NON-IONIC, ANIONIC, & ZWITTERIONIC SURFACTANTS INDUCED RAPIDLY REVERSIBLE HYPER-ABSORPTIVE STATE IN THOMAS CANINE FUNDIC POUCH FOR CEPHALORIDINE...BLOOD LEVELS...MANY TIMES GREATER THAN VALUES IN CONTROLS.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
相互作用
CEPHALORIDINE SEEMS TO HAVE GREATEST POTENTIAL FOR NEPHROTOXICITY.../IT SHOULD NOT/ BE USED WITH GENTAMICIN /OR OTHER AMINOGLYCOSIDES, AMIKACIN, NEOMYCIN, PAROMOMYCIN & TOBRAMYCIN/ UNLESS LIFE-THREATENING CONDITION EXISTS /MAY INCR NEPHROTOXICITY/.
cefaloridine(头孢洛宁)具有最大的肾毒性潜力.../不应该/与庆大霉素/或其他氨基糖苷类药物，阿米卡星，新霉素，巴龙霉素和妥布霉素/除非存在生命威胁的情况/可能会增加肾毒性。
CEPHALORIDINE SEEMS TO HAVE GREATEST POTENTIAL FOR NEPHROTOXICITY.../IT SHOULD NOT/ BE USED WITH GENTAMICIN /OR OTHER AMINOGLYCOSIDES, AMIKACIN, NEOMYCIN, PAROMOMYCIN & TOBRAMYCIN/ UNLESS LIFE-THREATENING CONDITION EXISTS /MAY INCR NEPHROTOXICITY/.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
相互作用
头孢拉定肾毒性会因同时使用呋塞米而增强。在患有轻度预先存在的肾病的患者中，应避免这种治疗方法。
CEPHALORIDINE NEPHROTOXICITY IS ENHANCED BY CONCURRENT FUROSEMIDE ADMIN. SUCH THERAPY SHOULD BE AVOIDED IN PATIENTS WHO HAVE EVEN MILD PREEXISTING RENAL DISEASE.
...CEPHALOSPORINS...MAY BE AFFECTED BY CONCURRENT USE OF PROBENECID OR SULFINPYRAZONE. DIMINISHED TUBULAR SECRETION OF...WEAK ACIDS COULD RESULT IN HIGHER & MORE SUSTAINED SERUM LEVELS & HENCE, INTENSIFICATION OF DRUG ACTIVITY. /CEPHALOSPORINS/
Groups of ten male rats were treated with a high challenge dose of cephaloridine (3750 mg/kg), with methylprednisolone (100 mg/kg) or with cephaloridine and methylprednisolone by single sc injection. A control group received the injection vehicles only. Urine was collected from all animals daily over 18-hr collection periods, up to 96 hr after treatment. Blood was collected at 24, 48, 72 and 96 hr after treatment. At necropsy, kidneys were weighed, processed and examined histopathologically. Results show that methylprednisolone significantly ameliorated the nephrotoxicity of the challenge dose of cephaloridine. Cephaloridine-only treated rats had severe toxic nephrosis characterized by acute tubular necrosis, and elevated blood urea and creatinine. by contrast, the majority of cephaloridine plus methylprednisolone treated rats had only a slight or moderate toxic nephrosis, and had lower blood urea and creatinine levels compared with rats treated with cephaloridine only, indicating preservation of kidney function. Interestingly, rats treated with cephaloridine and methylprednisolone had higher urinary enzymes ... as well as protein and glucose, compared with rats treated with cephaloridine only. this is taken to indicate that rats treated with cephaloridine only had such marked kidney damage and necrosis that the population of cells able to produce these marker enzymes was significantly and rapidly depleted, but the protection afforded by methylprednisolone allowed cephaloridine plus methylprednisolone treated rats to sustain urinary enzyme output. Effects on urinary glucose and other parameters ... demonstrate interactions between glucocorticoid pharmacology and cephaloridine nephrotoxicity.
.../CEPHALORIDINE/ POORLY ABSORBED FROM GI TRACT. PEAK PLASMA CONCN ARE REACHED ABOUT 30 MIN AFTER DRUG IS INJECTED; 10 TO 20% OF PLASMA CEPHALORIDINE IS BOUND TO PROTEIN.
IM INJECTIONS OF 0.5 & 1 G YIELD PEAK PLASMA CONCN OF 15 & 30 UG/ML, RESPECTIVELY. APPROX 75% OF GIVEN DOSE IS EXCRETED IN URINE, MAINLY BY GLOMERULAR FILTRATION. CEPHALORIDINE ACCUM IN BLOOD OF PATIENTS WITH DECR RENAL FUNCTION, & IN AZOTEMIC PATIENTS PLASMA CONCN ARE VERY HIGH...
[EN] DERIVATIVES OF AMANITA TOXINS AND THEIR CONJUGATION TO A CELL BINDING MOLECULE<br/>[FR] DÉRIVÉS DE TOXINES D'AMANITES ET LEUR CONJUGAISON À UNE MOLÉCULE DE LIAISON CELLULAIRE
申请人：HANGZHOU DAC BIOTECH CO LTD
公开号：WO2017046658A1
公开（公告）日：2017-03-23
Derivatives of Amernita toxins of Formula (I), wherein, formula (a) R 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9, R 10, X, L, m, n and Q are defined herein. The preparation of the derivatives. The therapeutic use of the derivatives in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.
[EN] A CONJUGATE OF A CYTOTOXIC AGENT TO A CELL BINDING MOLECULE WITH BRANCHED LINKERS<br/>[FR] CONJUGUÉ D'UN AGENT CYTOTOXIQUE À UNE MOLÉCULE DE LIAISON CELLULAIRE AVEC DES LIEURS RAMIFIÉS
申请人：HANGZHOU DAC BIOTECH CO LTD
公开号：WO2020257998A1
公开（公告）日：2020-12-30
Provided is a conjugation of cytotoxic drug to a cell-binding molecule with a side-chain linker. It provides side-chain linkage methods of making a conjugate of a cytotoxic molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and immunological disorders.
[EN] CROSS-LINKED PYRROLOBENZODIAZEPINE DIMER (PBD) DERIVATIVE AND ITS CONJUGATES<br/>[FR] DÉRIVÉ DE DIMÈRE DE PYRROLOBENZODIAZÉPINE RÉTICULÉ (PBD) ET SES CONJUGUÉS
申请人：HANGZHOU DAC BIOTECH CO LTD
公开号：WO2020006722A1
公开（公告）日：2020-01-09
A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.
The present application provides compounds of formula: Methods of using these compounds for killing bacterial growth and treating bacterial infections are also provided.
本申请提供了以下化合物的公式：还提供了使用这些化合物杀灭细菌生长和治疗细菌感染的方法。
METALLO-BETA-LACTAMASE INHIBITORS
申请人：Merck Sharp & Dohme Corp.
公开号：US20160333021A1
公开（公告）日：2016-11-17
The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
