The active substance of Levomycetin in all its forms is chloramphenicol - a substance that belongs to the group of antibiotics amphenicols .
Drops in the eyes contain chloramphenicol at a concentration of 2.5 mg/ml.
Possible dosages of the active substance for capsules And tablets- 250 and 500 mg, for extended-release tablets - 650 mg (tablets have 2 layers - the outer contains 250, the inner - 400 mg ).
Levomycetin alcohol solution Available in a concentration of 0.25; 1, 3 and 5%. Levomycetin ointment can have a concentration of 1 or 5%.
Drugs from different manufacturers have different compositions of auxiliary components.
All versions of the same product produced by pharmaceutical companies in post-Soviet countries differ slightly, since they use the same technology for producing chloramphenicol. Thus, Levomycetin DIA eye drops do not differ from the drops produced, for example, by the Belmedpreparaty company.
Release form
- eye drops 0.25%(ATC code S01AA01);
- liniment 1%, 5%;
- alcohol solution 1%, 3%, 5% and 0.25% (ATC code D06AX02);
- pills And capsules 250 and 500 mg, extended-release tablets 650 mg (ATC code J01BA01).
pharmachologic effect
Antibacterial. The drug stops inflammation and cures infections of any tissues and organs, provided that they are caused by sensitive to chloramphenicol microflora.
Pharmacodynamics and pharmacokinetics
Levomycetin is antibiotic or not? An antibiotic of synthetic origin, which is identical to the product produced by the microorganisms Streptomyces venezuelae during their life.
Chloramphenicol destructive for most gram (+) and gram (-) bacteria (including strains that are resistant to the action of And ), spirochete , rickettsia , individual large viruses.
Shows low activity against Clostridium, Pseudomonas aeruginosa, acid-fast bacteria and protozoa.
The mechanism of action of the drug is related to the ability chloramphenicol disrupt the synthesis of proteins of microorganisms. The substance blocks the polymerization of activated amino acid residues that are associated with m-RNA.
Resistance to chloramphenicol in microbes it develops relatively slowly; cross-resistance to other chemotherapeutic drugs, as a rule, does not occur.
When applied topically, the required concentration is created in the aqueous humor, vitreous fibers, cornea and iris. The drug does not penetrate the lens.
Pharmacokinetic parameters when taken chloramphenicol inside:
- absorption - 90%;
- bioavailability - 80%;
- degree of binding to plasma proteins - 50-60% (in prematurely born
- term infants - 32%);
- Tmax - from 1 to 3 hours.
Therapeutic concentration in the bloodstream remains for 4-5 hours after oral administration. About a third of the dose taken is found in bile; the highest concentration of Levomycetin is created in the kidneys and liver.
The drug is able to cross the placental barrier, its serum concentration in the fetus can reach 30-80% of the serum concentration in the mother. Penetrates into milk.
Biotransformed mainly in the liver (90%). Under the influence of normal intestinal flora, it undergoes hydrolysis with the formation of inactive metabolites.
Elimination time is 24 hours. It is excreted mainly by the kidneys (90%). From 1 to 3% is excreted with the intestinal contents. T1/2 for an adult - from 1.5 to 3.5 hours, in children 1-16 years old - from 3 to 6.5 hours, in children 1-2 days after birth - 24 hours or more (with low weight longer body), on days 10-16 of life - 10 hours.
Patients who have previously received cytostatic drugs or passing , pregnant women, young children (especially the first 4 weeks of life) the medicine is prescribed for health reasons.
Side effects
Systemic side effects of Levomycetin:
- disorders of the digestive system - nausea, , dyspepsia, vomiting, irritation of the pharynx and oral mucosa, dysbacteriosis;
- disorders of hemostasis and hematopoiesis - reticulocytopenia, leukemia and thrombocytopenia, agranulocytosis, hypohemoglobinemia, aplastic anemia ;
- disorders of the sensory organs and nervous system - depression, Optic neuritis , mental and motor disorders, headache, disturbance of consciousness and/or taste, hallucinations (auditory or visual), delirium, decreased visual/hearing acuity;
- hypersensitivity reactions;
- addition of a fungal infection;
- cardiovascular collapse (usually in children of the first year of life).
When using eye drops, liniment and alcohol solution, local allergic reactions are possible.
Instructions for use of Levomycetin
Levomycetin eye drops: instructions for use
Levomycetin eye drops (DIA, Akri, AKOS, Ferein) are applied into the conjunctival sac of each eye, one 3-4 times a day. The course of treatment usually lasts from 5 to 15 days.
When using the drug, you should tilt your head back, gently pull the lower eyelid towards the cheek so that a cavity is formed between the skin and the surface of the eye, and, without touching the eyelid and the surface of the eye with the tip of the dropper bottle, add 1 drop of the medicine into it.
After instillation, press the outer corner of the eye with a finger and do not blink for 30 seconds. If you cannot avoid blinking, you need to do this as carefully as possible so that the solution does not spill out of the eye.
For children during the neonatal period (the first 28 days after birth), the drug is used for health reasons.
For purulent otitis, the drug is injected into the ear 1-2 times a day. 2-3 drops each. If there is significant discharge from the ear canal that washes away the applied solution, Levomycetin can be used up to 4 times a day.
At bacterial rhinitis Your doctor may recommend putting drops into your nose.
Eye drops for stye
Application for barley chloramphenicol in combination with , which is included in the solution as an auxiliary component, helps prevent infection conjunctiva and the development of complications after opening the abscess, accelerates maturation barley , partially relieves redness and reduces pain intensity, shortens recovery time by 2-3 days.
Treatment is carried out simultaneously for both the patient and the healthy eye. The product should be instilled 1-2 drops 2-6 times a day. In case of severe pain, Levomycetin can be instilled every hour.
Levomycetin tablets: instructions for use
Tablets and capsules are taken depending on the indications 3-4 times a day. A single dose of Levomycetin in tablets/capsules for an adult is 1-2 tablets. 250 mg. The highest dose is 4 tablets. 500 mg per day.
In particularly severe cases (for example, with peritonitis or typhoid fever ) the dose can be increased to 3 or 4 g/day.
Duration of use - no more than 10 days.
Levomycetin is often used for diarrhea, which occurs due to food poisoning, as well as in cases where intestinal upset is a consequence of a bacterial infection.
Levomycetin tablets for diarrhea are taken before meals, one every 4-6 hours. The highest dose is 4 g/day. If after taking the first 500 mg tablet the disorder has stopped, you should not take the second one.
How to take Levomycetin for cystitis
Despite the fact that the use of Levomycetin drops in infants can dry out the mucous membrane and reduce the flow of snot, it has been proven that topical application antibiotics often does not allow us to effectively combat bacterial infection .
If we talk about the treatment regimen according to the principle “ off-label prescription” (not for its intended purpose), then Levomycetin is instilled into the ear 3-4 drops, into the nose - 1-2 drops. Treatment lasts from 5 to 10 days. The frequency of procedures is 1-2 per day.
Before applying the drug into the nose, it is necessary to first instill a vasoconstrictor. Before inserting into the ear, the external auditory canal should be cleared of pus.
Application in veterinary medicine
In veterinary practice Levomycetin is used for colibacillosis , salmonellosis , leptospirosis , dyspepsia , colienteritis , coccidosis And pullorosis chickens, infectious and mycoplasmosis birds, urinary tract infections And bronchopneumonia .
The dose for farm animals, as well as for cats and dogs, is selected depending on the weight and severity of the disease.
How to give the drug to chickens? To avoid mass deaths of chickens from intestinal infection They are given 1 tablet of Levomycetin along with food for 3-5 days, 2 times a day. This dosage is calculated for 15-20 chicks.
Analogs
Level 4 ATX code matches:Preparations with the same active ingredient: Levomycetin Actitab , Levomycetin sodium succinate .
Analogues by mechanism of action:
- for Levomycetin tablets -
;bacterial keratitis
, purulent ulcers of the cornea
, blepharitis, conjunctivitis
, chlamydial
And gonorrheal diseases
in adults, as well as blennorrhea
in newborn babies.
Albucid , unlike Levomycetin, causes severe eye irritation.
Use of Levomycetin for children
Use of Levomycetin tablets in pediatrics
Tablet forms of the drug are used in pediatrics under constant monitoring of serum concentration chloramphenicol . Depending on age, the dose of Levomycetin tablets for children ranges from 25 to 100 mg/kg/day.
For newborn infants under 2 weeks of age (including premature infants), the formula for calculating the daily dose is as follows: 6.25 mg/kg per dose with a frequency of applications up to 4 times per day.
For infants over 14 days old, 12.5 mg/kg is prescribed per dose every 6 hours or 25 mg/kg every 12 hours.
For severe infections (for example, ) the dose is increased to 75-100 mg/kg/day.
How to take Levomycetin for diarrhea?
The drug is a fairly serious drug and therefore must be prescribed by a doctor. However, it is often given to children when it is necessary to relieve an intestinal disorder.
As a rule, the dose for children 3-8 years old is from 375 to 500 mg/day. (125 mg per 1 dose), for children 8-16 years old - 750-1000 mg (250 mg per 1 dose).
For diarrhea, a single use of the medicine is allowed. If the child’s condition does not improve, and symptoms persist 4-5 hours after taking the pill, you should consult a physician.
Levomycetin eye drops for children
Eye drops for newborns (in the first 4 weeks after birth) are used only for health reasons.
Levomycetin eye drops for infants are also used with caution. Usually, antibiotic instill 1 drop per conjunctival sac each eye every 6-8 hours.
At barley Eye drops are not recommended for use in children under 10 years of age.
The use of external therapy in children
The solution is not intended for the treatment of children under 1 year of age; liniment is not used for the treatment of premature and newborn infants.
Levomycetin and alcohol
Alcohol and chloramphenicol incompatible. When used simultaneously with ethanol, there is a high risk of developing a disulfiram-like effect, which manifests itself , hyperemia of the skin, nausea and vomiting, reflex cough, convulsions.
Levomycetin during pregnancy
Levomycetin for external and systemic use is contraindicated during pregnancy. If the drug is prescribed to a nursing woman, the child must be switched to artificial feeding for the duration of treatment.
If indicated, eye drops can be used in pregnant women and during lactation, however, provided that the dosage recommended by the instructions is not exceeded.
Description
Tablets are white or white with a yellowish tint, with a score* and a bevel.
*The score is intended to divide the tablet to make it easier to swallow.
Compound
Each tablet contains:
active substance: chloramphenicol – 500 mg;
Excipients: povidone K-25, calcium stearate, potato starch.
Pharmacotherapeutic group
Antibacterial agents for systemic use. Amphenicols.
ATS code: J01BA01.
pharmachologic effect
A broad-spectrum bacteriostatic antibiotic that disrupts the process of protein synthesis in a microbial cell at the stage of transfer of t-RNA amino acids to ribosomes. Effective against strains of bacteria resistant to penicillin, tetracyclines, and sulfonamides. Active against many gram-positive and gram-negative bacteria, pathogens of purulent, intestinal infections, meningococcal infections: Escherichia coli, Shigella dysenteria, Shigella flexneri spp., Shigella boydii spp., Shigella sonnei, Salmonella spp.(incl. Salmonella typhi, Salmonella paratyphi), Staphylococcus spp., Streptococcus spp.(incl. Streptococcus pneumoniae), Neisseria meningitidis, Neisseria gonorrhoeae, a number of strains Proteus spp., Burkholderia pseudomallei, Rickettsia spp., Treponema spp., Leptospira spp., Chlamydia spp.(incl. Chlamydia trachomatis), Coxiella burnetii, Ehrlichia canis, Bacteroides fragilis, Klebsiella pneumoniae, Haemophilus influenzae. Does not affect acid-fast bacteria (incl. Mycobacterium tuberculosis), anaerobes, methicillin-resistant strains of staphylococci, Acinetobacter, Enterobacter, Serratia marcescens,indole positive strains Proteus spp., Pseudomonas aeruginosa spp., protozoa and fungi. Microbial resistance develops slowly. Refers to reserve antibiotics and is used when other antibiotics are ineffective.
Indications for use
Severe, life-threatening infections caused by microorganisms sensitive to choramphenicol, especially Haemophilus influenzae, and typhoid fever.
Used as a reserve antibiotic when other antibacterial agents are ineffective or impossible to use.
- Typhoid fever ( Salmonella typhi);
– Paratyphoid A and B;
– Sepsis caused by salmonella;
– Meningitis caused by Salmonella;
– Meningitis caused by Haemophilus influenzae;
– Purulent bacterial meningitis;
– Rickettsial diseases.
Directions for use and doses
Doses:
Adults (inclincluding elderly patients): The usually recommended dose is 500 mg every 6 hours (50 mg/kg body weight per day in 4 divided doses). Treatment should be continued for another 2 or 3 days after body temperature normalizes. For severe infections (meningitis, sepsis), this dose may initially be doubled, but it should be reduced as soon as clinical improvement occurs.
Children over 6 years old: 50.0–100.0 mg/kg/day in 4 divided doses.
In children and elderly patients, it is necessary to monitor the concentration of chloramphenicol in the blood plasma. Recommended peak plasma concentration of chloramphenicol (approximately 2 hours after dosing): 10–25 mg/L; . the “residual” concentration in the blood plasma before the next dose should not exceed 15 mg/l.
Mode of application: orally, 30 minutes before meals.
If you missland taking the medicine, you must take the missed dose as soon as this omission is noticed. However, ifdThis time of administration coincides with the next dose, do not take the missed dose nextdvet. Take the drug according to the recommended regimendozation without doubling the dose to compensate for the missed dose.
Tablet of the drug Levomycetin is notdsplits into pieces, so when neobthe need to use chloramphenicol in a dose of less than 500 mg, it is recommended to use a medicinal solutiondqualitydother productsddriver, providing the possibility of such aOPS
Side effect
Like all drugs, chloramphenicol can cause unwanted side effects.bny reactions, aboutdHowever, they do not occur in everyone.
The incidence of side effects isdena next yeardations:
Rarely - May occur in up to 1 in 1000 people: reversible dose-dependent suppression of bone marrow functions and irreversible aplastic anemia, hypoplastic anemia, agranulocytosis.
Frequency unknown – outgoingdI'm fromthemeatingddata, frequency of occurrence of certaindit is impossible to eat: secondary fungal infection, reticulocytopenia, leukopenia, granulocytopenia, thrombocytopenia, erythrocytopenia, pancytopenia, increased bleeding time, hypersensitivity reactions (including allergic skin reactions), angioedema, when treating patients with typhoid fever, the Jarisch-Herxheimer reaction may occur, psychomotor disorders, depression, confusion, peripheral neuritis, headache, optic neuritis, visual and auditory hallucinations, decreased visual and hearing acuity, acidotic cardiovascular collapse, dyspepsia, nausea, vomiting (the likelihood of development is reduced when taken 1 hour after meals), diarrhea, irritation of the mucous membrane of the oral cavity and pharynx, glossitis, stomatitis, enterocolitis, dysbiosis (suppression of normal microflora), paroxysmal nocturnal hemoglobinuria, fever, collapse (in children under 1 year), “gray syndrome” of newborns *.
* “Gray syndrome” of newborns is accompanied by vomiting, bloating, respiratory distress, and cyanosis. Later, vasomotor collapse, hypothermia, and acidosis occur. The cause of the development of “gray syndrome” of chloramphenicol, due to the immaturity of liver enzymes, is a toxic effect on the myocardium. Mortality reaches 40%.
If you experience any unwanted reactions, consult your doctor. Thisrecommendationapplies to any possible adverse reactions, including those not listed in the leaflet.treasurehigher. You can also report tendernesseadverse reactions to the Adverse Reactions Database (DaysTviyam) on medications, including reports of drug ineffectivenessnny drugs. By reporting side effects, you can help provide more information about the safety of the drug.
Contraindications
Hypersensitivity to the active and auxiliary components of the drug, history of toxic reactions to chloramphenicol, active immunization, suppression of bone marrow hematopoiesis, acute intermittent porphyria, glucose-6-phosphate dehydrogenase deficiency, liver and/or renal failure, psoriasis, eczema, fungal skin diseases, prevention and treatment of mild infections, children under 6 years of age, pregnancy, lactation.
Chloramphenicol is contraindicated in patients taking medications that may suppress bone marrow function.
Overdose
Chloramphenicol levels above 25 mcg/ml are considered toxic.
If more than 6 tablets are taken, the stomach should be rinsed and then symptomatic treatment should be carried out. In case of severe overdose, for example, "gray syndrome" in children, it is necessary to quickly reduce the concentration of chloramphenicol in the blood plasma using hemoperfusion through ion exchange resins, which will significantly increase the clearance of chloramphenicol.
The most severe consequences of chloramphenicol poisoning can occur in young children. With long-term (exceeding recommended periods) use in high doses - bleeding (due to depression of hematopoiesis or disruption of the synthesis of vitamin K by intestinal microflora).
Treatment: there is no specific antidote. In case of a serious overdose of the drug, symptomatic therapy is recommended - the use of activated carbon, hemoperfusion. In case of massive overdose, discuss the issue of replacement blood transfusion.
Precautionary measures
During treatment with chloramphenicol, alcohol intake is prohibited: with simultaneous intake of alcohol, a disulfiram reaction may develop (skin hyperemia, tachycardia, nausea, vomiting, reflex cough, convulsions).
Severe complications from the hematopoietic system are associated with the use of large doses of chloramphenicol (more than 4000 mg/day) for a long time.
The use of the drug is contraindicated during the period of active immunization.
Clostridiumdifficile-associated diarrhea (CDAD) has been reported to occur with the use of virtually all antibacterial agents, including chloramphenicol, and can range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal microflora of the colon, leading to excessive growth WITH. difficile.
WITH. difficile produces toxins A and B, which contribute to the development of diarrhea. Hypertoxin-producing strains WITH. difficile are associated with increased morbidity and mortality, since these infections may be refractory to antibiotic therapy and may require colectomy, CDAD should be suspected in all patients with diarrhea following antibiotic use.
A careful history is necessary, as diarrhea may occur within 2 months after the use of antibacterial drugs.
If CDAD is suspected or confirmed, continued use of non-targeted antibiotics WITH. difficile, must be stopped. It is necessary to use appropriate fluids and electrolytes, protein supplements, antibiotics against WITH. difficile, surgical evaluation must be performed. Repeated courses of treatment with chloramphenicol should be avoided. Treatment should not be carried out before the start of treatment and more than is really necessary.
Excessively high blood levels of the drug may occur in patients with impaired liver or kidney function. In such patients, the use of the drug is contraindicated.
The use of chloramphenicol, like other antibiotics, can lead to overgrowth of non-susceptible microorganisms, including fungi. If infections caused by non-susceptible microorganisms occur during drug therapy, appropriate measures must be taken.
The use of chloramphenicol can cause severe blood disorders (aplastic anemia, bone marrow hypoplasia, thrombocytopenia, granulocytopenia). There are two types of bone marrow depression associated with chloramphenicol use. Mild bone marrow depression is usually observed, dose-dependent and reversible, which can be detected by early changes in blood tests. Sudden fatal bone marrow hypoplasia without previous symptoms occurs very rarely. Basic blood tests should be performed before starting treatment and approximately every two days during drug therapy. Chloramphenicol should be discontinued if reticulocytopenia, leukopenia, thrombocytopenia, anemia, or any other blood laboratory changes occur. However, it should be noted that such studies do not exclude the possible subsequent occurrence of irreversible bone marrow suppression. Concurrent use of other drugs that inhibit red bone marrow function with chloramphenicol is contraindicated.
When using the drug in patients with diabetes mellitus, false positive results are possible in tests for the presence of glucose in the urine.
Dentistry. The use of the drug leads to an increase in the frequency of microbial infections of the oral cavity, slower healing processes and bleeding gums, which may be a manifestation of myelotoxicity. Dental interventions should, if possible, be completed before starting therapy.
Previous treatment with cytostatics or radiation therapy. Possible accumulation of chloramphenicol and toxic reactions in the form of bone marrow suppression and liver dysfunction.
Geriatric use. Features of use in elderly people have not been sufficiently studied due to the small number of people aged 65 years and older who took part in clinical trials. There are clinical studies showing no differences in the therapeutic response to drug treatment between elderly and young patients. However, dose selection for elderly patients should be cautious, generally starting at the lower end of the dosing range. The drug is significantly excreted through the kidneys and the risk of toxic reactions may be higher in patients with impaired renal function. Since decreased renal function is more likely in elderly patients, caution should be exercised in dose selection and renal function should be monitored.
Use during pregnancy and perioddlactation
Adequate, well-controlled studies on the use of the drug during pregnancy have not been conducted. Chloramphenicol crosses the placental barrier, but it is unknown whether it has toxic effects on the fetus. The use of the drug during pregnancy is contraindicated.
The drug is excreted in mother's breast milk. Due to the possibility of severe adverse reactions in a child, breastfeeding should be stopped during treatment with the drug. The development of “gray syndrome” is possible: toxic reactions, including fatal cases, have been described in newborns; the signs and symptoms associated with these reactions have been called "gray syndrome". Cases of "gray syndrome" have been described in newborns born to a mother who received chloramphenicol during pregnancy. Cases up to 3 months of life have been described. In most cases, chlorifenicol therapy was initiated within the first 48 hours of life. Symptoms appeared 3 to 4 days after continuous treatment with high doses of chloramphenicol. The symptoms appeared in the following order:
– bloating with or without vomiting;
– progressive pale cyanosis;
– vasomotor collapse, often accompanied by irregular breathing;
– death within a few hours after the onset of these symptoms.
Progression of symptoms is associated with high doses. Preliminary serum studies showed unusually high concentrations of chloramphenicol (more than 90 mcg/ml with repeated doses). Measures of assistance: exchange blood transfusion or hemosorption. Cessation of therapy in the early stages often led to reverse symptoms until complete recovery.
Impact on the ability to drive vehiclesddangers and potential dangersWithnew mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Interaction with other drugs
Chloramphenicol suppresses the cytochrome P450 enzyme system, therefore, when used simultaneously with phenobarbital, phenytoin, indirect anticoagulants, and tolbutamide, a weakening of the metabolism of these drugs, a slower elimination and an increase in their concentration in plasma are observed. Dosage adjustments of anticonvulsants and anticoagulants may be necessary if they are used concomitantly with chloramphenicol.
When used simultaneously with phenobarbital, a decrease in the concentration of chloramphenicol is possible (it is necessary to monitor the concentration of chloramphenicol in the blood). Reduces the antibacterial effect of penicillins and cephalosporins.
When used together with penicillins and rifampicin, complex effects (including decrease/increase in plasma concentrations) have been reported, requiring monitoring of chloramphenicol plasma concentrations.
When used with rifampicin, a decrease in the concentration of chloramphenicol is possible.
Simultaneous administration with drugs that inhibit hematopoiesis (sulfonamides, cytostatics), affecting metabolism in the liver, with radiation therapy increases the risk of side effects.
When prescribed with oral hypoglycemic drugs, their effect is enhanced (by suppressing metabolism in the liver and increasing their concentration in plasma).
Calcineurin inhibitors (cyclosporine and tacrolimus): Chloramphenicol therapy may increase plasma concentrations of calcineurin inhibitors (cyclosporine and tacrolimus).
Barbiturates: The metabolism of chloramphenicol is accelerated by barbiturates such as phenobarbital, resulting in a decrease in its plasma concentration.
Estrogens: There is a small risk that chloramphenicol may reduce the contraceptive effect of estrogens.
Paracetamol: Concomitant use of chloramphenicol in patients receiving paracetamol should be avoided as the half-life of chloramphenicol is significantly prolonged.
Myelotoxic drugs increase the manifestations of hematotoxicity of the drug. Chloramphenicol is contraindicated in patients receiving drugs known to cause agranulocytosis. These include: carbamazepine, sulfonamides, phenylbutazone, penicillamine, cytotoxic agents, some antipsychotics, including clozapine and especially depot antipsychotics, procainamide, nucleoside reverse transcriptase inhibitors, propylthiouracil.
Best before date
3 years. Do not use after the expiration date stated on the package.
Vacation conditions
On prescription.
Manufacturer:
RUE “Belmedpreparaty”,
Republic of Belarus, 220007, Minsk,
st. Fabricius, 30, t./f.: (+375 17) 220 37 16,
e-mail: [email protected]
For quotation: Loskutov I.A. Antibacterial agents. RMJ. 1997;13:4.
At the beginning of this century, the ophthalmologist's arsenal in the treatment of infectious eye lesions was more than modest. Thus, there are known recommendations for the use of subconjunctival injections of mercuric cyanide for “dangerously damaged or infected eyes.” In 1938, Domagk received the Nobel Prize in Medicine for his research into the antibacterial properties of p-sulfamylchysoidine. The introduction of sulfonamides was the first achievement that radically changed approaches to treatment infectious diseases The second fundamentally new step was the discovery of antibiotics.
Levomycetin
Fluoroquinolone derivatives:
ciprofloxacin, ofloxacin, norfloxacin
Aminoglycosides:
gentamicin, tobramycin, neomycin
Polymyxins:
polymyxin B sulfate
Tetracyclines:
tetracycline, gramicidin, sulfacyl sodium
Rice. 1. Bacterial conjunctivitis
Levomycetin
(Chloramphenicol)
It is the most widely used antibiotic in ophthalmic practice and has an antimicrobial effect due to the suppression of protein synthesis.
Broad-spectrum antibiotic first isolated from Streptomyces venezuelae. It has a bacteriostatic effect by inhibiting protein synthesis by suppressing the transport of activated amino acids from soluble RNA to ribosomes. The presence of chloramphenicol in detectable quantities in the moisture of the anterior chamber after instillation into the conjunctival cavity has been proven. The development of resistance to chloramphenicol may occur during the treatment of a number of infections, in particular staphylococcal infections, but this is rare.
Indications. Levomycetin should be prescribed only for such serious infectious diseases for which other potentially less dangerous drugs are ineffective or contraindicated. It is recommended to conduct a bacteriological study to identify the pathogen and determine the degree of its sensitivity to chloramphenicol.
It should be borne in mind that against the background of local use of chloramphenicol, the development of such serious complications as bone marrow hypoplasia, accompanied by aplastic anemia, even with a fatal outcome, is possible.
The most sensitive to instillation of chloramphenicol or ointment with this drug are the following pathogens of infectious diseases of the cornea or conjunctiva: Staphylococcus aureus; streptococci, including Streptococcus pneumonia, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Moraxella lacunata (Morax-Axenfeld bacillus), Neisseria species.
Long-term administration of chloramphenicol, like any other antibiotic, can lead to excessive growth of insensitive microorganisms and fungi. If a new infection is detected during treatment with chloramphenicol, it is necessary to stop instillation or laying ointments until the nature of the pathogenic factor is clarified.
Adverse reactions in the form of allergies or inflammatory changes are usually due to individual intolerance. Use 1% eye ointment and eye drops in a concentration of 0.16% to 0.5%. Two drops of the solution or a small amount of ointment are prescribed locally into the conjunctival cavity of the affected eye every 3 hours during the day and night for the first 48 hours, after which the intervals for instilling or laying the ointment can be increased.
Fluoroquinolone derivatives
The history of quinolones began with the accidental discovery of the antibacterial effect of a substance discovered during distillation during the synthesis of chloroquine. Based on the study of this substance, nalidixic acid was synthesized, which was active against gram-positive microorganisms. Analogs of this compound containing a fluorine atom had a wider spectrum of antibacterial activity. A distinctive feature of quinolones is the ability to suppress the functioning of nucleic acids in the bacterial chromosome itself. In relation to fluorinated quinolones, resistance on the part of microorganisms develops very rarely. Ciprofloxacin
(Ciprofloxacinum)
A synthetic fluoroquinolone antibiotic with a broad spectrum of action, effective against both gram-negative and gram-positive microorganisms. Ciprofloxacin differs from other quinolone drugs by the presence of a fluorine atom in the 6th position, a piperazine structure in the 7th position, and a cyclopropyl ring in the 1st position.
After instillation, systemic absorption of the drug is possible. Thus, when a 0.3% solution of ciprofloxacin was instilled into both eyes every 2 hours from the moment of morning awakening for 2 days, followed by instillation every 4 hours from the moment of awakening for another 5 days, the maximum concentration of ciprofloxacin in the blood plasma was 5 ng/ml. The average concentration was less than 2 ng/ml.
Ciprofloxacin is active against a wide range of gram-negative and gram-positive microorganisms in in vitro studies. The bactericidal effect of the drug is explained by its effect on DNA gyrase, which is necessary for the synthesis of bacterial DNA. Ciprofloxacin is active against the following microorganisms:
Rice. 2. Bacterial conjunctivitis
- gram-positive - Staphylococcus aureus (including methicillin-resistant strains), S. epidermidis; Streptococcus pneumoniae, S. viridans;
- gram-negative - Haemophilus influenzae, Pseudomonas aeruginosa, Serratia marcescens.
Ciprofloxacin has been shown to be active against the following microorganisms in vitro:
gram-positive - Enterococcus faecalis; Staphylococcus haemoliticus, S. hominis, S. saprophyticus; Streptococcus pyogenes;
- gram-negative - Acinetobacter calcoaceticus (subspecies anitratus); Aeromonas caviae, A. hydrophila; Brucella melitensis; Campylobacter coli, C. jejuni; Citrobacter diversus,
C. freundii; Edwardsiella tarda; Enterobacter aerogenes, E. cloacae; Escherichia coli; Haemophilus ducreyi, H. influenzae,
H. parainfluenzae; Klebsiella pneumoniae
K. oxytoca; Legionella pneumophila;
Moraxella (Branhamella) catarrhalis; Morganella morganii; Neisseria gonorrhoeae,
N. meningitidis; Pasteurella multocida;
Proteus mirabilis, P. vulgaris; Providencia rettgeri, P. stuartii; Salmonella enteritidis,
S. typhi; Shigella sonneii, S. flexneri;
Vibrio cholerae; V. parahaemolyticus,
V. vulnificus; Yersinia enterocolitica.
Among other microorganisms, it should be noted that Chlamydia trachomatis and Mycobacterium tuberculosis are moderately sensitive to ciprofloxacin.
Ciprofloxacin does not cross-react with other antimicrobials such as b- lactam antibiotics and aminoglycosides, so microorganisms resistant to these drugs may be sensitive to ciprofloxacin. Clinical studies have shown that during therapy with ciprofloxacin in the form of eye drops, 76% of patients with corneal ulcers that were positive according to the results of bacteriological studies were cured. Complete restoration of the epithelial cover of the cornea was achieved in 92% of cases of ulcerative corneal lesions. An extended clinical study showed that after 3 and 7 days of instillation in 52% of patients with conjunctivitis and positive results of bacteriological cultural studies experienced clinical recovery and by the time instillations were stopped, 70-80% of all causative microorganisms were destroyed.
Indications. Instillation of eye drops of a 0.3% solution of ciprofloxacin is indicated for eye infections with antibiotic-sensitive microorganisms: corneal ulcers caused by Pseudomonas aeruginosa, Serratia marcescens, Staphylococcus aureus, S. epidermidis, Stre p tococcus pneumoniae, Streptococcus of the Viridans group; for conjunctivitis caused by Haemophilus influenzae, Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae.
For the treatment of corneal ulcers, it is recommended to instill 2 drops of a 0.3% solution of ciprofloxacin into the affected eye every 15 minutes for the first 6 hours, and then 2 drops of the solution every half hour during the day. On the 2nd day, instill 2 drops into the affected eye every hour. From the 3rd to the 14th day, 2 drops are instilled into the affected eye every 4 hours. Treatment can be continued after the 14th day if epithelization of the cornea has not occurred. For bacterial conjunctivitis, 1 or 2 drops are instilled into the conjunctival cavity every 2 hours from the moment of morning awakening for 2 days and 1-2 drops every 4 hours for the next 5 days.
Ofloxacin
(Ofloxacin)
The chemical structure of ofloxacin differs from the structure of other quinolones by the presence of a six-membered (pyridobenzoxazine) ring from the 1st to 8th positions of the basic cyclic structure.
The pharmacokinetics of ofloxacin was studied during a 10-day course of instillation of a 0.3% antibiotic solution. The mean serum concentration of ofloxacin ranged from 0.4 to 1.9 ng/ml. The maximum serum concentration of ofloxacin after 10 days of treatment was more than 1000 times lower than that after the standard oral dosage of this drug. The average level of ofloxacin in tears 4 hours after instillation was 9.2 μg/g. Ofloxacin is excreted unchanged in the urine.
Ofloxacin in vitro o is active against a wide range of gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal effect of ofloxacin is manifested through the inhibition of DNA gyrase, an essential bacterial enzyme critical for the duplication, transcription and repair of bacterial DNA. Cross-resistance has been shown for ofloxacin and other fluoroquinolones, although this is not the case for ofloxacin and other classes of antibiotics. Thus, microorganisms resistant to b-lactam antibiotics or aminoglycosides may be sensitive to ofloxacin, and vice versa.
The use of ofloxacin is indicated for conjunctivitis caused by antibiotic-sensitive strains of the following microorganisms:
- gram-positive - Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae;
- gram-negative - Enterobacter cloacae, Haemophilus influenzae, Proteus mirabilis, Pseudomonas aeruginosa.
The minimum inhibitory concentration (70% MIC, i.e. the concentration required to suppress 70% of pathogen strains; the lower the 70% MIC value, the stronger the effect of the antibiotic) for ofloxacin is approximately half the 70% MIC for gentamicin against Staphylococcus aureus . Ofloxacin is more effective against Staphylococcus epidermidis than antibiotics such as chloramphenicol and gentamicin. Ofloxacin is twice as active as chloramphenicol against Streptococcus pneumonia. The activity of ofloxacin exceeds that of tobramycin against Klebsiella pne umonia by 32-fold, and its 70% MIC is lower than the 70% MIC of tobramycin against Pseudomonas aeruginosa.
The standard regimen for prescribing the drug is as follows: instillation of 1-2 drops of a 0.3% solution of ofloxacin into the conjunctival cavity of the affected eye every 2-4 hours for the first 2 days and then every 4 hours for the next 5 days.
Norfloxacin
(Norfloxacin)
A fluoroquinolone antibiotic for instillation, differing from other fluoroquinolones by the presence of a fluorine atom in the 6th position and a piperazine structure in the 7th position. Thus, it has been shown that the presence of a fluorine atom in the 6th position increases the effectiveness of the drug against gram-negative bacteria, and the piperazine structure ensures activity against pseudomonads. Norfloxacin inhibits bacterial DNA synthesis, which allows the drug to be considered bactericidal.
The drug has been shown to be active in vitro and in clinical studies against most strains of the following microorganisms:
- gram-positive - Staphylococcus aureus, S. epidermidis, S. warnerii; Streptococcus pneumonia;
- gram-negative - Acinetobacter calcoaceticus, Aeromonas hydrophila, Haemophilus influenzae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia marcescens.
Norfloxacin is active in vitro against the following microorganisms (clinical activity has not been established):
- gram-positive - Bacillus cereus, Enterococcus faecalis, Staphylococcus saprophyticus;
- gram-negative - Citrobacter diversus, C. freundii; Edwardsiella tarda; Enterobacter aerogenes, E. cloacae; Escherichia coli; Hafnia alvery;
- Haemophilus aegyptius (Koch-Wicks bacillus); Klebsiella oxytoca, K. pneumoniae, K. rhinoscleromatis; Morganella morganii; Neisseria gonorrhoeae; Proteus vulgaris; Providencia alcalifaciens, P. rettgeri, P. stuartii; Salmonella typhi; Vibrio cholerae, V. parahaemoliticus; Yersinia enterocolitica;
- other microorganisms - Ureaplasma urealyticum.
Norfloxacin is inactive against obligate anaerobes.
The recommended dose for adults and children over 1 year of age is 1 to 2 drops of a 0.3% solution of norfloxacin 4 times a day in the affected eye for 7 days. In case of severe eye damage, on the 1st day it is possible to instill 1 - 2 drops every 2 hours from the moment of morning awakening.
Aminoglycosides
Gentamicin sulfate
(Gentamicini sulfas)
A water-soluble antibiotic of the aminoglycoside group, isolated from the culture of Micromonospora purpurea.
Gentamicin sulfate exhibits in vitro activity against a number of strains of the following microorganisms:
Staphylococcus aureus, S. epidermidis, Streptococcus pyogenes, S. pneumoniae, Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Neisseria gonorrhoeae, Pseudomonas aeruginosa, Serratia marcescens.
Sterile eye drops or gentamicin sulfate ointment are prescribed for conjunctivitis, keratitis, keratoconjunctivitis, corneal ulcers, blepharitis, blepharoconjunctivitis, acute meibomyitis and dacryocystitis caused by sensitive strains of microorganisms.
Typically, 1 to 2 drops (3 mg/ml) of gentamicin solution are prescribed every 4 hours into the affected eye. For severe lesions, the frequency of instillation can be increased to one instillation every hour.
Tobramycin
(Tobramycinum)
Water-soluble antibiotic of the aminoglycoside series. Many strains of staphylococci are sensitive to tobramycin, including S. aureus and S. epidermidis (including penicillin-resistant strains); streptococci, including some b-hemolytic strains of group A, as well as
Pseudomonas aerug inosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Proteus mirabilis, Morganella morganii, most strains of Proteus vulgaris, Haemophilus influenzae and H. aegyptius, Moraxella lacunata, Acinetobacter ealeoaceticus, some strains Neisseria.
Bacterial sensitivity studies showed that in some cases, microorganisms resistant to gentamicin remained sensitive to tobramycin.
A 0.3% solution of tobramycin is instilled into the affected eye, 1 to 2 drops every 4 hours.
Neomycin
(Neomycinum)
An aminoglycoside whose antibacterial effect is associated with the suppression of protein synthesis due to the formation of a bond with ribosomal RNA, which makes it difficult to read the genetic code of bacteria. Neomycin has a bactericidal effect against a number of gram-positive and gram-negative microorganisms. More often used in combination preparations.
Polymyxins
Polymyxin B sulfate
(Polymyxini B sulfas)
An antibiotic from the polymyxin group with bactericidal activity against a large number of gram-negative microorganisms. Polymyxin B sulfate is able to increase the permeability of the bacterial cell wall by interacting with phospholipid components of the membrane. Systemic absorption after instillation of polymyxin is insignificant. Instillation of the drug at a dose of 10,000 units in 1 ml leads to a maximum increase in its level in the blood serum to 1 unit/ml. This antibiotic is most often used in combination with neomycin.
Rice. 3. Blepharitis
Tetracyclines
Tetracycline hydrochloride
(Tetracyclini hydrochloridum)
Used for the treatment of superficial infectious lesions of the eyeball, as well as for the prevention of ophthalmia of newborns caused by Neisseria gonorrhoeae or Chlamydia trachomatis.
The following microorganisms exhibit sensitivity to tetracycline:
Staphylococcus aureus, streptococci, including S. pneumoniae, Escherichia coli, Neisseria strains, Chlamydia trachomatis.
The drug is prescribed as a 1% ointment or suspension.
Gramicidin
(Gramicidinum)
Gramicidin is a mixture of three antibacterial compounds (gramicidins A, B and C) produced by the growth of Bacillus brevis.
The bactericidal effect of gramicidin extends to a large number of gram-positive microorganisms. This antibiotic increases the permeability of the bacterial cell wall by forming a network of channels in the membrane of the microorganism. More often used in combination with other antibiotics.
Sulfacyl sodium
(Ssulfacylum-natrium)
Sulfonamides are bacteriostatic drugs. They inhibit the bacterial synthesis of dehydrofolic acid by preventing the combination of pteridine with aminobenzoic acid by competitively inhibiting the activity of the enzyme dehydropteroate synthetase. Resistance to this drug may develop through two mechanisms:
- changes in dehydropteroate synthetase with decreased sensitivity to sulfonamides;
- formation of more aminobenzoic acid.
Local use of sulfonamides is effective when the causative agent of an eye infection is a sensitive strain of microorganisms such as
Escherichia coli, Staphylococcus aureus, Streptococcuspneumoniae, streptococci of the viridans group, Haemophilus influenzae, certain strains of Klebsiella and Enterobacter.
Rare but fatal complications of sulfonamides use include:
- Stevens-Johnson syndrome;
- toxic epidermal necrolysis;
- agranulocytosis;
- aplastic anemia.
It should be borne in mind that the effectiveness of sulfonamides can be significantly reduced due to para-aminobenzoic acid, which is present in large quantities in purulent exudate. It is also important that sulfonamides are incompatible with silver preparations.
Prescribe 10, 15 and 30% solutions of the drug in the form of instillations into the affected eye.
Bacitracin
(Bacitracin zinc)
Zinc salt of cyclic polypeptides formed as a result of the growth of microorganisms of the licheniformis group of bacteria Bacillus subtilis.
A bactericidal drug effective against a range of gram-positive and gram-negative bacteria. The effect is due to the influence on the synthesis processes of the microorganism wall. Bacitracin suppresses synthetic processes by inhibiting the regeneration of phospholipid receptors involved in the synthesis of peptidoglycans. Used in combined antibacterial drugs.
Trimethoprim
(Trimetoprimum sulfas)
A synthetic antibacterial drug active against a wide range of aerobic gram-positive and gram-negative microorganisms. Trimethoprim blocks the formation of tetrahydrofolic acid from dihydrofolic acid by reversibly inhibiting the activity of the enzyme dihydrofolate reductase. Moreover, the blockade of a bacterial enzyme is much more pronounced than the blockade of the corresponding enzyme in the human body, which allows us to speak about the selectivity of the effect on bacterial biosynthesis. In vitro studies have shown the antibacterial effect of trimethoprim against the following microorganisms:
Staphylococcus aureus, S. epidermidis, Streptococcus pyogenes, S. faecalis, S. pneumoniae, Haemophilus influenzae, H. aegyptius, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, P. vulgaris, Enterobacter aerogenes, Serratia marcescens.
Systemic absorption of trimethoprim when administered topically is negligible. Thus, when drops containing 1 mg of trimethoprim were instilled in 1 ml, the maximum concentration of the drug in the blood serum was 0.03 μg/ml.
Literature:
1. Conte J. Manual of antibiotics and infectious diseases 1995. 8th Ed.
2. Chitkara D, et al. Lack of effect of preoperative norfloxacin on bacterial contamination of anterior chamber aspirates after cataract surgery. Br J Ophthalmol 1994;78:772-4.
3. Suharwady J, Ling C, et al. A comparative trial between diclofenac-gentamicin and betamethasone-neomycin drops in patients undergoing cataract extraction. Eye 1994;8:550-4.
4. Stevens R, Holland G, Pashal J, et al. Mycobacterium Fortuitum keratitis: a comparison of topical ciprofloxacin and amikacin in an animal model. Cornea 1992;11:500-4.
5. Snyder M, Katz H. Ciprofloxacin-resistant bacterial keratitis. Am J Ophthalmol 1992;114:336-8.
6. Colin J, Hasle D. Corneal and conjunctival infections. Current Opinion in Ophthalmol 1993;4(4):54-8.
7. Abel R, Abel A. Perioperative antibiotic, steroidal and nonsteroidal antinflammatory agents in cataract intraocular lens surgery. Current Opinion in Ophthalmol 1996;7(1):39-42.
8. Miller I, Vogel R, Cook T, et al. Topically administered norfloxacin compared with topically administered gentamicin for the treatment of external ocular bacterial infections. Am J Ophthalmol 1992;113:638-44.
9. Assil K, Zarnegar S, Fouraker B, et al. Efficacy of tobramycin-soaked collagen shields versus tobramycin eyedrop loading dose for sustained treatment of experimental Pseudomonas Aeruginosa-induced keratitis in rabbits. Am J Ophthalmol 1992;113:418-23.
(Continuation)
LP-004849
Trade name:
Levomycetin
International nonproprietary or generic name:
chloramphenicol
Dosage form:
film-coated tablets
Compound
Composition per tablet:
Description:
Dosage 250 mg: round, biconvex, film-coated tablets, white or almost white. In cross-section, the tablet core is white, grayish-white or yellowish-white.
Dosage 500 mg: oblong, biconvex, film-coated tablets, white or almost white, scored. In cross-section, the tablet core is white, grayish-white or yellowish-white.
Pharmacotherapeutic group:
antibiotic
ATX code:
Pharmacological properties
Pharmacodynamics
A broad-spectrum bacteriostatic antibiotic that disrupts the process of protein synthesis in the microbial cell.
Effective against strains of bacteria resistant to penicillins, tetracyclines, and sulfonamides.
Active against many gram-positive and gram-negative bacteria, pathogens of purulent infections, typhoid fever, dysentery, meningococcal infection, hemophilic bacteria, Escherichia coli, Shigella dysenteria spp., Shigella flexneri spp., Shigella boydii spp., Shigella sonnei spp., Salmonella spp. (including Salmonella typhi, Salmonella paratyphi), Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae), Neisseria meningitidis, a number of strains of Proteus spp., Pseudomonas pseudomallei, Rickettsia spp., Treponema spp., Leptospira spp., Chlamydia spp. (including Chlamydia trachomatis), Coxiella burnetii, Ehrlichia canis, Bacteroides fragilis, Klebsiella pneumoniae, Haemophilus influenzae.
Does not affect acid-fast bacteria (including Mycobacterium tuberculosis), Pseudomonas aeruginosa, Clostridia, methicillin-resistant strains of staphylococci, Acinetobacter, Enterobacter, Serratia marcescens, indole-positive strains of Proteus spp., Pseudomonas aeruginosa spp., protozoa and fungi.
Resistance of microorganisms to chloramphenicol develops slowly.
Pharmacokinetics
Absorption - 90% (fast and almost complete). Bioavailability - 80% after oral administration and 70% after intramuscular administration. Communication with plasma proteins is 50-60%, in premature newborns - 32%. The time to reach maximum concentration (TC max) after oral administration is 1-3 hours, after intravenous administration - 1-1.5 hours. Volume of distribution - 0.6-1 l/kg. Therapeutic concentration in the blood remains for 4-5 hours after administration. Penetrates well into body fluids and tissues. Its greatest concentrations are created in the liver and kidneys. Up to 30% of the administered dose is found in bile. The maximum concentration (Cmax) in the cerebrospinal fluid (CSF) is determined 4-5 hours after a single oral dose and can reach, in the absence of inflammation of the meninges, 21-50% of the maximum concentration (Cmax) in plasma and 45-89% - with the presence of inflammation of the meninges. Passes through the placental barrier, concentrations in fetal blood serum can be 30-80% of those in maternal blood. Passes 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 excreted within 24 hours by the kidneys - 90% (by glomerular filtration - 5-10% unchanged, by tubular secretion in the form of inactive metabolites - 80%), through the intestines - 1-3%. The half-life in adults is 1.5-3.5 hours, in case of impaired renal function - 3-11 hours. The half-life in children from 3 years to 16 years is 3-6.5 hours. It is poorly excreted during hemodialysis.
Indications for use
Infections of the urinary and biliary tract caused by sensitive microorganisms.
Contraindications
Hypersensitivity to chloramphenicol or other components of the drug, inhibition of bone marrow hematopoiesis, acute intermittent porphyria, glucose-6-phosphate dehydrogenase deficiency, liver and/or renal failure, pregnancy, lactation, children under 3 years of age and weighing less than 20 kg.
Carefully
Patients who have previously received treatment with cytotoxic drugs or radiation therapy.
Use during pregnancy and breastfeeding
The drug is contraindicated during pregnancy and breastfeeding.
Directions for use and doses
Orally (30 minutes before meals, and if nausea and vomiting develop - 1 hour after meals) 3-4 times a day.
A single dose for adults is 250-500 mg, daily - 2000 mg.
For children over 3 years of age and weighing more than 20 kg, use 12.5 mg/kg every 6 hours or 25 mg/kg every 12 hours (under the control of the concentration of the drug in the blood serum).
The average duration of treatment is 8-10 days.
Side effect
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, dysbacteriosis (suppression of normal microflora).
From the hematopoietic organs: reticulocytopenia, leukopenia, granulocytopenia, thrombocytopenia, erythrocytopenia; aplastic anemia, agranulocytosis.
From the nervous system: psychomotor disorders, depression, confusion, peripheral neuritis, optic neuritis, visual and auditory hallucinations, decreased visual and hearing acuity, headache.
Allergic reactions: skin rash, angioedema.
Other: secondary fungal infection.
Overdose
Symptoms: suppression of bone marrow hematopoiesis, gastrointestinal disorders, liver and kidney damage, neuropathy (including the optic nerve) and retinopathy.
Treatment: hemosorption, symptomatic therapy.
Interaction with other drugs
It suppresses the enzyme system of cytochrome P450, therefore, when used simultaneously with phenobarbital, phenytoin, and indirect anticoagulants, a weakening of the metabolism of these drugs is observed, a slower elimination and an increase in their concentration in plasma.
Reduces the antibacterial effect of penicillins and cephalosporins.
When used simultaneously with erythromycin, clindamycin, lincomycin, a mutual weakening of the effect is observed 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 inhibit hematopoiesis (sulfonamides, cytostatics), affecting metabolism in the liver, with radiation therapy increases the risk of side effects.
When prescribed with oral hypoglycemic drugs, their effect is enhanced (by suppressing metabolism in the liver and increasing their concentration in plasma).
Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
special instructions
When taking ethanol simultaneously, a disulfiram-like reaction may develop (skin hyperemia, tachycardia, nausea, vomiting, reflex cough, convulsions).
During treatment, systematic monitoring of peripheral blood patterns is necessary.
Impact on the ability to drive vehicles and machinery
During treatment with the drug, special care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Release form
Film-coated tablets, 250 mg, 500 mg.
10 or 15 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.
1, 2, 3, 4, 5, 6 or 10 blister packs with instructions for use in a cardboard pack.
Storage conditions
In original packaging, at a temperature not exceeding 30 °C.
Keep out of the reach of children.
Best before date
3 years.
Do not use after the expiration date indicated on the package.
Vacation conditions
Dispensed by prescription.
Legal entity in whose name the registration certificate was issued / Organization receiving consumer complaints
BRIGHTFARM LLC, Russia
249033, Kaluga region, Obninsk, st. Gorkogo, 4
Manufacturer
CJSC "Obninsk Chemical and Pharmaceutical Company" (CJSC "OKhPK"), Russia
Legal address: 249036, Kaluga region, Obninsk, st. Koroleva, 4
Address of place of production: Kaluga region, Obninsk, Kyiv highway, building. 103, building 107
Chloramphenicol (chloramphenicol) - 500 mg
(in terms of 100% substance).Excipients
: starchpotato - 33.5 mg; low molecular weight povidone (medical low molecular weight polyvinylpyrrolidone) - 11 mg; calcium stearate - 5.5 mg. Description:Tablets are white or white with a slight yellowish tint, flat-cylindrical in shape with a chamfer and a score on one side.
Pharmacotherapeutic group: Antibiotic ATX:D.06.A.X.02 Chloramphenicol
S.01.A.A.01 Chloramphenicol
J.01.B.A.01 Chloramphenicol
Pharmacodynamics:A broad-spectrum bacteriostatic antibiotic that disrupts the process of protein synthesis in the microbial cell. Effective against strains of bacteria resistant to penicillin, tetracyclines, and sulfonamides.
Active against many gram-positive and gram-negative bacteria, pathogens of purulent infections, typhoid fever, dysentery, meningococcal infection, hemophilic bacteria, Escherichia coli, Shigella dysenteria spp., Shigella flexneri spp., Shigella boydii spp., Shigella sonnei spp., Salmonella spp.(incl. Salmonella typhi, Salmonella paratyphi), Staphylococcus spp., Streptococcus spp.(incl. Streptococcus pneumoniae), Neisseria meningitidis, a number of strains Proteus spp., Pseudomonas pseudomallei, Rickettsia spp., Treponema spp., Leptospira spp., Chlamydia spp.(incl. Chlamydia trachomatis), Coxiella burnetii,Ehrlichia canis, Bacteroides Fragil i s, Klebsiella pneumoniae, Haemophilus influenzae.
He acts on acid-fast bacteria (incl. Mycobacterium tuberculosis), Pseudomonas aeruginosa, clostridia, methicillin-resistant staphylococcus strains,Acinetobacter, Enterobacter, Serratia marcescens,indole-positive strainsProteus spp., Pseudomonas aeruginosa spp.,protozoa and fungi.Microbial resistance develops slowly.
Pharmacokinetics:Absorption - 90% (fast and almost complete). Bioavailability - 80%. Communication with plasma proteins is 50-60%, in premature newborns - 32%. The time to reach maximum concentration after oral administration is 1-3 hours. Volume of distribution is 0.6-1.0 l/kg. Therapeutic concentration in the blood remains for 4-5 hours after administration.
Penetrates well into body fluids and tissues. The highest concentrations are created in the liver and kidneys. Up to 30% of the administered dose is found in bile. The maximum concentration in the cerebrospinal fluid is determined 4-5 hours after a single oral administration and can reach 21-50% of the maximum concentration in plasma for non-inflamed meninges and 45-89% for inflamed meninges. Passes through the placental barrier, concentrations in the fetal blood serum can be 30-80% of the concentration in the maternal blood. Passes 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 excreted within 24 hours by the kidneys - 90% (by glomerular filtration - 5-10% unchanged, by tubular secretion in the form of inactive metabolites - 80%), through the intestines - 1-3%. The half-life in adults is 1.5-3.5 hours, in case of impaired renal function - 3-11 hours. The half-life in children - from 1 month to 16 years - 3-6.5 hours, in newborns from 1 to 2 days - 24 hours or more ( varies especially in children with low birth weight), 10-16 days -10 hours. Weakly susceptible to hemodialysis.
Indications:Infections of the urinary and biliary tract caused by microorganisms sensitive to chloramphenicol.
Contraindications:Hypersensitivity, suppression of bone marrow hematopoiesis, acute intermittent porphyria, glucose-6-phosphate dehydrogenase deficiency, liver and/or kidney failure, skin diseases (psoriasis, eczema, fungal infections), pregnancy, lactation, children under 2 years of age.
Carefully:Patients who have previously received treatment with cytotoxic drugs or radiation therapy.
Pregnancy and lactation:The drug is contraindicated during pregnancy and breastfeeding. Directions for use and dosage:Orally (30 minutes before meals, and if nausea and vomiting develop - 1 hour after meals, 3-4 times a day).
A single dose for adults is 0.25-0.5 g, daily dose is 2 g/day. For severe forms of infections (including typhoid fever, peritonitis), in a hospital setting the dose may be increased to 3-4 g/day.
Children are prescribed under controlled concentrations of the drug in the blood serum at 12.5 mg/kg (base) every 6 hours or 25 mg/kg (base) every 12 hours, for severe infections (bacteremia, meningitis) - up to 75-100 mg/kg ( basis)/day The average duration of treatment is 8-10 days.
Side effects:From the digestive system: dyspepsia, nausea, vomiting (the likelihood of development is reduced when taken 1 hour after a meal), diarrhea, irritation of the oral mucosa and pharynx, dermatitis (including perianal dermatitis - when used rectally), dysbiosis (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 and hearing acuity, headache.
Allergic reactions: skin rash, angioedema.
Others: secondary fungal infection, collapse (in children under 1 year).
Overdose:Symptoms: “gray syndrome” in premature infants and newborns when treated with high doses (the cause of development is the accumulation of chloramphenicol due to the immaturity of liver enzymes and its direct toxic effect on the myocardium) - bluish-gray skin color, low body temperature, irregular breathing, lack of reactions, cardiovascular failure. Mortality - up to 40%.
Treatment: hemosorption, symptomatic therapy.
Interaction:Simultaneous administration with drugs that inhibit hematopoiesis (sulfonamides, cytostatics), affecting metabolism in the liver, with radiation therapy increases the risk of side effects.
When taking ethanol simultaneously, a disulfiram reaction may develop.
When prescribed with oral hypoglycemic drugs, their effect is enhanced (by suppressing metabolism in the liver and increasing their concentration in plasma).
When used simultaneously with erythromycin, clindamycin, lincomycin, a mutual weakening of the effect is noted due to the fact that chloramphenicop candisplacethese drugsfrombound stateor prevent their binding to the 50S subunit of bacterial ribosomes.
Reduces the antibacterial effect of penicillins and cephalosporins.
Chloramphenicol suppresses the cytochrome P450 enzyme system, therefore, when used simultaneously with phenobarbital, phenytoin, and indirect anticoagulants, a weakening of the metabolism of these drugs is observed, a slowdown Special instructions:Severe complications from the hematopoietic system are usually associated with the use of large doses (more than 4 g/day) for a long time.
During treatment, systematic monitoring of peripheral blood patterns is necessary.
In the fetus and newborns, the liver is not developed enough to bind , and the drug can accumulate in toxic concentrations and lead to the development of “gray syndrome”, so children in the first months of life are prescribed the drug only for health reasons.
When taking ethanol simultaneously, a disulfiram reaction may develop (skin hyperemia, tachycardia, nausea, vomiting, reflex cough, convulsions).
Impact on the ability to drive vehicles. Wed and fur.:During treatment with the drug, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Release form/dosage:Tablets 0.5 g. Package:10 tablets per
contour blister packaging. 10 tablets per contour cellless bottle packaging.
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