DORMONOCT Tablet Ref.[50616] Active ingredients: Loprazolam

Source: Health Products Regulatory Authority (ZA)  Revision Year: 2019  Publisher: Sanofi-aventis south africa (pty) ltd, 2 Bond Street, Midrand, 1685, South Africa

5.1. Pharmacodynamic properties

Pharmacological classification: A 2.2 Sedatives, hypnotics.

Loprazolam is a short-acting benzodiazepine with hypnotic properties. Loprazolam has little effect on paradoxical sleep patterns (REM).

5.2. Pharmacokinetic properties

Absorption

The absolute bioavailability following a single oral dose of 1 mg is 80%. The maximum concentration (Cmax) is 5,5-6,0 ยตg/ml per one hour (Tmax) following a single oral dose of 1 mg loprazolam.

Distribution

Plasma protein binding is 80%.

Metabolism

Loprazolam is metabolised in the liver. The principal metabolite is the piperazine N-oxide of loprazolam.

Elimination

The half-life is 6-8 hours.

In the elderly, the plasma half-life is increased (approximately 1,5 fold). Loprazolam is excreted 40% by the urinary route and 55% in the faeces, while 3-25% of the ingested dose is recovered in the bile.

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