Ciprofloxacin

Ciprofloxacin

When taken orally, ciprofloxacin is quickly and fairly completely absorbed from the gastrointestinal tract (mainly in the duodenum and jejunum). Eating slows down absorption, but does not change the maximum concentration (Cmax) and bioavailability. The bioavailability of the drug is 50-85%.

The time to reach maximum concentration (TCmax) is 60-90 minutes, Cmax linearly depends on the dose taken and is about 2.4 and 5.4 μg/ml at doses of 500 and 1000 mg, respectively. 12 hours after oral administration of 500 mg, the concentration of the drug in plasma decreases to 0.2 mcg/ml.

Ciprofloxacin is well distributed in tissues and body fluids. High concentrations of the drug are achieved in bile, lungs, kidneys, liver, gall bladder, uterus, seminal fluid, prostate tissue, tonsils, endometrium, fallopian tubes and ovaries. The concentration in tissues is 2-12 times higher than in plasma. Ciprofloxacin also penetrates well into bones, ocular fluid, bronchial secretions, saliva, skin, muscles, pleura, peritoneum, lymph, and through the placenta. The drug penetrates into the cerebrospinal fluid in small quantities, where its concentration in the absence of inflammation of the meninges is 6-10% of that in the blood serum, and in the case of inflammation - 14-37%. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in blood serum.

The volume of distribution in the body is 2-3.5 l/kg.

The degree of binding of ciprofloxacin to plasma proteins is 20-40%.

Metabolized in the liver (15-30%) with the formation of low-active metabolites (diethylciprofloxacin, sulfociprofloxacin, oxociprofloxacin, formylciprofloxacin).

The half-life (T1/2) is about 4 hours, in case of chronic renal failure - up to 12 hours. It is excreted mainly by the kidneys by tubular filtration and tubular secretion in unchanged form (40-50%) and in the form of metabolites (15%), the rest part - the gastrointestinal tract. A small amount is excreted in breast milk.

Renal clearance - 3-5 ml/min/kg; total clearance - 8-10 ml/min/kg.

In chronic renal failure (creatinine clearance above 20 ml/min), the percentage of ciprofloxacin excreted through the kidneys decreases, but accumulation in the body does not occur due to a compensatory increase in ciprofloxacin metabolism and excretion through the gastrointestinal tract.

Ciprofloxacin

Ciprofloxacin is an antibiotic that has a bactericidal effect against a wide range of pathogenic microorganisms. It does not slow down or stop the development and reproduction of microscopic objects, as bacteriostatic drugs do, but completely destroys bacteria, causing their death and subsequent removal from the body. The mechanism of action of this antibiotic is based on the inhibition of bacterial DNA gyrase, an enzyme responsible for DNA duplication, without which the process of protein synthesis is unthinkable.

Among the bacteria that are affected by ciprofloxacin, there are both gram-negative and gram-positive specimens. Bacteria of the genus Staphylococcus, Streptococcus, Enterobacteriaceae, Escherichia coli and Haemophilus influenzae, Klebsiella, Morganella, Neisseria, Salmonella, Shigella, Legionella, Providence, Yersinia, Chlamydia, Mycobacteria and many others are sensitive to it.

Taking ciprofloxacin is associated with a number of restrictions. So, while undergoing treatment with this drug, it is necessary to refrain from excessive exposure to the open sun. An important condition for the effective operation of the drug is the consumption of a sufficient volume of fluid to maintain diuresis at a normal level (otherwise hemato- and crystalluria may occur).

The method of administration and dose of ciprofloxacin are determined individually depending on the severity and localization of the infection in the body, the age and body weight of the patient, his general health in general and the functional state of the urinary system in particular.

The recommended single dose for tablets is 250 mg for uncomplicated and 500 mg for complex infections when taken twice daily. The drug is taken on an empty stomach along with plenty of liquid. The average course of treatment with ciprofloxacin is 7 to 10 days. For severe infections, the drug can be used in the form of intravenous infusions of 400 mg twice a day (a detailed list of antibiotic doses depending on the disease is given in the package insert). In ophthalmological and ENT practice, ciprofloxacin is used topically in the form of eye and ear drops. For mild and moderate eye infections, it is enough to instill 2 drops of the drug into the conjunctival sac every 4 hours, for severe ones - every hour. Eye ointment, as a dosage form of ciprofloxacin, is currently not widely used and is produced by only one plant - the Russian OJSC Tatkhimfarmpreparaty. In otolaryngology, the recommended dose of ciprofloxacin is 3-4 drops instilled into the external auditory canal 2-4 times a day.

Tsiprobay

The tablets should be taken orally on an empty stomach, without chewing, with a small amount of liquid.

Can be taken regardless of meals. If the drug is used on an empty stomach, the active substance is absorbed faster. In this case, the tablets should not be taken with dairy products or fortified with calcium (for example, milk, yogurt, juices with a high calcium content). Calcium contained in regular food does not affect the absorption of ciprofloxacin.

If, due to the severity of the condition or for other reasons, the patient is unable to take tablets, he is recommended to undergo parenteral therapy with an infusion solution of ciprofloxacin, and after improvement of the condition, switch to taking the tablet form of the drug.

In the absence of other prescriptions, it is recommended to follow the following dosage regimen:

Adults

When treating elderly patients, the lowest possible doses of ciprofloxacin should be used, based on the severity of the disease and CC (for example, with CC 30-50 ml/min, the recommended dose of ciprofloxacin is 250-500 mg every 12 hours).

Children

In the absence of other prescriptions, the following dosage regimen should be followed.

For the treatment of complications of pulmonary cystic fibrosis caused by Pseudomonas aeruginosa, children aged 5 to 17 years are prescribed orally 20 mg/kg body weight 2 times a day (maximum dose 1500 mg) or intravenously 10 mg/kg body weight 3 times/day. day (maximum dose 1200 mg). The duration of treatment is 10-14 days.

For the prevention and treatment of pulmonary anthrax, 15 mg/kg body weight is prescribed orally 2 times a day (do not exceed the maximum single dose of 500 mg and the daily dose of 1000 mg) or intravenously 10 mg/kg body weight 2 times/day. days (do not exceed the maximum single dose of 400 mg and the maximum daily dose of 800 mg).

The drug should be started immediately after suspected or confirmed infection.

The total duration of treatment with ciprofloxacin for pulmonary anthrax is 60 days.

Dosage regimen for impaired renal or liver function

In case of impaired renal function in adults with CC from 31 to 60 ml/min/1.73 m2 or plasma creatinine concentration from 1.4 to 1.9 mg/100 ml, the maximum dose of ciprofloxacin when taken orally should be 1000 mg/day or IV 800 mg/day days When CC is 30 ml/min/1.73 m2 or less, or its plasma concentration is 2 mg/100 ml or more, the maximum dose of ciprofloxacin when taken orally should be 500 mg/day or IV 400 mg/day.

For renal impairment and hemodialysis, the dosage regimen is similar to that described above; on days of hemodialysis, ciprofloxacin is taken after this procedure. In case of impaired renal and liver function, the dosage regimen is also similar to that described above.

In case of impaired renal function and peritoneal dialysis in outpatients, 500 mg of ciprofloxacin is prescribed orally or an infusion solution of ciprofloxacin is added to the dialysate (intraperitoneal): 50 mg of ciprofloxacin per liter of dialysate is administered 4 times a day every 6 hours.

If liver function is impaired, no dose adjustment is required.

The dosage regimen in children with renal and hepatic insufficiency has not been studied.

Duration of use

The duration of therapy depends on the severity of the disease and its clinical and bacteriological control. It is important to continue treatment for at least another 3 days after the fever or other clinical symptoms of the disease have disappeared.

Average duration of treatment: 1 day - for acute uncomplicated gonorrhea and cystitis; up to 7 days - for infections of the kidneys, urinary tract, abdominal cavity; during the entire period of neutropenia in immunocompromised patients; maximum 2 months - for osteomyelitis; 7-14 days - for other infections.

For infections caused by streptococci, due to the risk of late complications, treatment should be continued for at least 10 days.

For infections caused by chlamydia, therapy should also be carried out for at least 10 days.

Method of use of solution for infusion

Ciprofloxacin is administered as an intravenous infusion lasting at least 60 minutes. The infusion solution should be injected slowly into a large vein to prevent complications at the infusion site. The infusion solution can be administered alone or together with other compatible infusion solutions.

Compatibility with other solutions

Ciprofloxacin infusion solution is compatible with saline, Ringer's solution, lactated Ringer's solution, 5% and 10% dextrose (glucose), 10% fructose, and 5% dextrose (glucose) with 0.225% sodium chloride or 0.45% sodium chloride .

The solution obtained after mixing ciprofloxacin with compatible infusion solutions should be used as quickly as possible for microbiological reasons, as well as due to the sensitivity of the drug to light.

If compatibility with another infusion solution/preparation has not been confirmed, Tsiprobay infusion solution should be administered separately. Visible signs of incompatibility are precipitation, turbidity or discoloration of the solution.

Incompatibility occurs with all solutions/preparations that are physically or chemically unstable at the pH value of the Tsiprobay infusion solution (for example, penicillins, heparin solutions), and, in particular, with solutions that change the pH value to the alkaline side (the pH of the Tsiprobay infusion solution is 3.9-4.5).

Tsiprobay solution for infusion is photosensitive, so the bottle should be removed from the box only before use. In direct sunlight, the guaranteed stability of the solution is 3 days.

When storing Tsiprobay infusion solution at low temperatures, a precipitate may form, which dissolves at room temperature. Therefore, it is not recommended to store the infusion solution in the refrigerator.

Overdose

In cases of oral overdose, reversible toxic effects on the renal parenchyma have been observed in several cases. Therefore, in case of overdose, in addition to standard measures (gastric lavage, use of emetics, administration of large amounts of fluid, creation of an acidic urine reaction), it is also recommended to monitor kidney function and take magnesium- and calcium-containing antacids, which reduce the absorption of ciprofloxacin. Only a small amount of ciprofloxacin (less than 10%) is removed by hemo- or peritoneal dialysis. A specific antidote is unknown. It is necessary to carefully monitor the patient's condition, carry out routine emergency measures, and ensure sufficient fluid intake.