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PMSC | 213




Faisal A. Al Moaiqel
                30 05 03 008
Abdulaziz Alenazi              COX 1,2
                30 05 01 007
Mohammed Al-Sherbrain          Inhibitors
                30 05 02 013
Meshal A. Almaghrabi
                30 05 02 008
Khalid N. Al Dalbahi
                28 05 03 016
Objectives
 Overview.
 Mechanism     of Action.
 Medical Uses.
 Side Effects.
OVERVIEW
Overview




what’s COXs and their roles?
 Cyclooxygenase    is an enzyme responsible
  about formation prostanoids . Ex:
  prostaglandins - fatty-acid derivatives
  located all over body.
 The role of COX is mediates the
  conversion of arachidonic acid into
  PGH2,which is then converted to various
  PGs by specific syntheses COX 1,2 .
Overview




How NSAIDs work ?
 RegularNon-steroidal anti-inflammatory
 drugs (NSAIDs) work by inhibit the
 production of prostaglandins (PGs) ,
 which will inhabit their inflammation and
 immune response effects.
Overview




COX-1
 COX-1   is expressed in many tissues
  (including the gastrointestinal tract,
  platelets, and kidney)
 And it's responsible for producing
  prostanoids that regulate normal
  physiologic functions.
Overview




COX-2
    COX-2 is the inducible form responsible
    for the production of prostanoids in
    response to a variety of evoking stimuli
    (including cytokines, growth factors,
    mitogens, and tumor promoters) in
    different tissues and for the mediation of
    inflammation and pain in certain diseases.
Mechanism
of Action
Mechanism of Action




 Most NSAIDs act as non-selective inhibitors
 of the enzyme cyclooxygenase, inhibiting
 both the cyclooxygenase-1 (COX-1) and
 cyclooxygenase-2 (COX-2) isoenzymes.
Mechanism of Action




 Cyclooxygenase  catalyzes the formation
 of prostaglandins and thromboxane from
 arachidonic acid . Prostaglandins act
 (among other things) as messenger
 molecules in the process of inflammation.
Medical Uses
Medical Uses




 NSAIDs are usually indicated for the
 treatment of acute or chronic conditions
 where pain and inflammation are present.
 Research continues into their potential for
 prevention of colorectal cancer, and
 treatment of other conditions, such as
 cancer and cardiovascular disease.
Medical Uses




 NSAIDs are generally indicated for the
  symptomatic relief of the following
  conditions:
 Rheumatoid arthritis.
 Inflammatory arthropathies.
 Dysmenorrhea.
 Headache and migraine.
Medical Uses




 Aspirin, the only NSAID able to irreversibly
  inhibit COX-1, is also indicated for
  inhibition of platelet aggregation. This is
  useful in the management of arterial
  thrombosis and prevention of adverse
  cardiovascular events. Aspirin inhibits
  platelet aggregation by inhibiting the
  action of thromboxane A2
Side Effects
Side Effects


The Main Side Effect of NSAIDs
Is:
 Cardiovascular.
    The link between COX-2 inhibitors and
     increased risk of heart attack is now well
     established.
Others:
 Gastrointestinal.
 Inflammatory bowel disease.
 Renal Disorders.
Thanks! :)

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Cox 1,2 inhibitors

  • 1. PMSC | 213 Faisal A. Al Moaiqel 30 05 03 008 Abdulaziz Alenazi COX 1,2 30 05 01 007 Mohammed Al-Sherbrain Inhibitors 30 05 02 013 Meshal A. Almaghrabi 30 05 02 008 Khalid N. Al Dalbahi 28 05 03 016
  • 2. Objectives  Overview.  Mechanism of Action.  Medical Uses.  Side Effects.
  • 4. Overview what’s COXs and their roles?  Cyclooxygenase is an enzyme responsible about formation prostanoids . Ex: prostaglandins - fatty-acid derivatives located all over body.  The role of COX is mediates the conversion of arachidonic acid into PGH2,which is then converted to various PGs by specific syntheses COX 1,2 .
  • 5. Overview How NSAIDs work ?  RegularNon-steroidal anti-inflammatory drugs (NSAIDs) work by inhibit the production of prostaglandins (PGs) , which will inhabit their inflammation and immune response effects.
  • 6. Overview COX-1  COX-1 is expressed in many tissues (including the gastrointestinal tract, platelets, and kidney)  And it's responsible for producing prostanoids that regulate normal physiologic functions.
  • 7. Overview COX-2  COX-2 is the inducible form responsible for the production of prostanoids in response to a variety of evoking stimuli (including cytokines, growth factors, mitogens, and tumor promoters) in different tissues and for the mediation of inflammation and pain in certain diseases.
  • 9. Mechanism of Action  Most NSAIDs act as non-selective inhibitors of the enzyme cyclooxygenase, inhibiting both the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) isoenzymes.
  • 10. Mechanism of Action  Cyclooxygenase catalyzes the formation of prostaglandins and thromboxane from arachidonic acid . Prostaglandins act (among other things) as messenger molecules in the process of inflammation.
  • 12. Medical Uses  NSAIDs are usually indicated for the treatment of acute or chronic conditions where pain and inflammation are present. Research continues into their potential for prevention of colorectal cancer, and treatment of other conditions, such as cancer and cardiovascular disease.
  • 13. Medical Uses  NSAIDs are generally indicated for the symptomatic relief of the following conditions:  Rheumatoid arthritis.  Inflammatory arthropathies.  Dysmenorrhea.  Headache and migraine.
  • 14. Medical Uses  Aspirin, the only NSAID able to irreversibly inhibit COX-1, is also indicated for inhibition of platelet aggregation. This is useful in the management of arterial thrombosis and prevention of adverse cardiovascular events. Aspirin inhibits platelet aggregation by inhibiting the action of thromboxane A2
  • 16. Side Effects The Main Side Effect of NSAIDs Is:  Cardiovascular.  The link between COX-2 inhibitors and increased risk of heart attack is now well established. Others:  Gastrointestinal.  Inflammatory bowel disease.  Renal Disorders.