Single 1 g dose of cefotaxime in the treatment of infections due to penicillinase-producing strains of Neisseria gonorrhoeae.

Purpose To evaluate the tolerability, safety, pharmacokinetics and drug interaction of cefotaxime sodium–tazobactam sodium injection (6:1) in Chinese healthy subjects. The results of the safety and pharmacokinetic studies supported further clinical trials. Method A randomized, single-blind, ascending dose, placebo-controlled, single-center study was conducted. Sixty healthy subjects (38 males, 22 females) participated in this study. For the single-dose part, 0.47, 1.17, 2.34, 3.51, and 4.68 g of cefotaxime sodium–tazobactam sodium injection (6:1) was administered. For the multiple-dose part, the subjects were administered 2.34 and 3.51 g cefotaxime sodium–tazobactam sodium injection (6:1) three times a day for 7 consecutive days. For the drug interaction part, the subjects received 2.0 g cefotaxime sodium and 0.34 g tazobactam sodium alone and in combination. Results Most adverse events and adverse drug reactions were mild. Moderate rash was considered a serious adverse event because of prolongation of hospitalization. The main pharmacokinetic parameters of cefotaxime and tazobactam had no significance difference between the 1.17, 2.34, and 3.51 g dose cohorts and between genders. There was no difference in trough concentrations on days 6, 7, and 8. The R C max and R AUC were (0.921 ± 0.070) and (0.877 ± 0.057) for cefotaxime, and (0.913 ± 0.046) and (0.853 ± 0.060) for tazobactam, respectively. Following the administration of cefotaxime and tazobactam alone and in combination, the 90% conﬁdence intervals of the geometric mean ratios for C max and AUC were within the predetermined range of 80–125%. In the single-dose part, the renal cumulative excretion ratios were (51.7 ± 6.2)% for cefotaxime, and (84.3 ± 8.1)% for tazobactam. There was no significant difference in the maximum excretion rates and cumulative excretion ratios for cefotaxime and tazobactam, alone or in combination. Conclusions Cefotaxime sodium–tazobactam sodium injection (6:1) was well-tolerated at doses of 0.47 to 4.68 g. The pharmacokinetics of cefotaxime and tazobactam were reported as linear over a dose range of 1.17–3.51 g. Cefotaxime was partially excreted via urine, whereas tazobactam was mainly excreted via urine. There was no significant accumulation after administration over 7 consecutive days. The pharmacokinetics and excretion of cefotaxime and tazobactam were not affected by the co-administration of cefotaxime–tazobactam.

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“…De Koning et al. ( De Koning et al., 1983 ) reported that one patient developed erythematous macular rash 2 days after treatment with CTX.…”

Section: Discussionmentioning

confidence: 99%

“…Babu (Babu and Sharmila, 2011) reported a case of a 7-day-old male neonate with CTX-induced near-fatal anaphylaxis. De Koning et al (De Koning et al, 1983) reported that one patient developed erythematous macular rash 2 days after treatment with CTX.…”

Section: Discussionmentioning

confidence: 99%

Tolerability, Safety, Pharmacokinetics and Drug Interaction of Cefotaxime Sodium–Tazobactam Sodium Injection (6:1) Following Single and Multiple Intravenous Doses in Chinese Healthy Subjects

Chen

Sun

Hu³

et al. 2020

Front. Pharmacol.

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Treatment of Uncomplicated Infections due to Neisseria gonorrhoeae

Rice¹

1986

JAMA

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Beta-lactams in sexually transmitted diseases: Rationale for selection and dosing regimens

Kunimoto

Brunham

Ronald

1984

Eur. J, Clin. Microbiol.

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A review is given of the selection and rational of optimal treatment regimens for patients with sexually transmitted pathogens, e.g. in cases of gonorrhea, chlamydial infections, chancroid, syphilis, pelvic inflammatory diseases and ophthalmia neonatorum. The scientific basis for the selection of a beta-lactam agent is discussed, including dose, MIC, the critical serum level and maintenance interval, and the duration of therapy. Except in the case of penicillinase-producing Neiserria gonorrhoeae, penicillin remained until recently the most effective agent available against many sexually transmitted diseases. However, ceftriaxone, a new third-generation cephalosporin, has been shown to have a long half-life (8 h) and excellent in vitro efficacy against Neiserria gonorrhoeae (including penicillinase-producing strains) and Haemophilis ducreyi. In view of its exceptional clinical efficacy against both gonorrhea and chancroid, clinical studies of its efficacy against other sexually transmitted diseases appear warranted.

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Single 1 g dose of cefotaxime in the treatment of infections due to penicillinase-producing strains of Neisseria gonorrhoeae.

Cited by 10 publications

References 7 publications

Tolerability, Safety, Pharmacokinetics and Drug Interaction of Cefotaxime Sodium–Tazobactam Sodium Injection (6:1) Following Single and Multiple Intravenous Doses in Chinese Healthy Subjects

Tolerability, Safety, Pharmacokinetics and Drug Interaction of Cefotaxime Sodium–Tazobactam Sodium Injection (6:1) Following Single and Multiple Intravenous Doses in Chinese Healthy Subjects

Treatment of Uncomplicated Infections due to Neisseria gonorrhoeae

Beta-lactams in sexually transmitted diseases: Rationale for selection and dosing regimens

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