Author: Yumiko Shinohara ; Atsushi Sakai ; Kihachiro Shimizu ; Taisuke Sugihara ; Hiroko Tokuoka ; Yuji Michisuji ; Akihiro Kubo ; Shinya Yamaji ; Nobuhiro Mori ; Kyoichi Totsuka

The effect of pretreatment with ranitidine, an antacid, on the absorption of AS-924, a novel prodrug-type cephem antibiotic derived from ceftizoxime (CTIZ), was examined in eight healthy adult male volunteers by the cross-over method, using cefteram-pivoxil (CTER-PI) as the control drug. The C(max) and area under the concentration (AUC) values and cumulative urinary excretion rate (0-24 h) of cefteram (CTER) after administration of CTER-PI decreased by 32, 38 and 37%, respectively, in the ranitidine pretreatment group whereas those of AS-924 were not affected by the antacid. The urinary levels of pivaloyl-carnitine determined to evaluate the solubility of these antibiotics in the gastrointestinal tract suggested that this was not affected by ranitidine. These results indicate that the absorption of CTER-PI was affected by pretreatment with ranitidine largely due to inactivation of this antibiotic in the gastrointestinal tract at high pH rather than to a decrease in solubility. In contrast, isomerization of AS-924 was hardly induced by the elevation of pH, thus demonstrating that AS-924 was less likely to be affected by pretreatment with antacids.

01 Nov 2001·International Journal of Antimicrobial AgentsQ2 · MEDICINE

Pharmacokinetics of cefcapene pivoxil and AS-924 in gastrectomized patients

Q2 · MEDICINE

Article

Author: Fujimoto, M

To investigate the effects of gastrectomy on the absorption of drugs, the blood concentrations of the active moieties, cefcapene (CCAP) and ceftizoxime (CTIZ), were determined in 36 gastrectomized patients after oral administration of cefcapene pivoxil (CCAP-PI) and AS-924, prodrug type cephem antibiotics with different solubility-profiles. In patients with gastrectomy, the C(max) and AUC for CCAP-PI whose solubility depended on the acidity of gastric juice, were lower than in the controls; whereas those for AS-924 were comparable with values in the control group. The T(max) was affected by the extent of gastrectomy; the T(max) value was the lowest in patients who had undergone total gastrectomy Roux-Y, followed by Billroth II and Billroth I procedure of subtotal gastrectomy. These results indicate the need to select drugs and to instruct gastrectomized patients regarding dosage and administration, taking the pharmacokinetics of drugs into consideration.

01 Nov 2001·International Journal of Antimicrobial AgentsQ2 · MEDICINE

Effects of gastrointestinal stimulant and suppressant pretreatment on the pharmacokinetics of AS-924, a novel ester-type cephem antibiotic

Q2 · MEDICINE

Article

Author: Kazuo Yano ; Atsushi Sakai ; Taisuke Sugihara ; Jingoro Shimada ; Akira Yanagawa ; Takashi Kitamura ; Shinya Yamaji ; Nobuhiro Mori ; Tetsushi Kano

The effects of pretreatment with the gastrointestinal stimulant domperidone and the suppressant scopolamine butylbromide on the absorption of AS-924, a novel prodrug-type cephem antibiotic, were investigated in six healthy adult male volunteers by a cross-over method. The T(max) of ceftizoxime (CTIZ), the active moiety of AS-924, was slightly prolonged by scopolamine butylbromide (T(max)=1.8 vs. 1.5 h for the group without pretreatment). However, there were no significant differences in pharmacokinetic parameters including T(max), cumulative urinary excretion rates of CTIZ and cumulative urinary excretion rates of pivaloylcarnitine for 12 h after the dosing between the pretreated and control groups. Domperidone did not affect the absorption of AS-924.

100 Deals associated with Ceftizoxime alapivoxil

External Link

KEGG	Wiki	ATC	Drug Bank
D09793	Ceftizoxime alapivoxil	-	-

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	NDA/BLA	JP	Asahi Kasei Corp.	-
Bacterial Infections	NDA/BLA	-	Kyoto Pharmaceutical Industries Ltd.	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis