国家: 加拿大
语言: 英文
来源: Health Canada
FLUMAZENIL
SANDOZ CANADA INCORPORATED
V03AB25
FLUMAZENIL
0.1MG
SOLUTION
FLUMAZENIL 0.1MG
INTRAVENOUS
100
Ethical
MISCELLANEOUS CENTRAL NERVOUS SYSTEM AGENTS
Active ingredient group (AIG) number: 0122202001; AHFS:
CANCELLED PRE MARKET
2017-08-01
_Flumazenil Injection SDZ _ _ _ _Page 1 of 27 _ PRODUCT MONOGRAPH FLUMAZENIL INJECTION SDZ Flumazenil Injection, Manufacturer’s Standard 0.1 mg/mL THERAPEUTIC CLASSIFICATION BENZODIAZEPINE ANTAGONIST Sandoz Canada Inc. 145, Jules-Léger Date of Revision: July 4, 2012 Boucherville, QC, Canada J4B 7K8 Control No: 154070 _Flumazenil Injection SDZ _ _ _ _Page 2 of 27 _ FLUMAZENIL INJECTION SDZ Flumazenil Injection, Manufacturer’s Standard 0.1 mg/mL THERAPEUTIC CLASSIFICATION Benzodiazepine Antagonist ACTION AND CLINICAL PHARMACOLOGY Flumazenil Injection SDZ, an imidazobenzodiazepine, is a benzodiazepine antagonist which blocks the central effects of agents that act via the benzodiazepine receptor, by competitive inhibition. The antagonism is specific, since in animal experiments the effects of compounds which have no affinity for the benzodiazepine receptor (e.g. barbiturates, meprobamate, ethanol, GABA-mimetics, and adenosine receptor agonists) were not affected by flumazenil. Flumazenil does not reverse the central effects of opioids. Following the intravenous administration of radiolabelled flumazenil to human volunteers, the distribution of radioactivity corresponded closely to the distribution of benzodiazepine receptors as determined by positron emission tomography. The hypnotic-sedative effects of benzodiazepines are rapidly reversed by flumazenil. However, the residual effects may reappear gradually within a few hours, depending on the dose and plasma concentration of flumazenil, the time elapsed since the benzodiazepine agonist was given, and the dose and elimination half-life of the previously administered benzodiazepine agonist. Flumazenil has shown some weak intrinsic agonistic (e.g. anticonvulsant) activity without therapeutic relevance. PHARMACOKINETICS _ _ In young male volunteers, the pharmacokinetics of intravenous flumazenil were linear over a dose range of 2-100 mg. Increasing doses of flumazenil were accompanied by a corresponding increase in the area under the plasma concentration-time curve 阅读完整的文件