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BIMM118 Main targets: Phospholipase Cβ: G-Protein-coupled Receptors see Lipid and Inositol Signaling Adenylate cyclase: • Two repeats of six transmembrane α-helices and two catalytic domains that convert ATP into cAMP • Activated or inhibited by G-proteins (a brain specific isoform is also activated through activated CaM): GTP-bound G αs activates AC, GTP-bound G αi inhibits activity (Forskolin: direct activator of AC => cAMP⇑)
BIMM118 G-Protein-coupled Receptors Cholera-toxin: causes ADP-ribosylation of G sα => release of GTP inhibited => G sα trapped in active form. cAMP regulates secretion of fluid into the intestinum => enormous loss of liquid and electrolytes => death! Pertussis-toxin: causes ADP-ribosylation of G iα , release of GDP inhibited => G iα locked in its INactive form => can not inhibit AC!
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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
Page 75 and 76: BIMM118 Drug Metabolism • Most me
Page 77 and 78: BIMM118 Drug Metabolism
Page 79 and 80: BIMM118 Drug Metabolism - Oxidation
Page 83 and 84: BIMM118 • Drug oxidation requires
Page 85 and 86: BIMM118 Epoxidation: Dealkylation:
Page 89 and 90: BIMM118 Azo-reduction: Nitro-reduct
Page 91 and 92: BIMM118 Drug Metabolism - Phase I
Page 93 and 94: BIMM118 Drug Metabolism - Glucuroni
Page 99 and 100: BIMM118 Acetylation: Drug Metabolis
Page 101 and 102: BIMM118 Drug Metabolism - Phase I &
Page 103 and 104: BIMM118 Antagonists: Drug Action: R
Page 105 and 106: BIMM118 Drug Targets
Page 107 and 108: BIMM118 Drug Targets: Receptors Res
Page 109 and 110: BIMM118 Receptors • Rapidly actin
Page 111 and 112: BIMM118 Calcium as Second Messenger
Page 113 and 114: BIMM118 Three types: Type L N T Cal
Page 115 and 116: BIMM118 Removal of Ca ++ : • Ca +
Page 123 and 124: BIMM118 G-Protein-coupled Receptors
Page 125: BIMM118 G-Protein-coupled Receptors
Page 129 and 130: BIMM118 Cyclic Nucleotides - PKA al
Page 131 and 132: BIMM118 Phosphodiesterases: Cyclic
Page 133 and 134: BIMM118 Regulation of Receptors •
Page 135 and 136: BIMM118 Receptor Down-Regulation
Page 137 and 138: BIMM118 • Examples: Nuclear Recep
Page 139 and 140: BIMM118 Phospholipids, Phosphoinosi
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 175 and 176: BIMM118 Cholinergic System - Antago
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BIMM118 Cholinergic System - Antago
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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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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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