For the management of anxiety disorders, and for treatment of status epilepticus.
Lorazepam binds to an allosteric site on GABA-A receptors, which are pentameric ionotropic receptors in the CNS. Binding potentiates the effects of the inhibitory neurotransmitter GABA, which upon binding opens the chloride channel in the receptor, allowing chloride influx and causing hyperpolerization of the neuron.
Somnolence, confusion, and coma, LD<sub>50</sub>=3178mg/kg (orally in mice).
Readily absorbed with an absolute bioavailability of 90%.
12 hours
Lorazepam is rapidly conjugated at its 3-hydroxy group into lorazepam glucuronide which is then excreted in the urine.