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

Excipients: core: lactose monohydrate 95.2 mg, corn starch 47.6 mg, povidone 25 12.0 mg, crospovidone 20.0 mg poloxamer 0.2 mg magnesium stearate 8.0 mg, talc 4, 0 mg;

film sheath: hypromellose 2910/5 - 9.42 mg, macrogol 6000 - 0.53 mg, talc - 0.7 mg, titanium dioxide - 2.35 mg.

Description:

Round biconvex tablets covered with a shell, white or almost white, with a half-and-half risk on one side and an engraving "200" on the other. On the fracture: white or almost white.

Pharmacotherapeutic group:antimicrobial agent-fluoroquinolone

ATX: & nbsp

S.01.A.E.01 Ofloxacin

J.01.M.A.01 Ofloxacin

Pharmacodynamics:

A broad-spectrum antimicrobial agent from the group of fluoroquinolones acts on the bacterial DNA enzyme that ensures replication,transcription, repair and recombination of DNA and, thus, maintaining the stability of DNA bacteria (the destabilization of DNA chains leads to their death).

Has a bactericidal effect.

It is active against microorganisms producing beta-lactamase and fast-growing atypical mycobacteria.

Sensitive:

Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoae, Neisseria meningitis, Escherichia coli, Citrobacter, Klebsiella, Enterobacter, Hafnia, Proteus (indole-positive and indole-negative), Salmonella, Shigella, Yersinia enterocolica, Campylobacter jejuni, Aeromonas, Plesiomonas, Vibrio cholerae, Vibrio parahemolyticus, Hemophilus influenzae, Chlamydie, Legionella.

Different sensitivity to the drug has: Enterococci, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Serratia marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, Mycobacterium fortuitum.

In most cases, they are insensitive: Ureaplasma urealyticum, Nocardia asteroides, anaeroby (Bacteroides spp., Peptococcus, Peptostreptococcus, Eubacterium spp., Fusobacterium spp., Clostridium difficile). He acts on Treponema pallidum.

Pharmacokinetics:

Absorption after ingestion is rapid and complete (95%). Bioavailability is over 96%, the connection with plasma proteins is 25%, the maximum concentration (C_mOh) after taking in a dose 200 mg is on the average 2,6 mg / ml and is reached within one hour (TCmOh)- Apparent volume of distribution - 120 liters. Well penetrates through

the blood-brain barrier, the placental barrier, is secreted with the mother's milk.

Metabolized in the liver (about 5%) with formation Noxide ofloxacin and desmethylofloxacin.The half-life is 4.5-7 h (regardless of the dose). It is excreted by the kidneys - 75-90% (unchanged), about 4% - with bile.

After repeated administration, serum concentrations increase slightly (the accumulation range after taking the drug twice a day: 1.5).

Excretion of ofloxacin can be reduced in patients with severe liver damage (for example, with cirrhosis of the liver with ascites).

In patients with renal failure, the half-life (T1 / 2) is longer, with renal clearance decreasing depending on the creatinine clearance (CK).

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to off-laxacin:

■infections of the lower respiratory tract (with the exception of cases pneumococcal or mycoplasmal infection);

■ infection of the ear, throat, nose (with the exception of acute tonsillitis,

caused by βhemolytic streptococcus);

■ infection of the lower and upper urinary tract (gonorrhea);

■ infections of the pelvic organs;

■ infection of bones and joints;

■ infections of the skin and soft tissues.

Contraindications:

hypersensitivity to ofloxacin,other quinolones or components of the preparation;

■ deficiency of glucose-6-phosphate dehydrogenase;

■ epilepsy (including in the anamnesis), reduction of the convulsive threshold (incl. after craniocerebral trauma, stroke or inflammatory processes in the central nervous system);

the defeat of the tendons during the previous treatment with quinolones;

age to 18 years;

■ pregnancy, lactation.

deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

Carefully:

in patients with cerebral artery atherosclerosis, cerebral circulatory disorders (in the anamnesis), psychotic reactions (in the anamnesis), myasthenia gravis (in the anamnesis), chronic renal / hepatic insufficiency, organic lesions of the central nervous system, in patients with risk factors for lengthening the interval QT on ECG: elderly age, uncorrected electrolyte imbalance (eg, hypokalemia, hypomagnesemia), congenital elongated interval syndrome QT, heart disease (eg, heart failure, myocardial infarction, bradycardia), simultaneous use of drugs that cause lengthening of the interval QT (for example, antiarrhythmic drugs of class IA and III, tricyclic antidepressants, macrolides, antipsychotics, antifungals, imidazole derivatives, some antihistamines, including astemizole, terfenadine, ebastine), for general anesthesia from the barbiturate group, antihypertensive drugs); hepatic porphyria, diabetes mellitus, deficiency of glucose-6-phosphate dehydrogenase.

Pregnancy and lactation:

Pregnancy

Based on a limited amount of data in humans, the use of fluoroquinolones in the first trimester of pregnancy was not associated with an increased risk of major malformations or other unwanted effects on the outcome of pregnancy. In animal studies, articular cartilage damage was detected in immature animals, but there were no teratogenic effects. therefore ofloxacin should not be used during pregnancy.

Breast-feeding

Ofloxacin in small amounts is excreted in human milk. Due to possible arthropathy and other serious toxic effects in infants who are breastfeeding, breastfeeding should be discontinued during ofloxacin treatment.

Dosing and Administration:

Tablets Ofloxacin Zentiva should be taken orally, with plenty of liquid. They can be taken on an empty stomach or together with food. It is necessary to avoid simultaneous reception with antacids (preparations containing aluminum, calcium, iron or zinc).

The dose of ofloxacin and the duration of treatment depend on the severity and type of infection, the general condition of the patient and the function of the kidneys.

The average daily intake for adults is from 200 mg to 800 mg. The average duration of treatment is 5-10 days. Ofloxacin should not last more than 2 months.

A dose of up to 400 mg per day can be given in 1 reception, preferably in the morning. Doses over 400 mg per day should be divided into 2 divided doses with an equal time interval.

In severe infections or in the treatment of patients with overweight, the daily dose can be increased to 800 mg.

With infection of the lower respiratory tract, the drug is prescribed at a dose of 400 mg per day, increasing the dose if necessary to 400 mg twice a day.

When infections of the upper parts of the urinary tract drug prescribed in a dose of 200-400 mg per day, increasing the dose if necessary to 400 mg 2 times a day.

When infections of the lower parts of the urinary tract drug prescribed in a dose of 200-400 mg per day for 3-5 days.

With uncomplicated gonorrheal urethritis and cervicitis, 400 mg once is prescribed. With non-nasal urethritis and cervicitis, the drug is prescribed 400 mg per day.

With infections of the skin and soft tissues, the daily dose of the drug is 400 mg twice a day.

Correction of dose in patients with renal insufficiency

For patients with impaired renal function, the following doses are recommended:

Creatinine clearance (ml / min)	Dosing units (mg)	amount receptions	Intervals (h)
50-20	100-200	1	24
<20 *	100	1	24
or hemodialysis	or
or peritoneal	200	1	48
dialysis

Serum concentrations of ofloxacin should be monitored in patients with severe renal disease and in dialysis patients.

If creatinine clearance is not possible, it should be calculated from the serum creatinine level using formula Cockcroft for adults.

Men:

body weight (kg) х (140 - age (years))

KK (ml / min) = ------------------------------------------- ---------------------------------

72 x serum creatinine concentration (mg / dL)

body weight (kg) х (140 - age (years))

KK (ml / min) = ------------------------------------------- ---------------------------------

0.814 x serum creatinine concentration (μmol / L)

Women: KK (ml / min) = 0.85 x (the above value)

In patients with hepatic insufficiency it is not recommended to exceed the maximum daily dose of 400 mg.

In elderly patients with normal renal function, dose adjustment is not required. However, special attention should be paid to monitoring kidney function and ECG (risk of lengthening the interval QT), selecting the appropriate dose.

Side effects:

The frequency of adverse reactions was determined according to the following gradation (classification of the World Health Organization):

- very frequent - more than 1/10,

- frequent - from more than 1/100 to less than 1/10,

- infrequent - from more than 1/1000 to less than 1/100,

- rare - from more than 1/10000 to less than 1/1000,

- very rare - from less than 1/10000, including individual messages.

Infectious and parasitic diseases: infrequent - a fungal infection, the development of a secondary infection caused by drug-resistant microorganisms and fungi.

Disturbances from the blood system and lymphatic system: very rare - anemia, hemolytic anemia, leukopenia, eosinophilia, thrombocytopenia, agranulocytosis, pancytopenia, bone marrow aplasia.

Immune system disorders: rare - anaphylactic reaction, anaphylactoid reaction, angioedema; very rare - anaphylactic shock, anaphylactoid shock.

Disorders from the metabolism and nutrition: rare - anorexia; very rare - hypoglycemia in patients with diabetes, receiving hypoglycemic drugs.

Disorders of the psyche: infrequent - agitation, sleep disturbance, insomnia; rare - psychotic disorder (hallucinations), anxiety, confusion, "nightmarish" dreams, depression; very rare - psychotic disorder and depression with self-destructive behavior, including suicidal thoughts and suicide attempts.

Impaired nervous system: infrequent - headache, dizziness; rare - drowsiness, paresthesia, dysgeusia, smell disorder; very rare - peripheral sensory neuropathy, peripheral sensory-motor neuropathy, seizures, extrapyramidal symptoms or other disorders of muscle coordination. Disorders from the side of the organ of vision: infrequent - a burning sensation in the eyes; rare - impaired vision.

Hearing impairments and labyrinthine disturbances: infrequent - vertigo; very rare - ringing or noise in the ears, hearing loss.

Heart Disease: rare - tachycardia; very rare - ventricular arrhythmias, ventricular pirouette tachycardia (noted predominantly in patients with risk factors for lengthening the interval QT), interval lengthening QT on the ECG. Vascular disorders: rare - arterial hypotension.

Disturbances from the respiratory system, chest and mediastinal organs: infrequent - cough, nasopharyngitis; rare - shortness of breath, bronchospasm; very rare - allergic pneumonitis, severe shortness of breath.

Disorders from the gastrointestinal tract: infrequent - abdominal pain, diarrhea, nausea, vomiting; rare - enterocolitis (in some cases, hemorrhagic); very rare - pseudomembranous colitis.

Disorders from the liver and bile ducts: very rare - cholestatic jaundice, hepatitis (can be severe).

Impact on laboratory and instrumental research results: rare - increased activity of "hepatic" transaminases (aspartate aminotransferase (ACT), alanine aminotransferase (ALT), lactate dehydrogenase (LDH), gamma-glutamyltranspeptidase (GGT) and / or alkaline phosphatase (AF)) and / or bilirubin concentrations, an increase in creatinine in the blood plasma.

Disturbances from the skin and subcutaneous tissues: infrequent - rash, itching; rare - hives, "hot flashes" of heat, hyperhidrosis,pustular rash; very rare - erythema multiforme, toxic epidermal necrolysis, photosensitivity reaction, vascular purpura, vasculitis (which can lead in some cases to skin necrosis), Stevens-Johnson syndrome; acute generalized exanthematous pustulosis; persistent drug rash.

Disturbances from the musculoskeletal and connective tissue: rare - tendonitis; very rare - arthralgia, myalgia, tendon rupture (Achilles tendon, as with the use of other fluoroquinolones, this side effect can be observed within 48 hours after the start of treatment and can be bilateral), rhabdomyolysis and / or myopathy, muscle weakness (which may be particularly important significance in patients with severe myasthenia gravis), muscle ruptures.

Disorders from the kidneys and urinary tract: very rare - acute renal failure, acute interstitial nephritis.

Congenital, hereditary and genetic disorders: very rare - attacks of porphyria in patients with porphyria.

Overdose:

Symptoms from the central nervous system (CNS): dizziness, confusion, disorientation, convulsions, drowsiness.

Symptoms from the gastrointestinal tract (GI tract): nausea, vomiting, erosion on the mucous membranes.

Treatment: gastric lavage, administration of activated carbon and other adsorbents for the first 30 minutes, symptomatic therapy, forced diuresis and adequate hydration. When hemodialysis is removed 10-30 % of the preparation. It is necessary to conduct ECG monitoring due to possible lengthening of the interval QT. There is no specific antidote.

Interaction:

Antacids, sucralphate, metal cations.

Food products, antacids containing aluminum (sucralfate, maalox, etc.), calcium, magnesium, zinc or iron salts, reduce the absorption of ofloxacin, forming insoluble complexes. Ofloxacin should be taken about 2 hours before or 2 hours after taking antacids.

Theophylline, fenbufen or similar non-steroidal anti-inflammatory drugs

In clinical studies, there was no evidence of pharmacokinetic interactions of ofloxacin with theophylline. Nevertheless, a marked decrease in the convulsive threshold of the brain can be observed with the simultaneous use of quinolones with theophylline, non-steroidal anti-inflammatory drugs or other means that reduce the convulsive threshold.

Drugs that cause lengthening of the interval QT

Ofloxacin, like other fluoroquinolones, should be used with caution in patients receiving drugs that cause an ECG to lengthen the interval QT (for example, antiarrhythmic drugs of class IA and III, tricyclic antidepressants, macrolides, antipsychotics)

Indirect anticoagulants (coumarin derivatives, including warfarin)

The parameters of the blood coagulation system (prothrombin time (PV) and the international normalized ratio (INR)) should be monitored in patients receiving concomitantly ofloxacin and antagonists of vitamin K, in connection with the possible intensification of the effect of these drugs.

Glibenclamide

Ofloxacin can cause a slight increase in serum glibenclamide concentration when it is used simultaneously, so for patients receiving concomitantly ofloxacin and glibenclamide, it is recommended to carry out a thorough control of the glucose content in the blood.

Cimetidine, furosemide, methotrexate and drugs that block tubular secretion, increase the concentration of ofloxacin in the blood plasma.

Special instructions:

Ofloxacin is not a first-choice drug for the treatment of pneumonia caused by pneumococcus or mycoplasma, or for the treatment of acute tonsillitis caused by β-hemolytic streptococcus.

Allergic reactions

Hypersensitivity and allergic reactions were recorded with the use of fluoroquinolones after the first administration. Anaphylactic and anaphylactoid reactions can progress to a state of life-threatening shock, even after the first application. In these cases, ofloxacin treatment should be discontinued and appropriate treatment initiated.

Diseases associated with Clostridium difficile

Diarrhea, especially severe, persistent and / or with an admixture of blood, during or after treatment of ofloxacin, may be a symptom of pseudomembranous colitis. If pseudomembranous colitis is suspected, ofloxacin should be discontinued immediately. It should immediately begin appropriate supportive and specific antibiotic therapy. Drugs that inhibit peristalsis are contraindicated in this clinical situation.

Patients who are prone to convulsions

Like other quinolones, ofloxacin Use with extreme caution in patients predisposed to seizures.

It can be patients with pre-existing lesions of the central nervous system, concomitant treatment with non-steroidal anti-inflammatory drugs or drugs that reduce the convulsive threshold, such as theophylline. In the case of convulsive seizures, ofloxacin should be discontinued. Tendonitis

Tendinitis, which is rarely seen with quinolones, can sometimes lead to rupture of the tendon, in particular the Achilles tendon. Older patients are more likely to develop tendonitis. The risk of rupture of the tendon may increase with the simultaneous use of corticosteroids. If you suspect a tendonitis, ofloxacin should be stopped immediately.

It is necessary to begin appropriate treatment (immobilization) of tendon damage.

Patients with renal involvement

Because the ofloxacin is mainly excreted through the kidneys, the dose of ofloxacin should be adjusted in patients with kidney damage.

Patients with psychotic disorders in the history

Psychotic reactions were reported in patients who received fluoroquinolones. In some cases, these reactions progressed to suicidal thoughts or self-destructive behavior, including suicide attempts, sometimes after taking a single dose. If the patient develops these reactions, ofloxacin should be discontinued, and appropriate interventions should be initiated. Ofloxacin should be used with caution in patients with a history of psychotic disorders or in patients with mental illness. Patients with impaired hepatic function

Ofloxacin should be used with caution in patients with impaired liver function. When fluoroquinolones were used, cases of fulminant hepatitis, leading to acute hepatic insufficiency (including fatal cases) were noted. Patients should be advised to stop treatment and contact their doctor when developing symptoms of liver damage such as anorexia, jaundice, dark urine, pruritus or tenderness of the abdomen.

Malignant myasthenia gravis (myasthenia gravis)

Ofloxacin should be used with caution in patients with a history of malignant myasthenia gravis.

Prevention of photosensitization

Due to the risk of photosensitivity, exposure to intense sunlight and ultraviolet radiation should be avoided during ofloxacin treatment. Secondary infection

As with other antibiotics, the use of ofloxacin, especially prolonged, may lead to the development of resistance to ofloxacin in the causative agent. It is important to re-determine sensitivity to antibiotics. The elongation of the OT interval

Very rare cases of lengthening the interval QT have been reported in patients taking fluoroquinolones.

Caution should be exercised when using ofloxacin, in patients with known risk factors for lengthening the interval QT:

■ elderly age

uncorrected electrolyte imbalance (eg, hypokalemia, hypomagnesemia)

congenital elongated interval syndrome QT

■ heart disease (eg, heart failure, myocardial infarction,

bradycardia)

■ simultaneous use of drugs that cause lengthening of the interval

QT (for example, antiarrhythmic drugs of class IA and III, tricyclic antidepressants, macrolides, antipsychotics).

Hypoglycaemia

As with all quinolones, cases of hypoglycemia have been reported, usually in patients with diabetes mellitus receiving concomitant treatment with an oral hypoglycemic drug (eg, glibenclamide) or insulin. In such patients, it is recommended that blood glucose be monitored closely.

Peripheral Neuropathy

Sensory or sensorimotor peripheral neuropathy was noted in patients receiving fluoroquinolones, including ofloxacin, with the disorder can occur in a short time. If the patient has symptoms of neuropathy, ofloxacin should be discontinued.

Patients with deficiency of glucose-6-phosphate dehydrogenase

Patients with a latent or diagnosed deficiency of glucose-6-phosphate dehydrogenase may be predisposed to hemolytic reactions if they receive quinolones. Ofloxacin should be used with caution in such patients. Patients with rare hereditary diseases

Patients with lactase deficiency, lactose intolerance, glucose-galactose malabsorption, should not take this drug.

Impact on laboratory performance

Determination of the content of opiates or porphyrins in urine can lead to false-positive results in the treatment with ofloxacin. It is necessary to confirm the positive results of screening for the presence of opiates or porphyrins using more specific methods.

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

Undesirable reactions (dizziness, drowsiness, visual impairment), recorded against the background of ofloxacin therapy, may impair the ability

patient to concentration and response, and can lead to risk in situations where these qualities are of particular importance (for example, driving a car or working with mechanisms). When the above-described undesirable phenomena appear, one should refrain from performing these activities.

Form release / dosage:

Tablets, film-coated, 200 mg.

Packaging:For 7 or 10 tablets in a blister of PVC / A1. 1 blister (10 tablets) or 2 blisters (7 or 10 tablets each), along with instructions for use in a cardboard box.

Storage conditions:

At a temperature of 10 ° C to 25 ° C in a dry place.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015708 / 01

Date of registration:09.02.2009

The owner of the registration certificate:Zentiva c.s.Zentiva c.s. Czech Republic

Manufacturer: & nbsp

ZENTIVA, k.s. Czech Republic

Representation: & nbspZENTIVA PHARMA, LLCZENTIVA PHARMA, LLC

Information update date: & nbsp29.01.2014

Illustrated instructions

Instructions

Ofloxacin Zentiva (Ofloxacin Zentiva)