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BIMM118 Sympatholytics α - selective antagonists Adrenergic System - Antagonists Promote vasodilation => decreased peripheral resistance => blood pressure (Side effects: reflex tachycardia and postural hypotension) Relaxation of the smooth muscles in the bladder neck Clinical applications: Hypertension; Urinary retention Non-selective α-antagonist: • Phentolamine (for pheochromocytoma) • Ergot alkaloids see 5HT receptor α 1 -selective antagonists: • Prazosin (Minipress®) first α 1 - selective antagonist • Terazosin longer half-life • Doxazosin longer half-life
BIMM118 Sympatholytics α 2 - selective antagonists • Yohimbine Adrenergic System - Antagonists – Chief active compound in Pausinystalia yohimbine (bark) – Effects opposite of Clonidine – Enters CNS => increased sympathetic output => increased heart rate, blood pressure, can cause severe tremors – Ingredient in many weight loss products – Extensive (past) use in treatment of male sexual dysfunction
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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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Page 145 and 146: BIMM118 • Prostaglandins: Arachid
Page 147 and 148: BIMM118 • Leukotrienes: Arachidon
Page 149 and 150: BIMM118 Growth Factor Receptors •
Page 151 and 152: BIMM118 Signaling through Adapter p
Page 153 and 154: BIMM118 • “Classical” hormone
Page 155 and 156: BIMM118 Cytokine Receptors • Curr
Page 157 and 158: BIMM118 Ser/Thr-kinase Receptors Tr
Page 159 and 160: BIMM118 NFκB - originally identifi
Page 161 and 162: BIMM118 Autonomic Nervous System
Page 163 and 164: BIMM118 Transmitters: • Acetylcho
Page 165 and 166: BIMM118 Cholinergic receptors: •
Page 167 and 168: BIMM118 Cholinergic System - Agonis
Page 173 and 174: BIMM118 Cholinergic System - Antago
Page 181 and 182: BIMM118 Autonomic Nervous System
Page 183 and 184: BIMM118 Transmitters: • Acetylcho
Page 185 and 186: BIMM118 Adrenergic receptors: • a
Page 187 and 188: BIMM118 Sympathomimetics Adrenergic
Page 189 and 190: BIMM118 Sympathomimetics Non-select
Page 191 and 192: BIMM118 Sympathomimetics α 1 - sel
Page 193 and 194: BIMM118 β 1 - receptors • Mostly
Page 195: BIMM118 Sympathomimetics β 2 - sel
Page 199 and 200: BIMM118 Sympatholytics β - selecti
Page 201 and 202: BIMM118 β-Sympatholytics Epinephri
Page 203 and 204: BIMM118 Cardiovascular Pharmacology
Page 209 and 210: BIMM118 Potential drug targets: Ant
Page 211 and 212: BIMM118 Antihypertensive Drugs:Vaso
Page 213 and 214: BIMM118 Antihypertensive Drugs: Vas
Page 215 and 216: BIMM118 Antihypertensive Drugs: RAA
Page 217 and 218: BIMM118 Antihypertensive Drugs: RAA
Page 219 and 220: BIMM118 • Nitroglycerin - Organic
Page 221 and 222: BIMM118 Arrhythmias: Cardiac Arrhyt
Page 223 and 224: BIMM118 Arrhythmias: Cardiac Arrhyt
Page 225 and 226: BIMM118 Arrhythmias: Other antiarrh
Page 227 and 228: BIMM118 Congestive Heart Failure Cl
Page 229 and 230: BIMM118 Cardiac Glycosides: Congest
Page 231 and 232: BIMM118 Cardiac Glycosides: Congest
Page 233 and 234: BIMM118 Renal Pharmacology Diuretic
Page 235 and 236: BIMM118 Functions Renal Pharmacolog
Page 237 and 238: BIMM118 Diuretics: • Increase out
Page 239 and 240: BIMM118 Diuretics: Renal Pharmacolo
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Page 243 and 244: BIMM118 Diuretics: Osmotic diuretic
Page 245 and 246: 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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BIMM118 Sex Steroids • Female rep
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BIMM118 Sex Steroids • Female rep
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BIMM118 Sex Steroids Estrogens - Es
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BIMM118 Anti-Estrogens • Tamoxife
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BIMM118 Progesterons Sex Steroids T
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BIMM118 Sex Steroids • Male repro
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BIMM118 Androgens Sex Steroids •
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BIMM118 Anabolic Androgens • Dehy
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BIMM118 GnRH analogs/modifiers Sex
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BIMM118 Oral Contraceptives Sex Ste
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BIMM118 Contraceptives Sex Steroids
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BIMM118 Drugs against Allergies •
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BIMM118 Allergy - Symptoms
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BIMM118 Allergy - Food • Allergic
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BIMM118 Latex has cross-reactive ep
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BIMM118 Allergy - Drugs Predominant
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BIMM118 Allergy - Mediators
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BIMM118 Allergy - Histamine Histami
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BIMM118 Allergy - Drugs Targeting H
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BIMM118 H1-Antagonists (“Antihist
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BIMM118 H1-Antagonists (“Antihist
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BIMM118 Mast Cell Stabilizers • C
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BIMM118 Allergy - Leukotrienes Cys-
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BIMM118 Drugs Targeting the CNS •
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BIMM118 Drugs Targeting the CNS Glu
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BIMM118 Dopamine • Inhibitory ami
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BIMM118 Drugs Targeting the CNS Sit
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BIMM118 Hypnotics / Anxiolytics Bar
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BIMM118 Hypnotics / Anxiolytics Ben
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BIMM118 Antidepressants Clinical De
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BIMM118 Tricyclic antidepressants:
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BIMM118 Schizophrenia Endogenous ps
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BIMM118 Classical neuroleptics: Adv
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BIMM118 Pathology: Parkinson’s Di
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BIMM118 Dopamine replacement: Parki
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BIMM118 Pathology: Epilepsy - Group
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BIMM118 Treatment strategies: Inhib
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BIMM118 Ethanol Most widely consume
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BIMM118 Treatment strategies: • D
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BIMM118 General Anesthetics State o
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BIMM118 General Anesthetics Inhalat
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BIMM118 General Anesthetics Intrave
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BIMM118 Opioid Analgesics Opiates:
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BIMM118 Opiates: Mechanism of analg
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BIMM118 Codeine (3-methoxy-morphine
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BIMM118 Meperidine (Pethidine): - A
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BIMM118 Mode of action: Local Anest
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BIMM118 Classification: Local Anest
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BIMM118 Clinical use and Administra
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BIMM118 NSAIDs Non-Steroidal Anti-I
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BIMM118 NSAIDs Non-Steroidal Anti-I
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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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