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% — головокружение, headache, blurred vision, excitation, alarm, nervousness, tremor, insomnia; 1–3% — астения, paraesthesia, emotional lability (tearfulness), depersonalization, euphoria, disforija, depression, paranoia, blurred vision (diplopia, visual field defect); less 1% — нарушение концентрации внимания, 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% — сердцебиение; 1–3% — дилатация кожных сосудов, flushing.

From the digestive tract: 3–9% — сухость во рту, nausea, vomiting (11%).

Other: ataxia (10%), 3–9% — одышка, hyperventilation, pain at the injection site, Sweating; 1–3% — тромбофлебит, rash; после быстрого введения флумазенила — тревога, 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). В анестезиологии — в начальной дозе 0,2 mg for 15 from; при необходимости — по 0,1 mg after 60 с до суммарной дозы — 1 mg; обычная доза — 0,3–0,6 мг. В интенсивной терапии — в начальной дозе 0,3 mg; if necessary repeat injection every 60 с до суммарной дозы — 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 ч после аппликации флумазенила необходимо воздержаться от работы с потенциально опасными механизмами, 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.