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

Active substance: ciprofloxacin lactate monohydrate in terms of ciprofloxacin - 200 mg; Excipients - sodium chloride 900.0 mg, disodium edetate 2.0 mg, lactic acid 0.005 ml, water for injection q.s up to 100 ml.

Description:

Transparent solution from colorless to light yellow color.

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

Low toxicity for macroorganism cells is explained by the absence of DNA-gyrase in them. While receiving ciprofloxacin occurs parallel to others making resistance. Antibiotics, does not belong to the group of gyrase inhibitors, which makes it highly effective against bacteria which are resistant, such as 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:

After intravenous infusion, 200 or 400 mg of ciprofloxacin, the maximum concentration (C_max) is 2.1 and 4.6 μg / ml, respectively, the time to reach the maximum concentration (TC_max) - 60 min. The connection with plasma proteins is 20-40%. The volume of distribution is 2-3.5 l / kg

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 / min / 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 decreases, 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 is from 5 to 17 years. Prevention and treatment of pulmonary form of anthrax (infection with Bacillus anthracis).

Contraindications:

Hypersensitivity to ciprofloxacin and other drugs of the quinolone group, as well as to auxiliary substances, pregnancy, lactation period, children's age (up to 18 years - until the completion of the skeleton formation, except for therapy, complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs from 5 up 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 disorder, mental illness, epilepsy, renal and / or hepatic insufficiency, congenital QT interval prolongation, heart disease (heart failure, myocardial infarction, bradycardia), electrolyte imbalance (eg, hypokalemia, hypomagnesemia ), simultaneous administration of drugs that extend the QT interval (including antiarrhythmic IA and III classes), simultaneous use with inhibitors of CYP 450 1A2 isoenzymes (including number of 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:

Intravenously infuzionalno. The duration of the infusion is 30 minutes at a dose of 200 mg and 60 minutes at a dose of 400 mg. Infusion solutions ready for use can be mixed with 0.9% sodium chloride solution, Ringer's and Ringer's lactate solution, 5% and

10% dextrose solution, 10% fructose solution, and also a solution containing 5% dextrose solution with 0.225-0.45% sodium chloride solution.

Adults

In infections of the lower respiratory tract - 200-400 mg 2 times a day, the course is 7-14 days. In severe pneumonia, including streptococcal, and infectious complications of cystic fibrosis - 400 mg 3 times a day, the course is 7-14 days.

In case of infections of the ENT organs - 200-400 mg 2 times a day, the course is 10 days.

With infections of the urinary tract: acute uncomplicated - 100 mg 2 times a day, the course - 7-14 days; cystitis in women (before menopause) - once 100 mg; Complicated - 200 mg twice a day, the course is 7-14 days.

With chronic bacterial prostatitis - 400 mg 2 times a day, the course is 28 days.

With uncomplicated gonorrhea - 100 mg once, with extragenital - 100 mg 2 times a day.

At typhoid fever - 400 mg 2 times a day, the course is 10 days.

With infectious diarrhea - 200 mg 2 times, the course of treatment - 5-7 days.

In light and medium-sized infections of the skin and soft tissues - 400 mg 2 times a day, with heavy 400 mg 3 times a day, the course of 7-14 days.

Particularly severe infections (infections of bones and joints, septicemia, peritonitis), especially caused Pseudomonas, Staphylococcus - 400 mg 3 times a day.

Pulmonary form of anthrax (treatment and prevention) - 400 mg twice a day, 60 days.

For the prevention of infections during surgical interventions - 200-400 mg for 0.5-1 h before surgery; When the duration of the operation is more than 4 hours, re-enter in the same dose. In other infections (depending on the severity of the flow) - 200-400 mg 2 times a day. Older patients are prescribed lower doses, depending on the severity of the infection and the CC score.

In Pediatrics

In the treatment of complications caused by Pseudomonas aeruginosa in children with cystic fibrosis of the lungs from 5 to 17 years - 10 mg / kg 3 times a day (maximum dose of 1200 mg). Duration of treatment is 10-14 days.

With a pulmonary form of anthrax (prevention and treatment) - 10 mg / kg 2 times a day. The maximum single dose is 400 mg, the daily dose is 800 mg. The total duration of taking ciprofloxacin is 60 days.

Dosing in special cases

Patients with impaired renal function

With SC 31-60 ml / min / 1.73 m2 or serum creatinine concentration of 1.4 to 1.9 mg / 100 ml), the maximum daily dose is 800 mg. With QC below 30 ml / min / 1.73 m² or serum creatinine concentration above 2 mg / 100 ml and during hemodialysis the maximum daily dose is 400 mg. With hemodialysis ciprofloxacin injected after a hemodialysis session.

Patients on hemodialysis or peritoneal dialysis

With peritoneal dialysis, the infusion solution is added to dialysate (intraperitoneally) at a dose of 50 mg per liter of dialysate 4 times a day (every 6 hours).

The average course of treatment: 1 day - with acute uncomplicated gonorrhea and cystitis; up to 7 days - with infections of the kidneys, urinary tract and abdominal cavity; no more than 2 months - with osteomyelitis and 7-14 days - with all other infections. With streptococcal infections, due to the danger of late complications, treatment should last at least 10 days. In patients with immunodeficiency treatment is carried out throughout the neutropenia period.

Treatment should be carried out at least 3 days after the normalization of body temperature or the disappearance of clinical symptoms.

After intravenous administration of ciprofloxacin, treatment can be continued with oral administration of the drug.

Side effects:

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

From the nervous system: dizziness, headache, fatigue, insomnia, tremor, anxiety, 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 can do harm to themselves), migraine, syncope, cerebral artery thrombosis, agitation, disorientation, paresthesia and dysesthesia, hypoesthesia, convulsions, vertigo, 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, hearing loss.

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

On the part of the hematopoiesis system: Leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, haemolytic anemia, neutropenia, agranulocytosis, pancytopenia, inhibition of bone marrow hematopoiesis.

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

From the urinary system: Hematuria, crystalluria (especially at low alkaline urine and diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, albuminuria, urethral bleeding, hematuria, decreased azotvydelitelnoy kidney, interstitial nephritis.

On the part of the respiratory system: violation of breathing (including bronchospasm).

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

Local Reactions: swelling, pain, burning, redness at the injection site, phlebitis.

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. It is necessary to carefully monitor the patient's condition, carry out symptomatic therapy, and 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:

Due to a decrease in the activity of microsomal oxidation in hepatocytes, it increases the concentration and lengthens T1 theophylline (and other xanthines, for example, caffeine), oral hypoglycemic drugs, and 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 by 10 times (from 6 to 24), which increases the risk of pronounced decrease in blood pressure and drowsiness.

The infusion solution is pharmaceutically incompatible with all infusion solutions and preparations that are physico-chemically unstable under acidic conditions (the pH of the infusion solution of ciprofloxacin is 3.5-4.6). Do not mix the IV solution with solutions having a pH of more than 7.

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, renal metabolism of methotrexate may be slowed, which may be accompanied by an increase in the concentration of methotrexate in the blood plasma (the probability 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 Stach 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 CYP450 1A2, leads to an increase C_max and MIC of 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% is possible,respectively (correction of the dosage regimen of clozapine during its simultaneous use with ciprofloxacin and a short time after completion of the combination therapy is necessary). The simultaneous use of lidocaine and ciprofloxacin leads to a decrease in clearance of lidocaine by 22% with its lactose administration (possibly increasing side effects of lidocaine).

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 MIC of sildenafil in 2 times (application of this combination is possible only after the evaluation of the benefit / risk ratio).

Special instructions:

With simultaneous intravenous administration of ciprofloxacin and drugs for general anesthesia from the barbituric acid derivative group, continuous monitoring of cardiac activity (heart rate, heart rate, arterial pressure, ECG monitoring) is necessary.

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 of being resistant to fluoroquinolones, Neisseria gonorrhoeas strains should take into account local information about ciprofloxacin resistance and confirm the sensitivity of the pathogen in laboratory tests. 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, you should immediately stop taking ciprofloxacin and tell your 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, methylxangin, caffeine, duloxetine, clozain), since an increase in the concentration of these drugs in the blood serum, due to inhibition of their metabolism by ciprofloxacin, can cause specific undesirable reactions. Local reaction (inflammatory reaction) of the skin at the site of administration of the drug: edema, occurs more often if the infusion time is 30 minutes or less. The reaction quickly passes after the end of nifusion and is not a contraindication for the subsequent administration of the drug, unless its course becomes complicated. In vitro in laboratory tests ciprofloxacin suppresses the growth of Mycobacterium spp., which can lead to false-negative results in the diagnosis of this pathogen in patients taking ciprofloxacin. It is necessary to take into account the content of sodium chloride in the solution of ciprofloxacin in the treatment of patients in whom sodium intake is limited (heart failure, kidney failure, nephrotic syndrome).

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

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

Form release / dosage:

Solution for infusions 2 mg / ml.

Packaging:

To 100 ml in a polyethylene bottle (from low density polyethylene) with a detachable cap, packed in a plastic bag. The bottle in the package together with the instruction for use is placed in a cardboard box

Storage conditions:

In the dark place at a temperature of no higher than 30 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:2.5 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011896 / 01

Date of registration:01.12.2011

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®)