Levomycetin Actitab (Tablets) Instructions for Use

Marketing Authorization Holder

Aliym, JSC (Russia)

ATC Code

J01BA01 (Chloramphenicol)

Active Substance

Chloramphenicol (Rec.INN WHO registered)

Dosage Forms

	Levomycetin Actitab	Film-coated tablets, 250 mg: 10, 12, 15, 20, 24, 30, 36, 40, 45, 48, 50, 60, 72, 75 or 90 pcs.
		Film-coated tablets, 500 mg: 10, 12, 15, 20, 24, 30, 36, 40, 45, 48, 50, 60, 72, 75 or 90 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets light blue in color, biconvex, oblong in shape with rounded ends, with a score; on the cross-section, the core is white or white with a yellowish tint.

Excipients: microcrystalline cellulose, copovidone (Kollidon VA-64), colloidal silicon dioxide (Aerosil), povidone, crospovidone, calcium stearate.

Shell composition ready-made mixture for film coating [polyvinyl alcohol, macrogol, talc, titanium dioxide, aluminum lake based on indigo carmine dye, yellow iron oxide dye].

10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (4) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
12 pcs. – contour cell packaging (1) – cardboard packs.
12 pcs. – contour cell packaging (2) – cardboard packs.
12 pcs. – contour cell packaging (3) – cardboard packs.
12 pcs. – contour cell packaging (4) – cardboard packs.
12 pcs. – contour cell packaging (5) – cardboard packs.
12 pcs. – contour cell packaging (6) – cardboard packs.
15 pcs. – contour cell packaging (1) – cardboard packs.
15 pcs. – contour cell packaging (2) – cardboard packs.
15 pcs. – contour cell packaging (3) – cardboard packs.
15 pcs. – contour cell packaging (4) – cardboard packs.
15 pcs. – contour cell packaging (5) – cardboard packs.
15 pcs. – contour cell packaging (6) – cardboard packs.

Film-coated tablets light blue in color, biconvex, oblong in shape with rounded ends, with a score; on the cross-section, the core is white or white with a yellowish tint.

Excipients: microcrystalline cellulose, copovidone (Kollidon VA-64), colloidal silicon dioxide (Aerosil), povidone, crospovidone, calcium stearate.

Shell composition ready-made mixture for film coating [polyvinyl alcohol, macrogol, talc, titanium dioxide, aluminum lake based on indigo carmine dye, yellow iron oxide dye].

10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (4) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
12 pcs. – contour cell packaging (1) – cardboard packs.
12 pcs. – contour cell packaging (2) – cardboard packs.
12 pcs. – contour cell packaging (3) – cardboard packs.
12 pcs. – contour cell packaging (4) – cardboard packs.
12 pcs. – contour cell packaging (5) – cardboard packs.
12 pcs. – contour cell packaging (6) – cardboard packs.
15 pcs. – contour cell packaging (1) – cardboard packs.
15 pcs. – contour cell packaging (2) – cardboard packs.
15 pcs. – contour cell packaging (3) – cardboard packs.
15 pcs. – contour cell packaging (4) – cardboard packs.
15 pcs. – contour cell packaging (5) – cardboard packs.
15 pcs. – contour cell packaging (6) – cardboard packs.

Clinical-Pharmacological Group

Antibiotic of the chloramphenicol group

Pharmacotherapeutic Group

Systemic antibacterial agents; amphenicols

Pharmacological Action

A broad-spectrum bacteriostatic antibiotic, it disrupts the process of protein synthesis in the microbial cell at the stage of amino acid transfer by tRNA to ribosomes.

It is effective against strains of bacteria resistant to penicillin, tetracyclines, and sulfonamides.

It is active against the following microorganisms: Escherichia coli, Shigella dysenteriae, Shigella flexneri, Shigella boydii, Shigella sonnei, Salmonella spp. (including Salmonella typhi, Salmonella paratyphi), Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae), Neisseria meningitidis, Neisseria gonorrhoeae, a number of Proteus spp. strains, Burkholderia pseudomallei, Rickettsia spp., Treponema spp., Leptospira spp., Chlamydia spp. (including Chlamydia trachomatis), Coxiella burnetii, Ehrlichia canis, Klebsiella pneumoniae, Haemophilus influenzae.

It does not act on acid-fast bacteria (including Mycobacterium tuberculosis), anaerobes, methicillin-resistant strains of staphylococci, Acinetobacter spp., Enterobacter spp., Serratia marcescens, indole-positive strains of Proteus spp., Pseudomonas aeruginosa, protozoa, and fungi. Microbial resistance develops slowly.

Pharmacokinetics

After oral administration, plasma protein binding is 50-60%. T_max after administration is 1-3 hours. V_d is 0.6-1.0 L/kg. Therapeutic concentration in the blood is maintained for 4-5 hours after administration. It penetrates well into body fluids and tissues. The highest concentrations are achieved in the liver and kidneys. Up to 30% of the administered dose is found in bile. C_max in the cerebrospinal fluid is reached 4-5 hours after a single dose and can reach 21-50% of the plasma C_max in the absence of meningeal inflammation and 45-89% in the presence of meningeal inflammation. It crosses the placental barrier; concentrations in the fetal serum can be 30-80% of that in the maternal blood. It penetrates into breast milk. The main amount (90%) is metabolized in the liver. In the intestine, under the influence of intestinal bacteria, it is hydrolyzed to form inactive metabolites.

It is eliminated within 24 hours by the kidneys – 90% (via glomerular filtration – 5-10% unchanged, via tubular secretion as inactive metabolites – 80%), through the intestine – 1-3%. T_1/2 in adults is 1.5-3.5 hours, in case of impaired renal function – 3-11 hours. T_1/2 in children is 3.0-6.5 hours. It is poorly removed during hemodialysis.

Indications

• Infections of the urinary and biliary tracts caused by susceptible microorganisms.

ICD codes

Dosage Regimen

Orally (30 minutes before meals, and if nausea and vomiting develop – 1 hour after meals), 3-4 times/day. A single dose for adults is 0.25-0.5 g, the daily dose is 2 g. In severe forms of infections (in a hospital setting), it is possible to increase the dose to 3-4 g/day (under the control of blood condition, renal and liver function). Children over 3 years of age and/or with a body weight over 20 kg are prescribed 12.5 mg/kg every 6 hours or 25 mg every 12 hours; in severe infections – up to 75-100 mg/kg/day (under the control of the drug concentration in the blood serum). The average duration of treatment is 8-10 days.

Adverse Reactions

From the digestive system: dyspepsia, nausea, vomiting (the likelihood of development is reduced when taken 1 hour after meals), diarrhea, irritation of the oral mucosa and pharynx, dermatitis, dysbacteriosis (suppression of normal microflora).

From the hematopoietic organs: reticulocytopenia, leukopenia, granulocytopenia, thrombocytopenia, erythrocytopenia; rarely – aplastic anemia, agranulocytosis.

From the nervous system: psychomotor disorders, depression, confusion, peripheral neuritis, optic neuritis, visual and auditory hallucinations, decreased visual acuity and hearing, headache.

Allergic reactions: skin rash, angioedema.

Other: secondary fungal infection.

Contraindications

• Hypersensitivity;
• Suppression of bone marrow hematopoiesis;
• Acute intermittent porphyria;
• Glucose-6-phosphate dehydrogenase deficiency;
• Hepatic and/or renal failure;
• Skin diseases (psoriasis, eczema, fungal infections);
• Pregnancy;
• Lactation period;
• Children under 3 years of age and/or body weight less than 20 kg.

Use with caution in patients who have previously received treatment with cytotoxic drugs or radiation therapy.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Use in Hepatic Impairment

Contraindicated in hepatic failure.

Use in Renal Impairment

Contraindicated in renal failure.

Pediatric Use

Contraindicated in children under 3 years of age, as well as in children with a body weight of less than 20 kg.

Special Precautions

Severe complications from the hematopoietic system are usually associated with the use of high doses for a long time.

When taken simultaneously with ethanol, a disulfiram-like reaction may develop (facial flushing, abdominal and stomach cramps, nausea, vomiting, headache, decreased blood pressure, tachycardia, shortness of breath).

Overdose

Symptoms: nausea, vomiting.

Treatment: gastric lavage, symptomatic therapy, hemoperfusion.

Drug Interactions

It inhibits liver microsomal enzymes, so when used simultaneously with phenobarbital, phenytoin, and indirect anticoagulants, a decrease in the metabolism of these drugs, a slowdown in their elimination, and an increase in their plasma concentration are noted.

It reduces the antibacterial effect of penicillins and cephalosporins. When used simultaneously with erythromycin, clindamycin, lincomycin, a mutual weakening of the effect is noted due to the fact that Chloramphenicol can displace these drugs from the bound state or prevent their binding to the 50S subunit of bacterial ribosomes. Simultaneous administration with drugs that suppress hematopoiesis (sulfonamides, cytostatics), affect liver metabolism, or with radiation therapy increases the risk of side effects. When prescribed with oral hypoglycemic drugs, an enhancement of their effect is noted (due to suppression of metabolism in the liver and an increase in their plasma concentration).

Myelotoxic drugs enhance the manifestations of the hematotoxicity of the drug.

Storage Conditions

List B. Store out of the reach of children, in a dry place, protected from light, at a temperature not exceeding 25°C (77°F).

Dispensing Status

By prescription

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.