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Healthcare Communications

Ofloxacin

 

Quinolones

* Non-fluorinated nalidixic acid
* Fluorinated (fluoroquinolones)
norfloxacin, ciprofloxacin, ofloxacin, sparfloxacin
- Broader spectrum of activity
- Relatively infrequent development
of resistance

 

 

Ofloxacin

* Synthetic broad spectrum antimicrobial agent for oral administration
* Orally effective agent for Ps. aeruginosa
* Effective in LRTI, skin and skin structures, STDs and UTI
* Well tolerated

 

Mechanism of Action

* Bactericidal
* Inhibits DNA gyrase, an enzyme essential for supercoiling, duplication, transcription, and repair of bacterial DNA

 

Antibacterial Spectrum

Aerobes, Gram-Positive: Staph. aureus, Staph. epidermidis, Strep. pneumoniae, Strep. pyogenes

Aerobes, Gram-Negative: E. coli, Klebsiella pneomoniae, Enterobacter aerogenes, E. cloacae, H. influenzae, H. ducreyi, P. mirabilis, P. vulgaris, Ps. aeruginosa, N. gonnorhoeae, Serratia marcescens, M. catarrhalis

Other microorganisms :
Chlamydia, Mycoplasma, U. urealyticum, M. tuberculosis

 

Resistance

Resistance is rare
- due to spontaneous mutation
(10-9 to 10-12 ) approx.

 

Pharmacokinetics

- Oral bioavailability
- 98% approx.
- Cmax 2.2 mcg/ml in 1- 2 hours with
200 mg orally
- Widely distributed in body tissues and fluids including blister fluid, cervix, lung tissue, ovary, prostatic fluid & tissue, skin, and sputum
- Mainly renal excretion, average urine conc. with a single 200 mg dose is 220 mcg/ml. approx. Clearance reduced in patients with impaired renal function
- 4-8% excreted in the feces
- Half-life 5-6 hours in young adults; 7-8 hours in elderly

 

Indications

Lower Respiratory Tract Infections
- Acute bacterial exacerbations of chronic bronchitis
- Community-acquired pneumonia
Skin and Skin Structure infections

Sexually Transmitted Diseases
- Gonorrhea
- Nongonococcal urethritis and cervicitis due to Chlamydia trachomatis
- Mixed infections
Urinary Tract Infections
- Uncomplicated & complicated urinary tract infections

Adverse Reactions

- Generally well tolerated
- Nausea, insomnia, headache, dizziness, diarrhoea, vomiting, rash, pruritus, external genital pruritus in women, vaginitis, dysgeusia.

 

Precautions & Contraindications

- Caution in patients with renal and hepatic impairment and a known or suspected CNS disorder
- Use in pregnancy only if potential benefit justifies potential risk to the fetus. Produces concentrations in milk , hence caution in lactating women
- Contraindicated in persons with a history of hypersensitivity to ofloxacin or other quinolones

 

Drug Interactions

- Antacids, sucralfate, iron and zinc interfere with absorption
- Inhibits cytochrome P450 enzyme activity; may result in prolonged half-life for drugs metabolized by this system (e.g., cyclosporine, theophylline / methylxanthines, warfarin, etc.)
- Monitor blood glucose levels in diabetics as disturbances of blood glucose may occur in patients treated with quinolones & antidiabetics

 

Dosage

Adults : 200-400 mg daily usually for 5-7 days . Dose greater than 400 mg should be given in 2 divided doses
Urinary Tract Infections : 200-800 mg daily ,
Lower respiratory tract infection : 400-800 mg daily,
Gonorrhoea : 400 mg as single dose
Not recommended for children
Renal disease : I n patients with creatinine clearance < 50 ml/min give a normal initial dose, followed by the usual recommended unit dose q24h
Patients with Cirrhosis: A maximum dose of 400 mg should not be exceeded.

 

 

Salient Features

- Broad spectrum coverage especially gm -ve bacteria
- Oral therapy for Pseudomonas aeruginosa infection
- Effective against bacteria resistant to other important agents e.g., penicillins and cephalosporins
- Resistance is rare
- Wide distribution in the body
- Convenient dosing
- Effective in LRTI, skin and skin structures, STDs and UTI
- Well tolerated