Active Ingredient History
Lorazepam (brand name Ativan) is indicated for the management of anxiety disorders or for the short-term relief of the symptoms of anxiety or anxiety associated with depressive symptoms. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic. 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 hyperpolarization of the neuron. Studies in healthy volunteers show that in single high doses Ativan (lorazepam) has a tranquilizing action on the central nervous system with no appreciable effect on the respiratory or cardiovascular systems. Ativan (lorazepam) is readily absorbed with an absolute bioavailability of 90 percent. The mean half-life of unconjugated lorazepam in human plasma is about 12 hours and for its major metabolite, lorazepam glucuronide, about 18 hours. At clinically relevant concentrations, lorazepam is approximately 85% bound to plasma proteins. Lorazepam is rapidly conjugated at its 3-hydroxy group into lorazepam glucuronide which is then excreted in the urine. Lorazepam glucuronide has no demonstrable CNS activity in animal. Most adverse reactions to benzodiazepines, including CNS effects and respiratory depression, are dose dependent, with more severe effects occurring with high doses. Paradoxical reactions, including anxiety, excitation, agitation, hostility, aggression, rage, sleep disturbances/insomnia, sexual arousal, and hallucinations may occur. Small decreases in blood pressure and hypotension may occur but are usually not clinically significant, probably being related to the relief of anxiety produced by lorazepam. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Anxiety Disorders (approved 1977)
Acute Pain (Phase 2)
Alcohol Drinking (Phase 4)
Alcoholism (Phase 4)
Alcohol Withdrawal Delirium (Phase 4)
Allergy and Immunology (Phase 3)
alpha 1-Antitrypsin Deficiency (Phase 1)
Alzheimer Disease (Phase 1)
Analgesia (Phase 2)
Anxiety (Phase 4)
Anxiety Disorders (Phase 4)
Bipolar Disorder (Phase 4)
Breast Neoplasms (Phase 2)
Bronchoscopy (Phase 4)
Catatonia (Phase 1)
Cocaine-Related Disorders (Phase 2)
Cognition Disorders (Phase 4)
Conscious Sedation (Phase 4)
Critical Illness (Phase 2/Phase 3)
Delirium (Phase 2/Phase 3)
Dementia (Phase 3)
Dental Care for Disabled (Phase 4)
Depression (Phase 4)
Depressive Disorder, Major (Phase 1)
Dexmedetomidine (Phase 4)
Diabetic Foot (Phase 1/Phase 2)
Down Syndrome (Phase 2)
Epidermolysis Bullosa (Early Phase 1)
Epilepsia Partialis Continua (Phase 3)
Epilepsy (Phase 3)
Epilepsy, Reflex (Phase 2)
Fear (Phase 4)
Healthy Volunteers (Phase 4)
Heart Arrest (Phase 4)
Hypothermia (Phase 4)
Liver Cirrhosis (Phase 1)
Lorazepam (Early Phase 1)
Mania (Phase 2)
Methamphetamine (Phase 2)
Nausea (Phase 2)
Neoplasm Metastasis (Phase 2/Phase 3)
Neoplasms (Phase 2/Phase 3)
Neuroimaging (Early Phase 1)
Nodding Syndrome (Phase 1)
Obsessive Behavior (Phase 2)
Pain (Phase 4)
Pregnancy Complications (Phase 4)
Pregnancy Trimester, First (Phase 4)
Psychomotor Agitation (Phase 4)
Psychophysiologic Disorders (Phase 3)
Psychotic Disorders (Phase 4)
Respiratory Insufficiency (Phase 1)
Rhinitis, Allergic (Phase 3)
Rhinitis, Allergic, Perennial (Phase 3)
Schizophrenia (Phase 4)
Seizures (Phase 3)
Sleep Disorders, Intrinsic (Phase 2)
Sleep Wake Disorders (Phase 4)
Status Epilepticus (Phase 3)
Substance-Related Disorders (Phase 1/Phase 2)
Ultrasonography (Early Phase 1)
Vertigo (Phase 3)
Voice Disorders (Phase 1)
Vomiting (Phase 2)
Wounds and Injuries (Phase 4)
| Trial | Phase | Start Date | Organizations | Indications |
|---|
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