Questions and Answers
What is the anti-inflammatory mechanism of glucocorticoids?
What is the primary function of cyclooxygenase (COX)-1 isoform?
Which of the following is a result of COX-2 inhibition?
What is the effect of NSAIDs on platelet aggregation?
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Which of the following NSAIDs is a selective COX-1 inhibitor?
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What is the effect of NSAIDs on the kidney?
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What is the purpose of prostaglandin analogs?
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What is the effect of COX-2 inhibition on cardiovascular events?
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What is the result of phospholipase A2 release following tissue injury or irritation?
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What is the effect of NSAIDs on fever?
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Which of the following NSAIDs is a selective COX-2 inhibitor?
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Study Notes
Glucocorticoids
- Glucocorticoids are steroid hormones produced naturally by the adrenal glands in the body, also known as cortisol.
- They have powerful anti-inflammatory effects, but are also immunosuppressive.
Natural and Synthetic Glucocorticoids
- Glucocorticoids can be synthetically made and taken orally or injected, examples include hydrocortisone and prednisone.
- Synthetic glucocorticoids are used to relieve pain quickly, especially in sports medicine.
Transportation and Function
- Glucocorticoids are lipid-soluble and need a carrier protein called trans Cortin to transport them around the body.
- They go inside cells, bind to glucocorticoid receptors, and upregulate or downregulate certain genes.
- Glucocorticoids inhibit nuclear factor Kappa B's activity, suppressing inflammation and the production of inflammatory cytokines.
Anti-Inflammatory Effects
- Glucocorticoids inhibit the formation of inflammatory mediators by inhibiting enzymes phospholipase a2 and Cox.
- They reduce the production of prostaglandins, leucotrienes, and thromboxanes, which are inflammatory mediators.
Replacement Therapy
- Synthetic glucocorticoids are used as replacement therapy for people with Addison's disease, where the adrenal glands produce low levels of cortisol.
Side Effects
- Long-term use of glucocorticoids can lead to immunosuppression, making people more prone to infection.
- It can also lead to Cushing syndrome, characterized by weight gain, obesity, and fluid retention.
- Glucocorticoids can affect bone health, leading to osteoporosis by inhibiting osteoblast activity and stimulating osteoclast activity.
Glucocorticoids
- Glucocorticoids are steroid hormones produced by the adrenal glands, also known as cortisol, with powerful anti-inflammatory effects and immunosuppressive properties.
Natural and Synthetic Glucocorticoids
- Synthetic glucocorticoids can be taken orally or injected, examples include hydrocortisone and prednisone, and are used to relieve pain quickly, especially in sports medicine.
Transportation and Function
- Glucocorticoids require a carrier protein called trans Cortin for transportation around the body due to their lipid-soluble nature.
- They bind to glucocorticoid receptors inside cells, upregulating or downregulating certain genes.
- Glucocorticoids inhibit nuclear factor Kappa B's activity, suppressing inflammation and the production of inflammatory cytokines.
Anti-Inflammatory Effects
- Glucocorticoids inhibit the formation of inflammatory mediators by inhibiting enzymes phospholipase a2 and Cox.
- They reduce the production of prostaglandins, leucotrienes, and thromboxanes, which are inflammatory mediators.
Replacement Therapy
- Synthetic glucocorticoids are used as replacement therapy for people with Addison's disease to supplement low cortisol levels.
Side Effects
- Long-term use of glucocorticoids can lead to immunosuppression, making people more prone to infection.
- Prolonged use can cause Cushing syndrome, characterized by weight gain, obesity, and fluid retention.
- Glucocorticoids can negatively impact bone health, leading to osteoporosis by inhibiting osteoblast activity and stimulating osteoclast activity.
Inflammatory Response
- Tissue injury or irritation releases phospholipase A2, converting phospholipids into arachidonic acid.
- Arachidonic acid is a substrate for cyclooxygenase (COX) and 5-lipoxygenase (5-LOX).
Cyclooxygenase Pathway
- COX enzyme has two forms: COX-1 and COX-2.
- COX-1 is constantly expressed throughout the body, responsible for:
- Producing thromboxane and prostaglandins, which stimulate normal body functions.
- Regulating gastric acid, promoting platelet aggregation, and maintaining renal blood flow.
- COX-2 is induced at sites of inflammation, leading to:
- Production of prostaglandins that mediate inflammation, pain, and fever.
Mechanism of Action of NSAIDs
- NSAIDs act by inhibiting COX enzymes, decreasing prostaglandin production, resulting in:
- Anti-inflammatory effects.
- Antipyretic effects.
- Analgesic effects.
- NSAIDs can be divided into three categories based on COX enzyme selectivity:
- Selective COX-1 inhibitors.
- Relatively non-selective COX inhibitors.
- Selective COX-2 inhibitors.
Adverse Effects of NSAIDs
- Common adverse effects occur in the gastrointestinal tract due to:
- Inhibition of COX-1-mediated production of PGE2 and PGI2, increasing risk of GI bleeding and peptic ulcers.
- Agents with higher COX-1 selectivity have a higher risk.
- Inhibition of COX-1-mediated production of TXA2 leads to:
- Antiplatelet effect and increased risk of bleeding.
- Aspirin-induced antiplatelet effect persists even after therapy is stopped.
- Adverse effects on the kidney result from:
- Decreased production of renal prostaglandins, increasing risk of kidney injury in susceptible patients.
- Adverse effects on the cardiovascular system result from:
- Agents with high COX-1 selectivity having a protective cardiovascular effect.
- Agents with high COX-2 selectivity increasing the risk of cardiovascular events.
Prostaglandin Analogs
- Prostaglandin analogs interact with specific G-protein coupled prostaglandin receptors, harnessing beneficial effects.
- Examples of prostaglandin analogs include:
- Alprostadil (erectile dysfunction and ductus arteriosus).
- Lubiprostone (chronic constipation).
- Misoprostol (stomach ulcers and inducing labor).
- Bimatoprost, Latanoprost, and Travoprost (open-angle glaucoma).
- Iloprost and Treprostinil (pulmonary arterial hypertension).
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Description
Learn about glucocorticoids, their natural and synthetic forms, and their effects on the body. Discover how they are used in medicine and sports.
