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Tequin

Company: Bristol-Myers Squibb
Approval Status: December, 1999
Treatment for: Community-acquired respiratory tract infections
Areas: Urology & Kidneys; Pregnancy & Gynecology; Respiratory

| General Information | Clinical Results | Side Effects | Mechanism of Action | Literature References | Additional Information |


General Information

The first quinolone antibiotic to come in bioequivalent 400 mg injectable and tablet formulations, this is a solution of gatifloxacin indicated for community-acquired respiratory tract infections and certain bacteria-caused sexually transmitted diseases. It was created with a unique 8-methoxy structure that seems to increase bactericidal action and lessen the rate of growth of resistance of gram-positive bacteria. Therefore, it can treat some infections that other antibiotics like penicillin cannot. There were estimated to be 125 million cases of such infections last year in the U.S.

The following community-acquired respiratory tract infections may be treated with Tequin:

  • Acute bacterial exacerbation of chronic bronchitis
  • Acute sinusitis
  • Community-acquired pneumonia

Other indications include:

  • Uncomplicated urinary tract infections (cystitis)
  • Complicated urinary tract infections
  • Pyelonephritis (from e.Coli)
  • Uncomplicated urethral and cervical gonorrhea
  • Acute, complicated rectal infections in women

Clinical Results

Tequin has exhibited an overall success rate of <=90% in acute exacerbation of chronic bronchitis, <96% for acute sinusitis, and <=97% for community-acquired pneumonia. The in vitro activity of Tequin against important respiratory tract pathogens was greater than 99%.


Side Effects

Few; drug is tolerated well by almost all patients. The most common side effects are mild dizziness, nausea, vomiting, stomach pain, diarrhea, or headaches. It is not suggested that the patient operate heavy machinery until they see if dizziness occurs; also, because of photosensitivity occasionally exhibited by those taking some quinonlones (although not, so far, Taquin) tanning beds should be avoided.


Mechanism of Action

Gatifloxacin, like other fluoroquinines, has a different mechanism of action from other antibiotics, thereby making it useful for infections that will not respond to penicillin, cephalosporins, macrolides, aminoglycosides, or tetrocyclines. Its antibacterial properties stem from an inhibition of DNA gyrase (an enzyme that repairs bacterial DNA) and topoisomerase IV (another enzyme that partitions a bacteria’s chromosomes), thus aiding the natural selection against the development of mutant, gram-positive bacteria. Its chemical formula is:

(±) -1-cyclopropyl-6-fluoro-1, 4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid sesquihydrate

It is administered as a racemate.

Oral administration: tablets, 200 and 400 mg, for oral administration; once daily, 400 mg for 7-14 days depending on indication
Injection: single-use 20- or 40-mL vials (10 mg/mL), for intravenous administration; 400 mg (40mL) once daily for 7-14 days depending on indication


Literature References

National Committee for Clinical Laboratory Standards, Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria That Grows Aerobically - Fourth Edition; Approved Standard, NCCLS Document M7-A4, Volume 17, No. 2, NCCLS, January 1997

National Committee for Clinical Laboratory Standards, Performance Standards for Antimicrobial Disk Susceptibility Tests - Sixth Edition; Approved Standard, NCCLS Document M2-A6, Volume 17, No. 1, NCCLS, January 1997


Additional Information

Orally administered Tequin is rapidly absorbed after administration and there is no relation to, or restrictions on, food intake. Oral and intravenous routes are considered interchangeably since the speed of efficacy is virtually identical.

There are no restrictions as to age or gender, except for the caveats listed below. Elderly females do show differences with other groups, but this is considered normal due to body weights and no adjustment of dosage is required for them.

Gatifloxacin has NOT yet been tested for safety on pediatric patients, adolescents (less than 18 yr), pregnant or lactating women.

There is a slight interaction with Digoxin; other drugs are largely not affected.

Like other quinolones, Tequin should be used with caution in patients with CNS disorders such as epilepsy and severe cerebral arteriosclerosis.

Pharmocodynamic interactions have been noted when congenital conditions that prolong the QTc interval were present; therefore Gatifloxacin should not be taken with Class IA and Class III antiarhythmics. Patients being treated for heart rhythm interval problems should inform their doctor.

Patients with hypokalemia caused by diuretic drugs should inform their doctor.




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Tequin Drug Information

The Tequin drug information shown above is licensed from Thomson CenterWatch. The information provided here is for general educational purposes only and does not constitute medical or pharmaceutical advice which should be sought from qualified medical and pharmaceutical advisers.





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