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BIMM118 Drugs Targeting the CNS 5-Hydroxytryptamine (5-HT = Serotonin) • Excitatory or Inhibitory amino acid: – Generated from tryptophane – Termination mainly by reuptake and MAO B – Seven distinct receptor types exist (7-TM): 5-HT 1 group (CNS, blood vessels) (cAMP) 5-HT 2 group (CNS, blood vessels) (IP 3 /DAG) 5-HT 3 group (peripheral nervous system) 5-HT 4 group (enteric nervous system) – Main functions: • Intestine: increases motility • Blood vessel: constriction (large vessels) dilation (arterioles) • Nerve ending: triggers nociceptive receptors 5-HT injection causes pain (5-HT found in nettle stings) • Neurons: excites some neurons, inhibits others inhibition mostly presynaptic (inhibit transmitter release) LSD = agonist of 5-HT 2A receptor
BIMM118 Drugs Targeting the CNS Sites of drug action in the CNS:
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BIMM118 “One of the features whic
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BIMM118 Definitions • Prophylacti
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BIMM118 History of Pharmacology •
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BIMM118 New Drug Discovery • Synt
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BIMM118 New Drug Discovery • Extr
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BIMM118 Orphan Drugs • Drugs for
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BIMM118 Drug Approval Historically,
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BIMM118 • Safety Drug Approval -
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BIMM118 Drug Efficacy • Efficacy
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BIMM118 Drug Efficacy - Dietary Sup
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BIMM118 Preclinical Studies • Pha
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BIMM118 • Toxicological effects P
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BIMM118 • Acute Toxicity Toxicity
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BIMM118 • Animal Studies: Toxicit
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BIMM118 Phase I Studies • Studies
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BIMM118 Phase II Studies • Pharma
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BIMM118 Phase III Studies • Rando
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BIMM118 Phase IV studies: • Postm
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BIMM118 The Four Cornerstones of Ph
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BIMM118 Oral Drug Administration
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BIMM118 Percutaneous Drug Administr
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BIMM118 Percutaneous Drug Administr
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BIMM118 Other Topical Drug Administ
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BIMM118 • Advantages: - 100% “A
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BIMM118 Drug Distribution • To be
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BIMM118 • Membrane Permeation: -
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BIMM118 Drug Distribution Bioavaila
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BIMM118 Drug Distribution Volume of
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BIMM118 Clearance (CL) [ml/min]: Dr
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BIMM118 Drug Distribution Dosage Re
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BIMM118 Drug Distribution • Drug
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BIMM118 BLOOD LEVEL TOXIC LEVELS Ma
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BIMM118 • Therapeutic Index: Ther
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BIMM118 Drug Metabolism • Most me
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BIMM118 Drug Metabolism
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BIMM118 Drug Metabolism - Oxidation
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BIMM118 • Drug oxidation requires
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BIMM118 Epoxidation: Dealkylation:
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BIMM118 Azo-reduction: Nitro-reduct
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BIMM118 Drug Metabolism - Phase I
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BIMM118 Drug Metabolism - Glucuroni
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BIMM118 Acetylation: Drug Metabolis
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BIMM118 Drug Metabolism - Phase I &
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BIMM118 Antagonists: Drug Action: R
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BIMM118 Drug Targets
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BIMM118 Drug Targets: Receptors Res
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BIMM118 Receptors • Rapidly actin
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BIMM118 Calcium as Second Messenger
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BIMM118 Three types: Type L N T Cal
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BIMM118 Removal of Ca ++ : • Ca +
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BIMM118 G-Protein-coupled Receptors
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BIMM118 Cyclic Nucleotides - PKA al
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BIMM118 Phosphodiesterases: Cyclic
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BIMM118 Regulation of Receptors •
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BIMM118 Receptor Down-Regulation
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BIMM118 • Examples: Nuclear Recep
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BIMM118 Phospholipids, Phosphoinosi
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BIMM118 • Prostaglandins: Arachid
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BIMM118 • Leukotrienes: Arachidon
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BIMM118 Growth Factor Receptors •
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BIMM118 Signaling through Adapter p
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BIMM118 • “Classical” hormone
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BIMM118 Cytokine Receptors • Curr
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BIMM118 Ser/Thr-kinase Receptors Tr
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BIMM118 NFκB - originally identifi
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BIMM118 Autonomic Nervous System
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BIMM118 Transmitters: • Acetylcho
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BIMM118 Cholinergic receptors: •
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BIMM118 Cholinergic System - Agonis
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BIMM118 Cholinergic System - Antago
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BIMM118 Autonomic Nervous System
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BIMM118 Transmitters: • Acetylcho
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BIMM118 Adrenergic receptors: • a
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BIMM118 Sympathomimetics Adrenergic
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BIMM118 Sympathomimetics Non-select
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BIMM118 Sympathomimetics α 1 - sel
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BIMM118 β 1 - receptors • Mostly
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BIMM118 Sympathomimetics β 2 - sel
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BIMM118 Sympatholytics α 2 - selec
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BIMM118 Sympatholytics β - selecti
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BIMM118 β-Sympatholytics Epinephri
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BIMM118 Cardiovascular Pharmacology
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BIMM118 Potential drug targets: Ant
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BIMM118 Antihypertensive Drugs:Vaso
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BIMM118 Antihypertensive Drugs: Vas
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BIMM118 Antihypertensive Drugs: RAA
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BIMM118 Antihypertensive Drugs: RAA
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BIMM118 • Nitroglycerin - Organic
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BIMM118 Arrhythmias: Cardiac Arrhyt
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BIMM118 Arrhythmias: Cardiac Arrhyt
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BIMM118 Arrhythmias: Other antiarrh
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BIMM118 Congestive Heart Failure Cl
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BIMM118 Cardiac Glycosides: Congest
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BIMM118 Cardiac Glycosides: Congest
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BIMM118 Renal Pharmacology Diuretic
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BIMM118 Functions Renal Pharmacolog
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BIMM118 Diuretics: • Increase out
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BIMM118 Diuretics: Renal Pharmacolo
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BIMM118 Renal Pharmacology Major si
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BIMM118 Diuretics: Osmotic diuretic
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BIMM118 Renal Pharmacology Uric aci
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BIMM118 Gastrointestinal Pharmacolo
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BIMM118 Antacids: Gastrointestinal
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BIMM118 Antacids: Gastrointestinal
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BIMM118 Diabetes mellitus Pancreas:
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BIMM118 Diabetes mellitus
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BIMM118 Diabetis mellitus: Diabetes
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BIMM118 Insulin: Diabetes mellitus
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BIMM118 Insulin: • Insulin Glargi
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BIMM118 Diabetes mellitus Oral hypo
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BIMM118 Diabetes mellitus Oral hypo
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BIMM118 Novel concepts (cont’d):
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BIMM118 Artherosclerosis: Hyperlipi
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BIMM118 Artherosclerosis: Hyperlipi
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BIMM118 Cholesterol: - 60-70% (=100
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BIMM118 Lipid-lowering drugs: Hyper
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BIMM118 Lipid-lowering drugs: Hyper
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BIMM118 Hyperlipidemia
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BIMM118 Adrenal gland: • Medulla:
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BIMM118 Adrenocortical Hormones Ste
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BIMM118 Glucocorticoids (GC): Adren
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BIMM118 Glucocorticoids (GC): • H
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BIMM118 Glucocorticoids (GC): • T
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BIMM118 Steroid-based Drugs • Sex
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Page 311 and 312: BIMM118 Sex Steroids Estrogens - Es
Page 313 and 314: BIMM118 Anti-Estrogens • Tamoxife
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Page 317 and 318: BIMM118 Sex Steroids • Male repro
Page 319 and 320: BIMM118 Androgens Sex Steroids •
Page 321 and 322: BIMM118 Anabolic Androgens • Dehy
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Page 329 and 330: BIMM118 Drugs against Allergies •
Page 331 and 332: BIMM118 Allergy - Symptoms
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Page 371 and 372: BIMM118 Classical neuroleptics: Adv
Page 373 and 374: BIMM118 Pathology: Parkinson’s Di
Page 375 and 376: BIMM118 Dopamine replacement: Parki
Page 377 and 378: BIMM118 Pathology: Epilepsy - Group
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Page 381 and 382: BIMM118 Ethanol Most widely consume
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Page 399 and 400: BIMM118 Mode of action: Local Anest
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BIMM118 Chemotherapeutic Agents •
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BIMM118 Antibiotics • Resistance:
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BIMM118 Classification: • Cell wa
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BIMM118 Antibiotics - Cell wall syn
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BIMM118 Antibiotics - Protein synth
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BIMM118 Sulfonamides Antibiotics -
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BIMM118 Quinolones Antibiotics - Qu
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BIMM118 Antibiotics - Summary
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BIMM118 Fungal Growth Patterns •
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BIMM118 Fungal Habitats • Most cl
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BIMM118 Superficial Mycoses • Tin
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BIMM118 • Tinea corporis Cutaneou
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BIMM118 • Sporotrichosis Subcutan
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BIMM118 Systemic Mycosis • Histop
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BIMM118 Opportunistic Mycosis - Som
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BIMM118 Opportunistic Mycosis • C
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BIMM118 Differences between fungi a
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BIMM118 Antifungal Drugs - Polyenes
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BIMM118 Imidazoles • Clotrimazole
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BIMM118 Antifungal Drugs - Azoles T
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BIMM118 Antifungal Drugs - Antimeta
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BIMM118 Antifungal Drugs - Allylami
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