Drugs for Inflammation Flashcards
what is acute inflammation?
- associated with physical injury, chemical damage, infection, antigens
- lasts 8-10 days, followed by repair and healing
what is chronic inflammation?
- may occur if the body is unable to contain or neutralize the agent causing initial inflammation
- leading to tissue damage, with symptoms worsening over time
what is produced when tissue is damaged?
- arachidonic acid
arachidonoyl ester is converted into arachidonic acid by what enzyme?
-phospholipase A2
what enzyme converts arachidonic acid to prostaglandins
- cyclooxygenase
what purpose cyclooxygenase 1 and 2 have?
COX 1: recruits platelets
COX 2: makes pro-pain and pro-inflammatory prostaglandins
what do prostaglandins do?
- enhance vasodilation, gastric cytoprotection, decrease gastric acid production
what does thromboxane A2 do?
- stimulates platelet aggregation
what enzyme converts arachidonic acid into leukotrienes?
-lipoxygenase
what do leukotrienes do?
- enhance immune response
- bronchoconstriction
what is the goal of anti-inflammatory drugs?
- to prevent or decrease the intensity of the inflammatory response and reduce fever
what are the two primary drug classes for anti-inflammatory drugs?
- NSAIDS
- glucocorticoids
what are NSAIDs used for?
- mild to moderate pain, inflammation and fever by inhibiting the enzymatic activity of cyclooxygenase
what is an example of an irreversible inhibitor of cyclooxygenase ?
-aspirin
what are glucocorticoids used for?
- severe or disabling inflammation
- used for short term control of severe disease
where are cyclooxygenase-1 enzymes located?
- present in all tissues
where are cyclooxygenase-2 enzymes located?
- present at sites of tissue injury
what is the function of cyclooxygenase-1?
-protects gastric mucosa, supports kidney function, promotes platelet aggregation
what is the function of cyclooxygenase-2?
-mediates inflammation, sensitizes pain, mediates fever in the brain
what does the inhibition of COX1 and COX2 enzymatic activity do?
- reduces inflammation and fever
- inhibits the formation of gastric mucosa
- increases gastric acid secretion
- inhibits platelet aggregation
what risks are associated with selective COX2 inhibitors?
-high risk of MI, stroke, and asymptomatic hypertension
what are the two options of glucocorticoid therapy?
- systemic glucocorticoid therapy
- topical and intranasal glucocorticoids
what is the mechanism of action for systemic glucocorticoid therapy?
- inhibits the release of histamine
- blocks the activity of phospholipase A2 and COX2 enzymes
- inhibits the immune response
what are adverse effects of systemic glucocorticoid therapy?
- adrenal insufficiency, hyperglycaemia, mood changes, osteoporosis, immunosuppression
