Quinolone
Gram positive bacteria: methicillin-susceptible Staphylococcus epidermidis, Staphylococcus saprophyticus
Gram negative bacteria: Enterobacteriaceae, H. influenzae, other Haemophilus spp., N. gonorrhoeae, N. meningitides, M. catarrhalis, P. aeruginosa,
Inhibition of topoisomerase (DNA gyrase) enzymes, which inhibits relaxation of supercoiled DNA and promotes breakage of double stranded DNA.
Fluoroquinolones produce both concentration-dependent (peak:MIC), and a combination of concentration and time-dependent killing (AUC:MIC).
400mg dose; Cmax: 1.5mg/ml; Volume of distribution: 1.7 L/kg; Table 2
CNS: headache, insomnia, dizziness; hallucinations, depression, psychotic reactions (rare)
Connective tissue: tendon injury
Renal: interstitial nephritis
Cardiovascular: QTC prolongation, torsades de pointes, arrhythmias
Oral: 200mg, 300mg, 400mg tablet
Intravenous: 200mg/50ml
Opthalmic/Otic: 0.3% solution
Chronic bronchitis: 400 mg PO/IV every 12 hr x 10 days
Community-acquired pneumonia: 400 mg PO/IV every 12 hr x 10 days
Cystitis: (E. coli, K. pneumoniae) 200 mg PO/IV every 12 hr x 3 days
Cystitis: (other approved organisms) 200 mg PO/IV every 12 hr x 7 days
Gonorrhea: 400 mg IV or ORALLY as a single dose
Nongonococcal cervicitis/urethritis: 300 mg PO/IV every 12 hr x 7 days
Pelvic inflammatory disease: 400 mg PO/IV every 12 hr x 10-14 days
Prostatitis: 300 mg PO/IV every 12 hr for 6 weeks
Skin/skin structure infection: 400 mg PO/IV every 12 hr x 10 days
Urinary tract infection, complicated: 200 mg PO/IV every 12 hr x 10 days
Conjunctivitis: Day 1 and 2, 1-2 drops in affected eye every 2-4 hr; day 3-7, 1-2 drops 4 times a day
Corneal ulcers: Day 1 and 2, 1-2 drops in affected eye every 30 minutes while awake; day 3-7, 1-2 drops every hour while awake; day 7-9, 1-2 drops 4 times a day
Otitis externa: 10 drops into affected ear once a day x 7 days
Otitis media with perforated Tympanic membranes: 10 drops into affected ear twice a day x 14 days
Conjunctivitis: (1 year of age and older) Day 1 and 2, 1-2 drops in affected eye every 2-4 hr; day 3-7, 1-2 drops 4 times a day
Corneal ulcers: (1 year of age and older) Day 1 and 2, 1-2 drops in affected eye(s) every 30 minutes while awake; day 3-7, 1-2 drops every hour while awake; day 7-9, 1-2 drops 4 times a day
Otitis externa: (6 months-13 years of age) 5 drops in affected ear once a day for 7 days; (13 years and older) 10 drops into affected ear(s) once a day x 7 days
Otitis media, acute with tympanostomy tubes: (1-12 years of age) 5 drops in affected ear twice a day x 10 days
Otitis media, chronic suppurative with perforated Tympanic membranes: (12 years and older) 10 drops in affected ear twice a day x 14 days
Renal failure: CrCl < 20 mL/min, one-half the usual dose q24 hr
Hepatic failure: severe hepatic impairment (cirrhosis), maximum of 400 mg q24 hr
Precautions:
Divalent cations: aluminum, magnesium zinc, iron, calcium, antacids, sucralfate – reduced bioavailability of quinolones (can cause therapeutic failure)
Theophylline, caffeine, xanthines: clearance of these is inhibited with fluoroquinolones
Category C: Risk unknown. Human studies inadequate.
Therapeutic: Culture and sensitivities, signs and symptoms of infection
Toxic: Urinalysis, BUN, SCr, AST and ALT, Physicial examination: encephalopathic changes
APO-OFLOX (Apotex – CANADA, MALAYSIA)
EXOCIN (Allergan - UNITED KINGDOM, ITALY, SOUTH AFRICA, IRELAND, DENMARK, PORTUGAL, FINLAND, SPAIN, GREECE)
FLOXAL - (Riel – AUSTRIA, GERMANY, SWITZERLAND, HUNGARY, CZECH REPUBLIC)
FLOXIN (ORTHO MCNEIL PHARMACEUTICAL – USA, CANADA)
INOFLOX (Biomedis, SINGAPORE, MALAYSIA)
OCUFLOX (Allergan – USA, CANADA, MEXICO)
OFLOX (Basics – GERMANY, CHILE, AUSTRIA)
TARIVID (Aventis - UNITED KINGDOM, IRELAND, JAPAN, NETHERLANDS, SOUTH AFRICA, SWEDEN, SWITZERLAND, BELGIUM, NORWAY, AUSTRIA, DENMARK, PORTUGAL, HONG KONG, ISRAEL, GERMANY, THAILAND, FINLAND, MALAYSIA, HUNGARY, CZECH REPUBLIC)
ZANOCIN (Ranbaxy – MALAYSIA, HUNGARY, CZECH REPUBLIC)