Anti-Inflammatory Agents: NSAIDs, Cheat Sheet of Pharmacology

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ANTI-INFLAMMATORY

AGENTS [ NSAIDs]

Presented by: HARSHDEEP KAUR [ 1422828] PHARM D 2nd^ year

○ Anti-inflammatory agents are a diverse group of substances that reduce inflammation, the body's natural response to injury or infection. This response involves a complex cascade of events, including:

1. Increased blood flow to the injured area: This brings white blood cells and other immune cells to the site to fight off infection and repair tissue.
2. Release of chemicals: These chemicals, such as prostaglandins and leukotrienes, cause swelling, redness, pain, and warmth. ○ Nonsteroidal anti-inflammatory drugs (NSAIDs): These are the most common type of anti-inflammatory agent. They work by blocking the production of prostaglandins, which are chemicals that contribute to pain, swelling, and fever. Examples of NSAIDs include ibuprofen, aspirin, and naproxen.

INTRODUCTION

1. Phospholipase A2 converts phospholipids in the cell membrane into arachidonic acid following tissue injury or irritation.
2. Arachidonic acid is a substrate for two major enzymes: cyclooxygenase (COX) and 5- lipoxygenase (5-LOX).
3. COX exists in different forms, including COX-1 and COX-2.
4. COX-1 is expressed constantly throughout the body and helps regulate normal body functions.
5. COX-1 is responsible for release of thromboxane and prostaglandins which stimulate normal body functions such as secretion of protective gastric mucus, regulation of gastric acid , promotion of platelet aggregation and maintenance of renal blood flow.
6. COX-2 is induced at sites of inflammation and mediates inflammation, pain, and fever.
7. NSAIDs act primarily by inhibiting COX enzymes, leading to decreased production of prostaglandins and producing anti-inflammatory, antipyretic, and analgesic effects.

○ NSAIDs [ Non-steroidal anti-inflammatory drug] act primarily by inhibiting COX enzymes which simply leads to decreased production of prostaglandins. ○ Prostaglandins play a crucial role in various physiological processes, including:

1. Pain and inflammation: Prostaglandins sensitize pain receptors and contribute to inflammatory responses causing swelling, redness, and warmth.
2. Fever: Prostaglandins in the hypothalamus elevate the body's temperature set point.

ANTI-INFLAMMATORY DRUGS

CLASSIFICATION OF NSAIDsCLASSIFICATION OF NSAIDs Non selective COX inhibitor Preferential COX- 2 inhibitors Highly selective COX-2 inhibitors Analgesic and antipyretic having weak inflammatory

1. Salicylates: Aspirin, diflunisal.
2. Propionic acid derivatives: Ibuprofen, naproxen, ketoprofen, flurbiprofen.
3. Fenamic acid derivatives: Mefenamic acid, flufenamic acid.
4. Acetic acid derivatives: Ketorolac, indomethacin.
   5. Enolic acid derivatives: Piroxicam, tenoxicam, lornoxicam Diclofenac, aceclofenac, nimesulide, meloxicam Etoricoxib, paracoxib Paracetamol, nefopam

MECHANISM OF ACTION

○ Indigestion and heartburn: NSAIDs can irritate the stomach lining, leading to burning sensations and discomfort. ○ Ulcers and bleeding: In severe cases, prolonged or high-dose use can cause stomach ulcers and internal bleeding. ○ Reduced kidney function: NSAIDs can affect blood flow to the kidneys, especially in people with pre-existing kidney problems. ○ Increased blood pressure: Some NSAIDs can elevate blood pressure, raising the risk of heart attack and stroke. o Heart attack and stroke: In high doses or for extended periods, NSAIDs can increase the risk of these cardiovascular events.

ADVERSE EFFECT

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