PHARMACEUTICAL CHEMISTRY QUESTIONS OF THE FINAL EXAMINATION, 2011/2012 1. Sedato-hypnotics and anxiolytics. Classification. Representatives of barbituric acid derivatives and benzodiazepines. Structure, chemical and physical characteristics, structure-activity relationships. 2. Main groups of major analgetics. Morphine and its semi-synthetic derivatives. Main representatives of agonist, partial agonist and antagonist derivatives. Structure, chemical, physical and pharmacological characteristics. 3. Minor analgetics and non-steroid anti-inflammatory agents. Classification and structural characterization. Chemical and physical characteristics. 4. Neuroleptics. Classification. Phenothiazines and related compounds. Major representatives of atypical neuroleptics. Structure, chemical and physical characteristics, structure-activity relationships. 5. Antidepressive agents. Classification. More detailed about the tricyclic compounds and SSRI drugs. Structure, chemical and physical characteristics, structure-activity relationships. 6. Representatives of parasympathomimetic and parasympatholytic drugs. Structure, chemical and physical characteristics and their interactions with the receptor. 7. Sympathomimetic drugs and their major representatives. Selective ß2-agonists, as brochodilators. Structure, chemical and physical characteristics and their relationship with the activity. 8. Local anaesthetics, classification, major representatives. Structure, chemical and physical characteristics, structure-activity relationships. 9. Cardiac glycosides, structure and properties of main representatives. Mechanism of action. 10. Antihypertensive agents. Classification. More detailed about the ACE-inhibitors. Structure, chemical and physical characteristics. Criteria of the receptor-binding. 11. Classification of antiarrhythmic agents, their main representatives. Chemical properties, structure-activity relationship. 12. Antianginal drugs. Main representatives of nitrites and nitrates. General structure of 1,4-dihydropyridines, some representatives. Structure, chemical and physical properties. 13. Cardiovascular agents. Anticoagulants. Vitamin K antagonists, structures, properties, analysis. Heparine, structure, properties. 14. Vitamines. Structure of A- and D-vitamines, chemical and physical characteristics. Structure of vitamine B1, B2 ,B6 and C. Chemical and physical characteristics. 15. Classification of steroid hormones. Main representatives of corticosteroids. Chemical and physical characteristics. 16. Diuretics. Classification. Saluretics and loop diuretics in detail. Structures, properties, mechanism of action, analysis. 17. Classification of chemotherapeutic drugs. China-alkaloids fluoroquinolones. Structure, chemical and physical characteristics. and synthetic 18. Classification of sulfonamides. Structural elements of antibacterial sulfonamides. Chemical, physical and pharmacological properties. 19. General structure of -lactam antibiotics, classification and major representatives. Reactivity, physical and chemical characteristics. 20. Tetracycline-type antibiotics. Structure of main representatives, chemical and physical properties. Chloramphenicol, structure and properties. 21. Antihistamines, classification and their major representatives. Structure, chemical and physical characteristics. New generation non-sedative drugs. 22. Lipophilicity in drug research. Methods of the determination of the partition coefficient. 23. Basicity of drugs and bio-molecules in terms of macro-and microconstants. Calculation of the pH-dependent concentration of the various macro- and microforms. 24. Determination of the protonation constants of bases and dissociation constants of acids. Calculation of the pH-dependent number of bound hydrogen ions and the charge of the molecule. 25. Thermodynamic and structural preconditions of drug-receptor interactions. Complementarity and bioisosteric substitutions. Bonding types and energies of drugreceptor interactions. 26. Theory and practice of the impurity tests in the Ph. Eur. (heavy metals, iron, arsenic, chlorides). 27. Theory and practice of the impurity tests in the Ph. Eur. (calcium, potassium, ammonium, phosphates). 28. The practice of the pH measurement in the Ph. Eur. Examples for the application of the potentiometric titrations in the Ph. Eur. 29. Aspects of validation of analytical processes, the calculated parameters, comparison with practical examples (TLC, HPLC, titration). 30. Special aspects in the qualitative and quantitative analysis of drug preparations. 31. Application of chemical identification reactions in the analysis of pharmaceutical preparations. 2 32. Determination of organic bases in drug preparations using non-aqueous titrations. Examples for the measurements of bases in the presence of other basic components, neutral compounds and acids. 33. Determination of organic acids in drug preparations. Examples. 34. Spectrophotometric determination possibilities of two analytes. Theory and practice of difference spectrophotometry. 35. NMR. Spin, precession, Larmor frequency, relaxations, FID, chemical shift, multiplicity, and couplings. The NMR spectrometer. 36. Theory and practice of thin-layer chromatography. Application in the qualitative and quantitative drug analysis. 37. Theory and practice of high performance liquid chromatography. Main chromatographic parameters. Application in the drug analysis. 38. The steps of a mass spectrometric measurement. Application areas of MS. 49. Theory and practice of capillary electrophoresis. 40. Stages and system of drug research. Finding new chemical entities by combinatorial chemistry. Components of drug mixtures. The actual composition will be available at the exam. acetylsalicylic acid aminophenazone ascorbic acid benzocaine caffeine chloramphenicol codeine hydrochloride codeine phosphate ephedrine hydrochloride hexachlorophene hexobarbital homatropine methylbromide hydrocortisone acetate lidocaine metamizole sodium papaverine hydrochloride paracetamol phenobarbital sodium progesterone quinine sulphate resorcinol salicylic acid sucrose tetracaine hydrochloride theophylline 3