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Active ingredients
Loperamide
Release form
Pills
Composition
1 caps Loperamide hydrochloride 2 mg. Excipients: lactose monohydrate, corn starch, talc, magnesium stearate. The composition of the capsule shell: titanium dioxide, ferric oxide yellow, sodium indigotindisulfonate, gelatin, ferric oxide black, sodium erythrosin.
Pharmacological effect
Antidiarrheal drug. It reduces the tone and motility of the smooth muscles of the intestine, apparently due to binding to opioid receptors in the intestinal wall. Inhibits the release of acetylcholine and prostaglandins, reducing peristalsis and increasing the time it takes for the contents to pass through the intestines. Increases the tone of the anal sphincter. The action comes quickly and lasts 4-6 hours.
Pharmacokinetics
After ingestion, absorption of loperamide is about 40%, and is extensively metabolized during the "first pass" through the liver. A small amount of unchanged loperamide enters the systemic circulation. Does not penetrate the BBB. Metabolized in the liver. T1 / 2 is 9-14 hours. It is excreted through bile with feces in the form of conjugated metabolites, a small part is excreted in the urine.
Contraindications
Intestinal obstruction constipation, bloating, subileus, acute dysentery (as monotherapy), acute ulcerative colitis, pseudomembranous colitis resulting from the use of broad-spectrum antibiotics, children up to 4 years old, I trimester of pregnancy, increased sensitivity to loperamide.
Use during 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 outweighs the potential risk to the fetus. Since a small amount of loperamide is found in breast milk, taking during breastfeeding is not recommended.
Dosage and administration
For adults with acute diarrhea, the first dose is 4 mg, then 2 mg after each defecation in the case of liquid stool. In chronic diarrhea, the first dose is 2 mg, the supporting dose is selected so that the stool frequency is 1-2 times per day (2-12 mg / day). The maximum daily dose for adults is 16 mg.Children aged 4-8 years - 1 mg 3-4 times / day for 3 days 9-12 years - 2 mg 4 times / day for 5 days.
Side effects
On the part of the digestive system: abdominal pain, bloating, nausea, constipation, dry mouth. From the side of the central nervous system: increased fatigue, drowsiness, dizziness. Allergic reactions: skin rash.
special instructions
Be wary when using liver failure. It should not be used in clinical situations where the suppression of intestinal motility is required. In the absence of effect after 2 days of loperamide, it is necessary to clarify the diagnosis and exclude infectious genesis of diarrhea. With caution used in patients with impaired liver function. When loperamide overdose naloxone is used as an antidote.