1 Nonsteroidal Anti-Inflammatory Drugs Flashcards
NSAID – distinct pharmacologic properties:
- Ability to decrease inflammation
- Ability to relieve mild-to-moderate pain
- Ability to decrease elevated body temperature associated with fever
- Ability to decrease blood clotting by inhibiting platelet aggregation
Best representative of an NSAID is…
Aspirin – acetylsalicylic
Aspirin interferes with biosynthesis of…
prostaglandins
In 1970 aspirin was found to inhibit the synthesis of a group of compounds known as prostaglandins.
Prostaglandins
They are a group of lipid like compounds that exhibit a wide range of physiologic activities.
They appear to be hormones that act locally to help regulate cell function.
Which type of cells produce prostaglandins?
ALL the cells… except blood cells
Prostaglandins, thromboxanes, and leukotrienes are referred to as …
Eicosanoid
True or false: The 20-carbon fatty acid prostaglandin is derived from can be metabolized by one specific enzyme.
False: The 20-fatty acid can be metabolized by
several enzymes systems
Primary enzyme system involves the _____ enzyme, and synthesizes _________ and _________
Cyclooxygenase (COX)
prostaglandins and thromboxanes
Secondary enzyme involves the _____ enzyme, and synthesizes __________
lipoxygenase (LOX)
leukotrienes
A drug that blocks COX will eliminate all ________ and ________ synthesis in that cell
Prostaglandin and thromboxane
Aspirin are ________ inhibitors, they do not inhibit _______ enzyme
Aspirin are cyclooxygenase (COX)
inhibitors,
they do not inhibit lipoxygenase (LOX)enzyme
Leukotrienes mediate what?
airway inflammation.
Drugs have been developed to reduce leukotriene-mediated inflammation by blocking _____ enzymes, or by blocking leukotriene
receptors on _______ tissues
Block LOX enzymes
Or block receptors on respiratory tissues
Do prostaglandins increase or decrease with inflammation?
Increased prostaglandin synthesis is usually detected at the site of local inflammation
What are the roles of Eicosanoids in health and disease? How do you decrease these for treatment?
Treat with aspirin to decrease prostaglandins
- Increased prostaglandins at sites of local inflammation
- Mediate pain stimuli and increase sensitivity
- Prostaglandins help elevate body temperature
Increased prostaglandin production accompanies dysmenorrhea
Thromboxanes cause platelet aggregation that result in blood clot formation
Other Pathologies: • Hypertension •Colon Cancer • Asthma - increased blood flow • DM • MS- CNS inflammation