NSAIDS Flashcards
What are the clinical features of inflammation?
Swelling, redness, pain & heat
What is the enzyme that breaks down phospholipids?
Phospholipase
What is Phospholipids broken down to?
Arachidonic acid
- -> Leukotriene
- -> Prostaglandins
- -> Thromboxane
- -> Prostacyclin
What are Prostaglandins (PGE2) responsible for?
Uterine contraction
Vasodilation- contraction of GI smooth muscles
Inhibition of gastric acid secretion
What are Thromboxane responsible for?
Platelet aggregation
What are Prostacyclins (PGI2) responsible for?
Inhibits platelet aggregation
Vasodilation
Gastric xytoprotection
What are Leukotrienes responsible for?
Chemotaxis
Hyperalgesia (hyper sensitivity to pain)
Broncho-constricion
Edema
What condition would your body produce a lot of Leukotrienes for? Specifically LTC4, LTD 4, LTE4
Asthma
How to corticosteroids work?
Work on Cyclo-oxygenase, shutting off the Cox 1 & Cox 2 pathways
Is Acetominophen (tylenol) an NSAID?
NO!
Is Aspirin an NSAID?
YES!
What is also known as the Constitutive pathway?
COX 1
Because it will always be there
What is know as the inducible pathway?
COX 2
Because this is not always available, you have to turn this on when needed.
Why would you not want COX 2 to always be on?
Because It makes you more sensitive to pain, so only turn on when needed
What do NSAIDs inhibit?
COX 1 & COX 2 pathways
Where is Prostacycline (PGI2) located?
Vascular endothelium
Where is the Cyclooxygenase (COX) pathway located?
Endoplastmatic reticulum
What are the 3 Isoforms of COX?
COX 1 (constitutive) -->Pysiological conditions COX 2 (Inducible) ---> inflammation, pain COX 3 --> Brain
Are NSAIDs selective or nonselective COX inhibitors?
NON selective
What is Acetylsalicylic acid?
Aspirin
What are some examples of Nonselective COX 1/COX 2 inhibitors?
Acetylsalicylic acid Diclofenac Indomethacin Sulindac Piroxicam Piroxicam beta-cyclodextrin (prodrug) Lornoxicam Tenoxicam Flurbiprofen Ibuprofen Ketoprofen Naproxen
What are the benefits of NSAIDs?
- Analgesia–> Prevents pain
- Antipyresis–> reduces body temp
- Reduces inflammation
- Anti-thrombotic action–> in low doses prevents clotting/platelet aggregation
- Closes the Patent Ductus Arteriosus (Indomethacin)
What are some side effects of NSAIDs?
Gastric mucosal damage Bleeding Decreased renal flow Delay/prolonged labor/contractions Asthma/anaphylaxis
What is a direct result of NSAID use that can cause ulcers
Direct toxicity “Ion trapping”
What are the 2 compounds that Aspirin splits into when metabolized?
Acetic Acid
Salicylate