Lincomycin hydrochloride
Lincomycin hydrochloride: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Lyncomycin hydrochloride
ATX code: J01FF02
Active ingredient: lincomycin (lincomycin)
Manufacturer: Belmedpreparaty (Republic of Belarus), Moskhimfarmpreparaty them. N. A. Semashko (Russia), Sishui Xierkang Pharmaceutical (China)
Description and photo updated: 2018-23-11
Prices in pharmacies: from 67 rubles.
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Lincomycin hydrochloride is an antibacterial drug for systemic use.
Release form and composition
Dosage forms of Lincomycin hydrochloride release:
- solution for infusion and intramuscular injection: transparent, colorless or somewhat yellowish, with a slight specific odor (in a cardboard box 1 or 2 blisters of 5 or 10 ampoules of 1 or 2 ml);
- capsules: hard gelatinous, white, size No. 0; the capsules contain a white powder, the presence of seals of the capsule mass in the form of a tablet or a column is permissible, crumbling when pressed with a glass rod (in a cardboard box, 2 blisters of 10 capsules each).
Composition of 1 ml injection solution:
- active substance: lincomycin - 300 mg (in the form of lincomycin hydrochloride monohydrate);
- auxiliary components: disodium edetate dihydrate - 0.1 mg; sodium hydroxide (solution 1 M) - up to pH 6; water for injection - up to 1 ml.
Composition of 1 capsule:
- active substance: lincomycin - 250 mg (in the form of lincomycin hydrochloride);
- auxiliary components: granulated sugar, potato starch, calcium stearate;
- capsule: glycerin, titanium dioxide, gelatin, sodium lauryl sulfate, purified water.
Pharmacological properties
Pharmacodynamics
Lincomycin hydrochloride is an antibiotic produced by Streptomyces lincolnensis that has a bacteriostatic effect.
The active substance inhibits bacterial protein synthesis due to reversible binding with the 50S-subunit of ribosomes, contributes to the disruption of the formation of peptide bonds.
Usually, sensitivity to the action of Lincomycin hydrochloride is shown by:
- aerobic gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive), Actinomyces israelii, Viridans group streptococci, Streptococcus agalactiae;
- anaerobic microorganisms: Bacteroides spp. (excluding B.fragilis), Fusobacterium spp., Prevotella spp., Peptococcus spp., Veillonella spp.;
- other microorganisms: Gardnerella vaginalis, Chlamydophila pneumonia, Chlamydia trachomatis, Mycoplasma hominis.
Microorganisms for which acquired resistance can be a problem:
- aerobic gram-positive / gram-negative microorganisms: Staphylococcus aureus (methicillin-resistant), Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Streptococcus pneumonia, Moraxella catarrhalis;
- anaerobic microorganisms: Clostridium perfringens, Bacteroides fragilis, Propionibacterium spp., Peptostreptococcus spp.
Microorganisms with natural resistance:
- aerobic gram-positive / gram-negative microorganisms: Enterococcus spp., Listeria monocytogenes, Escherichia coli, Neisseria gonorrhoeae, Klebsiella spp., Pseudomonas aeruginosa;
- anaerobic microorganisms: Clostridium difficile;
- other microorganisms: Ureaplasma urealyticum, Mycoplasma pneumonia.
Lincomycin hydrochloride does not act on viruses, fungi, protozoa.
Resistance to the action of lincomycin develops slowly. In high doses, it has a bactericidal effect. The optimum effect develops in an alkaline environment at a pH of 8–8.5.
There is cross-resistance between clindamycin and lincomycin.
Pharmacokinetics
Absorption and distribution:
- injection solution: after parenteral administration, the substance is widely distributed in the body. It is characterized by good penetration into the tissues of the lungs, kidneys, liver, through the placental barrier and into breast milk; in joints and bone tissue it is found in high concentrations. In a small amount, it penetrates the blood-brain barrier, with meningitis, permeability increases. The maximum concentration in blood plasma after a single intramuscular injection of 600 mg of lincomycin is achieved in 30 minutes. When the same dose is administered intravenously for 120 minutes, the maintenance of the therapeutic concentration is observed for 14 hours;
- capsules: absorption is 20–35% (food intake slows down the rate and extent of absorption). After oral administration of 500 mg of lincomycin, the maximum serum concentration is approximately 0.003 mg / ml, which is reached in 2–4 hours. This indicator is reduced by about 2 times when lincomycin is taken simultaneously with food. Therapeutic blood concentrations after oral administration persist for 6-8 hours. In pleural and peritoneal fluids, as well as in the blood of the fetus, the concentration of the substance is 25-50% of the level in the blood, in breast milk - 50-100%, in bone tissue - about 40%, in soft tissues - about 75%.
Partially metabolized in the liver. T 1/2 (half-life) - about 5 hours, with liver / kidney disease, this indicator increases, there is a significant individual variability in the dynamics of the concentration of lincomycin in the blood plasma. With end-stage renal failure, T 1/2 is in the range from 10 to 20 hours, with violations of hepatic function - from 8 to 12 hours. It is excreted both in the form of metabolites and unchanged, by the kidneys and with bile.
Indications for use
According to the instructions, Lincomycin hydrochloride is prescribed for the treatment of severe infections that are caused by microorganisms sensitive to its action:
- upper / lower respiratory tract infections, including chronic sinusitis, otitis media (as adjunctive therapy), pneumonia, bronchitis;
- infections of soft tissues and skin (the drug is used in cases where the appointment of penicillins is not indicated);
- joint and bone infections, including septic arthritis, osteomyelitis;
- septic endocarditis;
- sepsis.
Contraindications
Absolute:
- severe hepatic / renal impairment;
- colitis (capsules);
- meningitis (capsules);
- congenital fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase deficiency (capsules);
- early infancy (up to 1 month);
- lactation period;
- individual intolerance to the components of the drug.
Relative (Lincomycin hydrochloride is prescribed under medical supervision):
- fungal diseases of the vagina, skin, oral mucosa;
- myasthenia gravis (injection solution);
- pregnancy.
Instructions for the use of Lincomycin hydrochloride: method and dosage
Injection solution
Recommended dosage regimen:
- intramuscularly: every 24 hours at 600 mg (adults) or 10 mg / kg (children). For more severe infections, Lincomycin hydrochloride may be given every 12 hours or more;
- intravenously: every 8-12 hours, 600-1000 mg (adults) or 10-20 mg / kg per day (children). When treating more severe infections, the dose may be increased. In life-threatening situations, adults can be administered up to 8,000 mg per day.
It must be taken into account that severe cardiopulmonary reactions have been observed with the use of high doses and high rates of administration.
Before intravenous administration, 1000 mg of Lincomycin hydrochloride is diluted in at least 100 ml of an appropriate solution. The drug is administered intravenously only by drip, the duration of the infusion is 1 hour or more.
Features of infusion (diluent volume / time of infusion):
- 600-1000 mg: 100 ml / 1 hour;
- 2000 mg: 200 ml / 2 hours;
- 3000 mg: 300 ml / 3 hours;
- 4000 mg: 400 ml / 4 hours.
The duration of the course is determined by the form and severity of the infection and can vary from 7 to 14 days (with osteomyelitis - at least 21 days).
In case of impaired renal function, the dose of Lincomycin hydrochloride is reduced. It is usually 25–30% of the recommended dose for non-impaired patients.
Capsules
Lincomycin hydrochloride is taken orally with a sufficient amount of water, preferably 1-2 hours before / after meals (food intake slows down and reduces absorption).
Recommended daily doses:
- adults: 1000-2000 mg in 3-4 divided doses (single dose is 500 mg);
- children: 30 mg / kg in 3–4 equal doses, in severe infections, an increase to a maximum dose of 60 mg / kg is possible.
The duration of the course is determined by the form and severity of the infection and can vary from 7 to 14 days (with osteomyelitis - at least 21 days).
In case of impaired renal function, the dose of Lincomycin hydrochloride is reduced. It is usually 25–30% of the recommended dose for non-impaired patients.
Side effects
Injection solution
- digestive system: epigastric pain, nausea, diarrhea, vomiting, abdominal pain, stomatitis, glossitis, increased activity of hepatic transaminases, transient hyperbilirubinemia; with prolonged use - pseudomembranous colitis, candidiasis of the gastrointestinal tract;
- genitourinary system: in rare cases - renal dysfunction (in the form of azotemia, oliguria and / or proteinuria);
- hematopoietic organs: reversible neutropenia, thrombocytopenia, leukopenia; rarely - aplastic anemia, agranulocytosis, pancytopenia;
- senses: in some cases - dizziness, tinnitus;
- allergic reactions: skin rash, itching in the anus, urticaria, exfoliative / bullous dermatitis, erythema multiforme, anaphylactic shock, Quincke's edema, serum sickness, Stevens-Johnson syndrome;
- local reactions: pain at the site of intramuscular injection; with intravenous administration - phlebitis; with rapid intravenous administration - relaxation of skeletal muscles, general weakness, lowering blood pressure, dizziness;
- others: vaginitis.
Capsules
- digestive system: stomatitis, glossitis, abdominal pain, vomiting, nausea, diarrhea, colitis (including pseudomembranous), gastrointestinal candidiasis, esophagitis, itching of the anus, jaundice, impaired liver function (including increased activity of hepatic transaminases);
- genitourinary system: impaired renal function (in the form of azotemia, oliguria, proteinuria), vaginitis;
- skin: itching, urticaria, rash, exfoliative / vesicular-bullous dermatitis;
- senses: vertigo, tinnitus;
- hematopoietic organs: pancytopenia, aplastic anemia, neutropenia, agranulocytosis, leukopenia, thrombocytopenic purpura;
- allergic reactions: anaphylactic reactions, serum sickness, angioedema; rarely - erythema multiforme (sometimes similar to Stevens-Johnson syndrome);
- others: growth of insensitive flora, fungi.
Overdose
The main symptoms: increased severity of adverse reactions, abdominal pain, colitis, nausea, diarrhea, vomiting.
Therapy: symptomatic. The specific antidote is unknown. Peritoneal dialysis and hemodialysis are not effective.
special instructions
To avoid the occurrence of aseptic necrosis and thrombophlebitis, Lincomycin hydrochloride solution is best administered deeply intramuscularly.
Intravenous administration without prior dilution is prohibited.
Lincomycin hydrochloride can be used in patients with hepatic insufficiency only for health reasons.
When signs of pseudomembranous colitis appear (in the form of diarrhea, leukocytosis, fever, abdominal pain, discharge with fecal mucus and blood) in mild cases, it is enough to cancel the drug, then ion-exchange resins (colestyramine) are prescribed. In severe cases, it is necessary to compensate for the loss of fluid, protein and electrolytes, vancomycin is used as a solution for oral administration in a daily dose of 500-2000 mg (for 3-4 doses) for 10 days, or bacitracin.
If diarrhea or an admixture of blood in the stool occurs, Lincomycin hydrochloride should be immediately withdrawn.
In the treatment of severe infections, it is recommended to use it in combination with aminoglycosides or other antibiotics that act on gram-negative bacteria.
To reduce the likelihood of developing drug-resistant bacteria and to maintain the efficacy of lincomycin and other antibacterial agents, Lincomycin hydrochloride should only be used to treat / prevent infections with proven or suspected susceptible organisms.
Caution during therapy should be observed against a background of allergic diseases, bronchial asthma and diseases of the gastrointestinal tract (especially colitis) in history.
Prolonged use of Lincomycin hydrochloride can lead to an overgrowth of insensitive organisms. In this regard, re-assessment of the patient's condition is of great importance. If superinfection occurs during therapy, appropriate measures must be taken.
During prolonged use, it is necessary to periodically monitor the activity of hepatic transaminases and the functional state of the kidneys.
There is an antagonism between lincomycin and erythromycin, so their combined use is not recommended.
Lincomycin hydrochloride can block neuromuscular conduction, and therefore caution should be exercised when combined with neuromuscular blockers.
Influence on the ability to drive vehicles and complex mechanisms
During therapy with Lincomycin hydrochloride, it is recommended to refrain from driving motor vehicles, which is associated with the likelihood of dizziness and relaxation of skeletal muscles.
Application during pregnancy and lactation
- pregnancy: therapy is contraindicated (unless the use of Lincomycin hydrochloride is necessary for health reasons);
- lactation period: therapy is contraindicated.
Pediatric use
Lincomycin hydrochloride therapy is contraindicated in patients under 1 month of age.
The preparation in the form of capsules is not recommended for use in children under 6 years of age who may have difficulty swallowing.
With impaired renal function
Contraindication: severe renal failure.
For violations of liver function
Contraindication: severe hepatic impairment.
Drug interactions
Lincomycin hydrochloride solution is physically compatible with the following solutions / drugs: 5% and 10% dextrose solutions, 5% dextrose and 0.9% sodium chloride, 10% dextrose and 0.9% sodium chloride, Ringer's solution, infusion solutions with B vitamins and with / without ascorbic acid, polymyxin sulfate, cephalothin, penicillin, cephaloridin, tetracycline, ampicillin, sodium colistimethate, chloramphenicol, methicillin.
Lincomycin hydrochloride is physically / pharmaceutically incompatible with novobiocin, kanamycin; additionally for capsules - with ampicillin, phenytoin, theophylline, barbiturates, calcium gluconate, heparin and magnesium sulfate.
Antagonism is observed when combined with the following drugs: penicillins, cephalosporins, erythromycin, chloramphenicol and other bactericidal antibiotics; synergism - when used simultaneously with aminoglycosides.
Other possible interactions:
- curariform drugs: the muscle relaxation they cause increases;
- means for inhalation anesthesia (chloroform, cyclopropane, enflurane, halothane, isoflurane, methoxyflurane, trichlorethylene): neuromuscular blockade, respiratory paralysis or depression may occur;
- narcotic analgesics: the risk of respiratory depression increases, up to and including apnea;
- antidiarrheals / adsorbents: absorption of lincomycin is reduced (when taken orally; recommended intervals are 2 hours before or 4 hours after taking these drugs).
Taking Lincomycin hydrochloride may affect the result of the analysis of the plasma concentration of alkaline phosphatase (erroneously high level is possible).
Analogs
Lincomycin hydrochloride analogues are: Lincomycin, Ekolinkom, Lincomycin hydrochloride-Vial.
Terms and conditions of storage
Store in a place protected from light and moisture at a temperature of 15-25 ° C. Keep out of the reach of children.
Shelf life:
- injection solution - 3 years;
- capsules - 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Lincomycin hydrochloride
According to reviews, Lincomycin hydrochloride is an effective antibiotic. Most often it is used in the treatment of severe infectious diseases and in dentistry. In some cases, patients indicate the development of adverse reactions.
The price of Lincomycin hydrochloride in pharmacies
The approximate price for Lincomycin hydrochloride (injection solution, 10 ampoules of 1 or 2 ml) is 134 or 185 rubles.
Lincomycin hydrochloride: prices in online pharmacies
Drug name Price Pharmacy |
Lincomycin hydrochloride 30% solution for injection 1 ml 10 pcs. RUB 67 Buy |
Lincomycin hydrochloride 300 mg / ml solution for intravenous and intramuscular administration 1 ml 10 pcs. RUB 68 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!