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grepafloxacin (Raxar)
Tradename: Raxar. Galaxo Wellcome is voluntarily withdrawing grepafloxaxcin due to safety concerns (November 1999). A small number of severe cardiovascular events (QT prolongation) have been reported. Due to the availability of other agents in this class, grepafloxacin is being withdrawn.
Indications:
- bacterial infections due to susceptible organisms
- acute bacterial exacerbations of chronic bronchitis
- community acquired pneumonia
- Haemophilus influenza
- Streptococcus pneumonia
- Moraxella catarrhalis
- uncomplicated gonorrhea (urethral in male, endocervical & rectal in females) caused by Neisseria gonorrhea
- non-gonococcal urethritis & cervicitis caused by Chlamydia trachomatis
Dosage: 400-600 mg PO QD
Tabs: 200 mg
Dosage adjustment in renal failure: none necessary
Pharmacokinetics:
-> metabolized in the liver by cyt P450 1A2
Antimicrobial activity:
Gram positive
- Streptococcus pneumonia (penicillin susceptible)
- Streptococcus pyogenes
- Streptococcus agalactiae
- Staphylococcus aureus (MSSA)
- Staphylococcus epidermidis (methicillin-sensitive)
Gram negative
- Neisseria gonorrhoeae
- Moraxella catarrhalis
- Haemophilus influenzae
- Escherichia coli
- Klebsiella species
- Enterobacter species
- Proteus mirabilis
- Proteus vulgaris
- Morganella species
- Citrobacter species
Atypical bacteria
- Chlamydia trachomatis
- Mycoplasma pneumonia
Adverse effects:
1) common > 10%
- nausea
- taste aversion
2) less common 1-9%
- headache, dizziness, diarrhea, vaginitis, abdominal pain, vomiting, pruritus, dyspepsia, leukorrhea, asthenia, insomnia, rash, anorexia, somnolence, dry mouth, photosensitivity, constipation, pain, nervousness
3) uncommon <1%
- many, including prolongation of the QT interval
Drug interactions:
1) any drug which inhibits cyt P450 1A2 (including grepafloxacin itself) can increase grepafloxacin levels
2) any drug which induces cyt P450 1A2 can diminish grepafloxacin levels
3) grepafloxacin inhibits cyt P450 1A2, thus inhibits its own metabolism & metabolism of other drugs metabolized by cyt P450 1A2
Interactions
drug interactions
drug adverse effects of fluoroquinolones
Related
cytochrome p450 1A2 (cytochrome P3-450, phenacetin deethylase, cytochrome p450-4, CYP1A2)
General
fluoroquinolone
Properties
INHIBITS: DNA gyrase
MISC-INFO: elimination route LIVER
KIDNEY
1/2life 12-16 HOURS
Database Correlations
PUBCHEM correlations
References
- Galaxo-Wellcome package insert
- Kaiser Permanente News Bulletin
- Prescriber's Letter 13(3): 2006
Cytochrome P450 drug interactions
Detail-Document#: 220233
(subscription needed) http://www.prescribersletter.com