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Flashcards in Anti Inflammatory Medications Deck (26)
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What is aspirin more selective to in regards to its anti inflammatory effect



What makes the drugs go for either the COX1 or COX2

Cox 1 and 2 have slightly different structure, Cox 2 has a set of hydrophobic residues at the active site that can be targeted by these drugs but this is completely absent in Cox1


What is unique about the interaction of aspirin on Cox 1 and 2

It irreversible binds with Cox 1 and covalently modifies the active site by chemically reacting with the serine residues


What are glucocorticoids used for

To reduce inflammation and immunity


What are their side effects (GC)

They cause an increase in glucose level in the blood.


What are NSAIDs used for

To reduce fever, reduce inflammation and treat pain


What do NSAIDs work on



What do GCs work on

They work upstream of NSAIDs, inhibiting PLA2 (phospholipase A2)


What are the effects of mineral corticoids

Antidiuretic, keeps water and Na ions from going into the filtrate in the nephrons


What are the effects of acitaminophen

It reduces fever, headaches and pains. Does not reduce inflammation significantly


What is important to know regarding the dosing effects of these drugs

Drugs that have a shorter half life are quicker to act but they have to be dosed more often whereas drugs with longer half lives dont have to be taken very often but they take a while to kick in


What is the significance of dosing in terms of anti inflammatory effect and analgesic effects

Higher dosing is required for anti inflammatory than analgesic, for ibuprofen double the amount is required for anti inflammatory response as compared to the analgesic response


What is one major side effects of all kinds of NSAIDs

Nephropathy due to lower GFR


What is the interaction of NSAIDs and Aspirin

Both compete for the active site of COX1. However, NSAIDs have a higher affinity for COX1 than aspirin so taking an NSAID with aspirin can reduce the cardioprotective effect of aspirin. It is recommended that aspirin should be taken several hours before NSAID is registered to a patient


Is Acetaminphine an NSAID or GC



What is the side effect of acetaminophen



Examples of GC

Cortisol and hydrocortisone


How does GCs inhibit inflammation

1. Inhibits COX2 which is required for making NFkappaB

2. Upregulates Annexin 1 which blocks PLA2, PLA2 is also needed for inflammation since it makes leukotrines from arachidonic acid metabolism

3. It inhibits MAPK Phosphatase 1 which is involved in several pathways


Compare NSAIDs with GCs

1. Mild inflammation and fever
2. Controls pain
3. Only provides symptomatic relief to the pain and fever
4. Does not have non immunomodulatory effect

1. Severe inflammatory suppression effect
2. Autoimmune diseases
3. Transplants
4. Serious side effects


Side effects of GCs

1. Hyperglycemia
2. Behavioral changes, can induce psychosis
3. Weight gain and increased apetite
4. Na ions and water retention leading to hypertension
5. Loss in K
6. Pancreatitus and GI bleed
7. Left shift of WBCs leading to more bands and segs, (called bandemia)


What are the long term effects of GC

1. Cushing's syndrome - fat redistribution to the trunk or in the center of the body
2. Osteoporosis and impaired growth and development in children
3. Glucoma and catercts
4. HPA axis being messed up that has to do with stress response
5. Prone to infections and poor wound healing
6. Withdrawl


How do we select GCs

1. Consider the tissue that is being targetted
2. Kinetics and half life, how fast is it absorbed and how and where is it absorbed in the body
3. Mineralcorticoid effects:

There is an inverse relationship between
Mineralcorticoid (antidiuretic effect) effect and glucocorticoid effect.


How are GCs and MCs administered

1. Topical
2. Oral
3. Injections
4. IV for fast acting


Dosing considerations for GCs

1. Physiologic conc. is low dose
2. Diurnal variation: 2/3rds in the morning and 1/3rds in the afternoon to mimic cirdcadian rythm
3. High doses for short period of times
4. High doses for acute treatment and then switch to low doses


GC drug interactions

1. CYP enzyme metabolism, can have drug interactions that are metabolized by the same pathway
2. Side effects like hyperglycemia and hypertension can be beneficial or detrimental
3. Taken with food to reduce the risk of GI bleeding
4. Cytoprotective agents can be given such as proton pumps to reduce the incidence of GI bleeds


What is the selectivity for Celecoxib