Sulazepam
Sulazepam: A Benzodiazepine Derivative That Remained Unmarketed[edit | edit source]
Sulazepam is a derivative of the widely-known benzodiazepine, diazepam. Notably characterized as the thioamide variant of diazepam, it undergoes metabolism to produce several active metabolites. Although it exhibits a spectrum of pharmacological activities typical of benzodiazepines, sulazepam was never introduced commercially.
Chemistry[edit | edit source]
- Structural Relation to Diazepam: Sulazepam is chemically distinguished from diazepam by the presence of a thioamide functional group[1]. This subtle chemical modification yields a compound with unique metabolic and pharmacokinetic profiles.
Pharmacology[edit | edit source]
- Metabolism: Upon administration, sulazepam is metabolized into several products:
- Diazepam: The parent compound from which sulazepam is derived.
- Desmethyldiazepam: A major active metabolite common to several benzodiazepines.
- Oxydiazepam: Another metabolite that contributes to the overall pharmacological activity of sulazepam[2].
- Pharmacological Properties:
- Sedative: Induces calmness or sleepiness.
- Muscle Relaxant: Reduces muscle tension or involuntary muscle contractions.
- Hypnotic: Promotes or prolongs sleep.
- Anticonvulsant: Prevents or reduces the severity of epileptic fits or other convulsions.
- Anxiolytic: Relieves anxiety.
These effects are consistent with those observed for other benzodiazepine derivatives[3].
Development and Market Status[edit | edit source]
Although sulazepam was researched as a potential therapeutic, it was never launched commercially. The reasons for its non-market introduction remain speculative but may encompass a multitude of factors including:
- Competition from already established benzodiazepines
- Unforeseen clinical findings
- Market dynamics or strategic decisions by the developer
The pharmaceutical industry has numerous instances of compounds with promising in-vitro or early-stage clinical data that, for various reasons, do not proceed to market launch[4].
Conclusion[edit | edit source]
Sulazepam offers an interesting insight into the world of drug discovery and development. Despite its close structural and pharmacological relationship with diazepam, a gold-standard in benzodiazepine therapy, sulazepam's journey did not lead to market availability. Such instances highlight the intricate and multifaceted nature of pharmaceutical research and commercialization.
References[edit | edit source]
- ↑ O'Neil, M.J. (Ed.). (2006). The Merck Index (14th ed.). Whitehouse Station, NJ: Merck & Co., Inc.
- ↑ Mandrioli, R., Mercolini, L., & Raggi, M.A. (2006). Benzodiazepine metabolism: An analytical perspective. Current Drug Metabolism, 8(8), 827-844.
- ↑ Griffiths, R.R., & Johnson, M.W. (2005). Relative abuse liability of hypnotic drugs: A conceptual framework and algorithm for differentiating among compounds. The Journal of Clinical Psychiatry, 66(suppl 9), 31-41.
- ↑ DiMasi, J.A., Feldman, L., Seckler, A., & Wilson, A. (2010). Trends in risks associated with new drug development: Success rates for investigational drugs. Clinical Pharmacology & Therapeutics, 87(3), 272-277.
Benzodiazipines[edit source]
- Alprazolam
- Chlordiazepoxide
- Diazepam (Oral)
- Estazolam
- Flurazepam
- Lorazepam
- Midazolam
- Oxazepam
- Quazepam
- Temazepam
- Triazolam
Anticonvulsants Drugs[edit source]
Drug class for Sulazepam[edit source]
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