SYSTEMIC EFFECTS OF ADMIN CORTICOSTEROIDS SUCH AS...DEXAMETHASONE...MAY BE DIMINISHED BY LARGE DOSES OF BARBITURATES... FLUPREDNISOLONE...ALSO MAY BE EXPECTED TO INTERACT WITH PHENOBARBITAL, ALTHOUGH THERE HAVE BEEN NO REPORTS DOCUMENTING SUCH INTERATIONS.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
相互作用
苯妥英是一种已知能增加人类氢化可的松代谢的药物。它很可能会与泼尼松龙产生类似的相互作用。
PHENYTOIN IS...KNOWN TO INCR METAB OF HYDROCORTISONE...IN HUMANS. IT IS LIKELY THAT...FLUPREDNISOLONE...WOULD INTERACT SIMILARLY.
The effect of glucocorticoids on oral anticoagulant therapy is variable, and the efficacy of oral anticoagulants has been reported to be enhanced or diminished with concomitant glucocorticoid administration. Patients receiving glucocorticoids and oral anticoagulants concomitantly should be monitored (e.g., using coagulation indices) in order to maintain desired anticoagulant effect. /Corticosteroids/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
相互作用
因为皮质类固醇抑制抗体反应，这些药物可能会降低对类毒素和活疫苗或灭活疫苗的免疫应答。此外，皮质类固醇可能会增强活、减毒疫苗中某些微生物的复制，并且药物的超生理剂量可能会加剧对某些疫苗的神经反应。通常应推迟常规疫苗或类毒素的接种，直到皮质类固醇治疗停止。在接受免疫抑制剂量糖皮质激素治疗的患者中，接种活病毒或活、减毒疫苗，包括天花疫苗，是禁忌的。此外，如果给这类患者接种灭活疫苗，可能无法获得预期的血清抗体反应。美国公共卫生服务免疫实践咨询委员会（ACIP）和美国 Academy of Family Physicians (AAFP) 表示，在接受短期（小于2周）治疗、低到中等剂量的皮质类固醇治疗的患者中，接种活病毒疫苗通常不是禁忌的，长期交替日治疗使用短效制剂、维持生理剂量（替代疗法）或如果皮质类固醇通过局部、眼科、关节内、滑囊内或肌腱内给药。如果在接受皮质类固醇治疗的患者中需要免疫接种，可能需要进行血清学测试以确保足够的抗体反应，可能需要额外的疫苗或类毒素剂量。在接受非免疫抑制剂量糖皮质激素治疗的患者或在接受糖皮质激素作为替代疗法（例如，阿狄森病）的患者中，可以进行免疫接种程序。/皮质类固醇/
Because corticosteroids inhibit antibody response, the drugs may cause a diminished response to toxoids and live or inactivated vaccines. In addition, corticosteroids may potentiate replication of some organisms contained in live, attenuated vaccines and supraphysiologic dosages of the drugs can aggravate neurologic reactions to some vaccines. Routine administration of vaccines or toxoids should generally be deferred until corticosteroid therapy is discontinued. Administration of live virus or live, attenuated vaccines, including smallpox vaccine, is contraindicated in patients receiving immunosuppressive dosages of glucocorticoids. In addition, if inactivated vaccines are administered to such patients, expected serum antibody response may not be obtained. The Public Health Service Advisory Committee on Immunization Practices (ACIP) and American Academy of Family Physicians (AAFP) state that administration of live virus vaccines usually is not contraindicated in patients receiving corticosteroid therapy as short-term (less than 2 weeks) treatment, in low to moderate dosages, as long-term alternate-day treatment with short-acting preparations, in maintenance physiologic dosages (replacement therapy), or if corticosteroids are administered topically, ophthalmically, intra-articularly, bursally, or into a tendon. If immunization is necessary in a patient receiving corticosteroid therapy, serologic testing may be needed to ensure adequate antibody response and additional doses of the vaccine or toxoid may be necessary. Immunization procedures may be undertaken in patients receiving nonimmunosuppressive doses of glucocorticoids or in patients receiving glucocorticoids as replacement therapy (e.g., Addison's disease). /Corticosteroids/
/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
获得了氟泼尼松龙溶液相和非溶液相的溶解速率与大鼠体内植入小粒的溶解速率之间的极好相关性。
EXCELLENT CORRELATIONS WERE OBTAINED BETWEEN DISSOLUTION RATES OF SOLVATED & NON-SOLVATED PHASES OF FLUPREDNISOLONE & IN VIVO DISSOLUTION RATES OF PELLET IMPLANTS IN RATS.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
在肝脏中大部分结合，但在肾脏中也存在 /人类，口服/。
CONJUGATED MOSTLY IN LIVER BUT ALSO IN KIDNEY /HUMAN, ORAL/.
Synthesis and Structure-Activity Relationships in a Series of Antiinflammatory Corticosteroid Analogs, Halomethyl Androstane-17.beta.-carbothioates and -17.beta.-carboselenoates
摘要：
The preparation and topical antiinflammatory potencies of a series of halomethyl 17 alpha-(acyloxy)11 beta-hydroxy-3 -oxoandrosta-1,4-diene-17 beta-carbothioates, carrying combinations of 6 alpha-fluoro, 9 alpha-fluoro, 16-methyl, and 16-methylene substituents, are described. Key synthetic stages were the preparation of carbothioic acids and their reaction with dihalomethanes. The carbothioic acids were formed from 17 beta-carboxylic acids by initial reaction with dimethylthiocarbamoyl chloride followed by aminolysis of the resulting rearranged mixed anhydride with diethylamine, or by carboxyl activation with 1,1'-carbonyldiimidazole (CDI) or 2-fluoro-N-methylpyridinium tosylate (FMPT) and reaction with hydrogen sulfide, the choice of reagent being governed by the 17 alpha-substituent. Carboxyl activation with FMPT and reaction with sodium hydrogen selenide led to the halomethyl 16-methyleneandrostane-17 beta-carboselenoat analogues. Antiinflammatory potencies were measured in humans using the vasoconstriction assay and in rats and mice by a modification the Tonelli croton oil ear assay. Best activities were shown by fluoromethyl and chloromethyl carbothioates with a 17 alpha-propionyloxy group. S-Fluoromethyl 6(alpha,9 alpha-difluoro-11 beta-hydroxy-16 alpha-methyl-3-oxo-17 alpha-(propionyloxy)androsta-1,4-diene-17 beta-carbothioate (fluticasone propionate, FP) was selected for clinical study as it showed high topical antiinflammatory activity but caused little hypothalamic-pituitary-adrenal suppression after topical or oral administration to rodents.
[EN] COMPOUNDS THAT INHIBIT MCL-1 PROTEIN<br/>[FR] COMPOSÉS INHIBANT LA PROTÉINE MCL-1
申请人：AMGEN INC
公开号：WO2018183418A1
公开（公告）日：2018-10-04
Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (I), or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
[EN] DIPEPTIDE AND TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS<br/>[FR] INHIBITEURS DE DIPEPTIDE ET DE TRIPEPTIDE ÉPOXY CÉTONE PROTÉASES
申请人：ONYX THERAPEUTICS INC
公开号：WO2014152127A1
公开（公告）日：2014-09-25
Provided herein are dipeptide and tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of proliferative diseases including cancer and autoimmune diseases.
CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY
申请人：Cerulean Pharma Inc.
公开号：US20130196906A1
公开（公告）日：2013-08-01
Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of a disease or disorder, e.g., autoimmune disease, inflammatory disease, central nervous system disorder, cardiovascular disease, or metabolic disorder. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.
The present disclosure is directed to modulators of SOS1 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
本公开涉及SOS1的调节剂及其在治疗疾病中的应用。还公开了包含相同成分的药物组合物。
[EN] ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS<br/>[FR] ANTI-INFECTIEUX A BASE D'ISOTHIAZOLOQUINOLONES ET DE SELS CORRESPONDANTS
申请人：ACHILLION PHARMACEUTICALS INC
公开号：WO2005019228A1
公开（公告）日：2005-03-03
The invention provides compounds and salts of Formula (I) and Formula (II): which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of a compound of Formula (I) or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
