Chloramphenicol

Хлорамфеникол Constitutional formula

The description is actual on 11.06.2015

  • Latin name: Chloramphenicolum
  • ATH code: D06AX02, D06AX52, D10AF03, G01AA05, J01BA01
  • Chemical formula: C11H12Cl2N2O5
  • CAS code: 56-75-7

Chemical name

D-(−)-treo-1-(p-nitrophenyl) - a 2-dichlorine-acetylamino-1,3-pro-pan-diol

Chemical properties

Chloramphenicol – the brightest representative of group of antibiotics of an amfenikola. Antibacterial properties are most expressed at its left-handed isomer.

Substance represents bitter crystals without color and a smell. Means is badly dissolved in water, is well soluble in pyridine, propylene glycol, ethanol, ethylene glycol. It is used as an antibiotic of a broad spectrum of activity in animal husbandry, medicine, veterinary science. The racemic form of medicine is called synthomycin. A trade name of Chloramphenicol – Levomycetinum.

Substance in 40 years of the 20th century from Streptomyces venezuelae was for the first time synthesized. Now the antibiotic is received by 10-phasic synthesis from styrene. It is rather effective, however is toxic and quite often causes side reactions. The drugs containing this substance let out in the form of ointment, solution for intravenous and intramuscular administration, spirit solution, capsules or tablets.

Pharmacological action

Antibacterial, bacteriostatic.

Pharmacodynamics and pharmacokinetics

The mechanism of effect of this substance is based on its ability to break processes of protein synthesis of microorganisms by dioxo-peptidil-transferase enzyme inhibition. Chloramphenicol possesses bacteriostatic action, shows activity to stafilokkoka, streptococci, gram-negative bacteria (Neisseria gonorrhoeae, Escherichia coli, Salmonella spp., Rickettsia spp., Neisseria meningitidis, Haemophilus influenzae, Shigella spp., Serratia spp., Proteus spp.), to Spirochaetaceae and large viruses. Characteristic of an antibiotic is that it affects the strains steady against penicillin, streptocide and streptomycin. Tolerance to drug develops slowly.

After intake it is quickly acquired through a digestive tract, the maximum concentration is reached in 2-3 hours, by biological availability of means to 90%. About a half of substance contacts proteins of a blood plasma.

Chloramphenicol is exposed to reactions of a metabolism in a liver. Within 1,5-3 hours lek. means is removed through kidneys, with a stake and bile. Also substance is exposed to hydrolysis in intestines, forming inactive metabolites.

At local use or hit in a conjunctival sac means has low extent of system absorption.

However, the antibiotic creates sufficient concentration in moisture of an eye or on a skin surface to have bacteriostatic action.

Indications to use

In the form of tablets and capsules substance is used for treatment of a typhoid, a salmonellosis in a generalizirovanny form, a paratyphoid, a brucellosis, various rickettsioses, by tularemias, abscesses of a brain, dysentery, meningococcal infections.

Means is used at trachoma, clamidiosis, an erlikhioza, purulent wound fevers, peritonitis, various infections to urine - and zhelchevyvodyashchy ways, an inguinal lymphogranuloma, an iyersinioza.

For outside use medicine is appointed at infectious diseases of skin: burns, wounds, trophic ulcers, furuncles, decubituses, for treatment of cracks on nipples at the feeding mothers.

In a conjunctival sac drug is dug in for treatment of bacterial infections of eyes, a keratitis, conjunctivitis, a blepharitis, a sclerite, an episcleritis, a keratoconjunctivitis.

Contraindications

It is impossible to appoint drugs which part this substance is:

  • at blood diseases;
  • to children aged about one month;
  • to patients with diseases of a liver and deficit glyukozo-6-fosfatdegidrogenazy;
  • at psoriasis, fungal infections of skin and eczema;
  • to pregnant women and the feeding women;
  • at an allergy to Chloramphenicol or other antibiotics of this group.

Extra care needs to be observed at heart diseases and vessels, to patients, inclined to an allergy.

Side effects

Drug intake can cause:

Small children, aged till 12 months can have a cardiovascular collapse.

Application instruction of Chloramphenicol (Way and dosage)

Means is used intravenously, intramusculary, orally, locally, konjyunktivalno.

The scheme of treatment and duration depends on a disease and a dosage form, is defined in an individual order by the attending physician.

Application instruction of Chloramphenicol

Pill is taken in 30 minutes before meal or in an hour later.

At intramuscular, intravenous administration and intake by the adult appoint 2 grams of active ingredient a day divided into 3-4 receptions on 250-500 mg. The maximum daily dosage – 4 grams can be appointed by the attending physician. At the same time it is necessary to make control of indicators of blood and work of kidneys.

To children:

  • aged till 3 flyings appoint 10-15 mg to body weight kg;
  • aged from 3 till 8 flyings – on 15-20 mg on one kg of weight;
  • to children 8 years – 20-30 mg on kg are more senior.

Frequency rate of reception – same, as well as for adults.

Treatment duration an antibiotic usually makes from one week to 10 days. At most — 14 days.

At topical administration Chloramphenicol solution of 5% or 10% is applied on affected areas by means of gauze napkins several times a day. Medicine can be imposed with an occlusive bandage, in that case bandagings carry out time in 3-4 days (to hold no more than five days) until the wound begins to drag on and will be cleared.

Konjyunktivalno substance use in the form of 1% or 0,25% a ditch, in combination with other drugs.

Overdose

At overdose manifestation of a cardiovascular syndrome, especially at newborn children is the most probable.

Symptoms: decrease in body temperature, confused breath, cardiovascular insufficiency, lack of reactions to external irritants. The probability of development of a lethal outcome in children reaches 40%.

As treatment appoint hemosorption and eliminate undesirable symptoms.

Interaction

Use of medicine with clindamycin, erythromycin, lincomycin increases efficiency of both drugs.

At the Chloramphenicol combination to hypoglycemic means action of the last amplifies, concentration of hypoglycemic drugs in blood increases due to delay of their metabolism in liver tissues.

The combined drug intake, oppressing activity of marrow, and this antibiotic leads to strengthening of effect of the drugs influencing marrow.

Medicine reduces efficiency of antibiotics of a number of penicillin.

The drug combination to phenobarbital, warfarin and Phenytoinum leads to delay of a metabolism of both means and increase in time of their removal from an organism.

Terms of sale

According to the recipe.

Storage conditions

Depending on a dosage form various storage conditions are required for drug. As a rule, means is stored in the place dry, cool, unavailable to small children.

Period of validity

Spirit solution is stored 1 year.

2 years – drops for eyes and spray for topical administration.

5 years – tablets and capsules.

Special instructions

At treatment of the patients who are earlier passing radiation therapy or a course of tsitostatik it is necessary to be careful.

To children

When using this substance in pediatric practice it is also necessary to be careful. Medicine is appointed to children of one month, the dosing mode – according to the recommendations described above.

If the course of treatment more than one week, then is recommended to make systematic control of a peripheral picture of blood.

Coincidence on the ATH code of the 4th level:

Chloramphenicol synonyms: Laevovinisolum, Levomycetinum, sodium Levomycetinum succinate, Spirit solution of Levomycetinum, Levomitsetin-AKOS, sodium Chloramphenicol succinate sterile, Levomitsetin-Lekt, Levomycetinum Aktitab, sodium Levomycetinum succinate, Synthomycin.

Also there are analogs of means containing additional active ingredients: Levomekol, Levometil (Dioksometiltetragidropirimidin + Chloramphenicol); Levosin (Dioksometiltetragidropirimidin + Sulfadimethoxine + Trimecainum + Chloramphenicol).

Responses

Despite a high probability of development of side reaction and toxicity of the drugs containing this component use it quite often. Much like the low cost of means and a variety of dosage forms. The antibiotic is used most often locally in order that will get rid of an enanthesis and an acne. In general drug has good reputation.

The Chloramphenicol price where to buy

The cost of the tablets Levomycetinum, 500 mg makes about 30 rubles for 10 pieces.

The price of spirit solution of Levomycetinum for external use, 3% — about 65 rubles for a bottle, with a capacity of 25 ml.

Section: Active ingredients
PAY ATTENTION! Information on active ingredients on the website is help generalizing, collected from public sources and can form the basis for making decision on use of these substances it is not aware of treatment. Before substance Chloramphenicol use surely consult with the attending physician.