Journal name: World Journal of Pharmaceutical Research
Original article title: Ester prodrug of paracetamol
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Subtitle: synthesis, characterization and evaluation
Original source:
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Arun Parashar
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Ester prodrug of paracetamol
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
Paracetamol is a widely used medication for pain and fever relief but is also a leading cause of acute liver failure in several countries, including the United States and the United Kingdom. Overdoses can lead to severe liver damage, primarily due to the formation of a toxic metabolite, N-acetyl-p-benzoquinoneimine (NAPQI), which depletes glutathione, an important antioxidant in the liver. This study aimed to design and evaluate a safer paracetamol analog in the form of a prodrug that could potentially mitigate hepatotoxicity while retaining therapeutic effects.
Hepatotoxicity and Glutathione Preservation
The synthesized paracetamol prodrug derived from alanine demonstrated significant hepatoprotective properties. It effectively prevented the rise in liver enzymes typically associated with hepatotoxicity. Notably, it preserved glutathione levels in the liver, which is crucial for detoxification processes. This attribute stands out as it offers a protective mechanism against the oxidative stress caused by paracetamol's toxic metabolite.
Gastroprotective Effects
In addition to hepatoprotection, the prodrug exhibited gastroprotective effects, reducing gastric lesions more effectively than paracetamol itself. Given that gastrointestinal damage is a common concern associated with many analgesics, this aspect of the prodrug provides a potential therapeutic benefit by minimizing the risk of gastric complications while delivering pain relief.
Analgesic and Antipyretic Efficacy
While the prodrug showed positive outcomes in gastroprotection and hepatoprotection, its analgesic and antipyretic effects were found to be inferior when compared to those of paracetamol. The prodrug resulted in reduced efficacy in pain relief and fever reduction, raising questions about its overall therapeutic benefit relative to paracetamol.
Conclusion
The paracetamol prodrug synthesized from alanine showcased promising benefits in hepatoprotection and gastroprotection; however, its therapeutic efficacy was compromised compared to paracetamol. This research highlights the potential for designing safer analogs of paracetamol with reduced hepatotoxicity, paving the way for future investigations that could lead to the development of non-toxic and therapeutically effective alternatives.
FAQ section (important questions/answers):
What was the main objective of the study on paracetamol prodrug?
The study aimed to design and evaluate a safer analog of paracetamol, focusing on reducing hepatotoxicity while preserving its analgesic and antipyretic effects.
How was the paracetamol prodrug synthesized in the study?
The synthesis involved three main steps: protecting the amino group of an amino acid, reacting it with paracetamol, and then removing the protection using trifluoroacetic acid and dichloromethane.
What are the key findings related to the prodrug's analgesic effects?
The prodrug demonstrated a 36% inhibition in writhing tests compared to 53.3% by paracetamol, indicating reduced analgesic efficacy.
What gastroprotective effects did the prodrug display?
The prodrug showed excellent gastroprotective effects, reducing gastric lesions by 20.3% compared to the control group.
How did the prodrug perform regarding hepatotoxicity when compared to paracetamol?
The prodrug exhibited hepatoprotective effects, preventing the rise in liver enzymes and preserving glutathione levels, which paracetamol significantly depletes.
What conclusion was drawn regarding the prodrug's therapeutic efficacy?
Although the prodrug showed excellent hepatoprotective and gastroprotective effects, its overall therapeutic efficacy was compromised compared to paracetamol.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Ester prodrug of paracetamol”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.
1) Drug:
A drug is a chemical substance used for medical treatment, diagnosis, or prevention of diseases. In this study, paracetamol is a widely consumed analgesic and antipyretic drug. However, its hepatotoxic effects prompted the research into a prodrug formulation, aimed at reducing its associated risks while maintaining therapeutic benefits.
2) Activity:
In pharmacological terms, 'activity' refers to the efficacy of a drug in producing a desired therapeutic effect. The study measured various activities including analgesic, antipyretic, and gastroprotective activities. Understanding these activities is crucial for evaluating the performance of the new prodrug compared to paracetamol and determining its suitability in treatment.
3) Ulcer:
An ulcer is a sore that develops on the lining of the stomach or intestines, often caused by increased gastric acid or NSAIDs. The research included evaluating the prodrug's capacity to heal gastric lesions, exploring its gastroprotective properties, and addressing the common side effects associated with many analgesics, including paracetamol.
4) Post:
'Post' in this context refers to events or measurements taken after a specific intervention or treatment, such as drug administration. The study monitored post-drug administration effects, particularly for antipyretic activity and ulcer healing, highlighting the timing of these effects in evaluating the prodrug's therapeutic profile.
5) Pharmacological:
Pharmacological relates to the study of drugs' effects on biological systems. This research explored the pharmacological properties of the paracetamol prodrug, assessing its efficacy, including analgesic and hepatoprotective effects. Understanding these properties is essential for developing safer medication options that retain necessary therapeutic functions while minimizing adverse effects.
6) Discussion:
The discussion section of a research paper provides context for the findings, interpreting results and contrasting them with existing literature. Here, it analyzes the prodrug's lower therapeutic efficacy compared to paracetamol but emphasizes its hepatoprotective and gastroprotective benefits, encouraging future research for improved formulations.
7) Toxicology:
Toxicology studies the adverse effects of substances on living organisms. In this study, toxicology plays a central role because paracetamol is known to cause liver damage. The importance of developing a prodrug lies in combating these toxic effects while retaining the beneficial therapeutic properties of paracetamol.
8) Science (Scientific):
Science is the pursuit of knowledge through systematic observation and experimentation. This study embodies scientific inquiry by exploring the synthesis and evaluation of a prodrug as a means to address the limitations of paracetamol. It reflects the ongoing effort to advance therapeutic strategies and improve patient safety.
9) Substance:
A substance refers to matter with a specific chemical composition and properties. In this study, the prodrug and paracetamol are key substances evaluated for their pharmacological effects. Investigating the properties of these substances helps discern their therapeutic benefits and risks, vital for medical applications.
10) Toxicity:
Toxicity is the degree to which a substance can harm organisms. In the context of this study, the toxicity of paracetamol is a significant concern. The prodrug was designed to minimize toxicity while maintaining efficacy, emphasizing the need for medications that are therapeutic yet safe for patients.
11) Medicine:
Medicine is the science and practice of diagnosing, treating, and preventing disease. This research centers on the development of a safer medicine by creating a paracetamol prodrug, intended to reduce the risk of liver toxicity associated with traditional paracetamol usage while retaining its analgesic properties.
12) Water:
Water is essential for biological processes and serves as a solvent in many pharmaceutical formulations. In this study, it relates to the hydration of animal subjects during experiments and the administration of substances, underscoring the importance of fluid management in pharmacological research, especially in vivo.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Ester prodrug of paracetamol’. Further sources in the context of Science might help you critically compare this page with similair documents:
Statistical analysis, Significantly different, Continuous effort, Therapeutic efficacy, Analgesic effect, Hepatic failure, Hepatoprotective effect, Molecular weight, Animal studies, Antipyretic effect, Paracetamol overdose, Glutathione depletion, Pain and fever, Liver enzyme, Therapeutic benefit, Gastroprotective effect, Amino acid sequence, Toxic metabolite, Therapeutically active, Glutathione level, In-vivo activities, Phthalic anhydride, Upper Gastrointestinal Complications.