Pharmacognosy
A.Y. 2019/2020
Learning objectives
The course will provide the student the basic knowledge about pharmacokinetic and pharmacodynamic of natural or synthetic biologically active molecules, with emphasis on how these processes will affect pharmacological activities of active compounds and the final therapeutic effect.
The course will also explore more in detail pharmacologically active preparations from vegetal and animal sources (with special emphasis on the preparations present in the European Pharmacopoeia), their active components and therapeutic applications.
The course will also explore more in detail pharmacologically active preparations from vegetal and animal sources (with special emphasis on the preparations present in the European Pharmacopoeia), their active components and therapeutic applications.
Expected learning outcomes
Knowledge of the mechanisms responsible for the absorption, distribution, metabolism and excretion of pharmacologically active molecules, either natural or synthetic. Knowledge of the main pharmacokinetic parameters. Knowledge of the main classes of pharmacological targets, with a specific focus on membrane and intracellular receptors. Ability to evaluate the behavior of a pharmacologically active compound based on its pharmacokinetic and pharmacodynamic characteristics.
Knowledge of the pharmacologically active compounds and therapeutic activities of phytotherapics belonging to different chemical or therapeutic classes. Ability to identify potential pharmacokinetic or pharmacodynamic interactions between different phytotherapics or between phytotherapics and drugs.
Knowledge of the pharmacologically active compounds and therapeutic activities of phytotherapics belonging to different chemical or therapeutic classes. Ability to identify potential pharmacokinetic or pharmacodynamic interactions between different phytotherapics or between phytotherapics and drugs.
Lesson period: Second semester
Assessment methods: Esame
Assessment result: voto verbalizzato in trentesimi
Single course
This course cannot be attended as a single course. Please check our list of single courses to find the ones available for enrolment.
Course syllabus and organization
Linea AL
Responsible
Lesson period
Second semester
Course syllabus
Introduction and definitions. Elements of History of Pharmacology. Introduction to drug development. The phases of the research. Introduction to pharmacoeconomics. Scientific database consultation and use. Critical analysis of examples of scientific communication.
Biological membrane crossing, Routes of administration, absorption and bioavailability of active principles. First-pass effect. Absorption kinetics. Transporters and drug absorption: P-gl and MRPs. Factors affection drug absorption. Engineered absorption.
Drug distribution and Kp. Apparent distribution volume. Plasma protein binding. Factors affecting drug distribution.
Drug metabolism. Inhibition and induction of drug metabolic enzymes. Enterohepatic recirculation. Factors affecting drug metabolism and variability in the response to drugs.
Pharmacogenetics and pharmacogenomics: polymorphisms affecting drug metabolism and activity.
Drug elimination. Drig renal excretion. Tubular secretion and reabsorption. Renal clearance. Transporters and other factors affecting drug elimination.
Plasmatic drug concentration: pharmacokinetics. Systemic clearance. Plasmatic halflife. Clearance, plasmatic halflife, elimination rate constant and distribution volume. Single and multiple dosing. Steady state plasmatic concentration. Therapeutic window and therapeutic ratio. Saturation kinetics. Therapeutic regimen corrections. Individual variations in response to drugs and drug interactions.
Neurotransmitters, hormones and receptors. Drug-receptor interactions. Definition of intrinsic activity, agonism, inverse agonism, antagonism, potency, efficacy.
Proteins as drug targets. Enzymes, Transporters, Receptors. Channel receptors, G-protein-coupled receptors, enzymatic activity-coupled receptors. Enzyme inhibition. Voltage-gated channels. ATP-dependent pumps and exchangers.
Transporters and their role in drug absorption and elimination. Examples of drugs affecting transporters activity.
Ligand activated channels. Nicotinic and GABA receptors. Tyrosin kinase receptors and signal transduction.
Seven transmembrane domains receptors and major transduction mechanisms (heteromeric G-proteins, adenylyl-cyclase, phospholipases C and D, small G-proteins). Mechanisms of receptor adaptation: tachyphylaxis, desensitization, down-regulation.
Nuclear receptors and regulation of gene transcription. Mechanism of action of glucocorticoids.
Occupation theory of receptors. Dose-response curves, EC50 and Kd. Drug potency and efficacy. Reversible and irreversible antagonists. Dose-Ratio. Partial agonists. Reserve of receptors. Inverse agonists.
Protein phosphorylation and control of biological functions. Kinases and phosphatases. Intracellular calcium-ion concentrations. Ca-channels, pumps and transporters. Ca-binding proteins.
Definition of natural drugs, variability of active principles, secondary metabolism and its physiological function, balsamic time, preservation of vegetable and animal drugs,
Quality control, standardization. Elements of chemical-physical analysis.
Powdres, extracts, tinctures and essences.
Classification of vegetable drugs. Alkaloids.
Autonomic nervous system and somatic nervous system. Anatomical and functional arrangement of the autonomic nervous system. Actions mediated by the sympathetic and parasympathetic nervous system.
Cathecolaminergic transmission: organization, biochemistry and function of the synapse, adrenaline and noradrenaline, alpha- and beta-adrenergic receptors, agonists and antagonists. Introduction to dopaminergic transmission. Dopaminergic receptors. Vegetable drugs active on the cathecolaminergic transmission (Ephedra sinica, Erythroxylum coca, Catha edulis, Yohimbe).
Cholinergic transmission: organization, biochemistry and function of the cholinergic synapse, nicotinic and muscarinic receptors, agonists and antagonists, acetylcholin-esterase inhibitors. Neuromuscular junction blockers and curare. Vegetable drugs active on the cholinergic transmission (Atropa belladonna, Datura stramonium, Hyosciamus niger, Pilocarpus jaborandi, Physostigma venenosum, Nicotiana tabacum, Areca cathecu, Lobelia inflata, Hemlock)
Elements of neuropeptidergic transmission. Opioid neuropeptides and their receptors. Papaver somniferum. Substance P. Capsicum and capsaicin.
Elements of lipidergic transmission. Endocannabinoids. Cannabis sativa.
Antitumor drugs (Vinca spp, Taxus spp, Podophyllum peltatum, Camptotheca acuminata). Colchicum.
Xanthine-based drugs: Coffea spp., Thea spp, Theobroma cacao, Cola acuminata.
Chinolinic-based drugs (Chinchona). Nux vomica. Ipecac.
Inflammation and autacoids. Nitric oxide. Reactive oxygen species (ROS): formation and elimination. Mechanisms of ROS-induced damage. Antioxidant drugs: poliphenols-based drugs (Artichoke, Java tea, Sweet clover, Wild celery, Kella, Milk Thistle, Citrus spp, Propolis, Passiflora incarnata, Achillea, Equisetum, Echinacea spp, Blueberry, tannins, Hamamelis virginiana, Krameria); fluroglucinols-based drugs (Hops, St. John's-wort).
Introduction to serotoninergic transmission. Serotoninergic receptors. Vegetable drugs active on the serotoninergic transmission (Claviceps purpurea, Psilocybe mexicana, Lophophora williamsii, Mimosa hostilis). Salvia divinorum.
Lipidic autacoids: arachionic acid metabolites and PAF. Vegetable drugs affecting lipidic autacoids (Glycyrrhiza glabra, Ginkgo biloba).
Glycosides-based drugs: anthraquinone, cyanogenic, sulphated, saponin, coumarin and digitalic glycosides (Aloe spp, Rhamnus spp, Cassia spp, Rheum spp, Common laurel, Prunus spp, Black mustard, Garlic, Mead wort, Salix alba, Bearberry, Horse-chestnut, Milkwort, Butcher's broom, common Ivy, Primrose, Panax ginseng, Centella asiatica, Common Marigold, Eleutherococcum, Digitalis spp, Strophantus spp, Urginea maritima, Nerium oleander, Lily of the valley, Adonis vernalis)
Lipid-based drugs: oils (coconut oil, almond oil, castor oil, olive oil, peanut oil, fish oil) and waxes (lanolin). Pharmacological activities of polyunsaturated fatty acids.
Carbohydrate-based drugs (honey, manna ash, cyclodextrin, starch, gum arabic, tragacanth, karaya e guar, Althea officinalis, Malva silvestris, Linum usitatissimum, dextran).
Terpenes-based drugs. Essential Oils (Lavender, Oreganon, Mint, Eucalyptus, Niaouli, Grand Wormwood, Turmeric, Lemon balm, Ginger, Chamomile, Feverfew, Valeriana officinalis, Black Horehound, Rosemary, Thyme, Hawthorn, Sage). Oleoresins (Myrrh, Turpentine). Balms.
Biological membrane crossing, Routes of administration, absorption and bioavailability of active principles. First-pass effect. Absorption kinetics. Transporters and drug absorption: P-gl and MRPs. Factors affection drug absorption. Engineered absorption.
Drug distribution and Kp. Apparent distribution volume. Plasma protein binding. Factors affecting drug distribution.
Drug metabolism. Inhibition and induction of drug metabolic enzymes. Enterohepatic recirculation. Factors affecting drug metabolism and variability in the response to drugs.
Pharmacogenetics and pharmacogenomics: polymorphisms affecting drug metabolism and activity.
Drug elimination. Drig renal excretion. Tubular secretion and reabsorption. Renal clearance. Transporters and other factors affecting drug elimination.
Plasmatic drug concentration: pharmacokinetics. Systemic clearance. Plasmatic halflife. Clearance, plasmatic halflife, elimination rate constant and distribution volume. Single and multiple dosing. Steady state plasmatic concentration. Therapeutic window and therapeutic ratio. Saturation kinetics. Therapeutic regimen corrections. Individual variations in response to drugs and drug interactions.
Neurotransmitters, hormones and receptors. Drug-receptor interactions. Definition of intrinsic activity, agonism, inverse agonism, antagonism, potency, efficacy.
Proteins as drug targets. Enzymes, Transporters, Receptors. Channel receptors, G-protein-coupled receptors, enzymatic activity-coupled receptors. Enzyme inhibition. Voltage-gated channels. ATP-dependent pumps and exchangers.
Transporters and their role in drug absorption and elimination. Examples of drugs affecting transporters activity.
Ligand activated channels. Nicotinic and GABA receptors. Tyrosin kinase receptors and signal transduction.
Seven transmembrane domains receptors and major transduction mechanisms (heteromeric G-proteins, adenylyl-cyclase, phospholipases C and D, small G-proteins). Mechanisms of receptor adaptation: tachyphylaxis, desensitization, down-regulation.
Nuclear receptors and regulation of gene transcription. Mechanism of action of glucocorticoids.
Occupation theory of receptors. Dose-response curves, EC50 and Kd. Drug potency and efficacy. Reversible and irreversible antagonists. Dose-Ratio. Partial agonists. Reserve of receptors. Inverse agonists.
Protein phosphorylation and control of biological functions. Kinases and phosphatases. Intracellular calcium-ion concentrations. Ca-channels, pumps and transporters. Ca-binding proteins.
Definition of natural drugs, variability of active principles, secondary metabolism and its physiological function, balsamic time, preservation of vegetable and animal drugs,
Quality control, standardization. Elements of chemical-physical analysis.
Powdres, extracts, tinctures and essences.
Classification of vegetable drugs. Alkaloids.
Autonomic nervous system and somatic nervous system. Anatomical and functional arrangement of the autonomic nervous system. Actions mediated by the sympathetic and parasympathetic nervous system.
Cathecolaminergic transmission: organization, biochemistry and function of the synapse, adrenaline and noradrenaline, alpha- and beta-adrenergic receptors, agonists and antagonists. Introduction to dopaminergic transmission. Dopaminergic receptors. Vegetable drugs active on the cathecolaminergic transmission (Ephedra sinica, Erythroxylum coca, Catha edulis, Yohimbe).
Cholinergic transmission: organization, biochemistry and function of the cholinergic synapse, nicotinic and muscarinic receptors, agonists and antagonists, acetylcholin-esterase inhibitors. Neuromuscular junction blockers and curare. Vegetable drugs active on the cholinergic transmission (Atropa belladonna, Datura stramonium, Hyosciamus niger, Pilocarpus jaborandi, Physostigma venenosum, Nicotiana tabacum, Areca cathecu, Lobelia inflata, Hemlock)
Elements of neuropeptidergic transmission. Opioid neuropeptides and their receptors. Papaver somniferum. Substance P. Capsicum and capsaicin.
Elements of lipidergic transmission. Endocannabinoids. Cannabis sativa.
Antitumor drugs (Vinca spp, Taxus spp, Podophyllum peltatum, Camptotheca acuminata). Colchicum.
Xanthine-based drugs: Coffea spp., Thea spp, Theobroma cacao, Cola acuminata.
Chinolinic-based drugs (Chinchona). Nux vomica. Ipecac.
Inflammation and autacoids. Nitric oxide. Reactive oxygen species (ROS): formation and elimination. Mechanisms of ROS-induced damage. Antioxidant drugs: poliphenols-based drugs (Artichoke, Java tea, Sweet clover, Wild celery, Kella, Milk Thistle, Citrus spp, Propolis, Passiflora incarnata, Achillea, Equisetum, Echinacea spp, Blueberry, tannins, Hamamelis virginiana, Krameria); fluroglucinols-based drugs (Hops, St. John's-wort).
Introduction to serotoninergic transmission. Serotoninergic receptors. Vegetable drugs active on the serotoninergic transmission (Claviceps purpurea, Psilocybe mexicana, Lophophora williamsii, Mimosa hostilis). Salvia divinorum.
Lipidic autacoids: arachionic acid metabolites and PAF. Vegetable drugs affecting lipidic autacoids (Glycyrrhiza glabra, Ginkgo biloba).
Glycosides-based drugs: anthraquinone, cyanogenic, sulphated, saponin, coumarin and digitalic glycosides (Aloe spp, Rhamnus spp, Cassia spp, Rheum spp, Common laurel, Prunus spp, Black mustard, Garlic, Mead wort, Salix alba, Bearberry, Horse-chestnut, Milkwort, Butcher's broom, common Ivy, Primrose, Panax ginseng, Centella asiatica, Common Marigold, Eleutherococcum, Digitalis spp, Strophantus spp, Urginea maritima, Nerium oleander, Lily of the valley, Adonis vernalis)
Lipid-based drugs: oils (coconut oil, almond oil, castor oil, olive oil, peanut oil, fish oil) and waxes (lanolin). Pharmacological activities of polyunsaturated fatty acids.
Carbohydrate-based drugs (honey, manna ash, cyclodextrin, starch, gum arabic, tragacanth, karaya e guar, Althea officinalis, Malva silvestris, Linum usitatissimum, dextran).
Terpenes-based drugs. Essential Oils (Lavender, Oreganon, Mint, Eucalyptus, Niaouli, Grand Wormwood, Turmeric, Lemon balm, Ginger, Chamomile, Feverfew, Valeriana officinalis, Black Horehound, Rosemary, Thyme, Hawthorn, Sage). Oleoresins (Myrrh, Turpentine). Balms.
Prerequisites for admission
Subjects taught in preparatory courses are mandatory.
Teaching methods
Frontal lesson and open discussion.
Teaching Resources
Farmacologia generale e molecolare. F. Clementi e G. Fumagalli. III edizione
UTET, Milano
Goodman & Gilman: Le Basi Farmacologiche della Terapia; Il Manuale. Brunton, Parker, Blumenthal, Buxton. McGraw-Hill, Milano
Farmacognosia. F. Capasso, R. De Pasquale, G. Grandolini, N. Mascolo.
Casa editrice Springer, Milano
Slides available at the Course official web site:
https://asalaf.ariel.ctu.unimi.it
UTET, Milano
Goodman & Gilman: Le Basi Farmacologiche della Terapia; Il Manuale. Brunton, Parker, Blumenthal, Buxton. McGraw-Hill, Milano
Farmacognosia. F. Capasso, R. De Pasquale, G. Grandolini, N. Mascolo.
Casa editrice Springer, Milano
Slides available at the Course official web site:
https://asalaf.ariel.ctu.unimi.it
Assessment methods and Criteria
Knowledge will be assessed with a written test, carried out directly on computers located in IT classrooms, accessed using username and password of the institutional email. The test is structured in two parts: the first part is a multiple choice test with 15 questions in 20 minutes, and the second part proposes 4 open questions that can be discussed in an hour. Passing of the first part is mandatory in order to seat in the second part, that takes place immediately after the first part. Scoring of the first part is generated automatically assigning 1 point for each correct answer, -0.5 for each wrong answer, while no answer is scored 0. The test is passed with a score of 9 or above. Scoring of the first part accounts for 30% of the final score.
8 tests are programmed during the Academic Year, according to the avalability of IT classrooms.
8 tests are programmed during the Academic Year, according to the avalability of IT classrooms.
BIO/14 - PHARMACOLOGY - University credits: 10
Lessons: 80 hours
Professor:
Sala Angelo
Shifts:
-
Professor:
Sala AngeloLinea MZ
Responsible
Lesson period
Second semester
Course syllabus
- Pharmacodynamics: Neurotransmitters, hormones and receptors. Drug-receptor interactions: theory and methods of study. Definition of intrinsic activity, agonism, inverse agonism, antagonism, potency, efficacy.
- Receptors and signal transduction: Neurotransmitters, hormone and drug receptors. Channel receptors, G-protein-coupled receptors, tyrosin-kinase receptors, cytokine receptors, guanylate cyclase-coupled receptors (examples). Major transduction mechanisms (modifications of calcium and sodium ion concentrations, heteromeric G-proteins, adenylyl-cyclase, phospholipases C and D, small G-proteins, signalling cascade of tyrosin-kinase receptors, guanylate cyclase and NO). Cross-talk between different transduction pathways. Nuclear receptors and regulation of gene transcription.
- Arachidonic acid cascade: metabolism of arachidonic acid, cyclo-oxygenase 1 and 2, lipoxygenase, prostaglandins, tromboxanes, leukotrienes and their biological activities. Non-steroidal anti-inflammatory drugs: from salicylates to COXIBs, mechanisms of action and therapeutic applications.
- Autonomic nervous system: autonomic and somatic nervous system. Anatomical and functional arrangement of the autonomic nervous system. Actions mediated by the sympathetic and parasympathetic nervous system.
- Cholinergic transmission: organization, biochemistry and function of the cholinergic synapse, nicotinic and muscarinic receptors, agonists and antagonists (ganglion blockers, neuromuscular blockers), acetylcholin-esterase inhibitors. Therapeutic uses and side effects.
- Adrenergic transmission: organization, biochemistry and function of the adrenergic synapse, adrenaline and noradrenaline, alpha- and beta- adrenergic receptors, major physiological roles, agonists and antagonists and other drugs that interfere with the adrenergic transmission. Therapeutic uses and side effects.
- Dopaminergic transmission: organization, biochemistry and function of the dopaminergic synapse. Dopaminergic receptors. Basic information on major physiological roles, agonists and antagonists and other drugs that interfere with the dopaminergic transmission.
Other transmitter systems
- Purinergic transmission. Role of extracellular nucleotides and nucleosides in intercellular communication. Synthesis and metabolism of nucleotides and nucleosides. P1 and P2 receptors: distribution, transduction mechanisms, major physiopathological roles. Pharmacological agents that interfere with the purinergic transmission and therapeutic perspectives.
- Serotoninergic transmission: organization, biochemistry and function of the serotoninergic synapse. Serotoninergic receptors. Basic information on major physiological roles, agonists and antagonists and other drugs that interfere with the serotoninergic transmission. Therapeutic uses and side effects.
- Glutamatergic transmission: organization, biochemistry and function of glutamatergic synapse, tripartite synapse, gluatamate receptors, LTP and LTD, agonists, antagonists and other drugs acting on glutamatergic transmission. Therapeutic use and side effects.
- GABAergic transmission: organization, biochemistry and functions of GABAergic synapse, molecules acting on GABAergic transmission
Drug Absorption, Distribution and Excretion. Basic pharmacokinetics: Routes of administration, absorption, distribution and bioavailability of drugs and xenobiotics. Plasma protein binding. Metabolism, detoxification. Metabolic induction and inhibition. Kinetics of endovenous infusion, fixed-dose regimem (single-dose and repeated-dose therapy). Dose-response relationship. Therapeutic ratio. Drug excretion. Individual variations in response to drugs, adverse reactions, drug interactions.
- Introduction to pharmacognosy: Definition and classification of natural drugs, variability of active principles, secondary metabolism and its physiological function, preservation and analysis of vegetable and animal drugs, quality control, standardization, natural drugs in Pharmacopoeia.
- Carbohydrate-based drugs: starch (wheat, corn, rice and potato), cellulose. Acacia senegal, Astragalus gummifer, Sterculia spp, Cyanopsis tetragonolobus (gum arabic, gum tragacanth, karaia e guar), Plantago spp., Malva silvestris, Althea officinalis, Linum usitatissimum, Tilia spp., Aloe spp., vegetable fibers.
- Glycoside-based drugs: anthraquinone, cyanogenic, sulphated, saponin, coumarin and digitalic glycosides. Anthraquinone glycosides: Cassia spp., Ramnus spp., Rheum spp., Aloe spp.; therapeutic uses, mechanism of action, side effects. Cardio-active glycosides: Digitalis spp., Strophantus spp., use in congestive cardiac failure, mechanism of action, side effects.
- Lipid-based drugs: simple and complex lipids, fatty acid composition of lipids, features, quality control, nutritional and pharmacological aspects of vegetable oils. Olive oil, coconut oil, cocoa butter, soybean oil, evening primrose oil, castor oil.
- Alkaloid-based drugs: generalities of alkaloids
- Drugs containing indole alkaloids: Rauwolfia serpentina, Physostigma venenosum, ergot alkaloids, other hallucinogenic indole alkaloids
- Drugs containing tropane alkaloids: Erythroxylum coca, Atropa belladonna, Datura stramonium, Hyosciamus niger
- Drugs containing imidazole alkaloids: Pilocarpus Jaborandi
- Drugs containing isoquinoline and phenanthrenic alkaloids: curares, Papaver somniferum (opium varieties, major opium alkaloids, introduction to central mechanisms of nociception, opioids, opiates and their receptors, clinic and therapeutic use of opiates, abuse and withdrawal syndrome).
- Drugs containing phenylalkylamine alkaloids: Catha edulis, Ephedra sinica, Pejote and San Pedro Cactus, Capsicum and capsaicin (introduction to peripheral transmission of pain and its interference by capsaicin, opioids, cannabinoids, vanilloids and prostaglandins)
- Drugs containing piperidine/pyridine alkaloids: Nicotiana tabacum, Areca cathecu, Lobelia inflata
- Xanthine-based drugs: Coffea spp., Thea spp., Theobroma cacao, Cola acuminata, Ilex paraguensis
- Phenolic drugs: Ursina grape, salicylic drugs.
- Flavonoid-based drugs: generalities and protective roles of antioxidants. Passiflora incarnata, Citrus spp., Ginkgo biloba.
- Salicylate drugs: Allium Sativum (immunomodulatory, antithrombotic and hypocholesterolemic activity).
- Drugs with antimalarial and antiarrhythmic activity; Cinchona spp., alkaloid content, pharmacological properties of the quina components, antimalarial activity (introduction to malaria, plasmodium life cycle, therapy and prevention of malaria) and antiarrhythmic activity.
- Drugs active on the immune system: Introduction to immune function and to factors that depress the immune system, natural immunomodulators and their mechanism of action. Echinacea spp., Panax ginseng, Eleutherococcum, Witania, Glycyrrhiza glabra, Thuja occidentalis, Angelica sinensis, Polygonum multifloreum, Astragalus membranaceus, Picrorhiza kurroa
- Psychostimulant and hallucinogens: definition of substances with depressing, ansiolitic, stimulatory and hallucinogenic effects on the CNS. Amanita muscaria, Piptadenia peregrina, Peganum harmala, Psilocybe mexicana, Lophophora williamsii, recalls to ergot alkaloids. Psychedelic anaesthetics: ketamine, fenciclydine. Cannabis sativa.
- Antitumor drugs: incidence and pathogenesis of human cancer, carcinogenesis and tumor transformation, natural antitumor agents. antibiotics; Vinca spp., Taxus, Phodophyllum peltatum, Camptotheca acuminata, other phytotherapic drugs with antitumor activity (Viscum album, Enotera, sho-saiko-to).
- Drugs acting on the skin: Melaleuca alternifolia, Ocimum gratissimum, Aloe vera, Capsicum frutescens, Curcuma longa, Hypericum perforatum, Mahonia aquifolium, Strobilanthes formosanus, Persea americana, Calendula officinalis, Centella asiatica, Hamamelis virginiana, Vitis Vinifera.
- Natural antidepressants: Hypericum perforatum (characteristics, active components, mechanism of action, therapeutic use)
- Hints on neurodegenerative diseases
- Herbal drug-drug interactions: pharmacodynamic and pharmacokinetic interactions, examples, mechanisms and consequences
- Receptors and signal transduction: Neurotransmitters, hormone and drug receptors. Channel receptors, G-protein-coupled receptors, tyrosin-kinase receptors, cytokine receptors, guanylate cyclase-coupled receptors (examples). Major transduction mechanisms (modifications of calcium and sodium ion concentrations, heteromeric G-proteins, adenylyl-cyclase, phospholipases C and D, small G-proteins, signalling cascade of tyrosin-kinase receptors, guanylate cyclase and NO). Cross-talk between different transduction pathways. Nuclear receptors and regulation of gene transcription.
- Arachidonic acid cascade: metabolism of arachidonic acid, cyclo-oxygenase 1 and 2, lipoxygenase, prostaglandins, tromboxanes, leukotrienes and their biological activities. Non-steroidal anti-inflammatory drugs: from salicylates to COXIBs, mechanisms of action and therapeutic applications.
- Autonomic nervous system: autonomic and somatic nervous system. Anatomical and functional arrangement of the autonomic nervous system. Actions mediated by the sympathetic and parasympathetic nervous system.
- Cholinergic transmission: organization, biochemistry and function of the cholinergic synapse, nicotinic and muscarinic receptors, agonists and antagonists (ganglion blockers, neuromuscular blockers), acetylcholin-esterase inhibitors. Therapeutic uses and side effects.
- Adrenergic transmission: organization, biochemistry and function of the adrenergic synapse, adrenaline and noradrenaline, alpha- and beta- adrenergic receptors, major physiological roles, agonists and antagonists and other drugs that interfere with the adrenergic transmission. Therapeutic uses and side effects.
- Dopaminergic transmission: organization, biochemistry and function of the dopaminergic synapse. Dopaminergic receptors. Basic information on major physiological roles, agonists and antagonists and other drugs that interfere with the dopaminergic transmission.
Other transmitter systems
- Purinergic transmission. Role of extracellular nucleotides and nucleosides in intercellular communication. Synthesis and metabolism of nucleotides and nucleosides. P1 and P2 receptors: distribution, transduction mechanisms, major physiopathological roles. Pharmacological agents that interfere with the purinergic transmission and therapeutic perspectives.
- Serotoninergic transmission: organization, biochemistry and function of the serotoninergic synapse. Serotoninergic receptors. Basic information on major physiological roles, agonists and antagonists and other drugs that interfere with the serotoninergic transmission. Therapeutic uses and side effects.
- Glutamatergic transmission: organization, biochemistry and function of glutamatergic synapse, tripartite synapse, gluatamate receptors, LTP and LTD, agonists, antagonists and other drugs acting on glutamatergic transmission. Therapeutic use and side effects.
- GABAergic transmission: organization, biochemistry and functions of GABAergic synapse, molecules acting on GABAergic transmission
Drug Absorption, Distribution and Excretion. Basic pharmacokinetics: Routes of administration, absorption, distribution and bioavailability of drugs and xenobiotics. Plasma protein binding. Metabolism, detoxification. Metabolic induction and inhibition. Kinetics of endovenous infusion, fixed-dose regimem (single-dose and repeated-dose therapy). Dose-response relationship. Therapeutic ratio. Drug excretion. Individual variations in response to drugs, adverse reactions, drug interactions.
- Introduction to pharmacognosy: Definition and classification of natural drugs, variability of active principles, secondary metabolism and its physiological function, preservation and analysis of vegetable and animal drugs, quality control, standardization, natural drugs in Pharmacopoeia.
- Carbohydrate-based drugs: starch (wheat, corn, rice and potato), cellulose. Acacia senegal, Astragalus gummifer, Sterculia spp, Cyanopsis tetragonolobus (gum arabic, gum tragacanth, karaia e guar), Plantago spp., Malva silvestris, Althea officinalis, Linum usitatissimum, Tilia spp., Aloe spp., vegetable fibers.
- Glycoside-based drugs: anthraquinone, cyanogenic, sulphated, saponin, coumarin and digitalic glycosides. Anthraquinone glycosides: Cassia spp., Ramnus spp., Rheum spp., Aloe spp.; therapeutic uses, mechanism of action, side effects. Cardio-active glycosides: Digitalis spp., Strophantus spp., use in congestive cardiac failure, mechanism of action, side effects.
- Lipid-based drugs: simple and complex lipids, fatty acid composition of lipids, features, quality control, nutritional and pharmacological aspects of vegetable oils. Olive oil, coconut oil, cocoa butter, soybean oil, evening primrose oil, castor oil.
- Alkaloid-based drugs: generalities of alkaloids
- Drugs containing indole alkaloids: Rauwolfia serpentina, Physostigma venenosum, ergot alkaloids, other hallucinogenic indole alkaloids
- Drugs containing tropane alkaloids: Erythroxylum coca, Atropa belladonna, Datura stramonium, Hyosciamus niger
- Drugs containing imidazole alkaloids: Pilocarpus Jaborandi
- Drugs containing isoquinoline and phenanthrenic alkaloids: curares, Papaver somniferum (opium varieties, major opium alkaloids, introduction to central mechanisms of nociception, opioids, opiates and their receptors, clinic and therapeutic use of opiates, abuse and withdrawal syndrome).
- Drugs containing phenylalkylamine alkaloids: Catha edulis, Ephedra sinica, Pejote and San Pedro Cactus, Capsicum and capsaicin (introduction to peripheral transmission of pain and its interference by capsaicin, opioids, cannabinoids, vanilloids and prostaglandins)
- Drugs containing piperidine/pyridine alkaloids: Nicotiana tabacum, Areca cathecu, Lobelia inflata
- Xanthine-based drugs: Coffea spp., Thea spp., Theobroma cacao, Cola acuminata, Ilex paraguensis
- Phenolic drugs: Ursina grape, salicylic drugs.
- Flavonoid-based drugs: generalities and protective roles of antioxidants. Passiflora incarnata, Citrus spp., Ginkgo biloba.
- Salicylate drugs: Allium Sativum (immunomodulatory, antithrombotic and hypocholesterolemic activity).
- Drugs with antimalarial and antiarrhythmic activity; Cinchona spp., alkaloid content, pharmacological properties of the quina components, antimalarial activity (introduction to malaria, plasmodium life cycle, therapy and prevention of malaria) and antiarrhythmic activity.
- Drugs active on the immune system: Introduction to immune function and to factors that depress the immune system, natural immunomodulators and their mechanism of action. Echinacea spp., Panax ginseng, Eleutherococcum, Witania, Glycyrrhiza glabra, Thuja occidentalis, Angelica sinensis, Polygonum multifloreum, Astragalus membranaceus, Picrorhiza kurroa
- Psychostimulant and hallucinogens: definition of substances with depressing, ansiolitic, stimulatory and hallucinogenic effects on the CNS. Amanita muscaria, Piptadenia peregrina, Peganum harmala, Psilocybe mexicana, Lophophora williamsii, recalls to ergot alkaloids. Psychedelic anaesthetics: ketamine, fenciclydine. Cannabis sativa.
- Antitumor drugs: incidence and pathogenesis of human cancer, carcinogenesis and tumor transformation, natural antitumor agents. antibiotics; Vinca spp., Taxus, Phodophyllum peltatum, Camptotheca acuminata, other phytotherapic drugs with antitumor activity (Viscum album, Enotera, sho-saiko-to).
- Drugs acting on the skin: Melaleuca alternifolia, Ocimum gratissimum, Aloe vera, Capsicum frutescens, Curcuma longa, Hypericum perforatum, Mahonia aquifolium, Strobilanthes formosanus, Persea americana, Calendula officinalis, Centella asiatica, Hamamelis virginiana, Vitis Vinifera.
- Natural antidepressants: Hypericum perforatum (characteristics, active components, mechanism of action, therapeutic use)
- Hints on neurodegenerative diseases
- Herbal drug-drug interactions: pharmacodynamic and pharmacokinetic interactions, examples, mechanisms and consequences
Prerequisites for admission
Subjects taught in preparatory courses are mandatory
Teaching methods
Classroom-taught lessons
Teaching Resources
· Farmacologia generale e molecolare. F Clementi e G. Fumagalli, EDRA (last edition)
· Farmacologia. Rang HP, Dale MM, Ritter JM, Moore PK. Edizione italiana a cura di A Gorio e AM Di Giulio, Casa Editrice Masson (last edition)
· Farmacognosia. Capasso F, De Pasquale R, Grandolini G, Mascolo N. Springer (last edition)
· Fitoterapia. L'impiego razionale delle droghe vegetali. Capasso F, Grandolini G, Izzo AA. Springer (last edition)
· Trease and Evans' - Pharmacognosy, Edition 16 - Elsevier
Slides of the lessons from the ARIEL website
· Farmacologia. Rang HP, Dale MM, Ritter JM, Moore PK. Edizione italiana a cura di A Gorio e AM Di Giulio, Casa Editrice Masson (last edition)
· Farmacognosia. Capasso F, De Pasquale R, Grandolini G, Mascolo N. Springer (last edition)
· Fitoterapia. L'impiego razionale delle droghe vegetali. Capasso F, Grandolini G, Izzo AA. Springer (last edition)
· Trease and Evans' - Pharmacognosy, Edition 16 - Elsevier
Slides of the lessons from the ARIEL website
Assessment methods and Criteria
The final examination consists of two steps and only students passing the first one will have access to the second one. The first 60-min long evaluation consists of 30 multiple choice questions. The evaluation score is as follows: correct answer +1; no answer 0; incorrect answer -0.5. The total score must be at least 18 to be positively evaluated. The list of students to be admitted to the second step will be published on the ARIEL website within 1 week.
The second evaluation is an oral examination, consisting of two/three questions (which might require integrated answers) on the whole program. The marks of the first and of the second evaluations will contribute for one-third and two-thirds to the final mark, respectively.
The second evaluation is an oral examination, consisting of two/three questions (which might require integrated answers) on the whole program. The marks of the first and of the second evaluations will contribute for one-third and two-thirds to the final mark, respectively.
BIO/14 - PHARMACOLOGY - University credits: 10
Lessons: 80 hours
Professor:
Ceruti Stefania Maria
Shifts:
-
Professor:
Ceruti Stefania MariaProfessor(s)
Reception:
Tuesday from 10.30 am, upon arrangement by writing to the institutional email
Via Balzaretti 9 or using Zoom Cloud Meetings videoconference