Ciprolet®
Due to a decrease in the activity of microsomal oxidation processes in hepatocytes, it increases the concentration and lengthens the half-life of theophylline (and other xanthines, for example, caffeine), oral hypoglycemic drugs, indirect anticoagulants, and helps reduce the prothrombin index.
When combined with other antimicrobial drugs (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole), synergism is usually observed; can be successfully used in combination with azlocillin and ceftazidime for infections caused by Pseudomonas spp.;
with mezlocillin, azlocillin and other beta-lactam antibiotics - for streptococcal infections; with isoxazolylpenicillins and vancomycin - for staphylococcal infections; with metronidazole and clindamycin - for anaerobic infections.
Enhances the nephrotoxic effect of cyclosporine, an increase in serum creatinine is noted, in such patients it is necessary to monitor this indicator twice a week.
When used simultaneously, it enhances the effect of indirect anticoagulants.
The international normalized ratio (INR) should be monitored fairly frequently during co-administration with ciprofloxacin and for a short time after completion of combination therapy.
Non-steroidal anti-inflammatory drugs (excluding acetylsalicylic acid) increase the risk of developing seizures.
Combined use with uricosuric drugs leads to a slower elimination (up to 50%) and an increase in the plasma concentration of ciprofloxacin.
Increases the maximum concentration of tizanidine by 7 times (from 4 to 21) and the area under the concentration-time pharmacokinetic curve. The simultaneous use of probenecid and ciprofloxacin increases the concentration of ciprofloxacin in the blood plasma (probenecid slows down the rate of excretion of ciprofloxacin by the kidneys). With simultaneous use of ciprofloxacin, the renal metabolism of methotrexate may slow down, which may be accompanied by an increase in the concentration of methotrexate in the blood plasma (the likelihood of side effects of methotrexate increases).
Concomitant use of duloxetine and potent inhibitors of the CYP450 1A2 isoenzyme (such as fluvoxamine) may lead to an increase in the MIC and Cmax of duloxetine. Although there is no clinical data on possible interactions with ciprofloxacin, the likelihood of such an interaction can be anticipated when ciprofloxacin and duloxetine are used concomitantly.
The simultaneous use of ropinirole and ciprofloxacin, a moderate inhibitor of the CYP450 1A2 isoenzyme, leads to an increase in the Cmax and MIC of ropinirole by 60 and 84%, respectively. Monitor for side effects of ropinirole during co-administration with ciprofloxacin and for a short time after completion of combination therapy. The simultaneous use of lidocaine and ciprofloxacin leads to a decrease in the clearance of lidocaine by 22% when administered intravenously (increased side effects of lidocaine are possible. With the simultaneous use of clozapine and ciprofloxacin at a dose of 250 mg for 7 days, an increase in serum concentrations of clozapine and N-desmethylclozapine by 29% is possible and 31%. 2 times (use of this combination is possible only after assessing the benefit/risk ratio).
Ciprolet
Release form, composition and packaging
Solution for infusion in the form of a clear, colorless or light yellow liquid.
- 1 ml ciprofloxacin 2 mg
- 1 fl. ciprofloxacin 200 mg
Excipients: sodium chloride, lactic acid, disodium edetate, citric acid monohydrate, sodium hydroxide, hydrochloric acid, water for injection.
Clinical and pharmacological group: Antibacterial drug of the fluoroquinolone group
pharmachologic effect
Ciprofloxacin is an antimicrobial drug from the fluoroquinolone group.
The mechanism of action of ciprofloxacin is associated with the effect on DNA gyrase (topoisomerase) of bacteria, which plays an important role in the reproduction of bacterial DNA. The drug has a rapid bactericidal effect on microorganisms that are both in the stage of rest and reproduction.
The spectrum of action of ciprofloxacin includes the following types of gram(-) and gram(+) microorganisms:
E.coli, Shigella, Salmonella, Citrobacter, Klebsiella, Enterobacter, Serratia, Hafnia, Edwardsiella, Proteus (indole-positive and indole-negative), Providencia, Moprganella, Yersinia, Vibrio, Aeromonas, Plesiomonas, Pasteurella, Haemophilus, Campylobacter, Pseudomonas, Legionella, Neisseria , Moraxella, Branhamella, Acinetobacter, Brucella, Staphylococcus, Sreptococcus agalactiae, Listeria, Corynebacterium, Chlamydia.
Ciprofloxacin is effective against bacteria that produce beta-lactamases.
Sensitivity to ciprofloxacin varies among: Gardnerella, Flavobacterium, Alcaligenes, Streptococcus faecalis, Streptococcus pyogenes, Streptococcus pneumonia, Streptococcus viridans, Mycoplasma hominis, Mycobacterium tuberculosis, Mycobacterium fortuitum
Most often resistant: Streptococcus faecium, Ureaplasma urealyticum, Nocardia asteroides. Anaerobes, with some exceptions, are moderately sensitive (Peptococcus, Peptostreptococcus) or resistant (Bacteroides).
Ciprofloxacin has no effect on Treponema pallidum and fungi.
Resistance to ciprofloxacin develops slowly and gradually; plasmid resistance is absent.
Ciprofloxacin is active against pathogens resistant, for example, to betalactam antibiotics, aminoglycosides or tetracyclines.
Pharmacokinetics
After intravenous administration of ciprofloxacin, a high concentration in the blood plasma (up to 4 mcg/ml) is achieved within 20-30 minutes. Binding to plasma proteins is negligible (20-40%). Volume of distribution - 2-3 l/kg.
Ciprofloxacin penetrates well into organs and tissues. Approximately 2 hours after ingestion or intravenous administration, it is found in tissues and body fluids in concentrations many times higher than in blood serum. Ciprofloxacin is excreted from the body mainly unchanged, mainly through the kidneys. The plasma half-life after both oral and intravenous administration is 3 to 5 hours.
Significant amounts of the drug are also excreted in bile and feces, so only significant impairment of renal function leads to a slower elimination.
Indications
Treatment of uncomplicated and complicated infections caused by pathogens sensitive to the drug:
- respiratory tract infections. For outpatient treatment of pneumococcal pneumonia, ciprofloxacin is not a first-line drug, but it is indicated for pneumonia caused, for example, by Klebsiella, Enterobacter, bacteria of the genus Pseudomonas, Haemophilus influenzae, bacteria of the genus Branhamella, Legionella, Staphylococcus;
- infections of the middle ear and paranasal sinuses, especially if they are caused by gram-negative bacteria, including bacteria of the genus Pseudomonas, or staphylococci;
- eye infections;
- kidney and urinary tract infections;
- skin and soft tissue infections;
- bone and joint infections;
- infections of the pelvic organs (including adnexitis and prostatitis); gonorrhea; gastrointestinal infections;
- infections of the gallbladder and biliary tract;;
- peritonitis;
- sepsis.
Prevention and treatment of infections in patients with reduced immunity (for example, during treatment with immunosuppressants and neutropenia);
Selective intestinal decontamination during treatment with immunosuppressants.
Dosage regimen
In the absence of special prescriptions from a doctor, the following approximate doses are recommended:
Indications for use / Single/daily doses for adults
Uncomplicated lower and upper urinary tract infections / 2 x 100 mg
Complicated urinary tract infections (depending on severity) / 2 x 200 mg
Respiratory tract infections / 2 x 200-400 mg
Other infections / 2 x 200-400 mg
Acute gonorrhea and acute uncomplicated cystitis in women can be treated with a single dose of 200 mg (intravenously).
For urinary tract infections, including acute uncomplicated gonorrhea, ciprofloxacin can be administered intravenously at a dose of 100 mg 2 times a day.
For respiratory tract infections, depending on the severity and pathogen, ciprofloxacin is administered at a dose of 200-400 mg 2 times a day, for other infections - 200-400 mg 2 times a day. As the patient's condition improves, they switch to taking the drug orally.
Patients with impaired renal function:
When creatinine clearance is less than 20 ml/min (or serum creatinine level is above 3 mg/100 ml), the following is prescribed: 2 times a day half the standard dose or 1 time a day the full standard dose.
Patients with liver dysfunction:
No dose adjustment is required.
Patients on peritoneal dialysis:
For peritonitis, ciprofloxacin is prescribed orally at a dose of 0.5 g 4 times a day or the drug is added in the form of a solution for infusion at a dose of 0.05 g 4 times a day per 1 liter of dialysate intraperitoneally.
Duration of use:
The duration of treatment depends on the severity of the disease, clinical course and results of bacteriological examination.
The presence of Tsiprolet in two dosage forms allows you to begin treatment of severe infections intravenously and continue it orally.
It is recommended to continue treatment for at least 3 days after the temperature normalizes or clinical symptoms disappear. The duration of treatment for acute uncomplicated gonorrhea and cystitis is 1 day. For infections of the kidneys, urinary tract and abdominal cavity - up to 7 days. For osteomyelitis, the course of treatment can be up to 2 months. For other infections, the course of treatment is 7-14 days. In patients with reduced immunity, treatment is carried out throughout the entire period of neutropenia.
Mode of application:
The infusion duration should be 30 minutes at a dose of 200 mg and 60 minutes at a dose of 400 mg. The drug solution can be administered undiluted or after adding to other infusion solutions.
Ciprofloxacin solution contains 0.9% sodium chloride and is compatible with the following infusion solutions: 0.9% sodium chloride solution, Ringer's solution, and Hartmann's lactated Ringer's solution, 5% and 10% glucose solutions, 10% fructose solution, and 5 % glucose solution containing 0.225% or 0.45% sodium chloride.
Side effect
Ciprofloxacin is well tolerated by patients. The following, usually reversible, side effects may occur during treatment with ciprofloxacin:
From the cardiovascular system: in very rare cases - tachycardia, hot flashes, migraine, fainting.
From the gastrointestinal tract and liver: nausea, vomiting, diarrhea, digestive disorders, abdominal pain, flatulence, lack of appetite.
From the nervous system and psyche: dizziness, headache, fatigue, insomnia, agitation, tremor; in very rare cases: peripheral sensory disturbances, sweating, unsteady gait, seizures, feelings of fear and confusion, nightmares, depression, hallucinations, disturbances of taste and smell, visual disturbances (diplopia, chromatopsia), tinnitus, temporary hearing loss especially in high sounds. If these reactions occur, you should immediately discontinue the drug and notify your doctor.
From the hematopoietic system: eosinophilia, leukopenia, thrombocytopenia, very rarely - leukocytosis, thrombocytosis, hemolytic anemia.
Allergic and immunopathological reactions: skin rashes, itching, drug fever, as well as photosensitivity; rarely - Quincke's edema, bronchospasm, arthralgia; very rarely - anaphylactic shock, myalgia, Stevens-Johnson syndrome, Lyell's syndrome, interstitial nephritis, hepatitis.
Local reactions: phlebitis
