UTMB Pharm Exam 1
Acute Inflammation - correct answer-initial response of increased plasma and leukocytes
from blood to site of injury
Chronic Inflammation - correct answer-progressive shift in type of cells present at the site
and simultaneous destruction + healting of tissue
Autoimmune - correct answer-inability to distinguish self from non-self, progressive tissue
injury > pain, loss of function, disability, decreased quality of life
Misoprostol - correct answer-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 - correct answer-A prostaglandin
Action: increase uveoscleral outflow
(Bimatoprost for eyelash growth/pigmentation)
Use: open angle glaucoma, elevated intraocular pressure (ophthalmic soln)
Epoprostenol
Illoprost - correct answer-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 - correct answer-A Prostaglandins
Action: smooth muscle relaxation
Use: Erectile dysfunction, patency of neonate ductus arteriosus
Lubiprostone - correct answer-Action: increase intestinal fluid secretion
Use: Chronic constipation, IBS
SE: nausea, diarrhea
NSAIDs - correct answer-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
COX-1 vs. COX-2 - correct answer-diffences in safety and efficacy depend on the balance of
COX-1 vs. COX-2
COX-1 inhibition - correct answer-Prevention of CV events, most adverse events(like
stomach ulcers and gastric bleeding; less platelet aggregation)
,COX-2 inhibition - correct answer-anti-inflammatory and analgesia
Metabolism of ASA - correct answer-irreversibly acetylates (inactivates COX)
becomes salicylate
3 Actions of ASA - correct answer-anti-inflammatory
antiPyretic
Analgesic
Acetylsalicylic acid (ASA aka Aspirin) - correct answer-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)
Decreases vasoconstriction
Reduces risk of: TIAs(storke;low dose); MI sudden death, unstable angina; CV risk in
revascularization procedures
ASA Pharmacokinetics - correct answer-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 - correct answer-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 - correct answer-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
Approximately 15%-->HTN rxn
Reye syndrome (pedi, viral illness)
Pregnancy category C(1 and 2 trimesters), catagory D (3rd); excreted in breastmilk-avoid if
breastfeeding
ASA toxicity - correct answer-Mild (salicylism) = N/V, hyperventilation, headache, confusion,
dizziness, TINNITUS(ringing)
Severe with large doses: restlessness, delirium, hallucinations, convulsions, coma,
respiratory and metabolic acidosis, respiratory failure and DEATH
-monitor serum slicylate concentrations and pH
,-increased urine pH enhances elimination of salicylate
-Tx: IVF, dialysis may be needed, correction of electrolyte imblances
Children prone to salicylate intoxication (as little as 10mg can cause death)
Drug interactions with ASA - correct answer-Hemorrhage-->Heparin
Decreased urate excretion-->Probenecid, Sulfinpyrozone
Increasese plasma concentration leading to prolonged half-lives, therapeutic effects, and
toxicity
-Bilirubin
-Phenytoin
-Valproic acid
-Sulfinpyrazone
-Thiopental
-Thyroxine
-Triiodothyronine
ASA Overdose - correct answer--mainly see in children/elderly
-maintain ABC's(airway, breathing, circulation)
-activated charcoal
-alkalinize urine with Sodium bicarb
-maintain IV fluids
Renal effect of NSAIDs - correct answer-Inhibition of prostaglandin sythesis
Prostaglandins maintain renal blood flow
-decreased synthesis=vasoconstriction
-results in water?Na retention (edema)
CAUTION: hx of CHF, renal dz
Propionic Acid Derivatives - correct answer-Same actions as ASA except
GI effects: less than ASA
REVERSIBLE inhibitors of COX (more COX-1)
Well absorbed: IV used to close PDA; avoid during 3rd trimester
Ex: ibuprofen (motrin)
Acetic Acid Derivatives - correct answer-Like ASA
REVERSIBLY inhibits cyclooxygenase
Idomethacin(Indocin)-potent anti-inflammatory but toxicity limits use
-acute gout flare, close PDA, ankylosing spondylitis,OA
Sulindac (Clinoril)- prodrug closely related with less toxicity
Oxicam Derivatives - correct answer-Piroxicam (Feldene) and meloxicam (Mobic)
RX: RA, Ankylosing spondylitis, and OA
ONCE A DAY DOSING (long half life)
Piroxicam-->GI side effects are common
Meloxicam-->inhibits both COX-1 and COX-2(more) and has less GI effects
, Heteroaryl Acetic Derivatives - correct answer-Like ASA
RX: long-term use in RA, OA, and AS
More COX-2 selective
Diclofenac(Voltaren)-->more potent than indomethacin, ACCUMULATES IN SYNOVIAL
FLUID. Ophthalmic & topical preparations available
Tolmetin-older drug
Ketorolac (Toradol) -->potent analgesic, moderated anti-inflammatory. IM/IV FORM used
post-op and short-term for moderate to severe pain up to 5 days. Avoid with pedi pt
Nabumetone (Relafen) - correct answer-NSAID Like ASA (anti-inflammatory, antipyretic, and
analgesic)
RX: OA/RA
Metabolized in liver-->be careful with pt w/ hepatic impariment
Dose adjustments for creatinine clearance
Will tolerated(low SE)
Celecoxib (Celebrex) - correct answer-COX-2 Inhibitor:Selective inhibition COX-2>COX-1;
better for managing chronic inflammation than non-selective ASA
Celecoxib(Celebrex): OA, RA(mostly), acute to moderate pain, and familial adenomatous
polyposis
LESS DYSPEPSIA & GI BLEEDING
ONCE DAILY DOSING
Does not inhibit platelet aggregation, no increased bleeding
SE: Renal Toxicity (avoid with sever hepatic and renal disease); potential for increasing MI or
stroke
ContraIndication with SULFA ALLERGY
Acetaminophen (Tylenol) - correct answer-NOT an NSAID
APAP=N-acetyl-p-aminophenol
Action: Inhibits prostaglandin synthesis in the CNS
-AntiPyretic
-Analgesic
-Weak anti-inflammatory due to peripheral inactivation (not active in tissue)
-does not affect platelet function
Rapidly absorbed in GI tract
Conjugated in liver
Uses: Analgesic and antipyretic of choice for children with viral infections or chickenpox
(ASA + Viral infection + Pedi=Reyes)
CATEGORY B for pregnancy. Compatible during lactation
Acetaminophen Contraindications - correct answer-Hepatic disease
Viral hepatitis
hx of EtOH abuse
All at higher risk of acetaminophen-induced hepatotoxicity
Acute Inflammation - correct answer-initial response of increased plasma and leukocytes
from blood to site of injury
Chronic Inflammation - correct answer-progressive shift in type of cells present at the site
and simultaneous destruction + healting of tissue
Autoimmune - correct answer-inability to distinguish self from non-self, progressive tissue
injury > pain, loss of function, disability, decreased quality of life
Misoprostol - correct answer-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 - correct answer-A prostaglandin
Action: increase uveoscleral outflow
(Bimatoprost for eyelash growth/pigmentation)
Use: open angle glaucoma, elevated intraocular pressure (ophthalmic soln)
Epoprostenol
Illoprost - correct answer-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 - correct answer-A Prostaglandins
Action: smooth muscle relaxation
Use: Erectile dysfunction, patency of neonate ductus arteriosus
Lubiprostone - correct answer-Action: increase intestinal fluid secretion
Use: Chronic constipation, IBS
SE: nausea, diarrhea
NSAIDs - correct answer-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
COX-1 vs. COX-2 - correct answer-diffences in safety and efficacy depend on the balance of
COX-1 vs. COX-2
COX-1 inhibition - correct answer-Prevention of CV events, most adverse events(like
stomach ulcers and gastric bleeding; less platelet aggregation)
,COX-2 inhibition - correct answer-anti-inflammatory and analgesia
Metabolism of ASA - correct answer-irreversibly acetylates (inactivates COX)
becomes salicylate
3 Actions of ASA - correct answer-anti-inflammatory
antiPyretic
Analgesic
Acetylsalicylic acid (ASA aka Aspirin) - correct answer-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)
Decreases vasoconstriction
Reduces risk of: TIAs(storke;low dose); MI sudden death, unstable angina; CV risk in
revascularization procedures
ASA Pharmacokinetics - correct answer-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 - correct answer-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 - correct answer-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
Approximately 15%-->HTN rxn
Reye syndrome (pedi, viral illness)
Pregnancy category C(1 and 2 trimesters), catagory D (3rd); excreted in breastmilk-avoid if
breastfeeding
ASA toxicity - correct answer-Mild (salicylism) = N/V, hyperventilation, headache, confusion,
dizziness, TINNITUS(ringing)
Severe with large doses: restlessness, delirium, hallucinations, convulsions, coma,
respiratory and metabolic acidosis, respiratory failure and DEATH
-monitor serum slicylate concentrations and pH
,-increased urine pH enhances elimination of salicylate
-Tx: IVF, dialysis may be needed, correction of electrolyte imblances
Children prone to salicylate intoxication (as little as 10mg can cause death)
Drug interactions with ASA - correct answer-Hemorrhage-->Heparin
Decreased urate excretion-->Probenecid, Sulfinpyrozone
Increasese plasma concentration leading to prolonged half-lives, therapeutic effects, and
toxicity
-Bilirubin
-Phenytoin
-Valproic acid
-Sulfinpyrazone
-Thiopental
-Thyroxine
-Triiodothyronine
ASA Overdose - correct answer--mainly see in children/elderly
-maintain ABC's(airway, breathing, circulation)
-activated charcoal
-alkalinize urine with Sodium bicarb
-maintain IV fluids
Renal effect of NSAIDs - correct answer-Inhibition of prostaglandin sythesis
Prostaglandins maintain renal blood flow
-decreased synthesis=vasoconstriction
-results in water?Na retention (edema)
CAUTION: hx of CHF, renal dz
Propionic Acid Derivatives - correct answer-Same actions as ASA except
GI effects: less than ASA
REVERSIBLE inhibitors of COX (more COX-1)
Well absorbed: IV used to close PDA; avoid during 3rd trimester
Ex: ibuprofen (motrin)
Acetic Acid Derivatives - correct answer-Like ASA
REVERSIBLY inhibits cyclooxygenase
Idomethacin(Indocin)-potent anti-inflammatory but toxicity limits use
-acute gout flare, close PDA, ankylosing spondylitis,OA
Sulindac (Clinoril)- prodrug closely related with less toxicity
Oxicam Derivatives - correct answer-Piroxicam (Feldene) and meloxicam (Mobic)
RX: RA, Ankylosing spondylitis, and OA
ONCE A DAY DOSING (long half life)
Piroxicam-->GI side effects are common
Meloxicam-->inhibits both COX-1 and COX-2(more) and has less GI effects
, Heteroaryl Acetic Derivatives - correct answer-Like ASA
RX: long-term use in RA, OA, and AS
More COX-2 selective
Diclofenac(Voltaren)-->more potent than indomethacin, ACCUMULATES IN SYNOVIAL
FLUID. Ophthalmic & topical preparations available
Tolmetin-older drug
Ketorolac (Toradol) -->potent analgesic, moderated anti-inflammatory. IM/IV FORM used
post-op and short-term for moderate to severe pain up to 5 days. Avoid with pedi pt
Nabumetone (Relafen) - correct answer-NSAID Like ASA (anti-inflammatory, antipyretic, and
analgesic)
RX: OA/RA
Metabolized in liver-->be careful with pt w/ hepatic impariment
Dose adjustments for creatinine clearance
Will tolerated(low SE)
Celecoxib (Celebrex) - correct answer-COX-2 Inhibitor:Selective inhibition COX-2>COX-1;
better for managing chronic inflammation than non-selective ASA
Celecoxib(Celebrex): OA, RA(mostly), acute to moderate pain, and familial adenomatous
polyposis
LESS DYSPEPSIA & GI BLEEDING
ONCE DAILY DOSING
Does not inhibit platelet aggregation, no increased bleeding
SE: Renal Toxicity (avoid with sever hepatic and renal disease); potential for increasing MI or
stroke
ContraIndication with SULFA ALLERGY
Acetaminophen (Tylenol) - correct answer-NOT an NSAID
APAP=N-acetyl-p-aminophenol
Action: Inhibits prostaglandin synthesis in the CNS
-AntiPyretic
-Analgesic
-Weak anti-inflammatory due to peripheral inactivation (not active in tissue)
-does not affect platelet function
Rapidly absorbed in GI tract
Conjugated in liver
Uses: Analgesic and antipyretic of choice for children with viral infections or chickenpox
(ASA + Viral infection + Pedi=Reyes)
CATEGORY B for pregnancy. Compatible during lactation
Acetaminophen Contraindications - correct answer-Hepatic disease
Viral hepatitis
hx of EtOH abuse
All at higher risk of acetaminophen-induced hepatotoxicity
