Pharmacology Weeks 7-8

Question 1

COX-1 vs COX-2

Answer 1

expn: 1. constitiutive // 2. inducible
loc: 1. everywhere// 2 mostly inflamed tissue
role: 1. protection, maintenance (GI cytoprotection, platelet aggregation) // 2. mitogenic, pro-inflammatory

Question 2

autocoid

Answer 2

rapidly synthesized, acts locally, acts quickly, rapidly degraded

Question 3

Liposygenase pathway of Arachadonic Acid casacade produces…

Answer 3

leukotrienes (and lipoxins, but not important for pharm)
-cysteinyl leukotrienes (LTC4, LTD4, LTE4, LTF4) bind to LT1 receptors –> vasoconstriction, bronchoconstict, inflammation

Question 4

cyclooxygenase (COX) pathways of Arachadonic Acid cascade produces…

Answer 4

• prostaglandins (PG): inflammation, pain, vasodilate, mucous production…
• Thromboxane A2 (TxA2): platelet aggregation, vasoconstrict
• Prostacyclin (PGI2): platelet inhibition, vasodilation

Question 5

ASA

Answer 5

acetyslicylic acid/asprin

• non-selective COX inhibitor; competes with arachidonic acid for active site binding
• irreversible inhibitor

Question 6

Celecoxib

Answer 6

COX-2 selective inhibitor (-coxib)

-larger molecule can’t access COX-1 active site

Question 7

COX inhibitor antiplatelet effects

Answer 7

PGI2 relies more on COX-2, so only non-selective inhibitors will have antiplatelet effect

Question 8

Ibuprofane

Answer 8

s

Question 9

Latanaprost

Answer 9

• prostaglandin analogue (antagonist)
• decreases intraocular pressure in glaucoma
• prost- = PG analogue

Question 10

montelukast

Answer 10

LTR antagonist

• treatment of athsma: oral!
• blocks bronchoconstriction

Question 11

Pharm management of T2D

Answer 11

• sulfonylureas:close K+ channels = insulin release
• biguanides: insulin sensitizer; MOA unknown, suppress glucose outpout
• alpha-glucosidase inhibitors: stop starch breakdown (causes bloating)
• thiazolidinediones: metabolic enzymes targeted
• incretin therapy (DPP-4 inhibitors): increase GLP-1