Tsiprom

General characteristics. Structure:

Active ingredient: 250 mg or 500 mg of ciprofloxacin.

Excipients: starch corn, methylhydroxybenzoate, пропилгидроксибензоат, silicon dioxide colloid, magnesium stearate, talc, sodium krakhmalglikolit, cellulose microcrystallic, Opadry White dye, titanium dioxide, macrogoals (PEG-6000).

Pharmacological properties:

Pharmacodynamics. Antimicrobic drug of group of ftorkhinolon of bactericidal action. Inhibits DNK-girazu enzyme (topoisomerases ІІ and ІV which are responsible for process of formation of chromosomal DNA in a superspiral about nuclear RNA), breaks DNA biosynthesis, growth and divisions of bacteria; causes the expressed morphological changes (including a cell wall and membranes) and bystry death of a cell. Affects microorganisms in a growth period and rest.

Has a broad spectrum of activity. Gram, highly active concerning the majority, - negative microorganisms: pyocyanic, hemophilic and intestinal sticks, shigellas, salmonellas, meningokokk, gonokokk, some kinds of enterococci. Active rather many strains of stafilokokk (which produce and do not produce a penicillinase metitsillinrezistentny), and also a kampilobakter, legionet, mycoplasmas, a chlamydia, mycobacteria. Ciprofloxacin is active against microorganisms which produce beta lactamelements. Less expressed influence on anaerobe bacterias. To drug resistant: Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. Influence concerning Treponema pallidum it is studied insufficiently.

In acid medium activity decreases. Resistance develops slowly and gradually ("multistage" type).

Pharmacokinetics. After oral administration of ciprofloxacin the tablet is quickly and well soaked up in digestive tract, absorption is carried out preferential in duodenal and thin guts. Absolute bioavailability – about 70%. The maximum concentration is reached in 1-1,5 hours after reception and at doses of 250 mg and 500 mg makes 0,1 mkg/mg and 0,2 mkg/mg respectively. Reception of food slows down absorption, but does not change _Cmax and bioavailability. 20-40% contact proteins of plasma. Gets into fabrics, liquids and cells, forming high concentration in kidneys, a gall bladder, a liver, lungs, mucous bronchial tubes and sine, female generative organs, the englobing cells (polinikleara, macrophages), urine, a phlegm, bile, liquid of a skin blister; it is found in a prostate, cerebrospinal fluid (less than 10% of level in plasma, at meningitis – to 45% and more), saliva, skin, fatty tissue, muscles, bones, cartilages, passes through a placenta. The elimination half-life makes 4 hours. It Biotransformirutsya in a liver (15-30%) with formation of low-active metabolites (diethylciprofloxacin, sulfociprofloxacin, oxociprofloxacin, formylciprofloxacin).

About 40-50% of a dose that is accepted orally, is removed by kidneys (by glomerular filtering and canalicular secretion) in an invariable look and about 15% - in the form of metabolites. The rest is removed by a GIT (with bile and excrements); a small amount is excreted by mammary glands that lactate. Concentration in urine considerably exceed the minimum bacteriostatic concentration for the majority to causative agents of infections of urinary tract. Cumulation after intake in a dose of 500 mg twice a day within 5 days is not revealed. At chronic cirrhosis the pharmacokinetics does not change, at patients with a renal failure the elimination half-life lasts.

Indications to use:

Infections of ENT organs (average otitis, sinusitis, mastoiditis, tonsillitis, pharyngitis), the lower respiratory tracts (an acute bronchitis and an aggravation chronic, pneumonia, except pneumococcal, a bronchoectatic disease, a mucoviscidosis), bodies of a small pelvis (cystitis, pyelonephritis, prostatitis, an adnexitis, a salpingitis, an oophoritis, an endometritis, tubular abscess, pelvic peritonitis), skin and soft tissues (the infected ulcers, a poraneniya, burns, infections of outside acoustical pass, abscesses, cellulitises), bones and joints (osteomyelitis, septic arthritis), venereal (gonorrhea, a venereal ulcer, clamidiosis), an abdominal cavity (intra belly abscesses, peritonitis, salmonellosis, including a typhoid, a campilobacteriosis; иерсиниоз, a shigellosis, cholera), a bakteriyamiya, a septicaemia, heavy infections against the background of an immunodeficiency and a neutropenia, prevention of infections at surgical interventions.

Route of administration and doses:

The dose and duration of therapy are always defined by the doctor individually. As a rule, to adults and teenagers 15 years at infections of urinary tract and respiratory infections are more senior appoint 250 mg-500 of mg 2 times a day; if necessary the dose is raised to 750 mg; a course of treatment – 7–10 days.

At not complicated gonorrhea of 250 mg-500 of mg once; at association of a gonococcal infection with Chlamidia and mycoplasmal appoint 750 mg each 12 hours within 7-10 days.

At a shankroida – on 500 mg 2 times a day within 3-5 days. At meningococcal a nasopharyngitis appoint once in a dose 500 or 750 mg.

At osteomyelites appoint 750 mg 2 times a day. Treatment duration at osteomyelites – up to 8 weeks.

At digestive tract infections – on 250 mg – 500 mg there are each 12 hours within 5–10 days. Tablets should be swallowed whole, without chewing, to wash down with a small amount of liquid, after reception of food.

At a renal failure the dose is reduced depending on clearance of creatinine (ordinary twice). For elderly people the dose is reduced (ordinary on 1/3).

Features of use:

With care appoint at TsNS pathology in the anamnesis: at mental diseases, epilepsy, decrease in a convulsive threshold, apoplexy, heavy ateroskleroza of vessels of a brain (risk disturbance of blood supply, a stroke), at advanced age, at heavy renal failures and a liver (necessary control of concentration in a blood plasma).

During treatment it is necessary to avoid solar and UF-radiations, intensive exercise stresses, to control the drinking mode, рН urine.

Can reduce the speed of psychomotor reactions, especially against the background of alcohol that should be considered to patients who work with potentially unsafe mechanisms or manage vehicles.

If heavy diarrhea develops, it is necessary to exclude pseudomembranous colitis (at which ciprofloxacin is contraindicated).

Simultaneous to the vnurishnyovena of introduction of barbiturates demands control of function of cardiovascular system (arterial pressure, ECG indicators).

To teenagers up to 15 years it is appointed only in case of resistance of the activator to the others of chemotherapeutic drugs.

During pregnancy contraindicated. Feeding by a breast is stopped for the period of treatment.

Side effects:

From a nervous system and sense bodys: dizziness, headache, feeling of fatigue, concern, trembling, sleeplessness, peripheral paralgeziya, migraine, increase in intracranial pressure, alarming state, consciousness misting, syncopal state, depression, hallucinations, psychotic reactions, thrombosis of vessels of a brain, disturbance of taste and to a scent, sight and perception of color, diplopia, sonitus.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): tachycardia, eosinophilia, leucio-and thrombopenia, granulocytopenia, anemia, change of level of a prothrombin, tranzitorny increase in level of hepatic transaminases, bilirubin, creatinine, alkaline phosphatase, glucose.

From urinogenital system: a glomerulonephritis, a hamaturia, a crystalluria, a dysuria, an urination delay, the albuminaria, urethral bleedings, the passing renal failure, intersticial nephrite.

Allergic reactions: a skin rash, an itch, a Quincke's edema, a vasculitis, arthritis, Stephens's syndromes – Johnson and Layell, an acute anaphylaxis.

Others: cholestatic jaundice, tendovaginitis, photosensitization, mialgiya, гепатонекроз

Interaction with other medicines:

Activity grows at association with a beta laktamnymi antibiotics, aminoglycosides, Vancomycinum, clindamycin, metronidazole.

Sukralfat, bismuth drugs, antacids which contain ions of aluminum of magnesium or calcium, Cimetidinum, ranitidine, vitamins C microelements, gland sulfate, zinc, диданозин, purgatives reduce absorption (it is recommended to apply in 2 hours prior to or in 4 hours after these drugs).

Probenetsid, азлоцилин increase concentration in blood. Reduces clearance and increases level in plasma of caffeine, aminophylline and theophylline (the probability of development of side effects grows).

Strengthens effect of warfarin and other peroral anticoagulants (prolongs a bleeding time).

Increases nephrotoxicity of cyclosporine, risk of increase in excitement of the central nervous system and unconscious reactions against the background of non-steroidal anti-inflammatory drugs. Drugs which alkalinize urine (citrates, sodium bicarbonate, karboangidraza inhibitors) reduce solubility (the probability of a crystalluria grows).

Contraindications:

Hypersensitivity to drug components (including to the others a ftorkhinolon), deficit of a glyukozo-fosfatdegidrogenaza, children's and teenage age (up to 15 years), pregnancy, feeding by a breast (for treatment stop).

Overdose:

There are no specific symptoms of overdose.

Gastric lavage, uses of the drugs causing vomiting, introduction of a large amount of liquid, formation of acid reaction of urine, in addition – a hemodialysis and peritoneal dialysis; all measures are carried out against the background of support of the vital functions.

Storage conditions:

To store in unavailable to children, the dry place at a temperature below 30 degrees Celsius.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a strip packaging, on 1 strip packaging in a cardboard box.