Pharmacology - EA0107015

• Title: Pharmacology
• Guaranteed by: Ústav farmakologie (14-100)
• Faculty: Faculty of Medicine in Pilsen
• Actual: from 2022
• Semester: winter
• Points: 9
• E-Credits: 9
• Examination process: winter s.:
• Hours per week, examination: winter s.:3/2, C+Ex [HT]
• Capacity: unknown / unknown (unknown)
• Min. number of students: unlimited
• 4EU+: no
• Virtual mobility / capacity: no
• State of the course: cancelled
• Language: English
• Teaching methods: full-time
• Teaching methods: full-time
• Note: deregister from the exam date if a requisite was not fulfilled
• Guarantor: prof. PharmDr. Radek Kučera, Ph.D.
• Co-requisite : EA0105084, EA0105085, EA0106013, EA0106014
• Interchangeability : EAP0103100
• Is co-requisite for: EA0110023, EA0110029, EA0110019, EA0110024, EA0110432, EA0110030, EA0110032, EA0110057, EA0110116
• Is interchangeable with: EAP0103100

Annotation

English

Last update: BURIANKO (26.04.2005)

Pharmacokinetics/dynamics, individ. variation, side effects, interactions, evaluation of new drugs, rational pharmacother., pharmacopoeia, drug formulations, prescribing of drugschemical mediators, nervous system, drugs affecting heart + vascular system, haemostasis + thrombosis, diuretics, dislipoproteinaemias, respiratory + gastrointestinal systems, uterus, anti-inflammatory + immunosuppressant drugs, radiopharmaceuticals, locally acting drugs, disinfectant +antiseptic agents, chemotherapy of infectious + malignant disease, hormones, vitamins, toxicology, phytotherapy, phytotoxicology

Czech

Last update: BURIANKO (26.04.2005)

Farmakokinetika, farmakodynamika, individuální variabilita, nežádoucí účinky, interakce, hodnocení nových léčiv, účelná farmakoterapie, lékopis, lékové formy ,základy recepturychemické mediátory, nervový systém, látky ovlivňující cévy a srdce, hemostáza, tromboza, diuretika, dislipoproteinémie, dýchací a trávicí ústrojí, uterotonika a tokolytika, antiflogistika a imunosupresiva, rtg kontrastní látky, radiofarmaka, lokálně působící látky, desinficiencia, antiseptika, chemoterapie infekčních a nádorových onemocnění, hormony, vitaminy, základy toxikologie, fytoterapie, fytotoxikologie

Literature

Last update: Irena Zemenová (02.10.2019)

GENERAL PRINCIPLES OF PHARMACOLOGY

1. Rang-Dale-Ritter: Pharmacology - 6^th Edit., (Churchill - Livingstone).

2. Dale - Haylett: Pharmacology Condensed, (Churchill - Livingstone)

3. British National Formulary (latest edition)

 

Special pharmacology

1. H.P.Rang, M.M.Dale, P.K.Moore: Pharmacology (Churchill Livingstone)

2. M.M.Dale, D.G. Haylett: Pharmacology condensed (Churchill Livingstone)

3. A.J.Trevor, B.G.Katzung, S.B.Masters: Katzung and Trevor?s Pharmacology  McGraw - Hill

Requirements to the exam

Last update: prof. PharmDr. Radek Kučera, Ph.D. (20.11.2020)

 

Credit requirements:

 

 

 

Attendance at seminars, passing two interim tests, oral presentation covering latest news in pharmacy and therapeutics, submission of computer simulated experiments report and passing a credit test (covering the materials from the seminars) are compulsory. There is one regular date and two resit dates for the credit test.

 

Credit in SIS and signed credit in Credit Book is needed.

 

 

 

Exam requirements:

 

Credit in SIS and signed credit in Credit Book is needed.

 

 

 General Pharmacology

 

       

 

1.                  Pharmacology and its subdivisions, origins and sources of drugs, names of drugs

 

2.                  Preclinical drug evaluation, clinical trials (phases)

 

3.                  Routes of administration of drugs, advantages, disadvantages, dosage forms

 

4.                  Drug transport through biological membranes – passive, carrier-mediated

 

5.                  Basic pharmacokinetic parameters and processes, first order and zero order kinetics, saturation kinetics.

 

6.                  Absorption of drugs, Bateman function, bioavailability, determination of bioavailability, AUC

 

7.                  Distribution, of drugs, volume of distribution, redistribution, binding to plasma proteins, tissue barriers.

 

8.                  Elimination, elimination half-life (α, β phase), elimination rate constant, clearance

 

9.                  Dosage regimens, continuous and intermittent administration of drugs, accumulation, accumulation index

 

10.              Biotransformation of drugs, phases, examples

 

11.              The role of the liver in drug metabolism, first pass effect

 

12.              Induction and inhibition of enzymes, clinical significance.

 

13.              Renal and extrarenal excretion of drugs

 

14.              General principles of drug action, molecular mechanisms of drug action, the importance of placebo and nocebo

 

15.              Specific effect of drugs - targets of drug action, receptor theory - types of receptors.

 

16.              Dose-response relationship, therapeutic index, therapeutic window, therapeutic risk

 

17.              Factors influencing pharmacokinetics and pharmacodynamics of drugs, adherence, compliance

 

18.              Drug interactions, synergism, antagonism

 

19.              Pharmacogenetics, genetic polymorphism

 

20.              Tolerance, tachyphylaxis, resistance

 

21.              Influence of diseases on the effect of drugs, polypharmacy

 

22.              Adverse drug reactions

 

23.              Drug induced allergic (hypersensitivity) reactions, idiosyncratic drug reactions

 

24.              Carcinogenic and mutagenic effects

 

25.              Drugs in pregnancy, teratogenic effect, drugs in lactation,

 

26.              Drug therapy in infants and children, drug therapy in the elderly

 

 

 

 

 

Special Pharmacology

 

 

 

1.                  Cholinergic neurotransmission, effects of drugs on cholinergic transmission, muscarinic and nicotinic actions of acetylcholine, direct-acting cholinergic agonists, clinical use

 

2.                  Reversible and irreversible anticholinesterase agents

 

3.                  Antimuscarinic agents – alkaloids and their derivatives, synthetic anticholinergic drugs, antispasmodics

 

4.                  Neurotransmission in autonomic ganglia, drugs acting on autonomic ganglia, ganglion-blocking drugs, nicotine, characteristics, effects of tobacco smoking and pharmacologic treatment of tobacco dependence

 

5.                  Adrenergic neurotransmission, effects of drug on adrenergic transmission, adrenoceptors, direct and indirect mechanism of action

 

6.                  Catecholamines, synthesis, biotransformation, uptake, adrenaline, noradrenaline, isoprenaline, dopamine, dobutamine

 

7.                  Alpha-adrenoceptor agonists, selective alpha-1 and alpha-2 agonists

 

8.                  Ephedrine, amphetamines

 

9.                  Beta-adrenoceptor agonists (β1, β2)

 

10.              Alpha-adrenoceptor antagonists, classification, clinical use

 

11.              Ergot alkaloids and their derivatives, serotonin (5-HT), 5-HT receptors and drugs acting on them

 

12.              Beta-adrenoceptor antagonists (β-blockers)

 

13.              Drugs used in ophthalmology

 

14.              Nitric oxide (NO)

 

15.              Neuromuscular-blocking agents, classification, depolarizing and nondepolarizing agents, antidotes, clinical use, adverse effects, drug interactions, malignant hyperthermia

 

16.              Dantrolene, Botulinum toxin type A, centrally acting muscle relaxants

 

17.              Local anaesthetics – chemical structure, pharmacokinetics, effects, types of local anaesthesia, classification by clinical use

 

18.              Adverse effects and intoxications of local anaesthetics, prevention and therapy

 

19.              Cocaine

 

20.              General anaesthesia, stages, inhalation anaesthetics in general, volatile inhalation anaesthetics, nitrous oxide (N2O) and xenon in general anaesthesia

 

21.              Intravenous general anaesthetics, neuroleptanalgesia, combined anaesthesia

 

22.              Risks of general anaesthesia, premedication, drug interactions with general anaesthetics, specific and nonspecific antagonists in general anaesthesia

 

23.              Hypnotics, principles of use, barbiturates and their effects, clinical use, current significance

 

24.              Benzodiazepines as hypnotics and Z-hypnotics

 

25.              Ethanol – acute effects, clinical use, methanol and therapy of methanol intoxication, alcoholism, effects on health, methods of treatment of alcohol addiction

 

26.              Antiepileptic drugs, principles of use, adverse effects, “classic” antiepileptic drugs

 

27.              “Newer” antiepileptic drugs

 

28.              Drug treatment of Parkinson’s disease – classification, mechanism of action, adverse effects, dopamine agonists and acetylcholine antagonists used in Parkinson’s disease

 

29.              Classification of psychiatric medication

 

30.              Typical and atypical antipsychotics

 

31.              Antidepressants – tricyclic

 

32.              Antidepressants – monoamine oxidase inhibitors

 

33.              Antidepressants – SSRI, SNRI and atypical antidepressants

 

34.              Mood stabilizers

 

35.              Anxiolytics (tranquilizers)

 

36.              Psychostimulants, CNS stimulants, anorectic drugs

 

37.              Drugs used in Alzheimer’s disease. Nootropics and related drugs.

 

38.              Psychoactive agents (hallucinogens)

 

39.              Cannabinoids, endocannabinoids: receptors, role in organism, possible use

 

40.              Substance (drug) dependence

 

41.              Opium and its alkaloids, endogenous opioids, morphine, morphine intoxication, morphine dependence

 

42.              Derivatives and substitutes of morphine, opioid antagonists and dualists

 

43.              Eicosanoids, significance, methods of influencing the eicosanoid synthesis, inflammatory cytokine inhibitors

 

44.              Analgesic-antipyretics, classification, adverse effects

 

45.              Nonsteroidal anti-inflammatory drugs – classification, clinical use, adverse effects, cyclooxygenase I and II

 

46.              Pharmacotherapy of migraine

 

47.              Anti-rheumatic drugs – disease-modifying drugs, monoclonal antibodies

 

48.              Drugs used in gout

 

49.              Immunomodulation, immunosuppressive drugs, immunostimulant drugs

 

50.              Inotropic agents, digoxin and related drugs

 

51.              Antiarrhythmic drugs  – mechanism of action, classification, overview

 

52.              Antiarrhythmic drugs – characteristics and representatives of individual groups, unclassified drugs

 

53.              Vasoconstrictor drugs

 

54.              Methylxanthines and their derivatives

 

55.              Angiotensin-converting enzyme inhibitors and angiotensin receptor blockers

 

56.              Aldosterone antagonists, drugs affecting natriuretic peptides

 

57.              Diuretics in general – sites of action, classification by mechanism of action, osmotic diuretics and aquaretics

 

58.              Thiazides, sulphonamide diuretics, carbonic anhydrase inhibitors

 

59.              Loop diuretics, use, risks, potassium-sparing diuretics

 

60.              Overview of vasodilator drugs (+ mechanism of action), direct vasodilator drugs (potassium channel openers – hydralazine, minoxidil and others)

 

61.              Calcium channel blockers

 

62.              Nitrites and nitrates

 

63.              Overview of drugs used in heart failure

 

64.              Overview of drugs used in coronary artery disease

 

65.              Antihypertensive drugs and their clinical use, adverse effects, contraindications

 

66.              Drugs used in atherosclerosis and drugs affecting lipid metabolism

 

67.              Drugs affecting blood coagulation – Overview of mechanisms of action

 

68.              Parenteral anticoagulants – indirect thrombin inhibitors (heparin)

 

69.              Parenteral anticoagulants – indirect factor Xa inhibitors (low molecular weight heparins and pentasaccharides)

 

70.              Direct oral anticoagulants: thrombin inhibitors (gatrans), factor Xa inhibitors (xabans)

 

71.              Antivitamins K

 

72.              Antidote for anticoagulants

 

73.              Fibrinolytics, thrombolytics

 

74.              Drugs affecting platelet aggregation

 

75.              Agents that reduce increased bleeding, haemostatic agents

 

76.              Drugs used in anaemia

 

77.              Antitussives, expectorants

 

78.              Histamine and antihistamines H1

 

79.              Antiasthmatics, drugs used in obstructive lung disease

 

80.              Intestinal adsorbents, disinfectants, laxatives, antidiarrheal drugs, antiinfectives, antiflatulent agents

 

81.              Acids and antacids, pancreatic and proteolytic enzymes

 

82.              Drugs used in peptic ulcer disease

 

83.              Prokinetics, probiotics.

 

84.              Emetics, antiemetics

 

85.              Intestinal anti-inflammatory drugs and monoclonal antibodies (idiopathic inflammatory bowel diseases)

 

86.               Substances with hepatoprotective effect, cholagogues, dissolution of gallstones

 

87.              Hormones of the hypothalamus, hormones of the adenohypophysis and neurohypophysis, their analogues and clinical use

 

88.              Thyroid and parathyroid hormones, iodine, iodides and antithyroid drugs

 

89.              Mineralocorticoids, their antagonists, substitution therapy

 

90.              Insulin and glucagon

 

91.              Pharmacotherapy of diabetes, overview, oral antidiabetics, and their significant side effects

 

92.              Glucocorticoids

 

93.              Androgens, anabolic steroids

 

94.              Oestrogens, progestogens: clinical use

 

95.              Contraceptives, side effects, main contraindications

 

96.              Uterotonics, tocolytics

 

97.              Hormone antagonists

 

98.              Drugs in the treatment of benign prostatic hyperplasia

 

99.              Antibacterial agents: classification, mechanisms of action, pharmacokinetics, indications, resistance, principles of antibiotic treatment

 

100.          β-lactam antibiotics: penicillins. Beta-lactamase inhibitors

 

101.          β-lactam antibiotics: cephalosporins, carbapenems, monobactams

 

102.          Aminoglycosides, quinolones

 

103.          Glycopeptides, lipopeptides polypeptides, macrolides and azalides, lincosamides oxazolidinones

 

104.          Tetracyclines and glycylcyclines, rifamycins, nitroimidazoles, sulphonamides

 

105.          Chloramphenicol, fidaxomycin, fosfomycin, nitrofurantoin, fusidic acid, mupirocin, chemotherapeutics for urinary and intestinal infections, topical antibiotics

 

106.          Antituberculosis and antileprosy drugs

 

107.          Antifungals

 

108.          Antivirals in general, drugs used in hepatitis B and C, herpes infections and influenza; ribavirin

 

109.          Antiretrovirals, HIV therapy

 

110.          Antiparasitic drugs

 

111.          Anticancer drugs - general overview, mechanism of action

 

112.          Anticancer drugs - principles of therapy, combinations, adverse effects, resistance, substances used to protect healthy tissue from toxic effects of anticancer drugs

 

113.          Anticancer drugs - alkylating agents

 

114.          Anticancer drugs - antimetabolites

 

115.          Intercalating agents + topoisomerase inhibitors

 

116.          Mitosis inhibitors

 

117.          Anticancer drugs with combined mechanisms of action, monoclonal antibodies

 

118.          Hormones and antihormones in cancer treatment

 

119.          Platinum derivatives

 

120.          X-ray contrast agents and their adverse effects

 

121.          Disinfectants, antiseptics

 

122.          Drugs used for local action on the skin and mucous membranes (excluding disinfectants)

 

123.          Antagonists and specific antidotes for poisoning and overdose

 

124.          Antidotes for metal poisoning in general, intoxication with mercury, arsenic and lead compounds, and their therapy

 

125.          Calcium, magnesium, potassium

 

126.          Zinc, selenium, antioxidants

 

127.          Vitamins A, E, K

 

128.          Vitamin D and hormones affecting Ca metabolism

 

129.          Substances used in the treatment of osteoporosis

 

130.          Vitamin C, B vitamins

 

131.          Phytotherapy, alternative medicine (principles, significance)

 

Syllabus

Last update: prof. PharmDr. Radek Kučera, Ph.D. (08.10.2020)

Sylallabus of lectures 2020/21 see atttached file 

 

GENERAL PRINCIPLES OF PHARMACOLOGY

Pharmacology, toxicology, clinical pharmacology, pharmacotherapy, pharmacy, pharmacognosy, pharmacovigilance, pharmacoeconomy.

Drugs and medicine. Sources of drugs. Names of drugs. Use of pharamacological agents in medicine. Drug formulations. Combination products in oral therapy.
Pharmacopoeia. Prescription writing. Prescription of CD. POM. OTC drugs. Proprietary and nonproprietary remedies and drugs. Prescribing for children?s and old patients.
Pharmacokinetics, pharmacodynamics.
Drug administration. Lipid solubility and ionization of drugs. Fick?s-law. Movement of drugs across cellular barriers. Encephalic barrier. Placenta. Special drug delivery systems. Transdermal dosage forms. Absorption, distribution and redistribution of drugs. Bioavailability. Binding of drugs to plasma proteins. Volume of distribution. Elimination of drugs. Biotransformation of drugs. Phases. Microsomal, non-microsomal biotransformation. Cyt. P-450. Enzymes inhibition and induction. Excretion of drugs (renal, extrarenal). Enterohepatic circulation. First pass metabolism. Prodrugs.
Pharmacokinetics models. Single, two and multicompartment system. Linear and nonlinear kinetics. Zero and first order kinetics. Plasma half life, clearence, elimination constants. Bateman function. AUC. Continuous or intermittent drug administration. Infusion. Accumulation of drugs. Plateau-Css. Loading and maintenance dose.
Drug action. Specific, non-specific action. Mechanisms of action.. Primary drug targets (receptors, channels, enzymes, carriers). G proteins, second messengers. Agonists. Dose-effects relationship. Efficacy, potency. Antagonists. Drug antagonism and synergism. Partial agonism. Competitive and noncompetitive antagonism. Physiological and chemical antagonism.
Factors influencing drug kinetics and dynamics. Genetics and ethnic factors. Pharmacogenetics. Genetic polymorphism.
Interaction of drugs. Interaction drug - food.
Unwanted and adverse effects of drugs. Therap. index. Tolerance. Tachyphylaxis. Overdose. Resistance. Drug allergy and idiosyncrasy. Teratogenicity. Carcinogenicity. Treatment of poisonings. Antidotes.
Drug misuse and dependence.
Drug discovery and development. Preclinical and clinical trials. Double-blind trials. Phases. Placebo. Drug registration. Clinical pharmacokinetics. Therapeutic drugs monitoring. Use of drugs in neonates. Use of drug in children. Drugs and the elderly. Drug during pregnancy and breast-feeding. Teratogenicity. Mutagenesis, cancerogenesis. Compliance.
Drug-disease interaction. Influence of concomitant disease on pharmacokinetics and pharmacodynamics (disease of git, kidneys, liver, heart congest, failure, thyroid gl.) Therapeutic risk. Rational pharmacotherapy.

SPECIAL PHARMACOLOGY

Peripheral nervous system and its transmitters.
The autonomic nervous system. Parasympathetic. Sympathetic. Enteric nervous system. Neurotransmitters, co-transmitters.
Cholinergic transmission. Acetylcholine synthesis, storage, release. Drugs affecting these events. Muscarinic receptors - agonists, antagonists. Nicotinic receptors agonists, antagonists. Nicotine. Ganglion blocking agents.
Cholinesterases. Anticholinesterases. Organophosphates. Reactivators of cholinesterases.
Neuromuscular blocking agents. Drugs influencing skeletomuscles spasms and spasticity. Dantrolen.
Noradrenergic transmission. Events in the adrenergic varicosity. Catecholamines, biotransformation. Uptake of NA. Adrenoceptors (alpha 1, alpha 2), agonists and antagonists. Selectivity and ISA. Drug affecting NA nervous.
Treatment of glaucoma. Mydriatics and cyclopegics.
5-HT (serotonin), receptors, function.
Treatment of migraine. Purine mediators and receptors. Peptides.
Nitric oxide. NO synthase. Nitrates.
Prostanoids and their analogs. COX 1 and COX 2. NSAIDs. Analgesics and antipyretics. DMARDs. Histamine. Antihistamines (anti H1).
Drugs for treatment of heart failure - vasodilators, diuretics, inotropic agents. Antidysrhytmics. V.W. classification. Adenosine, digoxin, magnesium. Antihypertensive drugs. Diuretics, beta-adrenoceptor antagonists. Ca - antagonists. Renin - angiotensin system. ACE inhibitors. Activators of K-channels. Vasodilatators generally.
Drug used in angina pectoris - organic nitrates, calcium antagonists, beta-adrenoceptor antagonists, nicorandil. Drugs used to treat myocardial infarction.
Atherosclerosis and lipoproteins. Lipid lowering drugs - statins, fibrates, bile acid ? binding resin.
Homeostasis and thrombosis. Vitamin K. Anticoagulations ? heparin, low-molecular-weigh heparins (LMWHs). Warfarin.
Antiplatelet agents. Fibrinolytic drugs. Antifibrinolytics and haemostatics.
The haemopoetics system. Anemias. Iron. Folic acid. Vitamin B12..Erythropoetine. Haemopoetic growth factors. Myeloid growth factors.
Drugs in treatment of asthma ? bronchodilators, anti-inflammatory agents. Drug in chronic bronchitis, expectorants, cough suppressants.
Diuretics incl. subclasses. Treatment of gastro duodenal ulcers. Emesis and ant emetics. Prokinetics. Treatment of diarrhoea, constipation, gallstones. Drug affecting biliary composition and flow. Liver protective drugs. Treatment of chronic bowel diseases. Antispasmodics. Pancreatin.
Treatment of IDDM and NIDDM. Insulins and oral antidiabetics. Treatment of obesity.
Glucocorticoids. Mineralocorticoids. Drug acting on corticosteroids synthesis.
Thyroid hormones. Drugs influencing activity of thyroid.
Bone metabolism and its disorders. Calcium homeostasis. Drug influencing bone metabolism.
The reproductive system. Female sex hormones. Contraceptive drugs. Postmenopause hormone replacement therapy. Gonadotrophines.
Drug acting on the uterus.
The male reproductive system. Androgens and antiandrogens. Anabolic steroids. Erectile dysfunction. Phosphodiesterases. Sildenafil and relative drugs. Drugs for BHP.
Hormones of hypothalamus and anterior pituitary. Poster pituitary hormones.
Antihormones.
Drug action in CNS, targets of drugs in CNS, CNS transmitters. CNS - amino acid transmitters. Glutamate, glycine, strychnine, tetanotoxin.
Drug in Parkinson?s disease. Drug for Alzheimer?s disease and dementia. Nootropic drugs. Cerebral vasodilators.
General anaesthetics. Inhalation an. Intravenous an. Stages of anaesthetic. Perioperative drugs.
Anxiolytics and hypnotics.
Antipsychotic drugs.
Drugs in affective disorders. Antidepresant drugs. Drugs for bipolar disorder. Antiepileptic drugs.
Analgesic drugs and control of pain (opiates, opioids).
Local anesthetics.
Drug dependence and drug abuse. Nicotine and tabaco smoking. Ethanol. Methanol intoxication. Cannabinoids. Benzodiazepines. Barbiturates.
CNS stimulants and psychotomimetics (hallucinogens). Cocaine. Amphetamines. Methylxanthines. Analeptics. Hallucinogens (e.g. LSD).
Antibacterial agents. Their targets. Resistance to antibiotics. Penicillins. Cephalosporins, cephamycins. Other beta-bactams. Glycopeptides. Aminoglycosides. Macrollides. Tetracyclines. Chloramphenicol. Clindomycin. Fluoroquinolones. Streptogramins. Lincosamides. Oxalisidonones. Fusidic acid. Miscelaneous - vancomycin (glycopeptides), colistin (polymycins). Chemotherapy of git and urinary tract infections.
Sulphonamides. Trimethoprim. Antituberculosis drugs. Anileprosy agents.
Antifungal drugs. Anthelmintic drugs. Antiviral drugs (anti HIV, other antiviral drug). Immunosuppressive drugs. Immunomodulators.
Animalarial drugs. Amoebicidal drugs. Treatment of other protozoal infections.
Anticancer drugs. Combinations. Treatment schedules. Cell cycle and anticancer drugs. Rules for administrator. Adverse effects. Treatment of adverse effect.
Alkylating drugs. Antimetalolites. Cytotoxic antibiotics. Plant derivatives and miscellaneous agents. Hormones in cancer therapy. Radioactive isotopes. Miscellaneous agents.
Vitamins - water soluble, lipid soluble. Antioxidants. Essential elements - Se, Zn, Mg.
Lead-, mercury-, arsenic- intoxication. Antidotes of metal and metalloids intoxications.
The main preparations in dermatology.