- Overview
- Properties
- Related Genes
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Overview
| Generic Names: | TUS-1; alprazolam |
|---|---|
| Trade Names: | Alplax; Alpronax; Alviz; Bestrol; Cassadan; Constan; D 65MT; Esparon; Frontal; Intensol; Niravam; Restyl; Solanax; Tafil; Tranax; Trankimazin; Tranquinal; Xanax; Xanax XR; Xanor |
| PharmGKB Accession Id: | PA448333 |
Description
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) (source: Drug Bank)
Indication
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. (source: Drug Bank)
ATC Therapeutic Category
- N05BA:Benzodiazepine derivatives
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
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 (GABA<sub>A</sub>) 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. (source: Drug Bank)
Pharmacology
Alprazolam, a benzodiazepine, is used to treat panic disorder and anxiety disorder. Unlike chlordiazepoxide, clorazepate, and prazepam, alprazolam has a shorter half-life and metabolites with minimal activity. Like other triazolo benzodiazepines such as triazolam, alprazolam may have significant drug interactions involving the hepatic cytochrome P-450 3A4 isoenzyme. Clinically, all benzodiazepines cause a dose-related central nervous system depressant activity varying from mild impairment of task performance to hypnosis. Unlike other benzodiazepines, alprazolam may also have some antidepressant activity, although clinical evidence of this is lacking. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Avoid excessive quantities of coffee or tea (Caffeine).
Avoid taking with grapefruit juice.
Take with food.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. Hydroxylated in the liver to α-hydroxyalprazolam, which is also active. This and other metabolites are later excreted in urine as glucuronides. (source: Drug Bank)
Protein Binding
80% (mainly to albumin) (source: Drug Bank)
Absorption
Readily absorbed from the gastrointestinal tract. Bioavailability is 80-90%. (source: Drug Bank)
Toxicity
Oral, mouse: LD<sub>50</sub>=1020 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time. (source: Drug Bank)
Isomeric SMILES Code:
Cc1nnc2n1-c3ccc(cc3C(=NC2)c4ccccc4)Cl (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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CYP1A2 |
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Publications |
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CYP2C19 |
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Publications |
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CYP2C9 |
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Publications |
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CYP2D6 |
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Publications |
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CYP3A |
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Publications |
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CYP3A4 |
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Publications |
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CYP3A43 |
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Publications |
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CYP3A5 |
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Publications |
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GABRA1 |
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Publications |
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GABRB2 |
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Publications |
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GABRG2 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| GABRA1 |
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(source: Drug Bank) |
| GABRA2 |
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(source: Drug Bank) |
| GABRA3 |
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(source: Drug Bank) |
| GABRA4 |
|
(source: Drug Bank) |
| GABRA5 |
|
(source: Drug Bank) |
| GABRA6 |
|
(source: Drug Bank) |
| TSPO |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
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fluoxetine |
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Publications |
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fluvoxamine |
|
Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| amprenavir |
|
Increases the effect and toxicity of benzodiazepine (source: Drug Bank) |
| carbamazepine |
|
Reduces the effect of the benzodiazepine (source: Drug Bank) |
| cimetidine |
|
Increases the effect of the benzodiazepine (source: Drug Bank) |
| clarithromycin |
|
The macrolide increases the effect of the benzodiazepine (source: Drug Bank) |
| clozapine |
|
Increased risk of toxicity (source: Drug Bank) |
| delavirdine |
|
The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank) |
| digoxin |
|
The benzodiazepine increases the effect (source: Drug Bank) |
| efavirenz |
|
The antiviral agent increases the effect and toxicity of benzodiazepine (source: Drug Bank) |
| erythromycin |
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The macrolide increases the effect of the benzodiazepine (source: Drug Bank) |
| erythromycin |
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The macrolide increases the effect of the benzodiazepine (source: Drug Bank) |
| fluconazole |
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Increases the effect of the benzodiazepine (source: Drug Bank) |
| fosamprenavir |
|
Amprenavir increases the effect and toxicity of benzodiazepine (source: Drug Bank) |
| indinavir |
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The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| itraconazole |
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The imidazole increase the effect of the benzodiazepine (source: Drug Bank) |
| ketoconazole |
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The imidazole increases the effect of the benzodiazepine (source: Drug Bank) |
| mephenytoin |
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Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank) |
| nelfinavir |
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The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| omeprazole |
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Increases the effect of the benzodiazepine (source: Drug Bank) |
| phenytoin |
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Possible increased levels of the hydantoin, decrease of benzodiazepine (source: Drug Bank) |
| ritonavir |
|
The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| saquinavir |
|
The protease inhibitor increases the effect of the benzodiazepine (source: Drug Bank) |
| telithromycin |
|
Increases the effect/toxicity of the benzodiazepine (source: Drug Bank) |
| voriconazole |
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The imidazole increases the effect of the benzodiazepine (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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Anxiety Disorders |
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Publications |
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Depression |
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Publications |
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Panic Disorder |
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Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
