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VetMed Pharmacology8
Anti-Inflammatory Pharmacology
| Question | Answer |
|---|---|
| Non-Steroidal Anti-Inflammatory Drug | class of pharmaceutical that exerts an anti-inflammatory effect by inhibiting prostaglandin and/or leukotrienes but is not composed of a cholesterol "core" |
| COX-1 Function | synthesizes "protective" prostaglandins like PGI2 in the GI mucosa and renal tubule epithelium |
| COX-2 Function | synthesizes pro-inflammatory prostaglandins |
| Non-Selective NSAIDs MOA | inhibit activity of COX-1 and COX-2 results in decreased PGG2 and PGH2 production |
| PGG2 and PGH2 | precursors for general prostaglandin synthesis |
| Only NSAID that Permanently Inhibits COX | aspirin (through acetylation) possibly phenylbutazone |
| NSAID General Properties | most are organic acids high plasma protein binding ionized form more extensively excreted in urine |
| Pathophysiology of NSAID Action | suppress inflammatory prostaglandin synthesis suppress WBC degranulation and diapedesis decrease injury/destruction from WBCs reduce tissue edema reduce visceral and musculoskeletal pain suppresses hyper-coagulation states reduces life-threatening p |
| Best NSAID for Visceral Abdominal Pain | flunixin meglumine (Banamine) |
| Best NSAID for Musculoskeletal Pain | phenylbutazone |
| Novel NSAID Uses | tx certain neoplastic dz such as osteosarcoma maintain gestation closer of premature PDA diagnostic determination of bone marrow platelet production |
| NSAID Sequelae | GI ulceration renal toxicity if co-administered w/ aminoglycosides increase risk of haemorrhage renal toxicity (pseudo-OD) if hypoproteinemic displacement of protein-bound pharmaceuticals |
| C/I for NSAIDs | renal tubular dysfunction GI ulceration existing/ongoing haemorrhage |
| Non-Selective NSAIDs | salicylic acid para-aminophenols indole/indene acetates heteroacryl acetic acid arylpropionoates anthranilic acid enolic acids alkanones phenylbutazone, flunixin meglumine |
| Selective COX-2 Inhibitor NSAID MOA | inhibit inflammatory PG's but avoid PGI2 inhibition |
| Selective COX-2 NSAIDs | diaryl-substituted furanones diaryl-substituted pyrazoles indole acetic acid suflonanilides misc - meloxicam, topoxalin, carprofen, deracoxib |
| Metabolization of NSAIDs | glycine, either/phenolic glucuronide, ester/acyl glucoronide conjugation rxns in mitochondria and smooth-ER in hepatocytes |
| Metabolization of Aspirin | hydrolyzed to salicylic acid in GI tract, plasma, liver, and RBC cytosol |
| Primary Excretion of NSAIDs | glomerular filtration/tubular secretions |
| Decreases Renal Tubular Re-absorption | NSAID conjugation high urinary flow |
| Dipyrone | NSAID that is less likely to mask severe visceral pain requiring surgery |
| Leukotrienes | generated by the biochemical conversion of membrane phospholipids to arachidonic acid with lipoxoygenases to leukotrienes |
| Proinflammatory Leukotrienes ("4-series") | LTB4 LTC4 LTD4 LTE4 |
| Anti-inflammatory Leukotrienes ("5-series") | LTB5 LTC5 LTD5 LTE5 |
| Zyleuton (Zyflo) | orally active inhibitor of 5-lipoxygenase |
| Monteleukast (Singulair) | leukotriene receptor antagonist |
| Zafirlukast (Accolate) | oral leukotriene receptor antagonist |
| Cetirizine hydrochloride (Zyrtec) | antihistamine and a racemic selective H1 receptor antagonist |
| Leukotriene MOA's (4) | Anti-FLAP Agents LTB4 Receptor Antagonists 5-Lipoxygenase Inhibitor Agents LTC4, LTD4, LTE4 Receptor Antagonists |
| Advantages of Leukotriene Inhibitors | suppress symptoms associated primarily with leukotriene over-production avoid side effects of anti-PG NSAIDs avoid CNS side effects of anti-histamines avoid side effects of glucocorticoids |
| Theophylline Analogs MOA | inhibit cyclic nucleotide phosphodiesterase resulting in increased cAMP and increased cGMP --> bronchodilation |
| Antihistamine Fxn | block histamine H1 receptors |
| Results of Stimulation of H1 Receptors | vasodilation bronchoconstriction endothelial cell separation pain/itching |
| Cromolyn Sulfate | antihistamine that suppresses degranulation of mast cells and leukotriene release used to prevent bronchospasms in feline asthma |
| Glucocorticoid | anti-inflammatory agent that possess a cholesterol core structure highly bound to plasma proteins most are conjugated with sulfate or glucoronide |
| Glucocorticoid MOA | inhibits phospholipase A2 --> reduces availability of arachidonic acid substrate --> decreased production of COX, leukotrienes, HETE, HPETE also stabilizes cellular membranes inhibition of PA2 inhibition of nuclear receptor complexes --> immunosuppress |
| Glucocorticoid Physiological Effects | resist stressful scenarios stimulates gluconeogenesis, enhances glycogen deposition adipose tissue redistribution mediates lipolysis |
| Glucocorticoid Metabolism | sequential addition of H+ or O atoms --> conjugation rxns |
| Synthetic Glucocorticoid Metabolism | hepatic 11beta-hydroxysteroid dehydrogenase |
| Clinical Applications of Glucocorticoids | anti-inflammatory vascular collapse cerebral edema immunosuppression renal disease hepatic disease lymphoreticular neoplasia |
| Antu-Inflammatory More Effective in Managing Visceral Pain | NSAIDs over Glucocorticoids |
| Glucocorticoid Sequelae | protein synthesis inhibition immunosuppression GI ulceration corneal ulcer exacerbation renal dysfunction degenerative joint disease |
| Steroid Hormone Inhibitors | mitotane ketoconazole (Cushing's/Hyperadrenocorticism) aminoglutethimide (breast/prostate carcinoma) metyrapone (Cushing's) trilostane (cancer) cyproheptadine (PDH) pergolide (PDH) |
| Crysotherapeutics MOA | suppress abnormal immune response by inhibiting macrophage and T-lymphocyte maturation |
| Crysotherapeutic Uses | may cure auto-immune conditions Ex: pemphigus foliaceus, pemphigus vulgaris, rheumatoid arthritis, sjogren syndrome, lupus |
| Diagnostic Use of Corticosteroids and ACTH | differentiating a pituitary tumor from an adrenal tumor in Cushing's syndrome |
| Ketoconazole (agent, fxn, sequelae) | antifungal agent inhibits biosynthetic capacity of cytochrome P450, making it one of the most effective tx of Cushing's causes hepatic dysfxn and inhibits Rx activation |
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