Smooth Muscle Prostaglandins Part 1 Flashcards
____________________ are chemical mediators found in most body tissues that regulate cell functions and promote the inflammatory response
prostaglandins
what are the 5 types of prostaglandins
- PGD2 2. PGE2 3. PGF2 4. PGI2 5. thromboxane A2
where is PGD2 located?
- airways 2. brain 3. mast cells
where is PGE2 located ?
- brain 2. kidneys 3. platelets 4. vascular smooth muscle
where is PGF2 located?
- airways 2. eyes 3. uterus 4. vascular smooth muscle
where is PGI2 located
- brain 2. endothelium 3. kidneys 4. platelets
where si thromboxane A2 located?
- kidneys 2. macrophages 3. platelets 4. vascular smooth muscle
effects of PGD2
bronchoconstriction
effects of PGE2
- bronchodilation 2. gastroprotection 3. increases activity of GI sm. muscle 4. increase sensitivity to pain 5. increase body temperature 6. vasodilation
effects of PGF2
- increases activity of GI smooth muscle 2. bronchoconstriction 3. increases uterine contraction
effects of PGI2
- decrease platelet aggregation 2. gastroprotection 3. vasodilation
effects of Thromboxane A2
- increase platelet aggregation 2. vasoconstriction
prostaglandin synthesis comes from the precursor ________________________
arachadonic acid
in prostaglandin synthesis, physiologic prostaglandins originate from _________________, and pathologic prostaglandins originate from ______________
COX-1; COX-2
which prostaglandin synthesis pathway plays a role in pain and inflammation, is inducible, and is only in circulation in response to a condition?
COX-2
MOA of NSAIDS (asprin, ibuprofen, and tylenol)
inhibit COX1 and COX2
NSAIDS (asprin, ibuprofen and tylenol) tx ____________________, but do not ___________________
sx; tx the underlying disorder
__________________ is a peripheral and central analgesic, but __________________ is only a peripheral analgesic
ASA; ibuprofen
uses of NSAIDs (asprin, ibuprofen, and tylenol)
- analgesic 2. antipyretic 3. anti-inflammatory
_______________ binds irreversibly to plt COX-1, and ____________ bind reversibly to plt COX-1
ASA; NSAIDs
What is the antiplt effects of asprin
- prevents the synthesis of thromoxane A2 2. inhibits platelet aggregation 3. effects last for the lifetime of the plt (7-10 days)
what is the antiplt effects of non-asprin NSAIDs?
- anti-plt effects only last while the drug is present in the blood (~4.5 half lifes) 2. plt fx returns after 4 half lives
Asprin and all NSAIDS (except tylenol and COX-2 specific drugs) have what effects on plts?
- inhibit plt aggregation 2. interfere with blood coagulation 3. increase the risk of bleeding
which drug is the prototype anti-prostaglandin drug
asprin
T/F: asprin is nephrotoxic at high doses
TRUE
asprin effects in the kidneys
- constricts renal arteries and arterioles 2. decreases the bloodflow to the kidneys 3. decreases GFR 4. increases the retention of salt and water
which anti-prostaglandin drug is safer in regards to GI bleeds? (NSAIDS or ASA?)
NSAIDS
__________________ is effective in the tx of mild to moderate pain of the skin, muscles, joints, and other connective tissue
ASA
prostaglandins normal fx in the kidney
- increases blood flow via VD at times of decreased blood flow 2. counters the VC effects of local vasoconstrictors (epi, AngII)
__________________ is a propionic acid derivative medication that inhibits prostaglandin synthesis
Ibuprofen
___________________ is a selective COX 2 inhibitor
celecoxib
what meds are widely used over asprin due to having less Gastric irritation and GI upset
NSAIDs (ibuprofen and celecoxib)
half life of celecoxib
11 hours
celecoxib (compared to asprin) has less ________________, no _______________ effects, and can potentiate ______________________.
Gastric irritation; antiplt; pre-existing HTN
T/F: celecoxib is not protein bound
false; celecoxib is highly protein bound
what labs should be monitored if a pt is taking ibuprofen or celecoxib regularly
BUN/Cr due to possible renal damage
if pt has liver or renal damage, but needs to be prescribed a cox inhibitor like ibuprofen or celecoxib, what changes would you make to the dose?
decrease it
what route is celecoxib available in?
PO only
route that asprin is available in?
- P.O: enteric coated, chewable 2. PR
T/F: asprin is available in liquid form
false; unstable in liquid
route that Ibuprofen is available in?
PO: tablet, chewable, capsule, oral suspension, oral drops
advantage of tylenol over other COX inhibitors
does not cause: N/V, GI bleeding, or disrupt coagulation
tylenol is equal to asprin in its ______________&_____________ effects, but lacks ________________ effects
analgesic; antipyretic; anti-inflammatory
what routes is tylenol available in?
- P.O: tablet, liquid 2. PR 3. IV
which med is marketed OTC with many analgesic and cold remedies, and is also prescribed with codeine, hydrocodone, oxycodone, and percocet to enhance analgesic effects
tyelnol
C/I for NSAIDs (asprin, ibuprofen, and tylenol)
- PUD 2. GI or other bleeding d/o 3. hypersensitivity rxn (cross rxn with ASA and NSAIDs) 4. impaired renal fx 5. children with flu/chicken pox 2/2 reye’s syndrome 6. alcoholics 7. asthmatics
__________________ can be given to children for fever and/or pain but until at least 2 years of age
acetaminophen
what med is safe to give children for fever, but not until at least 6 mo of age
ibuprofen
what medication is c/i in children <12 years of age
asprin 2/2 reyes syndrome and rapidly progressive encephalopathy after acute viral illness
__________________ is a safe COX inhibitor for the elderly in recommended doses as long as do not have liver damage or abuser of etoh
acetaminophen
