No

Antibiotic, Quinolone

Treatment of acute bacterial exacerbations of chronic bronchitis caused by Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis; community-acquired pneumonia caused by Mycoplasma pneumoniae or the organisms previously mentioned; uncomplicated gonorrhea caused by Neisseria gonorrhoeae, and nongonococcal cervicitis and urethritis caused by Chlamydia trachomatis

C

Previous hypersensitivity to grepafloxacin and other quinolone derivatives; in patients with hepatic failure; given concomitantly with class I and III antiarrhythmics or bepridil due to the potential risk of cardiac arrhythmias (including torsade de pointes); patients with QT_c prolongation and use with drugs which prolong QT_c interval

Use caution in patients with cerebral arteriosclerosis or epilepsy, and in patients with GI disorders or hepatic or renal dysfunction; there is no data to support safety and efficacy in children <18 years of age

Percentage unknown: Syncope, headache, dizziness, fatigue, nausea, emesis due to medicinal taste, hepatotoxicity (ie, elevated serum transaminases), abdominal pain, diarrhea, hypersensitivity

CYP1A2 enzyme substrate

Inhibits DNA-gyrase in susceptible organisms; inhibits relaxation of supercoiled DNA and promotes breakage of double-stranded DNA

Absorption: Peak plasma levels at 2-3 hours

Distribution: High concentrations have been achieved in bile, gynecologic tissue, hair, blister fluid, lung and other tissue; V_d: 5 L/kg

Metabolism: Liver, unknown activity of metabolites

Bioavailability: 70%

Half-life: 15.7 hours

Elimination: Eliminated unchanged in urine (10%); the rest in bile, feces, and metabolites

Oral:

Community-acquired pneumonia: 600 mg/day for 10 days

Nongonococcal urethritis or cervicitis: 400 mg/day for 7 days

Uncomplicated gonorrhea: 400 mg as a single dose

May be taken with or without meals; multivitamins, antacids, or sucralfate should not be taken within 4 hours before or 4 hours after taking grepafloxacin

CBC, signs/symptoms of infection, liver/renal function tests

May cause drowsiness or dizziness; quinolones reported to cause restlessness, hallucinations, euphoria, depression, panic, and paranoia

None reported

No information available to require special precautions

No effects or complications reported

Take per recommended schedule; complete full course of therapy and do not skip doses. Take on an empty stomach (1 hour before or 2 hours after meals, dairy products, antacids, or other medications). Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Diabetics should monitor glucose levels closely; this medication may alter effect of oral hypoglycemic agents. You may experience dizziness, lightheadedness, anxiety, insomnia, or confusion (use caution when driving or engaging in tasks that require alertness until response to drug is known); photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight). Report immediately any CNS disturbances (hallucinations, agitation, confusion, seizures), chest pain, or palpitations. Report persistent GI disturbances; muscle or tendon pain, swelling, or redness; signs of opportunistic infection (sore throat, chills, fever, burning, itching on urination, vaginal discharge, white plaques in mouth); or worsening of condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed.

Tablet, as hydrochloride: 200 mg, 400 mg, 600 mg

Chodosh S, Lakshminarayan S, Swarz H, et al, "Efficacy and Safety of a 10-Day Course of 400 or 600 Milligrams of Grepafloxacin Once Daily for Treatment of Acute Bacterial Exacerbations of Chronic Bronchitis: Comparison With a 10-Day Course of 500 Milligrams of Ciprofloxacin Twice Daily," Antimicrob Agents Chemother, 1998, 42(1):114-20.

"Grepafloxacin - A New Fluoroquinolone," Med Lett Drugs Ther, 1998, 40(1019):17-8.

Kozawa O, Uematsu T, Matsuno H, et al, "Comparative Study of Pharmacokinetics of Two New Fluoroquinolones, Belofloxacin and Grepafloxacin, in Elderly Subjects," Antimicrob Agents Chemother, 1996, 40(12):2824-8.

McCormack WM, Martin DH, Hook EW 3d, et al, "Daily Oral Grepafloxacin vs Twice Daily Oral Doxycycline in the Treatment of Chlamydia trachomatis Endocervical Infection," Infect Dis Obstet Gynecol, 1998, 6(3):109-15.

Wagstaff AJ and Balfour JA, "Grepafloxacin," Drugs, 1997, 53(5):817-24.