General Pharmacology and Pharmacognosy
A.Y. 2024/2025
Learning objectives
The main objective of the course is to provide knowledge on the pharmacological activity of synthetic or natural drugs. Taking into consideration the complexity of botanicals, the course will define the parts of plant used for their pharmacological activity and the active principles responsible for it. Moreover, the course will provide the theoretical basis of pharmacokinetic and pharmacodynamic, examining the main neurotransmitter systems and the effects of active principles of specific natural drugs on these targets.
Expected learning outcomes
At the end of the course, students are expected to know and understand principles underlying concepts of pharmacokinetic and pharmacodynamic, applying this knowledge to the comprehension of the effects of the active principles from natural or synthetic source and their molecular target. In particular, students will be able to know and understand the main mechanisms of action of drugs, their relationship with the endogenous systems, the aspects which influence variability of active principles in the drug, and factors able to affect safety and/or efficacy (quality of botanicals).
Lesson period: Activity scheduled over several sessions (see Course syllabus and organization section for more detailed information).
Assessment methods: Esame
Assessment result: voto verbalizzato in trentesimi
Single course
This course can be attended as a single course.
Course syllabus and organization
Linea AK
Responsible
Lesson period
year
BIO/14 - PHARMACOLOGY - University credits: 8
Lessons: 64 hours
Professor:
Abbracchio Maria Pia
Shifts:
Turno
Professor:
Abbracchio Maria PiaLinea LZ
Responsible
Lesson period
year
Course syllabus
Introduction and definitions of interest in Pharmacology and Pharmacognosy.
Sustainability for the use of drugs obtained from natural sources. The phases of the research. Pharmacovigilance. Introduction to Pharmacoeconomics and definition of shadow costs.
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.
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. Drug renal excretion. Tubular secretion and reabsorption. Renal clearance. Transporters and other factors affecting drug elimination.
Plasmatic drug concentration: Pharmacokinetics. Systemic clearance. Plasmatic half-life. Clearance, plasmatic half-life, elimination rate constant and distribution volume relationship. 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.
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).
Nuclear receptors. Hormone responsive elements.
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.
Powders, 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.
Catecholaminergic 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 catecholaminergic transmission (Ephedra sinica, Erythroxylum coca, 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. Substance P: Capsicum. Opioid neuropeptides and their receptors. Papaver somniferum.
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.
Introduction to serotoninergic transmission. Serotoninergic receptors. Vegetable drugs active on the serotoninergic transmission (Claviceps purpurea, Psilocybe mexicana, Lophophora williamsii, Mimosa hostilis). Salvia divinorum.
Histamine: distribution and pathophysiologic role. Rubia Tibetica.
Elements of lipidergic transmission. Endocannabinoids. Cannabis sativa.
Lipidic autacoids: arachionic acid metabolites and PAF. Vegetable drugs affecting lipidic autacoids (Glycyrrhiza glabra, Ginkgo biloba).
Reactive oxygen species (ROS): Mechanisms of ROS-induced damage. Antioxidant drugs: Polyphenols-based drugs. Flavonoids and citroflavonoids. Propolis, Passiflora incarnata, Echinacea spp. Coumarins-based drugs (Sweet clover, Kella). Lignan- and neolignane-based drugs (Milk Thistle). Antocian-based drugs (Blueberry). Tannins-based drugs (Hamamelis virginiana, Aleppo's gall). Floroglucinols-based drugs (Hops, St. John's-wort).
Carbohydrate-based drugs (honey, manna ash, dextran, cyclodextrins, starchs, gums, Malva silvestris, Aloe spp).
Anthraquinonic glycoside-based drugs (Aloe spp, Rhamnus spp, Cassia spp, Rheum spp). Cyanogenic glycoside-based drugs (Prunus spp). Sulphated glycoside-based drugs (Black mustard, Garlic). Phenolic glicosyde-based drugs (Salix alba). Saponin glycosides-based drugs (Horse-chestnut, Butcher's broom, common Ivy, Panax ginseng, Centella asiatica, Common Marigold, Eleutherococcum). Digitalic glycoside-based drugs (Digitalis spp, Strophantus spp, Urginea maritima, Nerium oleander, Lily of the valley, Adonis vernalis)
Carbohydrate-based drugs (honey, manna ash, dextran ,cyclodextrins, starchs, gums, Malva silvestris, Aloe spp).
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.
Terpenes-based drugs. Essential Oils (Lavender, Oreganon, Mint, Eucalyptus, Turmeric, Lemon balm, Ginger, Chamomile, Feverfew, Valeriana officinalis, Hawthorn). Oleoresins (Myrrh). Carotenoids (Vitamin A, Lycopene; Annatto, Saffron).
Sustainability for the use of drugs obtained from natural sources. The phases of the research. Pharmacovigilance. Introduction to Pharmacoeconomics and definition of shadow costs.
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.
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. Drug renal excretion. Tubular secretion and reabsorption. Renal clearance. Transporters and other factors affecting drug elimination.
Plasmatic drug concentration: Pharmacokinetics. Systemic clearance. Plasmatic half-life. Clearance, plasmatic half-life, elimination rate constant and distribution volume relationship. 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.
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).
Nuclear receptors. Hormone responsive elements.
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.
Powders, 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.
Catecholaminergic 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 catecholaminergic transmission (Ephedra sinica, Erythroxylum coca, 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. Substance P: Capsicum. Opioid neuropeptides and their receptors. Papaver somniferum.
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.
Introduction to serotoninergic transmission. Serotoninergic receptors. Vegetable drugs active on the serotoninergic transmission (Claviceps purpurea, Psilocybe mexicana, Lophophora williamsii, Mimosa hostilis). Salvia divinorum.
Histamine: distribution and pathophysiologic role. Rubia Tibetica.
Elements of lipidergic transmission. Endocannabinoids. Cannabis sativa.
Lipidic autacoids: arachionic acid metabolites and PAF. Vegetable drugs affecting lipidic autacoids (Glycyrrhiza glabra, Ginkgo biloba).
Reactive oxygen species (ROS): Mechanisms of ROS-induced damage. Antioxidant drugs: Polyphenols-based drugs. Flavonoids and citroflavonoids. Propolis, Passiflora incarnata, Echinacea spp. Coumarins-based drugs (Sweet clover, Kella). Lignan- and neolignane-based drugs (Milk Thistle). Antocian-based drugs (Blueberry). Tannins-based drugs (Hamamelis virginiana, Aleppo's gall). Floroglucinols-based drugs (Hops, St. John's-wort).
Carbohydrate-based drugs (honey, manna ash, dextran, cyclodextrins, starchs, gums, Malva silvestris, Aloe spp).
Anthraquinonic glycoside-based drugs (Aloe spp, Rhamnus spp, Cassia spp, Rheum spp). Cyanogenic glycoside-based drugs (Prunus spp). Sulphated glycoside-based drugs (Black mustard, Garlic). Phenolic glicosyde-based drugs (Salix alba). Saponin glycosides-based drugs (Horse-chestnut, Butcher's broom, common Ivy, Panax ginseng, Centella asiatica, Common Marigold, Eleutherococcum). Digitalic glycoside-based drugs (Digitalis spp, Strophantus spp, Urginea maritima, Nerium oleander, Lily of the valley, Adonis vernalis)
Carbohydrate-based drugs (honey, manna ash, dextran ,cyclodextrins, starchs, gums, Malva silvestris, Aloe spp).
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.
Terpenes-based drugs. Essential Oils (Lavender, Oreganon, Mint, Eucalyptus, Turmeric, Lemon balm, Ginger, Chamomile, Feverfew, Valeriana officinalis, Hawthorn). Oleoresins (Myrrh). Carotenoids (Vitamin A, Lycopene; Annatto, Saffron).
Prerequisites for admission
Knowledge of the subjects taught in preparatory courses is required.
Teaching methods
Frontal lesson and Q&A
Teaching Resources
Farmacologia generale e molecolare. F. Clementi e G. Fumagalli. IV edition
UTET, Milano
Goodman & Gilman: Le Basi Farmacologiche della Terapia; Il Manuale. Brunton, Parker, Blumenthal, Buxton. II edition, Zanichelli, Milano
Botanica Farmaceutica e Farmacognosia. G. Sacchetti. Casa editrice UTET, Milano.
Slides available at the Course official web site on MyAriel.
UTET, Milano
Goodman & Gilman: Le Basi Farmacologiche della Terapia; Il Manuale. Brunton, Parker, Blumenthal, Buxton. II edition, Zanichelli, Milano
Botanica Farmaceutica e Farmacognosia. G. Sacchetti. Casa editrice UTET, Milano.
Slides available at the Course official web site on MyAriel.
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 sections: the first section 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. A passing score for first section is mandatory in order to seat in the second section of the test, that takes place immediately after the first one. Scoring of the first section 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 section accounts for 30% of the final score. Failing of the second section requires the repetition of the whole exam.
BIO/14 - PHARMACOLOGY - University credits: 8
Lessons: 64 hours
Professor:
Sala Angelo
Shifts:
Turno
Professor:
Sala AngeloProfessor(s)
Reception:
Tuesday from 10.30 am, upon arrangement by writing to the institutional email
Via Balzaretti 9 or using Zoom Cloud Meetings videoconference