Ciprofloxacin, capsules 250 mg - Product - ATC Classification

INSTRUCTION

(information for patients)

on medical administration of medicinal preparation

CIPROFLOXACIN

Trade name: ciprofloxacin.

International non-proprietary name: ciprofloxacin.

Description: hard white gelatin capsules, number 0.

Composition:

active substance: ciprofloxacin (as ciprofloxacin hydrochloride) – 250 mg;

excipients: calcium stearate (E 470), potato starch.

Composition of the hard gel capsule coating: gelatin, glycerol, purified water, titanium dioxide, sodium lauryl sulfate.

Drug formulation: capsules 250 mg.

Pharmacotherapeutic group: Systemic antimicrobial preparations. Fluoroquinolones.

ATC Code: J01MA02.

Pharmacological action

It has an antibacterial (bactericidal effect). It blocks the DNA-gyrase and prevents the DNA replication, violates bacteria growth and division. It causes evident morphological changes (including those in the cellular wall and membranes) and quick death of bacterial cells. It acts on microorganisms in the periods of growth and rest.

Ciprofloxacin is a broad spectrum antimicrobial preparation. Ciprofloxacin is active against Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Campylobacter jejuni, Citrobacter diversus, Citrobacter freundii, Enterobacter cloaceae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Morganella morganii, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Pseudomonas aeruginosa, Salmonella typhi, Serratia marcescens, Shigella flexneri, Shigella sonnei, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Acinetobacter spp., Aeromonas caviae, Aeromonas hydrophilia, Brucella melitensis, Campylobacter coli, Erwardsiella tarda, Enterobacter aerogenes, Haemophilus ducreyi, Klebsiella oxytoca, Legionella pneumophila, Moraxella (Branhamella) catarrhalis, Neiserria meningitidis, Pasteurella multocida, Salmonella enteritidis, Vibrio cholerae, Vibrio parahaemolyticus, Vibrio vulnuficus, Yersinia enterocolitica, Chlamydia trachomatis; the ciprofloxacin sensitivity to Mycobacterium tuberculosis varies.

Most staphylococci resistant to methicillin are resistant to ciprofloxacin, as well. Streptococcus pneumonia, Mycobacterium avium (intracellular), Enterococcus faecalis are moderately active (the preparation large concentrations are required for their suppression). Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroids are resistant to the preparation. The preparation is not active against Treponema pallidum. Resistance develops very slowly as on the one hand practically no persistent microorganisms survive and on the other hand bacterial cells lack enzymes inactivating ciprofloxacin.

Indications

- Infections of urinary and respiratory ducts (pneumonia except the pneumococcal one, acute and chronic bronchitis, bronchoectases, exacerbations in adult and childish (15 years of age and older) patients with cystic fibrosis);

- Infections of LOR-organs (otitis media, sinusitis, mastoiditis, tonsillitis, pharyngitis);

- Infections of organs of small pelvis (cystitis, pyelonephritis, adnexitis, endometritis, oophoritis, tubular abscess, pelvic peritonitis, prostatitis);

- Abdominal and hepatobiliary infections (peritonitis, intraabdominal abscesses, cholecystitis, cholangitis); infections of bones and joints (osteomyelitis, septic arthritis); skin and soft tissues (infected ulcers, wounds, burns, abscesses, cellulitis, infections of external acoustic duct);

- Venereal infections (gonorrhea, soft chancre, chlamydiosis);

- Severe systemic infections (sepsis, infections in neutropenic patients);

- Salmonella carriage;

- Infectious diarrhea (E. coli and Campylobacter jejuni are the causative agents);

Infection prevention in case of surgical interferences (in urology, gastroenterology, orthopedics).

Mode of administration and dosage

The preparation is swallowed with some liquid; for uncomplicated infections of lower and upper segments of urinary ducts 250 mg of the preparation is ingested 2 times a day for 3 days; for complicated infections of lower and upper segments of urinary ducts 500 mg of the preparation is ingested 2 times a day for 14 days; for severe infections (pneumonia, osteomyelitis) 750 mg of the preparation is ingested 2 times a day; for chronic Salmonella carriage 750 mg of the preparation is ingested 2 times a day for 4 weeks; for acute gonorrhea 250 mg or 500 mg of the preparation is ingested once; for diarrhea 500 mg of the preparation is ingested 2 times a day; for very severe infections the dose may increased up to 750 mg of the preparation 3 times a day; for preventing infections under surgical interferences 500 – 750 mg of the preparation is administered 30 – 60 minutes before the operation (when the operation has continued for more than 4 hours the dose is to be re-administered).

Ciprofloxacin is administered with caution in case of renal failure: when the creatinine clearance is 31 – 60 ml/min/1.73 m² the maximal ciprofloxacin dose is 1000 mg per day, when the creatinine clearance is 30 ml/min/1.73 m² or less the maximal ciprofloxacin dose is 500 mg per day.

When the renal function is impaired and a patient is on hemodialysis the maximal ciprofloxacin dose is 500 mg per day, on the hemodialysis day ciprofloxacin is to be taken after the hemodialysis procedure.

When the hepatic function is impaired the dose does not require correcting.

Side effects

Digestive system:nausea, vomiting, abdominal pain, meteorism, dysorexia, diarrhea, cholestatic jaundice (mostly after a disease of the liver has been survived), hepatitis, hepatonecrosis.

Nervous system: headache, dizziness, fatigability, vision disorders, anxiety, tremor, insomnia, nightmares, peripheral paralgesia (pain sensation anomaly), hyperhidrosis, diplopia, tinnitus, hearing attenuation, convulsions, cerebral hypertension, mental confusion, depression, hallucinations, photosensitivity, toxic psychosis as well as other psychotic reactions manifestations (sometimes progressing up the states when the patient cam harm himself), migraine, syncope states, thrombosis of cerebral arteries.

Cardiovascular system: tachycardia, heart rhythm disturbances, hypo- or hypertension.

Haemopoietic system: leucopenia, granulocytopenia, anemia, thrombocytopenia, leucocytosis, thrombocytosis, hemolytic anemia.

Laboratory values: hypoprothrombinemia, liver transaminase and alkaline phosphatase activities increase, hypercreatinemia, hyperbilirubinemia, hyperglycemia.

Urinary system: hematuria, crystalluria (primarily in case of alkaline urine and low diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, albuminuria, urethral bleedings, hematuria, reduction of renal function of nitrogen elimination, interstitial nephritis.

Allergic reactions: intching, urticaria, formation of blisters accompanied by bleedings, appearance of small vesicles forming scabs, medicinal fever, petechial hemorrhages on the skin, facial or laryngeal edema, dyspnea, eosinophilia, hypersensitivity, vasculitis, nodular erythema, multiform exudative erythema (including Stevens – Johnson’s syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

Others: arthralgia, arthritis, tendovaginitis, tendon ruptures, asthenia, myalgia, superinfection (candidosis, pseudomembranous colitis), hot flushes.

Contraindications

Hypersensitivity to ciprofloxacin (and to other fluoroquinolones), glucose-6-phosphate hydrogenase deficit, epilepsy, childhood up to 18 years (at the age of 15 – 17 years ciprofloxacin may be prescribed for managing mucoviscidosis complications of lungs only), pregnancy, breast feeding.

Overdosing

Several cases of reversible toxic effects on the parenchyma of the liver after the oral drug overdosing were described.

Treatment: stomach lavage, introduction of a large volume of liquid, provision of the urine acidic reaction, optional – hemodialysis and peritoneal dialysis (less than 10% of the dose ingested can be eliminated); every action is undertaken on the background of the vital function support. A specific antidote does not exist.

Special warnings

The blood urea, creatinine, liver transaminases should be monitored. For preventing crystalluria development the recommended daily dose cannot be exceeded. For supporting the urine acidic reaction much liquid should be drunk.

As the childish and adolescent skeleton has not formed by 15 years the preparation is contraindicated to children of that age group.

Administration during pregnancy and period of lactation. The preparation is contraindicated during pregnancy and period of breast feeding.

Measures of precaution

Ciprofloxacin may be prescribed to patients suffering from epilepsy, having convulsions in the anamnesis, vascular diseases and organic lesions of the brain only for vital indications as side effects can develop in the central nervous system. The preparation may be prescribed with caution for treating elderly patients; in case of renal failure, glucose-6-phosphate hydrogenase deficit. When a severe and long-time diarrhea has developed during or after the therapy the diagnosis of pseudomembranous colitis should be excluded as the latter requires the drug immediate withdrawal and the adequate therapy prescription. When tendon pain or the first signs of tendovaginitis appear the preparation administration should be cancelled (isolated cases of tendon inflammation and even rupture during a fluoroquinolone administration are described). Excessive insolation should be avoided.

Achill’s tendon is observed to rupture most often in elderly patients having been administered glucocorticosteroids earlier.

Impact on driving capacity and managing other potentially hazardous mechanisms. The ciprofloxacin intake can violate the driving ability and managing mechanisms (especially when taken with alcohol). The patients are not recommended to drive and to manage moving mechanisms during the period of treatment.

Interaction with other medicinal agents

The preparation activity increases when administered in combination with beta-lactam antibiotics, aminoglycosides, vancomycin, clindamycin, metronidazole. Sucralfate, bismuth preparations, antacids, agents containing aluminum, magnesium, calcium, cimetidine, ranitidine, vitamins with microelements, iron sulfate, laxatives delay absorption. Ciprofloxacin increases the plasma theophylline, aminophylline, and caffeine concentrations. It amplifies the cyclosporine nephrotoxicity, the risk of convulsions on the background of non-steroid anti-inflammatory drugs intake. It aggravates the warfarin and other oral anticoagulants effects (increasing the bleeding duration). Medicinal preparations alkalinizing the urine worsen its solubility (crystalluria becomes more probable). Ciprofloxacin inhibits the oxidative enzymes of the liver and can aggravate the effects of preparations metabolized with participation of enzymes of cytochrome P450 system. Metoclopramide accelerates absorption leading to a quicker maximal blood concentration achievement. Combined administration with uricosuric drugs results in the elimination delay (up to 50%) and the plasma ciprofloxacin concentration increase. When administered in combination with tizanidine the risk of evident hypotension and sleepiness increases.

Storage conditions

Store in protected from light place at temperature not above 25°C.

Keep away from children.

Shelf life

2 years.

Packing

250 mg capsules in a blister No. 10x2, No. 10x150..

Terms of sale

On physician’s prescription.

Manufacturer:

Belmedpreparaty RUE

30 Fabritsius Str., 220007 Minsk, Republic of Belarus,