Investigational Drug Details
| Drug ID: | D113 |
| Drug Name: | Alprazolam |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00404 |
| DrugBank Description: | Alprazolam is a triazolobenzodiazepine indicated for the treatment of anxiety and panic disorders.[Label] It is mainly metabolized by CYP3As and so is contraindicated with CYP3A inhibitors like ketoconazole and itraconazole.[Label] Benzodiazepine treatment should be stopped gradually by tapering down a patient's dose to avoid withdrawal symptoms.[A18125] Alprazolam's adverse effects are generally related to the sedation it can cause.[A18125] Alprazolam has been mixed with alcohol as a drug of abuse to potentiate the sedative effects of the drug which may lead to coma and death.[A18125] Alprazolam was given FDA approval on October 16, 1981[L6148]. |
| PubChem ID: | 2118 |
| CasNo: | 28981-97-7 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CC1=NN=C2CN=C(C3=CC=CC=C3)C3=C(C=CC(Cl)=C3)N12 |
| Structure: |
|
| InChiKey: | VREFGVBLTWBCJP-UHFFFAOYSA-N |
| Molecular Weight: | 308.765 |
| DrugBank Targets: | GABA-A receptor (anion channel); GABA-A receptor (benzodiazepine site) |
| DrugBank MoA: | Alprazolam is a triazolobenzodiazepine used to treat certain anxiety and panic disorders.[Label] Alprazolam acts on benzodiazepine receptors BNZ-1 and BNZ-2.[Label,A177973,A177925] The active metabolites 4-hydroxyalprazolam acts on these receptors with 0.20 times the potency of alprazolam and alpha-hydroxyalprazolam acts on these receptors with 0.66 times the potency.[Label] The effect of alprazolam on BNZ-1 mediates the sedation and anti-anxiety effects of the drug while the action on BNZ-2 mediates effects on memory, coordination, muscle relaxation, and anticonvulsive activity.[A177973,A18125] Alprazolam also couple with GABA-A receptors to enhance GABA binding to its receptor.[A177973] This interaction mediates inhibition of the nervous system and results in a calming effect.[A177973] The molecular mechanisms as well as the clinical effects of alprazolam have both been well demonstrated, however the means by which the molecular mechanism translates to a clinical effect is still not understood.[Label,A177973,A18125] |
| DrugBank Pharmacology: | Alprazolam is indicated to treat anxiety and panic disorders.[Label] The mechanism by which its cell receptor interactions translate to a clinical effect is not known.[Label,A177973,A18125] Alprazolam exerts its effects through interaction with BNZ-1, BNZ-2, and GABA-A receptors.[A177973,A18125] Alprazolam binding to BNZ-1 is thought to influence sedation and anti-anxiety, BNZ-2 may influence memory, coordination, muscle relaxation, and anticonvulsive activity, and GABA-A may calm patients by increasing the affinity of GABA-A receptors for GABA[A177973,A18125]. The metabolism of alprazolam is mediated largely through the action of CYP3As and so alprazolam is contraindicated with CYP3A inhibitors such as ketoconazole and itraconazole.[Label] Alprazolam, like other benzodiazepines, can cause dependancy and so when stopping treatment doses should be tapered down gradually[A18125]. Alprazolam's adverse effects are generally related to the sedating effects of the drug.[A18125] This effect has lead to abuse of alprazolam with alcohol to potentiate its sedating effect, which may lead to coma and death.[A18125] |
| DrugBank Indication: | Alprazolam is indicated for the management of anxiety disorder, anxiety associated with depression, panic disorder, and panic disorder with agoraphobia.[Label] Alprazolam may also be prescribed off label for insomnia, premenstrual syndrome, and depression.[A177973] |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name | |
|---|---|---|---|---|---|---|---|
| T03 | Angiotensin-converting enzyme | ACE | INHIBITOR | Target is a single protein chain | P12821 | ACE_HUMAN | Details |
| T06 | Sulfonylurea receptor 1 | ABCC8 | Target is a single protein chain | Q09428 | ABCC8_HUMAN | Details | |
| T47 | Sialin | SLC17A5 | Target is a single protein chain | Q9NRA2 | SLC17A5_HUMAN | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Article ID | PMID | Source | Title |
|---|