Active ingredient: Lorazepam - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Anti-anxiety Agents
• Hypnotics and Sedatives
• Antiemetics
• Anticonvulsants
• Benzodiazepines

Dosage Forms

• Tablet
• Injection

Brands / Synonyms

(+/-)-Lorazepam; Almazine; Alzapam; Anxiedin; Aplacassee; Ativan; Bonatranquan; Delormetazepam; Emotival; Idalprem; L-Lorazepam Acetate; Lorabenz; Lorax; Loraz; Lorazepam; Lorazepam Intensol; Lorsilan; O-Chlorooxazepam; O-Chloroxazepam; Pro Dorm; Psicopax; Punktyl; Quait; Securit; Sedatival; Sedazin; Somagerol; Tavor; Temesta; Wypax

Indications

For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety or anxiety associated with depressive symptoms

Pharmacology

Lorazepam, a benzodiazepine not transformed to active metabolites, is used to treat anxiety, status epilepticus, and for sedation induction and anterograde amnesia.

Mechanism of Action

Lorazepam binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.

Absorption

Readily absorbed with an absolute bioavailability of 90%.

Toxicity

Somnolence, confusion, and coma, LD₅₀=3178mg/kg (orally in mice).

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

Tablets: Lorazepam is contraindicated in patients with known sensitivity to the benzodiazepines or with acute narrow-angle glaucoma.

Injection: Lorazepam injection is indicated in adult patients for preanesthetic medication, producing sedation (sleepiness or drowsiness), relief of anxiety, and a decreased ability to recall events related to the day of surgery. It is most useful in those patients who are anxious about their surgical procedure and who would prefer to have diminished recall of the day of surgery.

Drug Interactions

Tablets: The benzodiazepines, including lorazepam, produce CNS-depressant effects when administered with such medications as barbiturates or alcohol.

Injection: Lorazepam injection, like other injectable benzodiazepines, produces depression of the central nervous system when administered with ethyl alcohol, phenothiazines, barbiturates, MAO inhibitors, and other antidepressants.When scopolamine is used concomitantly with injectable lorazepam, an increased incidence of sedation, hallucinations, and irrational behavior has been observed.