Pharm 1 - NSAIDs

drraythe's version from 2015-06-13 21:39


Question Answer
5 main pillars of inflammation?(1) Calor (Heat)
(2) Rubor (Redness)
(3) Tumor (Swelling)
(4) Dolor (Pain)
(5) Loss of fxn
The #1 chemical of the inflammatory response? (What mediates the inflammatory response)?Prostaglandins
Look at 2nd slide chart?Pain in my ass
What acid does COX1/2/prostaglandins come from?Arachidonic acid
What is the therapeutic target in treatment of inflammation?COX-2 INHIBITION
What kind of molecules are COX1 and COX2? What do they do?Enzymes. They turn arachidonic acid into prostaglandins
What kind of drug would you say a COX-inhibitor is?A TYPE of NSAID (non-steroidal anti-inflammatory)
What do the COX enzymes produce?Prostaglandins
For COX-1: When is it around? Where is it present? What kind of prostaglandins does it produce? What results from it?Constitutive (always there), present in many tissues ("house-keeping" COX), make "Good prostaglandins" Regulatory
For COX-2: When is it around? What kind of prostaglandins does it make? What results from it?Induced during inflammation, makes pro-inflammatory prostaglandins, causes signs of inflammation and nociception
Which COX has a wider channel? Which COX has a hydrophilic side pocket?COX-1 has a wider channel. COX-2 has a hydrophilic side pocket
What contributes to allowing a COX-2 inhibitor to be selective?Channel is narrow so less drugs can get in there. Also the side pocket is something unique it can be selective for
What are the specific COX-2 inhibitors available?Robenacoxib, Firocoxib, Mavacoxib (ALL HAVE COX IN THEIR NAMES)
How do specific COX-2 inhibitors compare to NSAIDS?No better analgesic or anti-inflammatory effects compared to traditional NSAIDs (he said they have better safety tho)
What are the preferential COX-1 inhibitors?Flunixin Meglumine
Acetylsalicylicacid (Aspirin)
What are the preferential COX-2 inhibitors?Nimesulide
Carprofin (2 nasty nancies kill + cook mindy)
What does COX-2 do (cause in the body) that COX-1 doesnt? (4)?Renal sodium balance, kidney development, anti-tumor effects, myocardial protection
What does COX-1 AND COX-2 both do?Inflammation
GI mucosal activity
Endothelial PGI (2) synthesis
What are the two major mechanisms for treating inflammation that are COX-INDEPENDANT?(1) Direct effect on transcription factors (NF-kappaB)
(2) Changes in the activity of cellular kinases
What drugs directly affect the transcription factors (NF-kappaB) (COX independent) (4)?Acetylsalycilicacid
Flunixin Meglumine (& I can transcript massive farts)
What are the two ways drugs can change the activity of cellular kinases (enzyme that phosphorylates shit) (COX-independant)?(1) Inhibition of apoptosis
(2) Inhibition of de-differentiation of chondrocytes
What are the three major COX-inhibitor side-effects?(1) GI effects (ulcers!)
(2) Renal toxicity
(3) Stops coagulation
GI side effects of COX inhibitors - problem they cause? How does it cause the problem? What does the extent of the damage depend on?Cause ULCERS, because they block PGE2's (which are responsible for blood flow, maturation of gastric lining cells and mucous secretion). Severity often depends on the SPECIES.
How could you avoid/treat the GI issues caused by COX-inhibitors?You give a PGE1 analogue to prevent the ulcer. MISOPROSTOL!!
How does a COX inhibitor cause renal toxicity?Prostaglandins mediate regulation of renal blood flow, and COX inhibitors stop these
What is the damage caused by COX-inhibitor renal toxicity?Papillary necrosis
(Related to kidney toxicity) what situations would you not use COX-inhibitors in? (2)?(1) Concurrent use of other nephrotoxic drugs
(2) Shock, dehydration, post-surgical
How do COX inhibitors affect the blood? Which COX does this (in general or specific)? Is it good or bad?They INHIBIT coagulation. ONLY COX-1 because they are in platelets. Acetylsalicylic acid binds IRREVERSIBLY to COX-1 in platelets. Can be good OR bad
What two factors affect oral admin of NSAIDs?Food intake and pH
How is absorption of NSAIDs after injection?Good
Do NSAIDs bind to proteins?Yes they are HIGHLY PROTEIN BOUND
How are NSAIDs metabolized? Excreted?Metabolized by mixed fxn oxidases in the liver. Excreted in urine
How can you help inflammation with supportive therapy (not drugs)?Immobilization, rest, Tx underlying cause, bladder emptying, food/water

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