Ofloxin^® (Solution) Instructions for Use

Marketing Authorization Holder

Zentiva, a.s. (Czech Republic)

ATC Code

J01MA01 (Ofloxacin)

Active Substance

Ofloxacin (Rec.INN registered by WHO)

Dosage Form

Ofloxin®

Infusion solution 200 mg/100 ml: vial 1 pc.

Dosage Form, Packaging, and Composition

Infusion solution transparent, with a light yellowish-greenish tint.

Excipients: sodium chloride, concentrated hydrochloric acid, disodium edetate dihydrate, water for injections.

100 ml – vials of colorless glass (1) – cardboard packs.

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic Group

Antimicrobial agent – fluoroquinolone

Pharmacological Action

Antimicrobial agent of the fluoroquinolone group with a broad spectrum of action. The bactericidal action of ofloxacin is associated with the blockade of the DNA gyrase enzyme in bacterial cells.

It is highly active against most gram-negative bacteria: Escherichia coli, Salmonella spp., Shigella spp., Proteus spp., Morganella morganii, Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Serratia spp., Citrobacter spp., Yersinia spp., Providencia spp., Haemophilus influenzae, Neisseria gonorrhoeae, Neisseria meningitidis, Mycoplasma spp., Legionella pneumophila, Acinetobacter spp., and also Chlamydia spp.

It is active against some gram-positive microorganisms (including Staphylococcus spp., Streptococcus spp., especially beta-hemolytic streptococci).

Enterococcus faecalis, Streptococcus pneumoniae, Pseudomonas spp. are moderately sensitive to ofloxacin.

Anaerobic bacteria (except Bacteroides urealyticus) are not sensitive to ofloxacin.

It is resistant to the action of beta-lactamases.

Pharmacokinetics

Protein binding is 25%. Ofloxacin is widely distributed in body tissues and fluids (organs of the urinary system, genital organs, prostate gland, lungs, ENT organs, gallbladder, bones, skin).

It is excreted in the urine unchanged (about 80% within 24 hours). A small part of the active substance (about 4%) is excreted in the feces. T_1/2 is 6 hours.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to ofloxacin, including: diseases of the lower respiratory tract, ear, throat, nose, skin, soft tissues, bones, joints, infectious and inflammatory diseases of the abdominal organs (except for bacterial enteritis) and pelvis, kidney and urinary tract infections, prostatitis, gonorrhea.

ICD codes

Dosage Regimen

Determine the dosage regimen individually based on infection severity, pathogen susceptibility, and patient renal function.

Administer the solution by slow intravenous infusion only. Do not administer by rapid IV injection or bolus.

For most infections in adults with normal renal function, administer 200 mg twice daily or 400 mg once daily.

For severe infections or in patients with excess body weight, increase the daily dose to a maximum of 600 mg.

Adjust the dosage in patients with renal impairment based on creatinine clearance (CrCl). For CrCl 10-50 mL/min, administer the standard dose every 24 hours. For CrCl less than 10 mL/min, administer half the standard dose every 24 hours.

Infuse each 200 mg dose in 100 mL solution over at least 30 minutes. Infuse each 400 mg dose in 200 mL solution over at least 60 minutes.

Complete the full course of therapy as prescribed, even if symptoms improve. The usual duration of treatment is 7 to 10 days.

Adverse Reactions

From the digestive system: nausea, vomiting, diarrhea, abdominal pain and cramps, loss of appetite, dry mouth, flatulence, gastrointestinal function disorders, constipation; rarely – liver function disorders, liver necrosis, jaundice, hepatitis, intestinal perforation, pseudomembranous colitis, gastrointestinal bleeding, disorders of the oral mucosa, heartburn, increased activity of liver enzymes, including GGT and LDH, increased serum bilirubin level.

From the nervous system: insomnia, dizziness, fatigue, drowsiness, nervousness; rarely – convulsions, anxiety, cognitive changes, depression, abnormal dreams, euphoria, hallucinations, paresthesia, syncope, tremor, confusion, nystagmus, suicidal thoughts or attempts, disorientation, psychotic reactions, paranoia, phobia, agitation, aggressiveness, emotional lability, peripheral neuropathy, ataxia, coordination disorders, exacerbation of extrapyramidal disorders, speech disorder.

Allergic reactions: skin rash, itching; rarely – angioedema, urticaria, vasculitis, allergic pneumonitis, anaphylactic shock, erythema multiforme, Stevens-Johnson syndrome, erythema nodosum, exfoliative dermatitis, toxic epidermal necrolysis, conjunctivitis.

From the reproductive system: itching in the area of the external genitalia in women, vaginitis, vaginal discharge; rarely – burning, irritation, pain and rash in the genital area in women, dysmenorrhea, menorrhagia, metrorrhagia, vaginal candidiasis.

From the cardiovascular system: rarely – cardiac arrest, edema, arterial hypertension, arterial hypotension, palpitation, vasodilation, cerebral thrombosis, pulmonary edema, tachycardia.

From the urinary system: rarely – dysuria, frequent urination, urinary retention, anuria, polyuria, kidney stone formation, renal failure, nephritis, hematuria, albuminuria, candiduria.

From the musculoskeletal system: rarely – arthralgia, myalgia, tendinitis, muscle weakness, exacerbation of myasthenia.

From the metabolism: rarely – thirst, weight loss, hyper- or hypoglycemia (especially in patients with diabetes mellitus receiving insulin or oral hypoglycemic agents), acidosis, increase in serum triglycerides, cholesterol, potassium.

From the respiratory system: rarely – cough, nasal discharge, respiratory arrest, dyspnea, bronchospasm, stridor.

From the sensory organs: rarely – hearing impairment, tinnitus, diplopia, nystagmus, impaired visual acuity, taste and smell disorders, photophobia.

Dermatological reactions: rarely – photosensitivity, hyperpigmentation, vesiculobullous eruptions.

From the hematopoietic system: rarely – anemia, bleeding, pancytopenia, agranulocytosis, leukopenia, reversible suppression of bone marrow hematopoiesis, thrombocytopenia, thrombocytopenic purpura, petechiae, ecchymoses, increased prothrombin time.

Other: chest pain, pharyngitis, increased body temperature, body aches; rarely – asthenia, chills, general malaise, nosebleed, increased sweating.

Contraindications

Hypersensitivity to ofloxacin or other quinolone derivatives; tendon damage during previous treatment with fluoroquinolones; pregnancy, breastfeeding period; children and adolescents under 18 years of age.

Use in Pregnancy and Lactation

Use is contraindicated during pregnancy and breastfeeding.

Use in Hepatic Impairment

Should be used with caution in patients with impaired liver function.

Use in Renal Impairment

Should be used with caution in patients with impaired renal function.

Pediatric Use

Use is contraindicated in children and adolescents under 18 years of age.

Geriatric Use

Should be used with caution in elderly patients, taking into account the state of renal function.

Special Precautions

During treatment, blood glucose levels should be monitored. During long-term therapy, renal function, liver function, and peripheral blood picture should be periodically monitored.

When using ofloxacin, sufficient hydration of the body should be ensured, and the patient should not be exposed to UV radiation.

In experimental studies, mutagenic potential was not identified. Long-term studies to determine the carcinogenicity of ofloxacin have not been conducted.

In studies on young animals of several species, Ofloxacin caused arthropathy and osteochondrosis.

The safety and efficacy of the drug in children and adolescents under 18 years of age have not been established.

Effect on the ability to drive vehicles and mechanisms

During the use of the drug, patients should exercise caution when driving vehicles and mechanisms, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use of ofloxacin and NSAIDs, the risk of developing a stimulating effect on the central nervous system and convulsions increases.

With simultaneous use with theophylline, an increase in its plasma concentration (including at steady state) and an increase in T_1/2 are possible. This increases the risk of developing adverse reactions associated with the action of theophylline.

With simultaneous use of ofloxacin with beta-lactam antibiotics, aminoglycosides and metronidazole, an additive interaction was noted.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.