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

CORE: Active substance: ciprofloxacin in the form of ciprofloxacin hydrochloride monohydrate 291 mg and 582 mg (corresponding to ciprofloxacin 250 mg, 500 mg). Excipients: microcrystalline cellulose, sodium carboxymethyl starch (type A), povidone, croscarmellose sodium, silicon dioxide colloidal anhydrous, magnesium stearate.

SHELL: hypromellose, talc, titanium dioxide, E171, propylene glycol.

Description:

250 mg tablets: round, biconvex tablets with a bevelled edge and a notch on one side, covered with a film shell of white color.

Tablets 500 mg: oval, biconvex tablets with a notch on one side, covered with a film shell of white color.

Pharmacotherapeutic group:Antimicrobial agent, fluoroquinolone.

ATX: & nbsp

J.01.M.A.02 Ciprofloxacin

Pharmacodynamics:

Antimicrobial preparation of a broad spectrum of action from the group of fluoroquinolones. It is bactericidal. The drug inhibits the DNA enzyme enzyme of bacteria, as a result of which DNA replication and the synthesis of bacterial cell proteins are disturbed.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. Ciprofloxacin It acts both on multiplying microorganisms, and on those in the resting phase.

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., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium (located intracellularly).

Gram-positive aerobic bacteria are also sensitive to ciprofloxacin: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin.

The sensitivity of bacteria Streptococcus pneumoniae, Enterococcus faecalis is moderate.To a drug resistant Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. The effect of the drug against Treponema pallidum has not been adequately studied.

Both in vitro and in vivo, ciprofloxacin is also sensitive to Bacillus anthracis.

Pharmacokinetics:

When taken orally ciprofloxacin quickly absorbed from the gastrointestinal tract. Eating slows down absorption, but does not change the maximum concentration and bioavailability. Bioavailability of the drug is 50-85%. The maximum concentration of the drug in the blood serum of healthy volunteers with oral intake (before meals) of 250, 500, 750 and 1000 mg of the drug is achieved after 1-1.5 hours and is 1.2; 2.4; 4.3 and 5.4 μg / ml, respectively.

Orally taken ciprofloxacin well distributed in the tissues and body fluids. High drug concentrations are observed in bile, lung, kidney, liver, gall bladder, uterus, semen, prostate tissue, tonsils, endometrium, fallopian tubes and ovaries. The concentration of the drug in these tissues is higher than in the serum. Ciprofloxacin also penetrates well into the bones, eye fluid, bronchial secretion, saliva, skin, muscles, pleura, peritoneum, lymph. In the cerebrospinal fluid penetrates in a small amount,where its concentration in non-inflamed meninges is 6-10% of that in the blood serum, and when inflamed - 14-37%. Ciprofloxacin also penetrates well through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in serum.

The volume of distribution in the body is 2-3.5 l / kg. The degree of binding of ciprofloxacin to plasma proteins is 30%.

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

The main way to remove ciprofloxacin from the body is the kidney (50-70%). From 15 to 30% is excreted through the intestine. In patients with unchanged kidney function, the elimination half-life is usually 3-5 hours. In chronic renal failure increases to 12 hours. A small amount is excreted in breast milk.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ciprofloxacin:

respiratory tract: pneumonia (with the exception of pneumococcal pneumonia), acute bronchitis and exacerbation of chronic bronchitis, bronchiectasis, cystic fibrosis (if the causative agent is gram-negative bacteria, especially Pseudomonas aeruginosa);
ear, nose and throat: acute otitis media, sinusitis, mastoiditis;
kidney and urinary tract: uncomplicated and complicated infections of the lower and upper urinary tract (urethritis, cystitis, pyelonephritis);
pelvic and genital organs (epididymitis, prostatitis, salpingitis, endometritis, oophoritis, tubular abscess and pelvic inflammation, gonorrhea, chancroid, chlamydia);
abdominal cavity organs: intraperitoneal abscess; cholecystitis, cholangitis (in combination with metronidazole or clindamycin), infectious diarrhea: salmonellosis, campylobacteriosis, iersiniosis, shigellosis, cholera, typhoid fever, travelers' diarrhea, bacteremia of Salmonella typhi.
skin and soft tissues: infected ulcers, infected wounds, abscesses, phlegmon, infections of the external auditory canal, infected burns;
musculoskeletal system: osteomyelitis, septic arthritis;

Infections in patients with decreased immunity (against immunosuppressant therapy or in patients with neutropenia).

Prevention of infections during surgical interventions (urological, on the gastrointestinal tract (in combination with metronidazole) and orthopedic).

Prevention and treatment of pulmonary form of anthrax.

Contraindications:

Hypersensitivity to ciprofloxacin or other drugs from the quinolone group or any other component of the drug.
Pregnancy and lactation.
Children and adolescents under 18 years (except for the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs in children aged 5 to 17 years, prevention and treatment of pulmonary form of anthrax);
Simultaneous reception with tizanidine (risk of pronounced reduction in blood pressure (BP), drowsiness).

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulatory disorders, mental illness, epileptic syndrome, epilepsy, renal and / or hepatic insufficiency, elderly age, glucose-6-dehydrogenase deficiency, glucocorticosteroid therapy.

Pregnancy and lactation:

During pregnancy and lactation it is not possible to prescribe a drug.

Dosing and Administration:

Inside, 0.25 g 2-3 times a day, with a serious course of infection - 0.5-0.75 g 2 times a day (every 12 hours). The drug should be taken on an empty stomach, swallow tablets whole, with enough liquid.The dose of ciprofloxacin depends on the severity of the disease, the type of infection, the body's condition, age, weight and kidney function in the patient.

Recommended dosing regimens:

uncomplicated infections of the kidneys and urinary tract: 250 mg each, and with complicated infections - 500 mg twice a day; course of treatment of uncomplicated infections of the lower parts of the urinary tract - 3 days; complicated urinary tract infections - 7-10 days;
chronic prostatitis: 500 mg twice a day, treatment duration -28 days;
Infectious-inflammatory diseases of the lower respiratory tract of medium severity - 250 mg - 500 mg, and in more severe cases 750 mg, 2 times a day;
acute gonorrhea: a single dose of ciprofloxacin at a dose of 250 mg - 500 mg; when combined gonococcal infection with Chlamydia and Mycoplasma - 750 mg every 12 hours for 7-10 days;
chancroid: 0.5 g 2 times a day for several days;
bacteriocarrier S.typhi: 250 mg twice a day; course of treatment up to 4 weeks. If necessary, a single dose may be increased to 500 mg or 750 mg;
severe infections (osteomyelitis, infection of the abdominal cavity) - 750 mg 2 times a day. The duration of therapy for osteomyelitis may be up to 2 months;
Gastrointestinal infections caused by Staphylococcus aureus - 750 mg every 12 hours for 7-28 days;
treatment of travelers diarrhea: 500 mg twice a day, duration from 5 to 7 days, in some cases - up to 14 days;
infections of the ear, throat and nose: medium severity 250-500 mg 2 times a day, severe degree 500-750 mg 2 times a day;
in the treatment of complications caused by Pseudomonas aeruginosa, in children with cystic fibrosis of the lungs from 5 to 17 years, the recommended dose of ciprofloxacin is 20 mg / kg of body weight 2 times a day (maximum dose of 1500 mg). Duration of treatment is 10-14 days;
prevention of infections in surgical interventions: from 500 to 750 mg of Ciprinol is prescribed 1-1.5 hours before surgery;
treatment and prevention of anthrax in patients: 500 mg of Cyprinol 2 times a day in adults and 15 mg per kg of body weight of Cyprinol in children 2 times a day. The drug should be taken immediately after a suspected or confirmed infection. At the beginning of treatment, the use of parenteral forms is recommended. The total duration of therapy is 60 days.

The duration of treatment depends on the severity of the disease, but treatment should always last at least three more days after the temperature normalization. Usually the duration of treatment is 7-10 days.

Patients with severe renal dysfunction should be given a half dose of the drug.

Dosing in chronic renal failure (chronic renal failure):
Creatinine clearance ml / min	Dose
>50	normal dosing regimen
30-50	250-500 mg once every 12 hours
5-29	250-500 mg once every 18 hours
patients on hemodialysis or peritoneal dialysis	250-500 mg once every 24 hours

Side effects:

On the part of the digestive system: nausea, diarrhea, vomiting, abdominal pain, flatulence, anorexia, cholestatic jaundice (especially in patients with liver disease), hepatitis, hepatonecrosis, pseudomembranous colitis.

From the central and peripheral nervous system: dizziness, headache, fatigue, agitation, convulsions, anxiety, tremor, insomnia, nightmarish dreams, peripheral paralysis (anomaly of perception of pain), hyperesthesia, hyposthenia, sweating, increased intracranial pressure, confusion, depression, hallucinations, as well as other manifestations of psychotic reactions (occasionally progressing to the states in which the patient can do harm to himself, with suicidal tendencies), a moment Ren.

From the sense organs: a violation of taste and smell, loss of taste (transient), visual impairment (diplopia, change in color perception), tinnitus, hearing loss, transient deafness (especially for high frequencies).

From the side of the cardiovascular system: tachycardia, heart rhythm disturbances, lowering of arterial pressure (BP), fainting, a sensation of "tides" of blood to the skin of the face, thrombosis of the cerebral arteries, peripheral edema.

From the hematopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia, pancytopenia, agranulocytosis, oppression of bone marrow hematopoiesis.

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

Allergic reactions: skin itching, urticaria, blistering accompanied by bleeding and small nodules forming scabs, drug fever, pinpoint hemorrhages (petechiae), edema of the face or larynx, dyspnea,eosinophilia, vasculitis, exantema, nodal erythema, exudative erythema multiforme, Stevens-Johnson syndrome (malignant exudative erythema), toxic epidermal necrolysis (Lyell syndrome), anaphylactic shock, serum sickness.

From the musculoskeletal system: arthralgia, arthritis, tendovaginitis, tendon ruptures, myalgia, edema in the joint region.

Other: general weakness, superinfections (candidiasis, pseudomembranous colitis), increased photosensitivity.

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

Overdose:

Symptoms: nausea, vomiting, diarrhea, headache and dizziness, violations of the liver and kidneys, crystalluria and hematuria, in more severe cases of confusion, tremors, hallucinations and convulsions.

Treatment: symptomatic, gastric lavage, the appointment of activated carbon and laxatives; ensure sufficient supply of liquid. The specific antidote is unknown. Hemodialysis does not have a clinical effect with intoxication.

Interaction:

With simultaneous use with didanosine ciprofloxacin ciprofloxacin absorption decreases due to formation of complexes with ciprofloxacin didanosine contained in the aluminum and magnesium salts. Due to the reduced activity of microsomal oxidation in hepatocytes, increases concentration and prolongs the half-life of theophylline and / or caffeine (xanthines and others.) Of oral hypoglycemic drugs (glibenclamide - which can lead to hypoglycemia), anticoagulants, thereby reducing prothrombin index.

Ciprofloxacin increases C_max 7 times (4 to 21 times) and AUC by 10 times (from 6 to 24 times) tizanidine, which increases the risk of significant decrease in blood pressure and sleepiness.

Simultaneous treatment with non-steroidal anti-inflammatory drugs (except acetylsalicylic acid) - increases the risk of seizures.

Simultaneous administration of antacids, sucralfate, and preparations containing aluminum ions, zinc, calcium, magnesium or iron, may cause a decrease in suction ciprofloxacin, however tsiprinol CP must be taken for 2 hours before taking antacids or after 6 hours after their administration.

With the simultaneous use of ciprofloxacin and cyclosporine, the nephrotoxic effect of cyclosporine is increased (control of the level of the creatinine of the blood 2 times a week is necessary).

Simultaneous administration of ciprofloxacin and glucocorticosteroids may increase the risk of a rupture of tendons.

Simultaneous administration of ciprofloxacin and phenytoin may lead to an increase or decrease in serum concentration of phenytoin. Metoclopramide accelerates the absorption of ciprofloxacin, which leads to a decrease in the time to reach its maximum concentration in the blood plasma.

Joint appointment of uricosuric drugs leads to a delay in excretion (up to 50%) and an increase in the plasma concentration of ciprofloxacin. When combined with other antimicrobial agents (beta-lactams, aminoglycosides, clindamycin, metronidazole) synergy is usually observed: the drug 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.

Simultaneous use of probenecid and ciprofloxacin reduces renal clearance of ciprofloxacin, increasing its plasma concentrations.

Simultaneous administration of ciprofloxacin and mexiletine may lead to an increase in the concentration of mexiletine.

With simultaneous use with ciprofloxacin, tubular transport of methotrexate is reduced, which can potentially lead to an increase in its plasma concentrations. This increases the risk of toxic effects of methotrexate. Patients receiving methotrexate therapy should be carefully monitored during treatment with ciprofloxacin.

Special instructions:

If a severe and prolonged diarrhea occurs during or after treatment with ciprofloxacin, the diagnosis of pseudomembranous colitis should be excluded, which requires immediate discontinuation of the drug and the appointment of appropriate treatment. If pain occurs in the tendons or when the first signs of tendovaginitis appear, treatment should be discontinued due to the fact that individual cases (mainly in elderly patients receiving glucocorticosteroids) of inflammation and even rupture of tendons during treatment with fluoroquinolones are described.During therapy with ciprofloxacin it is recommended to avoid excessive physical exertion.

During the treatment with ciprofloxacin, in order to avoid the development of crystalluria, it is inadmissible to exceed the recommended daily dose. It is also necessary to ensure the intake of a sufficient amount of fluid (under the control of diuresis) to maintain normal diuresis and maintain an acidic urine reaction.

During the period of ciprofloxacin treatment, ultraviolet irradiation should be avoided (including contact with direct sunlight).

During the period of therapy, an increase in the prothrombin index is possible (during surgical interventions it is necessary to monitor the state of the blood coagulation system).

In patients with deficiency of glucose-6-dehydrogenase, the appointment of ciprofloxacin may cause the development of hemolytic anemia.

During treatment, patients should not consume alcohol.

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

Patients receiving ciprofloxacin, you should be careful when driving a car and doing other potentially hazardous activities,requiring increased attention and speed of psychomotor reactions (especially with simultaneous use of alcohol).

Form release / dosage:

Tablets, film-coated, 250 mg and 500 mg.

Packaging:

10 tablets in a blister pack. 1 blister in a cardboard box, along with instructions for use.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

5 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014323 / 01

Date of registration:01.07.2008

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA-RUS, LLC Russia

Representation: & nbspKRKA KRKA Slovenia

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Cyprinol® (Ciprinol®)