Ciprofloxacin (Solution for infusion)
Active material: Ciprofloxacin
When ATH: J01MA02
CCF: Fluoroquinolone antibacterial drug
ICD-10 codes (testimony): A40, A41, A54, J01, J02, J03, J04, J15, J20, J31, J32, J35.0, J37, J42, K65.0, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, M00, M86, N10, N11, N15.1, N30, N34, N41, N70, N71, N72, Z29.2
When CSF: 06.17.02.01
Manufacturer: Synthesis of (Russia)
Pharmaceutical form, composition and packaging
Solution for infusion clear, slightly yellowish or slightly greenish.
| 1 ml | 100 ml | |
| Ciprofloxacin | 2 mg | 200 mg |
Excipients: rr sodium chloride 0.9%, lactic acid, dinatrievaya soly ЭDTA, water d / and.
100 ml – vials of dark glass (1) – packs cardboard.
Pharmacological action
Antibacterial drug broad-spectrum fluoroquinolones from the Group. Effective bactericidal. The drug inhibits the enzyme DNA gyrase bacteria, as a result of which violated DNA replication and synthesis of cell proteins of bacteria. Ciprofloxacin acts as the breeding of microorganisms, and the rest are in phase.
Ciprofloxacin active against gram-negative aerobic bacteria: Escherichia coli, Salmonella spp., Shigella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Proteus is wonderful, Proteus vulgaris, Serratia wilting, Hafnia avenue, edwardsiella tarda, Providencia spp., Morganella morganii, Vibrio spp., Yersinia spp., Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.; intracellular pathogens: Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium-intracellular; Gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus man, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). Most Staphylococcus, resistant to metitillino, resistant to ciprofloxacin.
C drug moderately sensitive Streptococcus pneumoniae, Enterococcus faecalis.
C drug resistant Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroids.
The drug against Treponema pallidum unclear.
Pharmacokinetics
Absorption
After the on / in infusion at a dose of 200 mg or 400 mg Cmax achieved through 60 and m is 2.1 ug / ml 4.6 ug / ml, respectively.
Distribution
Plasma protein binding – 20-40%. Vd – 2-3 l / kg. Ciprofloxacin is widely distributed in body tissues (with the exception of tissues, rich in fats, eg, nervous tissue). The content of the antibiotic in the tissues 2-12 times higher, than in plasma. Therapeutic concentrations achieved in saliva, tonsils, liver, gallbladder, bile, intestine, abdominal organs and pelvis, uterus, seminal fluid, Prostate tissue, the endometrium, the fallopian tubes and ovaries, kidney and urinary organs, lung tissue, bronchial secretions, bone, muscle, synovial fluid and articular cartilage, perytonealnoy fluid, skin. In spinnomozgovu liquid penetrates into the small number of, wherein when the concentration of the non-inflamed meninges 6-10% from that in serum, and when inflamed – 14-37%. Ciprofloxacin is also well into the aqueous humor, bronchial secretion, Plevra, bryushynu, lymph, placenta. Ciprofloxacin concentration in blood neutrophils 2-7 times higher, than serum. ciprofloxacin somewhat reduced activity at acidic pH values.
Provided with breast milk.
Metabolism
It is metabolized in the liver (15-30%) with the formation of low metabolites (dijetilciprofloksacin, sul'fociprofloksacin, oksociprofloksacin, formilciprofloksacin).
Deduction
When on / in a T1/2 – 5-6 no. Displayed in the kidney by tubular filtration and tubular secretion as unchanged (at / in the introduction – 50-70%) and as metabolites (at / in the introduction – 10%), the rest of the – through blood. After the on / in the concentration in the urine during the first 2 hours after administration almost 100 times more, than serum, which significantly exceeds the MIC for most pathogens of urinary tract infections.
Renal clearance – 3-5 ml / min / kg; total clearance – 8-10 ml / min / kg.
Pharmacokinetics in special clinical situations
In chronic renal failure (CC>20 ml / min) percentage output from the formulation is reduced kidney, but not the accumulation in the body is due to a compensatory increase in drug metabolism and excretion through the gastrointestinal tract. T1/2 chronic renal failure increases to 12 no.
Testimony
Infectious-inflammatory diseases, chuvstvitelnymti due to malaria infections:
-respiratory tract;
-uha, nose and throat;
-pochek and urinary tract;
-polovyh bodies (incl. gonorrhea, prostatitis);
-ginekologicheskie (incl. adnexitis) and post-partum infections;
-pischevaritelnoy system (incl. oral, teeth, jaws);
-zhelchnogo bladder and biliary tract;
-kozhnyh covers, mucous membranes and soft tissues;
is the support-motor apparatus;
-sepsis;
-peritonit;
Prevention and treatment of infections in patients with reduced immunity (with immunosuppressive therapy).
Dosage regimen
The drug should be administered in / in infusion for 30 m (dose 200 mg) and 60 m (dose 400 mg). infusion solution can be combined with 0.9% sodium chloride solution, Ringer, 5% and 10% dextrose (Glucose), 10% fructose solution, solution, contains 5% Dextrose solution 0.225% or 0.45% sodium chloride solution.
Ciprofloxacin Dose depends on the severity of the disease, type of infection, condition of the body, age, weight and renal function of the patient.
A single dose of 200 mg, in severe infections – 400 mg. The frequency – 2 times / day; duration of treatment – 1-2 of the week, if necessary, may increase treatment.
At acute gonorrhoea drug administered in / in a single dose 100 mg.
To Prevention of postoperative infections – 30-60 minutes before surgery on / in a dose of 200-400 mg.
Patients with severe renal insufficiency (CC<20 ml / min / 1.73 m) necessary to appoint half of the daily dose.
Side effect
From the digestive system: nausea, diarrhea, vomiting, abdominal pain, flatulence, anorexia, cholestatic jaundice (especially in patients with pre-existing liver disease), hepatitis, gepatonekroz.
From the central and peripheral nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, “nightmarish” dreams, peripheral paralgezija (anomaly of the perception of pain), Sweating, intracranial hypertension, anxiety, confusion, depression, hallucinations, manifestations of psychotic reactions (sometimes progressing to state, in which the patient may cause harm), migraine, fainting, thrombosis of cerebral arteries.
From the senses: disorders of taste and smell, blurred vision (diplopia, change of color), noise in ears, hearing loss.
Cardio-vascular system: tachycardia, abnormal heart rhythm, decrease in blood pressure, rush of blood to the face.
From the hematopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, gemoliticheskaya anemia.
From the laboratory parameters: gipoprotrombinemii, increase in liver transaminases and alkaline phosphatase, giperkreatininemiя, giperʙiliruʙinemija, giperglikemiâ.
From the urinary system: hematuria, kristallurija (particularly in alkaline urine and low diureze), glomerulonephritis, dizurija, polyuria, urinary retention, albuminuria, Urethral bleeding, hematuria, azotvydelitel'noj reduced kidney function, interstitial nephritis.
On the part of the musculoskeletal system: arthralgia, arthritis, tendinitis, tendon rupture, myalgia.
Allergic reactions: itching, hives, bullation, accompanied by bleeding, papules, forming scabs, drug fever, pinpoint hemorrhages (petechiae), swelling of the face or larynx, breathlessness, eozinofilija, increased light sensitivity, vasculitis, Nodular Erythema, exudative erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
Local reactions: pain and burning sensation at the injection site, phlebitis.
Other: generalized weakness, superinfekcii (candidiasis, psevdomembranoznыy colitis).
Contraindications
-defitsit glucose-6-fosfatdegidrogenazы;
-psevdomembranozny colitis;
-Children Under the age of 18 years (until completion of the formation of the skeleton);
-pregnancy;
is the period of lactation (breast-feeding).
FROM caution should designate product if expressed farm cerebrovascular, cerebrovascular disorders, psychic diseases, sudorozhnom syndrome, epilepsy, renal and / or hepatic insufficiency, elderly patients.
Pregnancy and lactation
Ciprofloxacin is contraindicated during pregnancy and lactation (breast-feeding).
Cautions
If you encounter during or after the treatment with ciprofloxacin severe and prolonged diarrhea should exclude the diagnosis of pseudomembranous colitis, that requires the immediate withdrawal of the drug and the appropriate treatment.
If there pains in the tendons or at the first signs tenosynovitis treatment should cease.
The treatment period of ciprofloxacin is necessary to provide sufficient liquid under normal diuresis.
The treatment period of ciprofloxacin should avoid exposure to direct sunlight.
Effects on ability to drive vehicles and management mechanisms
Patients, receiving Ciprofloxacin, Use caution when driving and other potentially hazardous activities, require increased attention and psychomotor speed reactions (especially while drinking habits).
Overdose
Treatment: spetsificheskiy antidote unknown. It is necessary to carefully monitor the patient's condition, gastric lavage, make routine emergency measures, provide sufficient flow of fluid. With hemo- or peritoneal dialysis can only be inferred slight (less 10%) the amount of drug.
Drug Interactions
As a result of reduced activity processes mikrosomalnogo oxidation in gepatocitah, ciprofloxacin concentration increases and prolongs the half-life of theophylline and other xanthines (eg, caffeine), oral hypoglycemic drugs, anticoagulants, helps reduce prothrombin index.
In an application with NSAIDs (except acetylsalicylic acid) increases the risk of seizures.
Metoclopramide accelerates the absorption of ciprofloxacin, which reduces the time to maximum concentration of the latter.
Joint appointment urikozuricheskih drugs leads to slower excretion (to 50%) and increased plasma concentration of ciprofloxacin.
When combined with other antimicrobial drugs (beta-lactam antibiotics, aminoglikozidy, klindamiцin, metronidazol) usually observed synergy. Ciprofloxacin can therefore be used successfully in combination with ceftazidime and azlocillin in infections, caused by Pseudomonas spp.; with mezlocillinom, azlocillinom and other beta-lactam antibiotics – when streptococcal infections; with izoksazolpenicillinami and vankomitinom – When staphylococcal infections; with metronidazole and clindamycin – under anaerobic infections.
Ciprofloxacin usilivaet nefrotoksicheskoe action cyclosporine, also there is an increase in serum creatinine, therefore such patients should be monitored this indicator 2 times a week.
At the same time taking Ciprofloxacin increases the effects of anticoagulants.
Pharmaceutical interaction
The infusion of the drug solution is incompatible with all pharmaceutically infusion solutions and drugs, are physico-chemically unstable at an acidic medium (pH ciprofloxacin infusion solution – 3.5-4.6). You can not mix the solution for on / in the solutions with, having a pH of greater than 7.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored in the dark place at a temperature of from 5 ° to 20 ° C in the reach of children. Do not freeze! Shelf life – 2 year.
