User:Mr. Ibrahem/Flumazenil

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Mr. Ibrahem/Flumazenil
Clinical data
Trade namesAnexate, Lanexat, Mazicon, Romazicon
Other namesFlumazepil, Ro 15-1788, ethyl 8-fluoro- 5,6-dihydro- 5-methyl- 6-oxo- 4H- imidazo [1,5-a] [1,4] benzodiazepine- 3-carboxylate
AHFS/Drugs.comMonograph
Pregnancy
category
  • AU: B3
Routes of
administration
IV
Legal status
Legal status
  • AU: S4 (Prescription only)
  • CA: ℞-only
  • UK: POM (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
MetabolismLiver
Onset of actionWithin 2 min[1]
Elimination half-life7–15 min (initial)
20–30 min (brain)
40–80 min (terminal)
Duration of action40 to 90 min[2]
ExcretionUrine 90–95%
Feces 5–10%
Identifiers
  • Ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate
Chemical and physical data
FormulaC15H14FN3O3
Molar mass303.293 g·mol−1
3D model (JSmol)
  • Fc(c1)ccc-2c1C(=O)N(C)Cc3n2cnc3C(=O)OCC
  • InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3 checkY
  • Key:OFBIFZUFASYYRE-UHFFFAOYSA-N checkY
  (verify)

Flumazenil, sold under the brand name Anexate, is a medication used to reverse the effects of benzodiazepines.[3] Routine use is not recommended in those with a decreased level of consciousness.[4] It is given by injection into a vein.[3] Effects begin within 2 minutes and may last for up to 90 minutes.[1][2]

Common side effects include sweating, blurry vision, headache, and dizziness.[1] Other side effects may include seizures and benzodiazepine withdrawal, especially in people with benzodiazepine dependence.[1] Panic attacks may also occur.[1] Safety in pregnancy is unclear.[5] It works by blocking benzodiazepines at the GABA receptor.[1]

Flumazenil was characterized in 1981, and approved for medical use in the United States in 1991.[6][1] It is available as a generic medication.[3] In the United Kingdom 0.5 mg cost the NHS about £13 as of 2021.[3] This amount in the United States is about 10 USD.[7]

References[edit]

  1. ^ a b c d e f g h "Flumazenil Monograph for Professionals". Drugs.com. Archived from the original on 30 September 2020. Retrieved 11 December 2021.
  2. ^ a b c Wilson, William C.; Grande, Christopher M.; Hoyt, David B. (5 February 2007). Trauma: Critical Care. CRC Press. p. 85. ISBN 978-1-4200-1684-0. Archived from the original on 11 December 2021. Retrieved 11 December 2021.
  3. ^ a b c d e BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1422. ISBN 978-0857114105.
  4. ^ Wood, Lawrence D. H.; Hall, Jesse B.; Schmidt, Gregory D. 1952 (2005). Principles of critical care. McGraw-Hill Professional. ISBN 978-0-07-141640-5. Archived from the original on 2020-12-16. Retrieved 2021-06-07.{{cite book}}: CS1 maint: numeric names: authors list (link)
  5. ^ "Flumazenil (Romazicon) Use During Pregnancy". Drugs.com. Archived from the original on 3 December 2020. Retrieved 11 December 2021.
  6. ^ Whitwam, James. G. (1988). "Flumazenil: a benzodiazepine antagonist". BMJ. 297 (6655): 999–1000. doi:10.1136/bmj.297.6655.999. PMC 1834756. PMID 2903780.
  7. ^ "Flumazenil Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 22 January 2021. Retrieved 11 December 2021.