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
COX – 1: responsible for mediating ___________.
COX2 - produced in ______ cell.
COX – 1: responsible for mediating normal cell activity
COX2 - produced in injured cell
Aspirin represents the major form of a group drugs known as …
the salicylates
Aspirin and other NSAIDs are effective in treating:
• Mild-to-moderate pain • Headache • Toothache • Diffuse muscular aches and soreness • RA • OA • Post-op (Toradol)
The primary NSAID used in treating fever in Adults
Aspirin
Aspirin is not recommended for use in children with …
Rye syndrome, a bleeding disorder
Primary problem with Aspirin like drugs is _______.
Caused by the ______________________.
Primary problem is gastrointestinal damage.
Caused by the loss of prostaglandins in the mucosal lining
What are the benefits of aspirin compared to other NSAIDS?
- NSAIDs have less GI problems
- NSAIDs are less toxic
- NSAIDs need a prescription and cost
COX 2 selective drugs _____ pain and inflammation
Decrease
COX 2 selective drugs have ___________ on the stomach
No adverse effects
They’re coated and dont kill good prostaglandins
COX2 selective drugs ________ platelets
Do not effect platelets because they leave thromboxins alone
COX2 selective drugs are ______ for patients with prolonged bleeding
Prolonged
COX2 selective drugs ________ risk of upper respiratory tract infections
Increase
Acetaminophen (Tylenol) compared to aspirin or NSAIDs
Fever reducer: Tylenol= Aspirin
Analgesic: Tylenol: Aspirin
Anti-inflammatory: Aspirin> tylenol
Anticoagulant: Aspirin > Tylenol
GI health: Tylenol > Aspirin
Reye Syndrome: Tylenol > Aspirin
What is the number 1 drug used to OA?
Tylenol
Pharmacokinetics of NSAIDs and Acetaminophen
Aspirin absorbed in stomach and small intestine
80-90% bound to plasma proteins
10-20% distributed throughout body
Biotransformed in blood stream
Metabolites oxidized in the liver
People with preexisting liver disease or who are chronic alcohol abusers are susceptible to liver damage
