Lincomycin - instructions for use, doses, side effects, contraindications

Antibiotic, produced Streptomyces lincolniensis, has a bacteriostatic effect. Suppress protein synthesis of bacteria due to reversible binding to 50S subunit of ribosomes, disrupts the formation of peptide bonds.

Active against gram-positive cocci (Staphylococcus spp., Streptococcus spp., in t.ch. Streptococcus pneumoniae); Haemophilus influenzae; Bacillus anthracis, Mycoplasma spp., Bacteroides spp., Corynebacterium diphtheriae, Clostridium perfringens, Clostridium tetani.

Effective in relation to Staphylococcus spp., resistant to penicillin, tetracyclines, chloramphenicol, streptomycin, cephalosporins (30% Staphylococcus spp., resistant to erythromycin, have cross resistance to lincomycin).

Does not apply to Enterococcus spp (incl. Enterococcus faecalis), Gram-negative microorganisms, fungi, viruses, protozoa; is inferior in activity to erythromycin against spore forming anaerobes, Neisseria spp., Corynebacterium spp.

The optimum action is in alkaline medium (pH 8-8.5). Resistance to lincomycin develops slowly.In high doses has a bactericidal effect.

Pharmacokinetics:

Time to reach the maximum concentration (TCmAh) 2-3 hours. It penetrates well into the tissues of the lungs, liver, kidneys, through the placental barrier, into breast milk; in high concentrations found in bone tissue and joints. Through the blood-brain barrier (BBB) lincomycin penetrates slightly, with meningitis - permeability increases.

Partially metabolized in the liver. The half-life (T1 / 2) is 5 hours. It is excreted unchanged in the form of metabolites with bile and kidneys.

Indications:

Bacterial infections caused by susceptible microorganisms (mainly staphylococci and streptococci, especially microorganisms resistant to penicillins, as well as allergies to penicillin): sepsis, subacute bacterial endocarditis, chronic pneumonia, lung abscess, empyema, pleural effusion, otitis media, osteomyelitis ( acute and chronic), purulent arthritis, postoperative septic complications, wound infection, skin and soft tissue infections (pyoderma, furunculosis, cellulitis, erysipelas).

Contraindications:

Hypersensitivity, pregnancy (except when necessary for "vital" indications), severe hepatic and / or renal failure; early infancy (up to 1 month); lactation period.

Carefully:Fungal diseases of the skin, mucous membrane of the mouth, vagina; myasthenia gravis.

Dosing and Administration:

Intramuscularly (in / m) and intravenously (iv).

The daily dose for adults with parenteral administration is 1.8 g, single dose is 0.6 g. In severe infection, the daily dose can be increased to 2.4 g (in 3 divided doses at an interval of 8 h).

In / in, children - in a daily dose of 10-20 mg / kg, regardless of age. In / in - only drip, with a speed of 60-80 cap / min. Before the introduction of 2 ml of a 30% solution (0.6 g) diluted with 250 ml of a 0.9% solution NaCl.

Duration of treatment, depending on the form and severity of the disease is 7-14 days (with osteomyelitis - 3 weeks or more).

With prolonged or repeated courses, treatment should be performed under the control of liver and kidney function.

In renal-hepatic insufficiency should be used in a daily dose not exceeding 1.8 g, with an interval between administrations of at least 12 hours.

Side effects:

From the digestive system: nausea, vomiting, diarrhea, epigastric pain, abdominal pain, glossitis, stomatitis, transient hyperbilirubinemia, increased activity of "liver" transaminases; with prolonged use - candidiasis of the gastrointestinal tract (GIT), pseudomembranous enterocolitis.

On the part of the organs of hematopoiesis: reversible leukopenia, thrombocytopenia, neutropenia.

Allergic reactions: urticaria, exfoliative dermatitis, angioedema, anaphylactic shock.

Local Reactions: with iv injection - phlebitis.

With a rapid on / in the introduction - lowering blood pressure (BP), dizziness, general weakness, relaxation of skeletal muscles.

Interaction:

Pharmaceutically incompatible with kanamycin, ampicillin, barbiturates, theophylline, calcium gluconate, heparin and magnesium sulfate.

Antagonism - with erythromycin, synergism - with aminoglycosides.

Strengthens the effect of drugs for inhalation anesthesia, muscle relaxants and opioid analgesics, increasing the risk of neuromuscular blockade and stopping breathing.

When used simultaneously with lincomycin, an inhibitor of P450, the effect of theophylline may increase and require a reduction in its dose.

Strengthens the neuromuscular blockade caused by muscle relaxants (especially with parenteral administration).

Special instructions:

To avoid the development of thrombophlebitis and aseptic necrosis, it is better to inject deeply into the / m.

In / in, you can not enter without prior dilution.

Against the background of long-term treatment, periodic monitoring of the activity of "liver" transaminases and kidney function is necessary.

The appointment to patients with severe hepatic insufficiency is permissible only for "vital" indications.

The parenteral form, containing in its composition benzyl alcohol, in preterm infants can lead to the development of bronchospasm.

When there are signs of pseudomembranous enterocolitis (diarrhea, leukocytosis, fever, abdominal pain, discharge with mucous masses of blood and mucus) in mild cases, it is sufficient to discontinue the preparation and prescribe ion-exchange resinscolestramine), in severe cases, compensation for loss of fluid, electrolytes and protein, vancomycin - Inward, in a daily dose of 0.5-2 g (for 3-4 doses) for 10 days or bacitracin.

Form release / dosage:

Solution for intravenous and intramuscular injection 300 mg / ml.

Packaging:

1 ml per ampoule of glass.

For 10 ampoules with a vial for opening ampoules and instructions for medical use are placed in a box of cardboard.

10 ampoules in a blister pack; 1 blister pack with a knife for opening ampoules and instructions for medical use are placed in a pack of cardboard.

In the case of ampoules with a ringa breakage crochet or a notch and a break point, the insertion of a knife for opening ampoules is not provided.

Storage conditions:

List B. In a place protected from light, inaccessible to children, at a temperature of 5 to 25 ° C.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000576

Date of registration:25.06.2010 / 09.06.2015

Expiration Date:Unlimited

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp10.04.2018

Illustrated instructions

Instructions

Lincomycin (Lincomycin)