Anti-Inflammatory Pharm

Question 1

Examples of anti-inflammatory drugs (NSAIDs)

Answer 1

aspirin, ibuprofen, naproxen, indomethacin, celecoxib

Question 2

MOA of NSAIDs

Answer 2

this class of drugs are COX inhibitors (Cyclooxygenases exist as isoenzymes: COX-1 has a broad tissue distribution while COX-2 has a narrower tissue distribution and is strongly activated during an inflammatory response)

Question 3

What does COX-1 have a positive effect on?

Answer 3

GI tract and renal system– this means that COX-1 inhibitors may cause GI irritation and renal side effects

Question 4

COX-2 inhibitors reduce GI and renal side effects, however they put the patient at risk for…

Answer 4

thrombosis. COX-2 inhibitors appear to increase the risk of thrombogenicity, MI, stroke and suppression of wound healing

Question 5

Which NSAID is a selective COX-2 inhibitor

Answer 5

celecoxib

Question 6

therapeutic uses for NSAIDs

Answer 6

treatment for inflammatory diseases, antipyretics, mild analgesics, antithrombic and treatment of menstrual cramping

Question 7

pharmacotoxicology of NSAIDs

Answer 7

Gastric distress: increased HCl secretion by parietal cells
Spontaneous hemorrhage: caused by non-selective NSAIDs

Question 8

What is thromboxane? (TXA)

Answer 8

a substance needed to help platelets clump together, activated by arachidonic acid

Question 9

How do COX-2 inhibitors interfere with platelet aggregation?

Answer 9

TYPICALLY, there is a counter-regulation of platelet aggregation by a substance called prostacyclin. Prostacyclin is activated by COX-2. When a COX-2 inhibitor is in place, prostacyclin is not activated, thus is unable to block platelet aggregation

Question 10

What is prostacyclin?

Answer 10

A substance that helps counter-regulate platelet aggregation

Question 11

Pharmacotoxicology of Aspirin

Answer 11

may induce Reye’s syndrome in children (a syndrome that may lead to encephalopathy, hypoglycemia, development of hepatic and renal fatty deposits and cerebral edema)

Question 12

Examples of steroid anti-inflammatory drugs (glucocorticoids/corticosteroids)

Answer 12

Hydrocortisone (cortisone) (short acting), prednisone (intermediate acting), dexamethasone (long acting)

Question 13

MOA of steroid anti-inflammatory drugs

Answer 13

cortisol receptor agonists that, in high doses, mimic the natural hormone cortisol and suppresses genes that regulate inflammatory responses

They block both LOX and COX activation by blocking arachidonic acid

Block cytokines, specifically TNF-alpha

Prevent leukocyte emigration to WBC cant get into tissues

Block the release of proteolytic enzymes

Question 14

Therapeutic uses of steroid anti-inflammatory drugs

Answer 14

Treatment of chronic asthma, RA, IBS, Addison’s disease, leukemia, and organ and tissue transplant rejection

Question 15

Pharmacotoxicology of Steroid anti-inflammatory drugs

Answer 15

GI irritation: decreased mucus production
Clotting disorders: blocking LOX and COX
Hyperglycemia: Inducing SNS which draws glucose into the blood for energy
Redistribution of fat

Question 16

Pharmacotoxicology for specifically Glucocorticoids

Answer 16

Can mimic the effects of aldosterone in the kidneys –> induction of hypernatremia and hypokalemia –> cardiac dysrhythmias and muscle cramping

Can induce demineralization of bones

Can induce psychoses

Question 17

MOA of diphenhydramine

Answer 17

diphenhydramine is an antihistamine, H1 histamine receptor antagonist (two different types of histamine receptors, H1 and H2; H2 tends to be in the gut): used to tamp down the effect of histamine in the inflammatory cascade

Question 18

MOA of zileuton

Answer 18

zileuton is a lipooxygenase inhibitor that blocks the synthesis of leukotrienes: treat pts who have asthma

Question 19

MOA of infliximab

Answer 19

infliximab is an antibody against TNF-α: used commonly for.. rheumatoid arthritis

Question 20

MOA of anakinra

Answer 20

anakinra is an antibody against IL-1

Question 21

MOA of tofacitinib

Answer 21

tofacitinib is a Janus kinase (JAK) inhibitor

Question 22

What are antihistamines used for?

Answer 22

antihistamines used in treatment of symptoms of allergies and mild inflammation… mild sleeping agents d/t CNS effect

Question 23

what are lipoxygenase inhibitors used for?

Answer 23

Lipooxygenase inhibitors: zileuton inhibits leukotriene-induced bronchoconstriction and mucus production associated with asthma

Question 24

What are anti-inflammatory medications that are specifically used in the treatment of RA and IBS (specifically Crohn’s)?

Answer 24

Tofactinib
Infliximab
Anakinra