General Pharmaceutical Chemistry - GAPL006
Title: Obecná farmaceutická chemie
Guaranteed by: Department of Pharmaceutical Chemistry and Pharmaceutical Analysis (16-16190)
Faculty: Faculty of Pharmacy in Hradec Králové
Actual: from 2024
Semester: winter
Points: 0
E-Credits: 6
Examination process: winter s.:written
Hours per week, examination: winter s.:28/28, C+Ex [HS]
Capacity: unknown / unknown (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:  
Guarantor: doc. PharmDr. Miroslav Miletín, Ph.D.
Examination dates   WS schedule   
Annotation -
Teaching of the subject General Pharmaceutical Chemistry is in the form of lectures and practical exercises. The course is completed by an exam. The subject is closely related to the preceding natural science and medicine based disciplines. It provides information on the important structural prerequisites for pharmaceuticals and the importance and influence of chemical structures, including their modifications and isomerism, on the physical and physicochemical properties of drugs and, consequently, on the pharmacokinetic and pharmacodynamic processes that take place when a drug is administered into the body. Attention is also paid to the issues of drug development, nomenclature, and sources of their acquisition.
Last update: Miletín Miroslav, doc. PharmDr., Ph.D. (14.01.2025)
Course completion requirements -

The course ends with an written exam. Credit must be obtained before the exam. Participation in all seminars and practical exercises and completion of the required tasks during these exercises is required for credit.

Last update: Miletín Miroslav, doc. PharmDr., Ph.D. (17.01.2025)
Literature -

Obligatory:

  • . . In HARTL, JIŘÍ; PALÁT, KAREL. . Farmaceutická chemie I (obecná část) . Praha: Karolinum, 1998, s. -. ISBN 80-7184-619-8..

Recommended:

  • . . In ZIMČÍK, PETR A KOL.. Farmaceutická chemie: návody k praktickým cvičením . Praha: Karolinum, 2009, s. -. ISBN 978-80-246-3382-4..

Last update: Miletín Miroslav, doc. PharmDr., Ph.D. (17.01.2025)
Teaching methods -

Lectures, seminars, practical classes.

Last update: Miletín Miroslav, doc. PharmDr., Ph.D. (17.01.2025)
Requirements to the exam -

The course ends with an examination. Credit must be obtained before the examination. Attendance at all seminars and practical exercises and completion of the required assignments during these exercises is required for credit.

The subject of the examination is the information contained in the scripts and in the course materials and Moodle.

Last update: Miletín Miroslav, doc. PharmDr., Ph.D. (17.01.2025)
Syllabus -

Lecture topics:
Development of chemical drugs
Sources of new drugs
Nomenclature of drugs
Structural factors influencing drug action
Modifications of structure, homology, analogies and their relevance to drug action
Importance of physicochemical properties for drug action
Importance of metabolism for drug action
Prodrugs
Biological drugs - structural types and resulting physicochemical and pharmacokinetic properties.

The seminars discuss the importance of struture and resulting physicochemical properties on drug action as well as influence of the stereochemical arrangement of the drug molecule in relation to the drug-organism interaction (construction of spatial models, spatial modelling using PC).

Practical exercises are focused on the study 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.). The practical exercises include work with scientific literature.

Last update: Miletín Miroslav, doc. PharmDr., Ph.D. (17.01.2025)
Learning resources -

Moodle

Teaching texts and presentations in the Study Materials folder.

Last update: Miletín Miroslav, doc. PharmDr., Ph.D. (17.01.2025)
Learning outcomes -

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.
  • Explain the basic structural differences between chemical and biological drugs, and the resulting physicochemical and pharmacokinetic properties.

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)