フルマゼニル

Pharmaceuticals -> Listed in ZINC15

Pharmaceuticals -> Various

1.9

1.26

Breast Feeding; Lactation; Milk, Human; Antidotes; GABA Modulators; Benzodiazepines

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

201-203 °C

201 - 203 °C

164.31 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

165.6 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

165.8 Ų [M+H]+ [CCS Type: TW; Method: Major Mix IMS/Tof Calibration Kit (Waters)]

This chemical does not meet GHS hazard criteria for 20% (1 of 5) of reports.

Warning

H302 (80%): Harmful if swallowed [Warning Acute toxicity, oral]

P261, P264, P270, P271, P301+P317, P304+P340, P317, P330, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 5 reports by companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Induced Liver Injury Rank (DILIrank 2.0)

Flumazenil

vNo-DILI-concern

0

No match

DOI:10.1016/j.drudis.2016.02.015

V - Various

QV - Various

Flumazenil antagonizes the CNS effects produced by benzodiazepines, but does not antagonize the central nervous system effects of drugs affecting GABA-ergic neurons by means other than the benzodiazepine receptor (including ethanol, barbiturates, or general anesthetics) and does not reverse the effects of opioids.

Flumazenil, an imidazobenzodiazepine derivative, is a benzodiazepine antagonist. It competitively inhibits the benzodiazepine binding site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak partial agonist in some animal models of activity, but has little or no agonist activity in man.

Initial distribution half-life is 4 to 11 minutes and the terminal half-life is 40 to 80 minutes. Prolongation of the half-life to 1.3 hours in patients with moderate hepatic impairment and 2.4 hours in severely impaired patients. Compared to adults, the elimination half-life in pediatric patients was more variable, averaging 40 minutes (range: 20 to 75 minutes).

40P7XK9392

FLUMAZENIL

Established Pharmacologic Class [EPC] - Benzodiazepine Antagonist

Flumazenil is a Benzodiazepine Antagonist.

FLUMAZENIL

Benzodiazepine Antagonist [EPC]

Agents counteracting or neutralizing the action of POISONS.

Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here.

Flumazenil is completely (99%) metabolized. Elimination of radiolabeled drug is essentially complete within 72 hours, with 90% to 95% of the radioactivity appearing in urine and 5% to 10% in the feces.

0.9 to 1.1 L/kg

1 L/hr/kg [healthy volunteers receiving a 5-minute infusion of a total of 1 mg]