by mtoom


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What does the Lipoxygenase pathway produce?
Leukotrienes
What 3 classes does the Cyclooxygenase pathway produce?
1. Prostaglandins (PGs)
2. Thromboxane A2 (TxA2)
3. Prostacyclin (PGI2)
What do HMG CoA reductase inhibitors do? What are they also known as?
1. Reduce synthesis of cholesterol.
2. Statins
What do monoamine oxidase inhibitors do?
Prevent breakdown of dopamine.
Give 2 examples of non-selective COX inhibitors.
Aspirin (ASA) and Ibuprofen.
What is Montelukast? How does it work (mechanism)? What does it treat? What are the physiological effects?
1. Leukotriene Receptor Antagonist (LTRA)
2. Inhibits effects of leukotrienes
3. Treats asthma
4. Inhibits restriction of airways; reduces inflammation associated with asthma
What are the 5 roles of PGE2?
1. Fever
2. Vasodilation
3. Pain
4. Inflammation
5. Mucous production
What are the 2 effects of TxA2?
1. Platelet activation
2. Vasoconstriction
What are the 2 effects of PGI2?
1. Platelet inhibition
2. Vasodilation
What are 3 good effects of COX inhibitors?
1. Antipyretic (Reduce fever)
2. Analgesic
3. Anti-inflammatory
What is the bad effect of a non-selective COX inhibitor?
Inhibits mucous secretion; can cause GI ulcers.
How is COX-1 expressed? Where is it expressed? What are its 2 general roles? What are its 2 specific functions?
1. Constitutively expressed
2. Expressed everywere
3. Has role in protection/maintenance
4. GI cytoprotection; platelet aggregation
How is COX-2 expressed? Where is it expressed? What are its 2 general roles? What are its 2 specific functions?
1. Induced expression
2. Expressed in inflammed tissue
3. Proinflammatory/mitogenic
4. Inflammation, carcinogenesis
Would you want to inhibit COX-1 or COX-2 to get only the desirable effects of the COX pathway?
You'd want to inhibit COX-2.
What is celecoxib?
It is a selective COX-2 inhibitor.
What mechanism was used to produce a selective COX-2 inhibitor (mechanism)?
COX-2 enzyme is larger than COX-1, thus larger molecules that cannot reach the active site on COX-1 will be COX-2 selective inhibitors.
What's the 2 advantages of having a COX-2 selective inhibitor?
1. Maximize anti-inflammatory function
2. Minimize anti-mucous function (decreasing ulcer activity)
What is the mechanism by which COX-2 inhibitor Vioxx may have been causing heart attacks?
Favoring platelet aggregation by inhibiting COX-2 without inhibiting COX-1.
What is net effect on platelets from non-selective COX inhibitor ASA (aspirin)?
Net effect is anti-platelet. PGI2 acts as a "check" on platelet aggregation and is inhibited when COX2 is inhibited.
Why does ASA (aspirin) have a net anti-platelet effect?
The effects of inhibiting COX-1 and COX-2 (with regard to platelet aggregation) do not nullify each other. TxA2 induces platelet aggregation and PGI2 acts as a "check" on excessive platelet aggregation. Result when both are inhibited is a net decrease in aggregation.
Why does platelet inhibition last for 8-10 days?
Because COX-1 inhibition is irreversible so platelet aggregation is inhibited for lifetime of the platelet (i.e. 8-10 days).
What is Latanaprost? What does it do? When is it used?
It is a prostaglandin analog (PGF2α analog) that decreases intraocular pressure. It is indicated in glaucoma.
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