NSAIDs Pharmacology

Question 1

PGI2

Production and synthesis

Answer 1

Produced in vascular endothelial cells from 
prostaglandin H2 (PGH2) by action of enzyme 
prostacyclin synthase

Synthesis of prostacyclin resumes within 6 hours after
administration of aspirin (vs tromboxane)

Question 2

PGI2

Functions

Answer 2

Inhibits platelet activation – (prevents platelet plug formation)

Vasodilation

Increases local blood flow

Ensure cardiovascular homeostasis with
thromboxane A2 in relation to vascular damage
(Physiological antagonism)

Cardioprotective

Question 3

TXA2

Production and duration

Answer 3

Produced from prostaglandin H2 by thromboxane-A (TXA) synthase in activated platelets and has prothrombotic properties

Short duration of action (30s) and broken down to inactive Thromboxane B2

Question 4

TXA2

Function

Answer 4

Stimulates activation of new platelets

Increases platelet aggregation.

Vasoconstriction (Implicated in angina)

Question 5

PGD2

Production and location

Answer 5

Major prostaglandin produced by mast cells

Large amounts of PGD2 are found only in the brain and in mast cells

Question 6

PGD2

Functions

Answer 6

Contraction of bronchial airways (development of allergic diseases such as asthma)

Regulation of reducing body temperature in sleep, and acts opposite to PGE2

Primary mediator of vasodilation (the “niacin flush”) after ingestion of niacin (nicotinic acid).

Implicated in balding of scalp tissue (Male pattern baldness)

Question 7

PGE2

Pharmaceutical name

Answer 7

Dinoprostone

Question 8

PGE2 Functions

Answer 8

Increase local blood flow

Prostaglandin which ultimately induces fever in response to bacterial pyrogens**

Direct vasodilatory actions

Inhibits release of noradrenaline from sympathetic nerve terminals

Softens cervix and causes uterine contractions

Stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts

Stimulates gastric mucosa formation

Question 9

COX

Terminology

Answer 9

COX = PTGS

Prostaglandin endoperoxide synthase

Question 10

Salicylic acid derivatives

Answer 10

Aspirin

Question 11

Enolic acid derivatives

Answer 11

Piroxicam
Lornoxicam
Meloxicam
Phenylbutazone

Question 12

Propionic acid derivatives

Answer 12

Naproxen
Ibuprofen
Ketoprofen

Question 13

Acetic acid derivatives

Answer 13

Indomethacin
Diclofenac
Ketorolac

Question 14

Para-amino phenol derivatives

Answer 14

Paracetamol

Question 15

Fenamates

Answer 15

Mefenamic acid

Question 16

Diaryl heterocyclic compounds

Answer 16

Coxibs

Question 17

COX 1 inhibitors

Answer 17

Diclofenac
Indomethacin
Naproxen
Ibuprofen
Piroxicam
Ketoprofen
Lornoxicam
Aspirin

Question 18

COX 2 INHIBITORS/COXIBs

Answer 18

Meloxicam
Etoricoxib
Celecoxib
Parecoxib

Question 19

COX 3 Inhibitors

Answer 19

Paracetamol