Lendormin (Brotizolam)

Brotizolam is used as a sedative‑hypnotic for disorders affecting sleep initiation and maintenance.

• Insomnia: Improves sleep onset and reduces nighttime awakenings in patients with difficulty maintaining sleep.
• Primary sleep disorder: Provides short‑term relief of symptoms in diagnosed primary insomnia.
• Sleep maintenance disorder: Helps sustain continuous sleep throughout the night for individuals with fragmented sleep patterns.
• Sleep onset insomnia: Reduces latency to fall asleep in patients experiencing prolonged time to sleep.
• Circadian rhythm sleep disorder: Assists in adjusting sleep timing when used under medical supervision.

• Brotizolam acts as a positive allosteric modulator at the benzodiazepine binding site of the GABA‑A receptor complex. By enhancing the affinity of GABA for its receptor, it increases chloride ion influx, leading to hyperpolarization of neuronal membranes and amplified inhibitory neurotransmission. This results in reduced neuronal excitability, producing sedative, hypnotic, anxiolytic and muscle‑relaxant effects. The enhanced GABAergic activity predominantly affects brain regions that regulate sleep and anxiety.

Brotizolam may cause a range of adverse reactions, varying from mild to severe.

Common Side Effects

• Drowsiness: Feeling of excessive sleepiness during daytime.
• Dizziness: Light‑headed sensation or loss of balance.
• Headache: Mild to moderate cranial pain.
• Dry mouth: Reduced salivation leading to oral dryness.
• Fatigue: Persistent feeling of low energy and tiredness.
• Impaired coordination: Reduced motor control leading to clumsiness.

Serious or Rare Side Effects

• Respiratory depression: Marked reduction in breathing effort, especially with other depressants.
• Dependence and withdrawal: Risk of physical dependence with prolonged use and possible withdrawal symptoms upon abrupt cessation.
• Severe allergic reaction: Signs such as rash, itching, swelling, or anaphylaxis.
• Paradoxical agitation: Unexpected increase in anxiety, aggression or restlessness.
• Psychomotor slowing: Noticeable slowing of thought processes and reaction time.
• Hepatic dysfunction: Elevated liver enzymes indicating possible liver stress.

When prescribing Brotizolam, clinicians should observe several safety considerations to minimise risk.

• Assess patient history: Review prior benzodiazepine exposure, dependence, or substance‑use disorders.
• Avoid in severe hepatic impairment: Use with caution or consider alternative therapy.
• Caution in elderly: Increased susceptibility to falls, confusion and prolonged sedation.
• Do not combine with alcohol: Concomitant use can intensify central nervous system depression.
• Pregnancy and lactation: Use only if benefits outweigh potential risks; discuss with obstetric provider.
• Store at ambient temperature: Keep in original packaging, protect from moisture and light.

Brotizolam can interact with other medicines, altering its sedative effect or safety profile.

Major Interactions (Avoid)

• Alcohol: Potentiates central nervous system depression, increasing risk of respiratory compromise.
• Opioids: Combined use may cause profound sedation, respiratory depression, and overdose.
• Other benzodiazepines: Additive effects heighten sedation and psychomotor impairment.
• Barbiturates: Synergistic depression of neuronal activity leading to severe CNS depression.
• Antidepressants (e.g., tricyclics): May increase sedation and cardiovascular side effects.

Moderate Interactions (Monitor Closely)

• CYP3A4 inhibitors (e.g., ketoconazole): Can raise Brotizolam plasma levels, requiring dose adjustment.
• CYP3A4 inducers (e.g., rifampicin): May reduce drug exposure, potentially decreasing efficacy.
• Antihistamines: May enhance drowsiness and impair alertness.
• Antihypertensives: Possible additive hypotensive effect, monitor blood pressure.
• Antipsychotics: May increase sedation; observe for excessive CNS depression.