BROMAZEPAM 6 KIARA

Indications

• Generalized anxiety disorder
• Severe anxiety
• Insomnia

Dosage

Children: Refer to the BNF for Children for appropriate dosing information.

Adults: The usual dose is 3 to 6 mg taken once daily, which may be adjusted according to response. For severe cases, doses may be increased to a maximum of 12 mg daily.

Mechanism of action

Bromazepam binds to the GABA-A receptor, resulting in a conformational change that enhances the inhibitory effects of gamma-aminobutyric acid (GABA), the primary inhibitory neurotransmitter in the central nervous system. This action increases neuronal hyperpolarization, leading to reduced excitability and overall calming effects.

Pharmacodynamics

As a lipophilic benzodiazepine, bromazepam exhibits sedative, hypnotic, anxiolytic, and skeletal muscle relaxant actions. Unlike some other anxiolytics, bromazepam does not have antidepressant properties. Its rapid absorption and onset of action contribute to a higher potential for abuse, misuse, and the development of dependence compared to other benzodiazepines.

Pharmacokinetics

Bromazepam is well-absorbed following oral administration, with peak plasma concentrations typically reached within 1 to 2 hours. It is extensively metabolized in the liver, primarily by cytochrome P450 enzymes, and has a long elimination half-life, allowing for sustained therapeutic effects. The drug is lipophilic, which facilitates its penetration across the blood-brain barrier, contributing to its central nervous system effects.

Contra-indications

• Severe respiratory insufficiency
• Sleep apnoea
• Myasthenia gravis
• Acute alcohol intoxication
• Known hypersensitivity to bromazepam or any of its components

Adverse effects

• Drowsiness
• Confusion
• Ataxia
• Dizziness
• Fatigue
• Paradoxical reactions (e.g., agitation, aggression)
• Dependence and withdrawal symptoms

Interactions

• CNS depressants (e.g., opioids, alcohol) may enhance sedative effects
• Antidepressants may increase the sedative effects of bromazepam
• Cimetidine may increase levels of bromazepam
• Rifampicin may reduce levels of bromazepam

Precautions

• Use with caution in elderly patients or those with liver impairment
• Monitor for signs of dependence and withdrawal
• Avoid abrupt discontinuation after prolonged use
• Assess for potential for abuse and misuse

Pregnancy

Bromazepam is contraindicated in pregnancy due to potential risks to the fetus, including congenital malformations and withdrawal symptoms in neonates.

Breast-feeding

Bromazepam is excreted in breast milk; therefore, it is recommended to either avoid breastfeeding or discontinue the drug.

Storage

Store in a cool, dry place, away from light. Keep out of reach of children.

Formulations

• Tablets: 3 mg, 6 mg, and 12 mg

Mechanism of action

Bromazepam binds to the GABA-A receptor producing a conformational change and potentiating its inhibitory effects. Other neurotransmitters are not influenced.

Pharmacodynamics

Bromazepam is a lipophilic, long-acting benzodiazepine and with sedative, hypnotic, anxiolytic and skeletal muscle relaxant properties. It does not possess any antidepressant qualities. Bromazepam, like other benzodiazepines, presents a risk of abuse, misuse, and dependence. According to many psychiatric experts, Bromazepam has a greater abuse potential than other benzodiazepines because of fast resorption and rapid onset of action.