PERK

 

For the use of a Registered Medical Practitioner or a Hospital or a Laboratory only

OFO-O

(Ofloxacin, Ornidazole and Dimethyl Polysiloxaine Tablets)

 

Description

OFO-O Tablets are a synthetic broad-spectrum anti-polymicrobial agent for oral administration. It contains , ofloxacin, a fluorinated carboxyquinolone, is the racemate, ()-9- fluoro-2,3-dihydro-3-methyl-10- (4-methyl-1-piperazinyl)-7-oxo-7H- pyrido[1,2,3-de]-1,4-benzoxazine -6- carboxylic acid. Its empirical formula is C18H20FN3O4, and its molecular weight is 361.4. and Ornidazole, which is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria. Chemically, ornidazole is 1 Chloro 3 - (2-methyl-5-nitroimidazol-1-yl) propan 2 ol and Dimethyl Polysiloxaine (also known as simethicone) which is the most popular anti-flatulant. OFO-O is a orange brown coloured, oblong, biconvex, film coated tablet, scored on one side and plain on the other.

 

Composition

Each film coated tablet contains:
Ofloxacin USP 200mg

Ornidazole   500mg

Dimethyl Polysiloxaine IP 50mg

 

Pharmacology

Ofloxacin has in vitroactivity against a broad spectrum of gram-positive and gram-negative aerobic and anaerobic bacteria. Ofloxacin is often bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. Ofloxacin is thought to exert a bactericidal effect on susceptible microorganisms by inhibiting DNA gyrase, an essential enzyme that is a critical catalyst in the duplication, transcription, and repair of bacterial DNA.

The antimicrobial activity of Ornidazole is due to the reduction of the nitro group to a more reactive amine that attacks microbial DNA, brings about loss of helical structure of DNA and subsequent DNA breakage thus inhibiting further synthesis and causing degradation of existing DNA.  

Dimethyl Polysiloxaine is a very strong anti-flatulent agent

Rationality
The pharmacokinetic behaviour of the three drugs should be similar to support the use of the three agents in fixed-dose-combination.

Both the drugs in Co-trimoxazole, which is an established combination of sulphamethoxazole and trimethoprim, have their pharmacokinetic parameters like t 1/2 (about 10 hrs for both the drugs) matching with that of each other.

Similarly, the half-lives of Ofloxacin, Ornidazole and MPS fall in the same range and hence, the time course of action of the three drugs might be similar which is an important criterion for the possibility of a rational fixed-dose-combination. As there is always associated flatulence problem in such patients hence the addition of Dimethyl Polysiloxaine gives greater and immediate symptomatic relief.

Hence, it can be said that Ofloxacin, Ornidazole and Dimethyl Polysiloxaine show synergistic potential which is one of the most important factor in deciding the feasibility of a FDC.

Pharmacokinetics

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. Absorption of ofloxacin after single or multiple doses of 100 to 400 mg is predictable, and 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.

 

Ornidazole is readily absorbed from the gastro-intestinal tract and peak plasma concentrations of about 30 mcg per ml have been achieved within 2 hours of a single dose of 1.5 g, falling to about 9 mcg per ml after 24 hours and 2.5 mcg per ml after 48 hours.

The plasma elimination half-life of ornidazole is 12 to 14 hours. Less than 15% is bound to plasma proteins. It is widely distributed in body tissues and fluids, including the cerebrospinal fluid.

Ornidazole is metabolised in the liver and is excreted in the urine, mainly as conjugates and metabolites, and to a lesser extent in the faeces; 85% of a single oral dose has been reported to be eliminated within 5 days, 63% in the urine and 22% in the faeces. Biliary excretion may be important in the elimination of ornidazole and its metabolites.  

Indications

OFO-O may be used in the treatment of mixed polymicrobial infections like

 

         Lower Respiratory Tract (Acute bacterial exacerbations of chronic bronchitis & Community-acquired Pneumonia)

         Skin and skin structure infections

         Sexually Transmitted Diseases

         Acute, complicated urethral and cervical gonorrhea.

         Nongonococcal urethritis and cervicitis

         Mixed infections of the urethra and cervix

         Urinary Tract Infections (cystitis)

         Prostatitis due to Escherichia coli.

         Hepatic and intestinal amoebiasis, giardiasis, trichomoniasis of urogenital tract

         Bacterial vaginosis.

         ENT Infections

Also used in the treatment and prophylaxis of susceptible aerobic and anaerobic infections in dental and gastrointestinal surgery & in other mixed aerobic anaerobic infections. OFO-O is also advocated in the management of H. pylori duodenal ulcer in combination with other drugs.  

 

Contraindications

OFO-O is contraindicated in persons with a history of hypersensitivity to ofloxacin, to other quinolones, or to any of the components in this medication and in patients hypersensitive to ornidazole and other imidazoles. There is no evidence of accumulation when used in pregnant women. Therefore dosage regimen requires no adjustment during pregnancy.     

Adverse Reactions

The most frequently encountered side effect is dizziness, alone or in combination with other adverse reactions. The other side effects occuring to a lesser extent are nausea, pyrosis, intestinal spasms and metallic taste. Vertigo, fatigue and other discomforts such as loose stools, insomnia, skin rash and headache have also been reported.  

 

Dosage and Administration

The usual dose of OFO-O tablets are 1 tablet orally every 12 h. These recommendations apply to patients with normal renal function (i.e., creatinine clearance > 50 ml/min).

  Mixed Amoebiasis

Adults : 1 tab  twice daily for 5-7 days
Children: tab
once daily for 5 to 10 days

  Mixed Amoebic dysentery

Adults : 3 tablets once daily for 3 days
Children :
1 tablet once daily for 3 days

  Mixed Giardiasis :

Adults : 3 tablets once daily for 1-2 days
Children:
1 tablet for 2 days

  Trichomoniasis

Adults : 3 tablets once or 1 tablet twice daily for 5 days. Sexual partner should be simultaneously treated.

  Bacterial vaginosis and STD

Adults : 3 tablets once or 1 tablet once daily for 5-7 days

  Mixed bacterial infections in Lower Respiratory Tract, Gynaecology, ENT, Surgical Infections and

  Dental Infections

Initiate oral therapy as soon as possible after I.V. infusion in surgical conditions.

Adults : 1 tablet twice daily for 5 to 10 days
Children :
  tablet twice daily

 

Overdosage and Treatment

No data is available on overdosage toxicity. In the event of an overdosage the stomach may be emptied and symptomatic treatment should be given.

 

Storage instructions

Store at a temperature below 25C, protect from light and moisture.

 

Presentation

Available in blister strips of 10 x 10's tablets'.

 

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