Lincomycin, 30% ampoules, 1ml, 10pcs

Composition

Active ingredient:

lincomycin (in the form of lincomycin hydrochloride – – 300 mg;

excipients:  

disodium edetate,

sodium hydroxide 1 M solution,

water for injection.

Pharmacological action

Pharmacodynamicaantibiotic produced by Streptomyces lincolniensis has a bacteriostatic effect. Inhibits bacterial protein synthesis due to reversible binding to the 50S subunit of ribosomes, disrupts the formation of peptide bonds. Active against gram-positive cocci (Staphylococcus spp., including Staphylococcus Aureus, Streptococcusspp., including Streptococcuspneumonia, Streptococcuspyogenes); Corynebacteriumdiphtheriae, Clostridiumperfringens, Clostridiumtetani. It is effective against Staphylococcus spp., resistant to penicillin, tetracyclines, chloramphenicol, streptomycin, cephalosporins (30% of Staphylococcus spp., resistant to erythromycin, have cross-resistance to lincomycin). It has no effect on Enterococcus spp. Enterococcus faecalis), gram-negative microorganisms, fungi, viruses, protozoa; inferior in activity to erythromycin against spore-forming anaerobes, Neisseria spp., Corynebacterium spp. The optimum action is found in an alkaline environment (pH 8-8.5). Resistance to lincomycin develops slowly. In high doses, it has a bactericidal effect. There is cross-resistance between lincomycin and clindamycin. Pharmacokinetics After parenteral use is widely distributed in the body. With a single intramuscular injection of 600 mg, the peak plasma concentration of lincomycin is reached after 30 minutes. With a 120-minute intravenous use of 600 mg of the drug, the therapeutic concentration is maintained for 14 hours. It penetrates well into the tissues of the lungs, liver, kidneys, through the placental barrier, into the mother’s milk. It is found in high concentrations in bone tissue and joints. It penetrates poorly through the blood-brain barrier, but the permeability of the blood-brain barrier increases with meningitis. However, the concentrations of lincomycin in the cerebrospinal fluid are insufficient for the treatment of meningitis. It is metabolized in the liver. It is excreted unchanged and in the form of metabolites through the gastrointestinal tract and in the urine. The elimination half-life is about 5 hours. In liver and kidney diseases, the elimination half-life increases, and there is a significant individual variability in the dynamics of the level of lincomycin in blood plasma. In case of renal failure (end-stage), the half-life is 10-20 hours, in case of liver dysfunction-8-12 hours. Hemodialysis and peritoneal dialysis are ineffective. Elderly patients. Pharmacokinetics in elderly patients with normal liver and kidney function corresponds to the pharmacokinetics of adult patients.

Indications

Lincomycin hydrochloride, a solution for intravenous and intramuscular use, is indicated for the treatment of severe infections caused by sensitive strains of microorganisms (see the section “Pharmacological properties”). Its use should be reserved for patients who are unable to use penicillin or who are allergic to penicillin.

Due to the risk of developing pseudomembranous colitis associated with lincomycin, the severity of the infection and the possibility of using less toxic drugs (for example, erythromycin) should be considered when prescribing lincomycin.

It is possible to perform surgical procedures in combination with antimicrobial therapy.

Concomitant use of lincomycin with other antimicrobial agents is possible if indicated.

Lincomycin should not be used for mild bacterial infections or viral diseases.

To reduce the development of drug-resistant bacteria and maintain the effectiveness of lincomycin and other antibacterial agents, lincomycin should only be used to treat or prevent infections with a proven or suspected sensitive microorganism. If there is data on the type and sensitivity of the infectious agent, they are used to select or change antibacterial therapy. In the absence of such data, local data on the epidemiology and sensitivity of microorganisms can be used for empirical treatment.

Contraindications

Hypersensitivity to lincomycin, clindamycin and auxiliary components of the drug, pregnancy (except when it is necessary for “vital” indications), lactation, early infancy (up to 1 month). With caution: severe hepatic and / or renal insufficiency, fungal diseases of the skin, oral mucosa, and vagina; myasthenia gravis (for parenteral use).

Side effects

From the digestive system: nausea, vomiting, diarrhea, epigastric pain, abdominal pain, glossitis, stomatitis, transient hyperbilirubinemia, increased activity of hepatic transaminases, with prolonged use-candidiasis of the gastrointestinal tract, pseudomembranous colitis. Hematopoietic disorders: reversible leukopenia, thrombocytopenia, neutropenia; rare: agranulocytosis, aplastic anemia, pancytopenia. Allergic reactions: urticaria, skin rash, exfoliative and bullous dermatitis, angioedema, anaphylactic shock, erythema multiforme, Stevens-Johnson syndrome, serum sickness, pruritus in the anus. From the genitourinary system: in rare cases – renal dysfunction (azotemia, oliguria and / or proteinuria). From the side of the senses: in some cases – tinnitus and dizziness. Local reactions: pain after intramuscular injection; with intravenous use – phlebitis. With rapid intravenous use: reduced blood pressure, dizziness, general weakness, relaxation of skeletal muscles. Other: vaginitis.

Interaction

is physically compatible:  5% dextrose solution,10% dextrose solution,5% dextrose and 0.9% sodium chloride,10% dextrose and 0.9% sodium chloride, Ringer’s solution, infusion solutions with B vitamins, infusion solutions with B vitamins and ascorbic acid, penicillin, cephalotin, tetracycline, cephaloridin, sodium colistimethate, ampicillin, methicillin, chloramphenicol, polymyxin sulfate. Physically incompatible:  novobiocin, kanamycin.

In vitro studies have observed antagonism between lincomycin and erythromycin. Due to the possible clinical significance, these drugs should not be used simultaneously.

Antidiarrheal drugs reduce the effect of lincomycin (the interval between their use should be at least 4 hours). Lincomycin has the property of blocking neuromuscular conduction, so caution should be exercised when using it together with neuromuscular conduction blockers. Increases the effect of drugs for inhalation anesthesia, muscle relaxants and opioid analgesics, increasing the risk of neuromuscular blockage and respiratory arrest.

It should be noted that the definitions of compatibility and incompatibility were established based only on physical observations, and not on chemical analyses. Adequate clinical evaluation of the safety and efficacy of these combinations has not been performed.

How to take, course of use and dosage

Adults:

Intramuscularly-600 mg (2 ml) every 24 hours. If the infection is more severe, take 600 mg (2 ml) every 12 hours or more.

Intravenously – from 600 mg (2 ml) to 1000 mg every 8-12 hours. In more severe cases, the dose may be increased. In life-threatening situations, it is possible to inject up to 8 grams per day.

Children over 1 month of age:

Intramuscularly at a dose of 10 mg / kg of body weight every 24 hours. In more severe cases – 10 mg / kg of body weight every 12 hours or more.

Intravenously – from 10 to 20 mg / kg / day, depending on the severity of the infection. It can be used in divided doses as described above for adults.

Note: Severe cardiopulmonary reactions were observed when lincomycin hydrochloride was administered at higher doses and at a faster rate of use.

Before intravenous use, it is necessary to dilute the antibiotic (1 g of lincomycin hydrochloride is diluted in at least 100 ml of the appropriate solution (see the section “Interaction with other drugs”)). Intravenously, lincomycin hydrochloride is administered only dropwise, the duration of the infusion should be at least 1 hour.

Patients with reduced renal function. For patients with impaired renal function, the dose of lincomycin should be between 25 and 30% of the recommended dose for patients with normal renal function.

Overdose

Symptoms:  increased severity of side effects, diarrhea, colitis.

Treatment: symptomatic therapy. The specific antidote to lincomycin is unknown. Hemodialysis and peritoneal dialysis are ineffective.

Special instructions

To avoid the development of thrombophlebitis and aseptic necrosis, it is better to inject deeply intramuscularly. Intravenous use without prior dilution is impossible. use to patients with hepatic insufficiency is permissible only for “vital” indications. If signs of pseudomembranous colitis appear (diarrhea, leukocytosis, fever, abdominal pain, excretion of blood and mucus with feces), in mild cases, it is sufficient to cancel the drug and prescribe ion exchange resins (colestyramine), in severe cases, compensation for loss of fluid, electrolytes and protein is indicated, vancomycin as a solution for oral use in a daily dose of 0.5-2 g (in 3-4 doses) for 10 days or bacitracin. For severe infections, it is recommended to use in combination with aminoglycosides or other antibiotics acting on gram-negative bacteria. If diarrhea or blood is present in the stool, the drug should be discontinued. Precautions To avoid the development of thrombophlebitis and aseptic necrosis, it is better to inject deeply intramuscularly. Intravenous use without prior dilution is impossible. The duration of the infusion should be at least 1 hour. To reduce the development of drug-resistant bacteria and maintain the effectiveness of lincomycin and other antibacterial agents, lincomycin should only be used to treat or prevent infections with a proven or suspected sensitive microorganism. Caution should be exercised when prescribing lincomycin to people with allergic diseases, a history of bronchial asthma and gastrointestinal diseases (especially colitis). Clostridium difficile-associated diarrhea (CDAD) has been reported with almost all antibacterial agents, including lincomycin, and can range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents changes the normal flora of the colon, leads to an excessively rapid growth of C. difficile. C. difficile produces toxins A and B, which contribute to the development of diarrhea. Hypertoxin-producing strains of C. Difficile cause increased morbidity and mortality, as these infections may be refractory to antibiotic therapy and may require colectomy. CDAD should be suspected in all patients who develop it after taking antibiotics. A medical history should be collected, as CDAD is reported to occur within two months of the use of antibacterial drugs. If CDAD is suspected or confirmed, continued use of non-targeted antibiotics may need to be discontinued. Infusion solutions and electrolytes, protein supplements, and antibiotics against C. difficile can be used. If signs of pseudomembranous colitis appear (diarrhea, leukocytosis, fever, abdominal pain, excretion of blood and mucus with feces), in mild cases, it is sufficient to cancel the drug and prescribe ion exchange resins (colestyramine), in severe cases, compensation for loss of fluid, electrolytes and protein is indicated, vancomycin as a solution for oral use in a daily dose of 0.5-2 g (in 3-4 doses) for 10 days or bacitracin. Due to cases of severe colitis (sometimes fatal) associated with lincomycin, it is a reserve antibiotic and should only be used for severe bacterial infections, when less toxic ones (for example, erythromycin) are ineffective or contraindicated. Long-term use of lincomycin can lead to an excessively rapid growth of insensitive organisms. Re-evaluation of the patient’s condition is essential. If superinfection occurs during treatment, appropriate measures should be taken. use of lincomycin in the absence of a proven or strongly suspected bacterial infection or prophylactic use is unlikely to provide benefit to the patient and increases the risk of developing drug-resistant bacteria. For severe infections, it is recommended to use in combination with aminoglycosides or other antibiotics acting on gram-negative bacteria. If diarrhea or blood is present in the stool, the drug should be discontinued. Against the background of long-term treatment, periodic monitoring of the activity of “hepatic” transaminases and kidney function is necessary. Although lincomycin penetrates the blood-brain barrier, the concentrations of lincomycin in the cerebrospinal fluid are insufficient to treat meningitis. Hypersensitivity reactions, including anaphylaxis, have been reported in patients receiving lincomycin therapy. If an anaphylactic reaction occurs, you should stop taking the drug and seek medical attention. The drug contains sodium (0.01 mg in 1 ampoule), which should be taken into account in patients on a low-sodium diet. Impaired liver and kidney function. The serum half-life of ~ lin-comacin may be prolonged in patients with severe renal impairment compared to patients with normal renal function. In patients with impaired liver function, the serum half-life of lincomycin may be twice as long as in patients with normal liver function. In patients with severe renal and/or hepatic impairment, lincomycin should be dosed with caution and serum levels should be monitored during high-dose therapy. Use during pregnancy and lactation. The use of the drug during pregnancy is not recommended and is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus. If it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be decided. Influence on the ability to drive a car and potentially dangerous mechanisms. When using lincomycin, it is impossible to exclude the possibility of dizziness and relaxation of skeletal muscles, so driving vehicles and other activities that require increased attention and reaction speed are not recommended.

Form of production

In ampoules of 1 ml. 10 ampoules together with the instructions for use are placed in a box. 5 ampoules are placed in a contour cell package,1 or 2 contour cell packages together with the instructions for use are placed in a pack.

Storage conditions

Store in a dark place at a temperature of 15 ° C to 25 ° C.

Keep out of the reach of children.

Shelf

life is 3 years.

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

Active ingredient

Lincomycin

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Purpose

For adults as prescribed by a doctor, for children as prescribed by a doctor

Indications

Osteomyelitis, Boils, Otitis Media, Purulent Wounds, Pyoderma, Pneumonia, Skin Infections