Pyrazolam

Pyrazolam: An In-depth Overview of its Discovery, Pharmacology, and Clinical Implications[edit | edit source]

Pyrazolam is a derivative of the benzodiazepine class, an important group of drugs with diverse therapeutic applications ranging from the treatment of anxiety disorders to muscle relaxation and the induction of anesthesia.

Historical Background[edit | edit source]

Pyrazolam was originally synthesized in the 1970s by a research team led by the renowned chemist, Dr. Leo Sternbach, at Hoffman-La Roche^[1]. While its potential was recognized, it was not developed for commercial use immediately. Fast forward to 2012, and the compound was "rediscovered" and began being distributed as a research chemical^[2].

Structural and Pharmacological Properties[edit | edit source]

Chemical Structure: Pyrazolam bears structural similarities to another well-known benzodiazepine, alprazolam. The distinctions in their molecular structures account for the unique pharmacological profiles of each compound^[3].

Anxiolytic Effects: Pyrazolam's primary therapeutic application lies in its potent anxiolytic effects. Remarkably, its anxiolytic activity is approximately 12 times more potent than diazepam, a commonly used benzodiazepine for anxiety^[4].

Anticonvulsant and Hypnotic Properties: While its primary use is an anxiolytic, when administered at higher doses, pyrazolam demonstrates anticonvulsant and hypnotic effects. These properties might be of interest for further clinical applications^[5].

Receptor Subtype Selectivity: Pyrazolam exhibits a preferential selectivity for the GABA_A receptor subtypes α2 and α3. This selectivity profile can help predict the drug's therapeutic effects and side effect profile^[6].

Metabolic Profile[edit | edit source]

Unlike many of its benzodiazepine counterparts, pyrazolam displays an intriguing metabolic characteristic: it does not seem to undergo any significant metabolic transformation within the body. Instead, it is primarily excreted unchanged in the urine. Furthermore, no metabolites have been identified in the urine samples of human volunteers, highlighting its unique metabolic stability^[7].

Safety and Side Effects[edit | edit source]

Pyrazolam's strong anxiolytic effects are complemented by its relatively mild side effect profile. Notably, when used within its therapeutic dose range for anxiety, it causes minimal ataxia and sedation, making it a potentially favorable option in clinical contexts where these side effects are less desirable^[8].

Conclusion[edit | edit source]

The journey of pyrazolam, from its inception at Hoffman-La Roche in the 1970s to its revival in 2012, illustrates the complex trajectory of drug development and rediscovery. As with any drug, comprehensive studies and clinical trials are essential to ascertain its safety, efficacy, and potential therapeutic applications. Given its promising profile, pyrazolam might yet find its place in modern therapeutics.

References[edit | edit source]

↑ Sternbach, L. H. (1972). The benzodiazepine story. Journal of Medicinal Chemistry, 15(5), 439-444.
↑ Morris, H., & Wallach, J. (2014). From PCP to MXE: a comprehensive review of the non-medical use of dissociative drugs. Drug Testing and Analysis, 6(7-8), 614-632.
↑ US Patent 4105776 - 5-ARYL-1,4-BENZODIAZEPINES
↑ Vinkers, C. H., & Olivier, B. (2012). Mechanisms underlying tolerance after long-term benzodiazepine use: A future for subtype-selective GABA_A receptor modulators?. Advances in Pharmacological Sciences, 2012.
↑ Fleck, M. W. (2006). Molecular actions of (nonbenzodiazepine) drugs on GABA_A receptors. Progress in Neuro-Psychopharmacology and Biological Psychiatry, 30(6), 920-930.
↑ Sieghart, W. (1995). Structure and pharmacology of gamma-aminobutyric acid_A receptor subtypes. Pharmacological Reviews, 47(2), 181-234.
↑ Greenblatt, D. J., & Wright, C. E. (1993). Clinical pharmacokinetics of alprazolam. Therapeutic implications. Clinical Pharmacokinetics, 24(6), 453-471.
↑ Lader, M. (2011). Benzodiazepines revisited—will we ever learn?. Addiction, 106(12), 2086-2109.

Benzodiazipines[edit source]

Anticonvulsants Drugs[edit source]

Drug class for Pyrazolam[edit source]

Anticonvulsants, and Benzodiazepines]

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[sternbach1-1] Sternbach, L. H. (1972). The benzodiazepine story. Journal of Medicinal Chemistry, 15(5), 439-444.

[researchchem2-2] Morris, H., & Wallach, J. (2014). From PCP to MXE: a comprehensive review of the non-medical use of dissociative drugs. Drug Testing and Analysis, 6(7-8), 614-632.

[structure3-3] US Patent 4105776 - 5-ARYL-1,4-BENZODIAZEPINES

[anxiolytic4-4] Vinkers, C. H., & Olivier, B. (2012). Mechanisms underlying tolerance after long-term benzodiazepine use: A future for subtype-selective GABA_A receptor modulators?. Advances in Pharmacological Sciences, 2012.

[anticonvulsant5-5] Fleck, M. W. (2006). Molecular actions of (nonbenzodiazepine) drugs on GABA_A receptors. Progress in Neuro-Psychopharmacology and Biological Psychiatry, 30(6), 920-930.

[receptor6-6] Sieghart, W. (1995). Structure and pharmacology of gamma-aminobutyric acid_A receptor subtypes. Pharmacological Reviews, 47(2), 181-234.

[metabolism7-7] Greenblatt, D. J., & Wright, C. E. (1993). Clinical pharmacokinetics of alprazolam. Therapeutic implications. Clinical Pharmacokinetics, 24(6), 453-471.

[sideeffect8-8] Lader, M. (2011). Benzodiazepines revisited—will we ever learn?. Addiction, 106(12), 2086-2109.

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