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

Ciprinol semi-finished granules, 709.00 mg (corresponding to 500.00 mg of ciprofloxacin) [100 g of semi-finished granules contain ciprofloxacin 70.5219 g, sodium alginate, sodium hydrogen carbonate, lactose monohydrate, giprolose].

Excipients: magnesium stearate 10 mg, silicon dioxide colloidal anhydrous 4 mg, talc 10 mg. Shell: Opadrai-Y-1-7000 * 22 mg.

* Ingredients Opadrai-Y-1-7000: hypromellose, titanium dioxide and macrogol 400 (polyethylene glycol).

Description:

Oval, biconcave, tablets covered with a film coat of white or almost 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, Aeroironas 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:

Suction

When taken orally ciprofloxacin quickly absorbed from the gastrointestinal tract. The maximum plasma concentration (C_max) is achieved 6 hours after ingestion and depends on the dose of the drug. In comparison with ciprofloxacin with immediate release of the substance in a dose of 250 mg, taken twice a day, C_max Cyprinol CP, taken once a day, is higher; while the area under the "concentration-time" curve (AUC) during the day is equivalent.

Pharmacokinetics of ciprofloxacin (prolonged-release tablets, coated film shell).
	FROM_max (ng / ml)	AUC_0-24h (ng / ml)	The elimination half-life (T1) (h)	The time required to reach the maximum concentration (TC_max) (h)
Ciprofloxacin prolonged action 500 mg * 1 time / day	1264,7	7612,4	5	3,6

Bioavailability of the drug is 50-85%. T1 elderly patients may be

is elongated.

Distribution

Ciprofloxacin binds to plasma proteins by 20-40%.The volume of distribution after oral administration of ciprofloxacin varies from 1.74 to 5 l / kg in the equilibrium state, which indicates the active penetration of ciprofloxacin in the tissue.

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 cerebrospinal fluid penetrates in a small amount, where its concentration in uninflated cerebral membranes is 6-10% of that in the serum, and when inflamed - 14-37% (which exceeds the minimum inhibitory concentration for most enterobacteria). Ciprofloxacin penetrates the placenta.

Metabolism

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

Excretion

Ciprofloxacin is excreted mainly by the kidneys: about 50% of the nonmetabolized drug and active metabolites, as well as 11-12% of inactive metabolites.Up to 8% of metabolites are excreted through the intestine.

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 pathogen 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 adolescence under 18 years.
Simultaneous reception with tizanidine (risk of pronounced reduction in blood pressure (BP), drowsiness).
Pseudomembranous colitis;
Pronounced renal (creatinine clearance (CK) <30 mL / min) and / or hepatic insufficiency;
Diseases of the central nervous system (epilepsy, reduced threshold of convulsive readiness, convulsive syndrome in the anamnesis, cerebral circulation disorder, mental diseases).

Carefully:

Severe cerebral artery atherosclerosis, renal and / or hepatic insufficiency, elderly age, deficiency of glucose-6-dehydrogenase (risk of hemolytic anemia),therapy with glucocorticosteroids.

Pregnancy and lactation:

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

Dosing and Administration:

Inside, 1 time per day. The drug should be taken after meals, swallow tablets whole, without chewing and washing down with a sufficient amount of liquid. The dose of ciprofloxacin depends on the severity of the disease, such as infection, body condition, age, weight and kidney function in the patient.

Recommended dosing regimens:

Indication	Degree of severity	Daily dose	Multiplicity of reception	The usual duration of treatment *
Infectious-inflammatory diseases of the ear, throat and nose	Light / moderate	1000 mg	1 time per day	10 days
Infectious and inflammatory diseases of the lower respiratory tract: pneumonia (with the exception of pneumococcal pneumonia), acute bronchitis and exacerbation of chronic bronchitis, bronchiectasis, cystic fibrosis (if the pathogen is Gram-negative bacteria, especially Pseudomonas aeruginosa)	Light / moderate Heavy / complicated	1000 mg 1500 mg	1 time per day 1 time per day	7-14 days 7-14 days
Infections of the kidneys and urinary tract. Acute uncomplicated cystitis	Light / moderate	500 mg 500 mg	1 time per day 1 time per day	3 days 7-14 days
	Heavy / complicated	1000 mg	1 time per day	7-14 days
Chronic bacterial prostatitis	Light / moderate	1000 mg	1 time per day	28 days
Infectious and inflammatory diseases of the abdominal cavity: intraperitoneal abscess, cholecystitis, cholangitis (in combination with metronidazole or clindamycin)	Complicated	1000mg	1 time per day	7-14 days
Infections of the skin and soft tissues	Light / moderate Heavy / complicated	1000 mg 1500 mg	1 time per day 1 time per day	7-14 days 7-14 days
Infectious and inflammatory diseases of the musculoskeletal system: osteomyelitis, septic arthritis	Light / moderate Heavy / complicated	1000 mg 1500 mg	1 time per day 1 time per day	4-6 weeks 4-6 weeks
Infectious diarrhea	Lightweight / moderate / heavy	1000 mg	1 time per day	5-7 days
Typhoid fever	Light / moderate	1000 mg	1 time per day	10 days
Gonorrhea	Complicated	500 mg	1 time per day	3-5 days

Treatment should be continued, at least for another 2 days after the disappearance of symptoms and signs of infection. In severe infections, treatment can begin with parenteral forms of the drug, then go on oral intake of the drug.

In elderly people, the dose of the drug is reduced depending on the creatinine clearance, the nature and severity of the infectious disease.

Dosing for patients with impaired renal function:

Creatinine clearance	Serum Creatinine	Dose
> 50 ml / min	<120 μmol (<1.4 mg / 100 ml)	Usual Dose
30-50 ml / min	120-179 μmol (1.4-1.9 mg / 100 ml)	500-1000 mg / day

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 decrease in the activity of microsomal oxidation in hepatocytes, it increases the concentration and prolongs the half-life of theophylline and / or caffeine (and other xanthines), oral hypoglycemic drugs (glibenclamide - which can lead to hypoglycemia), indirect anticoagulants, and decreases the prothrombin index.

Ciprofloxacin increases C_max 7 times (4 to 21 times) and AUC 10 times (6 to 24 times) of tizanidine, which increases the risk of a marked decrease in blood pressure and drowsiness.

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

Simultaneous administration of antacids, sucralfate, as well as preparations containing ions of aluminum, zinc, calcium, iron or magnesium, can cause a decrease in absorption of ciprofloxacin, so Ciprinol CP should be taken 2 hours before taking antacids or 6 hours after their intake.

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 treatmentfluoroquinolones. 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, 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:

Tablets of prolonged action, film-coated, 500 mg.

Packaging:

5 or 7 tablets in a contour cell package.

1 circuit cell pack of 7 tablets or 2 contour packs of 5 tablets together with instructions for use are placed in a pack of cardboard.

Storage conditions:

Store at a temperature of no higher than 25 ° C in the original packaging.

Keep out of the reach of children.

Shelf life:

Shelf life 5 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-007078/08

Date of registration:04.09.2008

The owner of the registration certificate:KRKA-RUS, LLC KRKA-RUS, LLC Russia

Manufacturer: & nbsp

KRKA-RUS, LLC Russia

Information update date: & nbsp20.10.2015

Illustrated instructions

Instructions

Ciprinol® SR (Ciprinol® SR)