Flumazenil
Mechanism :
Flumazenil is a benzodiazepine receptor antagonist. Flumazenil antagonizes the actions of benzodiazepines on the central nervous system. Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex.
Indication :
Contraindications :
Contra-indicated in patients in patients with a known hypersensitivity to flumazenil or benzodiazepines, in patients who have been given a benzodiazepine for control of a life-threatening condition, and in patients who are showing signs of serious cyclic antidepressant overdose.
Dosing :
0.01 mg/kg given once intravenously over 15 seconds.
Adverse Effect :
Dizziness, increased sweating, headache, injection site pain, and abnormal or blurred vision. Others: cutaneous vasodilation, flushing, sweating, hot flushes, abnormal vision, diplopia, paresthesia, visual field defect, abnormal sensation, hypoesthesia, nausea, vomiting, headache, fatigue, agitation, nervousness, anxiety, tremor, palpitations, dry mouth, insomnia, dyspnea, dizziness, hyperventilation, emotional lability
Interaction :
Benzodiazepine: Flumazenil is not recommended in epileptic patients who have been receiving benzodiazepine treatment for a prolonged period.
Zopiclone, Triazolo Pyridazines and others: The effects of nonbenzodiazepine agonists at benzodiazepine receptors, such as zopiclone, triazolo pyridazines and others, are also blocked by flumazenil.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unknown dialysability. Dose as in normal renal function |
| HD | Unknown dialysability. Dose as in normal renal function |
| HDF/High flux | Unknown dialysability. Dose as in normal renal function |
| CAV/VVHD | Unknown dialysability. Dose as in normal renal function |
Hepatic Dose :
Since flumazenil is primarily metabolized in the liver, careful titration of dosage is recommended in patients with impaired hepatic function. Initial dose may not be adjusted. However, subsequent doses should be reduced in size or frequency.