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Course Detail

Course Name Basic Pharmacological And Toxicological Screening Methods
Course Code MPC205T
Program M. Pharm. Pharmaceutical Chemistry
Semester 2
Credits 2
Campus Kochi

Scope

SCOPE: The course offers a basic understanding of the techniques and methodologies used to evaluate the pharmacological properties of newly synthesized drugs. This course covers fundamental principles, screening techniques, and applications in drug discovery and development. Students will learn about the importance of pharmacological screening in identifying potential drug candidates. It is designed to provide students with a thorough understanding of in vitro screening processes, molecular and cellular techniques, and the ethical and regulatory considerations involved. Through a combination of theoretical lectures and case studies, students will develop the skills necessary for planning a biological screening for their synthesised compounds. By the end of the course, students will have a comprehensive understanding of pharmacological screening techniques, and regulatory and ethical considerations necessary for pharmacological research and development.

Objectives and Outcomes

By the end of this course, students shall be able to

KNOWLEDGE

K1 Describe the basic concepts and objectives of pharmacological screening.

K2 Identify the key regulatory frameworks governing pharmacological research.

K3 Recognize the techniques used to investigate the mechanism of action of a compound

K4 Outline the steps involved in conducting Pharmacological Screening of a synthesised compound

K5 Summarize the components and significance of Pharmacological Screening

K6 Identify alternate models in Pharmacological Screening

SKILL

S1 Perform initial biological screening assays to evaluate the biological activity of compounds

S2 Develop protocols that comply with Regulatory Frameworks and Ethical Guidelines

S3 Execute selectivity testing of compounds against off-targets

S4 Assess compound toxicity and interpret the results to evaluate safety profiles.

S5 Execute efficacy studies in animal disease models

S6 Develop safety study protocols, incorporating alternate models

ATTITUDE

A1. Develop a strong commitment to ethical conduct in pharmacological research

A2. Foster a sense of integrity and responsibility in conducting and reporting scientific research.

A3. Cultivate critical thinking skills to interpret complex pharmacological data and make informed decisions.

A4. Encourage collaboration and teamwork in laboratory and research settings, recognizing the value of diverse perspectives.

A5. Promote professionalism in all aspects of pharmacological research, including interactions with colleagues, adherence to deadlines, and presentation of findings.

A6. Encourage innovation and creativity in developing new screening techniques and approaches to drug discovery.

LECTURE-WISE CONTENTS:

Each unit should include case studies or research articles related to Screening of Synthesized Drugs.

Unit 1: Introduction 6 hours

Need for Pharmacological Screening, GLP practices, CCSEA guidelines to conduct experiments on animals. Need of control and types of control in pharmacological studies.

Unit 2: In Vitro Studies 12 hours

Initial Biological Screening: Enzyme inhibition, Receptor binding assays, and Cell-based assays and their significance.

Dose-Response Studies: Determination of the concentration-response relationship to establish the potency and efficacy of the compound. Calculate IC50 or EC50 values.

Investigate the mechanism of action: Enzyme kinetics studies, Western blotting, RT-PCR for pathway analysis

Selectivity and Toxicity Testing: selectivity of the compound against off-targets using high- throughput screening or competitive binding assays. Cell viability assays (e.g., MTT, LDH release, SRB).

Invitro stability studies.

Unit 3: In Vivo Toxicity Studies 12 hours

Toxicology Studies: Criteria for conducting toxicity studies. OECD guidelines for conducting various toxicity studies – Acute, sub-acute, and chronic oral, dermal, and inhalational toxicity studies. (4 hrs)

Acute eye irritation studies and skin irritation studies. (1hr)

Reproductive toxicity studies – Male & Female reproductive toxicity studies and teratogenic studies. (3 hrs)

Genotoxicity studies – Ames Test, Micronucleus & chromosomal aberration studies; Carcinogenicity studies. (3 hrs)

ASSIGNMENTS

  1. CCSEA guidelines
  2. Literature review on small molecule synthesis studies involving Receptor Binding assays
  3. Toxicity studies of synthesised molecules
  4. Requirements for Cell Culture Studies
  5. Procurement and Handling of cell lines
  6. Alternate methods of toxicity testing

Text Books / References

REFERENCE BOOKS

  1. G. Vogel and W. H. Vogel, “Drug Discovery and Evaluation: Pharmacological Assays,” 2nd Edition, Springer Ver Lag Berlin Heidelberg, New York, 2002
  2. Laurence Brunton, Bjorn Knollman, Randa Hilal-Dandan, Goodman and Gilman’s The Pharmacological Basis of Therapeutics, 13th Edition, McGraw Hill Professional, 2017

JOURNALS

European Journal of Medicinal Chemistry (Elsevier) Journal of Medicinal Chemistry (ACS)

British Journal of Pharmacology (Wiley) Clinical Pharmacology & Therapeutics (Wiley)

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