Questions and Answers
Which of the following are examples of Salicylates (A type of NSAIDs)? Choose all that apply.
Glucocorticoids have relatively little effect on humoral immunity. (True/False)
True
What is a common adverse effect of NSAIDs?
What is the effect of NSAIDs on platelet function?
Signup and view all the answers
What is the risk associated with the use of NSAIDs in patients with pre-existing heart failure?
Signup and view all the answers
Why should patients taking aspirin for cardioprotection avoid concomitant NSAID use?
Signup and view all the answers
What is the effect of NSAIDs on renal blood flow?
Signup and view all the answers
What is the effect of NSAIDs on the kidneys?
Signup and view all the answers
Which patients are at high risk for NSAID-induced edema?
Signup and view all the answers
What is a potential interaction between NSAIDs and warfarin?
Signup and view all the answers
What is the cardiovascular effect of agents with high COX-2 selectivity?
Signup and view all the answers
What is a gastrointestinal adverse effect of NSAIDs?
Signup and view all the answers
Why should NSAIDs be used with caution in patients with asthma?
Signup and view all the answers
What is a cardiovascular risk associated with NSAIDs?
Signup and view all the answers
What is a common central nervous system adverse event associated with NSAIDs?
Signup and view all the answers
What is the mechanism of action of spironolactone?
Signup and view all the answers
Which NSAID may be the LEAST likely to be harmful in patients with cardiovascular disease?
Signup and view all the answers
What is the therapeutic use of ketoconazole?
Signup and view all the answers
What is a common adverse effect of spironolactone?
Signup and view all the answers
What is the effect of NSAIDs on sodium and water retention?
Signup and view all the answers
Why are NSAIDs contraindicated in patients with established cardiovascular disease?
Signup and view all the answers
What is the effect of aspirin on TXA2 production?
Signup and view all the answers
What is a potential renal effect of NSAIDs?
Signup and view all the answers
Why do NSAIDs pose a bleeding risk?
Signup and view all the answers
What is the effect of NSAIDs on prostaglandins in the stomach and small intestine?
Signup and view all the answers
Why should NSAIDs be taken with food or fluids?
Signup and view all the answers
How do NSAIDs affect the cardiovascular system?
Signup and view all the answers
What is a potential interaction between NSAIDs and other medications?
Signup and view all the answers
What is the effect of aspirin on platelet aggregation?
Signup and view all the answers
Why do glucocorticoids have a broad anti-inflammatory effect?
Signup and view all the answers
Why is aspirin often withheld for at least 1 week prior to surgery?
Signup and view all the answers
What is a potential effect of chronic glucocorticoid use?
Signup and view all the answers
How do NSAIDs affect platelet function?
Signup and view all the answers
Why are proton pump inhibitors or misoprostol often used concomitantly with NSAIDs?
Signup and view all the answers
What is a potential effect of NSAIDs on the kidneys?
Signup and view all the answers
What is the effect of NSAIDs with higher relative selectivity for COX-1 on GI events?
Signup and view all the answers
Why do NSAIDs pose a cardiovascular risk?
Signup and view all the answers
Why do NSAIDs other than aspirin not have a significant antiplatelet effect?
Signup and view all the answers
Ibuprofen, naproxen, fenoprofen, ketoprofen and flurbiprofen are examples of
Signup and view all the answers
Aspirin and diflunisal are examples of
Signup and view all the answers
Etodolac is a
Signup and view all the answers
Keterolac is a
Signup and view all the answers
Which is associated with aspirin
Signup and view all the answers
Study Notes
Anti-inflammatory drugs
- Anti-inflammatory drugs include NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) and Glucocorticoids.
NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)
- Types of NSAIDs:
- Salicylates: Aspirin, Diflunisal
- Propionic acid derivatives: Ibuprofen, Naproxen, Fenoprofen, Ketoprofen, Flurbiprofen
- Indole and indene derivatives: Etodolac
- Pyrrole derivatives: Ketorolac
Mechanism of Glucocorticoids
- Glucocorticoids have broad anti-inflammatory effects on multiple components of cellular immunity but relatively little effect on humoral immunity.
- Glucocorticoids bind to receptors inside cells and regulate the transcription of numerous other genes.
- Glucocorticoids curtail activation of nuclear factor-κB, suppress formation of proinflammatory cytokines such as IL-1 and IL-6, inhibit T cells from making IL-2 and proliferating, and inhibit the activation of cytotoxic T lymphocytes.
- Glucocorticoids also inhibit the activation of neutrophils and monocytes.
Aspirin
- Aspirin is a weak organic acid that irreversibly acetylates and inactivates cyclooxygenase.
- Aspirin inhibits cyclooxygenase, which diminishes the formation of prostaglandins and modulates aspects of inflammation mediated by prostaglandins.
- Aspirin does not arrest the progression of the disease or induce remission.
Adverse effects of NSAIDs
- Gastrointestinal effects:
- Increased risk of bleeding
- Ulceration
- Increased risk of bleeding (antiplatelet effect):
- Prolonged bleeding time
- Aspirin should be withheld for at least 1 week prior to surgery
- Renal effects:
- Retention of sodium and water
- Edema
- Decreased renal blood flow
- Cardiac effects:
- Increased risk for cardiovascular events
- MI and stroke
- Cardiovascular protective effect due to reduced production of TXA2
- Other adverse effects:
- Asthma exacerbations
- Central nervous system (CNS) adverse events
- Headache, tinnitus, and dizziness
- Hypersensitivity reactions
Inhibitors of endogenous steroids (Adrenocorticoids) secretion or function
- Ketoconazole:
- Strongly inhibits all gonadal and adrenal steroid hormone synthesis
- Used in the treatment of patients with Cushing syndrome when surgical management is not an option
- Spironolactone:
- Competes for the mineralocorticoid receptor
- Inhibits sodium reabsorption in the kidney
- Effective for the management of hyperaldosteronism, resistant hypertension, and hepatic cirrhosis
- Used with other standard therapies for treatment of heart failure with reduced ejection fraction
- Used in the management of hirsutism in women, probably due to antiandrogen activity on the hair follicle
- Adverse effects: hyperkalemia, gynecomastia, menstrual irregularities, and skin rashes
- Eplerenone:
- Selectively binds to the mineralocorticoid receptor
- Acts as a selective aldosterone antagonist
- Has a lower affinity for the androgen receptor
- Lessens the potential for gynecomastia and irregular menstrual bleeding associated with spironolactone
- Approved for the treatment of hypertension and for heart failure with reduced ejection fraction after an acute myocardial infarction
NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)
- Patients taking aspirin for cardioprotection should avoid concomitant NSAID use or take aspirin at least 30 minutes prior to the NSAID.
- NSAIDs prevent the synthesis of PGE2 and PGI2, prostaglandins responsible for maintaining renal blood flow, which can result in retention of sodium and water, leading to edema.
- Patients with a history of heart failure or kidney disease are at high risk for these effects, which can mitigate the beneficial effects of antihypertensive medications.
- NSAIDs can lead to acute kidney injury in susceptible patients.
Cardiac Effects
- Aspirin, with high COX-1 selectivity at low doses, has a cardiovascular protective effect due to reduced TXA2 production.
- Agents with higher relative COX-2 selectivity have been associated with an increased risk for cardiovascular events, possibly by decreasing PGI2 production mediated by COX-2.
- All NSAIDs except aspirin carry a boxed warning regarding the increased risk for cardiovascular events, including MI and stroke.
- Use of NSAIDs other than aspirin is discouraged in patients with established cardiovascular disease.
- Naproxen may be the least likely to be harmful in patients with cardiovascular disease.
Other Adverse Effects
- NSAIDs inhibit cyclooxygenases, which can cause a shift toward leukotriene production and increase the risk of asthma exacerbations.
- Central nervous system (CNS) adverse events, such as headache, tinnitus, and dizziness, may occur.
Pharmacokinetics
- NSAIDs are inhibitors of cyclooxygenases and, therefore, inhibit the synthesis of prostaglandins but not of leukotrienes.
Inhibitors of Endogenous Steroids (Adrenocorticoids) Secretion or Function
- Ketoconazole: an antifungal agent that strongly inhibits all gonadal and adrenal steroid hormone synthesis, used in the treatment of Cushing syndrome.
- Spironolactone: an antihypertensive drug that competes for the mineralocorticoid receptor, inhibiting sodium reabsorption in the kidney, and also antagonizes aldosterone and testosterone synthesis.
- Eplerenone: a selective aldosterone antagonist that binds to the mineralocorticoid receptor, approved for the treatment of hypertension and heart failure with reduced ejection fraction after an acute myocardial infarction.
Adverse Effects of Aspirin
- Gastrointestinal: the most common adverse effects of NSAIDs, ranging from dyspepsia to bleeding.
- Increased risk of bleeding (antiplatelet effect): aspirin inhibits COX-1–mediated formation of TXA2 and reduces platelet aggregation for the lifetime of the platelet.
Glucocorticoids
- Mechanism: glucocorticoids bind to receptors inside cells and regulate the transcription of numerous other genes, curtailing activation of nuclear factor-κB, suppressing formation of proinflammatory cytokines, and inhibiting T cells and neutrophils.
- Chronic adverse effects: glucocorticoids have broad anti-inflammatory effects on multiple components of cellular immunity but relatively little effect on humoral immunity.
Selected Drug-Drug Interactions: Glucocorticoids
- No specific interactions mentioned in the text.
NSAIDs
- Classification:
- Salicylates: Aspirin, Diflunisal
- Propionic acid derivatives: Ibuprofen, naproxen, fenoprofen, ketoprofen, flurbiprofen
- Indole and indene derivatives: Etodolac
- Pyrrole derivatives: Keterolac
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
Description
FA- D1 fall Anti-Inflammatory Drugs
