Flumazenil
When ATH:
V03AB25
Characteristic.
White or almost white crystalline powder, insoluble in water and slightly soluble in acidic aqueous solutions. Molecular weight 303,3.
Pharmacological action.
Blocking benzodiazepine receptors.
Application.
Eliminating the central effects of benzodiazepines, incl. during injection of the anesthesia, differential diagnosis with loss of consciousness of unknown aetiology (statement or exclusion of the diagnosis of benzodiazepine poisoning).
Contraindications.
Hypersensitivity, cyclic antidepressant poisoning. Contraindicated in patients, receiving benzodiazepines for the treatment of conditions, potentially life-threatening (such as intracranial hypertension, or status epilepticus).
Pregnancy and breast-feeding.
Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)
Side effects.
From the nervous system and sensory organs: 3–9% - dizziness, headache, blurred vision, excitation, alarm, nervousness, tremor, insomnia; 1-3% - asthenia, paraesthesia, emotional lability (tearfulness), depersonalization, euphoria, disforija, depression, paranoia, blurred vision (diplopia, visual field defect); less 1% - Violation of concentration, delirium, convulsions, drowsiness, transient hearing loss, hyperacusis, noise in ears; described cases of seizures in patients, epilepsy or severe liver disease (especially after long-term treatment with benzodiazepines or in the case of mixed drug overdose); there are reports, that patients with a history of panic disorder administration of flumazenil may trigger a panic attack.
Cardio-vascular system and blood (hematopoiesis, hemostasis): 3–9% - heartbeat; 1–3% - dilatation of skin vessels, flushing.
From the digestive tract: 3–9% - dry mouth, nausea, vomiting (11%).
Other: ataxia (10%), 3–9% - shortness of breath, hyperventilation, pain at the injection site, Sweating; 1–3% - thrombophlebitis, rash; After the rapid administration of flumazenil - anxiety, heartbeat, a sense of fear.
Cooperation.
Reduces the effects of zopiclone, triazolpiridazinov, benzodiazepines.
Dosing and Administration.
B / (pre-diluted 5% glucose solution or 0,9% sodium chloride solution). In anesthesiology - in the initial dose 0,2 mg for 15 from; if necessary - by 0,1 mg after 60 C to a total dose - 1 mg; The usual dose is 0.3-0.6 mg. In intensive care - in the initial dose 0,3 mg; if necessary repeat injection every 60 C to a total dose - 2 mg.
Precautions.
Should not be used in violation of the autonomic nervous and cardiovascular system during heavy poisoning three- and tetracyclic antidepressants. Not recommended for patients with epilepsy, receiving long-term benzodiazepines (possible provocation seizures). During 24 h after the application of flumazenil, it is necessary to refrain from working with potentially dangerous mechanisms, driving and other activities, requiring greater attention. When anesthesia should not be administered to complete the expiration of peripheral muscle relaxants. It will be appreciated, In patients with severe brain injuries (or unstable intracranial pressure) may develop increased intracranial pressure.
