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Benzodiazepine antagonist

Aka: Benzodiazepine antagonist, Flumazenil, Romazicon
  1. Indication
    1. BenzodiazepineSedation reversal
  2. Contraindications
    1. Mixed drug overdose with compounds that can cause Seizure (e.g. Tricyclic Antidepressants, Cocaine)
    2. Chronic Benzodiazepine use (dependence)
    3. Seizure Disorder
  3. Dosing: Adults
    1. BenzodiazepineSedation Reversal
      1. Initial: 0.2 mg IV over 15 seconds
      2. Titrate: 0.2 mg each minute to 1 mg total
    2. Overdose Reversal
      1. Initial: 0.2 mg IV over 30 seconds
      2. Titrate: 0.3-0.5 mg q30 seconds to 3 mg total
    3. Repeat dosing protocol
      1. Repeat Dose: 0.005 mg/kg q1-2 minutes
      2. Maximum cumulative dose: 1 mg
      3. May repeat regimen every 20 minutes
  4. Dosing: Children
    1. Initial: 0.005 to 0.2 mg IV over 3-5 minutes, titrating to effect
  5. Precautions
    1. May cause acute withdrawal if physically dependent
    2. Do not give routinely to comatose patients
      1. Only use if identity of drug is known
    3. Reverses Seizure protection of Benzodiazepines
      1. Increases risk of drugs that lower Seizure threshold
        1. Cocaine
        2. Tricyclic Antidepressants
  6. Pharmacokinetics
    1. Onset: 1 to 2 minutes
    2. Peak: 6 to 10 minutes

Romazicon (C0591091)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D005442
English Anexate, Romazicon, Hoffman La Roche Brand of Flumazenil, Hoffman-La Roche Brand of Flumazenil, Lanexat, Roche Brand of Flumazenil
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Flumazenil (C0016293)

Definition (MSH) A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.
Definition (NCI) An imidazo-benzodiazepine derivative, effective in reversing benzodiazepine-induced activities. Flumazenil antagonizes the benzodiazepine binding site of the gamma-aminobutyric acid (GABA)/benzodiazepine receptor complex in the central nervous system (CNS), thereby preventing the chloride channel opening events and inhibiting neuronal hyperpolarization. As a result, flumazenil reverses benzodiazepine-induced effects including sedation, psychomotor deficits, amnesia, and hypoventilation in a dose-dependent manner.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D005442
SnomedCT 387575000, 96247007
English Flumazenil, Flumazepil, 4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, ethyl ester, 4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic Acid, 8-fluoro-5,6-dihydro-5-methyl-6-oxo-, Ethyl Ester, flumazenil, flumazepil, flumazenil (medication), FLUMAZENIL, Flumazenil [Chemical/Ingredient], Flumazenil (product), Flumazenil (substance)
Swedish Flumazenil
Czech flumazenil
Finnish Flumatseniili
Russian FLUMAZEPIL, FLUMAZENIL, RO 15-1788, ФЛУМАЗЕНИЛ, ФЛУМАЗЕПИЛ
Japanese フルマゼピル, アネキセート, フルマゼニル
Croatian FLUMAZENIL
Spanish flumazenil (producto), flumacenil (producto), flumacenil, flumacenil (sustancia), flumazenil (sustancia), flumazenil, Flumazenil, Flumazepil
Polish Ro 15-1788, Flumazepil, Flumazenil
French Flumazénil
German Flumazenil, Flumazepil
Italian Flumazenile
Portuguese Flumazenil, Flumazepil
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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