OFLOXACIN http://www.aishikapharma.com/products/OFKA.

htm

OFKA ( Ofloxacin )

OFLOXACIN
Ofloxacin belongs to Fluoroquinolones group of Antimicrobials i.e. – These are the quinolones
having one or more Fluorine substitution in their structure.
Ofloxacin belongs to the first generation Fluoroquinolones.

Other members of the 1st generation Fluoroquinolones are- Norfloxacin, Ciprofloxacin &
Pefloxacin.

Mechanism of Action -:
Ofloxacin inhibits the enzyme Bacterial DNA gyrase,which nicks double standard DNA
introduces negative super coils and then repeals the nicked ends.

The DNA gyrase consists of; two A subunits and two B subunits, A subunit consist of nicking
of DNA while B subunit introduces -ve super coils and then A subunit repeals the stands.

Ofloxacin binds to A subunit with high affinity and interfere with it’s strand cutting &
repealing function.

In Gram+ bacteria the major target of Ofloxacin action is a similar enzymes Topoisomerase.

In place of DNA gyrase or Topoisomerase 4 enzyme the mammalian Cells passess an

Topoisomerase 2 , which has very low affinity for Fluoroquinolones (Ofloxacin)- Hence less
toxicity to the host Cells.

Spectrum of action -:
Intermediate between Ciprofloxacin & Norfloxacin in activity against gram-ve Bacteria, but it
is comparable to or more potent than Ciprofloxacin for gram+ve Organisms.
Good activity against Chlamydia and Mycoplasma.
Other susceptible organisms include – Enterobacter , E.coli, H.influenzae, K.pneumonae,
N.gonorrhoea, Proteus, Pseudomonas aeruginosa, Staph.aureus, Step.pneumonae,
Step.pyogens, anaerobes such as Bacteroides spp. Clostridium spp, Gardnerella vaginelis,
Peptostreptococcus spp. etc.
It also inhibits M.tuberculosis & it is highly active against M.leprae.
Pharmacokinetics -:
It is relatively lipid soluble. Oral bioavailability is higher , attains higher plasma
concentrations.

Food does not interfere with it’s absorption.

It is excreted largely unchanged in urine. Dose needs to be reduced in renal failure

Adverse effects -:
Ofloxacin has good safety records. Side effects occur in <10% cases but are generally mild.

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Gastrointestinal – nausea, vomiting, bad taste, anorexia.

CNS effects – dizziness, headache, restlessness, insomnia, impairment of concentration. Seizers
are rare, occur only at high doses.
Skin hypersensitivity – rashes, pruritis, urticaria etc.

Interactions -:
Better than other 1st generation Fluroquinolones which increase plasma concentration of
Theophylline, Caffeine and Warferin due to inhibition of their metabolism.
Antacids, sucralfates and iron salts given concurrently reduce the absorption of Ofloxacin.
NSAIDS may enhance the CNS toxicity of Ofloxacin.

INDICATIONS (USES) -:

CHRONIC BRONCHITIS AND OTHER RESPIRATORY / ENT INFECTIONS.

GI INFECTIONS.
SKIN & SOFT TISSUE INFECTIONS.
URNARY TRACT INFECTION & UROGENITAL INFECTIONS.
TYPHOID
GONORRHOEA
OFKA -OZ ( Ofloxacin + Ornidazole)

ORNIDAZOLE
Ornidazole is a member of Nitromidazole gp. Of antiamoebic drugs.

Ornidazole is active against Protozoa & Anaerobic bacteria.

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Mechanism of Action -:
Selectively toxic to anaerobic micro-organisms.

After entering the cell by diffusion it’s nitro group is reduced by certain red ox Proteins
operative only in anaerobic microbes to highly reactive nitro radical which exerts cytotoxicity
by damaging DNA & other critical molecules.

Aerobic environment attenuates cytotoxicity of Ornidazole by inhibiting it’s reductive

activation.

Pharmacokinetics -:

Ornidazole is almost completely absorbed from the small intestine.

It is widely distributed in the body attaining therapeutic concentration in vaginal secretions,
semen, saliva and CSF (cerebro spinal fluid).
Compared to Metronidaole, it is slowly metabolized in Liver & excreted in urine.
Plasma ½ life is 12-14 hours

Adverse effects -:
Adverse effects are generally mild & transient and mostly non serious.
Nausea, anorexia, metallic taste, abdominal cramps are the most common. Occasionally
diarrhea may be seen.
Less frequent side effects are – Headache, glossitis, dryness of mouth, dizziness, rashes &
transient neutropenia.
Prolonged administration may cause CNS neuropathy and CNS effects. Seizures occur after
very high doses.
Thrombophelebitis of injected vein if solution is not well diluted.

Contraindications -:
Neurological disorders

Blood dyscrasiae

1st Trimester of pregnancy

chronic alcoholism

Hypersensitivity to Ornidazole or other Nitromidazoles.

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Interactions -:
A disulfiram like intolerance to alcohal occurs.

Phenobarbitone, Rifampicin may reduce it’s therapeutic effects.

Cimetidine can reduce it’s metabolism.

Concomitant use of oral anticoagulants may increase the risk of hemorrhage.

INDICATIONS (USES) -:

AMOEBIASIS
GIARDIASIS
TRCHOMONAS VAGINITIS
ANAEROBIC BACTERIAL INFECTIONS
ULCERATIVE GINGIVITIS
TRENCH MOUTH
BACTERIAL VAGINOSIS

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