Lincomycin hydrochloride

General characteristics. Structure:

Active ingredient: 300 mg of lincomycin in 1 ml of solution.

Excipients: dinatrium эдетат, sodium hydroxide, water for injections.

Pharmacological properties:

Pharmacodynamics. Antibiotic of group of linkozamid. In therapeutic doses works bacteriostatically. At higher concentration has bactericidal effect. Suppresses synthesis of protein in a microbic cell.

It is active preferential concerning aerobic gram-positive bacteria: Staphylococcus spp. (including the strains producing a penicillinase), Streptococcus spp. (including Streptococcus pneumoniae (except for Enterococcus faecalis), Corynebacterium diphtheriae; anaerobic bacteria of Clostridium spp., Bacteroides spp.

The majority of gram-negative bacteria, mushrooms, viruses, the elementary are steady against lincomycin. Stability is developed slowly.

There is a cross resistance of microflora to lincomycin, clindamycin and other antibiotics of linkozamidny structure.

Pharmacokinetics. After intramuscular introduction in a dose of 600 mg the maximum concentration in plasma makes 12-20 mkg/ml and is reached in 0,5-1 h. At intravenous infusion in the same dose during 2 h the maximum concentration of lincomycin in a blood plasma makes 20 mkg/ml.

Linkng with proteins of plasma makes 72%. Easily gets through gistogematichesky barriers into fabrics. In blood of a fruit, peritoneal and pleural liquid concentration of lincomycin makes 25 – 50% of its level in blood, in maternal milk the level of lincomycin makes 50 - 100% of concentration in blood, in a bone tissue – about 40%. Through a blood-brain barrier gets badly (lincomycin level in liquor makes 1 – 18% of level in blood), but at meningitis permeability of a barrier to lincomycin increases (to 40% of level in blood). The volume of distribution of lincomycin makes 0,5 l/kg. It is partially metabolized in a liver. T1/2 makes about 5 h. It is removed in not changed look and in the form of metabolites with urine, bile and a stake.

At intramuscular administration of lincomycin its therapeutic concentration in blood is maintained during 17-20 h; at intravenous – during 14 h.

Indications to use:

The infectious and inflammatory diseases of a heavy current caused by microorganisms, sensitive to lincomycin, including sepsis, osteomyelitis, septic endocarditis, pneumonia, lung abscess, pleura empyema, wound fever. As a reserve antibiotic at the infections caused by strains of staphylococcus and other gram-positive microorganisms, resistant to penicillin and other antibiotics.

Route of administration and doses:

At intramuscular introduction by the adult - on 600 mg of 1 - 2 times/days. Intravenously kapelno enter on 600 mg into 250 ml of isotonic solution of sodium of chloride or glucose of 2 - 3 times/days.

To children aged from 1 month is also more senior at heavy infections appoint intramusculary in a dose 10 mg/kg/days in each 12 h or is more often, intravenous drop administration in a dose of 10-20 mg/kg/days in one or several introductions is allowed.

Features of use:

At an abnormal liver function and/or kidneys it is necessary to reduce a single dose of lincomycin on ⅓-½ and to increase an interval between introductions. At prolonged use systematic control of functions of kidneys and a liver, indicators of the general blood test is necessary.

Persons need to appoint lincomycin with care with the allergic reactions having bronchial asthma, colitis and gastrointestinal diseases in the anamnesis.

In case of development of pseudomembranous colitis lincomycin should be cancelled.

Side effects:

From the alimentary system: nausea, vomiting, pains in epigastriums, diarrhea, a glossitis, stomatitis; tranzitorny increase in level of serumal transaminases and bilirubin in a blood plasma; at prolonged use in high doses development of pseudomembranous colitis is possible, it is rare – disturbance of functions of a liver (jaundice).

From system of a hemopoiesis: reversible leukopenia, neutropenia, thrombocytopenia.

Allergic reactions: urticaria, exfoliative dermatitis, Quincke's edema, acute anaphylaxis, rash, mnogoformny exudative erythema, Stephens-Johnson's syndrome

The effects caused by chemotherapeutic action: candidiasis.

From urinogenital system: in rare instances – dysfunction of kidneys (an azotemia, an oliguria, and/or a proteinuria).

From sense bodys: in some cases – a sonitus and dizziness.

Local reactions: phlebitis (at intravenous administration).

At bystry intravenous administration: lowering of arterial pressure, dizziness, general weakness, relaxation of skeletal muscles.

Interaction with other medicines:

At simultaneous use with penicillin, cephalosporins, chloramphenicol or erythromycin antagonism of antimicrobic action is possible.

At simultaneous use with aminoglycosides an action synergism is possible.

At simultaneous use with means for an inhalation anesthesia or muscle relaxants of peripheral action strengthening of neuromuscular blockade is noted, up to development of an apnoea.

Reception of antidiarrheal drugs reduces effect of lincomycin.

Pharmaceutical interaction. Pharmaceutical it is incompatible with ampicillin, barbiturates, theophylline, calcium a gluconate, heparin and magnesium sulfate.

Lincomycin is incompatible in one syringe or a dropper with Kanamycinum or novobiocin.

Contraindications:

Hypersensitivity to lincomycin and clindamycin, the expressed abnormal liver functions and/or kidneys, pregnancy, a lactation, early chest age (up to 1 month).

Overdose:

Symptoms: emergence of side effects from digestive tract, including abdominal pains is possible, nausea, vomitings, diarrheas. At bystry intravenous administration of high doses of drug without cultivation cardiac standstill cases are described.

Treatment: in the presence of indications it is possible to cause vomiting or to carry out a gastric lavage. Specific antidotes are not known.

Storage conditions:

In the place protected from light, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 3 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

In ampoules on 1 ml in packaging No. 10 x 1, No. 10.