Protsipro - instructions for use, doses, side effects, contraindications

Active substance: ciprofloxacin hydrochloride 291.1 mg or 582.2 mg, equivalent to 250 mg or 500 mg of the free base of ciprofloxacin; auxiliary substances: starch, microcrystalline cellulose, magnesium stearate, purified talc, sodium carboxymethyl starch, silicon dioxide colloid, sodium croscarmellose, hypromellose, titanium dioxide, macrogol 6000.

Description:

White or almost white, round, biconvex tablets, covered with a film sheath, with a risk applied on one side.

Pharmacotherapeutic group:Antimicrobial agent, fluoroquinolone.

ATX: & nbsp

J.01.M.A.02 Ciprofloxacin

Pharmacodynamics:

Ciprofloxacin is a synthetic antimicrobial agent of a broad spectrum of action of a group of fluoroquinolones. The main mechanism of action is the suppression of the bacterial DNA-gyrase enzyme, as a result of which the replication of deoxyribonucleic acid and the synthesis of bacterial cell proteins are violated. The drug has a bactericidal effect on gram-negative microorganisms during rest and division and on Gram-positive microorganisms during the fission period.

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. Bioavailability of the drug is 50-85%. Maximum concentration of the drug in the blood serum of healthy volunteers at. 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 kg / ml, respectively.

Orally taken ciprofloxacin distributed in tissues and body fluids. High concentrations of the drug are observed 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 2.0-3.5 l / kg. In the cerebrospinal fluid the drug penetrates in a small amount, where its concentration is 6-10% of that in serum.

The degree of binding of ciprofloxacin to plasma proteins is

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

The main way to remove ciprofloxacin from the body is the kidney. The kidneys deduce 50-70%. From 15 to 30% is excreted through the intestine.

Patients with severe renal insufficiency (creatinine clearance below 20 ml / min / 1.73 m2) should be prescribed half the daily dose of the drug.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ciprofloxacin:

- respiratory tract;

- Ear, throat and nose;

- kidney and urinary tract;

- organs of the small pelvis and genital organs (gonorrhea, prostatitis, adnexitis);

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

- skin, mucous membranes and soft tissues;

- The musculoskeletal system.

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

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

Contraindications:

- Pregnancy;

- lactation period (breastfeeding);

- children and adolescents under the age of 18, except for the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs from 5 to 17 years; prevention and treatment of pulmonary form of anthrax;

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

- simultaneous reception with tizanidine (risk of pronounced blood pressure lowering, drowsiness).

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorder, mental illness, epilepsy, epileptic syndrome, 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 condition of the organism, the age, weight and functions of the kidneys 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;

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

- For the treatment of gonorrhea, cystitis in women (before menopause), 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 2 times a day);

- infections of bones and joints, skin and soft tissue - 500 mg 2 times a day, with a heavy course of 750 mg 2 times a day.

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

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.

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 a suspected or confirmed infection. The total duration of taking ciprofloxacin in the pulmonary form of anthrax is 60 days.

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.

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

Elderly patients are reduced by 30%.

Side effects:

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

Central nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, "nightmarish" dream, peripheral paralgeziya (anomaly perception of feeling pain), increased 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 senses: a violation of taste and smell, visual impairment (diplopia, change in color perception), noise in the ears, hearing loss.

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

On the part of the hematopoiesis system: eosinophilia, leukopenia, neutropenia, change in the number of platelets, hemolytic anemia

From the cardiovascular system: tachycardia, heart rhythm disturbances, arterial hypotension, "hot flashes" of blood to the skin of the face.

Allergic reactions: skin itching, urticaria, the formation of blisters accompanied by bleeding, and the appearance of small nodules that form scabs, drug fever, petechial hemorrhages, facial or laryngeal edema, shortness of breath, vasculitis, erythema nodosa, erythema multiforme exudative including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Laboratory indices: hypoprothrombinemia, increased urea concentration, creatinine, increased activity of "liver" transaminases, alkaline phosphatase, lactate dehydrogenase, bilirubin, hyperglycemia.

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

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

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, to do gastric lavage. Conduct 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 administration of ciprofloxacin with theophylline, oral hypoglycemic agents can cause an increase in their concentration in the blood plasma due to competitive inhibition of the binding sites in the cytochrome P 450, leading to increased half-life of these drugs and increase the risk of toxic action.

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 reception increases the effect of indirect anticoagulants.

Increases the nephrotoxic effect of cyclosporine, there is an increase in serum creatinine, in such patients monitoring of this indicator is required 2 times a week.

Special instructions:

Patients with epilepsy, episodes of seizures in history, vascular diseases and organic brain damage, in connection with the threat of the development of adverse reactions from the CNS ciprofloxacin should be prescribed only for "vital" indications.

Elderly patients with decreased renal function require an individual dose selection. Patients with impaired hepatic and renal function should be given reduced doses of the drug. When treating with fluoroquinolones, anaphylactic reactions can occur. At the first signs of such a reaction, it is necessary to cancel treatment and take urgent measures (administration of adrenaline, glucocorticosteroids).

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 stopped,that individual cases of inflammation and even rupture of tendons during treatment with fluoroquinolones are described.

In order to avoid the development of crystalluria, exceeding the recommended daily dose is inadmissible, adequate fluid intake is also necessary if normal diuresis is observed and urine acid reaction is maintained.

With prolonged treatment with ciprofloxacin, it is necessary to periodically monitor the parameters of kidney function, liver function and peripheral blood parameters.

When taking ciprofloxacin in some patients, phototoxic reactions can occur. Therefore, when taking fluoroquinolone derivatives, patients should avoid exposure to direct sunlight and artificial UV irradiation. And when the first signs of photosensitivity appear, treatment should be canceled.

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

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

Form release / dosage:

The tablets covered with a film membrane on 250 mg and 500 mg.

Packaging:

For 10 tablets in contour mesh aluminum / aluminum or PVC amber / aluminum package (blister).

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 after the expiry date printed on the package!

Terms of leave from pharmacies:On prescription

Registration number:П N011833 / 01

Date of registration:15.09.2008

The owner of the registration certificate:Protek Biosystems Pvt. Ltd.Protek Biosystems Pvt. Ltd. India

Manufacturer: & nbsp

PROTECH BIOSYSTEMS, PVT. Ltd. India

Representation: & nbspProtekh Biosystems Pvt.LtdProtekh Biosystems Pvt.LtdRussia

Information update date: & nbsp22.10.2015

Illustrated instructions

Instructions

Protsipro (Procipro)