Loperamide

When ATH:
A07DA03

Characteristic.

Loperamide hydrochloride-powder from white to yellowish. It is soluble in methanol, isopropyl alcohol, xloroforme, slightly soluble in water. Molecular weight 513,51.

Pharmacological action.
Antidiareynoe.

Application.

Symptomatic treatment of acute and chronic diarrhea, due to a change in diet and qualitative composition of food, violation of metabolism and absorption, and allergic, Emotional, drug, ray origin; When diarrhea contagious Genesis — as an adjuvant; ileostomy (to reduce the frequency and volume of stool, and density to impart its texture).

Contraindications.

Hypersensitivity, ileus, diverticulosis, severe ulcerative colitis, psevdomembranoznыy colitis, caused by taking broad-spectrum antibiotics; other conditions, in which unacceptable oppression intestinal peristalsis; ostraya dysentery (especially with the presence of blood in the stool, and accompanied by fever); childhood (to 2 years).

Restrictions apply.

Serious liver and children between the ages of 2 to 12 years (possible only with medical supervision).

Pregnancy and breast-feeding.

It should not be used during pregnancy (especially in the I trimester) and breastfeeding (adequate and well-controlled studies in pregnant and lactating women are not held).

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Side effects.

Adverse effects, noted during clinical trials of loperamide hydrochloride, difficult to distinguish from symptoms, syndrome associated with diarrhea; Typically, these effects were mild and self-limiting; in most cases they have been observed in the treatment of chronic diarrhea. These side effects include the following: hypersensitivity reactions, incl. each eruption, krapivnicu, extremely rare-anaphylaxis and bulleznuu rash, including toxic epidermal necrolysis (in most cases the patient is taking other drugs, which could cause an adverse reaction or to facilitate their emergence), abdominal pain, bloating or stomach discomfort, nausea, vomiting, constipation, fatiguability, drowsiness, dizziness, dry mouth.

In post-marketing studies were rare reports of paralytic ileus. Most of these messages was recorded in acute dysentery, overdose, in children under 2 years.

Cooperation.

Concomitant use of loperamide with opioid analgesics may increase the risk of severe constipation.

Overdose.

Symptoms: CNS depression (stupor, dystaxia, drowsiness, mioz, Muscle hypertonicity, respiratory depression), ileus.

Treatment: application (if necessary) antidote is naloxone. Considering, that the longer duration of action of loperamide, than naloxone, possible re-introduction of the antagonist. Takes a long and thorough monitoring of patients (at least 1 Nights) and symptomatic therapy, gastric lavage, appointment of activated carbon, IVL.

Dosing and Administration.

Inside. The dosage regimen depends on the indication. Adults, acute diarrhea: the initial dose 4 mg, then 2 mg after each unformed stool, The maximum daily dose - 16 mg; for chronic diarrhea for 4 mg / day. With the normalization of stool consistency, or lack of a chair 12 h treatment should be discontinued. Children 2-12 years, depending on the age and body mass index.

Precautions.

If during the 48 h in acute diarrhea is not observed clinical improvement or develops constipation, abdominal distention, Partial bowel obstruction, receiving loperamide should be discontinued.

In chronic diarrhea receiving loperamide available only on prescription.

You should be wary of loperamide in young children because of the greater sensitivity to opiatopodobnym effects of loperamide — action on the central nervous system. During treatment of diarrhea (especially in children) you need to replenish lost fluids and electrolytes. Dehydration can contribute to change in reaction to loperamide.

Be wary of elderly patients (possible masking of symptoms of dehydration and variability of reaction to loperamide).

Patients with hepatic dysfunction should be closely monitored for signs of CNS toxicity (It slows down the metabolism of loperamide).

In patients with travelers' diarrhea decrease in intestinal motility, caused loperamide, may cause long-term rise in temperature due to the slowdown elimination of microorganisms (Shigella, Salmonella, Some strains of Escherichia coli and etc.) and their penetration into the intestinal mucosa.

During the period of treatment must be careful when driving a car or operating machinery.