Ciprobide - instructions for use, dose, side effects, contraindications

Antimicrobial preparation of a broad spectrum of action from the group of fluoroquinolones. It is bactericidal. The drug inhibits the DNA enzyme enzyme of bacteria, as a result of which DNA replication and the synthesis of bacterial cell proteins are disrupted. Ciprofloxacin It acts both on multiplying microorganisms, and on those in the resting phase.

Gram-negative aerobic bacteria are sensitive to ciprofloxacin: enterobacteria (Escherichia coli, Salmonella spp., Shigella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Proteus mirabilis, Proteus vulgaris, Serratia marcescens, Hafnia alvei, Edwardsiella tarda, Providencia spp. , Morganella morganii, Vibrio spp., Yersinia spp.), Other gram-negative bacteria (Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.); some intracellular pathogens: Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium-intracellulare.

Gram-positive aerobic bacteria are also sensitive to ciprofloxacin: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin.

The sensitivity of bacteria Streptococcus pneumoniae, Enterococcus faecalis is moderate.

The drug is resistant Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. The effect of the drug on Treponema pallidum insufficiently studied.

Pharmacokinetics:

After intravenous infusion of 200 mg or 400 mg, the time to reach the maximum concentration (TC_max) - 60 min, the maximum concentration (C_max) Were 2.1 μg / ml and 4.6 μg / ml, respectively. The volume of distribution is 2-3 l / kg, the connection with plasma proteins is 20-40%.

Well distributed in body tissues (excluding tissue, rich in fats, for example, nervous tissue). The content in the tissues is 2-12 times higher than in the plasma. Therapeutic concentrations are achieved in saliva, tonsils, liver, gall bladder, bile, intestine, abdominal and pelvic organs, uterus, seminal fluid, prostate tissue, endometrium, fallopian tubes and ovaries, kidney and urinary organs, pulmonary tissue, bronchial secretion, bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin.The cerebrospinal fluid penetrates in a small amount, where its concentration in uninflated cerebral membranes is 6-10% of that in the serum, and when inflamed - 14-37%. Ciprofloxacin also well penetrates into the eye fluid, bronchial secretion, pleura, peritoneum, lymph, through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in serum. The activity decreases slightly at acidic pH values.

Metabolised in the liver (15-30%) with the formation of low-activity metabolites (diethylciprofloxacin, sulfociprofloxacin, oxocycloploxacin, formyl ciprofloxacin).

With intravenous administration, the half-life period (T1) is 5-6 hours, with chronic renal insufficiency up to 12 hours. It is excreted mainly by the kidneys through tubular filtration and tubular secretion in an unchanged form (with intravenous administration 50-70%) and in the form of metabolites (with intravenous administration - 10%), the rest - through the gastrointestinal tract. A small amount is excreted in breast milk. After intravenous administration, the concentration in the urine during the first 2 hours after administration is almost 100 times greater than in the serum, which significantly exceeds the maximum limit concentration for most pathogens of urinary tract infections.

Kidney clearance - 3-5 ml / min / kg, total clearance - 8-10 ml / min / kg.

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

Indications:

Infectious-inflammatory diseases caused by microorganisms susceptible to ciprofloxacin: lower respiratory tract; ear, nose and throat; kidney and urinary tract; genital organs (gonorrhea, prostatitis); gynecological (adnexitis) and postpartum infections; gastrointestinal tract (including the mouth, teeth, jaws); gallbladder and bile ducts; skin, mucous membranes and soft tissues; musculoskeletal system.

Ciprofloxacin is indicated for treatment of peritonitis and sepsis, as well as for the prevention and treatment of infections in patients with reduced immunity (for immunosuppressive therapy, neutropenia).

Prevention and treatment of pulmonary form of anthrax.

Contraindications:

Hypersensitivity to fluoroquinolones, deficiency of glucose-6-phosphate dehydrogenase, pseudomembranous colitis,Children's age (up to 18 years - the completion of the formation of the skeleton), pregnancy, lactation, the reception of tizanidine.

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, convulsive syndrome, epilepsy, marked renal and / or hepatic insufficiency, elderly age.

Dosing and Administration:

The drug should be administered intravenously drip for 30 minutes (200 mg) and 60 minutes (400 mg). The infusion solution can be combined with 0.9% sodium chloride solution, Ringer's solution, 5% and 10% dextrose solution, 10% fructose solution, and also a solution containing 5% dextrose solution with 0.225% or 0.45% sodium chloride solution .

The dose of ciprofloxacin depends on the severity of the disease, the type of infection, the body's condition, age, weight and kidney function in the patient. Recommended doses are usually: for intravenous administration, a single dose of 200 mg (in severe infections - 400 mg), the frequency of administration is 2 times / day, the duration of treatment depends on the severity of the disease - 1-2 weeks, if necessary and more.

In acute gonorrhea - once intravenously, 100 mg.

With peritonitis, sepsis, infection of bones and joints - 400 mg 3 times / day.

Pulmonary form of anthrax - 400 mg 2 times / day.

For the prevention of postoperative infections - for 30-60 minutes before the operation, intravenously, 200-400 mg.

Patients with severe renal insufficiency (creatinine clearance below 20 ml / min / 1.73 m 2) should be prescribed half the daily dose.

Side effects:

From the digestive system: nausea, diarrhea, vomiting, abdominal pain, flatulence, anorexia, cholestatic jaundice (especially in patients with liver disease), hepatitis, hepatonecrosis.

From the nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, nightmarish dreams, peripheral paralysis (anomaly of perception of pain), sweating, increased intracranial pressure, confusion, depression, hallucinations, and other manifestations of psychotic reactions (occasionally progressing to conditions in which the patient can do harm to himself), migraine, fainting, thrombosis of the cerebral arteries.

From the sense organs: violation of taste and smell, visual impairment (diplopia, change in color perception), tinnitus, hearing loss.

From the cardiovascular system: tachycardia, violation of the heart rate, lowering blood pressure, flushing of blood to the skin of the face.

From the hematopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia, agranulocytosis.

From the laboratory indicators: hypoprothrombinemia, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, hyperglycemia.

From the urinary system: hematuria, crystalluria (especially in alkaline urine and low diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, albuminuria, urethral bleeding, decreased renal nitrogen function, interstitial nephritis.

From the musculoskeletal system: arthralgia, edema in the joint, arthritis, tendovaginitis, tendon ruptures, myalgia.

Allergic reactions: itching, urticaria, the formation of blisters accompanied by bleeding, and small nodules forming scabs, drug fever, pinpoint hemorrhages (petechiae), edema of the face or larynx, dyspnea, eosinophilia, vasculitis, nodal erythema, exudative erythema multiforme,Stevens-Johnson syndrome (malignant exudative erythema), toxic epidermal necrolysis (Lyell's syndrome), anaphylactic shock.

Local reactions: pain and burning at the injection site, phlebitis.

Other: superinfection (candidiasis, pseudomembranous colitis), general weakness, increased photosensitivity.

Overdose:

The specific antidote is unknown. It is necessary to carefully monitor the patient's condition, make gastric lavage, carry out usual emergency measures, ensure sufficient fluid intake. With the help of hemo- or peritoneal dialysis, only a small amount (less than 10%) of the drug can be excreted.

Interaction:

Due to the decrease in the activity of microsomal oxidation in hepatocytes, it increases the concentration and prolongs T1 / 2 theophylline (and other xanthines, for example, caffeine), oral hypoglycemic drugs, indirect anticoagulants, and helps to reduce the prothrombin index. Non-steroidal anti-inflammatory drugs (excluding acetylsalicylic acid) increase the risk of seizures.

Metoclopramide accelerates absorption, which leads to a decrease in the time to reach its maximum concentration (C_max).

Joint appointment of uricosuric drugs leads to a delay in excretion (up to 50%) and an increase in the plasma concentration of ciprofloxacin.

When combined with other antimicrobial agents (beta-lactams, aminoglycosides, clindamycin, metronidazole) synergy is usually observed; can be successfully used in combination with azlocillin and ceftazidime in infections caused by Pseudomonas spp .; with mezlocillin, azlocillin, etc. beta-lactam antibiotics - with streptococcal infections; with isoxazole penicillins and vancomycin - with staphylococcal infections; with metronidazole and clindamycin - with anaerobic infections.

Increases in 7 times the maximum concentration of tizanidine, which increases the risk of pronounced reduction in blood pressure and drowsiness.

Increases the nephrotoxic effect of cyclosporine, there is an increase in serum creatinine, so these patients need to monitor this indicator 2 times a week.

With simultaneous reception increases the effect of indirect anticoagulants. The infusion solution is pharmaceutically incompatible with all infusion solutions and preparations,which are physico-chemically unstable under acidic conditions (the pH of the infusion solution of ciprofloxacin is 3.5-4.6). Do not mix the intravenous solution with solutions that have a pH of more than 7.

Special instructions:

Ciprofloxacin is not recommended for use in children under 18 years of age for the treatment of other infectious diseases other than treatment and prevention of pulmonary anthrax (after suspected or proven infection with Bacillus anthracis) (in children 5-17 years of age) as follows: 10 mg / kg body weight , iv twice a day. Do not exceed the maximum single dose of 400 mg IV (the maximum daily dose is 800 mg). The total duration of treatment with ciprofloxacin in pulmonary form of anthrax is 60 days.

If a severe and prolonged diarrhea occurs during or after treatment with ciprofloxacin, the diagnosis of pseudomembranous colitis should be excluded, which requires immediate discontinuation of the drug and the appointment of appropriate treatment.

If pain occurs in the tendons or when the first signs of tendovaginitis appear, treatment should be discontinued.

During the treatment with ciprofloxacin it is necessary to provide a sufficient amount of fluid while observing a normal diuresis.

During treatment with ciprofloxacin, contact with direct sunlight should be avoided.

Effect on the ability to drive transp. cf. and fur:

Patients receiving ciprofloxacin, caution should be exercised when driving a car and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions (especially with simultaneous use of alcohol).

Form release / dosage:Solution for infusions 2 mg / ml.

Packaging:

For 100 ml in a glass vial for infusion type 1 F. US with a label on the outer surface. The bottle is equipped with a polyethylene holder. For 100 ml in a sealed bottle of low density polyethylene with a measuring scale on the outer surface of the ring - holder at the bottom of the bottle, with a plastic cover. The bottle is placed in a sealed plastic bag.

Each vial with instructions for use packaged in cardboard tutu.

Storage conditions:

At a temperature of no higher than 25 ° C, in a place protected from light.

Do not freeze.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012788 / 01

Date of registration:19.12.2007

The owner of the registration certificate:Cadil Haltkar Co., Ltd.Cadil Haltkar Co., Ltd. India

Manufacturer: & nbsp

CADILA HEALTHCARE, Ltd. India

Representation: & nbspCADILA HELTKER LTD. CADILA HELTKER LTD. India

Information update date: & nbsp23.10.2015

Illustrated instructions

Instructions

Ciprobide (Ciprobid)