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Study Guide Antihistamines 1. Differentiate between 1st and 2nd generation antihistamines. How do they act?

The principal difference between the groups is that first-generation antihistamines are highly sedating, whereas second-generation antihistamines are not. PP SLIDES: first generation is sedating, is more anticholinergic, and has peripheral and CNS effects. Second generation are non sedating and do not pass the BBB Histamine1 blockers bind selectively to H1-histaminic receptors, thereby blocking the actions of histamine at these sites. H1 antagonists do not block H2 receptors. Also, they do not block release of histamine from mast cells or basophils 2. What are prototypes and common side effects? 1st generation antihistaminesdiphenhydramine (Benadryl) most sedating; promethazine (Phenergan) quite sedating; chlorpheniramine (Chlor-Trimeton) less sedating 2nd generation antihistamines azelastine (Astelin-nasal spray), cetirizine (Zyrtec), fexofenadine (Allegra), loratadine (Claritin), desloratidine (Clarinex) Common side effects: CNS depression (negligible with second generation), anticholinergic effects (dry mouth, nasal passages, and throat; urinary hesitancy, constipation, palpitations). PP SLIDES: Sedation first generation, other CNS effects such as dizziness, confusion avoid driving /operating heavy machinery, possibly GI disturbances helps to take with food, anticholinergic effects: frequent sips of fluid, suck on candy for dry mouth, caution interaction with alcohol 3. What are important teaching points? Avoid driving/operating heavy machinery, advise against drinking alcohol, advise against using any CNS depressants, should not be used while breast feeding, acute toxicity Immunosuppressants What are immunosuppressants used for? To suppress immune response to prevent organ rejection after transplants (Lifelong), to treat autoimmune diseases What are common adverse effects? Nephrotoxicity, infection, and hepatotoxicity (interactions with grapefruit juice resulting in toxicity) What are prototypes identified? Cyclosporine (Sandimmune), azathioprine (Immuran), tacrolimus (Prograf NSAID and Acetaminophen Study Guide How Do NSAIDS work?

They are nonselective inhibitors of cyclooxygenase, which is an enzyme that converts arachidonic acid into prostaglandins and related compounds. They reduce inflammation, pain, and fever. Describe the action of NSAIDS. At sites of tissue injury, COX catalyzes the synthesis of prostaglandin E2 (PGE2) and prostaglandin I2 (PGI2, prostacyclin), which promote inflammation and sensitize receptors to painful stimuli. In the brain COX-derived prostaglandins mediate fever and contribute to perception of pain. Promotes platelet aggregation. Inhibits all of this, thereby inhibiting inflammation, fever, and pain. What is the difference between a typical NSAID and a COX 2 inhibitor? Typical NSAIDs inhibit COX1 and COX2, whereas COX2 inhibitors only inhibit COX2. COX2 inhibitors are able to suppress pain and inflammation while causing fewer adverse gastric effects, however, increase risk of heart attack and stroke How does acetaminophen differ from aspirin and other NSAIDS? Acetaminophen can reduce pain and fever but cannot suppress inflammation. What are known worrisome side effects of NSAIDS? Gastric ulceration, renal impairment, bleeding What organ function can be damaged by acetaminophen? Liver What caution must be exercised when considering aspirin for children? Reyes syndrome: acetaminophen can be used in children with chickenpox or influenza (aspirin should not be) Rheumatoid Arthritis & Gout What is a DMARD and what are goals of treatment? Disease-modifying antirheumatic drugs Reduce joint destruction and retard disease progression (In general) Treatment is directed at (1) relieving symptoms (pain, inflammation, and stiffness), (2) maintaining joint function and range of motion, (3) minimizing systemic involvement, and (4) delaying disease progression What are adverse effects to be concerned about? Hepatic damage, bone marrow suppression, GI ulceration, pneumonitis What are colchicine and allopurinol used for? Colchicine: Treats acute attack or abort an impending attack (gout) Allopurinol: Treats chronic gout, decreases elevated uric acid caused by chemotherapy What type of drug is indomethicin?