Tarivid

Microbiology: Tarivid (ofloxacin) is one of the fluorinated quinolones. It is an orally administered broad-spectrum antibacterial drug, active against most gram-negative bacteria, many gram-positive bacteria and some anaerobes.
The susceptible gram-negative bacteria include Citrobacter, Enterobacter, Klebsiella, Proteus, Salmonella and Shigella spp, Y. enterocolitica, E. coli, H. influenzae, N. gonorrhoeae, Providencia, Serratia and Pseudomonas spp, V. cholerae, L. pneumophila and C. jejuni. Against P. aeruginosa, it is as potent as gentamicin and several times more potent than cefotaxime.
The susceptible gram-positive bacteria include S. aureus, S. pneumoniae, S. faecalis and L. monocytogenes. Some anaerobic organisms, including B. melaninogenicus, B. fragilis and C. welchii, are moderately susceptible. Ofloxacin is also active against C. trachomatis and M. pneumoniae.
Like other quinolones, ofloxacin is bactericidal through inhibition of the A subunits of the enzyme DNA gyrase which controls supercoiling of DNA in bacteria. The antibacterial activity of ofloxacin is not influenced by the bacterial resistance to non-quinolone antibacterial drugs, but it is markedly reduced by reduction of pH or the presence of urine.
Pharmacokinetics: Oral administration of a single 300-mg dose of ofloxacin produces a peak serum concentration of about 3 mcg/mL within 2 hrs. A dosage of 300 mg twice daily for up to 14 days produces a peak serum level ranging from 3-6 mcg/mL on the last day. Food only delays absorption, while antacids may markedly reduce absorption. Compared to norfloxacin and ciprofloxacin at the same dose, ofloxacin is more rapidly absorbed and produces a higher serum level and 4 times higher AUC (AUC represents the amount of drug absorbed).
Ofloxacin is widely distributed to most tissues and body fluids. The volume of distribution is >1 L/kg and the tissue concentrations achieved are at least as high as the serum level for most tissues.
After single doses of 100-600 mg, 70-98% of ofloxacin is excreted unchanged in the urine within 48 hrs and the urinary concentration remains above the MIC₉₀ for most bacterial species at 48 hrs after administration. The elimination half-life after doses of 200 mg or more is about 6 hrs or more (up to 7.5 hrs). In patients with renal impairment, peak serum concentrations are delayed; the elimination half-life and AUC are substantially increased depending on the degree of renal impairment and thus dosage adjustments may be necessary.

Tablet: Treatment of serious infections caused by ofloxacin-susceptible organisms, eg upper and lower urinary tract infections; gonococcal and nongonococcal urethritis and cervicitis; lower respiratory tract infections, except those caused by Streptococcus; skin and soft tissue infections; obstetric and gynaecological infections.
Lower Respiratory Tract: Acute bacterial exacerbation of chronic bronchitis or community-acquired pneumonia due to Haemophilus influenzae or Streptococcus pneumoniae.
Skin and Skin Structures: Uncomplicated skin and skin structure infections due to Staphylococcus aureus, Streptococcus pyogenes or Proteus mirabilis.
Sexually-Transmitted Diseases: Acute, uncomplicated urethral and cervical gonorrhoea due to Neisseria gonorrhoeae. Nongonococcal urethritis and cervicitis due to Chlamydia trachomatis. Mixed infections of the urethra and cervix due to Chlamydia trachomatis and Neisseria gonorrhoeae.
Urinary Tract: Uncomplicated cystitis due to Citrobacter diversus, Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis or Pseudomonas aeruginosa. Complicated urinary tract infections due to Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Citrobacter diversus or Pseudomonas aeruginosa.
Prostate: Prostatitis due to Escherichia coli.

The recommended oral dosage of Tarivid is as follows (before or after meals): Urinary Tract Infections: 200-400 mg daily in 1-2 divided doses for 1-10 days. Severe or Complicated Infections: Up to 600 mg daily and/or for up to 20 days.
Lower Respiratory Tract Infections: 200-600 mg daily in 1-3 divided doses for 3-10 days. Severe or Complicated Infections: Up to 800 mg daily and/or for up to 20 days.
Skin and Soft Tissue Infections: 400 mg daily for 7 days.
Gynaecological Infections: 400 mg daily for 7 days.
Uncomplicated Gonococcal Urethritis: A single dose of 200-400 mg.
Nongonococcal Urethritis: 400 mg daily for 9 days.


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Patients with Impaired Renal Function: Dosage should be adjusted for patients with a creatinine clearance ≤50 mL/min. After a normal initial dose, dosage should be adjusted as follows: Creatinine clearance 20-50 mL/min: Maintenance dose is the usual recommended dose every 24 hrs; creatinine clearance <20 mL/min: Administer ½ the usual recommended unit dose every 24 hrs.
Patients with Cirrhosis: The excretion of ofloxacin may be reduced in patients with severe liver function disorders (eg, cirrhosis with or without ascites). A maximum dose of 400 mg of ofloxacin/day should therefore not be exceeded.
When the patient's condition has improved, it is possible to switch from IV administration to oral medication in the same dosage. Until further experience has been obtained, the duration of treatment should not exceed 2 months.

Hypersensitivity to ofloxacin and other quinolone derivatives. Tarivid is not indicated in children or adolescents in the growth phase and in pregnant or breastfeeding women, because its safety in such patients has not yet been sufficiently documented and, judging from animal experiments, the risk of damage to the cartilage of joints in the growing organisms cannot be altogether excluded.

Tarivid is not recommended for the treatment of streptococcal infections and other infections caused by organisms susceptible to other long established antibiotics.
Use with caution in patients with reduced renal function: Reduce the dose according to the severity of renal dysfunction. Elderly patients may also require a dosage reduction since they may have reduced creatinine clearance.
If shock or shock-like symptoms occur, discontinue Tarivid and give appropriate treatments.
If hypersensitivity reactions develop during therapy, discontinue usage.

Beta-lactamase production should have no effect on ofloxacin activity. Appropriate culture and susceptibility tests should be performed before treatment in order to isolate and identify organisms causing the infection, and to determine their susceptibility to ofloxacin. Therapy with ofloxacin may be initiated before results of these tests are known; once results become available, appropriate therapy should be continued.
As with other drugs in this class, some strains of Pseudomonas aeruginosa may develop resistance fairly rapidly during treatment with ofloxacin. Culture and susceptibility testing performed periodically during therapy will provide information not only on the therapeutic effect of the antimicrobial agent but also on the possible emergence of bacterial resistance. If anaerobic organisms are suspected of contributing to the infection, appropriate therapy for anaerobic pathogens should be administered.
Note: Although treatment of infections due to this organism in this infection demonstrated a clinically acceptable overall outcome, efficacy was demonstrated in fewer than 10 infections.
Ofloxacin has not been shown to be effective in the treatment of syphilis. Antimicrobial agents used in high doses for short periods of time to treat gonorrhoea may mask or delay the symptoms of incubating syphilis. All patients with gonorrhoea should have a serologic test for syphilis at the time of diagnosis. Patients treated with ofloxacin should have a follow-up serologic test for syphilis after 3 months.
As with other quinolones, disturbances of blood glucose, including symptomatic hyper- and hypoglycaemia, have been reported, usually in diabetic patients receiving concomitant treatment with an oral hypoglycaemic agents or with insulin. In these patients, careful monitoring of blood glucose is recommended. If a hypoglycaemic reaction occurs in patient being treated with ofloxacin, discontinue ofloxacin immediately and consult a physician.
Patients who are being treated with Tarivid IV should not expose themselves unnecessarily to strong sunlight and should avoid ultraviolet rays (sunray lamp, solarium).
Effects on the Ability to Drive or Operate Machinery: Even if used in accordance with the directions, ofloxacin may affect alertness and reaction time to such an extent that ability to drive, cross the road safe or operate machinery may be impaired. Concurrent use of alcohol increases this risk.

Tarivid is not indicated in pregnant or breastfeeding women.

Tablet: The incidence of ofloxacin-related adverse reactions was 3.3% among nearly 16,000 patients in clinical trials (ranged from 2.5-8.5% in various studies).
The most frequent adverse effects were gastrointestinal symptoms (2.64%), mainly nausea, vomiting, epigastric discomfort, abdominal pain, diarrhoea and anorexia. These were followed by CNS effects (0.89%: Headache, dizziness and sleep disturbances) and dermatological or hypersensitivity reactions (0.53%: Skin eruption, pruritus, rash, eczema and itching). The incidence or severity of these various adverse effects did not appear to be dose-related and serious reactions were rare.
Minor changes in mean laboratory values were not considered clinically significant and were usually attributable to the disease process, but some cases of eosinophilia were considered possibly drug-related. Shock and shock-like symptoms (discomfort, perspiration, dyspnoea and hypotension) may occasionally occur.

Gastrointestinal absorption of ofloxacin is markedly reduced by concurrent administration of antacids containing aluminium or magnesium hydroxide. Therefore, Tarivid should not be taken at the same time, but 1-2 hrs before or after the antacid.
Unlike ciprofloxacin, pefloxacin and enoxacin, ofloxacin has no influence on the plasma concentrations of theophylline.

Store below 30°C.

Quinolones

J01MA01 - ofloxacin ; Belongs to the class of fluoroquinolones. Used in the systemic treatment of infections.

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