Lincolid Velpharm (Solution) Instructions for Use

Marketing Authorization Holder

Bright Way, LLC (Russia)

Manufactured By

Velpharm, LLC (Russia)

ATC Code

J01FF02 (Lincomycin)

Active Substance

Lincomycin (Rec.INN registered by WHO)

Dosage Form

Lincolid Velpharm

Solution for infusion and intramuscular administration 300 mg/ml

Dosage Form, Packaging, and Composition

Solution for infusion and intramuscular administration

1 ml – ampoules (10 pcs.) – cardboard packs – Prescription only
1 ml – ampoules (5 pcs.) – cardboard packs – Prescription only
2 ml – ampoules (10 pcs.) – cardboard packs – Prescription only
2 ml – ampoules (5 pcs.) – cardboard packs – Prescription only

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 exerts a bactericidal effect. It suppresses bacterial protein synthesis by reversibly 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 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 IM injection of 600 mg, C_max in blood plasma is reached after 30 minutes. After a 120-minute IV 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 as metabolites with bile and urine.

In renal failure (end-stage), T_1/2 is 10-20 hours; in liver function impairment – 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 intramuscularly or intravenously.

For adults, the single dose is 0.6 g (600 mg). The daily dose is 1.8 g (1800 mg), typically divided into three administrations.

For children, the daily dose is 10-20 mg/kg body weight. Divide the total daily dose into two or three equal administrations.

For intravenous infusion, dilute the required dose in a sufficient volume of a compatible solution, such as 0.9% Sodium Chloride or 5% Dextrose. Infuse over a period of at least 60-120 minutes.

For intramuscular injection, administer deeply into a large muscle mass to minimize local irritation and the risk of sterile abscess formation.

The standard treatment duration is 7 to 14 days, depending on the infection’s severity and clinical response.

For osteomyelitis, continue treatment for a minimum of 3 weeks or longer as clinically indicated.

In patients with moderate hepatic or renal impairment, consider reducing the frequency of administration. Monitor serum drug concentrations during high-dose therapy in these patients.

Do not administer intravenous bolus. Avoid rapid intravenous infusion due to the risk of severe hypotension and cardiopulmonary arrest.

Adverse Reactions

From the digestive system nausea, vomiting, diarrhea, abdominal pain, anal itching, glossitis, stomatitis, jaundice, transient hyperbilirubinemia, increased activity of hepatic transaminases; with prolonged 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 sensory organs tinnitus, vertigo.

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

With rapid IV 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. Should be used with caution in patients with moderate hepatic insufficiency.

Use in Renal Impairment

Contraindicated in severe renal insufficiency. 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 IM. It cannot be administered IV without prior dilution.

During long-term treatment, periodic monitoring of hepatic transaminase activity and renal function is necessary. If abnormalities are detected, the possibility of discontinuing the drug 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, discontinuation of the drug and prescription of ion-exchange resins are sufficient; in severe cases, replacement of fluid, electrolyte and protein loss, prescription of vancomycin or bacitracin is 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, 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 mucosal lesions 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 life-threatening conditions) has been reported. In these cases, the use of lincomycin should be discontinued and appropriate treatment initiated.

Lincomycin is characterized by neuromuscular blocking activity and may enhance 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 synergistic effect is possible.

In 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.