Pharmacological action – Loperamide Hydrochloride
Loperamide Hydrochloride Interacts with opiate receptors of the longitudinal and circular muscles of the intestinal wall and inhibits the release of acetylcholine and NG. Slows peristalsis and increase transit time of intestinal contents. Increases the tone of the anal sphincter, trapping stool and slowing of the urge to defecate. Due to the high affinity to the intestinal wall and a high degree of biotransformation in the “first pass” through the liver, almost falls into the systemic circulation. About 40% of the dose, absorbing into the gastrointestinal tract, metabolized in the liver. Time to reach C_max – about 8.5 hours after ingestion of the solution, and 5 h – capsules, 97% bound to plasma proteins. T_1 / 2 of 9-14 h (mean 11 h), displayed mainly in the form of conjugates in bile and feces.
Statement Loperamide Hydrochloride
Acute and chronic diarrhea (symptomatic treatment), ileostomy (to reduce the frequency and volume of stool, as well as to give the hardness of its consistency).
Contraindications Loperamide Hydrochloride
Hypersensitivity, dysentery (especially with the presence of blood in the stool and accompanied by fever), ulcerative colitis in acute, severe pseudomembranous colitis, pregnancy, breast-feeding (for the reception of loperamide to stop breast-feeding), child age (6 years).
Side effect Loperamide Hydrochloride
Drowsiness, dizziness, weakness, fatigue, dry mouth, nausea, vomiting, abdominal pain, constipation or abdominal distention (rare).
Overdose Loperamide Hydrochloride
Symptoms: CNS depression (stupor, loss of coordination, drowsiness, miosis, muscular hypertonia, respiratory depression), intestinal neprohodimost. Lechenie: as an antidote to use naloxone. Given that the duration of loperamide more than naloxone, possibly re-introduction of the antagonist. Immediately after the overdose administered activated charcoal and washed stomach, if necessary, support the function of respiration.
Precautionary measures Loperamide Hydrochloride
During the treatment of diarrhea (especially children) need to replenish lost fluids and electrolytes. If within 48 hours in acute diarrhea is observed clinical improvement or developing constipation, bloating, partial intestinal obstruction, taking loperamide should be discontinued. In patients with liver dysfunction requires careful monitoring for signs of toxic damage of the CNS. In case of weakness, fatigue, drowsiness or dizziness is not recommended to drive a car or work with machinery.
Dosing and Administration Loperamide Hydrochloride
Inside. In acute diarrhea: adults – 4 mg, then 2 mg, and children (age 6) – 2 mg, then 2 mg after each loose stool. For chronic diarrhea: adults – 4 mg, then a dose of providing stool frequency 1-2 times per day (2-12 mg / day) and the maximum daily dose – 16 mg, children – 2 mg, then pick up the same dose, but without exceeding the maximum daily (6 mg per 20 kg body weight).
