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

Excipients (core): crospovidone - 7 mg, microcrystalline cellulose - 43.9 mg, povidone (polyvinylpyrrolidone) - 16.3 mg, magnesium stearate - 3.7 mg, corn starch -13.0 mg. Auxiliary substances (shell): hypromellose - 8.5 mg, titanium dioxide - 4.5 mg, macrogol - 2.0 mg.

Description:

Tablets are cylindrical, biconvex, without risks, covered with a film shell of white or almost white color, on the fracture of white or white with a yellowish hue.

Pharmacotherapeutic group:Antimicrobial agent, fluoroquinolone.

ATX: & nbsp

J.01.M.A.02 Ciprofloxacin

Pharmacodynamics:

A broad-spectrum antimicrobial agent, a quinolone derivative, inhibits bacterial DNA-gyrase (topoisomerases II and IV,responsible for the process of supercoiling the chromosomal DNA around the nuclear RNA, which is necessary for reading the genetic information), violates DNA synthesis, growth and division of bacteria; causes significant morphological changes (including the cell wall and membranes) and the rapid death of the bacterial cell.

It acts bactericidal against gram-negative microorganisms in the period of rest and division (since it affects not only the DNA-gyre, but also causes lysis of the cell wall), gram-positive microorganisms - only during the fission period.

Low toxicity for macroorganism cells is explained by the absence of DNA-gyrase in them. Against the background of taking ciprofloxacin, there is no parallel development of resistance to other antibiotics that do not belong to the group of DNA-gyrase inhibitors, which makes it highly effective against bacteria that are resistant, for example, to aminoglycosides, penicillins, cephalosporins, tetracyclines.

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., Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii.

Gram-positive aerobic bacteria: Staphylococcus spp.(Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). Bacillus anthracis is also sensitive to ciprofloxacin.

The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin. Sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) - moderate (high concentrations are required to repress).

For drug resistant: Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. It is effective against Treponema pallidum. Resistance develops very slowly, because on the one hand, after the action of ciprofloxacin are left with persistent microorganisms, and on the other - the bacterial cells do not have the enzymes that inactivate it.

Pharmacokinetics:

When taken orally, it is quickly and fairly fully absorbed from the gastrointestinal tract (mainly in the 12-finger and jejunum). Eating slows down absorption, but does not change the maximum concentration (C_max) and bioavailability. Bioavailability - 50-85%, volume of distribution - 2-3.5 l / kg, communication with plasma proteins - 20-40%. Time to reach the maximum concentration (TC_max) with oral intake - 60-90 min, C_max linearly depends on the value of the dose taken and is at doses of 250, 500, 750 and 1000 mg, respectively, 1.2, 2.4, 4.3 and 5.4 μg / ml.After 12 hours after ingestion of 250, 500 and 750 mg the concentration of the drug in the plasma is reduced to 0.1, 0.2 and 0.4 μg / ml, respectively.

Well distributed in body tissues (excluding tissue, rich in fats, for example, nervous tissue). Concentration in tissues is 2-12 times higher than in plasma. Therapeutic concentrations are achieved in saliva, tonsils, liver, gall bladder, bile, intestine, abdominal and pelvic organs (endometrium, fallopian tubes and ovaries, uterus), seminal fluid, prostate tissue, kidney and urinary organs, lung 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 the absence of inflammation of the meninges is 6-10% of that in the serum, and when inflamed - 14-37%. Ciprofloxacin well penetrates also into the eye fluid, pleura, peritoneum, lymph, through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in blood serum. Metabolised in the liver (15-30%) with the formation of low-activity metabolites (diethylciprofloxacin, sulfociprofloxacin, oxocycloploxacin, formyl ciprofloxacin).

The half-life period (T1 / 2) is about 4 hours, with chronic renal insufficiency up to 12 hours. It is mainly excreted by the kidneys by tubular filtration and tubular secretion unchanged (40-50%) and metabolites (15%), the rest part - through the gastrointestinal tract. A small amount is excreted in breast milk. Kidney clearance - 3-5 ml / min / kg; total clearance - 8-10 ml / min / kg.

In chronic renal failure (creatinine clearance (CC) higher than 20 ml / min) percentage of ciprofloxacin outputted through the kidneys is reduced, but the accumulation in the body is not due to compensatory increase ciprofloxacin metabolism and excretion through the gastrointestinal tract.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms:

diseases of the lower respiratory tract (acute and chronic (at the stage of exacerbation) bronchitis, pneumonia, bronchiectatic disease, infectious complications of cystic fibrosis);
infection of the ENT organs (acute sinusitis);
infection of the kidneys and urinary tract (cystitis, pyelonephritis);
complicated intra-abdominal infections (in combination with metronidazole);
chronic bacterial prostatitis;
uncomplicated gonorrhea;
typhoid fever,
infectious diarrhea, including campylobacteriosis, shigellosis, diarrhea of "travelers";
infections of the skin and soft tissues (infected ulcers, wounds, burns, abscesses, phlegmon);
bones and joints (osteomyelitis, septic arthritis);
infection against the background of immunodeficiency (arising in the treatment of immunosuppressive drugs or in patients with neutropenia);
prevention and treatment of pulmonary form of anthrax.

Children.

treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs from 5 to 17 years;
prevention and treatment of pulmonary form of anthrax (infection with Bacillus anthracis).

Contraindications:

Hypersensitivity, simultaneous administration with tizanidine (risk of pronounced reduction in blood pressure, drowsiness), age to 18 years (until completion of the skeletal process, except for the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs from 5 to 17 years old, prevention and treatment of pulmonary form anthrax), pregnancy, lactation.

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, epilepsy, marked renal and / or hepatic insufficiency, tendon damage with previous treatment with fluoroquinolones, elderly age.

Dosing and Administration:

Inside. Tablets should be swallowed whole with a small amount of liquid after eating. When taking a tablet on an empty stomach, the active substance is absorbed more quickly.

For infections of the lower respiratory tract of light and medium degree - 0.5 g 2 times a day, in severe cases - 0.75 g 2 times. The course of treatment is 7-14 days.

For acute sinusitis - 0.5 g 2 times a day. The course of treatment is 10 days.

With infection of the skin and soft tissues of mild and moderate degree - 0.5 g 2 once a day, with a heavy current-0.75 g 2 times. The course of treatment is 7-14 days.

When infections of bones and joints - light and medium degree - 0.5 g2 times a day, with a heavy current -0.75 g 2 times. The course of treatment - up to 4-6 weeks.

With infections of the urinary tract - 0.25-0.5 g 2 times a day; course of treatment - 7-14 days, with uncomplicated cystitis in women - 3 days.

With chronic bacterial prostatitis - 0.5 g 2 times, the course of treatment - 28 days.

With uncomplicated gonorrhea - 0.25-0.5 g once.

Infectious diarrhea - 0.5 g 2 times, the course of treatment - 5-7 days. With typhoid fever - 0.5 g 2 times; course of treatment - 10 days.

With complicated intra-abdominal infections - 0.5 g every 12 hours for 7-14 days.

For the prevention and treatment of pulmonary form of anthrax - 0.5 g 2 times a day for 60 days.

Other infections (see"Indications for use") - 0.5 g 2 times a day.

In pediatrics:

in the treatment of complications caused by Pseudomonas aeruginosa, in children with cystic fibrosis of the lungs from 5 to 17 years - 20 mg / kg 2 times a day (maximum dose 1.5 g).

Duration of treatment is 10-14 days.

With a pulmonary form of anthrax (prevention and treatment) - 15 mg / kg 2 times a day.

The maximum single dose is 0.5 g, the daily dose is 1 g. The total duration of taking ciprofloxacin is 60 days.

Chronic renal failure: with QC greater than 50 ml / min dose adjustment is not required; with KK 30-50 ml / min - 0.25-0.5 every 12 hours; with CC 5-29 ml / min - 0.25-0.5 g every 18 hours if the patient hemodialysis or peritoneal dialysis -. 0.25-0.5 g / day, but should take the drug after hemodialysis.

Side effects:

On the part of the digestive system: nausea, diarrhea, vomiting, abdominal pain, flatulence, decreased appetite, cholestatic jaundice (especially in patients with liver disease), hepatitis, hepatonecrosis.

From the nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, "nightmarish" dream, peripheral paralgeziya (anomaly perception feelings of pain), increased sweating, increased intracranial pressure, confusion,depression, hallucinations, as well as 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 senses: a violation of taste and smell, visual impairment (diplopia, change in color perception), noise in the ears, hearing loss.

Cardio-vascular system: tachycardia, cardiac arrhythmias, lowering blood pressure.

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

Laboratory indices: hypoprothrombinemia, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, hyperglycemia.

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

Allergic reactions: itching, hives, blistering, accompanied by bleeding,and the appearance of small nodules that form scabs, drug fever, puncture of the face or larynx, dyspnea, eosinophilia, vasculitis, erythema nodosum, multiforme erythema exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

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

Other: asthenia, increased photosensitivity, superinfections (candidiasis, pseudomembranous colitis), "tides" of blood to the face.

Overdose:

Treatment: a specific antidote is unknown. Gastric lavage and other emergency measures, careful monitoring of the condition patient, ensuring 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 lengthens T1 / 2 theophylline (and other xanthines, for example, caffeine), oral hypoglycemic drugs, indirect anticoagulants, and helps to reduce the prothrombin index.

When combined with other antimicrobial drugs (beta-lactam antibiotics, 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 and other beta-lactam antibiotics - with streptococcal infections; with isoxazolylpenicillins and vancomycin - with staphylococcal infections; from metronidazole and clindamycin - in anaerobic infections.

Increases the nephrotoxic effect of cyclosporine, there is an increase in serum creatinine, in such patients monitoring of this indicator is required 2 times a week.

With simultaneous reception increases the effect of indirect anticoagulants.

Oral administration together with iron-containing drugs, sucralfate and antacid drugs containing magnesium, calcium, aluminum ions, leads to a decrease in absorption of ciprofloxacin, therefore it should be prescribed 1-2 hours before or 4 hours after the administration of the above medicines.

Non-steroidal anti-inflammatory drugs (excluding acetylsalicylic acid) increase the risk of seizures.

Didanosine reduces the absorption of ciprofloxacin due to the formation of complexes with dinanosine-containing ions of calcium, iron and magnesium.

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

The combined use of uricosuric drugs leads to slower elimination (50%) and increase plasma concentration of ciprofloxacin.

Increases C_max 7 times (from 4 to 21 times) and the area under the pharmacological concentration-time curve (AUC) is 10 times (6 to 24 times) of tizanidine, which increases the risk of pronounced reduction in blood pressure and drowsiness.

Special instructions:

Ciprofloxacin is not a drug of choice in suspected or established pneumonia caused by Streptococcus pneumoniae.

To avoid the development of crystalluria, exceeding the recommended daily dose is inadmissible, adequate fluid intake and maintenance of acid urine reaction are also necessary.

Patients with epilepsy, seizures in the anamnesis, vascular diseases and organic brain damage, in connection with the threat of development of adverse reactions from the central nervous system ciprofloxacin should be prescribed only for "vital" indications.

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

When pain occurs in the tendons or the first signs of tendovaginitis treatment should be discontinued (individual cases of inflammation and even rupture of tendons during treatment with fluoroquinolones are described).

During the treatment should avoid UV-irradiation (including contact with direct sunlight).

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

During treatment, one should refrain from engaging in potentially dangerous activities that require increased attention and speed of mental and motor reactions.

Form release / dosage:

Tablets, film-coated 250 mg.

Packaging:10 tablets are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil printed lacquered. For 20, 30, 40, 50, 60 or 100 tablets are placed in a polymer container for medicinal products. 1 container or 1, 2, 3,4 or 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N003190 / 01

Date of registration:21.11.2008

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Ciprofloxacin (Ciprofloxacin)