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36 Cards in this Set
- Front
- Back
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What are the major products of PGH2
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Prostaglandins D2, E2, F2a,Prostacyclin PGI2,Thromboxanes (e.g. TXA2)
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What roll does COX2 play in some tumor cells?
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highly expressed in some tumor cells,required for angiogenesis
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What are some of the rolls of COX 1?
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PGE 2 (renal function),Thromboxane A2 (Platelet function),PGI2 (gastric protection)
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What is the precursor to leukotriene B4, C4, D4, and E4?,What is the enzyme that produces them?
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arachadonic acid,lipoxygenase
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Together with LTD4 and LTE4 this eicosanoid causes contraction of the bronchial smooth muscle in asthma?
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Leukotriene C4
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This eicosanoid is synthesized primarily in platelets and is a potent inducer of platelet aggregation and causes vasoconstriction?
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thromboxane A2
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How do COX inhibitors decrease pain?
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prevent sensitization of nociceptors by prostaglandins
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What drug inhibits the production of leukotrienes?,What drugs block leukotriene receptors?
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zileuton,montelukast,zafirlukast
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What prostaglandin analog prevents peptic ulcers in patients on high dose NSAIDS?
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misoprostol
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What histamine receptors are involved in bronchodilation and vasodilation?
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H1 receptors
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What histamine receptors are involved in mediating gastric acid secretion by the parietal cells in the stomach?
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H2 receptors
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What are the first generation H1 antagonists used for?
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allergies,rhinitis,nausea of motion sickness
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What is the most sedating H1 blocker?
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promethazine
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What is promethazine used for?
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allergic reactions,motion sickness,post operative pain
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What H1 antagonist is a long acting drug used for skin allergies and also used as a mild anxiolytic?
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hydroxyzine
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What H1 antagonist may be used as a nasal spray and opthalmic agent?
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azelastine
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What H1 antagonist inhibits release of histamine and other intranasally, reduces airway hyperactivity, and increases bronchial cilia motility?
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azelastine
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What is the clinical use of cyclizine and meclizine?
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motion sickness
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Second generation H1 blockers are different in what ways?
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less lipid soluable,almost free of sedation effects,long lasting
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What drugs are used for anti allergic reactions without sedation?
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fexofenadine ,loratadine,cetrizine
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What are the H1 antagonist interactions?
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potentiate cns depressors,Contraindicated with MAO inhibitors
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What are the major H2 antagonists?
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Cimetidine (Tagamet),Ranitidine (Zantac®),Famotidine (Pepcid®),,Nizatidine (Axid®)
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What are the clinical uses of H2 antagonists?
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duodenal ulcer,gastric ulcer,zollinger ellison syndrome,GERD
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What is zollinger-ellison syndrome?
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acid hypersecretion,recurrent peptic ulceration,GI Bleed,Diarrhea
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What H2 antagonist is a significant inhibitor of CYP-450 inhibitor and also has antiandrogen effects?
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cimetidine
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COX 2 is expressed mainly in what kind of cells?
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inflammatory/immune cells
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What eicosanoid causes neutrophil adherence and migration and activates phospholipases?
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Leukotriene B4
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What potent anti-inflammatory drugs inhibit phospholipase A2 and COX2?
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corticosteroids
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Aspirin's anticlotting effect is attributed to what mechanism?
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inhibition of thromboxane formation
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What is the mechanism and clinical use of alprostadil?
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prostaglandin(PGE1) analog,treatment of erectile dysfunction
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What is the mechanism and clinical use of misoprostol (cytotec)?
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prostaglandin (PGE1) analog,Prevent peptic ulcers with high dose of NSAIDS
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What is the mechanism and clinical use of epoprostenol?
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PGI2 (prostacyclin) analog,Severe pulmonary hypertension
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What is the mechanism and clinical use of dinoprostone?
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PGE2 analog ,uterine contraction ,cervical ripening
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What are the first generation H1 antagonists?
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Hydroxyzine (Vistaril),Cyclizine (Marezene),Diphenhydramine (Benadryl),Dimenhydrinate (Dramamine),Clemastine (Tavist),Carbinoxamine (Histex),Promethazine (Phenergan),Azelastine (Optiva),Meclizine (Antivert)
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What are the adverse effects of H1 antagonists?
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Sedation.,GI distress,Nausea,Vomiting,Extrapyramidal reactions
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What are the adverse effects fo cimetidine?
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CYP 450 inhibitor,drug interactions,reduce hepatic flow,antiandrogen effects
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