Pharmacognosy

A.Y. 2014/2015
Lesson for
10
Max ECTS
80
Overall hours
Language
Italian
Learning objectives
The course aims at providing students with basic pharmacokinetic and pharmacodynamic information on therapeutic drugs and xenobiotics, and on how these processes affect drugs' pharmacological effects and their therapeutic outcome. Furthermore, the course is aimed at providing information on some relevant drugs of vegetable origin, of their active principles and therapeutic applications

Course structure and Syllabus

Linea A-L
Active edition
Yes
Responsible
Lessons: 80 hours
Professor: Sala Angelo
Syllabus
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.
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. Mechanisms of receptor adaptation: tachyphylaxis, desensitization, down-regulation, supersensitivity (theory and examples; relevance in the mechanism of drug action and in disease). Nuclear receptors and regulation of gene transcription.
Autonomic nervous system
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.
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.
Introduction to 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.
-Introduction to glutamatergic and GABAergic transmission.
Arachidonic acid cascade
Release and major metabolic routes of arachidonic acid, cyclo-oxygenases 1 and 2, lipo-oxygenase, prostaglandins, tromboxanes, leukotrienes and iso-eicosanoids. Major biological activities of arachidonic acid-derivatives. Non steroidal anti-inflammatory drugs: from salicylates to COX-2-selective inhibitors, mechanism of action and therapeutic uses.
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 active on the sympathetic nervous system: Ephedra sinica, Capsicum and capsaicin (introduction to peripheral transmission of pain and its interference by capsaicin, opioids, cannabinoids, vanilloids and prostaglandins), Erythroxylum coca, Claviceps purpurea, Catha edulis.
Drugs active on the parasympathetic nervous system: Atropa belladonna, Datura stramonium, Hyosciamus niger, Pilicarpus jaborandi, Physostigma venenosum, Nicotiana tabacum, Areca cathecu, Lobelia inflata, curare.
Drugs active on the central nervous system: 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 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.
Phenolic drugs:
Ursina grape, salicylic drugs.
Flavonoid-based drugs: generalities and protective roles of antioxidants.
Passiflora incarnata, Citrus spp., Ginkgo biloba.
Xanthine-based drugs:
Coffea spp., Thea spp., Theobroma cacao, Cola acuminata, Ilex paraguensis
Drugs active on the immune system:
Introduction to immunitary function and to factors that depress the immunitary system, natural immunomodulators and their mechanism of action. Echinacea spp., Panax ginseng, Eleutherococcum, Witania, Glycyrrhiza glabra, Allium sativum (immunomodulatory, antithrombotic and hypocholesterolemic activity).
Special topics:
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, fencyclidine. Cannabis sativa.
Alternative medicine: homeopathy, ayurveda, acupuncture, shiatsu, thermalism, biofeedback, chirotherapy.
Lesson period
Second semester
Linea M-Z
Active edition
Yes
Responsible
Lessons: 80 hours
Syllabus
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.
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. Mechanisms of receptor adaptation: tachyphylaxis, desensitization, down-regulation, supersensitivity (theory and examples; relevance in the mechanism of drug action and in disease). Nuclear receptors and regulation of gene transcription.
Autonomic nervous system
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.
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.
Introduction to 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.
-Introduction to glutamatergic and GABAergic transmission.
Arachidonic acid cascade
Release and major metabolic routes of arachidonic acid, cyclo-oxygenases 1 and 2, lipo-oxygenase, prostaglandins, tromboxanes, leukotrienes and iso-eicosanoids. Major biological activities of arachidonic acid-derivatives. Non steroidal anti-inflammatory drugs: from salicylates to COX-2-selective inhibitors, mechanism of action and therapeutic uses.
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 active on the sympathetic nervous system: Ephedra sinica, Capsicum and capsaicin (introduction to peripheral transmission of pain and its interference by capsaicin, opioids, cannabinoids, vanilloids and prostaglandins), Erythroxylum coca, Claviceps purpurea, Catha edulis.
Drugs active on the parasympathetic nervous system: Atropa belladonna, Datura stramonium, Hyosciamus niger, Pilicarpus jaborandi, Physostigma venenosum, Nicotiana tabacum, Areca cathecu, Lobelia inflata, curare.
Drugs active on the central nervous system: 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 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.
Phenolic drugs:
Ursina grape, salicylic drugs.
Flavonoid-based drugs: generalities and protective roles of antioxidants.
Passiflora incarnata, Citrus spp., Ginkgo biloba.
Xanthine-based drugs:
Coffea spp., Thea spp., Theobroma cacao, Cola acuminata, Ilex paraguensis
Drugs active on the immune system:
Introduction to immunitary function and to factors that depress the immunitary system, natural immunomodulators and their mechanism of action. Echinacea spp., Panax ginseng, Eleutherococcum, Witania, Glycyrrhiza glabra, Allium sativum (immunomodulatory, antithrombotic and hypocholesterolemic activity).
Special topics:
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, fencyclidine. Cannabis sativa.
Alternative medicine: homeopathy, ayurveda, acupuncture, shiatsu, thermalism, biofeedback, chirotherapy.
Lesson period
Second semester
Lesson period
Second semester
Assessment methods
Esame
Assessment result
voto verbalizzato in trentesimi