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

Active substance: ciprofloxacin hydrochloride monohydrate - 295 mg / 590 mg / 885 mg (in terms of ciprofloxacin 250 mg / 500 mg / 750 mg, respectively);

Excipients: corn starch - 3.6 mg / 7.2 mg / 10.8 mg, pregelatinized starch (starch 1500) - 10.0 mg / 20.0 mg / 30.0 mg, crospovidone (clolidone CL-M, collidine CML ) - 7.7 mg / 15.4 mg / 23.1 mg, lactose monohydrate (sugar, tablet) - 13.3 mg / 26.6 mg / 39.9 mg, microcrystalline cellulose 39.2 mg / 78 , 4 mg / 117.6 mg, talc 7.4 mg / 14.8 mg / 22.2 mg, magnesium stearate 3.8 mg / 7.6 mg / 11.4 mg.

Sheath: Hypromellose (hydroxypropylmethylcellulose, hydroxypropyl methylcellulose, methocel) 3.4 mg / 6.8 mg / 10.2 mg, macrogol 4000 (polyethylene oxide 4000, polyethylene glycol 4000) 1.3 mg / 2.6 mg / 3.9 mg, propylene glycol- 1.6 mg / 3.2 mg / 4.8 mg, talc 0.5 mg / 1.0 mg / 1.5 mg, copovidone (kollidone VA 64, collidine BA-64) 1.6 mg / 3 , 2 mg / 4.8 mg, titanium dioxide (titanium dioxide) -1.6 mg / 3.2 mg / 4.8 mg.

Description:

Tablets of white or almost white color, biconvex, covered with a film membrane, on the cross-section one layer of white is visible. Tablets of 250 mg of round form, tablets of 500 mg and 750 mg are oval.

Pharmacotherapeutic group:Antimicrobial agent, fluoroquinolone.

ATX: & nbsp

J.01.M.A.02 Ciprofloxacin

Pharmacodynamics:

A broad-spectrum antimicrobial agent, a quinolone derivative, suppresses 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 out genetic information), disrupts 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 on gram-negative organisms during rest and division (because it affects not only the DNA-gyrase, 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 inhibitors of gyrase, which makes it highly effective against bacteria that are resistant, for example, to aminoglycosides, penicillins, cephalosporins, tetracyclines and many other antibiotics.

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). It is active against Bacillus anthracis in vitro.

The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin. The sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) is moderate (their suppression requires high concentrations).

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 sufficiently absorbed from the gastrointestinal tract (GIT) (mainly in the 12-finger and jejunum). Food intake slows down absorption, but does not change the maximum concentration (C_max) and bioavailability.Bioavailability is 50-85%, the volume of distribution is 2-3.5 l / kg, the connection with plasma proteins is 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 1.2, 2.4, 4.3 and 5.4 μg / ml, respectively, at doses of 250, 500, 750 and 1000 mg, respectively. 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.

Ciprofloxacin is well distributed in the tissues of the body (excluding tissue rich in fats, for example, nerve 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, pulmonary tissue, bronchial secretion , bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin. In the cerebrospinal fluid (CSF) penetrates in a small amount, where its concentration in the absence of inflammation of the meninges is 6-10 % from that in the blood serum, and when inflamed - 14-37%. Ciprofloxacin well penetrates also 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 blood serum.

The activity is somewhat reduced at pH values less than 6.

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

The half-life period (T1) is about 4 hours, with chronic renal failure (CRF) up to 12 hours. It is excreted mainly by the kidneys through tubular filtration and tubular secretion unchanged (40-50%) and metabolites (15%), The rest is through the digestive tract. A small amount is excreted in breast milk.

Kidney clearance - 3-5 ml / min / kg; total clearance - 8-10 ml / min / kg. With CRF (creatinine clearance (CC) 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:

Bacterial infections caused by susceptible microorganisms:

diseases of the lower respiratory tract (acute and chronic (in the stage
exacerbations) bronchitis, pneumonia, bronchoectatic 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, 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 (LS) or in patients with neutropenia);
prevention and treatment of pulmonary form of anthrax (infection with Bacillus anthracis.

Children.

Therapy 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 reception with tizanidine (risk of pronounced reduction in blood pressure (BP), drowsiness), age to 18 years (except for the 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, infected with Bacillus anthracis), lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation, mental illness, epilepsy, severe renal and / or hepatic insufficiency, elderly age, tendon lesions with previous fluoroquinolone therapy.

Pregnancy and lactation:

The drug is contraindicated in pregnancy and lactation.

Dosing and Administration:

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

For infections of the lower respiratory tract of mild and moderate degree - 500 mg 2 times a day, with severe current - 750 mg 2 times a day. The course of treatment is 7-14 days.

For acute sinusitis, 500 mg twice a day. The course of treatment is 10 days.

With infection of the skin and soft tissues of mild and moderate degree - 500 mg 2 times a day, with severe current - 750 mg 2 times a day. The course of treatment is 7-14 days.

When infections of bones and joints - light and medium degree - 500 mg 2 times a day, with severe current - 750 mg 2 times a day. The course of treatment - up to 4-6 weeks.

With infections of the urinary tract - 250-500 mg 2 times a day; course of treatment - 7-l4 days, with uncomplicated cystitis in women - 3 days.

With chronic bacterial prostatitis - 500 mg 2 times a day, treatment course - 28 days.

With uncomplicated gonorrhea - 250-500 mg once.

Infectious diarrhea - 500 mg 2 times a day, the course of treatment - 5-7 days.

With typhoid fever, 500 mg twice a day; course of treatment - 10 days. -

With complicated intra-abdominal infections - 500 mg every 12 hours for 7-14 days.

For prevention and treatment of pulmonary form of anthrax - 500 mg twice a day for 60 days.

CRF: with QC more than 50 ml / min dose adjustment is not required; with KK 30-50 ml / min - 250-500 mg every 12 hours; with QC 5-29 ml / min - 250-500 mg every 18 hours. If the patient is undergoing hemodialysis or peritoneal dialysis - 250-500 mg / day, but the drug should be taken after a hemodialysis session.

In pediatrics:

in the treatment of complications caused by Pseudomonas aeruginosa, in children with cystic fibrosis of 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 pulmonary form of anthrax (prevention and treatment) - 15 mg / kg 2 times a day. The maximum single dose is 500 mg, the daily dose is 1 g.The total duration of taking ciprofloxacin is 60 days.

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 side of the nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, nightmarish dreams, peripheral paralysis (anomaly of perception of pain), 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.

On the part of the sense organs: a violation of taste and smell, visual impairment (diplopia, change in color perception), noise in the ears, hearing loss.

From the cardiovascular system: tachycardia, cardiac rhythm disturbances, lowering of arterial pressure, thrombosis of cerebral arteries.

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

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

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

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

Allergic reactions: skin itching, urticaria, the formation of blisters accompanied by bleeding, and the appearance of small nodules that form scabs, drug fever, pinpoint hemorrhages on the skin (petechiae), edema of the face or larynx, dyspnea, eosinophilia, vasculitis, erythema nodosum, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

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

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Treatment: a specific antidote is unknown. Gastric lavage and other emergency measures, careful monitoring of the patient's condition, 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 a decrease in the activity of microsomal oxidation in hepatocytes ciprofloxacin increases the concentration and lengthens T1 theophylline (and other xanthines, for example, caffeine), oral hypoglycemic drugs, anticoagulant means of indirect action, 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; with metronidazole and clindamycin - with 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 enhances the effect of anticoagulant means of indirect action.

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

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

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

Increases C_max 7 times (from 4 to 21 times) and the area under the 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 lesions, in connection with the threat of development of adverse reactions from the central nervous system (CNS) 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).

When using ciprofloxacin, direct sunlight and intense ultraviolet radiation should be avoided. In case of photosensitivity (the appearance of burn-like skin reactions), the drug should be discontinued.

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

During treatment, one should refrain from managing vehicles and servicing machines and mechanisms that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film-coated tablets, 250 mg, 500 mg, 750 mg.

Packaging:

10 tablets of 250 mg each; 5 tablets of 500 mg, 750 mg in contoured cell packs.

10, 20 tablets of 250 mg; 5, 10, 20 tablets of 500 mg and 750 mg in cans of polymeric.

Each bank, 1, 2 contour cell packs with 10 tablets of 250 mg, 1, 2, 4 contour cell packs with 5 tablets of 500 mg and 750 mg with instructions for use are placed in packs of cardboard.

Storage conditions:

In a dry, protected from light place, at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:5 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N001587 / 01

Date of registration:22.02.2011

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Ciprofloxacin (Ciprofloxacin)