Download - Overview of some drugs and their actions
PLA2
arachidonic acid
PGD-F TXA PGI 5-HPETE 12-HETE lipoxins
COXLOX
5 12 15
LTA-EmTOR
calcineurin
GCR-a
Hsp
90
DNA precursors
IL-1 R
LT R
CD52
IgEY
b2-adreno R
mACh R
Gs
Gq Ca2+ contraction
cAmp
growth, proliferation
AspirinCelecoxibIbuprofen
Paracetamol Zileuton
Cyclosporin, Tacrolimus
Corticosteroids
Zafirlukast
Cromoloyn sodium/Sodium cromoglycate
Anakinra
Alem-tuzumab
Omali-zumab
Ipratropium
Salbutamol
IL-2TNF-a, IL-1, ...
AdelimumabInfliximab
Methotrexate, Azathiprine, Mycophenolate Sodium
Agonist Antagonist
Enzyme
Ca2+
Drugs used in Inflammation
lipocortin-1
IL-1R antagonist
phosphodiesteraseTheophylline
RapamycinSirolimus
MHCII
DNA precursors
Antibiotics
wall
membrane
ribosome
DNA
ionophoresb-lactamsglycopeptides
tetracyclins aminoglycosides
macrolides fusidic acid
chloramphenicol
sulfa drugs/sulfonamidestrimethoprim
daunomycinbleomycinaziridines:
mitomycin C
DNA related enzymes
fluoroquinolonesrifampicin
antibiotics that inhibit cell wall synthesis
• Fosfomycin
• D-cycloserine
• Bacitracin
• Penicillin, Amp, Amox, Meth
• Vancomycin
• Clavulanate
• Augmentin
• Isoniazid
- inhibits pyruvyl transferase - inhibits L-Ala racemase, DADA synthase and ligase - inhibits bactoprenol- inhibits peptidoglycan transpeptidase- complexes D-Ala peptide side-chains- inhibits b-lactamase- mix of amoxicillin and clavulanate- inhibits mycolic acid synthesis
b-lactams: penicillins, carbapenems, cephalosporins, monobactamsglycopeptides: vancomycin
antibiotics that inhibit protein synthesis
• tetracycline, tetracycline
• spectinomycin, tetracycline
• streptomycin, aminoglycoside
• gentamycin, aminoglycoside
• erythromycin, macrolide
• chloramphenicol, amphenicol
• fusidic acid
- binds 30S, blocks rotation of tRNA in A-site- binds 30S and inhibits EF-G during translocation- binds 30S near A-site, decreases fidelity- binds 30S near A-site, decreases fideliy- binds 50S exit tunnel- binds 50S blocks translocation- inhibits EF-G
tetracyclines: tetracycline, spectinomycinaminoglycosides: streptomycin, gentamycinmacrolides: erythromycinamphenicols: chloramphenicol
antibiotics that inhibit DNA replication and transcription
• ciprofloxacin
• rifampicin- fluoroquinolone, bactTPII inhibitor, broad spectrum- DNA-dep RNA polymerase, blocks RNA exit tunnel, mycobacteria
Binding to DNA-related enzymesFluoroquinolones: CiprofloxacinRifampicin
antibiotics that inhibit precursor formation
Sulfa-drugsTrimethoprim
Binding to DNA itself:Anthracycline: DaunomycinChelators: BleomycinAziridines: Mitomycin C
• daunomycin
• bleomycin
• mitomycin C
- anthracycline, chelates and blocks hTPII- glycopeptide, chelates to cause ds and ss breaks, toxic- aziridine, alkylates at G-c, used in chemotherapy
antibiotics that inhibit membrane formation (in bacteria)
• sulfamethoxazole
• trimethoprim
• co-trimoxazole
- inhibits dihydropteroate synthase- inhibits dihydrofolate reductase
ionophores
• valinomycin
• gramicidin A
• polymixin
- ring-shaped K+ uniporter- polypeptide dimer- micelles
membrane
ribosome
heme degradation
Anti-protozoal drugs
ATP synthesis
DNA precursorssulfadoxinpyrimethamine
fansidar
arsenicals: melarsensuramin
amphotericin Bmiconazole
tetracycline
chloroquine