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Trovan - Zithromax

Clinical Pharmacology
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CLINICAL PHARMACOLOGY

TROVAFLOXACIN

Absorption

Trovafloxacin is well-absorbed from the gastrointestinal tract after oral administration. The absolute bioavailability is approximately 88%.

Pharmacokinetics

The mean pharmacokinetic parameters (±SD) of trovafloxacin after a 100-mg oral dose appear in the table below.

TROVAFLOXACIN PHARMACOKINETIC PARAMETERS 100-mg SINGLE ORAL DOSE

Cmax

(mg/mL)

Tmax

(hrs)

AUC(0-¥)

(mgh/mL)

T1/2

(hrs)

1.0±0.3
0.9±0.4
11.2±2.2
9.1
Cmax= Maximum serum concentration; Tmax= Time to Cmax; AUC (0-¥)

=Area under concentration vs. time curve to infinite time; T1/2= serum half- life


Oral absorption of trovafloxacin is not altered by concomitant food intake; therefore, it can be administered without regard to food.

The systemic exposure to trovafloxacin (AUC 0-¥)administered as crushed tablets via nasogastric t.b. into the stomach was identical to that of orally administered intact tablets. Administration of concurrent enteral feeding solutions had no effect on the absorption of trovafloxacin given via nasogastric t.b. into the stomach. When trovafloxacin was administered as crushed tablets into the duodenum via nasogastric tube, the (AUC 0-¥) and peak serum concentration (Cmax) were reduced by 30% relative to the orally administered intact tablets. Time to peak serum level (Tmax) was also decreased from 1.7 hrs to 1.1 hrs.

Distribution

The mean plasma protein bound fraction is approximately 76%, and is concentration-independent. Trovafloxacin is widely distributed throughout the body. Rapid distribution of trovafloxacin into tissues results in significantly higher trovafloxacin concentrations in most target tissues than in plasma or serum.

Reproductive Fluid or Tissue
Tissue-Fluid/Serum Ratio* (Range)
prostatic tissue
1.0 (0.5-1.6)
cervix (multiple dose)
0.6 (0.5-0.7)
ovary
1.6 (0.3-2.2)
fallopian t.b.
0.7 (0.2-1.1)
myometrium (multiple dose)
0.6 (0.4-0.8)
uterus
0.6 (0.3-0.8)
vaginal fluid (multiple dose)
4.7 (0.8-20.8)
* Mean values in adults over 2-29 hours following single 200-mg tablet administration (multiple 200-mg
Brand Name: Trovan - Zithromax
Generic Name: Trovafloxacin and Azithromycin
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