Tequin
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Community-acquired respiratory tract infections
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.