Loprazolam

Oral
Short-term management of insomnia

Debilitated patients: Initially, 0.5 mg once daily at bedtime. Max: 1 mg once daily.

Acute pulmonary insufficiency, severe respiratory insufficiency, myasthenia gravis, phobic or obsessional states, sleep apnoea syndrome; monotherapy use in depression or anxiety associated with depression and chronic psychosis and alcohol intake.

Patient with personality disorders, depression (particularly if suicidal risk is present), history of psychiatric disorders, and alcohol or drug abuse; chronic pulmonary insufficiency, cerebrovascular disease. Not recommended for long-term use. Avoid abrupt withdrawal. Concomitant use with opioids. Chronic renal or hepatic impairment. Elderly and debilitated patients. Pregnancy and lactation.

Significant: Paradoxical reactions, including hyperactive, aggressive, or suicidal behaviour; rebound insomnia which may be accompanied by other reactions such as restlessness, anxiety, sleep disturbances or mood changes; increased risk of sleep-related activities (e.g. sleep-driving, making phone calls while asleep, cooking and eating food); anterograde amnesia, CNS depression; increased risk of falls leading to severe injury; abuse or physical and psychological dependence.
Eye disorders: Blurred vision.
Gastrointestinal disorders: Nausea.
General disorders and administration site conditions: Ataxia.
Musculoskeletal and connective tissue disorders: Hypotonia.
Nervous system disorders: Headache, dizziness, drowsiness, speech disorder.

This drug may cause diziness, drowsiness and impaired concentration, if affected, do not drive or operate machinery.

Monitor respiratory and mental status.

Enhanced CNS depressant effects with other hyptonics, anxiolytics/sedatives, antidepressants, antipsychotics, antiepileptic drugs, sedative antihistamines, narcotic analgesics, or anaesthetics. Therapeutic effect may be potentiated by cisapride and other agents acting in the CNS.
Potentially Fatal: Increased risk of profound sedation, respiratory depression and coma when given with opioids.

Enhanced sedative effects with alcohol.

Description:
Mechanism of Action: Loprazolam is an intermediate-acting benzodiazepine that binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at various CNS sites, including limbic system and reticular formation. The enhancement of the GABA inhibitory effect on neuronal excitability results by increased neuronal membrane permeability to chloride ions, leading to hyperpolarisation and stabilisation.
Onset: 0.5-1 hour.
Duration: 10 hours.
Pharmacokinetics:
Absorption: Bioavailability: 79% ± 10%.
Distribution: Plasma protein binding: 80%.
Metabolism: Metabolised in the liver to form piperazine-N-oxide (active metabolite).
Excretion: Via faeces (52.5%); urine (38.8%). Elimination half-life: 3.5-12.8 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3033860, Loprazolam. https://pubchem.ncbi.nlm.nih.gov/compound/Loprazolam. Accessed Nov. 25, 2022.

Store below 25°C. Protect from light and moisture.

Hypnotics & Sedatives

N05CD11 - loprazolam ; Belongs to the class of benzodiazepine derivatives. Used as hypnotics and sedatives.

Anon. Loprazolam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/10/2022.

Buckingham R (ed). Loprazolam Mesilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/10/2022.

Joint Formulary Committee. Loprazolam. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/10/2022.

Loprazolam 1 mg Tablets (Focus Pharmaceuticals Limited). MHRA. https://products.mhra.gov.uk. Accessed 05/10/2022.

Loprazolam 1 mg Tablets (Zentiva Pharma UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 05/10/2022.