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LINCOMICINE HYDROCHLORIDE capsules 250 mg

Instruction manual

For medical use of the drug

Structure:

Active ingredient: lincomycin hydrochloride;

1 capsule contains lincomycin hydrochloride in terms of 100% lincomycin - 250 mg;

excipients: pregelatinized starch, calcium stearate;

composition of gelatin capsule No. 1:

cap: yellow sunset FCF (E 110), quinoline yellow (E 104), titanium dioxide (E 171), gelatin;

case: titanium dioxide (E 171), gelatin.

Dosage form.

Capsules

Basic physical and chemical properties: hard capsules with a white body and a yellow cap. The contents of the capsules is a white powder.

Pharmacotherapeutic group.

Antibacterial agents for systemic use. macrolides, lincosamides, streptogramins. lincosamides. code atx j01f f02.

Pharmacological properties.

Pharmacodynamics

Lincomycin is an antibiotic that is produced by Streptomyces lincolniensis or other actinomycetes and belongs to the group of lincosamides. The mechanism of action is associated with inhibition of protein synthesis of microorganisms due to the formation of an irreversible connection with the 50S subunits of ribosomes and a violation of peptidyl transferase activity and inhibition of translocation and transpeptidization reactions. Lincomycin hydrochloride has a bacteriostatic and / or bactericidal effect depending on the concentration of the drug and the sensitivity of the microorganism. Effective against anaerobic non-spore forming gram-positive bacteria, including Actinomyces spp .; Propionibacterium spp. and Eubacterium spp .; anaerobic and microaerophilic cocci, including Peptococcus spp., Peptostreptococcus spp. and microaerophilic streptococci; aerobic gram-positive cocci, including Staphylococcus spp .; streptococcus spp. (except S. faecalis), including streptococcus pneumoniae.

The following microorganisms are moderately sensitive to the drug: anaerobic non-spore forming gram-negative bacteria, including Bacteroides spp., Fusobacterium spp .; anaerobic sporogenous gram-positive bacteria, including Clostridium spp.

The following microorganisms are resistant or insensitive to the drug: streptococcus faecalis, Neisseria spp., Most strains of Haemophilus influenzae, Pseudomonas spp. and other gram-negative microorganisms. Due to the low absorption of lincomycin from the digestive tract and the creation of a high inhibitory concentration, the drug was very effective in bacterial dysentery caused by Shigella.

Pharmacokinetics

After oral administration, lincomycin is rapidly absorbed from the digestive tract (about 20–33% of the dose taken) and enters various organs and tissues, including bone tissue. The maximum concentration in the blood is reached after 2–4 hours. If the antibiotic is taken after a meal, adsorption is reduced by 50%. Concentrations are created in the blood of the fetus, peritoneal and pleural fluids, which are approximately 25-50% of the level in the blood, in breast milk - 50-100%, in bone tissue - about 40%, in soft tissues - 75%. The drug penetrates poorly through the blood-brain barrier, but permeability increases with meningitis (40% of that in the blood). Through the placenta, the drug penetrates well. The metabolism of lincomycin hydrochloride occurs in the liver. Excretion of the drug depends on the route of administration. When taken orally, approximately 4% is excreted in the urine, and about 33% with feces. The concentration of the drug in bile is 10 times higher than that in the blood. The half-life is 5.4 hours. Diseases of the liver and kidneys significantly affect the elimination of the drug.

Clinical characteristics.

Indications.

Lincomycin is indicated for the treatment of serious infections caused by lincomycin-sensitive strains of gram-positive aerobic microorganisms, such as streptococci, pneumococci and staphylococci, or drug-sensitive anaerobic bacteria:

  1. Upper respiratory tract infections: chronic sinusitis caused by anaerobic strains. Lincomycin can be used to treat individual cases of purulent otitis media or as an additional therapy along with an antibiotic that effectively acts against aerobic gram-negative pathogens. H. Infectionsinfluenzae, are not an indication for the use of the drug (see section "Pharmacodynamics").
  2. Infections of the lower respiratory tract, including infectious exacerbations of chronic bronchitis and infectious pneumonia.
  3. Serious infections of the skin and soft tissues caused by susceptible microorganisms in cases where antibiotic administration of the penicillin group is not indicated.
  4. Infections of bones and joints, including osteomyelitis and septic arthritis.
  5. Septicemia and endocarditis. In some cases of septicemia and / or endocarditis due to the sensitivity of pathogens to lincomycin, a pronounced response to lincomycin treatment was observed. However, the use of bactericides is often preferred to treat such infections.

Contraindications

  • Hypersensitivity to lincomycin, clindamycin, to the components of the drug; myasthenia gravis; colitis in the acute stage; meningitis.

Interaction with other drugs and other types of interactions.

Penicillins, cephalosporins, chloramphenicol: antimicrobial antagonism is possible.

Since the antagonism between lincosamides and erythromycin, as well as macrolide compounds whose chemical structure is related to erythromycin, is shown in vitro, clinically significant interactions are possible. Therefore, it is not recommended to use macrolides or streptogramins with lincomycin simultaneously.

Aminoglycosides: synergies of action are possible.

Kaolin-pectin mixtures, antidiarrheal drugs: the bioavailability of lincomycin is reduced by 90%, so these funds should be taken 2 hours or 3-4 hours after taking lincomycin.

Neostigmine, pyridostigmine: Lincosamides counteract the effects of these anticholinesterase drugs.

Muscle relaxants (including suxamethonium), drugs for inhalation anesthesia, opioid analgesics: lincosamides exhibit the properties of a neuromuscular blocker, therefore, they can enhance neuromuscular blockade up to the development of apnea.

Estrogens: the contraceptive effect of estrogen may be reduced. Although the risk is low, it is recommended to use additional methods of contraception during use and within 7 days after stopping the use of lincosamides.

Oral typhoid vaccine: antibacterial drugs, including lincosamides may reduce its therapeutic effect.

Taking antidiarrheal drugs reduces the effect of lincomycin.

There is absolute cross-resistance of microorganisms to lincomycin and clindamycin.

Kanamycin, novobiocin, ampicillin, barbiturates, theophylline, calcium gluconate, heparin and magnesium sulfate are pharmaceutically incompatible with lincomycin (this applies to parenteral forms of lincomycin).

Features of the application.

It is necessary to conduct microbiological studies in order to determine pathogens and their sensitivity to lincomycin.

The efficacy of lincomycin for the treatment of staphylococcal infections resistant to other antibiotics and sensitive to lincomycin has been demonstrated. Strains of staphylococci resistant to lincomycin were found, therefore, in combination with lincomycin therapy, bacteriological cultures and a study of the sensitivity of pathogens should be carried out. In the case of macrolides, partial cross-resistance is possible. If indicated, the drug can be used simultaneously with other antibacterial drugs.

In order to reduce the rate of emergence of drug-resistant bacteria and maintain the effectiveness of lincomycin and other antibacterial drugs, lincomycin should only be used to treat or prevent infections that are proven or very likely to be caused by susceptible bacteria.If there is information about the results of bacteriological culture and determination of sensitivity, it must be taken into account when choosing or changing antibiotic therapy. In the absence of such data, the empirical choice of therapy may be affected by local epidemiological data and local characteristics of sensitivity characteristics.

The use of lincomycin is not indicated for the treatment of minor bacterial infections and viral infections. Prescribing lincomycin in the absence of a confirmed or suspected high probability of bacterial infection is unlikely to be beneficial for the patient and increases the risk of bacteria with drug resistance.

Due to the risk of developing pseudomembranous colitis, the doctor should analyze the nature of the infection and evaluate the feasibility of using less toxic alternative drugs (for example, erythromycin) before prescribing lincomycin.

The occurrence of diarrhea and pseudomembranous colitis associated with toxins A and B produced by C. difficile (CDAD) has been reported with almost all antibacterial agents, including lincosamides. The severity of the manifestations can range from moderate diarrhea to lethal colitis. Treatment with antibacterial drugs inhibits the normal flora of the large intestine, which can cause excessive growth of C. difficile. C. difficile-associated diarrhea can occur in mild form with watery fluid bowel movements, but can also progress to severe persistent diarrhea, leukocytosis, fever, severe abdominal cramps, and mucus and / or blood in the bowel movements. In cases of mild pseudomembranous colitis, it is usually sufficient to stop taking the drug. With moderate to severe pseudomembranous colitis, treatment should be carried out with the introduction of solutions, electrolytes, proteins and the appointment of antibacterial agents effective against C. difficile in colitis.

Immediately after establishing the initial diagnosis of pseudomembranous colitis, treatment should begin. The diagnosis is usually made on the basis of clinical symptoms, but endoscopy data or the determination of C. difficile and its toxins in the bowel movements of the patient can also be used to confirm the diagnosis. During treatment, you can not prescribe drugs that inhibit intestinal motility.

In the absence of the necessary treatment, toxic megacolon, peritonitis, shock can develop. CDAD should be considered in all patients who develop diarrhea during or after antibiotic use. Please note that CDAD may occur within 2 months after the end of treatment with antibacterial agents. The development of colitis is most likely in severe diseases in elderly patients, as well as in debilitated patients. If lincomycin is used in such patients, closely monitor changes in the frequency of bowel movements.

Strains of C. difficile producing an excess of toxins increase morbidity and mortality, since such infections can be resistant to antibiotic therapy and often require colectomy.

Lincomycin should be prescribed with caution to patients with diseases of the digestive tract, especially with a history of colitis.

The use of antibacterial drugs can lead to excessive growth of insensitive microorganisms, in particular fungi, and the development of superinfection, which requires appropriate measures, given the specific clinical situation. If patients with existing fungal infections need lincomycin treatment, antifungal therapy should be given at the same time.

Cases of serious hypersensitivity reactions, including anaphylactic reactions and severe skin adverse reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis and erythema multiforme, have been reported in patients receiving lincomycin therapy. If an anaphylactic reaction or a serious skin reaction occurs, the use of the drug should be discontinued and appropriate treatment should begin.Serious anaphylactoid reactions require intensive emergency treatment using adrenaline, oxygen therapy and intravenous steroid administration. If indicated, airway patency should also be restored, if necessary by intubation.

Although lincomycin crosses the blood-brain barrier, the level of lincomycin in cerebrospinal fluid may not be sufficient to treat meningitis. Therefore, the drug should not be used in such cases.

In some cases, septicemia and / or endocarditis caused by susceptible microorganisms respond well to lincomycin therapy. However, with these diseases, the use of bactericidal drugs is preferred.

Lincomycin should be used with caution in patients with severe impaired liver / kidney function, accompanied by serious metabolic disorders. For such patients, it is necessary to change the dose of the drug (see the section “Dosage and administration”), and during high-dose therapy, serum lincomycin should be monitored, since the half-life of the drug in these categories of patients can be extended 2-3 times.

With prolonged antibiotic therapy with lincomycin, liver and kidney function, as well as blood counts, should be monitored.

Lincomycin should be used with caution in patients with a history of bronchial asthma and other significant manifestations of allergy.

Lincomycin is able to block neuromuscular transmission of impulses and therefore can enhance the action of other neuromuscular blockers. Therefore, lincomycin should be used with caution for the treatment of patients taking drugs of this class.

Due to the presence of the dye, yellow sunset FCF (E 110) as part of the drug, its use can cause allergic reactions, including bronchial asthma. The risk of allergies is higher in patients with hypersensitivity to acetylsalicylic acid.

Use during pregnancy or lactation.

In humans, lincomycin crosses the hematoplacental barrier and is detected in cord blood serum at 25% of the level in the mothers blood serum. there is no significant accumulation of the drug in the amniotic fluid. the safety of lincomycin for pregnant women has not been established. 302 children born to women who received lincomycin treatment at different stages of pregnancy did not observe an increase in the incidence of congenital anomalies or growth retardation compared with the control group during the first 7 years of life. lincomycin should not be used during pregnancy, unless treatment is absolutely necessary.

Lincomycin passes into breast milk in a concentration of 0.5 to 2.4 μg / ml, therefore, given the possibility of severe reactions to lincomycin in breast-fed infants, a decision should be made whether to stop breast-feeding or to discontinue treatment, depending on the importance of the drug for mothers.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

There was no effect of the drug on the reaction rate when driving motor vehicles or other mechanisms, but dizziness was reported.

Dosage and administration.

Doses and method of application must be determined based on the severity of the infection, the patients condition and the sensitivity of the bacterial pathogen. the duration of treatment is determined individually by the doctor.

It is advisable to take the drug 1–2 hours before or 1–2 hours after a meal. Capsules should be washed down with a sufficient amount of water.

Adults

500 mg 3-4 times a day.

Children (from 6 years old)

30-60 mg / kg / day, distributed in 3 or 4 equal doses.

Patients with impaired renal and / or liver function

If it is necessary to use lincomycin for the treatment of patients with severe impaired renal and / or liver function, the corresponding dose is 25-30% of the dose recommended for patients with normal renal / liver function.

Children.

The drug in this dosage form should not be used for children under 6 years of age.

Overdose.

Symptoms: possible gastrointestinal upsets, including abdominal pain, nausea, vomiting, diarrhea.

Treatment: it is necessary to induce vomiting or, if indicated, to rinse the stomach, conduct symptomatic and supportive therapy. There is no specific antidote. Hemodialysis and peritoneal dialysis are ineffective.

Adverse Reactions

  • Digestive tract: nausea, vomiting, discomfort / pain in the abdomen, glossitis, stomatitis, heartburn, esophagitis / esophageal ulcers, persistent diarrhea, antibiotic-associated colitis, incl. pseudomembranous colitis, which can occur during and 2–3 weeks after antibiotic treatment (see the section “Peculiarities of Use”). immune system: hypersensitivity reactions, incl. angioedema, serum sickness, anaphylaxis, for example, anaphylactic shock; some of them developed in patients with penicillin hypersensitivity. blood and lymphatic system: neutropenia, leukopenia, eosinophilia, agranulocytosis, thrombocytopenia / thrombocytopenic purpura; isolated cases of aplastic anemia and pancytopenia, in which it is impossible to exclude the role of lincomycin as a causative factor. skin and mucous membranes: rashes, incl. maculopapular, skin hyperemia, urticaria, pruritus, vaginitis. in isolated cases - erythema multiforme, which sometimes resembled Stevens-Johnson syndrome and was associated with the introduction of lincomycin, Stevens-Johnson syndrome, exfoliative and vesicle-bullous dermatitis; toxic epidermal necrolysis, acute generalized exanthematous pustulosis (see section "application features"). hepatobiliary system: changes in liver function tests (including elevated levels of transaminases), jaundice. urinary system: in isolated cases - impaired renal function, as evidenced by azotemia, oliguria and / or proteinuria, although there is no direct relationship between lincomycin and kidney damage. effects due to biological effects: with prolonged use at high doses, superinfection, including fungal infection (for example, candidiasis), is possible. other: dysgeusia, itching in the anus, tinnitus, weakness, dizziness, polyarthritis.

Shelf life.

3 years.

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

Storage conditions.

In the original packaging at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Packaging.

10 capsules in a blister, 2 blisters in a pack.

Vacation category.

On prescription.

Manufacturer.

Public Joint Stock Company “Scientific and Production Center“ Borshchag Chemical and Pharmaceutical Plant ”.

The location of the manufacturer and the address of the place of business.

Ukraine, 03134, Kiev, st. peace, 17.

Tags: Lincomycin