Definition
A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238)
Description
Alprazolam is only found in individuals that have used or taken this drug. It is a triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of panic disorders, with or without agoraphobia, and in generalized anxiety disorders. (From AMA Drug Evaluations Annual, 1994, p238) Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic. Hydroxylated in the liver to α-hydroxyalprazolam, which is also active. This and other metabolites are later excreted in urine as glucuronides. Route of Elimination: Alprazolam and its metabolites are excreted primarily in the urine. Half Life: 6.3-26.9 hours
- Uses/Sources: For the management of anxiety disorder or the short-term relief of symptoms of anxiety and for the treatment of panic disorder, with or without agoraphobia.
- Health Effects: They cause slurred speech, disorientation and "drunken" behavior. They are physically and psychologically addictive.
- Symptoms: Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
- Treatment: As in all cases of drug overdosage, respiration, pulse rate, and blood pressure should be monitored. General supportive measures should be employed, along with immediate gastric lavage. Intravenous fluids should be administered and an adequate airway maintained. If hypotension occurs, it may be combated by the use of vasopressors. Dialysis is of limited value. Flumazenil, a specific benzodiazepine receptor antagonist, is indicated for the complete or partial reversal of the sedative effects of benzodiazepines and may be used in situations when an overdose with a benzodiazepine is known or suspected. (L1712)
- Route of Exposure: Oral. Readily absorbed from the gastrointestinal tract. Bioavailability is 80-90%.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50: 1020 mg/kg (Oral, mouse)
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Gamma-aminobutyric acid receptor subunit alpha-1 Gamma-aminobutyric acid receptor subunit alpha-2 Gamma-aminobutyric acid receptor subunit alpha-3 Gamma-aminobutyric acid receptor subunit alpha-4 Gamma-aminobutyric acid receptor subunit alpha-5 Gamma-aminobutyric acid receptor subunit alpha-6 Translocator protein |
Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell. |
6738302 17139284 2867566 17016423 |
Gamma-aminobutyric acid receptor subunit beta-1 Gamma-aminobutyric acid receptor subunit beta-2 Gamma-aminobutyric acid receptor subunit beta-3 Gamma-aminobutyric acid receptor subunit delta Gamma-aminobutyric acid receptor subunit gamma-2 Gamma-aminobutyric acid receptor subunit gamma-3 Gamma-aminobutyric acid receptor subunit pi Gamma-aminobutyric acid receptor subunit rho-1 Gamma-aminobutyric acid receptor subunit rho-2 Gamma-aminobutyric acid receptor subunit gamma-1 Gamma-aminobutyric acid receptor subunit rho-3 Gamma-aminobutyric acid receptor subunit epsilon GABA-A receptor (anion channel) Bromodomain-containing protein 4 Platelet-activating factor receptor Gastrin/cholecystokinin type B receptor |
22137933 14978513 18384456 6738302 8496938 2156995 3336017 2867566 |
Alprazolam Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Puberty, Delayed | 8.8 |
|
Stereotypic Movement Disorder | 7.01 |
|
Prostatic Neoplasms | 6.42 |
|
EPILEPTIC ENCEPHALOPATHY, EARLY INFANTILE, 12 | 6.15 |
|
Thyroid Hormone Resistance Syndrome | 6.09 |
|
Androgenetic alopecia | 5.72 |
|
Glioblastoma multiforme | 5.33 |
|
Neoplasm, Residual | 5.19 |
|
ACTH Deficiency, Isolated | 5.14 |
|
Pain | 5.02 |
|
Retinitis | 4.91 |
|
Pituitary Apoplexy | 4.79 |
|
Anorexia | 4.71 |
|
Bradycardia | 4.68 |
|
Alzheimer's Disease | 4.62 |
|
Amnesia | 4.59 |
|
Hypothyroidism | 4.56 |
|
Brain Injuries | 4.49 |
|
Brain Ischemia | 4.44 |
|
Entamoebiasis | 4.44 |
|