Ofloxacin Wellfarm pills 200mg, 10pcs

Composition

Per tablet:

Active ingredient: ofloxacin-200 mg.

Excipients: microcrystalline cellulose, potato starch, povidone (low molecular weight medical polyvinylpyrrolidone 12600±2700, plasdon K-17), croscarmellose sodium (primellose), magnesium stearate.

Shell: opadray white 03F180011 (hypromellose, titanium dioxide, macrogol).

Pharmacological action

Pharmacotherapeutic group: antimicrobial agent-fluoroquinolone

ATX code: J01 MA 01

Pharmacological properties

Pharmacodynamics

Ofloxacin is a synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones, which has a bactericidal effect. The main mechanism of action of quinolones is specific inhibition of bacterial DNA gyrase. DNA gyrase is essential for bacterial DNA replication, transcription, repair, and recombination. Its inhibition leads to unwinding and destabilization of bacterial DNA and, consequently, to the death of the microbial cell.

It is highly active against most gram-negative and gram-positive microorganisms.

Fluoroquinolones have a concentration-dependent bactericidal activity and a moderate post-antibacterial effect. The ratio of AUC to minimum inhibitory concentration (MPC) or the ratio of maximum concentration to MPC is a predictive factor for successful clinical treatment.

Sensitive microorganisms

Non-permanently sensitive microorganisms (possibly due to acquired resistance): Citrobacter freundii, Escherichia coli, Klebsiella oxytoca, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia spp., Staphylococcus spp. (coagulase-negative strains), Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis, Campylobacter jejuni, Enterococcus faecalis, Streptococcus pneumoniae. Resistant microorganisms

Acinetobacter baumannii, Bacteroides spp., Clostridium difficile, Enterococci (including Enterococcus faecium), Listeria monocytogenes, Staphylococcus aureus (methicillin-resistant strains), Nocardia spp.

Resistance

Resistance to ofloxacin develops as a result of a gradual process of mutations in the genes encoding both type II topoisomerases: DNA gyrase and topoisomerase IV. Other mechanisms of resistance, such as the mechanism of influence on the permeability of the external structures of the microbial cell (a mechanism characteristic of Pseudomonas aeruginosa) and the mechanism of efflux (active removal of an antimicrobial agent from the microbial cell), can also affect the sensitivity of microorganisms to ofloxacin.

MPC boundary values

Borderline MPC values (mg / L) of ofloxacin approved by the European Committee for the Determination of Antibiotic Sensitivity (EUCAST).

Pharmacokinetics

After oral use, ofloxacin is rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability is almost 100%. The maximum concentration of ofloxacin in blood plasma after taking a single dose of 200 mg is 2.5-3 mcg / ml and is reached after 1 h. Binding to plasma proteins is 25%. The volume of distribution is approximately 120 liters. Less than 5% of ofloxacin undergoes biotransformation.

It is mainly excreted by the kidneys (80-90% of the dose is unchanged). There are two main metabolites found in the urine: : N-desmethylofloxacin and ofloxacin N-oxide. About 4% of ofloxacin is excreted in the bile as glucuronides. The half-life is 6-7 hours. Concentrations of ofloxacin in the urine and in infected urinary tracts exceed the concentration of ofloxacin in the blood serum by 5-100 times.

Special patient groups Elderly patients

In elderly patients, there is an increase in the elimination half-life, but the maximum concentration does not change.

Kidney failure

In renal insufficiency, the elimination half-life increases; total and renal clearance decrease in proportion to the decrease in creatinine clearance.

Indications

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to ofloxacin:

– pyelonephritis;

– prostatitis, epididymitis, orchitis;

– pelvic infections;

– cystitis.

As an alternative to other antimicrobial drugs, ofloxacin can be used to treat the following infectious and inflammatory diseases: :

– uncomplicated urinary tract

infections; – skin and soft tissue

infections; – bone and joint infections;

– acute sinusitis;

– exacerbation of chronic bronchitis, community-acquired pneumonia;

– prevention of infections caused by microorganisms sensitive to ofloxacin in patients with a significant decrease in immune status (for example, with neutropenia).

When using the drug, you should take into account the official national recommendations

for the proper use of antibacterial drugs, as well as the sensitivity of pathogens in a particular country.

Use during pregnancy and lactation

Pregnancy

Ofloxacin should not be used during pregnancy (see section “Contraindications”).

Breast-feeding period

Since ofloxacin is excreted in breast milk, because of the risk to the baby, women who are breast-feeding should not take ofloxacin, or if it is necessary to use it, stop breastfeeding.

Contraindications

– hypersensitivity to ofloxacin, to other hinolona or auxiliary substances of the drug;

– epilepsy;

– psevdoparalitichesky myasthenia gravis (myasthenia gravis) (see “Side effects”, the “Special instructions”);

– lesions of the tendons when receiving fluoroquinolones in history;

– children and adolescence under 18 (it is impossible to completely eliminate the risk of cartilaginous lesions of bone growth in children);

– pregnancy (it is impossible to completely eliminate the risk of destruction of the cartilage of the growth zones of the fetus);

– the period of breastfeeding (it is impossible to completely eliminate the risk of destruction of the cartilage of the growth zones of the child).

Caution

– patients predisposed to seizures (patients with prior Central nervous system (CNS), such as severe atherosclerosis of cerebral vessels, cerebral circulatory disorders, a history of organic lesions of the Central nervous system, brain injuries in history; in patients receiving both drugs that reduce the threshold of convulsive activity of the brain, such as fenbufen or other nonsteroidal anti-inflammatory drugs, theophylline);

– in patients with latent or manifestating deficiency of glucose-6-phosphate dehydrogenase (increased risk of hemolytic reactions in the treatment finalname);

– in patients with impaired renal function (requires mandatory monitoring of renal function, and the correction mode, see section “Method of use and dose”);

the patients with liver failure (monitoring of liver function tests);

– patients with porphyria (risk of exacerbation of porphyria);

– in patients with risk factors for QT interval prolongation: patients of advanced age; with uncorrected electrolyte disorders (hypokalemia, hypomagnesemia); the syndrome of congenital QT prolongation; cardiac (heart failure, myocardial infarction, bradycardia); the simultaneous use of drugs that can prolong the QT (antiarrhythmics of classes IA and III, tricyclic antidepressants, macrolides, antipsychotics);

– in patients with diabetes receiving oral hypoglycemic agent (e. g., glibenclamide) or insulin (risk of hypoglycemia);

– patients with severe adverse reactions to other chinolone such as severe neurological reactions (increased risk of similar adveA daily dose of up to 400 mg can be administered in 1 dose, preferably in the morning. A daily dose of more than 400 mg should be divided into 2 doses at equal intervals.

Tablets should be swallowed whole, washed down with a sufficient amount of water. The drug can be taken both before and during meals. Concomitant use of the drug with antacids should be avoided.

Special patient groups

Elderly patients

The age of patients does not require adjustment of the dose of ofloxacin. However, when using the drug in elderly patients, special attention should be paid to renal function, since if it decreases, an appropriate dosage adjustment may be required.

Patients with impaired liver function

If liver function is impaired, it is not recommended to exceed the daily dose of ofloxacin 400 mg.

Patients with impaired renal function

In patients with impaired renal function, the following dosage regimen is recommended, depending on creatinine clearance:

* with the exception of indications where the adjusted dose of ofloxacin is 100 mg

. * * It is recommended to monitor serum concentrations of ofloxacin in patients with severe renal impairment or in patients undergoing dialysis.

In cases where it is not possible to determine creatinine clearance (CC), it can be calculated from the concentration of serum creatinine using the Cockcroft formula for adults:

for men:

CC (ml / min) = or

Body weight (kg) x (140 – age in years) 72 x serum creatinine (mg/dl)

CC (ml / min) =

for women:

Body weight (kg) x (140 – age in years) 0.814 x serum creatinine (mmol / L)

CC (ml / min) = 0.85 x the indicator in men.

Duration of treatment

The duration of treatment depends on the severity of the disease. As with any antimicrobial treatment, treatment with ofloxacin should be continued for a minimum of 48-72 hours after normalization of body temperature or if there is evidence of eradication of the pathogen.

Overdose

Symptoms

The most important symptoms of overdose are symptoms from the central nervous system (such as dizziness, confusion, impaired consciousness, convulsions), prolongation of the QT interval, as well as reactions from the gastrointestinal tract (such as nausea and erosion of the gastrointestinal mucosa).

Treatment

In case of overdose, gastric lavage and symptomatic therapy are recommended. Antacids can be used to protect the gastric mucosa. It is necessary to monitor the ECG, as possible prolongation of the QT interval. Fractions of ofloxacin can be removed from the body by hemodialysis. There is no specific antidote.

Description

Round biconvex tablets, film-coated in white or almost white color. On a cross-section – the core is white or white with a yellowish tinge of color.

Special instructions

Kidney failure

Due to the fact that ofloxacin is mainly excreted by the kidneys, in patients with renal insufficiency, dose adjustment of ofloxacin is necessary (see the sections “With caution”, “Method of use and doses”).

Prevention of photosensitization

During treatment with ofloxacin, due to the risk of photosensitization, exposure to bright sunlight and ultraviolet rays should be avoided.

Secondary infection

As with other antimicrobial drugs, when taking ofloxacin, especially for a long time, it is possible to develop a secondary infection associated with the growth of microorganisms resistant to the drug, which should be re-evaluated to exclude and confirm the patient’s condition. If a secondary infection develops during therapy, the necessary measures should be taken to treat it.

Peripheral neuropathy

Patients treated with fluoroquinolones, including ofloxacin, have been reported to develop sensory and sensorimotor neuropathy, which may have a rapid onset. If patients develop symptoms of neuropathy, treatment with ofloxacin should be discontinued, which helps to minimize the possible risk of developing irreversible conditions (see the section “With caution”).

Patients with glucose-6-phosphate dehydrogenase deficiency

Patients with a diagnosed glucose-6-phosphate dehydrogenase deficiency may be predisposed to hemolytic reactions when treated with quinolones. Therefore, caution should be exercised when using ofloxacin in such patients (see section “With caution”).

Pseudomembranous colitis caused by Clostridium difficile

The appearance of diarrhea, especially in severe form, persistent and / or mixed with blood, during or after treatment with ofloxacin may be a manifestation of pseudomembranous colitis. If pseudomembranous colitis is suspected, treatment with ofloxacin should be discontinued immediately, and appropriate specific antibacterial therapy (oral vancomycin, oral teicoplanin, or oral metronidazole) should be prescribed immediately. When this clinical situation occurs, drugs that suppress intestinal motility are contraindicated.

Patients predisposed to developing seizures

As with other quinolones, ofloxacin should be used with caution in patients predisposed to seizures (patients with a history of CNS damage, in patients receiving concomitant medications that reduce the threshold for convulsive brain activity (theophylline, fenbufen [and other similar nonsteroidal anti-inflammatory drugs]), (see the section “With caution”). If seizures develop, treatment with ofloxacin should be discontinued.

Tendinitis

Tendinitis, which rarely occurs when quinolones are used, can sometimes lead to tendon rupture, including the Achilles tendon, especially in elderly patients and in patients taking concomitant glucocorticosteroids. This undesirable effect may develop within 48 hours of starting treatment and may be bilateral. In case of signs of tendinitis (inflammation of the tendon), it is recommended to immediately stop treatment with ofloxacin. Appropriate treatment (such as immobilization) of the damaged tendon may be required.

Prolongation of the QT interval

Some caution should be exercised when taking fluoroquinolones, including ofloxacin, in patients with known risk factors for QT prolongation, such as::

old age;

– uncorrected electrolyte imbalance (e. g. hypokalemia, hypomagnesemia);

– congenital prolongation of the QT interval;

– cardiovascular disease (heart failure, myocardial infarction, bradycardia);

– concomitant use of drugs that lengthen the QT interval (classes IA and III antiarrhythmic drugs, tricyclic antidepressants, macrolides, antipsychotics).

Pseudoparalytic myasthenia gravis

Fluoroquinolones, including ofloxacin, are characterized by neuromuscular blocking activity and may increase muscle weakness in patients with pseudoparalytic myasthenia gravis. In the post-marketing period, serious adverse reactions were observed, including pulmonary insufficiency that required mechanical ventilation, and death, which were associated with the use of fluoroquinolones in patients with pseudoparalytic myasthenia gravis. The use of ofloxacin in a patient with an established diagnosis of pseudoparalytic myasthenia gravis is not recommended (see the section “Side effects”).

Severe skin reactions

Severe bullous reactions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported with ofloxacin. Patients should be advised that if skin reactions and/or mucosal lesions develop, they should immediately consult a doctor before continuing treatment with ofloxacin.

Hypersensitivity and allergic reactions

Hypersensitivity reactions and allergic reactions (anaphylactic shock and anaphylactoid reactions that can progress to a life-threatening state) have been reported with the use of fluoroquinolones. In these cases, the use of ofloxacin should be discontinued and appropriate treatment should be initiated.

Psychotic reactions

Psychotic reactions, including suicidal thoughts/attempts, have been reported in patients taking fluoroquinolones, including ofloxacin. Ofloxacin should be used with caution in patients with psychotic disorders (including those with a history of psychotic disorders).

“With caution”). Psychiatric adverse reactions may occur even after a single dose. If such reactions occur, treatment with ofloxacin should be discontinued immediately and appropriate treatment should be given immediately, and if possible, an antibiotic other than fluoroquinolones should be switched to therapy.

Liver function disorders

Ofloxacin should be used with caution in patients with impaired liver function, as liver damage may occur.section “With caution”). Cases of fulminant hepatitis leading to liver failure (including fatal cases) have been reported with the use of fluoroquinolones. Patients should be advised to stop treatment and consult a doctor if they experience symptoms and signs of liver disease, such as anorexia, jaundice, dark urine, itchy skin, or abdominal pain.

Dysglycemia (hypo – and hyperglycemia)

When using fluoroquinolones, including ofloxacin, the development of both hyperglycemia and hypoglycemia, as well as severe hypoglycemia, up to the development of hypoglycemic coma, has been reported, especially in elderly patients, patients with diabetes mellitus taking oral hypoglycemic drugs or insulin (signs of hypoglycemia: confusion, dizziness, “wolfish” appetite, headache, nervousness, palpitation or rapid pulse, pallor skin, perspiration, trembling, weakness). The plasma glucose concentration of these patients should be carefully monitored. In case of adverse reactions, such as a decrease in glucose concentration, treatment with ofloxacin should be stopped immediately and appropriate treatment should be prescribed immediately, and therapy with an antibiotic other than fluoroquinolones should be switched, if possible.

Patients taking vitamin K antagonists

Due to the possible increase in prothrombin time/international normalized ratio and/or the development of bleeding in patients taking both ofloxacin and vitamin K antagonists (for example, warfarin), careful monitoring of blood clotting parameters is recommended.

Risk of developing resistance

The prevalence of acquired resistance may vary geographically and over time for individual species. Therefore, local resistance information is required. Microbiological diagnostics should be performed to isolate the pathogen and determine its sensitivity, especially in cases of severe infections or lack of response to treatment.

Infections caused by Escherichia coli

Resistance to fluoroquinolones of Escherichia coli, the most common causative agent of urinary tract infections, varies in different geographical areas. Doctors are advised to take into account the local resistance of Escherichia coli to fluoroquinolones.

Infections caused by Neisseria gonorrhoeae

Due to the increased resistance of Neisseria gonorrhoeae, ofloxacin should not be used as an empirical treatment for suspected gonococcal urinary tract infection. Tests for the sensitivity of the pathogen to ofloxacin should be performed in order to ensure targeted therapy.

Methicillin-resistant Staphylococcus aureus

There is a high probability that methicillin-resistant Staphylococcus aureus will be resistant to fluoroquinolones, including ofloxacin. Therefore, ofloxacin is not recommended for the treatment of established or suspected infections caused by methicillin – resistant Staphylococcus aureus, if laboratory tests have not confirmed the sensitivity of this microorganism to ofloxacin.

Bone and joint infections

In cases of bone and joint infections, the combined use of ofloxacin with other antibacterial agents should be considered.

Impact on laboratory parameters and diagnostic tests

Ofloxacin can inhibit the growth of Mycobacterium tuberculosis, leading to false negative results in the bacteriological diagnosis of tuberculosis.

When determining opiates and porphyrins in the urine during treatment with ofloxacin, a false positive result is possible. It may be necessary to confirm positive results using more specific methods.

Other things

During the treatment period, it is not recommended to use ethanol.

Influence on the ability to drive vehicles and mechanisms

Some adverse reactions, such as dizziness/vertigo, drowsiness, and visual disturbances, may reduce psychomotor response and concentration, and therefore increase the risk in situations where these abilities are particularly important (for example, when driving a car or using other mechanisms).

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C. Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Ofloxacin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets