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

Excipients: cellulose, microcrystalline 54,025 mg, magnesium, stearate 3,5 mg, sodium carboxymethyl starch 10.5 mg, silicon dioxide colloid 0,875 mg, film sheath: hypromellose (15 cps) 3.8 mg, talc 3.62 mg titanium dioxide 1.24 mg, macrogol - 6000 0.76 mg, silicon dioxide colloidal 0.58 mg.

Tablets 500 mg:

Active substance: Ciprofloxacin hydrochloride (monohydrate) in terms of ciprofloxacin 500 mg;

Excipients: cellulose microcrystalline 108.08 mg, magnesium stearate 7.0 mg, sodium carboxymethyl starch: 21.0, silicon dioxide colloid 1.75 mg, film sheath: hypromellose (15 cps) 7.6 mg, talc 7.24 mg, titanium dioxide 2.48 mg, macrogol - 6000 1.52 mg, silicon dioxide colloid 1.16 mg.

Description:

250 mg: White or almost white round biconvex tablet coated with a film membrane; cross-sectional view: tablet core and outer ring of white or almost white shell.

500 mg: White or almost white capsular tablet,Film coated with a notch on one side; cross-sectional view: tablet core and outer ring of white or almost white shell.

Pharmacotherapeutic group:Antimicrobial agent, fluoroquinolone

ATX: & nbsp

J.01.M.A.02 Ciprofloxacin

Pharmacodynamics:

A broad-spectrum antimicrobial agent, a quinolone derivative, suppresses bacterial DNA gyrase (topoisomerases II and IV, responsible for the process of supercoiling the chromosomal DNA around the nuclear RNA, which is necessary for reading the genetic information), disrupts DNA synthesis, growth and division of bacteria; causes significant morphological changes (including the cell wall and membranes) and the rapid death of the bacterial cell.

It acts bacteriocally on non-negative organisms in the period of rest and division (since it affects not only the DNA-gyrase, but also causes lysis of the cell wall), gram-positive microorganisms - only during the fission period.

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 drugs.antibiotics not belonging 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 is sensitive to Gram-negative aerobic bacteria: 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., 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).

It is active against Bacillus anthracis in vitro.

The majority of staphylococci, resistant to methicillin, are resistant to ciprofloxacin. Sensitivity of Streptococcus pneumoniae, Enterococcus faecalis, Mycobacterium avium (located intracellularly) - moderate (high concentrations are required to repress).

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

Resistance develops very slowly, because on the one hand, after the action of ciprofloxacin are left with persistent microorganisms, and on the other - the bacterial cells do not have the enzymes that inactivate it.

Pharmacokinetics:

When taken orally ciprofloxacin quickly and quite fully absorbed from the gastrointestinal tract (mainly in the 12-finger and jejunum). Eating slows down absorption, but does not change the bioavailability and maximum concentration (C_max). Bioavailability is 50-85%, volume of distribution is 2 - 3.5 l / kg, communication with plasma proteins is 20-40%. The time to reach the maximum concentration (TC_max) 60-90 min, C_max linearly depends on the value of the dose taken and is at doses of -. 250, 500, 750 and 1000 mg, respectively, 1.2, 2.4, 4.3 and 5.4 μg / ml. After 12 hours after ingestion of 750 mg and 250.500 drug concentration in the plasma is reduced to 0.1, 0.2 and 0.4 mcg / ml, respectively.

Well distributed in body tissues (excluding tissue, rich in fats, for example, nervous tissue). Concentration in tissues is 2-12 times higher than in plasma. Therapeutic concentrations are achieved in saliva, tonsils, liver, gall bladder, bile, intestine, abdominal and pelvic organs (endometrium, fallopian tubes and ovaries, uterus), seminal fluid, prostate tissue, kidney and urinary organs, lung tissue, bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin.The cerebrospinal fluid penetrates in a small amount, where its concentration in the absence of inflammation of the meninges is 6-10% of that in the blood serum, and in the presence of inflammation - 14-37%. Ciprofloxacin well penetrates also into the eye fluid, bronchial secretion, pleura, peritoneum, lymph, through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in blood serum. The activity decreases somewhat at pH <less than 6.

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

Half-life (T_1/2) - about 4 hours, with chronic renal failure (CRF) - up to 12 hours. It is mainly excreted by the kidneys by tubular filtration and tubular secretions in unchanged form (40-50%) and in the form of metabolites (15%), the rest - through intestines.

A small amount is excreted in breast milk.

Kidney clearance - 3-5 ml/mines/kg; total clearance 8-10 ml / min/kg. .

With CRF (creatinine clearance (CC) above 20 ml/min), the percentage of the drug released through the kidneys is reduced, but cumulation in the body does not occur due to a compensatory increase in the metabolism of the drug and excretion through the intestine.

Indications:

Adults. Infectious-inflammatory diseases caused by microorganisms sensitive to ciprofloxacin:

diseases of the lower respiratory tract (acute and chronic (at the stage of exacerbation) bronchitis, pneumonia, bronchiectatic disease, infectious complications of cystic fibrosis);
infection of the ENT organs (acute sinusitis);
infection of the kidneys and urinary tract (cystitis, pyelonephritis);
Complicated intra-abdominal infections (in combination with metronidazole), including peritonitis;
chronic bacterial prostatitis;
uncomplicated gonorrhea;
typhoid fever, infectious diarrhea (including campylobacteriosis, shigellosis, diarrhea of "travelers");
infections of the skin and soft tissues (infected ulcers, wounds, burns, abscesses, phlegmon);
bones and joints (osteomyelitis, septic arthritis);
septicemia;
infection on the background of immunodeficiency (arising in the treatment of immunosuppressive drugs or in patients with neutropenia).

Prevention and treatment of pulmonary form of anthrax.

Children. Therapy 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 (infection with Bacillus anthracis).

Contraindications:

Hypersensitivity to ciprofloxacin or other drugs of the quinolone group, as well as to auxiliary substances, pregnancy, the period of breastfeeding, children's age (up to 18 years - until the completion of the formation of the skeleton, except for therapy, 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), simultaneous administration with tizanidine (risk of pronounced reduction in blood pressure, drowsiness).

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation, mental illness, epilepsy, renal and/or hepatic insufficiency, congenital QT interval prolongation syndrome, heart disease (heart failure, myocardial infarction, bradycardia), electrolyte imbalance (eg, hypokalemia, hypomagnesemia), concomitant use of drugs prolonging the QT interval (including antiarrhythmic IA and III classes), simultaneous application with inhibitors of CYP 450 1A2 isoenzymes (including theophylline, methylxanthine, caffeine, duloxetine, clozapine), patients who have a history of indications for tendon disorders associated with the administration of quinolones, elderly age.

Dosing and Administration:

Inside. Tablets should be swallowed whole with a small amount of liquid after eating. When taking a tablet on an empty stomach, the active substance is absorbed more quickly.

Adults

For infections of the lower respiratory tract of mild and moderate degree - 500 mg 2 times a day, in severe cases - 750 mg 2 times. The course of treatment is 7-14 days.

For acute sinusitis, 500 mg twice a day. The course of treatment is 10 days.

With infection of the skin and soft tissues of mild and moderate degree - 500 mg 2 times a day, in severe cases - 750 mg 2 times. The course of treatment is 7-14 days.

When infections of bones and joints - mild and moderate - 500 mg 2 times a day, in severe cases - 750 mg 2 times. The course of treatment is up to 4-6 weeks.

With infections of the urinary tract - 250-500 mg 2 times a day; course of treatment - 7-14 days, with uncomplicated cystitis in women - 3 days.

With chronic prostatitis - 500 mg 2 times, the course of treatment - 28 days.

With uncomplicated gonorrhea - 250-500 mg once.

Infectious diarrhea - 500 mg 2 times, the course of treatment - 5-7 days.

With typhoid fever - 500 mg 2 times; course of treatment -10 days.

With complicated intra-abdominal infections - 500 mg.every 12 hours for 7-14 days.

With peritonitis, bacteremia and sepsis ciprofloxacin is used first in the form of intravenous infusion, then the treatment is continued 500-750 mg twice a day in the form of tablets.

In infections with immunodeficiency ciprofloxacin should be taken in combination with other antibacterial agents at a dose of 500 mg - 750 mg 2 times a day. In cases of infection against the background of secondary cellular immunodeficiency treatment is carried out throughout the neutropenia period.

For prevention and treatment of pulmonary form of anthrax - 500 g 2 times a day for 60 days.

In Pediatrics

In the treatment of complications caused by Pseudomonas aeruginosa, in children with cystic fibrosis of the lungs from 5 to 17 years, 20 mg/kg 2 times a day (maximum-dose-1.5 g). Duration of treatment is 10-14 days.

With a pulmonary form of anthrax (prevention and treatment) - 15 mg/kg. 2 times a day.

The maximum single dose is 500 mg, the daily dose is 1 g. The total duration of taking ciprofloxacin is 60 days.

Dosing in special cases

Adults

Patients with impaired renal function

With QC more than 50 ml/min dose adjustment is not required; with QC 30-50 ml/min - 0.25-0.5 g every 12 hours; with QC 5-29 ml/min - 0,25-0,5 g every 18 hours.If the patient undergoes hemodialysis or peritoneal dialysis - 0.25-0.5 g/day, but the drug should be taken after a hemodialysis session.

In Pediatrics

The dosage regimen in children with renal and hepatic insufficiency was not studied.

Side effects:

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

From the nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, nightmarish dreams, peripheral paralysis (anomaly of perception of pain), increased sweating, increased intracranial pressure, confusion, depression, hallucinations, as well as other manifestations of psychotic reactions occasionally progressing to conditions in which the patient may be harmed), migraine, fainting, cerebral artery thrombosis, agitation, disorientation, paresthesia and dysesthesia, hypesthesia, convulsions, vert yoke, impaired coordination of movements, hyperesthesia, peripheral neuropathy and polyneuropathy.

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

From the side of the cardiovascular system: tachycardia, heart rhythm disturbances, lowering of arterial pressure, prolongation of Q-T interval, ventricular arrhythmias (including "pirouette" type), vasodilation.

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

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

From the urinary system: hematuria, crystalluria (primarily with alkaline urine and low diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, albuminuria, urethral bleeding, decreased renal nitrogen function, interstitial nephritis, renal failure, serum sickness.

Allergic reactions: skin itching, urticaria, the formation of blisters accompanied by bleeding, and the appearance of small nodules that form scabs, drug fever, puncture of the face, larynx, conjunctiva, extremities, angioedema, anaphylactic shock, dyspnea, eosinophilia, increased photosensitivity, vasculitis, nodal erythema, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Other: arthralgia, arthritis, tendovaginitis, increased muscle tone, tendon ruptures (predominantly achilles), asthenia, muscle weakness, myasthenia gravis exacerbation, gait disturbance, myalgia, superinfections (candidiasis, pseudomembranous colitis), blood flushes to the face.

Overdose:

Symptoms: nausea, vomiting, confusion, mental agitation.

Treatment: the specific antidote is unknown. Gastric lavage and other emergency measures, careful monitoring of the patient's condition, ensuring 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:

Due to the decrease in the activity of microsomal oxidation in hepatocytes, it increases the concentration and lengthens T_1/2theophylline (and other xanthines, for example, caffeine), oral hypoglycemic drugs, helps to reduce the prothrombin index.

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 and other beta-lactam antibiotics - with streptococcal infections; with isoxazolylpenicillins and vancomycin - with staphylococcal infections; with metronidazole and clindamycin - with anaerobic infections.

Enhances the nephrotoxic effect of cyclosporine, there is an increase. serum creatinine, these patients need control of this indicator twice a week.

With simultaneous application increases the effect of indirect anticoagulants. Non-steroidal anti-inflammatory drugs (excluding acetylsalicylic acid) increase the risk of seizures.

Joint application with uricosuric medicines leads to a delay in excretion (up to 50%) and an increase in the plasma concentration of ciprofloxacin.

Increases the maximum concentration of tizanidine by 7 times (from 4 to 21) and the area under the pharmacokinetic curve "concentration-time" by 10 times (from 6 to 24), which increases the risk of pronounced reduction in blood pressure and drowsiness.

When used simultaneously with drugs that extend the Q-T interval (antiarrhythmic IA and III classes), the Q-T interval can be extended. With the simultaneous use of ciprofloxacin and omeprazole, there may be a slight decrease in the maximum plasma concentration in the plasma and a decrease in the area under the concentration-time curve.

The simultaneous use of probenecid and ciprofloxacin increases the concentration of ciprofloxacin in the blood plasma (probenecid slows the rate of excretion of ciprofloxacin by the kidneys). With the simultaneous use of ciprofloxacin, the renal metabolism of methotrexate may slow down, which may be accompanied by an increase in the concentration of methotrexate in the blood plasma - (the likelihood of side effects of methotrexate increases).

The simultaneous use of duloxetine and potent inhibitors of the CYP 450 1A2 isoenzyme (such as fluvoxamine) can lead to an increase in the minimum inhibitory concentration (MIC) and C_max duloxetine. Despite the lack of clinical data on the possible interaction with ciprofloxacin, it is possible to foresee the likelihood of such interaction with the simultaneous use of ciprofloxacin and duloxetine. The simultaneous use of ropinirole and ciprofloxacin, a moderate inhibitor of the isoenzyme CYP. 450 1A2, leads to an increase C_max and IPC ropinirole by 60%; and 84%, respectively. It is necessary to monitor the side effects of ropinirole during its combined use with ciprofloxacin and for a short time after completion of the combination therapy. With the simultaneous use of clozapine and ciprofloxacin at a dose of 250 mg for 7 days, an increase in serum concentrations of clozapine and n-desmethylclozapine by 29% and 31%, respectively (correction of the dosage regimen of clozapine during its simultaneous use with ciprofloxacin and for a short time after completion of combination therapy).With the simultaneous use of ciprofloxacin in a dose of 500 mg and sildenafil at a dose of 50 mg, there was an increase C_max and IPC sildenafil in 2 times (the application of this combination is possible only after the evaluation of the benefit / risk ratio).

Oral administration together with iron-containing drugs, sucralfate and antacid drugs containing magnesium, calcium and aluminum ions, leads to a decrease in ciprofloxacin absorption, so it should be prescribed 1-2 hours before or 4 hours after the administration of the above medications. Didanosine reduces the absorption of ciprofloxacin due to the formation of complexes with it. Metoclopramide accelerates absorption, which leads to a decrease in the time to reach it C_max.

Special instructions:

In order to avoid the development of crystalluria, exceeding is unacceptable; the recommended daily dose, sufficient fluid intake and maintenance of acid urine reaction are also necessary.

Patients with epilepsy, seizures in the anamnesis, vascular diseases to organic brain lesions in connection with the threat of development of adverse reactions from the central nervous system, ciprofloxacin should be prescribed only for "vital" indications.

If a severe and prolonged diarrhea occurs during or after treatment, the diagnosis of pseudomembranous colitis should be deleted, which requires immediate discontinuation of the drug and the appointment of appropriate treatment.

When pain occurs in the tendons or the first signs of tendovaginitis treatment should be discontinued (individual cases of inflammation and even rupture of tendons during treatment with fluoroquinolones are described).

During the treatment period, avoid direct exposure to sunlight and ultraviolet radiation sources.

In the treatment of severe infections, staphylococcal infections and infections caused by anaerobic bacteria, ciprofloxacin should be used in combination with appropriate antibacterial agents. Ciprofloxacin It is not a drug of choice in suspected or established pneumonia caused by Streptococcus pneumoniae. For infections suspected to be caused by Neisseria gonorrhoeae resistant to fluoroquinolones, local information on ciprofloxacin resistance should be taken into account and the sensitivity of the causative agent in laboratory tests should be confirmed.

In rare cases, after the first application, anaphylactic reactions may occur up to anaphylactic shock. In these cases, the use of ciprofloxacin should be stopped immediately and appropriate treatment should be given.

In elderly patients with tendon diseases, or previously treated with glucocorticosteroids, there may be cases of rupture of tendons (mainly Achilles tendon). Adverse reactions from the central nervous system may occur after the first use of the drug. In very rare cases, psychosis may manifest as suicidal attempts. In these cases, immediately stop taking ciprofloxacin and inform the doctor about it.

Ciprofloxacin is a moderate inhibitor of CYP 450 1A2 isoenzymes. Caution should be exercised with the simultaneous use of ciprofloxacin and drugs metabolized by these enzymes (including theophylline, methylxanthine, caffeine, duloxetine, clozapine), as an increase in the concentration of these drugs in the blood serum, due to inhibition of their metabolism.

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

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially dangerous: activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated 250 mg, 500 mg.

Packaging:

10 tablets in a blister of PVC film and aluminum foil. 1 blister with instructions for use packed in a cardboard box.

Storage conditions:

In dry, the dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011900 / 01

Date of registration:20.02.2012

Expiration Date:Unlimited

The owner of the registration certificate:Torrent Pharmaceuticals Co., Ltd.Torrent Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

TORRENT PHARMACEUTICALS, Ltd. India

Representation: & nbspTORRENT PHARMACEUTICALS LTD. TORRENT PHARMACEUTICALS LTD. India

Information update date: & nbsp28.12.2017

Illustrated instructions

Instructions

Quintor® (Quintor®)