DT-Web

DB01588 - Prazepam


Identification
Name Prazepam
Accession Number DB01588
Type small molecule
Description Prazepam is a benzodiazepine that is used in the treatment of anxiety disorders. It is a schedule IV drug in the U.S.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 324.804
Groups illicit
Monoisotopic Weight 324.102940883
Pharmacology
Indication For the treatment of anxiety disorders.
Mechanism of action Prazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation.
Absorption Not Available
Protein binding Not Available
Biotransformation Hepatic.
Route of elimination Not Available
Toxicity Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Cimetidine Cimetidine may increase the effect of the benzodiazepine, prazepam.
Clozapine Increased risk of toxicity
Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, prazepam.
Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, prazepam.
Omeprazole Omeprazole may increase the effect of the benzodiazepine, prazepam.
Tipranavir Tipranavir may decrease the metabolism and clearance of Prazepam. Consider alternate therapy or monitor for Prazepam toxic effects if Tipranavir is initiated or dose increased.
Triprolidine The CNS depressants, Triprolidine and Prazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Voriconazole Voriconazole may increase the serum concentration of prazepam by decreasing its metabolism. Monitor for prazepam toxicity if voriconazole is initiated or dose increased.
Food Interactions
  • Take with food.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Avoid alcohol.
  • Avoid taking with grapefruit juice.

Targets


Gamma-aminobutyric-acid receptor subunit alpha-1
Name Gamma-aminobutyric-acid receptor subunit alpha-1
Gene Name GABRA1
Pharmacological action yes
Actions potentiator
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Amin J, Brooks-Kayal A, Weiss DS: Two tyrosine residues on the alpha subunit are crucial for benzodiazepine binding and allosteric modulation of gamma-aminobutyric acidA receptors. Mol Pharmacol. 1997 May;51(5):833-41. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 1.0444
Gamma-aminobutyric-acid receptor subunit alpha-2
Name Gamma-aminobutyric-acid receptor subunit alpha-2
Gene Name GABRA2
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9613
Gamma-aminobutyric-acid receptor subunit alpha-3
Name Gamma-aminobutyric-acid receptor subunit alpha-3
Gene Name GABRA3
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9562
Gamma-aminobutyric-acid receptor subunit alpha-5
Name Gamma-aminobutyric-acid receptor subunit alpha-5
Gene Name GABRA5
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9827
Gamma-aminobutyric acid receptor subunit gamma-1
Name Gamma-aminobutyric acid receptor subunit gamma-1
Gene Name GABRG1
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9424
Gamma-aminobutyric acid receptor subunit gamma-2
Name Gamma-aminobutyric acid receptor subunit gamma-2
Gene Name GABRG2
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9751
Gamma-aminobutyric acid receptor subunit gamma-3
Name Gamma-aminobutyric acid receptor subunit gamma-3
Gene Name GABRG3
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9233
Gamma-aminobutyric-acid receptor subunit beta-1
Name Gamma-aminobutyric-acid receptor subunit beta-1
Gene Name GABRB1
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9516
Gamma-aminobutyric-acid receptor subunit beta-2
Name Gamma-aminobutyric-acid receptor subunit beta-2
Gene Name GABRB2
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9362
Gamma-aminobutyric-acid receptor subunit beta-3
Name Gamma-aminobutyric-acid receptor subunit beta-3
Gene Name GABRB3
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9564
Gamma-aminobutyric acid receptor subunit delta
Name Gamma-aminobutyric acid receptor subunit delta
Gene Name GABRD
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9315
Gamma-aminobutyric acid receptor subunit epsilon
Name Gamma-aminobutyric acid receptor subunit epsilon
Gene Name GABRE
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9297
Gamma-aminobutyric acid receptor subunit pi
Name Gamma-aminobutyric acid receptor subunit pi
Gene Name GABRP
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9144
Gamma-aminobutyric-acid receptor subunit rho-1
Name Gamma-aminobutyric-acid receptor subunit rho-1
Gene Name GABRR1
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9219
Gamma-aminobutyric acid receptor subunit rho-2
Name Gamma-aminobutyric acid receptor subunit rho-2
Gene Name GABRR2
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9253
Gamma-aminobutyric acid receptor subunit rho-3
Name Gamma-aminobutyric acid receptor subunit rho-3
Gene Name GABRR3
Pharmacological action yes
Actions potentiator
References
  • Schove LT, Perez JJ, Loew GH: Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site. Bioorg Med Chem. 1994 Oct;2(10):1029-49. - Pubmed
DTHybrid score 0.9224

Enzymes


Cytochrome P450 3A4
Name Cytochrome P450 3A4
Gene Name CYP3A4
Actions substrate
References
  • Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. - Pubmed
DTHybrid score 0.5905

Predictions


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