Chloramphenicol: instructions for using the medicine, structure, Contraindications

Title: Chloramphenicol (Laevomycetinum)

Active substance: Chloramphenicol

When ATH: J01BA01

Chloramphenicol: structure

1 Levomycetin tablet 250 It contains:
Chloramphenicol - 250 mg;
Excipients.

1 Levomycetin tablet 500 It contains:
Chloramphenicol - 500 mg;
Excipients.

1 vial of powder for solution for injection contains:
Chloramphenicol (in the form of chloramphenicol succinate sodium salt) – 500 or 1000 mg.

Chloramphenicol: pharmachologic effect

Levomycetin is an antimicrobial drug effective against a wide range of gram-positive and gram-negative microorganisms.. Has a pronounced bacteriostatic effect, in high concentrations against some strains exhibits a bactericidal effect. The mechanism of action is based on the ability to bind to the 50S subunit of bacterial ribosomes and inhibit protein synthesis in bacterial cells..
Strains of Escherichia coli are sensitive to the action of Levomycetin., Shigella spp. (including Shigella dysenteria), Salmonella spp., Streptococcus spp. (including Streptococcus pneumoniae), Neisseria spp., Proteus spp., Ricketsia spp., Treponema spp. and Chlamydia trachomatis. Besides, the drug is effective in diseases caused by certain strains of Pseudomonas aeruginosa.
The action of the drug does not apply to fungi, protozoa and strains of Mycobacterium tuberculosis.
The resistance of microorganisms to chloramphenicol develops slowly.

After oral administration, the drug is rapidly absorbed in the gastrointestinal tract. Bioavailability after oral administration reaches 80%. Peak plasma concentrations occur after 1-3 hours after admission. After oral administration, therapeutically significant concentrations remain in the blood plasma for 4-6 hours, after parenteral administration - during 8-12 hours. The degree of connection of chlorpheniramine with plasma proteins is about 50%. Levomycetin penetrates the hematoplacental and blood-brain barrier, excreted in breast milk. It is metabolized in the liver, excreted mainly by the kidneys, some of the drug is excreted by the intestines. The half-life reaches 1,5-3,5 hours.
In patients with impaired renal function, the half-life is increased to 3-4 hours, in patients with impaired liver function 11 hours.

Chloramphenicol: Indications for use

Used to treat patients with infectious diseases, caused by microorganisms sensitive to the action of chloramphenicol. The drug is prescribed in case of ineffectiveness or impossibility of using other antimicrobial agents in such diseases.:
Infectious diseases of the respiratory tract: pneumonia, lung abscess.
Infectious diseases of the abdominal organs: typhoid fever, paratif, shigellosis, salmonellosis, peritonitis.
Besides, the drug is prescribed to patients with meningitis, chlamydia, trachoma and tularemia.

Chloramphenicol: mode of application

Levomycetin tablets, application:

The drug is intended for oral use. Levomycetin tablet should be swallowed whole, without chewing or crushing, drinking plenty of fluids. It is recommended to take 30 minutes before meals. Patients, in whom this drug causes nausea, the tablet should be taken after 60 minutes after eating. The drug should be taken at regular intervals. The duration of the course of treatment and dose is determined by the attending physician individually for each patient..
Adults are usually given 250-500 mg 3-4 once a day.
Adults with severe infectious diseases are usually prescribed for 500-1000 mg 3-4 once a day. The use of Levomycetin in a dose 1000 mg 4 times a day is possible only in a hospital with constant monitoring of liver function, kidney and blood pictures.
The maximum daily dose for adults – 4000 mg.
Children aged 3 to 8 years are usually assigned according to 125 mg 3-4 once a day.
Children and adolescents aged from 8 to 16 years are usually assigned according to 250 mg Chloramphenicol 3-4 once a day.
The duration of treatment is usually 1-1,5 of the week. With good tolerability of the drug and the absence of side effects from the hematopoietic system, the duration of the course of treatment can be increased to 2 weeks.

Chloromycetin powder for solution for injection:

The solution is intended for parenteral (intramuscular and intravenous) introduction. Children are prescribed only intramuscular injection. To prepare a solution for intramuscular injection, the contents of the vial are dissolved in 2-3 ml water for injection or 2-3 ml 0,25% or 0,5% Novocaine. The solution should be injected deep into the outer upper quadrant of the gluteal muscle. To prepare a solution for intravenous jet administration, the contents of the vial are dissolved in 10 ml of water for injection or in 10 ml 5% or 40% glucose solution. The duration of an intravenous jet injection should be at least 3 minutes. Patients, suffering from diabetes mellitus for intravenous jet administration, the contents of the vial are dissolved in 10 ml water for injection or 10 ml 0,9% sodium chloride solution. Injections should be given at regular intervals. The duration of the course of treatment and the dose of the drug is determined by the attending physician individually for each patient..
Adults are usually given 500-1000 mg 2-3 once a day.
Adults with severe infectious diseases are usually prescribed for 1000-2000 mg 2-3 once a day.
The maximum daily dose is 4000 mg.
Children and adolescents aged from 3 to 16 years, the drug is usually prescribed at a dose 25 mg / kg body weight 2 once a day.
In ophthalmic practice, the finished solution can be used for parabulbar injections or instillations.. Water for injection may be used as a solvent 0,9% sodium chloride solution.
In the form of injections administered 0,2-0,3 ml 20% solution 1-2 once a day.
In the form of instillations, they are instilled into the conjunctival sac along 1-2 drops 5% solution formulation 3-5 once a day.
Duration of treatment 5-15 days.

With parenteral and oral administration of Levomycetin, the blood picture should be regularly monitored., as well as liver and kidney function.

Chloramphenicol: side effects

When using Levomycetin in patients, the development of such side effects was noted:
From the gastrointestinal tract and liver: nausea, vomiting, indigestion, violation of the chair, stomatitis, glossitis, violation of the intestinal microflora, enterocolitis. With prolonged use of the drug, patients may develop pseudomembranous colitis., requiring discontinuation of the drug. At high doses, hepatotoxicity may develop..
From the side of the cardiovascular system and the hematopoietic system: granulocytopenia, pancytopenia, erythropenia, anemia, including aplastic, agranulocytosis, thrombocytopenia, leukopenia, change in blood pressure, collapse.

Part of the central and peripheral nervous system: headache, dizziness, emotional lability, encephalopathy, confusion, fatigue, hallucinations, visual impairment, hearing and taste.
Allergic reactions: skin rash, itch, hives, dermatosis, angioedema.
Other: cardiovascular collapse, fever, superimposed infection, dermatitis, Jarisch-Herxheimer.

Chloramphenicol: Contraindications

Individual hypersensitivity to the drug, as well as thiamphenicol and azidamphenicol.
Levomycetin is contraindicated in patients, suffering from hematopoietic dysfunction, severe liver and/or kidney disease and deficiency of glucose-6-phosphate dehydrogenase.
The drug is not prescribed to patients with fungal skin diseases, psoriasis, eczema, porphyria, as well as acute respiratory diseases, including angina..
The drug is not used to prevent infectious complications during surgical interventions..

Levomycetin should not be prescribed for the treatment of women during pregnancy and breastfeeding., as well as for the treatment of children under the age of 3 years.
Use with caution in elderly patients, as well as patients with diseases of the cardiovascular system.
Patients, those with a tendency to develop allergic reactions should take the drug under the close supervision of the attending physician.
Caution should be exercised when prescribing Levomycetin to patients, whose work is related to the management of potentially dangerous mechanisms and driving a car.

Levomycetin and pregnancy

Levomycetin is contraindicated during pregnancy.
If it is necessary to use during lactation, you should consult with your doctor and decide on the interruption of breastfeeding..

Chloramphenicol: drug interaction

With prolonged use, in patients in the period before surgery or during surgery, it is possible to increase the duration of the therapeutic effect of alfetanil.
The combined use of Levomycetin with cytostatic agents is contraindicated, sulьfanilamidami, ristomycin, cimetidine and radiotherapy, since their combined use leads to inhibition of the function of the hematopoietic system.
The drug, with simultaneous use, enhances the effectiveness of oral hypoglycemic agents..
When combined with phenobarbital, rifampicin and rifabutin decrease in plasma concentrations of chloramphenicol.
Paracetamol with combined use increases the half-life of levomycetin.

With combined use, Levomycetin reduces the effectiveness of oral contraceptives, containing estrogens, iron supplementation, folic acid and cyanocobalamin.
The drug changes the pharmacokinetics of phenytoin, cyclosporine, цiklofosfamida, tacrolimus, and drugs, whose metabolism occurs with the participation of the cytochrome P450 system. If necessary, the combined use of these drugs with chloramphenicol should adjust their doses..
There is a mutual decrease in effectiveness with the combined use of chloramphenicol with penicillin., cephalosporins, klindamiцinom, Erythromycin, levorin and nystatin.
When using the drug in combination with ethyl alcohol, patients develop a disulfiram-like reaction..
There is an increase in the neurotoxicity of Levomycetin with simultaneous use with cycloserine.

Chloramphenicol: overdose

When using excessive doses of Levomycetin, patients develop hematopoietic disorders, accompanied by pale skin, sore throat, fever, weakness, increased fatigue internal bleeding and bruising. In patients with hypersensitivity and children, when using high doses of the drug, abdominal distention may develop., nausea, vomiting, dullness of the skin, cardiovascular collapse, as well as respiratory distress with metabolic acidosis. Besides, high doses of chloramphenicol can cause visual and hearing impairment, slowing down psychomotor reactions and hallucinations.
With an overdose, drug withdrawal is indicated.. When using excessive doses of the drug in the form of tablets, gastric lavage and the use of enterosorbents are indicated.. In case of overdose, symptomatic therapy is also carried out..

Chloramphenicol: release form

The tablets of 10 pieces in blisters, by 1 or 2 blisters in a cardboard box.
Powder for solution for injection 0,5 or 1 g in vial. By 1 or 10 bottles in a carton.

Chloramphenicol: storage conditions

Levomycetin is recommended to be stored in a dry place away from direct sunlight at a temperature not exceeding 25 degrees Celsius.
Shelf-life of the drug in the form of powder for solution for injection - 4 year;
The shelf life of the drug in the form of tablets - 3 year.
The shelf life of the finished water 5% solution for use in ophthalmology - 2 day.

Synonyms of chloramphenicol

Chloramphenicol, Chloroid, Alficetin, Berlicetin, Biophenicol, Hemicetin, Chlornithromycin, Chlorocycline, Chloromycetin, Chloronitrin, Chloroptic, Clobinecol, Detreomycin, Halomycetin, Leukomiin, Paraxin, Syntomycetin, Typhomycetin, Typhoid fever.
See also the list of analogues of the drug Levomycetin.

Pharmacological group of chloramphenicol

• Antimicrobial and antiparasitic agents
• Antibiotics
• Levomycetins

Chloramphenicol: Nosological classification (ICD-10)

Typhoid and paratyphoid (A01)
Other salmonella infections (A02)
Shigelez (A03)
Brucellosis (A23)
Trachoma (A71)
Pertussis (A37)
Meningococcal infection (A39)
Streptococcal septicemia (A40)
Other septicemia (A41)
Typhus (A75)
Bacterial pneumonia, not elsewhere classified (J15)
Abscess of the lung and mediastinum (J85)
Bacterial meningitis, not elsewhere classified (G00)
Varicose veins of the lower extremities with ulcers and inflammation (I83.2)
Impetigo (L01)
Skin Abscess, furuncle and carbuncle (L02)
Phlegmon (L03)
Pyoderma (L08.0)
Osteomyelitis (M86)
Thermal and chemical burns of unspecified localization (T30)

Manufacturer: Borshchahiv Chemical and Pharmaceutical Plant