Overview of some drugs and their actions.

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Overview of some drugs and their actions.

  1. 1. Agonist Drugs used in Inflammation Antagonist Enzyme Adelimumab lipocortin-1 PLA2 Infliximab IL-2 Aspirin arachidonic acid TNF-a, IL-1, ... Celecoxib LOX Ibuprofen COX IL-1R Paracetamol Zileuton antagonist 5 12 15 PGD-F TXA PGI 5-HPETE 12-HETE lipoxins Cromoloyn sodium/ Sodium cromoglycate Rapamycin Anakinra Sirolimus LTA-E IL-1 R mTOR growth, proliferation Zafirlukast LT R Cyclosporin, Tacrolimus Ca2+ calcineurin Alem-tuzumab CD52 Hsp90 Corticosteroids GCR-a YOmali-zumab IgE MHCII Theophylline phosphodiesterase b2-adreno R Gs cAmp Salbutamol Gq Ca2+ contraction DNA precursors mACh R Methotrexate, Azathiprine, Ipratropium Mycophenolate Sodium
  2. 2. Antibiotics membrane b-lactams ionophoresglycopeptides wall fluoroquinolones rifampicin ribosome DNA related tetracyclins enzymes aminoglycosides macrolides fusidic acid chloramphenicol daunomycin bleomycin aziridines: mitomycin C DNA sulfa drugs/ sulfonamides DNA precursors trimethoprim
  3. 3. antibiotics that inhibit cell wall synthesis b-lactams: penicillins, carbapenems, cephalosporins, monobactams glycopeptides: vancomycin• Fosfomycin - inhibits pyruvyl transferase• D-cycloserine - inhibits L-Ala racemase, DADA synthase and ligase• Bacitracin - inhibits bactoprenol• Penicillin, Amp, Amox, Meth - inhibits peptidoglycan transpeptidase• Vancomycin - complexes D-Ala peptide side-chains• Clavulanate - inhibits b-lactamase• Augmentin - mix of amoxicillin and clavulanate• Isoniazid - inhibits mycolic acid synthesisantibiotics that inhibit protein synthesistetracyclines: tetracycline, spectinomycinaminoglycosides: streptomycin, gentamycinmacrolides: erythromycinamphenicols: chloramphenicol• tetracycline, tetracycline - binds 30S, blocks rotation of tRNA in A-site• spectinomycin, tetracycline - binds 30S and inhibits EF-G during translocation• streptomycin, aminoglycoside - binds 30S near A-site, decreases fidelity• gentamycin, aminoglycoside - binds 30S near A-site, decreases fideliy• erythromycin, macrolide - binds 50S exit tunnel• chloramphenicol, amphenicol - binds 50S blocks translocation• fusidic acid - inhibits EF-G
  4. 4. antibiotics that inhibit DNA replication and transcriptionBinding to DNA-related enzymesFluoroquinolones: CiprofloxacinRifampicin• ciprofloxacin - fluoroquinolone, bactTPII inhibitor, broad spectrum• rifampicin - DNA-dep RNA polymerase, blocks RNA exit tunnel, mycobacteriaBinding to DNA itself:Anthracycline: DaunomycinChelators: BleomycinAziridines: Mitomycin C• daunomycin - anthracycline, chelates and blocks hTPII• bleomycin - glycopeptide, chelates to cause ds and ss breaks, toxic• mitomycin C - aziridine, alkylates at G-c, used in chemotherapyantibiotics that inhibit precursor formation Sulfa-drugs Trimethoprim• sulfamethoxazole - inhibits dihydropteroate synthase• trimethoprim - inhibits dihydrofolate reductase• co-trimoxazoleantibiotics that inhibit membrane formation (in bacteria) ionophores• valinomycin - ring-shaped K+ uniporter• gramicidin A - polypeptide dimer• polymixin - micelles
  5. 5. Anti-protozoal drugs membrane amphotericin B miconazole heme degradation chloroquine ribosome tetracycline ATP synthesis arsenicals: melarsen suramin sulfadoxin DNA precursors pyrimethamine fansidar

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