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|Chloromycetin 500 mg|
270 pills - 500 mg
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|Chloromycetin 250 mg|
270 pills - 250 mg
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Pharmaucetical actions of Chloromycetin
Chloramphenicol inhibits the enzyme peptidyltransferase, which leads to disruption of protein formation in the cell of the microorganism. After oral administration in the gastrointestinal tract, it is absorbed quickly, bioavailability is 75 - 90%, the maximum concentration in blood plasma is reached within 2 - 3 hours, the therapeutic concentration remains for 4–5 hours. It binds to plasma proteins by 50 - 60%. Chloramphenicol penetrates into body fluids and organs, through the placental and blood-brain barrier, is excreted in breast milk. In the cerebrospinal fluid, the content of chloramphenicol is 2 times less than in plasma. Most of the drug is biotransformed in the liver; the resulting metabolites, as well as approximately 10% of the unchanged drug, are excreted by the kidneys, and chloramphenicol is also partially excreted in feces and bile. In the intestine, chloramphenicol is hydrolyzed by intestinal bacteria to form inactive metabolites. When instilled into the conjunctival sac, chloramphenicol in the aqueous humor of the eye creates sufficient antibacterial concentrations, and also partially enters the systemic circulation. Chloramphenicol is active against most gram-negative cocci (meningococci and gonococci), gram-positive cocci (streptococci, staphylococci, enterococci, pneumococci), bacteria (hemophilic and Escherichia coli, Shigella, Salmonella, Klebsiella, Yersketea), Serration, Serration, some large viruses (causative agents of psittacosis, trachoma, inguinal lymphogranulomatosis and others); acts on strains that are resistant to penicillin, sulfonamides, streptomycin. Chloramphenicol is weakly active against Pseudomonas aeruginosa, acid-fast bacteria, protozoa and clostridia. The resistance of microorganisms to chloramphenicol develops relatively slowly. Since chloramphenicol has serious side effects, it is used when other chemotherapeutic agents are ineffective.
For systemic use (oral and parenteral): paratyphoid fever, typhoid fever, salmonellosis (generalized forms), rickettsioses (including Rocky Mountain spotted fever, typhus, Q fever), brucellosis, tularemia, brain abscess, dysentery, meningococcal infection lymphogranuloma, trachoma, chlamydia, ehrlichiosis, yersiniosis, urinary tract infections, purulent peritonitis, purulent wound infection, biliary tract infections. Eye liniment, eye drops: bacterial eye infections, including keratitis, conjunctivitis, keratoconjunctivitis, episcleritis, blepharitis, scleritis. For external use: bacterial skin infections, including boils, trophic ulcers, infected burns, wounds, bedsores, cracked nipples in nursing mothers.
Dosage of Chloromycetin
Chloramphenicol is taken orally, administered intravenously, intramuscularly, used conjunctivally, cutaneous. The dosage regimen is set individually. Inside take 0.5 hours before meals (with nausea and vomiting, take 1 hour after meals). For adults, a single dose is 0.25 - 0.5 g; the daily dose is 2.0 g (in very severe cases, an increase up to 4 g is possible, under the strict supervision of a physician and control of renal function and the state of the blood picture). The daily dose must be divided into 3 - 4 doses. For children under 3 years old, a single dose is 10 - 15 mg / kg of body weight, 3 - 8 years old - 0.15 - 0.2 g each, over 8 years old - 0.2 - 0.3 g each; take 3-4 times a day. The duration of therapy is 7-10 days (subject to good tolerance and indications, it is possible to use up to 14 days). Conjunctivally administered in the treatment of purulent-inflammatory pathology of the eyes and use a 0.25% aqueous solution or 1% liniment. Skin, topically: 5-10% liniment and alcohol solutions are applied several times a day to damaged skin areas (soaked in sterile gauze wipes or applied directly to the skin); use with an occlusive dressing is possible; dressings are carried out after 1 - 3 days (perhaps less often - after 4 - 5 days) until the wound is completely cleansed.
During chloramphenicol therapy, regular monitoring of the peripheral blood picture is necessary. When treating cracked nipples in nursing mothers, it is not necessary to stop breastfeeding the newborn.
Hypersensitivity, acute intermittent porphyria, pathology of the hematopoietic organs, fungal diseases of the skin, severe disorders of the functional state of the liver and / or kidneys, psoriasis, deficiency of glucose-6-phosphate dehydrogenase, eczema, neonatal period (up to 4 weeks) and early childhood.
Ristomycin enhances the hematotoxicity of chloramphenicol, cycloserine - the neurotoxicity of chloramphenicol. Phenobarbital accelerates biotransformation, reduces the concentration and duration of the effect of chloramphenicol. Chloramphenicol inhibits the metabolism of chlorpropamide, tolbutamide, oxycoumarin derivatives (increases anticoagulant and hypoglycemic properties). Erythromycin, nystatin, levorin, oleandomycin increase the antibacterial activity of chloramphenicol, benzylpenicillin salts reduce it. Chloramphenicol is incompatible with sulfonamides, cytostatics, pyrazolone derivatives, barbiturates, diphenin, alcohol.
Restrictions on the use
Propensity to allergic diseases, pathology of the circulatory system.
Application during pregnancy and lactation
During pregnancy, it is possible to use chloramphenicol if the expected effects of treatment are higher than the possible risk to the fetus (there are no strictly controlled and adequate studies on the use of chloramphenicol during pregnancy, it should be borne in mind that chloramphenicol is able to cross the placenta). After oral administration, chloramphenicol passes into breast milk and can cause serious side effects in breastfed babies. With local use, systemic absorption of the drug is possible. Therefore, breastfeeding women need to stop either using the drug or breastfeeding.
In case of an overdose of chloramphenicol, cardiovascular syndrome ("gray syndrome") develops in newborns and premature infants during high-dose therapy (due to the accumulation of the drug, which is caused by the immaturity of liver enzymes, as well as the direct toxic effect of the drug on the myocardium), which manifests itself in a bluish-gray color skin, hypothermia, lack of reactions, arrhythmic breathing, cardiovascular failure, death is possible (up to 40%). Required: symptomatic treatment, hemosorption.
Systemic effects: digestive system: nausea, dyspepsia, vomiting, irritation of the mucous membrane of the pharynx and mouth, diarrhea, dysbiosis;
blood (hemostasis, hematopoiesis): leukopenia, reticulocytopenia, thrombocytopenia, hypoglobinemia, aplastic anemia, agranulocytosis;
sense organs and nervous system: psychomotor disorders, delirium, headache, impaired consciousness, depression, optic neuritis, taste disturbances, auditory and visual hallucinations, decreased visual acuity and hearing;
allergic reactions: urticaria, skin rash, angioedema;
others: secondary fungal infection, dermatitis, cardiovascular collapse (in children under 1 year of age).
When applied conjunctivally and applied to the skin: local allergic reactions.