Tsiprinol CP

Active material: Ciprofloxacin
When ATH: J01MA02
CCF: Fluoroquinolone antibacterial drug
ICD-10 codes (testimony): A00, A01, A02, A03, A04.5, A04.6, A09, A22, A54, A56.0, A56.1, A57, E84, H66, H70, J01, J15, J20, J32, J42, J47, K65.0, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, M00, M86, N10, N11, N30, N34, N41, N45, N70, N71, N72, N73.0, T79.3, Z29.2
When CSF: 06.17.02.01
Manufacturer: KRKA d.d. (Slovenia)

Pharmaceutical form, composition and packaging

Sustained-release tablets, Film-coated white or nearly white, Oval, lenticular.

Excipients: magnesium stearate, Colloidal anhydrous silica, talc.

* – 100 g semi-finished product-granules contain ciprofloxacin 70.5219 g, sodium alginate, natriya carbonate, lactose monohydrate, giprolozu.

The composition of the shell: opadraj-Y-1-7000 (gipromelloza, Titanium dioxide, macrogol 400).

5 PC. – packings Valium planimetric (2) – packs cardboard.
7 PC. – packings Valium planimetric (1) – packs cardboard.

Pharmacological action

Antibacterial drug broad-spectrum fluoroquinolones from the Group. Effective bactericidal. Inhibits the enzyme DNA gyrase, as a result of which violated DNA replication and synthesis of cell proteins of bacteria. Low toxicity to cells macroorganism's due to the lack of DNA gyrase. Ciprofloxacin acts as the breeding of microorganisms, and micro-organisms, are in the resting phase.

To ciprofloxacin susceptible gram-negative aerobic bacteria: enterobacteria (Escherichia coli, Salmonella spp., Shigella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Proteus is wonderful, Proteus vulgaris, Serratia wilting, Hafnia avenue, 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.); certain intracellular pathogens: Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium (located intracellularly).

To ciprofloxacin sensitive Gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus man, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae). Bolshinstvostafilokokkov, resistant to metitillino, resistant to ciprofloxacin.

C drug moderately sensitive Streptococcus pneumoniae, Enterococcus faecalis.

C drug resistant Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophila, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroids.

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

The drug against Treponema pallidum unclear.

When taking Ciprinola^® WED development do not occur parallel resistance to other antibiotics, do not belong to the Group of gyrase inhibitors, that makes it highly effective against bacteria, that is resistant to aminoglycosides, penicillins, cephalosporins, tetracycline.

Pharmacokinetics

Absorption

After taking the drug inside ciprofloxacin is rapidly absorbed from the digestive tract. Bioavailability is 50-85%. C_max of serum is reached after 6 hours and depends on the dose of the drug.

Compared with ciprofloxacin with immediate release of substances in the dose 250 mg, taken 2 times / day, FROM_makh Ciprinola^® CP, received on 500 mg 1 time / day, higher; with indicators of AUC during the day equivalent. C_max is 1264 ng / ml, T_max – 3.6 no, AUC_0-24 – 7612.4 NG × h/ml.

Distribution

Ciprofloxacin is well distributed in the tissues and body fluids, While high concentrations are set in bile, light, kidney, liver, gallbladder, uterus, seminal fluid, Prostate tissue, tonsils, the endometrium, the fallopian tubes and ovaries. Concentration of ciprofloxacin in these tissues above, than serum. Ciprofloxacin also penetrates into bone, eye fluid, bronchial secretion, spittle, skin, muscle, in the pleura, the peritoneum and lymph. In spinnomozgovu liquid penetrates into the small number of, concentration of ciprofloxacin in nevospalennyh brain membranes is 6-10% from that in serum, When inflamed – 14-37% (that exceeds the MICK for most enterobacteria).

V_d is 1.74-5 l / kg, that testifies to the active penetration of ciprofloxacin in fabric.

Plasma protein binding – 20-40%.

It penetrates through the placental barrier.

Metabolism

It is metabolized in the liver (15-30%) with the formation of low metabolites (dijetilciprofloksacin, sul'fociprofloksacin, oksiciprofloksacin, formilciprofloksacin).

Deduction

Ciprofloxacin displayed mainly kidneys: about 50% nemetabolizirovannogo preparation and active metabolites, and 11-12% inactive metabolites. To 8% metabolites are excreted through the intestines.

T_1/2 is 5 no.

Pharmacokinetics in special clinical situations

Older patients T_1/2 lengthens.

Testimony

Infectious-inflammatory diseases, caused by susceptible to malaria infections, including:

-respiratory tract: pneumonia (with the exception of pneumococcal pneumonia), acute bronchitis and exacerbation of chronic bronchitis, bronchiectasis, mukovystsydoz (If the activator is a 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 urinary tract and upper sections/baby, cystitis, medicine/);

-pelvic and genital organs (epididymitis, prostatitis, salpingitis, endometritis, oophoritis, tubulyarnyi abscess and pelvioperitonit, gonorrhea, chancroid, Chlamydia);

-abdominal organs (vnutribrjushinnyj abscess, cholecystitis, cholangitis/in combination with metronidazole or clindamycin/);

-infectious diarrhea (salmonellosis, Campylobacteriosis, iersinioz, dysenteries, cholera, typhoid fever, travelers' diarrhea, bakterionositelstvo Salmonella typhi);

-skin and soft tissues (infected ulcers, infected wounds, abscesses, flegmona, infection of external auditory meatus, infected burns);

-Musculoskeletal System (osteomyelitis, septicheskiy arthritis).

Infections in patients with low immunity (While therapy immunodepressantami or in patients with neutropenia).

Prevention and treatment of the pulmonary form of anthrax.

Dosage regimen

Assign inside 1 time / day, after meal. The tablets should be swallowed whole, not chewing and drinking plenty of fluids.

Dose of antibiotic depends on the severity of the disease, type of infection, condition of the body, age, body weight and renal function.

At infectious and inflammatory diseases of the ear, nose and throat mild appoint 1 g 1 times / day for 10 days.

At infectious and inflammatory diseases lower respiratory tract infection (pneumonia/except pneumococcal pneumonia/, acute bronchitis and exacerbation of chronic bronchitis, bronchiectasis, cystic fibrosis/if the activator is a gram-negative bacteria, especially Pseudomonas aeruginosa/) mild to moderate severity appoint 1 g 1 times / day for 7-14 days, the heavy severity or complicated diseases – 1.5 g 1 times / day for 7-14 days.

At acute uncomplicated cystitis – by 500 mg 1 times / day for 3 days.

At Kidney and urinary tract infections, mild – by 500 mg 1 times / day for 7-14 days, severe and complicated diseases – by 1 g 1 times / day for 7-14 days.

At Chronic bacterial prostatitis mild and moderate- by 1 g 1 times / day for 28 days.

At complications of infectious and inflammatory diseases of the abdominal cavity organs (vnutribrjushinnyj abscess, cholecystitis, cholangitis/in combination with metronidazole or clindamycin/) – by 1 g 1 times/day for 7-14 days.

At infections of skin and soft tissues of mild to moderate severity appoint 1 g 1 times / day for 7-14 days, the heavy severity or complicated diseases – 1.5 g 1 times / day for 7-14 days.

At infectious and inflammatory diseases Musculoskeletal System (osteomyelitis, septicheskiy arthritis) mild to moderate severity appoint 1 g 1 times / day for 4-6 weeks, the heavy severity or complicated diseases – 1.5 g 1 times / day for 4-6 weeks.

At infectious diarrhea easy, moderate and severe degree of severity - By 1 g 1 times / day for 5-7 days.

At bruchnom tife mild - By 1 g 1 times / day for 10 days.

At uncomplicated gonorrhoea - By 500 mg 1 times / day for 3-5 days.

Treatment should continue to, least, for another 2 days after the disappearance of symptoms and signs of infection.

With heavy infections can begin treatment with Parenteral drug form, in the future, go to oral medication.

In elderly patients dose decrease depending on creatinine clearance, the nature and severity of infectious diseases.

Dosing for patients with impaired renal function.

Side effect

From the digestive system: nausea, diarrhea, vomiting, abdominal pain, flatulence, anorexia, cholestatic jaundice (especially in patients with pre-existing liver disease), hepatitis, gepatonekroz, psevdomembranoznыy colitis.

Part of the central and peripheral nervous system: dizziness, headache, fatigue, excitation, convulsions, anxiety, tremor, insomnia, nightmares, peripheral paralgezija (anomaly of the perception of pain), giperesteziya, gipostezii, Sweating, intracranial hypertension, confusion, depression, hallucinations, as well as other manifestations of psychotic reactions (occasionally progressive to States, in which the patient may cause harm, with suicidal tendencies), migraine.

From the senses: the taste and smell, transient loss of taste, visual impairment (diplopia, change of color), noise in ears, hearing loss, transient deafness (especially for high frequencies).

Cardio-vascular system: tachycardia, abnormal heart rhythm, decrease in blood pressure, fainting, feeling tidal blood to the skin, thrombosis of cerebral arteries, peripheral edema.

From the hematopoietic system: leukopenia, granulocytopenia, anemia, grombocitopenija, leukocytosis, thrombocytosis, gemoliticheskaya anemia, pancytopenia, agranulocytosis, suppression of bone marrow hematopoiesis.

By mochevydelitelnoj systems: hematuria, kristallurija (particularly in alkaline urine and low diureze), glomerulonephritis, dizurija, polyuria, urinary retention, albuminuria, Urethral bleeding, azotovydelitelnoj reduced kidney function, interstitial nephritis.

On the part of the musculoskeletal system: arthralgia, arthritis, tendinitis, tendon rupture, myalgia, swelling in the area of joint.

From the laboratory parameters: gipoprotrombinemii, increase in liver transaminases and alkaline phosphatase, giperkreatininemiя, giperʙiliruʙinemija, hyperuricemia, giperglikemiâ.

Allergic reactions: itching, hives, bullation, accompanied by bleeding, and small nodules, forming scabs, drug fever, pinpoint hemorrhages (petechiae), swelling of the face or larynx, breathlessness, eozinofilija, vasculitis, rash, Nodular Erythema, mnogoformnaya Erythema ekssoudatus, Stevens-Johnson syndrome (malignant exudative erythema), toxic epidermal necrolysis (Lyell's syndrome), anaphylactic shock, serum sickness.

Other: generalized weakness, superinfekcii (candidiasis, psevdomembranoznыy colitis), increased light sensitivity.

Contraindications

-simultaneous reception tizanidinom (the risk of significant decrease in blood pressure, drowsiness);

- Psevdomembranoznыy colitis;

— expressed kidney (CC less than 30 ml / min) and/or liver failure;

-central nervous system diseases (epilepsy, low threshold sudorojna preparedness, sudorozhny syndrome in history, cerebrovascular accident, mental diseases);

- Pregnancy;

- Lactation (breast-feeding);

- Childhood and adolescence up 18 years;

-hypersensitivity to ciprofloxacin or other drugs from quinolone or any other component of the drug.

FROM caution should designate product if expressed farm cerebrovascular, kidney and / or liver failure, definition, glucose-6-fosfatdegidrogenazы (risk of hemolytic anemia), therapy, glucocorticosteroids it, elderly patients.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breast-feeding).

Cautions

When encountered during or after treatment of ciprofloxacin is severe and prolonged diarrhea should exclude the diagnosis psevdomembranoznogo colitis, that requires the immediate withdrawal of the drug and the appropriate treatment.

If you experience pain in the joints or at the first signs of treatment should be discontinued because, that describes selected cases (mostly in elderly patients, at the same time receiving SCS) inflammation and even rupture the tendons during treatment with fluoroquinolones. During therapy, it is recommended to avoid excessive ciprofloxacin physical exertion.

During the treatment of ciprofloxacin, to avoid christallurii, unacceptable overextending dose. It is also necessary to ensure sufficient intake of fluid (under the control of diuresis) to comply with normal urine output and the maintenance of acid reaction urine.

During treatment, ciprofloxacin should be avoided to ultraviolet radiation (incl. contact with direct sunlight).

During therapy can increase prothrombin index (When performing surgical interventions should monitor the State of blood coagulation system).

In patients with a deficit glukozo-6-fosfatdegidrogenaza appointment of ciprofloxacin may cause the development of hemolytic anemia.

During treatment, patients should not drink alcohol.

Effects on ability to drive vehicles and management mechanisms

Patients, host ciprofloxacin, Use caution when driving and other potentially hazardous activities, require increased attention and psychomotor speed reactions (especially while drinking habits).

Overdose

Symptoms: nausea, vomiting, diarrhea, headache and dizziness, violations of the liver and kidney, christalluria and hematuria, in more severe cases, confusion, tremor, hallucinations and convulsions.

Treatment: gastric lavage, the appointment of activated charcoal and laxatives. An adequate intake of fluids. Symptomatic therapy. Spetsificheskiy antidote unknown. Hepatology has no clinical effect of intoxication.

Drug Interactions

Together with the use of ciprofloxacin with DDI absorption of ciprofloxacin is reduced due to the formation of complexes of ciprofloxacin with didanozine aluminium and magnesium salts.

As a result of reduced activity processes mikrosomalnogo oxidation in gepatocitah, improves concentration and lengthens t_1/2 Theophylline and/or caffeine (and other xantinov), oral hypoglycemic drugs (glibenclamide – that can lead to hypoglycemia), anticoagulants (helps reduce prothrombin index).

Ciprofloxacin increases with_makh in 7 time (from 4 to 21 times) and AUC 10 time (from 6 to 24 time) tizanidine increases for, that increases the risk reduction expressed ad and sleepiness.

Simultaneous reception NPVS (excluding acetylsalicylic acid) It increases the risk of seizures.

Admission antatsidov, sucralfate, as well as preparations, containing ions aluminium, Zinc, Calcium, iron or magnesium, can cause reduced intake of ciprofloxacin, therefore Ciprinol^® CP must be 2 hours before receiving antatsidov or through 6 hours after administration.

While applying ciprofoksacina and Cyclosporine amplified nefrotoksicescoe effects of Cyclosporine (requires control of creatinine blood levels 2 times a week).

Simultaneous reception of ciprofloxacin and SCS may increase the risk of tendon rupture.

The simultaneous appointment of ciprofloxacin and fenitoina may increase or decrease in serum concentration fenitoina.

Metoclopramide accelerates the absorption of ciprofloxacin, that leads to a decrease in time achieve it with_makh plasma.

Joint appointment urikozuricheskih drugs leads to slower excretion (to 50%) and increased plasma concentration of ciprofloxacin.

When combined with other antimicrobial drugs (beta-lactam antibiotics, aminoglikozidy, klindamiцin, metronidazol) usually observed synergy. The drug can be used successfully in combination with azlocillinom and ceftazidimom infections, caused by Pseudomonas spp.; with mezlocillinom, azlocillinom and other beta-lactam antibiotics – when streptococcal infections; with izoksazolilpenicillinami and vankomitinom – When staphylococcal infections; with metronidazole and clindamycin – under anaerobic infections.

Simultaneous use of probenecida and ciprofloxacin reduces kidney klirens ciprofloxacin, increasing its concentration in the plasma.

The simultaneous introduction of ciprofloxacin and mexiletina can lead to increased concentrations of mexiletina.

With simultaneous use with ciprofloxacin, the tubular transport of methotrexate decreases, which can potentially lead to an increase in its plasma concentrations. This increases the risk of toxic effects of methotrexate. Patients, receiving methotrexate therapy, it is necessary to be under close medical supervision during the period of treatment with ciprofloxacin.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children at or above 30 ° C. Shelf life – 2 year.