NSAIDS

Question 1

what are the large and chemically diverse group of drugs with the following properties?

Answer 1

analgesic
anti-inflammatory
anti-pyretic

Question 2

what does the activation of the arachidonic acid (AA) pathway cause?

Answer 2

pain
headache
fever
inflammation

Question 3

why is analgesia used as a treatment of headache and pain?

Answer 3

because it blocks the undesirable effects of prostaglandins which cause headaches

Question 4

what do we use Antipyretics for?

Answer 4

to reduce fever

Question 5

how do anti-pyretics reduce fever?

Answer 5

they Inhibit prostaglandin E2 within the area of the brain that controls temperature

Question 6

how do NSAIDS relief inflammation ?

Answer 6

• they inhibit leukotriene pathway
• they inhibit prostaglandin pathway
• they inhibit both

Question 7

what is the function of the AA pathway ?

Answer 7

to extract small parts of the cell membrane and produce products like leukotrienes, prostaglandins, prostacyclin, and thromboxane

Question 8

give examples of the products of the AA pathway

Answer 8

leukotrienes, prostaglandins, and thromboxane

Question 9

what THE STEROIDS inhibit

Answer 9

arachidonic acid -AA-

Question 10

the asprin and NSAIDS inhibit :

Answer 10

cyclooxygenase (prostaglandins , thromboxane)

cox1,cox2

Question 11

what is the enzyme that product AA

Answer 11

PHOSPHOLIPASE

Question 12

THE AA mechanism work in two way:

Answer 12

lipoxygenase that return aa to leukotrenes
-cyclooxygenase that return AA to prostaglandins and thromboxane
-

Question 13

what does thromboxane do in the body?

Answer 13

• vasoconstriction

- platelet aggregation

Question 14

what does the prostaglandins do in the body ??

Answer 14

vasodilation, fever and pain

Question 15

what do leukotrienes do in the body ?

Answer 15

vascular permeability

Question 16

Cox1 inhibitor action :

Answer 16

Supports renal and platelet function

Protect gastroduodenal mucus

Question 17

What is Cox 1 used for ?

Answer 17

Gastrointestinal toxicity,
renal toxicity,
Platelet impairment

Question 18

Cox 2 inhibitor action:

Answer 18

Immediate inflammation, pain and fever

Question 19

What is Cox 2 used as?

Answer 19

Anti-inflammatory
Anti-pyretic
Analgesic

Question 20

What do we use NSAID’s for ?

Answer 20

Arthritis
Muscular pain 
Headache
Toothache
Use with obioids to decrease the pain after giving dosage
Pain 
Edema
Vasoconstriction

Question 21

What are the adverse effects of NSAID’s

Answer 21

Diarrhea
Nausea
Vomiting
Gastric damage 
Skin reactions (rash) 
Rental reaction
Chronic nephritis
Renal papillary necrosis (renal hypertension)

Question 22

What are the 6 structurally related groups ? (Cox 1)

Answer 22

Acetic acids
Carboxylic acids
Propionic acids
Enolic acids 
Fenamic acids
Nonacidic compounds

Question 23

what are examples of acetic acid?

Answer 23

diclofenac potassium (Cataflam)
indomethacin (Indocin)
diclofenac sodium (Voltaren)

Question 24

examples of carboxylic acid:

Answer 24

Acetylated

• Aspirin (ASA) acetyl salicylic acid
• diflunisal (Dolobid)

Non-acetylated
-salicylamide (similar to aspirin but less harsh on the stomach)

Question 25

examples of propanoic acid:

Answer 25

Ibuprofen (Motrin, others)
ketorolac (Toradol)
naproxen (Naprosyn)

Question 26

examples of enolic acid

Answer 26

phenylbutazone (Butazolidin)

for treating arthritis

Question 27

examples of fanatic acid:

Answer 27

rarely used because it causes heart disease

Question 28

examples of cox 2 inhibitors

Answer 28

celecoxib (Celebrex)

Etorocoxib (Arcoxia).

Question 29

examples of non acidic compounds:

Answer 29

nabumetone (Relafen)

Question 30

can aspirin be given to children ?

Answer 30

No

Question 31

what is Non-aspirin salicylates?

Answer 31

ASA with magnesium or sodium

Question 32

what are the characteristics of Non-aspirin salicylates?

Answer 32

Cause less bleeding.
May not be as effective as aspirin.
Dimer of salicylic acid.
Absorbed primarily from lower intestine - less G.I. Irritation.

Question 33

how do salicylates work ?

Answer 33

block cyclooxygenase

Question 34

what are the Therapeutic effects of salicylates?

Answer 34

Analgesia.
Good for low intensity, somatic pain.
PGE1 sensitises pain receptors, salicylates decrease PG synthesis.