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57 Cards in this Set

  • Front
  • Back
This acid is derived from cell membrane lipids.


12
Arachidonic acid
What are the 2 main groups of eicosanoids?


12
1. Prostaglandings
2. Leukotrienes
This enzyme in the cell membrane generates arachidonic acid from lipid constituents.

12
Phospholipase A2
This enzyme converts arachidonic acid to PGG & PGH

12
Cycooxygenase
This enzyme converts arachidonic acid to leukotriene precursors
(HPETEs- Hydroperoxy-eicosatetraenoic acid)

12
Lipoxygenase
What are the five prostaglandins used as therapeutic agents?

12
1. Misoprostol (CYTOTEC)
2. Epoprostenol (FLOLAN)
3. Dinoprostone (PROSTINE2)
4. Treprostinil (REMODULIN)
5. Alprostadil (CAVERJECT or PROSTIN VR PEDIATRIC)
What are the four prostaglandin therapeutic agents used in eyedrop form?

12
1. Bimatoprost (LUMIGAN)
2. Travapost (TRAVATAN)
3. Unoporstone (RESCULA)
4. Latanoprost (XALATAN)
This synthetic PGE1 analog is used in the treatment of NSAID induced ulcers.

12
Misoprostol (CYTOTEC)
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.

12
Dinoprostone (PROSTINE2)
This synthetic preparation of PGE2 is administered vaginally and affects the collagenase of the cervix resulting in softening.

12
Dinoprostone (PROSTINE2)
This PGE1 analogis used to maintain the patency of neonate's DUCTUS ATERIOSUS.

12
Alprostadil (PROSTIN VR PEDIATRIC)
What are the adverse effects of Alprostadil (PROSTIN VR PEDIATRIC)?
Bradycardia, Hypotension, Hyperplexia
What is Alprostadil (CAVERJECT) used for?
Erectile dysfunction; intravernosal injxn or urethral suppositories-- acts as smooth muscle relaxant, increased blood flow--> ERECTION
What are the side effects of Alprostadil (CAVERJECT)?
Penile pain, penile fibrosis, flushing, diarrhea, headache and fever
Which prostaglandin is used for treatment of GLAUCOMA or ocular hypertension as an eye solution?
Latanoprost (XALATAN)
What three prostanoids were developed due to the success of Latanoprost's successful treatment of ocular hypertension?

12
1. Bimatoprost (LUMIGAN)
2. Travapost (TRAVATAN)
3. Unoprostone (RESCULA)= Docosanoid
What is the adverse effect of using ocular prostaglandins as therapeutic agents?

12
Iris Pigmentation
What is Epoprostenol indicated for?


12
Treatment of Primary Pulmonary hypertension.
_________ is a PGI2 and is also known as prostacyclin.


12
Epoprostenol (FLOLAN)
Pulmonary Hypertension


12
Is a an abnormal elevation of the pressure in the blood vessels of the lungs.
NSAIDs are WEAKER or STRONGER than narcotic analgesics.


13
WEAKER
What are the 3 main effects of NSAIDs?


13
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
This includes a series of events that can be elicited by infections, antigen-antibody reactions and thermal or physical injury.


13
INFLAMMATION-- Clinical signs inclued redness, swelling, heat, pain and loss of function
What are the three distinct phases of the inflammation response?


13
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
Rheumatoid arthritis, Juvenile rheumatoid arthritis, degenerative joint disease (Osteoarthritis) and Gout are examples of this type of disease.

13
INFLAMMATORY DISEASE
What are the therapeutic strategies in treating inflammation?


13
* Relief of PAIN
* Slow or stop tissue damaging process
DMARDS


13
Disease Modifying Anti-Rheumatic Drugs
Name three agents used in the treatment of inflammation.


13
1. NSAIDS
2. Glucocorticoids
3. DMARDs
What affects do NSAIDs have?


13
Reduce inflammation, pain and elevated body temperature
What is the major problem with use of DMARDs (disease modifying anti-rheumatic drugs)?


13
TOXICITY
The _______ regulate the set point at which body temperature is maintained


13
HYPOTHALAMUS
What is a natural source of Salicylates?


13
WILLOW BARK
This is a better glycoside from Willow Bark.


13
SALICIN
This chemical processing of Salicin results in salicylic alcohol and glucose


13
Salicin HYDROLYSIS
_________ can be converted to Salicylic acid by chemical modification


13
SALICYLIC ALCOHOL
Salicylic Alcohol can be converted to salicylic acid by chemical modification here.


13
IN VIVO= In the body
ACETYL SALICYLIC ACID
Aspirin
What is the Mechanism of Action for Aspirin (ASA)?


13
It non-selectively and irreversibly inhibits both isozymes of Cyclooxygenase (COX I & II) thereby inhibiting the synthesis of prostaglandins and thromboxanes
What is responsible for the irreversible nature of Aspirin's activity?


13
The acetyl group of ASA covalently binds the enzyme (COX I or II) and permanently inhibits its activity.
What is unique about aspirin's inhibition of cyclooxygenase?
Its IRREVERSIBILITY!
________ can inhibit granulocyte adherence to damaged vasculature, stabilize lysosomes, inhibit chemotaxis of polymorphonuclear leukocytes and macrophages.


13
Aspirin
ASA's antipyretic effects is due to ____________.


13
COX inhibition in the CNS
ASAs analgesic effects are Peripheral or Central?


13
PERIPHERAL AND CENTRAL EFFECTS
____ acts to promote platelet aggregation.


13
TXA2= Thromboxane A2
What are the adverse effects of ASPIRIN?
*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
What are some drug interactions associated with Aspirin?


13
* Enhances effects of Warfarin
*Antagonizes effects of Uricosurics
*Increases METHOTREXATE concentrations
What are the three steps in treatment of Salicylate intoxication?


13
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
Describe non-acetylated salicylates.


13
*Effective anti-inflammatory agents
*Less effective analgesics than ASA
*Weak COX inhibitors
Name 4 non-acetylated salicylates.


13
1. Choline salicylate (ARTHROPAN)
2. Sodium Salicylate
3. Magnesum Salicylate (MAGAN)
4. Salicylsalicylate (DISCALCID)
What is Acetaminophen's mechanism of action?


13
Is a weak COX-inhibitor in peripheral tissues
What explains APAP's antipyretic affects?


13
It has the ability to inhibit COX in the brain however it does not inhibit neutrophil activation.
Acute overdoseage of acetaminophen can result in...? (4)


13
*Dose-dependent fatal necrosis of liver
*Renal tubular necrosis
*HYPOglycemic coma
*Formation of toxic metabolite--N-hydroxylation-N-acetyl-para-benzoquinonime
Elevated aminotransferase, elevated bilirubin, liver damage and death are all symptoms seen 2-4 days after...?


13
Acute acetaminophen overdose
What is the principal antidotal treatment for acetaminophen toxicity?


13
Administration of Sulfhydrul compound-- act to replenish hepatic stores of GLUTATHIONE
**N- Acetylcystein (MUCOMYST): PO or IV
What are some of the side effects for Inomethacin (INDOCIN)?


13
HA, dizziness, vertigo, light-headedness, mental confusion, depression, psychosis & hallucination
What are the Hematopoietic effects witnessed with Indomethacin (INDOCIN)?


13
Neutorpenia, thrombocytopenia & aplastic anemia
What are specific contraindications for Indomethacin?


13
Psychiatric illness and CNS disorder-- eg./ epilepsy, Parkinsonism