Ciprofloxacin

General characteristics. Structure:

Description: solution for infusions transparent, slightly yellowish or slightly greenish color.

Active ingredient: ciprofloxacin;          

Excipients: solution of sodium of chloride of 0.9%, lactic acid, the EDTA disodium salt, water for and.

Pharmacological properties:

Antimicrobic drug of a broad spectrum of activity from group of ftorkhinolon. Works bakteritsidno. Drug inhibits DNK-girazu enzyme of bacteria owing to what DNA replication and synthesis of cellular proteins of bacteria are broken. Ciprofloxacin affects both the breeding microorganisms, and on being in a resting phase.

Ciprofloxacin is active concerning gram-negative aerobic bacteria: 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., Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.; intracellular activators: Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium-intracellulare; gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). The majority of the stafilokokk steady against Methicillinum are steady also against ciprofloxacin.

Streptococcus pneumoniae, Enterococcus faecalis are moderately sensitive to drug.

Corynebacterium spp are steady against drug., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides.

Effect of drug concerning Treponema pallidum is studied insufficiently.

 

Pharmacokinetics. Absorption

Later in/in infusion of drug in a dose of 200 mg or 400 mg of Cmax it is reached in 60 min. and makes 2.1 mkg/ml and 4.6 mkg/ml respectively.

Distribution

Linkng with proteins of plasma - 20-40%. Vd - 2-3 l/kg. Ciprofloxacin is well distributed in body tissues (except for the fabrics rich with fats, for example, of nervous tissue). The maintenance of an antibiotic in fabrics is 2-12 times higher, than in plasma. Therapeutic concentration are reached in saliva, almonds, a liver, a gall bladder, bile, intestines, abdominal organs and a small pelvis, a uterus, semen, prostate gland tissue, an endometria, fallopian pipes and ovaries, kidneys and urinary bodies, pulmonary fabric, a bronchial secret, a bone tissue, muscles, synovial fluid and joint cartilages, peritoneal liquid, skin. Gets into cerebrospinal fluid in a small amount where its concentration at an uninflammed meninx makes 6-10% of that in blood serum, and at inflamed - 14-37%. Ciprofloxacin also well gets into eye liquid, a bronchial secret, a pleura, a peritoneum, a lymph, through a placenta. Concentration of ciprofloxacin in neutrophils of blood is 2-7 times higher, than in serum. Activity of ciprofloxacin decreases at acid values рН a little.

It is allocated with breast milk.

Metabolism

It is metabolized in a liver (15-30%) with formation of low-active metabolites (diethylciprofloxacin, sulfociprofloxacin, oxociprofloxacin, formylciprofloxacin).

Removal

At in introduction of T1/2 - 5-6 h. It is removed generally by kidneys by tubular filtering and canalicular secretion in not changed look (at in introduction - 50-70%) and in the form of metabolites (at in introduction - 10%), other part - through a GIT. Later in/in introductions concentration in urine during the first 2 h after introduction almost in 100 times more, than in serum that considerably surpasses MPK for the majority of causative agents of infections of urinary tract.

Renal clearance - 3-5 ml/min.; the general clearance - 8-10 ml/min.

Pharmacokinetics in special clinical cases

At a chronic renal failure (KK> of 20 ml/min.) the percent of the drug removed through kidneys decreases, but cumulation in an organism does not happen owing to compensatory increase in metabolism of drug and removal through a GIT. T1/2 at a chronic renal failure increases to 12 h.

Indications to use:

Infectious and inflammatory diseases, the caused chuvstvitelnymt to drug microorganisms:

— respiratory tracts;

— fish soup, throat and nose;

— kidneys and urinary tract;

— generative organs (including gonorrhea, prostatitis);

— gynecologic (including adnexitis) and puerperal infections;

— alimentary system (including oral cavities, teeth, jaws);

— gall bladder and biliary tract;

— integuments, mucous membranes and soft tissues;

— musculoskeletal system;

— sepsis;

— peritonitis;

Prevention and treatment of infections at patients with reduced immunity (at therapy by immunodepressants).

Route of administration and doses:

The drug should be administered in/in kapelno within 30 min. (a dose of 200 mg) and 60 min. (a dose of 400 mg). Solution for infusion can be combined from 0.9% chloride sodium solution, Ringer's solution, 5% and 10% solution of a dextrose (glucose), 10% the fructose solution, solution containing 5% dextrose solution from 0.225% or 0.45% chloride sodium solution.

The dose of Ciprofloxacin depends on disease severity, type of an infection, a condition of an organism, age, weight and function of kidneys at the patient.

The single dose makes 200 mg, at heavy infections - 400 mg. Frequency rate of introduction - 2; treatment duration - 1-2 weeks, if necessary are possible increase in a course of treatment.

At acute gonorrhea drug is appointed in/in once in a dose of 100 mg.

For prevention of postoperative infections - in 30 — 60 min. prior to operation in/in in a dose of 200-400 mg.

Patients with a heavy renal failure (KK <20 ml/min. / 1.73 sq.m) need to appoint a half of a daily dose.

Features of use:

At emergence in time or after treatment by Ciprofloxacin of heavy and long diarrhea it is necessary to exclude the diagnosis of pseudomembranous colitis which demands immediate drug withdrawal and purpose of the corresponding treatment.

When developing pains in sinews or at emergence of the first symptoms of a tendovaginitis treatment should be stopped.

During treatment it is necessary to provide with Ciprofloxacin enough liquid at observance of a normal diuresis.

During treatment by Ciprofloxacin it is necessary to avoid contact with direct sunshine.

Influence on ability to driving of motor transport and to control of mechanisms

The patients accepting Ciprofloxacin should be careful during the driving of the car and occupations other potentially dangerous types of activity requiring special attention and speed of psychomotor reactions (especially at simultaneous alcohol intake).

Side effects:

From the alimentary system: nausea, diarrhea, vomiting, abdominal pains, a meteorism, anorexia, cholestatic jaundice (especially at patients with the postponed liver diseases), hepatitis, гепатонекроз.

From TsNS and peripheral nervous system: dizziness, a headache, increased fatigue, uneasiness, a tremor, sleeplessness, "dreadful" dreams, a peripheral paralgeziya (anomaly of perception of feeling of pain), perspiration, increase in intracranial pressure, uneasiness, confusion of consciousness, a depression, hallucinations, manifestations of psychotic reactions (sometimes progressing to states in which the patient can do himself harm), migraine, a faint, thrombosis of cerebral arteries.

From sense bodys: disturbances of taste and sense of smell, vision disorder (diplopia, change of color perception), sonitus, decrease in hearing.

From cardiovascular system: tachycardia, disturbances of a cordial rhythm, decrease in the ABP, rushes of blood to face skin.

From the hemopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolitic anemia.

From laboratory indicators: prothrombinopenia, increase in activity of hepatic transaminases and ShchF, giperkreatininemiya, hyperbilirubinemia, hyperglycemia.

From an urinary system: a hamaturia, a crystalluria (first of all at alkalinuria and a hypouresis), a glomerulonephritis, a dysuria, a polyuria, an ischuria, an albuminuria, urethral bleedings, a hamaturia, decrease in azotvydelitelny function of kidneys, intersticial nephrite.

From a musculoskeletal system: arthralgia, arthritis, tendovaginitis, ruptures of sinews, mialgiya.

Allergic reactions: a skin itch, a small tortoiseshell, blistering, followed by bleedings, the papules forming crusts, medicinal fever, dot hemorrhages (petechias), a face edema or throats, an asthma, an eosinophilia, the raised photosensitivity, a vasculitis, a nodal erythema, an exudative multiformny erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis (Lyell's disease).

Local reactions: pain and burning in an injection site, phlebitis.

Others: general weakness, superinfections (candidiasis, pseudomembranous colitis).

Interaction with other medicines:

Owing to decrease of the activity of processes of a microsomal oxidation in hepatocytes, ciprofloxacin increases concentration and extends an elimination half-life of theophylline and other xanthines (for example, caffeine), peroral hypoglycemic drugs, indirect anticoagulants, promotes decrease in a prothrombin ratio.

At simultaneous use with NPVS (except for acetylsalicylic acid) the risk of development of spasms increases.

Metoclopramidum accelerates ciprofloxacin absorption that leads to reduction of time of achievement of the maximum concentration of the last.

Joint purpose of uricosuric drugs leads to removal delay (up to 50%) and increase in plasma concentration of ciprofloxacin.

At a combination to other antimicrobic drugs (beta лактамные antibiotics, aminoglycosides, clindamycin, metronidazole) a synergism is usually observed. Therefore Ciprofloxacin can successfully be applied in a combination with azlotsilliny and a ceftazidime at the infections caused by Pseudomonas spp.; with mezlotsilliny, azlotsilliny and others beta лактамными antibiotics - at streptococcal infections; with izoksazolpenitsillina and Vancomycinum - at staphylococcal infections; with metronidazole and clindamycin - at mephitic gangrenes.

Ciprofloxacin strengthens nephrotoxic effect of cyclosporine, increase in serumal creatinine therefore at such patients control of this indicator 2 times a week is necessary is also noted.

At a concomitant use Ciprofloxacin strengthens effect of indirect anticoagulants.

Pharmaceutical interaction

Infusion solution of drug pharmaceutical is incompatible with all infusion solutions and drugs which physical and chemically are unstable at acid medium (рН infusion solution of ciprofloxacin - 3.5-4.6). It is impossible to mix solution for in/in introductions with the solutions having рН more than 7.

Contraindications:

— deficit glyukozo-6-fosfatdegidrogenazy;

— pseudomembranous colitis;

— children's age up to 18 years (before completion of process of formation of a skeleton);

— pregnancy;

— period of a lactation (breastfeeding).

With care it is necessary to appoint drug at the expressed atherosclerosis of vessels of a brain, disturbances of cerebral circulation, mental diseases, a convulsive syndrome, the epilepsy expressed to a renal and/or liver failure, patients of advanced age.

 

Use of the drug CIPROFLOXACIN at pregnancy and feeding by a breast
Ciprofloxacin is contraindicated to use at pregnancy and in the period of a lactation (breastfeeding).

 

Use at abnormal liver functions
With care it is necessary to appoint drug at the expressed liver failure.

 

Use at renal failures
Patients with a heavy renal failure (KK <20 ml/min. / 1.73 sq.m) need to appoint a half of a daily dose.

 

Use for elderly patients
With care patients of advanced age should appoint.

 

Use for children
Drug is contraindicated to children and teenagers up to 18 years (before completion of process of formation of a skeleton).

Overdose:

Treatment: 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 - or peritoneal dialysis the amount of drug can be removed only insignificant (less than 10%).

Storage conditions:

List B. Drug should be stored in the place protected from light at a temperature from 5 °C to 20 °C in places unavailable to children. Not to freeze! A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

100 ml - bottles of dark glass (1) - a pack cardboard.