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57 Cards in this Set
- Front
- Back
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This acid is derived from cell membrane lipids.
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Arachidonic acid
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What are the 2 main groups of eicosanoids?
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1. Prostaglandings
2. Leukotrienes |
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This enzyme in the cell membrane generates arachidonic acid from lipid constituents.
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Phospholipase A2
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This enzyme converts arachidonic acid to PGG & PGH
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Cycooxygenase
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This enzyme converts arachidonic acid to leukotriene precursors
(HPETEs- Hydroperoxy-eicosatetraenoic acid) 12 |
Lipoxygenase
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What are the five prostaglandins used as therapeutic agents?
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1. Misoprostol (CYTOTEC)
2. Epoprostenol (FLOLAN) 3. Dinoprostone (PROSTINE2) 4. Treprostinil (REMODULIN) 5. Alprostadil (CAVERJECT or PROSTIN VR PEDIATRIC) |
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What are the four prostaglandin therapeutic agents used in eyedrop form?
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1. Bimatoprost (LUMIGAN)
2. Travapost (TRAVATAN) 3. Unoporstone (RESCULA) 4. Latanoprost (XALATAN) |
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This synthetic PGE1 analog is used in the treatment of NSAID induced ulcers.
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Misoprostol (CYTOTEC)
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This prostaglandin is a synthetic preparation of PGE2. It is approved for inducing abortion in the second trimester & for ripening cervic for induction of labor in patients near term.
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Dinoprostone (PROSTINE2)
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This synthetic preparation of PGE2 is administered vaginally and affects the collagenase of the cervix resulting in softening.
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Dinoprostone (PROSTINE2)
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This PGE1 analogis used to maintain the patency of neonate's DUCTUS ATERIOSUS.
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Alprostadil (PROSTIN VR PEDIATRIC)
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What are the adverse effects of Alprostadil (PROSTIN VR PEDIATRIC)?
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Bradycardia, Hypotension, Hyperplexia
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What is Alprostadil (CAVERJECT) used for?
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Erectile dysfunction; intravernosal injxn or urethral suppositories-- acts as smooth muscle relaxant, increased blood flow--> ERECTION
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What are the side effects of Alprostadil (CAVERJECT)?
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Penile pain, penile fibrosis, flushing, diarrhea, headache and fever
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Which prostaglandin is used for treatment of GLAUCOMA or ocular hypertension as an eye solution?
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Latanoprost (XALATAN)
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What three prostanoids were developed due to the success of Latanoprost's successful treatment of ocular hypertension?
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1. Bimatoprost (LUMIGAN)
2. Travapost (TRAVATAN) 3. Unoprostone (RESCULA)= Docosanoid |
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What is the adverse effect of using ocular prostaglandins as therapeutic agents?
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Iris Pigmentation
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What is Epoprostenol indicated for?
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Treatment of Primary Pulmonary hypertension.
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_________ is a PGI2 and is also known as prostacyclin.
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Epoprostenol (FLOLAN)
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Pulmonary Hypertension
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Is a an abnormal elevation of the pressure in the blood vessels of the lungs.
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NSAIDs are WEAKER or STRONGER than narcotic analgesics.
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WEAKER
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What are the 3 main effects of NSAIDs?
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1. Analgesic Effect- relief of minor aches and pains
2. Anti-inflammatory effects- reduction of inflammation associated with various arthritic syndromes. 3. Antipyretic effect-reduction of elevated body temperature |
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This includes a series of events that can be elicited by infections, antigen-antibody reactions and thermal or physical injury.
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INFLAMMATION-- Clinical signs inclued redness, swelling, heat, pain and loss of function
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What are the three distinct phases of the inflammation response?
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1. ACUTE transient phase- local vasodilation & increased capillary permeability
2. Delayed,SUBACUTE phase characterized by infiltration of leukocytes and phagocytic cells 3. CHRONIC proliferative phase with tissue degeneration and fibrosis |
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Rheumatoid arthritis, Juvenile rheumatoid arthritis, degenerative joint disease (Osteoarthritis) and Gout are examples of this type of disease.
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INFLAMMATORY DISEASE
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What are the therapeutic strategies in treating inflammation?
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* Relief of PAIN
* Slow or stop tissue damaging process |
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DMARDS
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Disease Modifying Anti-Rheumatic Drugs
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Name three agents used in the treatment of inflammation.
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1. NSAIDS
2. Glucocorticoids 3. DMARDs |
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What affects do NSAIDs have?
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Reduce inflammation, pain and elevated body temperature
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What is the major problem with use of DMARDs (disease modifying anti-rheumatic drugs)?
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TOXICITY
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The _______ regulate the set point at which body temperature is maintained
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HYPOTHALAMUS
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What is a natural source of Salicylates?
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WILLOW BARK
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This is a better glycoside from Willow Bark.
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SALICIN
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This chemical processing of Salicin results in salicylic alcohol and glucose
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Salicin HYDROLYSIS
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_________ can be converted to Salicylic acid by chemical modification
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SALICYLIC ALCOHOL
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Salicylic Alcohol can be converted to salicylic acid by chemical modification here.
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IN VIVO= In the body
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ACETYL SALICYLIC ACID
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Aspirin
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What is the Mechanism of Action for Aspirin (ASA)?
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It non-selectively and irreversibly inhibits both isozymes of Cyclooxygenase (COX I & II) thereby inhibiting the synthesis of prostaglandins and thromboxanes
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What is responsible for the irreversible nature of Aspirin's activity?
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The acetyl group of ASA covalently binds the enzyme (COX I or II) and permanently inhibits its activity.
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What is unique about aspirin's inhibition of cyclooxygenase?
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Its IRREVERSIBILITY!
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________ can inhibit granulocyte adherence to damaged vasculature, stabilize lysosomes, inhibit chemotaxis of polymorphonuclear leukocytes and macrophages.
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Aspirin
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ASA's antipyretic effects is due to ____________.
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COX inhibition in the CNS
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ASAs analgesic effects are Peripheral or Central?
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PERIPHERAL AND CENTRAL EFFECTS
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____ acts to promote platelet aggregation.
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TXA2= Thromboxane A2
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What are the adverse effects of ASPIRIN?
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*G.I.- N/V, epigastric distress, ulceration, G.I. bleed, erosive gastritis
* Hepatic- Increased enyzyme levels * Renal- Salt & water retention; reduction of renal fn w/ CHF, renal disease, hypovolemia |
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What are some drug interactions associated with Aspirin?
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* Enhances effects of Warfarin
*Antagonizes effects of Uricosurics *Increases METHOTREXATE concentrations |
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What are the three steps in treatment of Salicylate intoxication?
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1. Limit further absorption of salicylates w/ activated charcoal
2. Hastens its elimination with IV bicarbonate-- may help correct any acid/ base imbalances 3. Supportive care-- IV fluids or cold baths for pyrexia |
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Describe non-acetylated salicylates.
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*Effective anti-inflammatory agents
*Less effective analgesics than ASA *Weak COX inhibitors |
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Name 4 non-acetylated salicylates.
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1. Choline salicylate (ARTHROPAN)
2. Sodium Salicylate 3. Magnesum Salicylate (MAGAN) 4. Salicylsalicylate (DISCALCID) |
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What is Acetaminophen's mechanism of action?
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Is a weak COX-inhibitor in peripheral tissues
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What explains APAP's antipyretic affects?
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It has the ability to inhibit COX in the brain however it does not inhibit neutrophil activation.
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Acute overdoseage of acetaminophen can result in...? (4)
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*Dose-dependent fatal necrosis of liver
*Renal tubular necrosis *HYPOglycemic coma *Formation of toxic metabolite--N-hydroxylation-N-acetyl-para-benzoquinonime |
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Elevated aminotransferase, elevated bilirubin, liver damage and death are all symptoms seen 2-4 days after...?
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Acute acetaminophen overdose
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What is the principal antidotal treatment for acetaminophen toxicity?
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Administration of Sulfhydrul compound-- act to replenish hepatic stores of GLUTATHIONE
**N- Acetylcystein (MUCOMYST): PO or IV |
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What are some of the side effects for Inomethacin (INDOCIN)?
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HA, dizziness, vertigo, light-headedness, mental confusion, depression, psychosis & hallucination
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What are the Hematopoietic effects witnessed with Indomethacin (INDOCIN)?
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Neutorpenia, thrombocytopenia & aplastic anemia
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What are specific contraindications for Indomethacin?
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Psychiatric illness and CNS disorder-- eg./ epilepsy, Parkinsonism
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