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

Each tablet, film-coated, 250 mg or 500 mg contains: Excipients: corn starch, silicon dioxide colloid, povidone, magnesium stearate, carboxymethyl starch sodium, microcrystalline cellulose, shell composition: hypromellose, titanium dioxide, talc purified, macrogol 6000.

Description:

250 mg tablets: round, biconcave tablet form, coated with a white or white film cover with a yellowish hue, with a half-and-half risk on one side.

Tablets 500 mg: oblong, biconvex form of a tablet covered with a film coat of white or with a white with a yellowish hue.

Pharmacotherapeutic group:Antimicrobial agent, fluoroquinolone.

ATX: & nbsp

J.01.M.A.02 Ciprofloxacin

Pharmacodynamics:

A broad-spectrum antimicrobial agent, a derivative of fluoroquinolone, inhibits bacterial DNA-gyrase, breaks down the synthesis of DNA, growth and division of bacteria; causes significant morphological changes (including the cell wall and membranes) and the rapid death of the bacterial cell. 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 Corynebacterium diphtheriae; Gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae).

Both in vitro and in vivo studies of ciprofloxacin are also sensitive to Bacillus anthracis.

The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin. The sensitivity of Streptococcus pneumoniae, Enterococcus faecalis is moderate.

The drug is resistant: Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides. It is effective against Treponema pallidum.

Pharmacokinetics:

When taken orally ciprofloxacin quickly absorbed from the gastrointestinal tract. 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 distributed in tissues and body fluids. High concentrations of the drug are achieved in bile, lungs, kidneys, liver, gall bladder, uterus, seminal fluid, 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.

The accumulating 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. In the cerebrospinal fluid the drug penetrates in a small amount, where its concentration is 6-10% of that of serum.

The degree of binding of ciprofloxacin to plasma proteins is 30%.

In patients with unchanged kidney function, the elimination half-life is usually 3-5 hours.If the kidney function is impaired, the elimination half-life increases.

The main way to remove ciprofloxacin from the body is the kidney. With the kidneys is deduced 50-70%. From 15 to 30% is excreted through the gastrointestinal tract. A small amount is excreted in breast milk. Kidney clearance of 3-5 ml / min / kg; total clearance - 8 - 10 ml / min / kg.

Patients with severe renal insufficiency (creatinine clearance below 20 ml / min / 1.73 m²) it is necessary to prescribe half the daily dose of the drug.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms:

- diseases of the respiratory tract (bronchitis, pneumonia, bronchiectasis, cystic fibrosis;

- infection of the ENT organs (otitis media, sinusitis);

- infection of the kidneys and urinary tract (cystitis, pyelonephritis);

- infections of the pelvic organs and genital organs (prostatitis, adnexitis, salpingitis, oophoritis, endometritis, tubular abscess, gonorrhea, soft chancre);

- Digestive system (including mouth, teeth, jaws); gallbladder and bile ducts;

- infections of the skin and soft tissues (infected ulcers, wounds, burns, abscesses, phlegmon);

- infection of bones and joints;

- prevention and treatment of infections in patients with reduced immunity (with immunosuppressant therapy), as well as the prevention and treatment of pulmonary form of anthrax (infection with Bacillus anthracis).

Pediatric use: treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs aged 5 to 17 years; prevention and treatment of pulmonary form of anthrax.

Contraindications:

-increased sensitivity to ciprofloxacin or other drugs from the group of fluoroquinolones;

- simultaneous administration of tizanidine (risk of pronounced reduction in blood pressure, drowsiness);

-pregnancy;

-period of lactation;

-Children and adolescents (up to the age of 18 - the completion of the formation of the skeleton, in addition to the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs aged 5 to 17 years; prevention and treatment of pulmonary form of anthrax);

- pseudomembranous colitis.

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, epileptic syndrome, epilepsy, marked renal and / or hepatic insufficiency, elderly age.

Dosing and Administration:

Inside, 0.25 g 2 - 3 times a day, with severe infections - 0.5 - 0.75 g 2 times a day (every 12 hours). The drug should be taken on an empty stomach, washed down with a sufficient amount of 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 doses are usually:

- uncomplicated diseases of the kidneys and urinary tracts - 250 mg each, and in complicated cases 500 mg twice a day;

- uncomplicated infections of the lower respiratory tract - 250 mg, and in more severe cases 500 - 750 mg, 2 times a day;

- for the treatment of gonorrhea, a single administration of ciprofloxacin in a dose of 250-500 mg is recommended;

- gynecological diseases, enteritis and colitis with severe course and high temperature, prostatitis - 500 mg 2 times a day (for the treatment of banal diarrhea can be used at a dose of 250 mg twice a day);

- infection of bones and joints - 750 mg twice a day.

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

In the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs aged 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 and treatment of pulmonary form of anthrax: adults - 500 mg 2 times a day; children (5-17 years) - 15 mg / kg of weight 2 times a day should not exceed a maximum single dose of 500 mg and a daily dose of 1000 mg. The drug should be taken immediately after the alleged and confirmed infection. The total duration of taking ciprofloxacin in the pulmonary form of anthrax is 60 days.

Patients with impaired renal function should adjust the dosage regimen.

Table of recommended doses of the drug for patients with chronic renal failure:

Creatinine clearance ml / min	Dose
>50	The usual dosing regimen
30-50	250-500 mg once every 12 hours
5-29	250-500 mg once every 18 hours
Patients on hemolytic or peritoneal dialysis	after dialysis 250-500 mg once every 24 hours

Side effects:

From the gastrointestinal tract: nausea, diarrhea, vomiting, abdominal pain, flatulence, anorexia, cholestatic jaundice (especially in patients with liver disease), hepatitis, hepatonecrosis.

From the nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, nightmarish dreams, peripheral paralysis (anomaly of perception of pain), sweating, increased intracranial pressure, confusion, depression, hallucinations, and other manifestations of psychotic reactions (occasionally progressing to conditions in which the patient can do harm to himself), migraine, fainting, thrombosis of the cerebral arteries.

From the sense organs: violation of taste and smell, visual impairment (diplopia, change in color perception), tinnitus, hearing loss.

From the cardiovascular system: tachycardia, heart rhythm disturbances, lowering blood pressure, flushing of blood to the skin of the face.

From the hematopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia.

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

From 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.

From the musculoskeletal system: arthralgia, arthritis, tendovaginitis, tendon ruptures, myalgia.

Allergic reactions: itching, urticaria, the formation of blisters accompanied by bleeding and small nodules that form scabs, drug fever, pinpoint hemorrhages (petechiae), face and laryngeal edema, shortness of breath, eosinophilia, vasculitis, nodal erythema, exudative erythema multiforme, Stevens-Johnson syndrome (malignant exudative erythema), toxic epidermal necrolysis (Lyell's syndrome).

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

Overdose:

There is a reversible toxic effect on the kidneys. The specific antidote is unknown. It is necessary to carefully monitor the patient's condition, make gastric lavage, carry out usual emergency measures, ensure sufficient fluid intake.With the help of hemo- or peritoneal dialysis, only a small amount (less than 10%) of the drug can be excreted.

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.

Simultaneous reception of ciprofloxacin with theophylline, oral hypoglycemic agents can lead to an increase in their concentration in the blood plasma, due to competitive inhibition in the binding sites of cytochrome P 450, which leads to an increase in the half-life of these drugs and an increased risk of toxic effects.

When combined with other antimicrobial drugs (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole) synergy is usually observed; can be successfully used in combination with azlocillin and ceftazidime in infections caused by Pseudomonas spp .; with mezlocillin, azlocillin, etc. beta-lactam antibiotics - with streptococcal infections; with isoxazolylpenicillins and vancomycin - with staphylococcal infections; with metronidazole and clindamycin - with anaerobic infections.

Non-steroidal anti-inflammatory drugs (excluding acid acetylsalicylic) increase the risk of seizures.

Metoclopramide accelerates absorption, which leads to a decrease in the time to reach its maximum concentration in the blood plasma.

The joint administration of uricosuric medicines leads to a delay in excretion (up to 50%) and an increase in the plasma concentration of ciprofloxacin.

Increases the maximum concentration in blood plasma by 7 times (from 4 to 21 times) of tizanidine, which increases the risk of pronounced reduction in blood pressure and drowsiness.

Simultaneous reception of antacids, as well as preparations containing ions of aluminum, zinc, iron or magnesium, can cause a decrease in absorption of ciprofloxacin, so the interval between the appointment of these drugs should be at least 4 hours.

With simultaneous use of ciprofloxacin and anticoagulants, bleeding time is prolonged.

With the simultaneous use of ciprofloxacin and cyclosporine, the nephrotoxic effect of the latter is enhanced.

Special instructions:

Patients with epilepsy, episodes of seizures in history, vascular diseases and organic brain damage due to the threat of development of adverse reactions withside of the central nervous system, ciprofloxacin should be prescribed only for "vital" indications.

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 tendons or when the first signs of tendovaginitis appear, treatment should be discontinued due to the fact that individual cases of inflammation and even rupture of tendons during treatment with fluoroquinolones are described.

During the treatment with ciprofloxacin it is necessary to provide a sufficient amount of fluid while observing a normal diuresis.

During treatment with ciprofloxacin, UV irradiation should be avoided.

Effect on the ability to drive transp. cf. and fur:Patients receiving ciprofloxacin, care should be taken when driving a car and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Film coated tablets, 250 mg and 500 mg.

Packaging:For 10 tablets in a blister (material for manufacturing a blister: aluminum foil / PVC - film). For 1 or 10 blisters together with the instructions for use are placed in a cardboard box.

Storage conditions:

At a temperature not higher than 30 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use at the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N008909

Date of registration:16.05.2008

The owner of the registration certificate:Cadil Haltkar Co., Ltd.Cadil Haltkar Co., Ltd. India

Manufacturer: & nbsp

CADILA HEALTHCARE, Ltd. India

Representation: & nbspCADILA HELTKER LTD. CADILA HELTKER LTD. India

Information update date: & nbsp23.10.2015

Illustrated instructions

Instructions

Ciprobide (Ciprobid)