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QuickView for Lorazepam (compound)


PubChem
Name: Lorazepam
PubChem Compound ID: 11609501
Description: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.
Molecular formula: C15H10Cl2N2O2
Molecular weight: 324.136 g/mol
DrugBank
Identification
Name: Lorazepam
Name (isomeric): DB00186
Drug Type: small molecule
Description: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.
Synonyms:
O-Chloroxazepam; (+/-)-Lorazepam; L-Lorazepam Acetate; O-Chlorooxazepam
Brand: Loraz, Wypax, Lorabenz, Quait, Pro Dorm, Aplacassee, Lorax, Almazine, Sedazin, Lorazepam Intensol, Sedatival, Psicopax, Idalprem, Securit, Temesta, Alzapam, Punktyl, Emotival, Delormetazepam, Somagerol, Tavor, Anxiedin, Bonatranquan, Lorsilan, Ativan
Category: Benzodiazepines, Anti-anxiety Agents, GABA Modulators, Hypnotics and Sedatives, Antiemetics, Anticonvulsants
CAS number: 846-49-1
Pharmacology
Indication: For the management of anxiety disorders, and for treatment of status epilepticus.
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 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.
Absorption: Readily absorbed with an absolute bioavailability of 90%.
Protein binding: 85%
Biotransformation: Hepatic
Route of elimination: Lorazepam is rapidly conjugated at its 3-hydroxy group into lorazepam glucuronide which is then excreted in the urine.
Half Life: 12 hours
Toxicity: Somnolence, confusion, and coma, LD50=3178mg/kg (orally in mice).
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Avoid excessive quantities of coffee or tea (Caffeine).
Take with food.
Drug interaction:
KavaKava may increase the effect of the benzodiazepine, lorazepam.
Valproic AcidValproic acid may increase the serum concentration of Lorazepam by reducing Lorazepam metabolism. The Lorazepam dose should be reduced by 50% during concomitant therapy. Monitor for increased Lorazepam effects and toxicity.
TriprolidineThe CNS depressants, Triprolidine and Lorazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
ClozapineIncreased risk of toxicity

Targets