Linkomitsin Velpharm (Solution) Instructions for Use

Marketing Authorization Holder

Velpharm, LLC (Russia)

ATC Code

J01FF02 (Lincomycin)

Active Substance

Lincomycin (Rec.INN registered by WHO)

Dosage Form

Lincomycin Velpharm

Solution for infusion and intramuscular injection 300 mg/1 ml: amp. 1 ml or 2 ml 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for infusion and intramuscular injection in the form of a clear, colorless or slightly yellowish liquid.

Excipients: disodium edetate dihydrate (disodium salt of ethylenediamine- N,N,N',N' -tetraacetic acid dihydrate (Trilon B)), sodium hydroxide 0.1 M solution, water for injection.

1 ml – ampoules of colorless glass (5) – cardboard packs.
1 ml – ampoules of colorless glass (10) – cardboard packs.
2 ml – ampoules of colorless glass (5) – cardboard packs.
2 ml – ampoules of colorless glass (10) – cardboard packs.

Clinical-Pharmacological Group

Antibiotic of the lincosamide group

Pharmacotherapeutic Group

Systemic antibacterial agents; macrolides, lincosamides, and streptogramins; lincosamides

Pharmacological Action

An antibiotic of the lincosamide group. In therapeutic doses, it acts bacteriostatically. At higher concentrations, it has a bactericidal effect. It suppresses bacterial protein synthesis due to reversible binding to the 50S ribosomal subunit, disrupting the formation of peptide bonds.

Active against Staphylococcus aureus (penicillinase-producing and non-producing strains), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans group, Corynebacterium diphtheria, Propionibacterium acnes, Clostridium tetani, Clostridium perfringens.

Effective against Staphylococcus spp. resistant to penicillin, tetracycline, chloramphenicol, streptomycin, cephalosporins (30% of Staphylococcus spp. resistant to erythromycin have cross-resistance to lincomycin).

Enterococcus spp. (including Enterococcus faecalis), Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae and other gram-negative bacteria, as well as fungi, viruses and protozoa are resistant to lincomycin.

The optimum of action is 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 a single intramuscular injection at a dose of 600 mg, C_max in blood plasma is reached after 30 minutes. After a 120-minute intravenous infusion 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 breast milk; it is found in high concentrations in bone tissue and joints. Partially metabolized in the liver. T_1/2 is 5 hours. It is excreted unchanged and in the form of metabolites with bile and urine.

In renal failure (end-stage) T_1/2 is 10-20 hours, in case of impaired liver function – 8-12 hours.

Indications

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

ICD codes

Dosage Regimen

Administer Linkomitsin Velpharm by intramuscular injection or slow intravenous infusion after dilution.

For adults, the typical single dose is 600 mg (2 ml). The standard daily dosage is 1.8 g, administered as three 600 mg injections at 8-hour intervals.

For severe infections, increase the daily dose to 2.4 g or more, administered in divided doses. For life-threatening conditions, doses up to 8 g per day have been used intravenously.

For children over one month of age, calculate the daily dose as 10-20 mg per kg of body weight. Divide the total daily dose into two or three equal administrations.

The standard treatment duration is 7 to 14 days. For osteomyelitis, continue therapy for a minimum of 3 weeks or longer based on clinical response.

For intramuscular administration, inject deeply into a large muscle mass. Do not exceed 2 ml (600 mg) per single intramuscular injection site.

For intravenous infusion, dilute each 1 ml (300 mg) in at least 50 ml of a compatible solution. Infuse the total dose over at least 60 minutes. Never administer intravenously as a bolus.

In patients with moderate hepatic or renal impairment, reduce the dose or increase the dosing interval. Monitor serum drug concentrations during high-dose therapy in these patients.

Adverse Reactions

From the digestive system nausea, vomiting, diarrhea, abdominal pain, anal itching, glossitis, stomatitis, jaundice, transient hyperbilirubinemia, increased activity of hepatic transaminases; with long-term use – gastrointestinal candidiasis, pseudomembranous colitis.

From the hematopoietic system: reversible leukopenia, thrombocytopenic purpura, neutropenia, agranulocytosis, aplastic anemia and pancytopenia.

Allergic reactions itching, urticaria, rash, exfoliative dermatitis, vesiculobullous dermatitis, angioneurotic edema, anaphylactic shock, multiforme erythema, Stevens-Johnson syndrome, serum sickness.

From the genitourinary system impaired renal function (azotemia, oliguria, proteinuria), vaginitis.

From the sense organs tinnitus, vertigo.

Local reactions with intravenous administration – thrombophlebitis, with intramuscular administration – local irritation, pain, formation of induration and sterile abscess at the injection site.

With rapid intravenous administration decreased blood pressure, dizziness, headache, drowsiness, general weakness, relaxation of skeletal muscles, respiratory arrest, cardiac arrest.

Contraindications

Hypersensitivity to lincomycin and clindamycin; severe hepatic and/or renal failure; pregnancy (except when necessary for vital indications), breastfeeding period; newborns (up to 1 month).

With caution

Fungal diseases of the skin, oral mucosa; vagina; myasthenia gravis; simultaneous use with drugs that block neuromuscular conduction; diabetes mellitus; moderate hepatic/renal failure; history of gastrointestinal diseases, especially colitis.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy (except when necessary for vital indications) and during breastfeeding.

Use in Hepatic Impairment

Contraindicated in severe hepatic insufficiency. It should be used with caution in patients with moderate hepatic insufficiency.

Use in Renal Impairment

Contraindicated in severe renal insufficiency. It should be used with caution in patients with moderate renal insufficiency.

Pediatric Use

Contraindicated in newborns (up to 1 month).

Geriatric Use

Pharmacokinetics in elderly individuals with normal liver and kidney function corresponds to the pharmacokinetics of adult patients.

Special Precautions

To avoid the development of aseptic necrosis, it is preferable to administer deep intramuscularly. It cannot be administered intravenously without prior dilution.

During long-term treatment, periodic monitoring of hepatic transaminase activity and renal function is necessary. If violations are detected, the possibility of drug withdrawal should be considered.

Prescription to patients with hepatic insufficiency is permissible only for vital indications.

The T_1/2 of lincomycin may be increased in patients with impaired liver and kidney function, so caution should be exercised when prescribing lincomycin to patients with moderate hepatic/renal insufficiency and the concentration of lincomycin in the blood should be monitored during therapy with high doses of lincomycin. In such patients, the possibility of reducing the frequency of drug administration should be considered.

Cases of pseudomembranous colitis developing 2 months after taking antibacterial drugs have been reported. If signs of pseudomembranous colitis appear, in mild cases it is sufficient to discontinue the drug and prescribe ion-exchange resins, in severe cases, compensation for the loss of fluid, electrolytes and protein, and the appointment of vancomycin or bacitracin are indicated. The use of drugs that inhibit intestinal peristalsis is contraindicated.

Lincomycin is not indicated for the therapy of meningitis, since its concentration in the cerebrospinal fluid is insufficient for the treatment of meningitis.

It is not recommended to use Lincomycin in patients with diabetes mellitus, except in cases where there is no alternative treatment, since there are no adequate data on the therapy of patients with endocrine or metabolic diseases.

When using lincomycin, especially long-term, the development of a secondary infection associated with the growth of microorganisms resistant to the drug (especially fungi) is possible, for the exclusion and confirmation of which a repeated assessment of the patient’s condition should be carried out. If a secondary infection occurs during therapy, the necessary measures for its treatment should be taken.

Lincomycin should be used with caution in patients with existing fungal diseases; such patients should also be prescribed antifungal therapy.

When using lincomycin, the development of severe bullous reactions, such as Stevens-Johnson syndrome, toxic epidermal necrolysis, has been reported. Patients should be informed that if skin reactions and/or damage to the mucous membranes develop, they should immediately consult a doctor before continuing treatment with lincomycin.

When using lincomycin, the development of hypersensitivity reactions and allergic reactions (anaphylactic shock and anaphylactoid reactions, which can progress to a life-threatening condition) has been reported. In these cases, the use of lincomycin should be discontinued and appropriate treatment should be started.

Lincomycin is characterized by neuromuscular blocking activity and may increase muscle weakness in patients with pseudoparalytic myasthenia gravis. The use of lincomycin in patients with an established diagnosis of pseudoparalytic myasthenia gravis is not recommended.

Cases of neutropenia and/or leukopenia during treatment with lincomycin have been reported, so periodic blood count monitoring is recommended during therapy.

Effect on the ability to drive vehicles and mechanisms

When using lincomycin, the possibility of dizziness and relaxation of skeletal muscles cannot be excluded, therefore driving vehicles and other activities requiring increased attention and speed of reactions are not recommended.

Drug Interactions

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

With simultaneous use with erythromycin, penicillins, cephalosporins, chloramphenicol, ampicillin and other bactericidal antibiotics, antagonism of antimicrobial action is possible.

With simultaneous use with aminoglycosides, a synergism of action is possible.

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

Antidiarrheal agents reduce the effect of lincomycin (the interval between their use should be at least 4 hours).

It enhances the effect of drugs for inhalation anesthesia, muscle relaxants and opioid analgesics, increasing the risk of neuromuscular blockade and respiratory arrest.

With simultaneous use of theophylline with lincomycin, inhibitors of cytochrome P450 isoenzymes, the effectiveness of theophylline may increase, which may require a reduction in its dose.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.