Antiinflammatory Drugs

Front 1

Function of PGE1?

Back 1

Protective on GI mucosa
(Misoprostol: Rx of NSAIDS ulcers)
(Alprostadil: Maintains PDA)

Front 2

Function of PGE2?

Back 2

uterine contractions
(dinoprostone used for cervical ripening)
(elevated in dysmenorrhea)

Front 3

Function of PGF2?

Back 3

uterine and bronchiolar muscle contraction
(Dinoprost & Carboprost: Abortificient)
(Latanoprost (prostaglandin analogue): Rx of glaucoma)
(elevated in dysmenorrhea)

Front 4

Function of PGI2 (prostacyclin)?

Back 4

inhibits platelet aggregation, vasodilator
(Epoprostenol: Used in pulmonary HTN)

Front 5

MOA for aspirin?

Back 5

inhibits thromboxanes

Front 6

Function of TXA2 (thromboxane)?

Back 6

Opposes the effects of PGI2, promotes platelets aggregation, bronchoconstriction and vasoconstriction

Front 7

Effects of PGI2 & TXA2 on platelets?

Back 7

PGI2 activates cAMP, which increases internal Ca++ pump, which decreases free Ca++, which stabilizes platelets.
TXA2 activates phospholipase C, which increases IP3, which mobilizes bound Ca++, which increases free Ca++, which causes platelet aggregation.

Front 8

LTB4 (leukotriene) function?

Back 8

mediates inflammation thru chemotaxis, which increases free radicals and causes cell injury

Front 9

LTA4, LTC4, and LTD4 function?

Back 9

release of slow-reacting substance of anaphylaxis, bronchoconstriction, and vasoconstriction

Front 10

Corticosteroid MOA?

Back 10

inhibits phospholipase A2 enzyme from the top, blocks cyclooxygenase: antiinflammatory effects, blocks lipoxygenase: immunosuppressant effects

Front 11

Zileuton MOA?

Back 11

lipoxygenase inhibitor

Front 12

Zafirlukast and
Montelukast (tablet) MOA?

Back 12

leukotrienes Inhibitors

Front 13

NSAIDs MOA?

Back 13

irreversible inhibits cyclooxygenase pathways: COX 1 and COX2, decrease PGs and TXA2, dose dependent (ex: aspirin or acetyl salicylic acid)

Front 14

Biggest pharmalogical effects of aspirin?

Back 14

antiinflammatory (inhibition of COX2) and antiplatelet aggregation (inhibition of TXA2), can also have uricosuric effects at high (can cause gout) and low doses, and 1 baby aspirin a day reduces MI by 44%

Front 15

High dose effects of aspirin?

Back 15

1. respiratory alkalosis
2. metabolic acidosis
3. gastritis (Inhibition of PGE2)
4. increase bleeding time (due to decrease platelets aggregation, increase prothrombin time or coagulation time (INR - international normalized ratio), and inhibition of synthesis of vit K factors)
5. uricosuric
6. salycylism (tinnitus, vertigo, and decrease hearing)

Front 16

Signs of acute aspirin toxicity?

Back 16

1. Respiratory alkalosis then Respiratory acidosis
2. Hypokalemia
3. Metabolic acidosis
4. Fever

Front 17

Signs of aspirin hypersensitivity?

Back 17

triad of asthma, nasal polyps, and atrophic rhinitis

Front 18

What is Reye's Syndrome due to?

Back 18

aspirin + viral infection in children

Front 19

How many tablets for severe aspirin toxicity?

Back 19

30 tablet for adults
4-6 tablets for kids
No antidote

Front 20

Emergency management of aspirin toxicity?

Back 20

alkalization of the urine

Front 21

Acetaminophen MOA?

Back 21

Inhibits only centrally found cycloxygenase (CNS), but has no effects on peripheral cyccloxygenases, not antiinflammatory

Front 22

What are the effects of acetaminophen toxicity?

Back 22

hepatotoxicity: depletion of GSH stores lead to accumulation of reactive metabolite (N-acetylbenzoquinoneimine) which reacts with the hepatocytes; antidote - acetylcysteine (mucomist)
that supplies -SH groups that inactivates the metabolite

Front 23

Ibuprofen

Back 23

reversible inhibitor of COX1 & COX2, Doesn't affect activity of warfarin or hypoglycemic

Front 24

naproxen

Back 24

reversible inhibitor of COX1 & COX2, used in gout

Front 25

etodolac

Back 25

reversible inhibitor of COX1 & COX2

Front 26

indomethacin

Back 26

reversible inhibitor of COX1 & COX2, popular till '99, but still used for PDA closure, side effects: Thrombocytopenia, agranulocytosis

Front 27

ketorolac (injectable) and nabumetone

Back 27

reversible inhibitor of COX1 & COX2

Front 28

sulindac

Back 28

reversible inhibitor of COX1 & COX2, no renal effects, cramps and rashes, side effects: pancreatitis

Front 29

tolmetin

Back 29

reversible inhibitor of COX1 & COX2, doesn't affect activity of oral hypoglycemic

Front 30

diclofenac (popular in Antigua, used topically in US)

Back 30

reversible inhibitor of COX1 & COX2, side effects: hepatotoxicity

Front 31

NSAIDs side effects?

Back 31

dyspepsia, interstitial nephritis, decrease clearance of some drugs (oral hypoglycemics, methotrexate, & lithium) which increases their activity, decrease activity of antihypertensive drugs (ACE inhibitors, loop diuretics, beta blockers)

Front 32

Selective COX2 Inhibitors

Back 32

Good: for inflammation (arthritis), stomach b/c its protected
Bad: COX1 receptors are activated, bad for heart b/c of platelet aggregation leading to blood clot & myocardial infarction

Front 33

Drugs ending with "triptan" are used for?

Back 33

migraines (ex: sumatriptan, zolmitriptan, frovatriptan

Front 34

MOA of "triptans"?

Back 34

agonist at 5HT1D receptors in cerebral blood vessels, side effects: possible asthenia, throat pressure

Front 35

Ergotamine and Methysergide MOA?

Back 35

Partial agonist at alpha1 and 5HT2 in blood vessels, vasoconstriction leads to decrease pulsation in acute attack of migraine

Front 36

Migraine Prophylaxis?

Back 36

1. Beta blockers (keep blood vessels dilated, but serious side effects)
2. Tricyclic antidepressant (stigma of the medication and won’t take it)
3. Calcium channel blockers (also a BP med)
4. Carbamazepine (anti-seizure med with serious complications)
5. Gabapentin (anti-anxiety)
6. Valproic acid (manic-depressive)