Ciprofloxacin

General characteristics. Structure:

Active ingredient: 250 mg or 500 mg of ciprofloxacin of a hydrochloride.

Excipients: starch corn, sodium is glikolit by starch, Natrium benzoicum, talc, magnesium stearate, colloid silicon dioxide, isopropyl alcohol, a gidroksipropilmetiltsellyuloza, methylene dichloride, titanium dioxide, polyethyleneglycol, glycol is sawn through.

Antimicrobic drug of a broad spectrum of activity from group of ftorkhinolon.

Pharmacological properties:

Pharmacodynamics. Drug inhibits DNK-girazu enzyme of bacteria owing to what DNA replication and synthesis of cellular proteins of bacteria is broken.

Ciprofloxacin affects both the breeding microorganisms, and on being in a resting phase. Gram-negative aerobic bacteria are sensitive to ciprofloxacin: enterobakteriya (E.coli, Salmonella spp., Shigella spp., Citrobacter spp., Klebsiella spp., Edwardsiella tarda, Enterobacter spp., Proteus mirabilis, Proteus vulgaris, Serratia marcescens, Hafnia alvei, Providencia spp., Morganella morganii, Vibrio spp., Yersinia spp.), other gram-negative bacteria (Haemophilus spp., Pseudomonas aeruginosa, Pseudomonas shigelloides, Campilobacter jeiuni, Neisseria, spp.); some intracellular activators: Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium aviumintracellulare.

Also gram-positive aerobic bacteria are sensitive to ciprofloxacin: Staphylococcusspp. (S.aureus, S.hominis, S.saprophyticus), Streptococcusspp. (St. pyogenes, St.agalactiae). The majority of the stafilokokk steady against Methicillinum are steady against ciprofloxacin. Sensitivity of bacteria of Streptococcus pneumoniae, Enterococcus faeclis is moderate.

Corinebacterium spp are steady against drug., Bacteroides fragilis, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difcile, Nocardia asteroids.

Pharmacokinetics. At intake, especially on an empty stomach, ciprofloxacin is well soaked up from a GIT. The peak of concentration in a blood plasma is observed in 1-2 h after intake.

Distribution volume in an organism makes 2-3,5 l/kg. In cerebrospinal fluid drug in a small amount where its concentration makes 6-10% of that serum.

High concentration of drug are observed in bile, lungs, kidneys, a liver, a gall bladder, a uterus, semen, prostate tissue, almonds, an endometria, fallopian pipes and ovaries. Concentration of drug in these fabrics is higher, than in serum. Ciprofloxacin also well gets into bones, eye liquid, a bronchial secret, saliva, skin, muscles, a pleura, a peritoneum, a lymph.

The collecting concentration of ciprofloxacin in neutrophils of blood is 2-7 times higher, than in serum.

Extent of linkng of ciprofloxacin with proteins of plasma makes 30%. An elimination half-life – about 4 h. At patients with invariable function of kidneys the elimination half-life increases. The main way of removal of ciprofloxacin from an organism – a kidney. With urine 50-70% are removed. From 15 to 30% are removed with excrement. Patients with a heavy renal failure (the clearance of creatinine is lower than 20 ml/min. / 1,73 sq.m) need to appoint a half of a daily dose of drug.

Indications to use:

It is applied at the infections caused by microorganisms, sensitive to drug:
- respiratory tracts (pneumonia, except pneumococcal, acute and chronic bronchitis, bronchiectasias, aggravations at patients with cystous fibrosis);
- ENT organs (average otitis, sinusitis, mastoiditis, tonsillitis, pharyngitis),
bodies of a small pelvis (cystitis, pyelonephritis, adnexitis, endometritis, oophoritis, tubular abscess, pelvic peritonitis, prostatitis);
- abdominal and gepatobiliarny infections (peritonitis, intraperitoneal abscesses, cholecystitis, cholangitis);
- bones and joints (osteomyelitis, septic arthritis);
- skin and soft tissues (the infected ulcers, wounds, burns, abscesses, cellulitis, an infection of outside acoustical pass);
- venereal (gonorrhea, venereal ulcer, clamidiosis);
- heavy system infections (sepsis, infections at patients with a neutropenia);
- salmonellonositelstvo;
- to infectious diarrhea (activators strains of E. соli and Campylobacter jejuni are);
- to prevention of infections at surgical interventions (in urology, gastroenterology, orthopedics).

Route of administration and doses:

Duration of treatment depends on disease severity, a clinical current and results of a bacteriological research. In certain cases perhaps additional purpose of other antimicrobic means. If the patient for any reasons is not able to take a pill, it is recommended to carry out treatment by an infusional form of drug, with the subsequent transition to intake.

Infections of lower parts of respiratory tracts: 500-750 mg 2 times a day - 7-14 days.

Infections of upper parts of respiratory tracts:
- An exacerbation of chronic sinusitis - 500-750 mg 2 times a day - 7-14 days;
- Chronic purulent average otitis - 500-750 mg 2 times a day - 7-14 days;
- Malignant outside otitis - 500-750 mg 2 times a day – 28 days - 3 months.

Infections of urinary tract:
- Uncomplicated cystitis: 250-500 mg 2 times a day - 3 days (to women in the period of a menopause – once 500 mg);
- The complicated cystitis, uncomplicated pyelonephritis: 500 mg 2 times a day - 7 days;
- The complicated pyelonephritis: 500-750 mg 2 times a day - Not less than 10 days in certain cases (for example, at abscesses) – up to 21 days;
- Prostatitis: 500-750 mg 2 times a day - 2-4 weeks (acute), 4-6 weeks (chronic).

Infections of generative organs:
- A fungal urethritis and a cervicitis - a single dose of 500 mg;
- An orchiepididymitis and inflammatory diseases of bodies of a small pelvis - 500-750 mg 2 times a day - not less than 14 days.

Infections of a GIT and intraabdominal infections:
- The diarrhea caused by a bacterial infection, including Shigella spp except Shigella dysenteriaetipa I and empirical treatment of heavy diarrhea of the traveler - 500 mg 2 times a day – 1 day;
- The diarrhea caused by Shigella dysenteriae of the I-type of 500 mg 2 times a day - 5 days;
- The diarrhea caused by Vibrio cholera - 500 mg 2 times a day - 3 days;
- A typhoid - 500 mg 2 times a day - 7 days;
- The intraabdominal infections caused by gram-negative microorganisms - 500 - 750 mg 2 times a day - 5-14 days.

Infections of skin and soft tissues: 500 - 750 mg 2 times a day - 7-14 days.

Infections of joints and bones: 500 - 750 mg 2 times a day - max. 3 months.

Prevention and treatment of infections at patients with a neutropenia: appointment together with other medicines - 500-750 mg 2 times a day is recommended - therapy continues before the end of the period of a neutropenia.

Prevention of the invasive infections caused by Neisseria meningitides: 500 mg once.

Post-contact prevention and treatment the Siberian yazvy:lechenia should begin as soon as possible after the assumed or confirmed infection - 500 mg 2 times a day - 60 days from the moment of infection confirmation.

Renal failure: the dose depends on clearance of creatinine: 30-60ml/mines - to 250-500 mg there are each 12 hours; less 30ml/mines - to 250-500 mg there are each 24 hours; to patients on a hemodialysis - to 250-500 mg there are each 24 hours (after the procedure of dialysis); to patients on peritoneal dialysis - to 250-500 mg there are each 24 hours.

Abnormal liver function: Dose adjustment is not required.

Features of use:

Serious infectious diseases and the mixed infectious processes. At these states ciprofloxacin is appointed in a combination with other antimicrobic drugs.

Streptococcal infection (including Streptococcus pneumoniae). Ciprofloxacin is not recommended for treatment in connection with insufficient efficiency.

Urogenital infections. These infections can be caused фторхинолон by steady Neisseriagonorrhoeae. In these cases it is necessary to appoint ciprofloxacin together with other antimicrobic drugs. If within 3 days of reception improvement is not observed, then treatment is recommended to be reconsidered.

Intra belly infectious diseases. Data on efficiency of ciprofloxacin for treatment of postoperative intra belly infectious diseases are limited.

Diarrhea of "traveller". At the choice of ciprofloxacin the available information on resistance to drug of the corresponding microorganisms in the visited country is considered.

Infectious diseases of bones and joints. Ciprofloxacin is appointed in a combination with other antimicrobic drugs after carrying out a microbiological research.

Malignant anthrax: Data on use of drug for people are limited. It is recommended to be guided by national and/or international documents on treatment of this disease.

Other specific serious infectious diseases: Ciprofloxacin is applied according to protocols of treatment or after careful assessment of a ratio "risk advantage" and carrying out the microbiological analysis in cases when other treatment is impossible or after a failure of the previous therapy.

Hypersensitivity. After reception of a single dose of drug hypersensitivity reactions, including anaphylactic and anaphylactoid reactions, - states, life-threatening are possible. Immediately to cancel medicine reception, to immediately inform the doctor or to call the Ambulance!

Skeletal and muscular system. Patients should not appoint ciprofloxacin with diseases of sinews or disturbances at reception of hinolon in the past. In need of treatment of serious infectious diseases at such patients for treatment of serious infectious diseases the microbiological research and assessment of a ratio "risk advantage" is carried out. Emergence of an inflammation or rupture of sinews, preferential, at elderly patients or at the same time accepting corticosteroids is possible. At any symptoms of the specified disease (hypostasis, an inflammation) administration of drug to stop and immobilize the affected extremity. With care it is applied at patients with a myasthenia гравис.

Photosensitivity. The patients accepting ciprofloxacin should avoid direct exposure to sunlight and UF of radiation.

Central nervous system. It is known that hinolona can lower a convulsive threshold and initiate spasms. With care it is applied by patients with TsNS diseases provoking convulsive attacks. It was reported about cases of emergence of a polyneuropathy (pain, burning, feeling of nervousness, a sonitus, muscular weakness, sensitivity disturbances, including tactile, painful, temperature, vibration and muscular and joint). At emergence of the specified phenomena – to stop administration of drug! To immediately inform the doctor.

Cardiovascular system. As use of ciprofloxacin is connected with cases of lengthening of an interval of QT on an ECG, it is necessary to be careful at treatment of patients with risk of development of arrhythmia: inborn lengthening of an interval of QT; concomitant use of antiarrhythmic drugs of the class IA and III, antidepressants, macroleads, neuroleptics; electrolytic disturbances; women and patients of advanced age are more sensitive; heart diseases.

Pseudomembranous colitis: At suspicion of pseudomembranous colitis (a liquid chair for a long time, perhaps, with impurity of blood or slime in it) it is necessary to stop immediately reception and to see urgently a doctor for performing the corresponding treatment! It is impossible to apply the medicines oppressing motility of intestines. To immediately inform the doctor.

Renal and uric systems: It is necessary to accept enough liquid.

Gepatobiliarny system: It was reported about cases of emergence of a necrosis of a liver and a life-threatening liver failure (jaundice, dark urine, an itch, lack of appetite). At emergence of the specified phenomena – to stop administration of drug! To immediately inform the doctor.

Deficit glyukozo-6-fofatdegidrogenazy. Development of hemolitic reactions is possible. Drug to such patients is not appointed, except for cases when the potential advantage exceeds possible risk.

Resistance. During long therapy and in cases of treatment of some infections can be emitted ciprofloxacin – resistant bacteria.

Meal and dairy products. It is necessary to avoid a concomitant use with dairy products or drinks, enriched with minerals (the milk, yogurts enriched with calcium, orange juice) as at the same time absorption of ciprofloxacin can decrease.

Use of Ciprofloxacin at pregnancy and in the period of a lactation: It is contraindicated. Use of Ciprofloxacin for children: At children and teenagers the risk - advantage" is applied only after ratio assessment ". Against the background of reception of ciprofloxacin udety arthropathies often appear.

Influence on ability to driving of motor transport and to control of mechanisms: Ability to drive the car and other mechanisms can decrease, in connection with influence of ciprofloxacin on speed of response.

Side effects:

As well as all medicines, ciprofloxacin can cause side effects with various frequency irrespective of whether it was accepted earlier.

Often (1 on 10 - 100 cases): nausea, diarrhea.

Infrequently (1 on 100 – 1 000 cases): fungal superinfections, an eosinophilia, lack of appetite, a hyperactivity, excitement, headaches, dizziness, frustration of a dream, taste disturbance, vomiting, pains in a stomach and intestines, dyspepsia, a meteorism, a superactivity of liver enzymes, increase in level of bilirubin, rash, an itch, urticaria, musculoskeletal pains (in extremities, a back, a thorax), joint pains, a renal failure, fatigue, temperature increase.

Seldom (1 na1 000 - 10 000 cases): a colon inflammation, change of quantity of leukocytes, anemia, decrease in quantity of thrombocytes, allergic reactions, increase in level of sugar in blood, confusion of consciousness, pathological dreams, a depression with the advent of suicide thoughts, sensitivity changes, trembling, spasms, dizziness, a vision disorder, disorders of hearing, tachycardia, decrease in the ABP, a faint, suffocation, abnormal liver functions, jaundice, hepatitis, photosensitivity, muscular pain, an inflammation of joints, the raised muscle tone, muscular spasms, a renal failure, blood/crystals in urine, nephrite, increase in activity of amylase.

Very seldom (less than 1 on 10 000 cases): hemolitic anemia, decrease in quantity of blood cells, oppression of function of marrow, anaphylactic reaction, an acute anaphylaxis, mental reactions with possible suicide attempts, migraine, an incoordination, unstable gait, disorder of perception of smells, the increased intracranial pressure, changes of perception of color, vasculites, pancreatitis, a necrosis of a liver, a petechia, an erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis, weakness in muscles, an inflammation and a rupture of sinews (generally an akhillova), hypostases, the increased sweating. 

Frequency is unknown (it cannot be estimated on the basis of the available data): peripheral neuropathy, ventricular tachycardia, arrhythmia, acute generalized pustular dieback, increase in a prothrombin time.

Interaction with other medicines:

Methotrexate: increase in concentration of a methotrexate at joint reception, increase in risk of development a methotrexate - the connected toxic reactions.

Phenytoinum, clozapine: influence on concentration in blood of these medicines is possible. Control of level of drugs in blood is recommended.

Antiarrhythmic drugs of the class IA, III: lengthening of an interval of Qtna ECG is possible. Control of an ECG is recommended.

Other derivatives of xanthine (caffeine, пентоксифиллин): the concomitant use can lead to increase in concentration of derivatives of xanthine in blood.

Metoclopramidum: considerable acceleration of absorption of ciprofloxacin that reduces time of achievement of the maximum concentration in plasma.

Non-steroidal anti-inflammatory drugs: joint reception (excepting acetylsalicylic acid) can provoke spasms.

Hypoglycemic means for intake (глибенкламидн): strengthening of their hypoglycemic effect is possible. Control of level of sugar in blood is necessary.

Ropinirol, the drugs containing lidocaine, clozapine sildenafit: influence on concentration in blood of these drugs is possible, are jointly applied only after ratio assessment "risk advantage".

Didanozin:vsasyvaniye of ciprofloxacin decreases.

Teofillin:vozmozhno increase in concentration and period of removal of theophylline. Observation of the doctor for identification of signs of toxicity of theophylline and dose adjustment is recommended.

Probenetsid:zamedlyaet ciprofloxacin removal.

Sukralfat, magnesium - or aluminum-bearing means for decrease in acidity of a stomach, drugs the zheleza:vsasyvaniye of ciprofloxacin is slowed down, the interval between reception of these drugs has to be not less than 4 hours.

The risk of bleedings Antikoagulyanty:povyshatsya. Control of coagulant system of blood is recommended.

Cyclosporine: strengthening of toxic influence of cyclosporine on kidneys. Control of function of kidneys is recommended.

Contraindications:

- pregnancy;
- breastfeeding period;
- children's and teenage age up to 18 years;
- hypersensitivity to ciprofloxacin or other drugs of ftorkhinolon.

Overdose:

The specific antidote is unknown. It is necessary to control carefully a condition of the patient, to make a gastric lavage, to carry out usual measures of acute management, to provide sufficient intake of liquid. By means of haemo - and peritoneal dialysis it can be removed only insignificant (less than 10%) amounts of drug.

If you accepted the Ciprofloxacin dose big, than the doctor recommended. If quantity of pill in day which you took exceed that quantity which was recommended by your doctor, or your child swallowed tablets, see a doctor or call the Ambulance! To stop reception of medicine! The overdose can be shown by dizziness, a headache, fatigue, spasms, hallucinations, confusion of consciousness, feeling of discomfort in a stomach, a renal failure and a liver, existence of crystals and blood in urine. As first aid it is recommended to wash out a stomach and to accept antacids.

Storage conditions:

List B. To store in the place protected from moisture and light at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging. On 10 or 20 tablets in bank polymeric sealing means – medical cotton. One bank, 1 or 2 blister strip packagings together with a leaf insert in secondary packaging.