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S3.M2.Pharm3,4
Anti-Inflammatory Drugs 1&2
27
Pharmacology
Professional
06/10/2010

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Cards

Term
***what is the MOA of GLUCOCORTICOIDS?*** guaranteed test question
Definition
***alter gene expression (not COX 1 or 2 or PLC)
Term
what is the BIOAVAILABILITY of NSAIDS?
Definition
ASPIRIN- 70%
SALICYLIC ACID-100%
Term
what is the MOA of NSAIDS?
Definition
-most are REVERSIBLE COMPETITIVE INHIBITORS of COX 1, 2 or both
-ASPIRIN IRREVERSIBLY inhibits COX 1 & 2
Term
what are the three main PHARMACOLOGICAL functions of NSAIDS?
Definition
-anti inflammatory--> inhibit PROSTIGLANDIN and THROMBOXANE synthesis
-antipyretic->via PG block on HYPOTHALAMUS
-analgesic ->inhibit PG influence on pain receptors
Term
common SIDE EFFECTS of NSAIDS?
Definition
-Headaches
-tinnitus (ear ringing)**
-dizziness
-fluid retention hypertension
-edema
Term
do SALICYLATES cross the BBB?
Definition
yes
Term
discuss metabolism and clearance of NSAIDS?
Definition
highly metabolized by the liver and excreted via the kidney
Term
is SALICYLIC ACID more highly excreted in acidic or basic urine?
Definition
basic (high pH=high excretion)
Term
pharmacologic effects of SALICYLATES: CNS?
Definition
low/med dose - antipyretic, analgesic High dose - CN VIII(stimulates), chemoreceptors, cortical & subcortical
Term
pharmacologic effects of SALICYLATES: RESPIRATION?
Definition
-STIMULATES via medulla
-toxic doses causes opposite**
Term
pharmacologic effects of SALICYLATES: CVS?
Definition
dilation of peripheral vessels, ↑plasma volume up to 20%
Term
pharmacologic effects of SALICYLATES: KIDNEYS?
Definition
↓GFR(higher doses), acute renal failure in compromised
Term
pharmacologic effects of SALICYLATES: BLOOD?
Definition
low dose (↓platelets for 7-8 days because platelets aren't cells, cant make more COX enzymes to replace the bound ones), high(sideropenia , hypoprothrominemia)
Term
pharmacologic effects of SALICYLATES: GI?
Definition
-stomach (erosive gastritis)
-liver (bile secretion)
-acid/base--> high doses -> resp alkalosis
--> toxic dose ->resp and metabolic acidosis
Term
pharmacologic effects of SALICYLATES: METABOLISM?
Definition
all high dose effects:
-hyperthermia--> ox phos proton uncoupling -hypoglycemia -->insulin stimulation -hyperglycemia and glycosuria-->adrenal release and glycogenolysis
-hyperkalemia -->↑K+ reabsorption in kidneys
Term
***what are the only SALICYLATES that can be used to treat the inflammation caused by CROHN'S DISEASE and ULCERATIVE COLITIS?***
Definition
Sulfysalizine --> others are contraindicated as they can further irritate GI ulcerations
Term
what is the least effective NSAID for treating ANKYLOSING SPONDYLITIS?
Definition
ASPIRIN
Term
what are some PROPHYLACTIC uses of salicylates?
Definition
-MI
-stable angina
-atrial fib
-arterial thromboembolism
-transient ischemic attack
Term
Alprostadil
Definition
-used for Erectile dysfunction
-keeps DUCTUS ARTERIOSIS OPEN
-A/E can cause penile pain and prolonged erection
Term
Carboprost
Definition
Use: 2nd trimester abortion, post partum hemorrhage
A/E: vomiting, ↑body temp
Term
Dinoprostone
Definition
Use: 2nd trimester abortion (benign
hydatiform mole), Ripening of cervix
Term
Epoprostenol
Definition
Use: pulmonary hypertension
A/E: flushing, headache, hypotension
Term
Latanoprost
Definition
Use: Open angle glaucoma (latinos get more glaucoma)
A/E: conjuctivitis, brown pigmentation of iris
Term
Misoprostol
Definition
Use: NSAID‐induced peptic ulcer, cramping, diarrhea, bone pain
Term
Ibuprofen
Definition
Uses: Closure of PDA
Term
Oxaprozin
Definition
used to treat GOUT
Term
Indomethicin
Definition
potent COX inhibitor
CLOSES PDA (ibuprofen also)
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