Course: Pharmacochemistry

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Course title Pharmacochemistry
Course code UOCHT/C068A
Organizational form of instruction Lecture
Level of course unspecified
Year of study not specified
Semester Winter and summer
Number of ECTS credits 5
Language of instruction English
Status of course unspecified
Form of instruction Face-to-face
Work placements This is not an internship
Recommended optional programme components None
Course availability The course is available to visiting students
Lecturer(s)
  • Imramovský Aleš, prof. Ing. Ph.D.
Course content
Object of pharmaceutical chemistry, basic notions - pharmacology, pharmacognosy, galenic pharmacy, medicinal drug, form of medicinal drug. Basic principles of general pharmacology - way of administration, fate of drug in organism: absorption, transport and distribution, metabolism (bio-transformations - oxidation, reduction, hydrolysis, conjugation, non-enzymatic transformations), excretion. Effects of medicinal drugs - specific and non-specific effect - relationships between structure and effect. Problems of research and development of new pharmaceuticals. European and Czech Pharmacopoeias, classification of drugs from pharmacological standpoint. General anaesthetics - mechanism of action. Syntheses of fluorine-containing inhalation anaesthetics (halothane), general intravenous anaesthetics (thiopental). Hypnotics and sedatives - effect and application. Syntheses of selected hypnotics of the 1st to 3rd generations. Psycho-pharmaceuticals - classification according to pharmacological effect - parameters of human psychic (ways of affecting the brain metabolism, neurotransmitters). Syntheses of representatives of individual groups: nootropic drugs (piracetam, cinnarizine), neuroleptic drugs, phenothiazine derivatives and their analogues, anxiolytics (benzodiazepins), drugs relieving anxiety states (benzodiazepins), antidepressants, derivatives of dibenzo[b,f]azepin and their analogues. Controlled substances, problems of addictive drugs and habit-forming medicinal drugs, derivatives of morphine (heroin), stimulants (amphetamine, pervitin), psychedelic drugs (mescaline, psilocybin, LSD, extasy, phencyclidine), legal restrictions in production and distribution of these compounds and their precursors. Anti-epileptic drugs - effect, total syntheses of representatives of the following groups: hydantoins, glutarimides, succinimides, iminostilbenes (carbamazepin, mesantion, phenytoin). Anti-Parkinsonism drugs - treatment of mobility coordination disorders (ataxy), tremor (L-dopa, amantadin, trihexylphenidyl). Central analeptics - sources of total syntheses (caffeine, camphor, pentazol, nikethamid, bemegrid). Analgesics - principles of analgesia (morphine and its derivatives, morphinans, derivatives of 6,7-benzomorphane and 4-phenylpiperidine). Analgesic-antipyretic substances (paracetamol, salicin, aspirin, methyl salicylate). Antihistaminics - effect of histamine, metabolism - syntheses of derivatives of benzo[b,f]thiepin, ethylenediamine, piperazine (dithiaden, zyrtec, xyzal). Local anaesthetics - tropane alkaloids - cocaine effects, synthetic substitutes (lidocaine, trimecaine, procaine, tetracaine, cinchocaine). Medicinal drugs for blood circulation system: cardiotonic drugs (digoxin, digitoxin). Sympathomimetic agents - influence upon vegetative nervous system (noradrenaline, adrenaline, ephedrine). Anti-arrhytmic agents - tuning of pulse rhythm (trimepranol, propranolol). Anti-hypertensive agents - influencing of blood pressure (substances blocking the sympathetic division, inhibition of ACE, ?-blockers, blockers of calcium channels; nifedipin, methyldopa, irbersartan, enalapril). Medicinal drugs affecting blood coagulation (heparin, pelentan, warfarin). Other medicinal drugs for blood circulation system (glycerol trinitrate, pentaerythritol tetranitrate, sildenafil-(viagra)). Spasmolytics - mechanism of action on unstriped muscles (syntheses: thiospasmine, adiphenine, papaverine, drotaverine). Antiphlogistics - inhibiting of inflammatory reactions - anthranilic acid derivatives, derivatives of arylacetic acids - ibobrufen). Laxatives (laxyl). Anthelmintics (niklosamid, thiabendazol). Antineoplastics (cancerostatics, cytostatics), alkylation agents (analogues of N-yperite), antimetabolites (modified bases of nucleic acids: thymine, uracil, cytosine, adenine), other antineoplastics (daunorubicin, prokarbazin, platidiam). Problems of chemical cancerogenesis, metabolic activation (benzidine, o-anisidine, naphthylamines.

Learning activities and teaching methods
Monologic (reading, lecture, briefing), Dialogic (discussion, interview, brainstorming)
Learning outcomes
The education of middle-level management staff and technological specialists for pharmaceutical and chemical firms producing small-scale chemical specialties requires interdisciplinary preparation with emphasis laid on practical aspects. Apart from basic knowledge in chemistry (inorganic, organic, physical, analytical) the required knowledge and skills include bioorganic chemistry, biochemistry, pharmacochemistry and basics of material science covering materials used in medicine. Furthermore, this Study Program involves courses in computer technology (IT), chemical and pharmaceutical information systems, processes and apparatus used in pharmaceutical chemistry, economics and management. An integral part of the students' training is development of their communication skills and solving problems in dealing with people. Those interested from among students are offered certified study composed of three specialized subjects lectured in English ("General and Inorganic Chemistry", "Organic Chemistry" and "Chemical Engineering").
Absolvents are able Applicate Strategy for Organic Drug Synthesis and Design.
Prerequisites
Knowledge from Organic Chemistry as well as Basic of Organic Synthesis are prerequisites for successful completion of the course. Pharmacochemistry = Chemistry of Synthetic drugs or their intermediates.

Assessment methods and criteria
Oral examination, Written examination

Understanding and active knowledge of the topics covered by the lectures.
Recommended literature
  • Holý, Antonín. Principy bioorganické chemie ve vývoji antivirotik a cytostatik. Olomouc: Univerzita Palackého, 2004. ISBN 80-244-0855-4.
  • Lednicer D. Strategies for Organic Drug Synthesis and Design. ISBN 9780470190395.
  • Paleček J., Hampl F.:. FARMAKOCHEMIE, skripta 2.vydání, VŠCHT Praha 2002,[ISBN 80-7080-495-5].. ISBN 80-7080-495-5.
  • Vardanyan, R. Synthesis of Essential Drugs. Elsevier Science: Tucson, USA. ISBN 978-0-444-52166-8.


Study plans that include the course
Faculty Study plan (Version) Category of Branch/Specialization Recommended year of study Recommended semester