Ofloxacin Suspension

Ofloxacin is an antibiotic that belongs to the class of medications called quinolones. It is used to treat certain infections caused by bacteria. It is most commonly used to treat infections of the lung, urinary tract, and skin. It can also be used to treat certain prostate infections and sexually transmitted infections. Ofloxacin works by killing some types of bacteria that can cause these infections.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of ofloxacin tablets and other antibacterial drugs, ofloxacin tablets should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria.
Ofloxacin tablets are indicated for the treatment of adults with mild to moderate infections (unless otherwise indicated) caused by susceptible strains of the designated microorganisms in the infections listed below
ACUTE BACTERIAL EXACERBATIONS OF CHRONIC BRONCHITIS:
due to Haemophilus influenzae orStreptococcus pneumoniae.
COMMUNITY-ACQUIRED PNEUMONIA:
due to Haemophilus influenzae or Streptococcus pneumoniae.
UNCOMPLICATED SKIN AND SKIN STRUCTURE INFECTIONS:
due to methicillin-susceptible Staphylococcus aureus, Streptococcus pyogenes, or Proteus mirabilis.
ACUTE, UNCOMPLICATED URETHRAL AND CERVICAL GONORRHEA:
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.
ACUTE PELVIC INFLAMMATORY DISEASE (INCLUDING SEVERE INFECTION):
due to Chlamydia trachomatisand/or Neisseria gonorrhoeae.

PHARMACODYNAMIC PROPERTIES OF OFLOXACIN

Ofloxacin is a quinolone antimicrobial agent. The mechanism of action of ofloxacin and other fluoroquinolone antimicrobials involves inhibition of bacterial topoisomerase IV and DNA gyrase (both of which are type II topoisomerases), enzymes required for DNA replication, transcription, repair and recombination.Ofloxacin has in vitro activity against a wide range of gram-negative and grampositive microorganisms. Ofloxacin is often bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. Fluoroquinolones, including ofloxacin, differ in chemical structure and mode of action from aminoglycosides, macrolides and β-lactam antibiotics, including penicillins. Fluoroquinolones may, therefore, be active against bacteria resistant to these antimicrobials. Ofloxacin has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections.
AEROBIC GRAM-POSITIVE MICROORGANISMS:
Staphylococcus aureus (methicillin-susceptible strains)
Streptococcus pneumoniae (penicillin-susceptible strains)
Streptococcus pyogenes
AEROBIC GRAM-NEGATIVE MICROORGANISMS:
Citrobacter (diversus) koseri
Enterobacter aerogenes
Escherichia coli
Haemophilus influenzae
Klebsiella pneumoniae
Neisseria gonorrhoeae
Proteus mirabilis
Pseudomonas aeruginosaAs with other drugs in this class, some strains of Pseudomonas aeruginosa may develop resistance fairly rapidly during treatment with ofloxacin

PHARMACOKINETIC PROPERTIES OF OFLOXACIN

Following oral administration, the bioavailability of ofloxacin in the tablet formulation is approximately 98%. Maximum serum concentrations are achieved one to two hours after an oral dose.The amount of drug absorbed increases proportionately with the dose. Ofloxacin has biphasic elimination. Following multiple oral doses at steady-state administration, the half-lives are approximately 4-5 hours and 20-25 hours. However, the longer half-life represents less than 5% of the total AUC. Accumulation at steady-state can be estimated using a half-life of 9 hours. The total clearance and volume of distribution are approximately similar after single or multiple doses. Elimination is mainly by renal excretion.
Approximately 32% of the drug in plasma is protein bound.
Following oral administration of recommended therapeutic doses, ofloxacin has been detected in blister fluid, cervix, lung tissue, ovary, prostatic fluid, prostatic tissue, skin, and sputum. The mean concentration of ofloxacin in each of these various body fluids and tissues after one or more doses was 0.8 to 1.5 times the concurrent plasma level. Inadequate data are presently available on the distribution or levels of ofloxacin in the cerebrospinal fluid or brain tissue. Ofloxacin has a pyridobenzoxazine ring that appears to decrease the extent of parent compound metabolism. Between 65% and 80% of an administered oral dose of ofloxacin is excreted unchanged via the kidneys within 48 hours of dosing. Studies indicate that less than 5% of an administered dose is recovered in the urine as the desmethyl or N-oxide metabolites. Four to eight percent of an ofloxacin dose is excreted in the feces. This indicates a small degree of biliary excretion of ofloxacin.
The administration of ofloxacin with food does not affect the Cmax and AUC∞ of the drug, but Tmax is prolonged.Clearance of ofloxacin is reduced in patients with impaired renal function (creatinine clearance rate ≤ 50 mL/min), and dosage adjustment is necessary.
Ofloxacin tablets is contraindicated in persons with a history of hypersensitivity associated with the use of ofloxacin or any member of the quinolone group of antimicrobial agents.
In clinical trials, the most frequently reported adverse events, regardless of relationship to drug, were: nausea 10%, headache 9%, insomnia 7%, external genital pruritus in women 6%, dizziness 5%, vaginitis 5%, diarrhea 4%, vomiting 4%. In clinical trials, the following events, regardless of relationship to drug, occurred in 1 to 3% of patients:Abdominal pain and cramps, chest pain, decreased appetite, dry mouth, dysgeusia, fatigue, flatulence, gastrointestinal distress, nervousness, pharyngitis, pruritus, fever, rash, sleep disorders, somnolence, trunk pain, vaginal discharge, visual disturbances, and constipation.
Store at room temperature, 15-30° C (59-86°F). Keep away from moisture.