Chemical formula: C₁₅H₁₄FN₃O₃ Molecular mass: 303.288 g/mol PubChem compound: 3373
Flumazenil interacts in the following cases:
Since flumazenil is primarily metabolised in the liver, careful titration of dosage is recommended in patients with impaired hepatic function.
Flumazenil reverses the central effects of benzodiazepines by means of competitive interaction at receptor level: the effects of non-benzodiazepine agonists acting via the benzodiazepine receptor, such as zopiclone, triazolopyridazine and others, are also antagonised by flumazenil. However, flumazenil does not block the effect of medicines that do not operate via this route. Interaction with other central nervous system depressants has not been observed. Particular caution is necessary when using flumazenil in cases of accidental overdose since the toxic effects of other psychotropic medicinal products (especially tricyclic antidepressants) taken concurrently may increase with the subsidence of the benzodiazepine effect.
In patients with severe brain injury (and/or instable intracranial pressure) receiving flumazenil – to reverse the effects of benzodiazepines – an increased intracranial pressure may develop.
The use of the antagonist is not recommended in patients with epilepsy, who have been treated with benzodiazepines for a prolonged period of time. Although flumazenil has some intrinsic anti-epileptic effects, the abrupt antagonising effect can cause convulsions in patients with epilepsy.
Emergency use of flumazenil during pregnancy is not contraindicated.
Flumazenil should only be used during pregnancy if the possible benefit to the patient outweighs the potential risks for the foetus.
Emergency use of flumazenil during lactation is not contraindicated.
It is not known whether flumazenil is excreted in human milk. For this reason, breast-feeding should be interrupted for 24 hours when flumazenil is used during lactation.
Although studies in animals have not shown evidence of embryo toxicity or teratogenicity, the possible risk to humans caused by flumazenil during pregnancy has not been determined.
Patients who have received flumazenil to reverse the effects of benzodiazepine sedation should be warned not to drive, to operate machinery or to engage in other activities demanding physical or mental exertion for at least 24 hours, since the effect of the benzodiazepine may return.
Any side-effects associated with Flumazenil usually subside rapidly without the need for special treatment.
Frequency categories are defined using the following convention:
Very common: ≥1/10
Common: ≥1/100 to <1/10
Uncommon: ≥1/1,000 to <1/100
Rare: ≥1/10, 000 to <1/1,000
Very rare: <1/10, 000
Not known (cannot be estimated from the available data)
The adverse events listed below have been reported.
Common: Allergic reactions
Rare: Severe hypersensitivity reactions (including anaphylaxis)
Common: Anxiety*, emotional lability, insomnia, somnolence
Uncommon: Fear
Unknown: Withdrawal symptoms, (e.g. agitation, anxiety, emotional lability, confusion, sensory distortions, tachycardia, dizziness, sweating), following rapid injection of doses of 1000 micrograms or more in patients with high-dose and/or long-term exposure to benzodiazepines ending at any time within the weeks preceding flumazenil administration; panic attacks (in patients with a history of panic reactions); abnormal crying, agitation, aggressive reactions (the side effect profile in children is generally similar to that in adults. When Flumazenil has been used for the reversal of conscious sedation, abnormal crying, agitation and aggressive reactions have been reported).
Common: Vertigo, headache, agitation*, tremor, dry mouth, hyperventilation, speech disorder, paraesthesia
Uncommon: Convulsions (in patients suffering epilepsy or severe hepatic insufficiency, mainly after long-term treatment with benzodiazepines or multiple medicinal products abuse).
Common: Diplopia, strabismus, lacrimation increased
Uncommon: Abnormal hearing
Common: Palpitations*
Uncommon: Tachycardia or bradycardia, extrasystole
Common: Flushing, hypotension, orthostatic hypotension, transient increased blood pressure (on awakening)
Uncommon: Dyspnoea, cough, nasal congestion, chest pain
Very common: Nausea (during anaesthesia)
Common: Vomiting (during anaesthesia), hiccup
Common: Sweating
Common: Injection site pain
Uncommon: Shivering
Rare: Severe hypersensitivity reactions (including anaphylaxis)
*: following rapid injection, generally did not require treatment
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