamide, Diara, Imodium, Lopedium, Loperamide, Superilop, etc.
Terms and conditions of storage
Store in a place protected from light and moisture, out of reach of children, at a temperature of 15-25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews of Loperamide hydrochloride
According to reviews, Loperamide hydrochloride is an effective, inexpensive and well-tolerated agent. Diarrhea is a problem that every person faces at one time or another, so this drug, according to most, should always be present in the home medicine cabinet.
Loperamide hydrochloride price in pharmacies
At the moment, the price of Loperamide hydrochloride in capsules is unknown due to the lack of the drug on the market.
The approximate cost of popular analogues:
- Vero-loperamide - 19-22 rubles. for a pack of 20 tablets of 2 mg;
- Imodium - 269–395 rubles. per pack of 10 lozenges, 2 mg;
- Lopedium - 26–31 rubles. per pack of 10 capsules of 2 mg.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
