First the structure of therapeutics and their interactions with organisms will be discussed at a general level, consequentially individual groups of therapeutics will be discussed in details (types, structure, action mechanisms, properties, particular substances). This course is designed for students of the Faculty of Science. The fundamental knowledge of chemistry, at least, especially that of organic chemistry, is expected. 1. General pharmacology a) Pharmacokinetics Influence of the organism on the therapeutics: adsorption, membrane permeation, distribution, metabolism, excretion b) Pharmacodynamics Influence of the therapeutics on the body: therapeutics with non-specific action vs. therapeutics with specific action (drug target structures) c) Adverse effects -- classification, types d) Therapeutics interactions -- pharmaceutical, pharmacokinetic and pharmacodynamic interactions 2. General pharmaceutical chemistry the subject, theraputics development, nomenclature, new therapeutics sources structural factors, structure modifications physico-chemical properties of therapeutics 3. General and local anesthetics a) General aenesthetics -- inhalational (gases and volatile substances) vs. intravenous (solid substances) Characterisation of general anesthesia b) Local anesthetics - ester, amide and anilide anesthetics Types of local anesthesia, their usage in common medical practice 4. Antidepressants, thymoprophylactics Treatment of affective disorders, monoamine theory of depression a) Thymoleptics - tricyklic antidepressants, heterocyclic antidepressants, SSRI, SNRI, NaSSA b) Thymoeretics - monoamine oxidase inhibitors (MAO) c) Thymoprophylactics - lithium 5. Opioid analgesics Definition of pain, types of opioid receptors Basic structure - 3-phenylpropylamine and particular structural types of opioid analgesics Morphine and its derivatives 6. Nonsteroidal antiphlogistics Pathophysiology of inflammation - prostaglandins, COX-1 and COX-2 Essential adverse effects - ulceration, inhibition of blood platelet-agregation, Na and water retention Selectivity towards COX types a) NSA: salicylates, pyrazolidindiones, phenamates, phenacs, prophens, oxicames, COX 2-inhibitors b) Analgesics-antipyretics: aniline derivatives, pyrazolone derivatives 7. Gastrointestinal therapeutics a) Acids x antacids: systemic and non-systemic, léčba prózy?? ?. treatment b) Antidiarrhoeals: intestinal adsorbents, disinfectants, opioids, others c) Laxatives: bulk-forming agents, stool-softeners, saline laxatives, osmotic laxatives, stimulant laxatives 8. Antibacterial chemotherapeutic agents Development, resistence, types of action mechanism ß-lactam antibiotics (penicillins, cephalosporins, carbapenems, monobactams), sulphonamides, chinolons, chloramphenicol, polypeptide atb, aminoglycosides, tetracyklines, macrolides, ansamycins, lincosamines 9. Gonadal hormones Biosynthesis, the menstrual cycle, hormonal contraceptives, menopause, HRT a) estrogens: estradiol, ethinylestradiol x antiestrogens b) gestagens: progesterone and its derivatives, 19-nortestosterone derivatives, 13-ethyl-18,19-dinortestosterone derivatives, atypical progestins c) androgens: testosterone and its derivatives, anabolic steroids, antiandrogens 10. Psychostimulants, hallucinogens, delirents Definition of dependence - psychological x physical, neurotransmitters involved in dependence Development a) sedative drugs: opioids b) stimulant drugs: methylxanthines, amphetamines, nicotine, cocaine, cannabinoids c) hallucinogens and delirents: LSD, psilocybin, meskalin
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