Ofloxacin-Teva - instructions for use, dose, side effects, contraindications

pregelatinized 54.0 / 108.0 mg, hypromellose 20.0 / 40.0 mg, croscarmellose sodium 16.0 / 32.0 mg, silicon dioxide colloid 0.4 / 0.8 mg, magnesium stearate 4.0 / 8 , 0 mg, Ophadrai II white envelope 33G28707 (hypromellose-6sP 6.00 / 9.60 mg, titanium dioxide E171 3.60 / 5.76 mg, lactose monohydrate 3.30 / 5.28 mg, macrogol-3000 1.20 / 1.92 mg, triacetin 0 , 90 / 1.44 mg).

Description:

Tablets 200 mg: white round biconvex tablets, film-coated, with a risk on both sides. On one side - engraving "FXN" on the one side of the risks and "200" - on the other side of the risks. On the cross-section - the core is white or almost white.

Tablets 400 mg: white oval biconvex tablets, film-coated, with a risk on one side and engraving "FXN" and "400" on the other. On the cross-section - the core is white or almost white.

Pharmacotherapeutic group:antimicrobial agent-fluoroquinolone

ATX: & nbsp

S.01.A.E.01 Ofloxacin

J.01.M.A.01 Ofloxacin

Pharmacodynamics:

The bactericidal action of ofloxacin is associated with the inhibition of bacterial DNA gyrase, which leads to destabilization of bacterial DNA and the death of bacterial cells. The prevalence of acquired resistance of certain bacterial species to ofloxacin can vary in different geographic regions and at different times, so it is very important to have information about the structure of local resistance, especially when treating severe infections. If the structure of local resistance is such that the expediency of using a particular drug is in doubt, you should consult a microbiologist for advice.

Ofloxacin has a broad spectrum of antimicrobial action, including microorganisms resistant to other antibiotics, including strains that produce beta-lactamases.

Sensitive microorganisms: aerobic Gram-positive microorganisms - Staphylococcus aureus (methicillin-sensitive), Staphylococcus epidermidis (methicillin-sensitive), Staphylococcus saprophyticus, Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes; aerobic gram-negative microorganisms - Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis, Morganella morganii, Neisseria gonorrhoeae, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Pseudomonas aeruginosa (quickly develops stability), Serratia marcescens; anaerobic microorganisms - Clostridium perfringens; other microorganisms - Chlamydia pneumoniae, Chlamydia trachomatis, Gardnerella vaginalis, Legionella pneumophila, Mycoplasma hominis, Mycoplasma pneumoniae, Ureaplasma urealyticum.

In most cases, they are insensitive:Nocardia asteroids; anaerobic

microorganisms - Bacteroides spp., Clostridium difficile, Eubacterium spp., Fusobacterium spp., Peptococcus spp., Peptostreptococcus spp., Enterococcus spp., most Streptococcus spp.; does not apply to Treponema pallidum.

The mechanism of bacterial resistance to ofloxacin is associated with one or more mutations of target enzymes, which are generally resistant to other fluoroquinolones.

Pharmacokinetics:

Absorption after ingestion is rapid and complete (about 95%). Bioavailability is 96%. About 25% of the administered dose binds to blood plasma proteins. The maximum concentration (CmOh) ⁼ 2.6 μg / ml is achieved 1 hour after ingestion of 200 mg of the drug. Apparent volume of distribution - 100 liters. Quickly penetrates and is well distributed in many organs, tissues and fluids of the body, penetrates into cells.Therapeutically significant concentrations in excess of the plasma concentration observed in the interstitial tissue, saliva, sputum, lung tissue, myocardium, bone, mucosa and the intestinal wall, peritoneal fluid, pancreatic juice and pancreatic tissue, prostate tissue, seminal fluid, organs of the female reproductive system, skin and subcutaneous tissue; penetrates into leukocytes and alveolar macrophages. It penetrates well through the blood-brain barrier, reaching therapeutic concentrations, penetrates through the hematoplacental barrier at high concentrations, and is excreted in breast milk. 14-60% penetrates into the cerebrospinal fluid. Biotransformation in the liver undergoes about 5% of the administered dose. The main metabolites of ofloxacin are: Noxide and Ndimethylofloxacin. Half-life (T1/2) is 5.7-7 hours and does not depend on the administered dose. With multiple administrations, the cumulative effect is not expressed, plasma concentrations increase slightly. Ofloxacin is excreted mainly by the kidneys in unchanged form (80-90% of the administered dose), about 4% - with bile. The extrarenal clearance is 20%.After administration in a dose of 200 mg, the total clearance is 258 ml / min. In small quantities is excreted through the intestine. In patients with renal insufficiency T1/2 ofloxacin is increased; total and renal clearance decrease proportionally. When hemodialysis is removed 10-30% ofloxacin. With hepatic failure, excretion can be slowed down.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ofloxacin, including:

- lower respiratory tract (exacerbation of chronic bronchitis, pneumonia);

- kidney and urinary tract, including pyelonephritis, urethritis;

- genital organs and pelvic organs, including cervicitis, prostatitis;

- skin and soft tissues.

Contraindications:

Hypersensitivity to ofloxacin, other quinolones or other components of the drug; age to 18 years; pregnancy; the period of breastfeeding; deficiency of glucose-6-phosphate dehydrogenase; epilepsy, including in the anamnesis; decreased convulsive threshold, including after a stroke; with craniocerebral trauma, acute disturbance of cerebral circulation,inflammatory diseases of the central nervous system; lesions of tendons against the background of the previously used fluoroquinolones; lactose intolerance, lactase deficiency, glucose-galactose malabsorption, peripheral neuropathy.

Carefully:

Organic diseases of the brain, including atherosclerosis of the cerebral vessels, cerebral circulation disorder (in the anamnesis); predisposition to

convulsive reactions; myasthenia gravis gravis; impaired renal function (creatinine clearance (CK) less than 50 ml / min); severe violations of liver function; hepatic porphyria; diabetes; heart disease, including chronic heart failure, myocardial infarction, bradycardia, paroxysmal ventricular tachycardia of the "pirouette" type, the syndrome of congenital lengthening of the interval QT; simultaneous use of drugs that extend the interval QT, including antiarrhythmic drugs IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal agents, imidazole derivatives, some antihistamines (astemizole, terfenadine, ebastine); simultaneous reception of drugs for non-inhaling general anesthesia from the barbiturate group, hypotensive drugs; psychoses and other mental disorders, including in the anamnesis; electrolyte imbalance (eg, hypokalemia, hypomagnesemia); elderly age.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Inside. The dose of ofloxacin should be selected depending on the type and severity of the infection, as well as the general condition of the patient and the function of the liver and kidneys. Tablets are taken whole, washed down with water, before or during meals.

200-800 mg per day in 2 divided doses at regular intervals. A dose of up to 400 mg per day can be taken in one session, preferably in the morning.

Patients with impaired renal function (KK less than 50 ml / min) correction of the dosage regimen is required depending on the QC value.

Concentration of creatinine in plasma (mg / dL)

Dose and multiplicity of administration

20-50 ml / min

1,5-5,0

100-200 mg every 24 hours

Less than 20 mL / min or hemodialysis and peritoneal dialysis

Not less than 5,0

100 mg every 24 hours or

200 mg every 48 hours

After hemodialysis or peritoneal dialysis, no additional doses are required.

Creatinine clearance can be calculated using the formulas below.

For men: [body weight (kg) x (140 - age (full years))] / [72 x concentration of creatinine in plasma (mg / dl)]

For women: 0.85 x SC men

In patients with severe hepatic impairment the excretion of ofloxacin can be reduced. In such cases, the daily dose of ofloxacin should not exceed 400 mg.

In elderly patients correction of the dose is not required.

The duration of treatment is determined by the sensitivity of the pathogen, the severity of the infectious disease and the response to therapy. Treatment should continue for at least 3 more days after complete normalization of body temperature or after confirmation of bacterial agent eradication. Usually the duration of treatment is 7-10 days, except for the treatment of gonorrhea, and should not exceed 2 months.

Side effects:

The incidence of adverse reactions is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including individual reports.

From the digestive system: often - nausea, vomiting, diarrhea, abdominal pain; infrequent - loss of appetite, constipation, flatulence; rarely - increased activity of "liver" transaminases,Hyperbilirubinemia, cholestatic jaundice, colitis (including hemorrhagic), dryness of the oral mucosa; very rarely - hepatitis, pseudomembranous colitis.

From the nervous system: infrequently - headache, dizziness, insomnia, anxiety, nervousness; rarely - "nightmarish" dreams, intense dreams, psychotic reactions, anxiety, arousal, phobias, depression, confusion, hallucinations, suicidal attempts, drowsiness, tremor, convulsions, numbness and paresthesia of limbs, motion uncertainty, increased intracranial pressure; very rarely - extrapyramidal disorders, sensory or sensory-motor neuropathy, peripheral neuropathy.

From the sense organs: infrequently - conjunctivitis; rarely - violation

color perception, diplopia, violation of taste, smell, balance; very rarely - noise in the ears, hearing impairment, including deafness in exceptional cases.

From the musculoskeletal system: very rarely - tendinitis, myalgia, muscle weakness in patients with myasthenia gravis, arthralgia, tendosinovitis, rupture of tendons, muscular and joint rhabdomyolysis symptoms, pain in the extremities.

From the cardiovascular system: infrequent - a feeling of heartbeat; rarely - heart failure, hypotension; very rarely - ventricular arrhythmia, including paroxysmal ventricular tachycardia of the "pirouette" type, lengthening of the interval QT, hypertension.

From the respiratory system: infrequently - dry cough, rhinopharyngitis; rarely shortness of breath, bronchospasm; unknown frequency - allergic pneumonitis.

From the skin and subcutaneous tissues: very rarely - petechiae, bullous hemorrhagic dermatitis, papular rash with a cortex, indicating the defeat of blood vessels (vasculitis).

On the part of the blood system and hemopoiesis: very rarely - leukopenia, including agranulocytosis, anemia (including hemolytic and aplastic), thrombocytopenia, pancytopenia, exacerbation of porphyria.

From the urinary system: very rarely - acute interstitial nephritis, renal dysfunction, hypercreatininaemia, increased urea concentration, dysuria, urinary retention, acute renal failure.

Allergic reactions: infrequently - skin rash, itching, hives; very rarely - multiforme exudative erythema (including Stevens-Johnson syndrome),toxic epidermal necrolysis (Lyell's syndrome), photosensitivity, allergic pneumonitis, allergic nephritis, eosinophilia, fever, angioedema, bronchospasm; hypotension, hypertension, anaphylactic shock, itching of the external genitalia in women.

Other: very rarely - intestinal dysbacteriosis, superinfection, chest pain, hyper- or hypoglycemia (in patients with diabetes mellitus when taking antidiabetic drugs), epistaxis, thirst, weight loss, vaginitis, vaginal discharge, fatigue, asthenia, general weakness .

Overdose:

Symptoms: dizziness, confusion, inhibition, disorientation, convulsions, drowsiness, vomiting, symptoms of irritation of the mucous membranes.

Treatment: gastric lavage, forced diuresis, symptomatic therapy; for the reduction of neurological disorders (convulsive syndrome) use diazepam.

Interaction:

With the simultaneous use of ofloxacin with sucralfate, antacid preparations and other preparations containing metal ions (aluminum, magnesium, zinc or iron), the absorption of ofloxacin decreases. Ofloxacin should be taken for

2 hours before or 2 hours after taking these drugs.

It is possible to increase the effectiveness of anticoagulant medications of indirect action (coumarin derivatives), including warfarin, with simultaneous reception with ofloxacin. It is necessary to control the blood coagulation system.

When used simultaneously with non-steroidal anti-inflammatory drugs (NSAIDs), including fenbufen, as well as derivatives of nitroimidazole and methylxanthines increases the risk of neurotoxic effects, including a decrease in the threshold of convulsive activity.

With the simultaneous use of ofloxacin and theophylline, the clearance of theophylline is reduced by 25% and increases T1 / 2 theofellin.

With simultaneous application with hypoglycemic drugs, it is possible to develop both hypo- and hyperglycemia. When used with glibenclamide increases the concentration of glibenclamide in the blood plasma and causes a state of hypoglycemia, in connection with which it is necessary to monitor the concentration of glucose in the blood plasma.

When used simultaneously with cyclosporin, there is an increase in T1 / 2 and C_max cyclosporine in the blood plasma.

Probenecid, cimetidine, furosemide, methotrexate with simultaneous application with ofloxacin reduce the tubular secretion of ofloxacin, which leads to an increase in the concentration of ofloxacin in the blood plasma.

With simultaneous application with drugs that extend the interval QT, including antiarrhythmic drugs IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal agents, imidazole derivatives, some antihistamines (astemizole, terfenadine, ebastine) it is possible to extend the interval QT.

With simultaneous use with drugs for non-induction general anesthesia from the barbiturate group, hypotensive drugs, a sharp and significant reduction in blood pressure is possible, so in this case, monitoring of the cardiovascular system parameters is required.

When used simultaneously with glucocorticosteroids (GCS), the risk of rupture of tendons increases, especially in elderly patients.

When used with drugs that alkalinize urine (carbonic anhydrase inhibitors, citrates, sodium hydrogen carbonate), the risk of crystalluria and nephrotoxic effects increases.

Ofloxacin is not compatible with ethanol.

Special instructions:

Ofloxacin should not be prescribed as a first-choice drug for the treatment of community-acquired pneumonia caused by Streptococcus pneumoniae andMycoplasma spp., and acute tonsillitis caused by Streptococcus pyogenes.

Perhaps the development of superinfection due to the growth of insensitive to ofloxacin microorganisms, especially Enterococcus spp. and Candida spp. In this case, it is necessary to conduct tests for sensitivity to antibiotics and adjust the treatment regimen.

If duringloxacin occurs during or after treatment with severe and prolonged diarrhea, it is necessary to exclude the possibility of developing pseudomembranous colitis, the confirmation of which requires withdrawal of the drug.

Ofloxacin inhibits growth Mycobacterium tuberculosis, which can lead to false-negative results of bacteriological tests in patients with tuberculosis.

Although ofloxacin rarely causes photosensitivity, during treatment with this drug, it is recommended to avoid prolonged exposure to direct sunlight or artificial ultraviolet radiation (UVI) (solarium, UFI treatment). For the prevention of excessive salt content in urine and subsequent crystalluria during the treatment it is recommended to conduct adequate hydration.

Rarely developing tendonitis can lead to rupture of tendons (mainly Achilles tendon). The risk of rupture of the tendons increases with the use of fluoroquinolones on the background of SCS. Tendinitis is more common in older patients. In case of signs of tendonitis, it is necessary immediately to stop treatment, to immobilize the Achilles tendon and consult an orthopedist.

When using ofloxacin, women should not use hygiene tampons due to the increased risk of thrush development.

Patients who are predisposed to developing paroxysmal ventricular tachycardia such as pirouettes or taking drugs that extend the interval QT, a Also for the detection of violations of ventricular conduction before the treatment of ofloxacin it is necessary to conduct an electrocardiogram study. (ECG) and regularly monitor ECG values during treatment.

If the duration of treatment is more than 2 weeks, it is necessary to check the blood formula and blood biochemical parameters.

During the period of treatment can not be consumed ethanol.

When used simultaneously with indirect anticoagulants, it is necessary to monitor the blood coagulation system.

With simultaneous use with hypoglycemic drugs, both hypo- and hyperglycemia are possible, and therefore it is necessary to monitor the concentration of glucose in the blood plasma.

In patients with impaired renal function (KK less than 50 ml / min), a serious violation of the liver requires dose adjustment of ofloxacin (see section "Method of administration and dose").

In case of liver disease, it is necessary to determine the indicators of the functional state of the liver before the treatment of ofloxacin, and also to monitor these parameters during treatment.

In patients with impaired liver or kidney function, it is necessary to monitor the concentration of ofloxacin in the plasma. In severe renal and hepatic insufficiency, the risk of toxic effects increases (a decreasing dose adjustment is required).

On the background of the treatment with ofloxacin, myasthenia flow may worsen gravisand an increase in porphyria attacks.

In patients who received fluoroquinolones, including ofloxacin, reported the development of sensory and sensory-motor neuropathy, which can have a rapid onset.When neuropathy symptoms appear, ofloxacin should be discontinued, which helps minimize the possible risk of developing irreversible conditions.

The drug Ofloxacin-Teva should be used with caution in patients predisposed to developing seizures (patients with central nervous system (CNS) history), including cerebral circulation, patients taking NSAIDs, and other drugs that reduce the convulsive threshold of the brain, such as theophylline) (see the section "Interaction with other medicinal products").

In case of adverse reactions from the central nervous system and allergic reactions, a drug change is necessary.

Impact on the results of laboratory tests: in the treatment of ofloxacin, false positive results can be obtained when determining opiates and porphyrins in urine.

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

During treatment ofloxacin, caution should be exercised when driving vehicles and controlling mechanisms due to the possibility of developing side effects from the nervous system (dizziness, drowsiness) that affect the ability to concentrate attention and the speed of psychomotor reactions.

Form release / dosage:

The film-coated tablets are 200 mg and 400 mg.

Packaging:

For 10 tablets in aluminum foil blisters / PVC / PVDC;

1.2 or 5 blisters with instructions for use in a cardboard bundle.

Storage conditions:Store at a temperature of no higher than 25 ° C in a dark place.

Keep out of the reach of children.

Shelf life:

3 of the year.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001231

Date of registration:17.11.2011

Date of cancellation:2016-11-17

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

TEVA Pharmaceutical Works Private, Ltd. Co. Hungary

Representation: & nbspTeva Teva Israel

Information update date: & nbsp17.11.2011

Illustrated instructions

Instructions

Ofloxacin-Teva (Ofloxacin-Teva)