LOPERAMIDE of 2 mg No. 10

General characteristics. Structure:

Active ingredient: loperamide a hydrochloride – 2 mg;

excipients: lactoses monohydrate of-135,4 mg, starch of potato –15,8 mg, silicon dioxide colloid (aerosil) of-3,2 mg, calcium stearate - 1,6 mg;

structure of a gelatin capsule: case: gelatin of-17,311 mg, titanium dioxide  of E 171 - 0,353 mg; lid: gelatin – 29,422 mg, titanium dioxide of E 171 - 0,303 mg, dye ferrous oxide of yellow E 172 - 0,520 mg, indigo carmine of E 132 - 0,091 mg.

Description.

Solid gelatin capsules No. 3, case of white color, lid of green color. Contents of capsules – powder of color, white or white with a yellow shade.

Pharmacological properties:

Pharmacodynamics. Loperamide, contacting opioid receptors of an intestinal wall (stimulation of cholinergic and adrenergic neurons through a guanine nucleotides), reduces a tone and motility of smooth muscles of intestines, slows down an intestines contents passage, reduces release of liquid and electrolytes with excrements. Raises a tone of a proctal sphincter, promotes deduction of fecal masses and an urezheniye of desires to defecation. Action comes quickly and 4-6 hours proceed.

Pharmacokinetics. Absorption - 40%. Communication with proteins of plasma - 97%. An elimination half-life - 9-14 hours. Does not get through a blood-brain barrier. Having got to a system blood stream, it is almost completely metabolized in a liver by conjugation. An insignificant part kidneys is removed preferential with bile (in the form of the conjugated metabolites).

Indications to use:

Symptomatic treatment of acute and chronic diarrhea (genesis: allergic, emotional, medicinal, beam; at change of a diet and qualitative structure of food, at disturbance of metabolism and absorption; as supportive application at diarrhea of infectious genesis).

Regulation of a chair at patients from ileostomy.

Route of administration and doses:

Inside: without chewing, washing down with water. Adult at acute and chronic diarrhea originally appoint 2 capsules (4 mg), then on 1 capsule (2 mg) after each act of defecation in case of a liquid chair. The maximum daily dose - 8 capsules (16 mg).

To children 6 years at acute diarrhea are more senior appoint on 1 capsule (2 mg) after each act of defecation in case of a liquid chair. The maximum daily dose - 3 capsules (6 mg).

Duration of treatment is 7 - 20 days. After normalization of a chair or in the absence of a chair more than 12 hours treatment by loperamide should be stopped.

Features of use:

Loperamide should be applied with extra care at patients with liver dysfunction since it is metabolized in a liver. At patients with dysfunction of a liver careful control of signs of toxic defeat of TsNS under the influence of drug is necessary. Such antidiarrheal means as Loperamide, can cause impassability of intestines and toxic megacolon. Treatment has to be interrupted at once if abdominal distention or other indirect symptoms appears. In the absence of effect after 2 days of use of Loperamide it is necessary to specify the diagnosis and to exclude infectious genesis of diarrhea. To children 6 years are younger it is not recommended to appoint Loperamide in capsules or tablets.

During treatment it is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Discomfort in a stomach, a meteorism, a gastralgia, dryness in a mouth, allergic reactions (skin rash), intestinal colic, nausea, vomiting, a lock, a headache, drowsiness or sleeplessness, dizziness, an ischuria, intestinal impassability.

Interaction with other medicines:

Simultaneous use of loperamide with opioid analgetics or Colestyraminum can increase risk of a heavy lock.

At simultaneous use with co-trimoxazole, ritonaviry bioavailability of loperamide increases that is caused by inhibition of his metabolism at "the first passing" through a liver.

Contraindications:

Hypersensitivity to drug, a lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption, a divertuculosis, intestinal impassability, ulcer colitis in an aggravation stage, diarrhea against the background of an acute pseudomembranous coloenteritis, in the form of monotherapy - dysentery and other infections of digestive tract; pregnancy (the I trimester), the lactation period, loperamide in capsules are not appointed to children up to 6 years.

Overdose:

Symptoms: oppression of the central nervous system (stupor, lack of coordination, drowsiness, miosis, muscular hypertension, respiratory depression), intestinal impassability.

Treatment: an antidote - Naloxonum; considering that duration of effect of loperamide is more, than at Naloxonum, perhaps repeated introduction of the last. Symptomatic treatment: absorbent carbon, gastric lavage, artificial ventilation of the lungs.

Medical observation, at least, within 48 hours is necessary.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

Capsules on 2 mg. On 10 capsules in a blister strip packaging. On 1 or 2 blister strip packagings together with the application instruction in a pack from a cardboard.