A clinical study of penetration of biapenem into pleural fluid

• Published in: CHEMOTHERAPY Vol. 42; no. Supplement4; pp. 285 - 289
• Main Authors: Kimura Makoto, Matsushima Toshiharu, Tano Yoshihiko, Adachi Michifumi, Kobashi Yoshihiro, Nakamura Junichi
• Format: Journal Article
• Language: English
• Published: Japanese Society of Chemotherapy 1994; 公益社団法人 日本化学療法学会
• Subjects: Biapenem; 胸水中移行; 胸水貯留
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.42.supplement4_285

The penetration of biapenem (BIPM)(a new carbapenem) was studied with regard to its levels in pleural fluid and serum in patients with pleural effusion.The subjects of this study were four patients with pleural effusion (carcinomatous pleurisy 3, pleural effusion of unknown cause 1). 300mg of BIPM was administered by drip infusion over one hour.Then the levels of BIPM in pleural fluid and serum were measured by a method of bioassay.The peak levels of pleural fluid for four cases were from 4.4 to 10.8μg/ml between 30 minutes and one hour after drip infusion. The mean peak level was 8.0±3.2μg/ml after 30 minutes d.i.v. The peak levels of serum for four cases were between 15.7 and 23.1μg/ml immediately after drip infusion.The mean peak level of serum was 18.7±3.3μg/ml.The AUC (area under curve) of pleural fluid was 35.5μg·Ehr/ml (24.1-42.0), and that of serum was 34.6μg·Ehr/ml (27.5-1.1). The mean T1/2 of pleural fluid was 3.2 hours (2.6-5.7), while that of serum was 1.5 hours (1.1-2.0). Based on the above results, the pleural fluid/serum ratio of Cmax and AUC of BIPM were determined to be 42.8% and 103%, respectively. This study revealed that the penetration of BIPM into pleural fluid was excellent among β-lactam agents. 新しいカルバペネム系抗菌薬biapenem (BIPM) を胸水貯留患者に投与後, 胸水中および血清濃度を測定し, BIPMの胸水中移行に関する検討を行った。対象症例は, 癌性胸膜炎3, 原因不明の胸水貯留1の計4例で, BIPM300mgを1時間で点滴静注し, 以後経時的に胸水および血液を採取し, 遠心分離後BIPMの濃度をBioassay法で測定した。胸水中濃度のピークは点滴終了の30分から1時間後に見られ, 平均値のピークは30分後の8.0±3.2μg/ml (4.4～10.1) であった。血清濃度のピークは, 4症例ともに点滴終了直後にみられ, 平均18.7±3.3μg/ml (15, 7～23.1) であった。胸水中および血清濃度の平均値によるAUCはそれぞれ35.5μg・hr/ml (24.1～42.0), 34.6μg・hr/ml (27.5～41.1) で, 胸水中および血清濃度の平均値によるT1/2はそれぞれ3.2時間 (2.4～5.7), 1.5時間 (1.1～2.0) であった。従って, Cmax pleural fluid/serum (P/S) は42.8%, AUCP/Sは103%となり, 他のβ-ラクタム系薬に比較し, 優れた胸水移行が示された。