NSAIDS and Paracetamol

Question 1

What are NSAIDs?

Answer 1

Non-Steroidal Anti-Inflammatory Drugs
They basically inhibit inflammation by inhibiting the release of prostaglandins and inhibiting the function of COX-I and COX-II

Question 2

NSAIDS inhbit both COX-1 and COX-2 while COXIBS only inhibit COX-2.

Describe the functions of COX-1 and COX-2.

Answer 2

COX-1
Synthesis of housekeeping enzyme
Responsible for gastric cytoprotection
Platelet Aggregation (thrombus formation)
Uterine Contraction
Renal Function

COX-2
Induce Inflammation at the site of tissue injury.
Cardioprotective

Question 3

Describe the adverse reactions of NSAIDS

Answer 3

1. Hypersensitivity Reactions
2. Tinnitus
3. Prolonged bleeding time
4. Renal Vasoconstriction
5. GIT- Ulceration, Perforation, Bleeding.
6. In pregnancy, there’s prolonged gestation(development)

Question 4

Describe the Adverse Effects of COXIBS (COX-2 Selective Inhibitors)

Answer 4

A/E
1. Inhibition of PGI(2)
2. Myocardial Infarction, Stroke
3. (NB)Avoid COXIBS in Heart Failure
4. Renal Ischaemia

but then, advantage of COXIB is reduction on GIT side Effects.

Question 5

Describe the PK and Uses and MOA of ASPIRIN

Answer 5

PK-Never IV, Water Insoluble.

Uses
1. Analgesic
2. Anti-Inflammatory
3. Anti-Pyretic

MOA
Irreversibly inhibits COX 1 and 2
used to prevent platelet aggragation at LOW DOSE

Question 6

Classify Aspirin(as a drug not class)

Answer 6

ASPIRIN is a Non-Selective COX inhibitor

Question 7

Classify **Piroxicam

Answer 7

It is a non-selective COX inhibitor

Question 8

Classify Diclophenac and Indomethacin

Answer 8

They are both non-selective COX inhibitors

Question 9

Classify Ibuprofen, Flurbiprofen and Naproxen

Answer 9

They are all Non-Selective COX inhbitors under propionic acid derivatives

Question 10

Classify Mefenamic Acid

Answer 10

It is a Non-Selective COX inhbitor

Question 11

Describe all COX-2 selective Inhibitor agents

Answer 11

1. Celecoxib
2. Etoricoxib
3. Parecoxib

COXIB

Causes Steven Johnstone Syndrome(SJS)

Question 12

Describe Aspirin Side Effects

Answer 12

Contraindicated in Children-they cause *Rey’s Syndrome (use only in Juvenule Arthritis)

Not safe in Pregnancy(esp, third trimester)

Question 13

Aspirin dose related effects

What effects do you have with 80-160mg of Aspirin?

Answer 13

*Anti-platelet Effect

Question 14

What effect do you have with 650-975mg of Aspirin?

Answer 14

Analgesic and Antipyretic Effects

Question 15

What effects do you have with 3-6g of Aspirin?

Answer 15

Anti-Inflammatory effect and Tinnitus

Question 16

What effect do you get with 6 to 10 grams of Aspirin?

Answer 16

Hyperventilation and Respiratory Alkalosis

Question 17

What effects do you get with 10 to 20 grams of Aspirin?

Answer 17

1. Fever
2. Dehydration
3. Metabolic Acidosis

Question 18

What effects do you get with 20-30g of Aspirin?

Answer 18

1. Renal Failure
2. Shock
3. Coma
4. Respiratory Failure
5. DEATH

Question 19

Describe the Effects of Paracetamol

Answer 19

Antipyretic and Analgesic
It has no Anti-Inflammatory Effects

Question 20

Describe the Mech. of Action of Paracetamol

Answer 20

Inhibits COX 1 and 2 in the brain

Question 21

Describe the Contraindications, Effects of Acute Dosage and Treatment of dosage of Paracetamol

Answer 21

Contraindications–Hepatic Cirrhosis
Acute Overdosage(>10g)-results in Death. The cause of death would be from Hepatic Necrosis

Treat overdose with N-Acetylcysteine

Question 22

Generally describe the uses of NSAIDS and Paracetamol

Answer 22

1. Prevention-Colon Cancer
2. Closure of Ductus Arteriosus in Infants
3. Pain
4. Inflammatory diseases- Rheumatoid and Osteo-Arthrititis
5. Anti-Pyretic(do not use aspirin in children)

Question 23

Describe how you can prevent GIT problems with NSAIDS

Answer 23

1. Take with food
2. Combine NSAID with PG-E2.

Question 24

You must never ever combine TWO NSAIDS. Explain WHY

Answer 24

COmbination increases the risk of analgesic neuropathy