Course code:
454B2
Course name:
Mechanisms of Action of Physiologically Active Compounds

Academic year:

2026/2027.

Attendance requirements:

There are no requirements.

ECTS:

4

Study level:

graduate academic studies

Study program:

Biochemistry: 1. year, winter semester, elective (E53B2) course

Teacher:

Milan R. Nikoliæ, Ph.D.
full professor, Faculty of Chemistry, Studentski trg 12-16, Beograd

Assistant:

Simeon L. Miniæ, Ph.D.
assistant professor, Faculty of Chemistry, Studentski trg 12-16, Beograd

Hours of instruction:

Weekly: two hours of lectures + two hours of labwork (2+0+2)

Goals:

Fundamentally, this is a pharmacology course, but one approached from a biochemical perspective. Building on an understanding of the pathophysiological changes in the human body resulting from disrupted systemic homeostasis, specifically regarding biosignaling and metabolic regulation, students will explore the interconnections between these processes and the potential for pharmacological modulation to restore functional homeostasis. Key aspects such as administration, transport, distribution, and metabolism, as well as the molecular mechanisms of action of modern "blockbuster" drugs, will be illustrated through examples involving psychopharmacology and therapies for hyperlipidemia, hypertension, diabetes, and chemotherapy. The final section of the course will address the potential applications of nanotechnology in modern medicine.

Outcome:

Upon successful completion of the course, a student will be able to independently and comprehensively consider the effects of biologically active substances (drugs and other xenobiotics), mechanisms of drug action, and strategies of drug transport in target tissues.

Teaching methods:

Lectures, experimental exercises, and seminar paper.

Extracurricular activities:

—

Coursebooks:

Main coursebooks:

  1. New Guide to Medicine and Drugs: The Complete Home Reference, 11th Edition (2021). DK Publishing. ISBN-13: 978-0241471029.
  2. Drug Metabolism: Current Concepts, 2005th Edition (2006). Springer. ISBN-13: 978-1402050282.
  3. Clinical Pharmacology Made Ridiculously Simple, 5th Edition, by James Olson (2019). MedMaster. ISBN-10: 1935660373.
  4. Power Point Presentations from lectures.

Supplementary coursebooks:

  • Selected review papers.

Additional material:

http://www.chem.bg.ac.rs/~mnikolic

  Course activities and grading method

Lectures:

10 points (2 hours a week)

Syllabus:

Thematic units:

– Modulation of signal transduction pathways in the regulation of impaired homeostasis: general principles of action of physiologically active substances (pharmaceutical drugs and natural products)

– Routes of drug entry into the body and protein systems for drug biotransport

– Drug metabolism and factors on which drug action depends

– Drugs for the cardiovascular system (antihypertensives; beta-blockers; antiarrhythmics; vasodilators; blood thinners): structures, properties, mechanisms of action

– Fundamentals of psychopharmacology: structures, properties and mechanisms of action of antipsychotics, antidepressants and psychostabilizers

– Drugs for lowering blood lipid content (antilipemics): structures, properties, and mechanisms of action of statins, fibrates and niacin, bile acid sequestrants, cholesterol absorption inhibitors

– Drugs for lowering blood glucose content; structures, properties, and mechanisms of action of oral antidiabetics (insulin secretagogues, insulin sensitizers, alpha-glucosidase inhibitors) and protein therapeutics (insulin, GLP-1 receptor agonists)

– Malignant cell: structure and principles of action of chemotherapeutics (alkylating agents, antimetabolites, antibiotics, antimitotic drugs, hormonal agents)

– Natural products as drugs (as phytotherapeutics): selected structures and mechanisms of action

– Molecular nanomedicine and nanorobots

Labwork:

20 points (2 hours a week)

Syllabus:

Pleiotropic effects (those independent of the primary pharmacological purpose) of physiologically active substances: determination of the antioxidant potential of representatives from a selected class of drugs and herbal teas, and/or the impact of selected drugs on the structure and activity of specific blood proteins. Depending on the number of students enrolled in the course, the work in the 2026/2027 academic year would involve atorvastatin (one of the most frequently prescribed statins, with excellent results in reducing the risk of heart disease) and rosuvastatin (a statin particularly effective at achieving target cholesterol levels at lower doses), as well as two GLP-1 receptor agonists: semaglutide (the drug Ozempic) and tirzepatide (the drug Mounjaro).

Semester papers:

30 points

Oral exam:

40 points