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Unit04 - Chem 1004 Spring 2011 Analgesics Cold and Allergy...

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1 Chem 1004 - Spring 2011 Blackboard: http://blackboard.gwu.edu Office Hours: MW 3:10-3:55 PM, 1957 E street, room 113 or by appointment Analgesics Cold and Allergy Medicines Optical Isomerism In 1763 Edmund Stone , an English clergyman, reported to the Royal Society the isolation of yellow, needle-shaped crystals from the bark of willow trees ( Salix alba ): sali cin • Mixture of two compounds: one of them helped reduce pain, fever and inflammation. Miracle drug • Side effects: very unpleasant taste, produced nausea and acute stomach irritation. Salicylic acid
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2 In 1898 , Felix Hoffmann, employee of a major German chemical firm, converted this compound into a different substance, which reverted back to the original once it was in the body, reducing the side effects in the stomach. - Very low toxicity - Remarkably effective antipyretic (fever reducing), analgesic (anti-pain), and anti- inflammatory agent. Miracle drug Salicylic acid + Acetic acid + H 2 O
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3 - works in the brain to reduce fever, - relieves inflammation in muscles and joints, - it apparently decreases the chances of stroke and heart attack. How Aspirin Works Aspirin blocks cyclooxygenase (COX-2) enzymes COX-2 are involved in the synthesis of prostaglandins . Prostaglandins : - produce fever and swelling , - increase the sensitivity of pain receptors , - inhibit blood vessel dilation , - regulate the production of acid and mucus in the stomach , - assist kidney functions . - Blood thinning agent. - Upsetting to the stomach, especially at the high doses often used in arthritis. - Aspirin given to kids with flu, chickenpox, or other viral sicknesses may cause a potentially deadly problem called Reye syndrome. - Changes the way kidneys make urine. - It can cause some people to have trouble breathing (rare). Aspirin side effects Aspirin substitutes Ibuprofen and acetaminophen, work by physically plugging the enzyme's channels rather than chemically altering them. Acetaminophen - Blocks COX : reduces fever - Little anti-inflammatory action Acetaminophen (Tylenol®) Ibuprofen - Better COX blocker and specialized cell inhibitor: better pain reliever and fever reducer than Aspirin . - Fewer side effects. Ibuprofen (Advil®)
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4 There are two kinds of cyclooxigenases, COX-2 and COX-1 Why the side effects? Arachidonic acid COX-2 COX-1 Prostaglandins Help keep the stomach lining intact and the kidneys functioning properly Prostaglandins Lead to inflammation, pain and fever Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) COX-2 gene transcription Future drug inhibitors Selective COX-2 inhibitors Vioxx® (Rofecoxib) Valdecoxib
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5 The general shape of the molecule and the identity and location of functional groups are important factors in determining the physiological activity of a drug. How do we design a specific COX-2 inhibitor? Chemists custom design drug molecules to meet the requirements of the receptor site.
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