Overview of some drugs and their actions.

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PLA2 arachidonic acid PGD-F TXA PGI 5-HPETE 12-HETE lipoxins COX LOX 5 12 15 LTA-E mTOR calcineurin GCR-a Hsp90 DNA precursors IL-1 R LT R CD52 IgE Y b2-adreno R mACh R Gs Gq Ca2+ contraction cAmp growth, proliferation Aspirin Celecoxib Ibuprofen Paracetamol Zileuton Cyclosporin, Tacrolimus Corticosteroids Zafirlukast Cromoloyn sodium/ Sodium cromoglycate Anakinra Alem- tuzumab Omali- zumab Ipratropium Salbutamol IL-2 TNF-a, IL-1, ... Adelimumab Infliximab Methotrexate, Azathiprine, Mycophenolate Sodium Agonist Antagonist Enzyme Ca2+ Drugs used in Inflammation lipocortin-1 IL-1R antagonist phosphodiesterase Theophylline Rapamycin Sirolimus MHCII

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Transcript of Overview of some drugs and their actions.

Page 1: 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

Page 2: Overview of some drugs and their actions.

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

Page 3: Overview of some drugs and their actions.

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

Page 4: Overview of some drugs and their actions.

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

Page 5: Overview of some drugs and their actions.

membrane

ribosome

heme degradation

Anti-protozoal drugs

ATP synthesis

DNA precursorssulfadoxinpyrimethamine

fansidar

arsenicals: melarsensuramin

amphotericin Bmiconazole

tetracycline

chloroquine