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Utibid

UTIBID (Norfloxacin) represents a new generation of quinolones carboxylic acid derivatives referred to as the Fluoroquinolones.

Composition
UTIBID 400
Each film coated tablet contains Norfloxacin USP 400 mg.

Chemistry
UTIBID (Norfloxacin) is a quinolone carboxylic acid derivative. Chemically it is 1-ethyl-6-fluoro-1, 4-dihydro-4-OXO-7-(1-piperazinyl)-3-quinoline carboxylic acid. Its empirical formula is C16H18FN3O3, and the structural formula is:

Utibid

It has a molecular weight of 319.33.

Microbiology
Norfloxacin has in vitro activity against a broad range of gram-positive and gram-negative aerobic bacteria.

The fluorine atom at the 6 position provides increased potency against gram-negative organisms, and the piperazine moiety at the 7 position is responsible for anti-pseudomonal activity. Norfloxacin inhibits bacterial deoxyribonucleic acid synthesis and is bactericidal. At the molecular level, three specific events are attributed to norfloxacin in E.coli cells.

1. Inhibition of the ATP-dependent DNA supercoiling reaction catalyzed by DNA gyrase.
2. Inhibition of the relaxation of supercoiled DNA.
3. Promotion of double-standard DNA breakage.


Resistance to Norfloxacin due to spontaneous mutation in vitro is a rare occurrence (range 10,1 to 10.'2 cells). Resistant organisms have emerged during therapy with Norfloxacin in less than 1 % of patients treated. Organisms in which development of resistance is greatest are the following:
Pseudomonas aeruginosa
Klebsiella pneumoniae
Acinetobacter species
Enterococcus species


Norfloxacin has been shown to be active against most strains of the following organisms both in vitro and in clinical infections.

Gram-positive aerobes
Enterococcus faecalis
Staphylococcus aureus
Staphylococcus epidermidis
Staphylococcus saprophyticus
Streptococcus agalactiae
Gram-negative aerobes
Citrobacter freundii
Enterobacter aerogenes
Enterobacter cloacae
Esherichia coli
Klebsiella pneumoniae
Neisseria gonorrhoeae
Proteus mirabilis
Proteus vulgaris
Pseudomonas aeruginosa
Serratia marcescens


Norfloxacin has been shown to be active in vitro against most strains of the following organisms; however, the clinical significance of these data is unknown.

Gram-positive aerobes

Bacillus cereus
Gram-negative aerobes

Acinetobacter calcoaceticus

Aeromonas species

Alcaligenes species

Campylobacter species

Citrobacter diversus

Edwardsiella tarda

Flavobacterium species

Klebsiella oxytoca

Klebsiella rhinoscleromatis

Morganella morganii

Providencia alcalifaciens

Providencia rettgeri

Providencia stuartii

Salmonella species

Shigella species

Vibrio cholerae

Vibrio parahaemolyticus

Yersinia enterocolitica


Other
Ureaplasma urealyticum


Norfloxacin is not generally active against obligate anaerobes. It has not been shown to be active against Treponema pallidum.

 

Clinical Pharmocology
Following oral administration, 30-40% of UTIBID (Norfloxacin) is rapidly absorbed from the GI tract. Peak serum concentrations (Cmax) of 1.5 to 2.0 mcg/ml (average in some studies 1.6 mcg/ml) are achieved in 1-2 hours (average tmax 1.5 hrs), after a 400 mg dose of Norfloxacin. With an 800 mg dose of Norfloxacin, average Cmax was 2.4 mcg/ml.


Absorption is only slightly delayed when Norfloxacin is administered with food. Due to the low protein binding (14%) and high lipid solubility, UTIBID (Norfloxacin) is widely distributed to the various tissues. Liver is the primary site of metabolism.

 

Six metabolites of Norfloxacin, of lesser antimicrobial potency, are excreted unconjugated in the urine. Liver impairment has no major effect on the pharmacokinetics of Norfloxacin.

 

Urine is the major route of excretion of UTIBID. 30% of the drug is excreted unchanged in the urine.

 

Renal clearance of UTIBID is high (about 2 to 21/2 times the glomerular filtration rate) and urinary concentrations of Norfloxacin are about 100 to 300 times the simultaneous serum concentrations. Urinary concentrations of Norfloxacin is in excess of MIC of most of the urinary pathogens for about 12 to 24 hours after a single 400 mg dose. In addition to glomerular filtration, there is also active tubular secretion of Norfloxacin. As the glomerular filtration rate falls, the mean serum elimination half-life tends to increase and necessitates dosage adjustment in moderate to severe renal impairment.

 

The serum elimination half-lives of Norfloxacin reported in various studies have ranged from 3.5 to 6.5 hours.

 

The average values for above with moderate renal failure are reportedly 6.5 hours and with more severe forms -arid renal impairment have been reported to be about 7.7 hours.


Indications and Usage
UTIBID is indicated for the treatment of adults with the following infections caused by susceptible strains of the designed microorganisms.
 

Urinary tract infections
Uncomplicated urinary tract infections (including cystitis due to Enterococcus faecalis. Esacherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonos aeruginosa, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Proteus vulgaris, Staphylococcus aureus or Streptococcus agalactiae.

 

Complicated urinary tract infections due to enterococcus faecalis, Esherichia colt, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, or Serratia marcescens.


Sexually transmitted disease
Uncomplicated urethral and cervical gonorrhoea due to Neisseria gonorrhoeae.


Contraindications
UTIBID is contraindicated in patients with a history of hypersensitivity to Norfloxacin or the other members of the quinolone group of antibacterial agents.


Warnings
The safety and efficacy of oral Norfloxacin in children, adolescents (under the age of 18), pregnant women, and nursing mothers have not been established.

 

The oral administration of single dose of Norfloxacin 6 times the recommended human clinical dose (on a mg/kg basis), caused lameness in immature dogs.


Histologic examination of the weight bearing joints of these dogs revealed permanent lesions of the cartilage. Other quinolones also produced erosion of the cartilage in weight-bearing joints and other signs of arthropathy in immature animals of various species. Norfloxacin has not been shown to be effective in the treatment of syphilis. Antimicrobial agents used in high doses for short period of time to great 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 Norfloxacin should have a follow-up serologic test for syphilis after 3 months.


Serious and occasionally fatal hypersensitivity (anaphylactoid or anaphylactic) reactions may occur. If an allergic reaction to Norfloxacin occurs, discontinue the drug. Serious acute hypersensitivity reactions may require immediate emergency treatment with epinephrine. Oxygen, intravenous fluids, antihistamines and airway management, including intubation should be administered as indicated.

 

Convulsions have been reported in patients receiving Norfloxacin. Convulsions, increased intracranial pressure, and toxic psychoses have been reported in patients receiving drugs in this class. Quinolones, may also cause central nervous system (CNS) stimulation, which may lead to tremors, restlessness, lightheadedness, confusion and hallucination.

 

If these reactions occur in patients receiving Norfloxacin, the drug should be discontinued and appropriate measures instituted.

 

The effects of Norfloxacin on brain function or on the electrical activity of the brain have not been tested. Therefore, until more information becomes available, Norfloxacin, like all other quinolones, should be used with caution in patients with known or suspected CNS disorders, such as severe cerebral arteriosclerosis, epilepsy and other factors which predispose to seizures.

 

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