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D&D Unit 2 > NSAIDs (complete) > Flashcards

NSAIDs (complete) Flashcards

1
Q

What is arachidonic acid?

A
  • a phospholipid, omega-6 fatty acid
  • stored as an ester
  • cleaved by esterases to become activated/processed into descendants
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2
Q

Describe the biosynthetic pathway for production of prostaglandins

A

Arachidonic acid —> endoperoxide – cyclic intermediate (using COX-1 and COX-2) —-> prostaglandins E2, D2, F2a (using endoperoxide isomerases)

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3
Q

Describe the biosynthetic pathway for production of prostacyclins

A

Arachidonic acid —> endoperoxide – cyclic intermediate (using COX-1 and COX-2) —-> prostacyclin I2 (prostacyclin synthase)

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4
Q

Describe the biosynthetic pathway for production of leukotrienes

A

Arachidonic acid —> leukotriene A4 (5-lipoxygenase) —> LTB4 and LTC C4/D4/E4

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5
Q

Compare cyclooxygenase 1 and 2

A

COX enzyme critical for prostaglandin and thromboxane production

Both catalyze synthesis of cyclic endoperoxide, PGH2 (unstable intermediate)

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6
Q

Where is COX-1 expressed?

A

Ubiquitously

1) GI tract
2) Platelets
3) Kidneys
4) Vascular smooth muscle
5) Bone

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7
Q

What is COX-1’s role in GI tract?

A
  • Decreases gastric acid secretion
  • Increases mucosal secretion (protects!)
  • Promotes smooth muscle contraction
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8
Q

What is COX-1’s role in platelets?

A

Have a pro-aggregatory effect

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9
Q

What is COX-1’s role in the kidneys?

A

Promotes increased renal blood flow

Increased diuresis

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10
Q

What is COX-1’s role in vascular smooth muscle?

A

For prostaglandin/prostacyclin pathway: vasodilation

Tromboxane: vasoconstriction

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11
Q

What is COX-1’s role in the bone?

A

Stimulates formation/resorption

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12
Q

Where is COX-2 expressed?

A

When induced by cytokines, shear stress, GFs

When up-regulated as needed for specialized functions

Located in inflamed/activated tissues:

1) Areas of pain/inflammation
2) Hypothalamus
3) Kidneys
4) Endothelial cells
5) Uterine smooth muscle
6) Ductus arteriosus

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13
Q

What is COX-2’s role in areas of pain/inflammation?

A

Enhance edema formation

Enhance leukocyte infiltration via vasodilation

Increase bradykini pain-producing activity

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14
Q

What is COX-2’s role in the hypothalamus?

A

FEVER!

Increased heat generation

Decrease in heat loss

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15
Q

What is COX-2’s role in the kidneys?

A

Maintains renal blood flow (stresses can alter that)

Critical in elderly, when renal function deteriorates

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16
Q

What is COX-2’s role in endothelial cells?

A

Endos are upregulated by blood flow stress

Vasodilation and anti-aggregatory platelet effects

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17
Q

What is COX-2’s role in uterine smooth muscle?

A

Contributes to labor contractions near parturition

A COX inhibitor would cause a lot of problems in the third trimester

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18
Q

What is COX-2’s role in the ductus arteriosus?

A

Maintains patent ductus arteriosus via vasodilation

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19
Q

What are the effects of prostaglandins on vascular smooth muscle?

A

PGE2 causes vasodilation

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20
Q

What are the effects of prostaglandins on platelets?

A

No effect

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21
Q

What are the effects of prostaglandins on GI tract smooth muscle/secretory cells?

A

PGE2/PGI2 inhibit HCl secretion

Increase mucous secretion

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22
Q

What are the effects of prostaglandins on kidney cells?

A

PGE2/PGI2 increase renal blood flow

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23
Q

What are the effects of prostaglandins on uterine cells?

A

PGF2a induces contractions

24
Q

What are the effects of prostaglandins on inflammatory cells?

A

PGE2/PGI2 potentiates …

1) pain
2) edema
3) fever

25
What are the effects of leukotrienes on inflammatory cell function?
LTB4 is chemoattractice for neutrophils Induces endothelial cells and neutrophils to express adhesion proteins
26
What are the effects of leukotrienes on pulmonary cells?
Intense contraction in bronchial smooth muscle ASTHMA!
27
What are the effects of leukotrienes on vascular smooth muscle?
Intense vasodilation ---> edema Promotes leukocyte margination/adhesion
28
Describe the functional interactions between prostacyclin and thromboxane on vascular smooth muscle and platelets.
Prost: vasodilation, disaggregation Throm: vasoconstriction, aggregation They are opposites!!!
29
What are the effects of aspirin on COX-1 and 2? (Therapeutic uses)
Irreversibly inactivates COX-1 and 2 Uses: 1) Analgesic 2) Antipyretic 3) Anti-inflammatory 4) Anti-platelet
30
What are the effects of NSAIDs on COX-1 and 2? (Therapeutic uses)
Reversibly inactivates COX-1 and 2 Uses: 1) Analgesic 2) Antipyretic 3) Anti-inflammatory NOT ANTI-PLATELET
31
What are the effects of acetaminophen on COX-1 and 2? (Therapeutic uses)
CNS reversibly inactivates COX2 Uses: 1) Analgesic 2) Antipyretic NOT ANTI-INFLAMMATORY or ANTI-PLATELET
32
What are the effects of COX-2 selective inhibitors on COX-1 and 2? (Therapeutic uses)
Inhibits only COX2 activity Uses: 1) Analgesic 2) Antipyretic 3) Anti-Inflammatory NOT ANTI-PLATELET
33
What are the adverse rxns from aspirin?
1) GI upset 2) Bleeding 3) Decreased renal function 4) Decreased labor contractions DOES NOT increase clotting
34
What are the adverse rxns from NSAIDs?
1) GI upset 2) Bleeding 3) Decreased renal function 4) Decreased labor contractions DOES NOT increase clotting
35
What are the adverse rxns from acetaminophen?
Unlike NSAIDs/aspirin NO... 1) ...GI upset 2) ...Bleeding 3) ...Decreased renal function 4) ...Decreased labor contractions 5) ...Increased clotting Potential for hepatotoxicity
36
What are the adverse rxns from COX-2 inhibitors?
1) Decreased renal function 2) Decreased labor contractions 3) Increased clotting 4) Increase risk of cardio thrombotic events NO GI UPSET or BLEEDING
37
Why is low dose aspirin able to exhibit anti-thrombotic/cardioprotective effect unlike high dose?
Aspirin inhibits platelet aggregation --- low dose is COX-1 specific B/c it's irreversible platelets cannot produce COX-1 (no nucleus) ---- TXA2 synthesis inhibited for life of platelet (>8 days) At high dose, the aspirin no longer concentrates around just platelets, also endothelial cells --- these have COX-2 (normally anti-thrombotic)
38
How is the low dose aspirin effect associated with COX-2 selective inhibitors?
COX-1 inhibition is favored over COX-2 Therefore the inhibition of pro-clotting is favored over that of anti-clotting
39
Again, what are the therapeutic uses of aspirin?
Low dose inhibits thrombus formation Results from irreversible inhibition of COX-1&2 Analgesic, antipyretic, anti-inflammatory, anti-platelet
40
Describe the metabolism and excretion of aspirin
M: rapid absorption from stomach/sm intestine --- ASA rapidly hydrolyzed to salicylate by esterases E: Salicylate more slowly eliminated by glycine/glucuronide conj. --- high dose = zero order kinetics
41
What are the side effects of aspirin?
1) Gastric irritation 2) Increased bleeding time 3) Renal dysfunction
42
What happens when a pt overdoses on aspirin?
Mild intox: tinnitus, headache, dizziness, diarrhea, seeing probs, thirt Acute intox-overdose: uncoupling of oxidative phosphorylation, respiratory alkalosis, metabolic acidosis
43
What are the contraindications for aspirin?
1) pts w/ gastric ulcers 2) pts on oral anticoags 3) pregnant pts 4) pts w/ hypersensitivity (allergy) 5) children s syndrome
44
What drugs interact w/ aspirin?
1) Warfarin (inhibit platelet function) | 2) Alcohol (add'l gastric irritation/bleeding)
45
What is a lethal dose of aspirin?
10-30 grams
46
Again, what are the therapeutic uses of traditional NSAIDs?
Anti-inflammatory, antipyretic, analgesic Sometimes used for arthritis, dysmenorrhea
47
What are the side effects of NSAIDs?
1) gastric irritation if taken w/o food | 2) platelets transient/reversible
48
What happens when you overdose on NSAIDs?
Rapid onset of renal failure, nausea, vomiting, GI pain/upset Generally better tolerated and safer in overdose than aspirin
49
What are the contraindications for NSAIDs?
Safety for use in pregnancy not established
50
What are the therapeutic uses of acetaminophen?
- A Cox 2 inhibitor only in the CNS - Analgesic, antipyretic, less anti-inflammatory Compared w/ aspirin: - Does not upset stomach - Weak effect on platelets/clotting time - Minimal renal effects - no Reyes - considered safe in pregnancy
51
Describe the metabolism and excretion of acetaminophen
- Absorbed in GI - Metabolized to inactive sulfate and glucuronide (phase II conj) - Large doses --->> toxic product in liver - t1/2 = 2-3 hrs
52
What are the side effects of acetaminophen?
- mild ^ in hepatic enzymes, reversible - larger dose: dizziness, excitement, disorientation - toxicity
53
What happens when you overdose on acetaminophen?
Glutathione stores are depleted --->> can't inactivate toxic metabolite --->> liver damage (death if untreated) t1/2 of Ac ^ 2-3 fold
54
What are the therapeutic uses for Celicoxib?
A COX-2 specific inhibitor - Anti-inflammatory, antipyretic, analgesic - Used for arthritis, menstrual pains, acute pain
55
Describe the metabolism and excretion of Celicoxib
M: well absorbed, metabolized by liver (CYP2C9) E: renal --- long half-life allows for 1/2 daily doses
56
What are the side effects of Celicoxib?
1) Renal | 2) Increased risk of adverse CV event
57
What are the contraindications for Celicoxib?
Do not use in pregnant women (blocks uterine contractions) Do not use in people who are prone to cardiovascular issues!! BADDD A sulfa drug --->> watch out for allergies

D&D Unit 2 (10 decks)

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