Bromazepam - Active Substances. Instruction and Application, Dosage

Name: Bromazepam

The Latin name of the substance Bromazepam

Bromazepamum (genus Bromazepami)

Chemical name: 7-Bromo-1,3-dihydro-5- (2-pyridinyl) -2H-1,4-benzodiazepin-2-one

Formula - C14H10BrN3O

Therapeutic substances Bromazepam - anxiolytics

The nosological classification (ICD-10)

F20 Schizophrenia
F39 Upset Mood [affective] unspecified
F41 Other anxiety disorders
R45.1 Restlessness and agitation

CAS code - 1812-30-2

Characteristics substance Bromazepam

Anxiolytic, benzodiazepine derivative.

Pharmacology of Bromazepam

Mode of action - anxiolytic, sedative.

It stimulates GABA receptors ascending activating reticular formation. It increases the braking effect of GABA in the central nervous system, enhances the effects of endogenous GABA, reduces the excitability of the cortex and the limbic system of the brain, slows polysynaptic spinal reflexes. Reduces tension and anxiety in large doses have a sedative and central muscle relaxant effect. It reduces emotional tension, anxiety, fear, anxiety, reduces the neurotic symptoms.

After ingestion blood Cmax is reached within 2 hours. The bioavailability of the tablet form is 60%. Linking blood protein is 70%. The volume of distribution - 50 liters. In repeated dose equilibrium concentration in the blood is normally achieved within 2-3 days. Treated microsomal oxidation (N-dealkylation, aliphatic hydroxylation) to form a 3-gidroksibromazepama and 2- (2-amino-5-bromo-3-hydroxybenzoyl) pyridine, and their glucuronides. T1 / 2 - 20 hours may be increased in elderly patients. Write mainly in the urine as conjugated metabolites (2% unchanged). Clearance of the drug is 40 ml / min. Accumulation at the re-appointment of the minimum.

Application of the Bromazepam substance

Alarm syndrome, including state of anxiety and tension, somatic complaints; anxiety and excitement in mental illness, including in affective disorders, schizophrenia (in combination therapy).

Contraindications of Bromazepam

Hypersensitivity (including to other benzodiazepines), cerebral and spinal ataxia, suicidal tendencies, angle-closure glaucoma; hypercapnia; severe respiratory distress, apnea during sleep; liver failure; myasthenia gravis; drug or alcohol (except for acute withdrawal) dependence, pregnancy, breast-feeding.

Restrictions to application

Age 18 years (safety and efficacy of the children are not identified).

Pregnancy and breast-feeding
Contraindicated during pregnancy. At the time of treatment should stop breastfeeding.

Side effects of Bromazepam substance 

From the nervous system and sensory organs: headache, dizziness, weakness, fatigue, drowsiness, mental retardation and motor responses, blunting of emotions, impaired concentration, ataxia, tremors, muscle weakness, diplopia, dysarthria, confusion, anterograde amnesia (with concomitant inappropriate behavior), a manifestation of latent depression, paradoxical reactions (restlessness, agitation, anxiety, irritability, aggressiveness, delusions, rage, sleep disturbances, nightmares, hallucinations, psychosis, inappropriate behavior).

From the digestive tract: nausea, dry mouth, excessive salivation, constipation, increased activity of hepatic transaminases and alkaline phosphatase, jaundice.

Other: urinary incontinence, skin rash, changes in libido.

Perhaps the development of drug dependence, withdrawal syndrome, rebound-a syndrome

Interaction of Bromazepam

Effect increase neuroleptics al. Anxiolytics, tricyclic antidepressants, hypnotics, sedatives and anticonvulsants, narcotic analgesics, anesthetics, antihypertensives, muscle relaxants, antihistamines with sedative properties alcohol. Carbamazepine, cimetidine, inhibitors of microsomal enzymes increase the T1 / 2. Reduces the therapeutic effect of levodopa. Increases toxicity of zidovudine.

Overdose of Bromazepam

Symptoms: oppression CNS varying degrees of symptoms (from somnolence to coma), in mild cases - drowsiness, confusion, lethargy; in more serious cases (especially in patients receiving other drugs which depress the central nervous system, including alcohol) - ataxia, areflexia, hypotension, respiratory depression and cardiac (up to respiratory arrest) activity, coma; rarely - death.

Treatment: gastric lavage, induction of vomiting, the appointment of activated carbon, respiration monitors, heart rate, blood pressure, maintain cardiovascular activity, and airway management, in / in a liquid. In the event of hypotension - in / in the introduction of dopamine, norepinephrine. As a specific antidote used BZ antagonist flumazenil receptors (in the hospital).

Dosing and Administration of Bromazepam

Inside. The mode set is strictly individual, the average dose for adults in outpatient treatment: at 1.5-3 mg 2-3 times a day; if necessary (in the hospital) increase the dose to 6-12 mg 2-3 times a day. Children older than 1 year (if applicable) the dose selected individually depending on body weight. Patients are elderly, debilitated patients, and patients with impaired liver function should be prescribed lower doses. The total duration of treatment - no more than 8-12 weeks, including the period of gradual dose reduction; continued treatment beyond this period is possible only after a careful assessment of the patient's condition.

Precautions substance Bromazepam
There should be appointed for the monotherapy of depression, including anxious depression, due to the possibility of suicide. Paradoxical reactions are more common in children and elderly patients. In the event of paradoxical reactions bromazepam should be abolished. It is recommended to reduce the dose gradually, as the risk of withdrawal symptoms above in a sharp lifting of the drug.

When receiving bromazepam (even at therapeutic doses) may develop physical and psychological dependence. Depending risk increases when large doses and with increasing duration of the reception, as well as in patients with alcohol dependence and drug history. Abolition of bromazepam should be done gradually by reducing the dose to reduce the risk of withdrawal symptoms and rebound-a syndrome. In abrupt cancellation after long-term use or high doses there is a withdrawal syndrome (headache and muscle pain, agitation, anxiety, confusion, tremors, convulsions), in severe cases - depersonalization, hallucinations, seizures (sudden elimination in epilepsy). Transient syndrome where symptoms giving rise to the appointment of bromazepam, resumed in a more pronounced form (rebound-Syndrome), may also be accompanied by mood changes, sleep disturbance, anxiety and others.

Benzodiazepines may cause anterograde amnesia, which develops when using doses close to the upper limit of therapeutic range (for documented bromazepam 6 mg dose), at higher dosage increases her risk.

With long-term treatment requires monitoring of liver enzymes. Should not be used during the drivers of vehicles and people, a profession which requires high concentration of attention. In the period of treatment is unacceptable consumption of alcoholic beverages.

Special instructions for Bromazepam
At the time of treatment should abandon admission alcohol.

Trading names of drugs with Bromazepam working substanceTrade Name Index

Bromazepam, Bromazepam Lannaher, Bromide, Lexotan