Lorazepam

Products

Lorazepam is commercially available as tablets, meltable tablets, and a solution for injection. In addition to the original Temesta, generics and a combination product with the sedative antihistamine diphenhydramine are also available (Somnium). Lorazepam has been approved in many countries since 1973.

Structure and properties

Lorazepam (C15H10Cl2N2O2, Mr = 321.2 g/mol) is a white to almost white crystalline powder that is practically insoluble in water. It is present in drugs as a racemate.

Effects

Lorazepam (ATC N05BA06) has antianxiety, sedative, anticonvulsant, and sleep-inducing properties. It crosses the bloodbrain barrier and binds in the brain to the GABAA receptor. It thereby enhances the effect of the inhibitory neurotransmitter GABA in the central nervous system.

Indications

Lorazepam is approved for the symptomatic treatment of anxiety, tension, and agitation of various causes and is also used for the short-term treatment of sleep disorders. Another indication is for sedation before and during surgical or diagnostic procedures. Other uses are discussed in the literature.

Abuse

Lorazepam, like all benzodiazepines, can be abused for a variety of purposes because of its antianxiety, disinhibitory, and depressant effects.

Dosage

According to the drug label. The duration of treatment should be kept as short as possible. Since withdrawal symptoms may occur upon discontinuation, the dose must be gradually reduced during this process.

Contraindications

  • Hypersensitivity
  • Myasthenia gravis
  • Severe respiratory insufficiency
  • Sleep apnea syndrome
  • Severe hepatic or renal insufficiency
  • Shock
  • Coma
  • Collapse states
  • Medication, alcohol, and drug addiction.
  • Acute intoxication with alcohol, sleeping pills, painkillers and psychotropic drugs.
  • Children under 12 years

Full precautions can be found in the drug label.

Interactions

Centrally depressant drugs and substances may potentiate the effects and adverse effects of lorazepam. These include alcohol, psychotropic drugs, neuroleptics, sleeping pills, anxiolytics, sedatives, antidepressants, antiepileptic drugs, narcotics, anesthetics, antihistamines, and other benzodiazepines. Other interactions are possible with clozapine, valproate, probenecid, theophylline, and scopolamine.

Adverse effects

The most common possible adverse effects include sedation, fatigue, drowsiness, muscle weakness, weakness, gait disturbance, confusion, depression, and drowsiness. Other adverse effects include sexual dysfunction, digestive problems, allergic reactions, central disturbances such as tremors, dizziness, visual disturbances, speech disorders and amnesia, hypotension, respiratory depression, and psychological and behavioral disturbances such as hostility, anger, excitability, aggressiveness, delusions, mania, nightmares, hallucinations, psychosis, maladaptive behavior. Lorazepam may be addictive. Abrupt discontinuation may lead to withdrawal symptoms after prolonged therapy.