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BIMM118 Antibiotics - Cell wall synthesis inhibitors Bacterial cell wall: Three types: • Gram-negative (e.g. E.coli, Salmonella) – Few peptidoglycan layers (Lipopolysaccheride) • Gram-positive (e.g. Staphylococci, Listeria) – Many peptidoglycan layers (Lipoteichoic acid) – Stains w/ crystal-violet/iodine • Acid-fast positive (Mycobacteria) – Cell wall contains waxy substance (Mycolic acid) – Stain w/ acid fast test (heating required)
BIMM118 Antibiotics - Cell wall synthesis inhibitors Beta-lactam antibiotics: 1928 - Alexander Fleming observes the antibacterial effects of Penicillin 1940 - Florey and Chain extract Penicillin Classification: • Penicillins – Narrow spectrum – penicillinase sensitive – Narrow spectrum – penicillinase resistant – Broad spectrum penicillins – Extended-spectrum penicillins • Cephalosporines • Carbapenems • Monobactams • Vancomycin, Bacitracin
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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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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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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
Page 379 and 380: BIMM118 Treatment strategies: Inhib
Page 381 and 382: BIMM118 Ethanol Most widely consume
Page 383 and 384: BIMM118 Treatment strategies: • D
Page 385 and 386: BIMM118 General Anesthetics State o
Page 387 and 388: BIMM118 General Anesthetics Inhalat
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Page 391 and 392: BIMM118 Opioid Analgesics Opiates:
Page 393 and 394: BIMM118 Opiates: Mechanism of analg
Page 395 and 396: BIMM118 Codeine (3-methoxy-morphine
Page 397 and 398: BIMM118 Meperidine (Pethidine): - A
Page 399 and 400: BIMM118 Mode of action: Local Anest
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Page 409 and 410: BIMM118 Chemotherapeutic Agents •
Page 411 and 412: BIMM118 Antibiotics • Resistance:
Page 413: BIMM118 Classification: • Cell wa
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Page 425 and 426: BIMM118 Antibiotics - Protein synth
Page 433 and 434: BIMM118 Sulfonamides Antibiotics -
Page 435 and 436: BIMM118 Quinolones Antibiotics - Qu
Page 437 and 438: BIMM118 Antibiotics - Summary
Page 439 and 440: BIMM118 Fungal Growth Patterns •
Page 441 and 442: BIMM118 Fungal Habitats • Most cl
Page 443 and 444: BIMM118 Superficial Mycoses • Tin
Page 445 and 446: BIMM118 • Tinea corporis Cutaneou
Page 447 and 448: BIMM118 • Sporotrichosis Subcutan
Page 449 and 450: BIMM118 Systemic Mycosis • Histop
Page 451 and 452: BIMM118 Opportunistic Mycosis - Som
Page 453 and 454: BIMM118 Opportunistic Mycosis • C
Page 455 and 456: BIMM118 Differences between fungi a
Page 457 and 458: BIMM118 Antifungal Drugs - Polyenes
Page 459 and 460: BIMM118 Imidazoles • Clotrimazole
Page 461 and 462: BIMM118 Antifungal Drugs - Azoles T
Page 463 and 464: BIMM118 Antifungal Drugs - Antimeta
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BIMM118 Antifungal Drugs - Allylami
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