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Acute Inflammation - ✔✔initial response of increased plasma and leukocytes from
blood to site of injury
Chronic Inflammation - ✔✔progressive shift in type of cells present at the site and
simultaneous destruction + healting of tissue
Autoimmune - ✔✔inability to distinguish self from non-self, progressive tissue injury >
pain, loss of function, disability, decreased quality of life
Misoprostol - ✔✔Action: Mucosal lining of stomach, Reduces gastric acid production in
chronic NSAID use
Uses: Prevention of gastric ulcers chronic NSAID use
SE: diarrhea, cramping
ABORTIFACIENT!-Black Box
Latano-/Travo-/Bimato- PROST - ✔✔A prostaglandin
Action: increase uveoscleral outflow
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,(Bimatoprost for eyelash growth/pigmentation)
Use: open angle glaucoma, elevated intraocular pressure (ophthalmic soln)
Epoprostenol
Illoprost - ✔✔Action: potent pulmonary vasodilator
Use: Pulmonary Arterial HTN (PAH)
Form: continuous IV infusion due to short half life, nebulizer
Side effect (Illoprost): Dizziness, Flushing, Headache, fainting (syncope)
Aloprostadil - ✔✔A Prostaglandins
Action: smooth muscle relaxation
Use: Erectile dysfunction, patency of neonate ductus arteriosus
Lubiprostone - ✔✔Action: increase intestinal fluid secretion
Use: Chronic constipation, IBS
SE: nausea, diarrhea
NSAIDs - ✔✔Action: ALL NSAIDS act by inhibiting cyclooxygenase enzymes resulting
in decreased PROSTaglandin synthesis --> inactivate COX
SE: CV events (thrombosis, MI, stroke), GI events(bleeding, ulceration, perforation),
renal toxicity
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,COX-1 vs. COX-2 - ✔✔diffences in safety and efficacy depend on the balance of COX-1
vs. COX-2
COX-1 inhibition - ✔✔Prevention of CV events, most adverse events(like stomach
ulcers and gastric bleeding; less platelet aggregation)
COX-2 inhibition - ✔✔anti-inflammatory and analgesia
Metabolism of ASA - ✔✔irreversibly acetylates (inactivates COX)
becomes salicylate
3 Actions of ASA - ✔✔anti-inflammatory
antiPyretic
Analgesic
Acetylsalicylic acid (ASA aka Aspirin) - ✔✔NSAID prototype (approved by FDA in
1939)
Action: irreversibly inactivates cyclooxygenase(unique)
Uses:
Topical-->acne, corns, calluses, and warts
Inhibits platelet aggregation --> irreversibly inhibits Thromboxane(COX-1 path) for 3-
7days (life of the platelet)
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, Decreases vasoconstriction
Reduces risk of: TIAs(storke;low dose); MI sudden death, unstable angina; CV risk in
revascularization procedures
ASA Pharmacokinetics - ✔✔Oral administration: salicylates passively absorbed in
stomach and small intestine
Rectal absorption is slow and urliable
Must be avoided in children and teenagers (<20) with viral infections, to prevent Reyes
syndrome
ASA Dosages - ✔✔Analgesic activity-->low doses( 2 35mg ASA QID =8 tablets)
Anti-inflammatory-->higher doses (12-20 tablets/day; w/RA)
Long-term MI prophylaxis (81-162mg/day)
Acute MI--> 162-325mg non-EC(chewed)
Stroke prophylaxis-->50-325mg/day
ASA side effects - ✔✔N/V, epigastric pain, microcopic bleeding (occult)-->take with
food
Avoid one week prior to surgery(anti-platelet)
Toxic doses: respiratory depression, metabolic acidosis, and hyperthermia
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