The flashcards below were created by user
Anonymous
on FreezingBlue Flashcards.
-
Eicosanoids are metabolites of __________ _______ that can be synthesized and released from nearly ___ cells to affect a broad range of biological.
-
Autocoids are ________ which are biologically active compounds that are _______ synthesized and released. they act _________. they have a short _____-_____ and duration of action.
- eicosanoids
- rapidly
- locally
- half-life
-
biologically active eicosanoids include:
PG, TX, LT
-
Actions of Eicosanoids
- inflammation
- pain
- fever
- GI tract
- bronchial smooth muscle
- platelet aggregation
- uterus
- cardiovascular
- others
-
Indirect inhibitors of eicosanoids:
- glucocorticoids
- fx cox1/2, lipocortin, Hcz
-
glucocorticoids prototypes
hydrocortisone/cortisol, prednisone, decxamethasone
-
glucocorticoids act by modifying gene expression. T/F?
true
-
glucocorticoids cellular actions:
- upregulate lipocortin
- down-regulate cox1/2
-
glucocorticoids clinical uses
- anti-inflammatory
- replacement therapy
-
glucocorticoids side fx
long term= cushings syndrome
-
NSAID prototypes
- aspirin
- Sulindac
- Indomethacin
- Ketorolac
- Ibuprofen
- Naproxem
-
NSAID mechanism
directly inhibit Cox-1 and Cox-2
-
which NSAIDS are irreversible
-
which NSAIDS are reversible
- indomethacin
- ibuprofen
- acetaminophen
-
reversibly binding NSAIDS are generally _______ acting.
short
-
are reversible NSAIDS useful as blocker of clot formation?
NO, only irreversible are
-
Stephens johnson syndrome can occur with?
acetic acids
-
what are the NSAID Acetic Acids and Pyrroles?
Indomethacin, Sulindac, Ketorolac
-
What are the NSAID PROprinoic acids?
IB, Naproxem
-
are proprinoic acids reversible binders of cox1/2?
YES
-
Are NSAID propinoic acids useful in blocking clot formation?
NO
-
Acetaminophen is believed to act by inhibiting _____, CNS specific.
COX 1
-
Acetaminophen fx:
- weak inhibition of prostanoid synthesis
- blocks prostanoid effects on T and pain in CNS
-
Is Acetaminophen useful as an anti-inflammatory?
NO
-
Acetaminophen has the risk of __________, but not ________ or _________ like most NSAIDS.
- hepatotoxicity
- GI fx
- blockade of plt aggregation
-
What are the NSAID Selective COX-2 inhibitors?
- rofecoxib (vioxx)
- celecoxib (celebrex)
- valdecoxib (bextra)
- Etoricoxib (arcoxia)
-
what is the cox 2 hypothesis?
cox 2 more specific to inflammatory response
-
what is the NSAID Selective COX-2 inhibitor mechanism of action?
REVERSIBLE direct binding of Cox-2. also binds cox 1 but is 30x more selective for cox 2
-
What is the advantage of using NSAID Selective COX-2 inhibitors?
REDUCED neg GI fx
-
Celebrex is ____x more selective for Cox-2
7.6
-
VIOXX is ____x more selective for Cox-2
35
-
BEXTRA is ____x more selective for Cox-2
30
-
ARCOXIA is ____x more selective for Cox-2
106
-
Cox-2 selective inhibitors cause 2-3 fold increase in risk for
heart attack
-
which Cox-2 selective inhibitor is on market now?
CELEBREX
-
COX-2 is being studied to treat
cancer and alzhiemers
-
5'-Lipoxygenase inhibitor prototypes
Zileuton (Zyflo)
-
5'-Lipoxygenase inhibitor prototypes are useful in tx of astham and anaphylaxis. Explain why:
Leukotrienes are the most powerful constrictors of bronchial smooth muscle, and this inhibits the enzyme that makes leukotrienes.
-
5'-Lipoxygenase inhibitor use:
long-term asthma management
-
5'-Lipoxygenase inhibitor prototypes side fx
- gastric indigestion
- short-acting-4x daily (compliance)
-
the future of eicosanoid therapy is to target:
individual receptors
-
Receptor AGONIST prototypes:
- Misoprostol (cytotec)
- Dinoprstone/PGE2 (prostin E2)
- Carboprost (Hemabate)
-
Misoprostol is a ______ ________. it's cellular action is mimic actions of _____.
-
Clinical uses of Misoprostol (receptor agonist)
- used w/ NSAID combo
- prevents negative GI fx of NSAIDS
- uterine stimulant
-
side fx of Misoprostol (receptor agonist)
-
DINOPROSTONE, CARBOPROST TROMETHAMINE, LATANOPROST mechanism, and cellular action. (receptor agonist)
- FP receptor agonist, EP receptor agonist
- mimics cellular action is PGE2, PGF2a
-
DINOPROSTONE, CARBOPROST TROMETHAMINE, LATANOPROST clinical uses: (receptor agonist)
- labor induction
- refractory postpartum hemorrhage
- induced abortion
- anti-glaucomal EYE drop (xalatan)
-
DINOPROSTONE, CARBOPROST TROMETHAMINE, LATANOPROST side fx: (receptor agaonist)
- diarrhea/ vomitting
- uterine hypertonus
-
(receptor agonist) EPOPROSTEROL/prostacyclin mechanism of action and cellular action:
- IP2 receptor agonist
- mimics action of PGI2
-
(receptor agonist) EPOPROSTEROL/prostacyclin uses:
serious pulmonary HTN
-
(receptor agonist) EPOPROSTEROL/prostacyclin side fx:
diarrhea, ^ HR, headache, nausea, flushing
-
Leukotriene receptor ANTAGONISTS prototypes:
- Monteleukast (singulair)
- Zafirlukast (Accolate)
-
Leukotriene receptor ANTAGONISTS mech of action and cell action
- CLT1-R receptor antagonist
- blocks actions of LTD4
-
Leukotriene receptor ANTAGONISTS clinical uses and side fx:
- chronic management of asthma
- mild-GI, headahce, heartburn, allergic rx
|
|