Lincomycin hydrochloride - instructions for use, dose, side effects, contraindications

Antibiotic, produced Streptomyces lincolnensis, has a bacteriostatic effect. Suppress protein synthesis of bacteria due to reversible binding to 50Sthe subunit of the ribosomes, disrupts the formation of peptide bonds. Sensitive in vivo; Staphylococcus aureus (penicillin-producing and non-producing strains), Streptococcus pneumoniae. Sensitive in vitro; aerobic gram-positive cocci - Streptococcus pyogenes, Streptococcus spp. groups viridans; aerobic Gram-positive sticks - Corynebacterium diphtheriae; anaerobic gram-positive spore-forming sticks - Propionibacterium acnes; anaerobic gram-positive spore-forming sticks - Clostridium tetani, Clostridium perfringens.

Ineffective in most strains Enterococcus faecalis; does not apply to Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae and other gram-negative bacteria, as well as fungi and viruses. The optimum action is in alkaline medium (pH 8-8.5). Resistance to lincomycin develops slowly.In high doses has a bactericidal effect.

Pharmacokinetics:

After parenteral administration, it is widely distributed in the body. 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. With a single intramuscular injection of 600 mg, the maximum plasma concentration of lincomycin is reached after 30 minutes. With a 120-minute intravenous administration of 600 mg of the drug, the therapeutic concentration is maintained for 14 hours.

Partially metabolized in the liver. The half-life is about 5 hours. In diseases of the liver and kidneys, the elimination half-life increases, there is a significant individual variability in the dynamics of concentration of lincomycin in the blood plasma. With renal failure (terminal stage), the half-life is 10-20 hours, with violations of the liver - 8-12 hours. It is excreted unchanged in the form of metabolites with bile and kidneys.

Indications:

Bacterial infections caused by microorganisms sensitive to lincomycin (primarily Staphylococcus spp. and Streptococcus spp., especially microorganisms resistant to penicillins, as well as allergic to penicillins): sepsis, subacute septic endocarditis, lung abscess, pleural empyema, pleurisy, otitis, osteomyelitis (acute and chronic), purulent arthritis, postoperative purulent complications, wound infection, skin infections and soft tissues (pyoderma, furunculosis, phlegmon, erysipelas).

Contraindications:

Hypersensitivity to lincomycin, other components of the drug, severe hepatic and / or renal failure, early infancy (up to 1 month).

Carefully:

Fungal diseases of the skin, mucous membrane of the oral cavity, vagina, myasthenia gravis.

Pregnancy and lactation:

It is contraindicated to use during pregnancy (except when it is necessary for "vital" indications) and during lactation (during treatment breastfeeding should be discontinued).

Dosing and Administration:

Intravenous drip, intramuscularly.

Daily dose for adults - 1800 mg, single dose - 600 mg.In severe infection, the daily dose can be increased to 2,400 mg (in 3 divided doses with an interval of 8 hours). Intravenously, children - in a daily dose of 10-20 mg / kg, regardless of age. Intravenous - only drip, at a rate of 60-80 cap / min. Before the introduction of 2 ml of a 30% solution (600 mg) diluted with 250 ml of 0.9% sodium chloride solution.

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 parenteral should be used in a daily dose not exceeding 1800 mg, with an interval between administrations of at least 12 hours.

Side effects:

From the digestive system: glossitis, stomatitis, nausea, vomiting, diarrhea, itching of the anus; jaundice, a violation of the liver (including increased activity of "liver" transaminases); with prolonged use in large doses, it is possible to develop colitis, including pseudomembranous.

From the hematopoiesis: neutropenia, leukopenia, agranulocytosis, thrombocytopenic purpura, aplastic anemia, pancytopenia.

Allergic reactions: angioedema, serum sickness, anaphylactic reactions; multiform erythema (in some cases similar to Stevens-Johnson syndrome).

From the skin: rash, hives, exfoliative or vesicle-bullous dermatitis.

From the genitourinary system: renal dysfunction (azotemia, oliguria, proteinuria), vaginitis.

From the cardiovascular system: stopping breathing and heart (with rapid intravenous injection).

From the sense organs: noise in the ears, vertigo.

Overdose:

Symptoms: increased manifestation of manifestations of dose-dependent side effects, diarrhea, colitis.

Treatment: symptomatic therapy, poorly removed with hemo- and peritoneal dialysis. The specific antidote to lincomycin is unknown.

Interaction:

Pharmaceutically incompatible with kanamycin. Strengthens the muscle relaxation caused by curare-like remedies. 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.

Special instructions:

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

Intravenous to enter without prior dilution is impossible.

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 hepatic insufficiency is permissible only for "vital" indications.

If there are signs of pseudomembranous colitis (diarrhea, leukocytosis, fever, abdominal pain, discharge with blood and mucus calves) 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 as a solution for oral administration in a daily dose of 0.5-2 g (for 3-4 doses) for 10 days or bacitracin.

When there is diarrhea or impurity of blood in the stool, you should stop taking the medication.

Effect on the ability to drive transp. cf. and fur:For the period of treatment, care must be taken when driving and potentially dangerous mechanisms due to possible dizziness (vertigo), which can lead to a slowing of the speed of psychomotor reactions and a decrease in the ability to concentrate.

Form release / dosage:

Solution for infusion and intramuscular injection 300 mg / ml.

Packaging:

1 ml per ampoule.

For 10 ampoules, together with the instructions for use and the ampoule scarifier, are placed in a cardboard box.

5 ampoules are placed in a contour mesh package.

For 1 or 2 contour mesh packages together with the instruction for use and the ampoule scarifier are placed in a pack of cardboard.

When using ampoules with a break ring, packaging is allowed ampoules without a scarifier ampoule.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C,

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001079

Date of registration:01.11.2011 / 17.02.2015

Expiration Date:Unlimited

The owner of the registration certificate:BELMEDPREPARATY, RUP BELMEDPREPARATY, RUP Republic of Belarus

Manufacturer: & nbsp

BELMEDPREPARATY, RUP Republic of Belarus

Information update date: & nbsp02.09.2016

Illustrated instructions

Instructions

Lincomycin hydrochloride (Lincomycin hydrochloride)