Loperamide hydrochloride

General characteristics. Structure:

Active ingredient: 2 mg of loperamide of a hydrochloride in each capsule.

Excipients: lactose monohydrate, corn starch, magnesium stearate; a firm gelatin capsule (contains: gelatin, glycerin, methylparahydroxybenzoate, пропилпарагидроксибензоат, sodium lauryl sulfate, titanium E 171 dioxide, the water purified).

Pharmacological properties:

Pharmacodynamics. Loperamide, contacting opioid receptors of an intestinal wall (stimulation sincaline - and adrenergic neurons through a guanine nucleotides), reduces a tone and motility of smooth muscles of intestines (at the expense of inhibition of release of acetylcholine and Pg). Slows down a peristaltics and increases time of passing of intestinal contents. Raises a tone of a proctal sphincter, promotes deduction of fecal masses and an urezheniye of desires to defecation. Action develops quickly and continues 4-6 h.

Unlike opiates, loperamide does not possess the central action as does not get through a blood-brain barrier; does not cause addiction and accustoming, is more selective on action therefore causes smaller number of by-effects.

Pharmacokinetics. Absorption – 40%. TCmax is 2,5 h - after reception of capsules. Communication with proteins of plasma (it is preferential with albumine) – 97%. Does not get through a blood-brain barrier. Is exposed to intensive metabolism in the course of oxidizing N-demethylation at the "first" passing through a liver.

It is almost completely metabolized by a liver by conjugation. T1/2 makes 9-14 h (on average 10,8 h). It is removed preferential with bile, an insignificant part is removed by kidneys (in the form of the conjugated metabolites).

Indications to use:

For a symptomatic treatment of acute diarrhea of any etiology, including cases of an exacerbation of chronic diarrhea, during the period up to 5 days at adults and children 8 years are more senior.

For a symptomatic treatment of chronic diarrhea at adults.

Route of administration and doses:

Inside, without chewing, washing down with water. At acute diarrhea to adults and patients of advanced age appoint 4 mg (2 capsules) in an initial dose; further - on 2 mg (1 capsule) after each act of defecation in case of a liquid chair. To children 8 years are more senior appoint in an initial dose 2 mg, further – on 2 mg after each act of defecation in case of a liquid chair.

At chronic diarrhea to adults and patients of advanced age appoint 4 mg/days (2 capsules) in an initial dose. Further the dose is adjusted so that the frequency of a chair made 1 - 2 times/days that is usually reached at a maintenance dose of 2 - 12 mg/days (1 - 6 capsules).

The maximum daily dose at acute and chronic diarrhea adults – 16 mg (8 capsules), at children have 6 mg on 20 kg of body weight - to 16 mg.

At emergence of a normal chair or in the absence of a chair more than 12 h medicine is cancelled.

Features of use:

Reception of medicine needs to be stopped immediately if the lock or abdominal distention develops.

As treatment of diarrhea loperamide has only symptomatic character, along with it it is necessary to apply etiotropic means, whenever possible.

At diarrhea, especially children, can have a hypovolemia and decrease in content of electrolytes. In such cases of the most important replacement therapy for completion of liquid and electrolytes is.

At acute diarrhea if during 48 h clinical improvement is not observed, reception of loperamide it is necessary to stop and exclude infectious genesis of diarrhea.

Not to apply at diarrhea with blood impurity in a chair and high temperature.

At patients AIDS it is necessary to stop immediately treatment at the first signs of abdominal distention. In some cases patients have AIDS with infectious colitis of both the virus, and bacterial nature at treatment by loperamide the toxic megacolon can develop.

At treatment of patients with renal failures there is no need to reduce a loperamide dose.

During treatment observance of a diet and completion of liquid is recommended.

Children from 4 to 8 years are not recommended to appoint loperamide in capsules, the recommended dosage form - solution for intake.

Use at abnormal liver functions. With care it is necessary to appoint drug at a liver failure. Patients with an abnormal liver function have to be under careful observation for the purpose of early detection of signs of toxic damage of the central nervous system.

Use at pregnancy and feeding by a breast. Loperamide is contraindicated in the I trimester of pregnancy.

Despite the absence of instructions on teratogenic or embriotoksichesky action, in II and III trimesters of pregnancy it is possible to appoint loperamide only in cases when the estimated advantage of therapy for mother exceeds potential risk for a fruit.

Loperamide in small amounts is emitted with breast milk therefore in need of use of drug in the period of a lactation breastfeeding should be stopped.

Influence on ability to driving of motor transport and to control of mechanisms. During treatment it is necessary to refrain from driving of transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and high speed of psychomotor reactions.

Side effects:

Below the listed undesirable effects classified as follows, very frequent (> 10%), frequent (> 1% and <10%), infrequent (> 0.1% and <1%), rare (> 0.01% and <0.1%) and very rare (<0.01%), including isolated cases.

Skin and hypodermic fatty tissue: very seldom - rash, an itch, urticaria, isolated cases of a Quincke's disease, violent rashes, including Stephens-Johnson's syndrome, a multiformny erythema and a toxic epidermal necrolysis.

From an organism in general: isolated cases allergic reactions, in certain cases - hypersensitivity reactions to loperamide, including an acute anaphylaxis and anaphylactoid reactions.

Disturbances from digestive tract: very seldom - an abdominal pain, nausea, a lock and/or abdominal distention, vomiting and dyspepsia, intestinal непроходимостиь, megacolon, including option of a toxic current.

From urinogenital system: isolated cases of an ischuria.

From a nervous system: very seldom - dizziness.

From sense bodys: very seldom - taste distortion.

From mentality: isolated cases - drowsiness.

Messages on adverse reactions during clinical and post-market researches of loperamide are typical for an acute diarrheal syndrome (abdominal pain / discomfort, nausea, vomiting, dryness in a mouth, fatigue, drowsiness, dizziness, locks and swelling). Therefore it is usually quite difficult to establish a causal relationship between reception of loperamide and emergence of the listed symptoms.

Interaction with other medicines:

Except for the drugs possessing similar pharmacological action because of possible mutual strengthening of effect, interaction with other medicines it is not revealed.

Contraindications:

— the acute dysentery and other infections of a GIT (caused including Salmonella spp., Shigella spp., Campylobacter spp.);
— intestinal impassability (including if necessary to avoid suppression of a vermicular movement);
— divertuculosis;
— acute ulcer colitis;
— a pseudomembranous coloenteritis (the diarrhea caused by reception of antibiotics);
— I trimester of pregnancy;
— period of a lactation (breastfeeding);
— children's age up to 8 years;
— hypersensitivity to loperamide and/or other components of medicine.

With care it is necessary to appoint drug at a liver failure.

Overdose:

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

Treatment: a gastric lavage, purpose of absorbent carbon (not later than in 3 h after loperamide reception), if necessary - the artificial ventilation of the lungs (AVL), performing symptomatic therapy. An antidote - Naloxonum. Since duration of effect of loperamide is more, than at Naloxonum (1 - 3 h), repeated appointment of the last can be required. For identification of possible oppression of TsNS it is necessary to watch closely a condition of the patient not less than 48 h.

Storage conditions:

In the place protected from light and moisture, at a temperature from 15 to 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the termination of a period of validity.

Issue conditions:

Without recipe

Packaging:

10 capsules in a blister strip packaging; 1 or 2 blister strip packagings together with a leaf insert in a pack (No. 10 x 1, No. 10 x 2).