Drugs Combating Acute Inflammation

Question 1

Two classes of drugs that can suppress prostaglandins

Answer 1

Steroidal anti inflammatory

Non steroidal anti inflammatory

Question 2

Example of steroidal and describe it

Answer 2

Corticosteroids
Very effective
Suppress pgs by production and preventing release of their precursor arachidonic acid from cell membrane phospholipid via inhibition of PLA2

Question 3

Describe non steroidal

Answer 3

Suppress pgs production by directly inhibiting their synthesis through cox enzyme system
Cox inhibitors

Question 4

What are NSAIDS used clinically for

Answer 4

▪️Anti inflammatory effect in diff types of inflammatory disorders such as arthritis,myositis
▪️Analgesic effect for mild to moderate painful conditions such as headache,toothache, rheumatic pain and dysmenorrhea
▪️Antipyretic effect to reduce body temp in case of fever

Question 5

What do most of the adverse effects of NSAIDs relate to

Answer 5

Inhibition of physiologically imp prostanoids (pgs,prodtacyclin, and thromboxane)
Also have cardiovascular hazards

Question 6

Give examples of reversible non selective cox inhibitors and explain

Answer 6

Ibuprofen,diclofenac
Differ in their affinity to cox1 and cox2
Have Variable analgesic, anti inflammatory activities as well as variable severity of their adverse actions

Question 7

Most effective analgesic but most gastric injurious agent

Answer 7

Ketorolac

Question 8

Most tolerable NSAID

Answer 8

Ibuprofen

Question 9

What is irreversible non selective cox inhibitor

Answer 9

Aspirin=acetyl salicylic acid
Low dose Inhibits only thromboxane(TXA2) synthesis in platelet
Anti platelet action for a life time
Main use: primary or secondary prophylaxis against thrombotic event in patients at risk
Ischemic cardiovascular or cerebrovascular diseases
High doses: rheumatic fever

Question 10

Adverse reactions in stomach

Answer 10

1-stomach: leading to gastric irritation,ulceration and bleeding
Acidic nature of some NSAIDs like aspirin contribute to gastric irritation therefore they are given with meals

Concomitant administration of proton pump inhibitors (drugs which inhibit gastric acid formation) can be used to provide prophylaxis against NSAIDs induced injury in patients with risk of peptic ulcer

Question 11

Adverse effects of kindey

Answer 11

Leading to analgesic nephropathy especially with prolonged use

Question 12

Adverse effects with hypersensitivity reactions

Answer 12

Blocking of cox inflammatory pathway leads to diversion of arachidonic acid pathway to lox pathway with further production of leukotrienes that may precipitate allergic reactions in form of bronchospasm, urticaria, angioedema in predisposed individuals

Question 13

Adverse effects of platelets

Answer 13

Leading to inc risk of bleeding or thrombosis according to drug used

Question 14

How to avoid systemic adverse effects

Answer 14

Topical formulations of drugs

Question 15

Give an example of selective cox inhibitors

Answer 15

Celecoxib
Less or minimal gastric injury
No anti platelet action
Lead to inc thrombotic risk by inhibiting endothelial PGI2 in favor of effect of platelet TXA2
Contraindicated in patients at cardiovascular risk of thrombosis ex: diabetic hypertensive patients

Question 16

What is paracetmol

Answer 16

Analgesic anti pyretic drug that lacks the anti inflammatory activity that is why it does not belong to NSAID group
Inhibits only the cox enzyme centrally and does not affect peripheral cox present elsewhere in body

Question 17

Properties of paractemol

Answer 17

Weak or no anti inflammatory activity
No effect on platelet aggregation
No gastric or renal injury

Question 18

When is paracetamol is preferably used

Answer 18

For fever or pain in absence of inflammation or in combination with NSAIDs in inflammatory disorders to decrease their doses and their adverse effects

Question 19

Max dose of paracetamol in adults

Answer 19

3-4 g daily