Concentrations of metronidazole and tinidazole in serum and gynecological organs were analyzed after a single 500 mg intravenous infusion and after three days of treatment with 400 mg t.i.d. of metronidazole or 500 mg b.i.d. of tinidazole. The studies were performed in 67 patients subjected to hysterectomy and/or oophorectomy because of myomatosis uteri, carcinoma uteri or endometriosis. At the time of organ removal (about 30 min after infusion), metronidazole and tinidazole levels in serum were 14.5 +/- 0.45 mg/l and 12.3 +/- 0.38 mg/l, respectively. Concentrations of both drugs in the uterus and Fallopian tube were about the same as the simultaneous serum levels and concentrations in the ovaries about 55% thereof. At steady-state, the concentrations of tinidazole in serum (23.5 +/- 1.0 mg/l) were remarkably higher than those of metronidazole (13.5 +/- 0.84 mg/l) about three hours after the last oral dose. Drug concentrations in organs of the female reproductive tract were 70 to 100% those of the simultaneous serum levels.
The steady-state concentrations of metronidazole and tinidazole in male genital tissues were analyzed in patients subjected to elective gonadal surgery. The nitroimidazoles were administered orally at 500 mg every 8 h, beginning 5 days before the operation. Eight hours after the last dose, the concentrations of tinidazole were 24.1 +/- 2.5 micrograms (mean +/- standard error of the mean)/g of prostatic tissue, 29.1 +/- 2.9 micrograms/g of vas deferens, 22.1 +/- 2.1 micrograms/g of epididymis, and 18.6 +/- 2.3 micrograms/g of testis. The corresponding values of metronidazole were 14.3 +/- 1.8 micrograms/g, 15.9 +/- 1.2 micrograms/g, 14.0 +/- 1.2 micrograms/g, and 12.5 +/- 1.7 micrograms/g, respectively.
Concentrations of metronidazole and tinidazole in serum and abdominal tissues were determined after a single 500-mg intravenous infusion or after a 5-day oral dosage of 500 mg three times daily in groups of 10 patients each. In the patients who got the single infusions, the concentrations in tissues (except fat) reached almost the serum levels 10 min after the infusion. At 24 h, the tinidazole concentrations in serum averaged 3.2 μg/ml and those of metronidazole 1.3 μg/ml. In the patients who got the 5-day oral dosages, the steady-state levels of tinidazole in both serum and tissues were twice as high as those of metronidazole.
Concentrations of erythromycin and 2'-acetyl erythromycin were analysed in serum or plasma and tonsil tissue after repeated dosage of erythromycin acistrate (EA), a new erythromycin prodrug, in two separate studies in 61 young patients. The reference preparations were: (1) enterocoated tablets of erythromycin base (EB enterotablets, (2) erythromycin base as enterocoated pellets (EB enterocapsules) and (3) erythromycin stearate (ES). All drugs were given 500 mg tid for three days before scheduled tonsillectomy. Tonsils were removed about 3 h after intake of the last dose. Blood samples were collected at 0, 2 and 6 h and at the time of tonsillectomy. At all time points EA produced several-fold higher total drug (erythromycin + 2'-acetyl erythromycin) concentrations in serum or plasma than any of the reference preparations. Similarly, after EA the mean total antibiotic levels in tonsil tissue exceeded the erythromycin levels after the reference preparations by at least a factor of 3. Tonsil/serum or plasma ratios of the total antibiotic were quite similar with all preparations (means 38-50%). Peak erythromycin levels in circulation did not differ significantly from each other in spite of two nonabsorbers after EB enterotablets. The same was true of tonsil tissue. There were, however, 15 tonsils with undetectable erythromycin: 4/25 (16%) with EA, 5/12 (42%) with EB enterotablets, 2/12 (17%) with EB enterocapsules and 4/12 (33%) with ES. The degree of hydrolysis of 2'-acetyl erythromycin to erythromycin was 23-43% higher in tonsil tissue than in circulation.
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