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Drugs in ATC Class N05CA
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Drugs in ATC Class: N05CA - Barbiturates, plain
| Tradename | Generic Name |
|---|---|
| NEMBUTAL | pentobarbital |
| NEMBUTAL SODIUM | pentobarbital sodium |
| PENTOBARBITAL SODIUM | pentobarbital sodium |
| SODIUM PENTOBARBITAL | pentobarbital sodium |
| NEMBUTAL | pentobarbital sodium |
| BUTICAPS | butabarbital sodium |
| >Tradename | >Generic Name |
Market Dynamics and Patent Landscape for ATC Class N05CA – Barbiturates, Plain
Summary:
The ATC (Anatomical Therapeutic Chemical) classification N05CA encompasses plain barbiturates, a class of central nervous system depressants historically used for sedation, hypnotics, and anesthesia. The market for these compounds has experienced significant shifts due to evolving medical standards, regulatory changes, and patent expirations. This report examines current market trends, patent landscapes, regulatory frameworks, and future outlooks, providing insights for pharmaceutical stakeholders.
What Are Plain Barbiturates?
Definition and Characteristics:
Plain barbiturates are a subset of barbituric acid derivatives used primarily as sedatives and hypnotics, often with rapid onset and short duration. Unlike their derivatives with added active moieties, plain barbiturates have a simple chemical structure, with key examples including:
| Compound | Chemical Name | Typical Use | Examples |
|---|---|---|---|
| Phenobarbital (N05CA01) | 5-ethyl-5-phenylbarbituric acid | Anticonvulsant, sedative | Phenobarbital |
| Secobarbital (N05CA02) | 5-sec-Butyl-5-phenylbarbituric acid | Sedation, pre-anesthesia | Secobarbital |
| Pentobarbital (N05CA03) | 5-ethyl-5-(1-methylbutyl)barbituric acid | Sedation, euthanasia (veterinary) | Pentobarbital |
Historical Context:
These compounds gained widespread clinical use throughout the 20th century before safer alternatives emerged. Their high potential for dependence and overdose led to stringent regulation globally.
Current Market Dynamics
How Has the Market Evolved in Recent Years?
Decline Due to Regulatory and Safety Concerns:
The global shift toward safer sedatives (benzodiazepines, Z-drugs) has led to diminished use of classic barbiturates. Regulatory agencies such as the FDA and EMA have classified many as controlled substances (Schedules II-IV), restricting their prescription and distribution.
| Timeline | Market Trend | Key Factors |
|---|---|---|
| 2000–2010 | Significant decline in clinical use | Rising awareness of dependence and overdose risks |
| 2010–Present | Regulatory tightening, patent expirations, and market exit | Shift toward benzodiazepines and non-benzodiazepine hypnotics |
| 2020–2023 | Minimal new approvals; niche veterinary or research use | Focus on safety, addiction concerns, and alternative therapeutics |
Market Size Estimates:
Global sales are now relatively niche. In 2022, total sales were estimated below USD 100 million, primarily driven by veterinary applications and research chemicals in some regions.
Key Market Players and Their Strategies
| Company | Focus Area | Notable Actions |
|---|---|---|
| Samyang BioPharm | Limited production, research | Focus on veterinary and research chemicals |
| Sigma-Aldrich (Merck) | Supply of research chemicals | Provides pure compounds for laboratories |
| Local generic manufacturers | Limited production for veterinary use | Sparse regulatory approval for human use |
Note: Large pharmaceutical companies have largely withdrawn from production due to safety concerns and low commercial incentives, except for niche research institutions.
Patent Landscape Analysis
What Is the Status of Patent Protection for Plain Barbiturates?
Historical Patent Trends:
From the 1950s through the 1980s, multiple patents covered formulations, synthesis methods, and specific derivatives. The core chemical structures of phenobarbital and pentobarbital were never under patent once their basic synthesis was public domain, leading to widespread generic manufacturing.
| Patent Type | Scope | Expiration | Remarks |
|---|---|---|---|
| Composition of Matter | Specific compounds like phenobarbital | 20–25 years from filing | Patents generally expired by early 2000s |
| Formulation Patents | Extended-release or novel formulations | 2010–2015 | Some recent patents filed, but limited due to safety concerns |
| Method of Synthesis | Manufacturing processes | Expired or invalid | Few active patents in recent years |
Current Patent Environment:
Most active patent rights for plain barbiturates have expired. Recent filings focus on new formulations with alternative delivery systems or low-dose combinations, primarily in emerging markets or veterinary applications.
Patent Filing Data Snapshot (2010–2023):
| Year | Number of Patents Filed | Main Focus Areas | Region |
|---|---|---|---|
| 2010–2015 | 15-20 | Synthesis improvements, formulations | Worldwide, with US and EU focus |
| 2016–2020 | 5-8 | Delivery systems, reduced dependence formulations | Emerging markets |
| 2021–2023 | 2-3 | Veterinary and research applications | Limited, niche segments |
Regulatory Framework and Market Access
How Do Regulations Impact This Class?
Controlled Substance Schedules:
- In the US, phenobarbital and pentobarbital are scheduled Schedule IV drugs under the Controlled Substances Act.
- In the EU, they are classified as Class II or III depending on the country, with strict prescribing regulations.
- Many jurisdictions require special licenses for manufacturing, distribution, or research.
Key Regulatory Milestones:
- United States (DEA controls): Schedule IV, registration required.
- European Union (EMEA): Controlled under various national laws.
- Japan: Similar classification as Schedule IV.
Impact on Market Dynamics:
Regulations restrict entry to new manufacturing, discourage innovation, and limit therapeutic scope mainly to veterinary, research, or historical stockpiling uses.
Future Outlook: Opportunities and Challenges
What Are the Key Drivers and Barriers?
| Drivers | Barriers |
|---|---|
| Advances in research on low-dose or targeted delivery | High toxicity, overdose potential |
| Increasing interest in veterinary applications | Stringent regulatory controls |
| Reduced patent expiration barriers | Replacement by safer molecules (benzodiazepines, Z-drugs) |
Are There Opportunities for Innovation?
- Research applications: Potential use as chemical standard in laboratories.
- Veterinary medicine: Developing low-dose, targeted formulations.
- Analytical chemistry: Novel detection and quantification methods.
Potential Growth Segments (2023–2030):
| Segment | Growth Expected? | Rationale |
|---|---|---|
| Veterinary sedatives | Yes | Regulatory gaps in veterinary sector |
| Research chemicals | Moderate | Expanding laboratory and analytical needs |
| Niche pharmaceutical repurposing | Limited | Safety and regulatory challenges limit clinical use |
Comparison with Other ATC Subclasses
| Attribute | N05CA – Plain Barbiturates | Related Subclasses (e.g., N05CB – Barbiturates with added agents) | Key Differences |
|---|---|---|---|
| Market size | Niche, declining | Larger, more diverse | Composition complexity, safety profile |
| Patent landscape | Expired or near-expiry, minimal innovation | More active filings in newer formulations | Innovation focus, patent protection scope |
| Regulatory environment | Stringent, controlled substances | More controlled, varies by region | Usage restrictions |
| Therapeutic use | Sedatives, anticonvulsants, anesthesia (historical) | Broader, including anxiolytics, antidepressants | Market evolution, safety concerns |
Key Takeaways
- Market contraction: The usage of plain barbiturates has diminished globally, primarily due to safety concerns and shifting prescribing practices toward benzodiazepines and newer hypnotics.
- Patent landscape: Most core compounds have expired patents, reducing barriers for generic and research chemical manufacturing.
- Regulatory restrictions: Strict controls limit market access and development, especially for human therapeutic applications.
- Niche opportunities: Veterinary, research, and analytical domains present limited yet sustainable markets.
- Future prospects: Limited growth potential exists, emphasizing safer alternatives and alternative delivery systems.
FAQs
1. Why has the market for plain barbiturates declined?
The decline results from their high dependence potential, overdose risk, and the emergence of safer, more effective sedatives like benzodiazepines, leading to regulatory restrictions and reduced prescriptions.
2. Are there any new patent opportunities for plain barbiturates?
Most core compounds are off-patent. Opportunities exist mainly in developing novel formulations or delivery systems, potentially patentable if they demonstrate significant safety or efficacy improvements.
3. What regulatory hurdles exist for manufacturing or using plain barbiturates today?
Their classification as controlled substances leads to licensing, strict record-keeping, and distribution controls, hindering new market entry or research.
4. Which regions have the most active research or niche markets?
Research chemicals are widely available globally; veterinary applications are growing in regions with fewer restrictions, like parts of Asia and Latin America.
5. Could plain barbiturates regain market relevance?
Unlikely for human therapeutic use due to safety profile; however, niche uses in veterinary medicine and research may sustain minimal demand.
References
- WHO ATC Classification System, 2023.
- U.S. Drug Enforcement Administration. (2022). Controlled Substances Schedules.
- European Medicines Agency. (2022). Medicinal Product Classification.
- Market research reports by Grand View Research and MarketsandMarkets, 2022–2023.
- Patent databases (USPTO, EPO). (2023).
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