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Pharmaceutical Chemistry I - GF341
Title: Farmaceutická chemie I
Guaranteed by: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis (16-16190)
Faculty: Faculty of Pharmacy in Hradec Králové
Actual: from 2023
Semester: winter
Points: 0
E-Credits: 4
Examination process: winter s.:
Hours per week, examination: winter s.:42/70, C [HS]
Capacity: unlimited / 240 (unknown)
Min. number of students: unlimited
4EU+: no
Virtual mobility / capacity: no
Key competences:  
State of the course: taught
Language: Czech
Teaching methods: full-time
Level:  
Note: deregister from the credit exam date if a requisite was not fulfilled
Guarantor: prof. PharmDr. Martin Doležal, Ph.D.
Comes under: 3.ročník 2024/25 Farmacie
Co-requisite : GF339
Pre-requisite : GF141, GF293, GF299
Is co-requisite for: GF342, GF244, GF339, GF344
Annotation -
Pharmaceutical Chemistry is a specific pharmaceutical subject representing the link between chemical and biological disciplines. Its task is to provide students with a complex understanding of drug and auxiliary substance chemistry. The drugs are studied from the point of view of their rational selection and preparation, quality criteria, suitable ways of storage, structure-activity and structure-metabolism relationships, and practical usage. The brief information concerning mechanisms of drug action covered in this subject forms the basis for a more profound study of this topic in pharmacology. This subject belongs to the state final examination group of subjects.
Last update: Doležal Martin, prof. PharmDr., Ph.D. (18.02.2025)
Course completion requirements -

mastering the subject matter according to the syllabus.

Last update: Doležal Martin, prof. PharmDr., Ph.D. (18.02.2025)
Literature -

Obligatory:

  • . . In Williams, David A., Lemke, Thomas L. (eds.). Principles of medicinal chemistry . Baltimore: Lippincott Williams & Wilkins, 2002, s. -. ISBN 0-683-30737-1..

Last update: Doležal Martin, prof. PharmDr., Ph.D. (18.02.2025)
Syllabus -

Definition and characterization of the subject

Historical development of pharmaceutical chemistry

Sources of new drugs

Drug nomenclature

Structural factors affecting biological activity

Drug structure modifications

Physicochemical properties in relation to biological activity

Drugs affecting the central nervous system:

  • General anesthetics
  • Sedative-hypnotics
  • Anticonvulsants
  • Neuroleptics
  • Anxiolytics
  • Antidepressants
  • Psychostimulants
  • Hallucinogens
  • Antiparkinsonian agents
  • Opiate analgesics
  • Nonopiate analgesics
  • Nonsteroidal anti-inflammatory agents
  • Antiemetics
  • Antitussives
  • Expectorants

Drugs affecting the peripheral nervous system

  • Local anesthetics
  • Skeletal muscle relaxants
Last update: Doležal Martin, prof. PharmDr., Ph.D. (18.02.2025)
Learning outcomes -

Basic learning objectives Pharmaceutical chemistry builds on the preparatory disciplines of science and medicine. It provides a comprehensive picture of drugs and excipients of a chemical nature, necessary for mastering other related disciplines, in particular pharmaceutical analysis and pharmacology. From this perspective, it is possible to pharmaceutical chemistry can be seen as a partly interdisciplinary subject with a certain connecting function between chemical, biological and specifically pharmaceutical subdisciplines. Broader attention is given to the importance and influence of chemical structures, including their modifications, on the pharmacokinetic and pharmacodynamic processes that take place when a drug is administered into the body. It also looks at the causal relationship between chemical structure and drug stability, as well as the prerequisites for possible interactions (chemical incompatibilities). Pharmacochemistry classifies drugs according to the nature and type of their use, i.e. from a functional point of view. Classification scale chemical remains in second place. This gives the possibility of comparing drugs that are similar in clinical use, although they are different in mechanism of action or chemistry. The chosen classification method not only demonstrates the logical link between pharmaceutical chemistry and pharmacology, but is also significant in terms of practice. It corresponds to the now commonly used classification of drugs within their anatomical-therapeutic-chemical classification (ATC). A specific area of pharmacochemistry is the study of the relationships between chemical structure and biological properties of chemically defined substances and the use of this knowledge for design and development of new, more effective and safer substances. Mastery of pharmaceutical chemistry, together with other knowledge, allows in many cases not only to make predictions biological activity but also other properties needed for the handling, preservation and practical use of pharmaceuticals. PATRICK, GRAHAM L. An introduction to medicinal chemistry. Oxford: Oxford University Press, 7th Ed.,
2023, 960 p. ISBN 9780198866664.
LEMKE, THOMAS, WILLIAMS, DAVID A. ROCHE, VICTORIA F. (EDS.). Foye´s principles of medicinal chemistry.
Philadelphia; Baltimore: Lippincott Williams & Wilkins, 2013, 1500 s. ISBN 978-1-4511-7572-1.
WILSON, CHARLES OWENS, GISVOLD, OLE. Textbook of organic medicinal and pharmaceutical chemistry.
Philadelphia: Lippincott Williams & Wilkins, 2004, 991 s. ISBN 0-7817-3481-9.

General Pharmaceutical chemistry

Builds on the preparatory disciplines of natural and medical sciences. It provides basic information on the structure of drugs and, where appropriate, excipients, necessary for understanding the physical, physicochemical and chemical properties of drugs and their resulting pharmaceutical-technological and pharmacokinetic properties.
After completing the course, students should be able to answer the following assignments:

  • Name the historical stages in the development of chemical drugs.
  • Describe historical and current sources of new drugs.
  • Define the basics of drug nomenclature (INN, other types of names).
  • Name the basic chemical bonds in drug molecules, and especially their properties important for understanding the behaviour of drugs of natural and synthetic origin in pharmaceutical products and in the human body.
  • Describe features of the structure of drugs that influence their pharmacokinetic properties and interactions with target sites in the body.
  • Indicate what modifications are made to the structure of drugs and their importance to the behaviour of drug molecules or the effect of drugs.
  • Explain which functional groups have acidic and basic properties, how we can affect the acidity and basicity of drug molecules, and what relevance these properties have to drug action.
  • Explain which substituents have lipophilic and which have hydrophilic properties, how we can affect the lipophilicity of drug molecules, and what importance these properties have for drug action.
  • Describe what types of isomerism you are familiar with and how they can affect drug action.
  • Name the basic steps in drug metabolism and their effect on pharmacokinetics.
  • Define prodrugs and by what bonds (modifications) of the drug molecule are used to prepare them.

Practical classes focus on experiments and demonstrations of the influence of selected physicochemical properties on the effect of drugs (increase in aqueous solubility, decrease in aqueous solubility, increase in lipid solubility, adsorption, basicity and acidity, etc.), as well as the study of the stereochemical arrangement of the drug molecule in relation to drug-organism interaction.
The acquisition of knowledge of general pharmaceutical chemistry together with other knowledge helps to assess or predict the behaviour of drug molecules in pharmaceutical dosage forms and after administration to the body. This knowledge is also important for the proper handling, storage and practical use of pharmaceuticals.

Last update: Miletín Miroslav, doc. PharmDr., Ph.D. (05.03.2025)
 
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