Cefixime

Pharmacological properties

cefixime is a third generation cephalosporin antibiotic with a wide spectrum of antibacterial action. acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. cefixime interacts with penicillin-binding proteins in the cytoplasm of the bacterial membrane and acylates the transpeptidase enzymes within the membrane, disrupting the transverse bonds of the peptide chains necessary to ensure the strength of the bacterial cell wall. cefixime inhibits the growth and division of bacterial cells and causes their lysis. bacteria with a high division rate are especially sensitive to cefixime.

Cefixime is resistant to β-lactamases (penicillinases and cephalosporinases), and is active against a wide range of gram-negative microorganisms, including penicillinase producing strains: N. gonorrhoeae, Citrobacter spp., Escherichia coli, Enterobacter spp., Klebsiella spp. Providencia spp. and Serratia species.

Gem-positive cocci are sensitive to cefixime: Streptococcus pyogenes, S. pneumoniae; all gram-negative microorganisms, including strains: H. influenzae, M. catarrhalis and N. gonorrhoeae producing β-lactamase.

Staphylococcus bacteria are moderately susceptible to cefixime. Bacteria of the genus Pseudomonas are resistant to cefixime.

Pharmacokinetics Tablets. Quickly absorbed in the digestive tract. Bioavailability is 40-50%. The maximum concentration in blood serum is reached after 4 hours (when taken with food - 0.8 hours earlier). With plasma proteins (mainly with albumin), 65% binds. T_½ is 3-4 hours. In patients with impaired renal function with creatinine clearance of 20-40 ml / min T_½ increases to 6.4 hours, with creatinine clearance 5–10 ml / min - up to 11.5 hours. It is excreted mainly with urine (50%) unchanged for 24 hours and with bile (10%).

Suspension. When taken orally, about 60% of the drug is absorbed. T_½ from blood plasma is 2.5-3.8 hours (an average of 3 hours). Distribution volume - 0.1 l / kg. Linking blood plasma proteins - 70%.

Indications

Tablets: infections caused by microorganisms sensitive to the drug: acute and chronic bronchitis, pneumonia, otitis media, pharyngitis, tonsillitis, sinusitis, infections of the genitourinary system.

Suspension: infections caused by microorganisms sensitive to the drug: acute and chronic bronchitis, otitis media, pharyngitis, tonsillitis, infections of the genitourinary system.

Application

Tablets: inside adults and children over the age of 12 years and a body weight of 50 kg, regardless of food intake. the usual dose is 400 mg / day. the course of treatment is from 3 days (treatment of uncomplicated cystitis) to 10-14 days.

With uncomplicated gonococcal urethritis or cervicitis, 400 mg is prescribed once. In elderly patients, dose adjustment is not required.

In patients with impaired renal function (creatine clearance of 20 ml / min), the daily dose should not exceed 200 mg.

If necessary, dosages of less than 400 mg of Loprax are used as a suspension.

Suspension: intended for use in pediatric practice. The usual daily dose in children aged 6 months to 12 years with a body weight of 50 kg is 8 mg / kg of a child’s body weight 1 time per day. At a dose of 4 mg / kg body weight - 2 times a day (every 12 hours). The duration of treatment is from 3 days (uncomplicated infections) to 10-14 days, depending on the severity of the disease and is set individually.

Children with a body weight of 50 kg or over the age of 12 years are prescribed the drug in doses recommended for adults: 400 mg once a day or 200 mg 2 times a day (every 12 hours).

To prepare the suspension, freshly boiled and cooled to room temperature water is used. Open the bottle and add water (approximately ½ volume of the bottle), close the lid and shake well. After that, add water to the level of the mark on the bottle, close the lid and shake again. Before each reception, the prepared suspension must be thoroughly shaken. Take orally before or after a meal; with gastrointestinal irritation - with food.

Contraindications

Tablets: hypersensitivity to cephalosporin antibiotics, BA, renal failure, pregnancy and lactation, children under 12 years of age.

Suspension: hypersensitivity to antibiotics of the cephalosporin group, AD, renal failure, pregnancy and lactation, children under 6 months of age.

Side effects

Minor and rarely develop.

From the side of the central nervous system: headache, dizziness.

On the part of the blood system and vascular system: eosinophilia, leukopenia, thrombocytopenia, neutropenia, hemolytic anemia, hypoprothrombinemia, thrombophlebitis.

From the gastrointestinal tract: intestinal cramps, diarrhea, nausea, vomiting, candidiasis of the oral mucosa; pseudomembranous colitis (cramping and pain in the stomach and intestines, bloody diarrhea, fever).

From the hepatobiliary system: icteric sclera or skin.

From the urinary system: interstitial nephritis.

From the side of the immune system: allergic reactions - skin rash, itching, urticaria, anaphylaxis, erythema multiforme or Stevens-Johnson syndrome, serum sickness.

From the reproductive system: vaginal candidiasis (vaginal itching or discharge).

General disorders: fatigue, weakness.

On the part of laboratory indicators: a transient increase in the level of liver transaminases, an increase in the level of nitrogen, urea or creatinine in the blood serum.

special instructions

Before starting laprax therapy, it is necessary to exclude the patients hypersensitivity to cephalosporins or penicillin antibiotics (cross-allergic reactions are possible). with the development of an allergic reaction to cefixime, the drug should be discontinued immediately.

It is prescribed with caution to patients with allergic reactions (especially drugs), patients with a history of bleeding, patients with gastrointestinal diseases (especially with ulcerative colitis, regional colitis or enteritis (Crohns disease)), in case of impaired liver function.

Long-term use of the drug can lead to the development of dysbiosis and cause increased growth of Candida albicans (candidiasis of the oral mucosa); severe diarrhea and pseudomembranous colitis may develop. With the use of cefixime, a deficiency of group B vitamins may develop. During treatment with the drug, pseudo-positive results of glucosuric tests and a positive direct Coombs reaction can be noted.

Cephalosporin antibiotics increase the toxicity of alcohol; alcohol is not recommended during treatment.

Suspension: children with kidney disease are prescribed a dose of 1.5–3 mg / kg of body weight per day.

In diseases caused by β-hemolytic group A streptococcus, the course of treatment should be at least 10 days in order to prevent the development of acute rheumatic fever or glomerulonephritis.

With prolonged treatment, monitoring of laboratory blood parameters, as well as liver and kidney function, is necessary.

During pregnancy and breastfeeding. Loprax crosses the hematoplacental barrier. There is no data on the safe use of the drug during pregnancy; during this period, the drug is not prescribed. At the time of treatment, it is necessary to stop breastfeeding.

Children. Tablets: prescribed for children over the age of 12 years.

Suspension: there is no data on the safe use of the drug in children under the age of 6 months.

Influence on the ability to drive vehicles or work with other mechanisms. It does not affect, however, possible adverse reactions from the central nervous system (individually in each case) must be taken into account.

Interactions

With the simultaneous administration of loprax and nephrotoxic drugs (diuretics), an increase in the nephrotoxic effect is possible, especially in patients with impaired renal function.

With concurrent administration with aminoglycosides, renal function must be monitored.

The combined use of cefixime and carbamazepine increases the concentration of carbamazepine in the blood serum.

Overdose

Symptoms: dizziness, nausea, vomiting.

Treatment: gastric lavage, symptomatic therapy. Hemodialysis or peritoneal dialysis is ineffective.

Storage conditions

At a temperature not exceeding 25 ° C.