Brotizolam

Brotizolam is a sleep inducing agent. Chemically, it is a triazolo-thienodiazepine. It shortens the time needed to fall asleep, reduces the frequency of awakenings, and prolongs total sleep time.

Brotizolam is absorbed following oral administration. The maximum plasma concentration following therapeutic dose is reached after 0.5-3 hours. The bioavailability of brotizolam is approximately 70%.

Brotizolam is considered an intermediate-active hypnotic. Its half-life of 3.1-8.4 hours lies between the short-acting and the long-acting hypnotics. The total half-life of brotizolam and metabolities is about 9 hours. Plasma level studies following repeated administration of the therapeutic dose revealed no indication of cumulation.

Brotizolam is about 90% bound to human serum albumin.

The total renal excretion, calculated on the basis of the administered dose, is about 65%, and the fecal excretion approximately 22%. About 4% unchanged brotizolam is found in the 24-hour pooled urine.

In elderly patients, the drug has shown no tendency to enzyme-induction or accumulation, despite a prolonged elimination half-life.

No significant changes in pharmacokinetics have been observed in patients with renal insufficiency. However, in patients with liver dysfunction, brotizolam has a significantly prolonged elimination half-life.