NSAIDs

Question 0

2 negative effects of prostaglandin (an eicosanoid) synthesis inhibition?

Answer 0

Kidneys: Fluid retention ^Na+
Stomach: ^Acid, ¥Mucous –> Mucousal irritation

Question 1

Prostaglandins:
^Renal blood flow
Inhibition of PG’s lead to?
** Renal failure in Compromised patients & Athletes

Answer 1

• DECREASE GFR
• ^ BP (fluid & Na+ retention)
• ^ K+ (heart arrhythmias)
• Oedema

Question 2

1) NSAIDs: MOA?

2) How do NSAIDs work?

Answer 2

1) Inhibit CYCLOOXYGENASE (COX)
2) Inhibit formation of eicosanoids
(e. g Prostaglandins)

Question 3

NSAIDs:

1) Adverse effects from?
2) 3 most common ADR?

Answer 3

1) Inhibition of COX-1 & COX-2 synthesis
(non-selective) 
2) (peptic ulcer, nausea, & vomiting)
- Epigastric distress 
- Microscopic bleeding (~ALL w/ aspirin)
- Renal Impairment

Question 4

1) COX-1 located? Inhibition causes?

2) COX-2 located? Inhibition causes?

Answer 4

1) COX-1 present in most tissues
Inhibition causes ADVERSE EFFECTS
2) COX-2 @ site of inflammation
Inhibition: Analgesic & Anti-inflam. effects
(NSAIDs --> COX -//-> Prostanoids)

Question 5

Selective COX-2 inhibitor ISSUES:
Coxibs: Patients can develop?
^Risk heart attack
Healing peptic ulcers?

Answer 5

• SIGNIFICANT GASTRO
  Duodenal ulcer & Bleeding
• Decrease PGF2 –> Decrease protective anticoagulative effect
• Slowed down

Question 6

1) NSAIDs: 3 common therapeutic properties? (Vary in strength of effects)
2) NSAIDs most effective when?

Answer 6

1) Analgesia / Anti-inflammatory / Anti-pyretic
2) Presence of inflammatory component
(Arthritis, muscle pain)

Question 7

1) Antipyretic action: NSAIDs inhibit what?

2) NSAIDs do not decrease temp in what?

Answer 7

1) PGE production

2) Heat stroke

Question 8

1) Aspirin: Action?
2) Used after ____ to prevent ____.
3) 2 other actions besides antiplatelet?
Treatment in?

Answer 8

1) PLATELET AGGREGATION - ANTIPLATELET
[˅ thromboxane (TXA2) synthesis]
2) MI ; Transient ischaemic attack (minor stroke)
3) Analgesic & Antipyretic
--> Rheumatic fever & RA

Question 9

1) Aspirin side effect?
2) Aspirin before surgery?
3) If taking salicylates (e.g. Aspirin)?

Answer 9

1) ^ Bleeding time
2) Do not take aspirin AT LEAST 1 WEEK before surgery.
3) DECREASE Anticoagulant dosage
(Salicylates inhibit PG synthesis)

Question 10

Aspirin:

1) For ____, but ^____ effects.
2) How to minimise GI disturbances?
3) ADR common in?

Answer 10

1) Mild pain; ^ GI effects
2) Take w/ Food & ^Fluids
3) Elderly & chronic users

Question 11

Aspirin causes IRREVERSIBLE inhibition by +Acetyl group (Acetylating; covalent bonding) to?

Answer 11

COX @ SERINE 530 (amino acid)

Question 12

1) How is low dosage aspirin eliminated?

2) How is anti-inflammatory dosages of Aspirin eliminated?

Answer 12

1) <600mg/day (low dosage)
First-order kinetics
2) 4g/day (anti-inflammatory dosage)
Zero-order kinetics

Question 13

Aspirin, ibuprofen, paracetamol: reversible/irreversible inhibition?

Answer 13

Irreversible: Aspirin
Reversible: Ibuprofen, Paracetamol

Question 14

1) Ibuprofen: well tolerated & effective pain relief e.g.?

2) Drug of choice for _____ because?

Answer 14

1) Dysmenorrhoea
(excessive menstrual pain)
2) INFLAMMATORY joint disease ;
Low incidence side effects

Question 15

Paracetamol:

1) Used as?
2) Toxic?
3) Treatment?

Answer 15

1) Antipyretic & Analgesia ONLY
2) FATAL HEPATOTXICITY >2-3 X Therapeutic dose
3) N-acetyl cysteine

Question 16

PIROXICAM: (potent drug)

1) Used for?
2) Dose?
3) Adverse?

Answer 16

1) Chronic inflammatory conditions
(arthritis, gout, ankylosing sponditis)
2) 20mg PO ONCE DAILY (T1/2 50hrs)
3) ^ GI Problems

Question 17

1) Actions on GIT:
Aspirin causes decrease PG’s resulting in?
Which causes what?
2) Stop use of Aspirin when?

Answer 17

In stomach:
^ Gastric acid secretion; ˅ Mucus levels
= MUCOSAL IRRITATION

2) Signs of RENAL IMPAIRMENT
(can cause Acute reversible renal impairment)

Question 18

Aspirin Hypersensitivity: S/S:

• Bronchoconstriction
  1) Urticaria (wheals)?
  2) Angiooedema?
  3) Fatal anaphylactic shock?

Answer 18

1) Red elevated patches (wheals) w/ severe itching
2) Acute swelling (subcut oedema): Face, neck, larynx, viscera (soft internal organs of the body)
3) Rare

Question 19

REYE’S SYNDROME:

1) Associated with?
2) Occurs in?
3) Often fatal. S/S?

Answer 19

1) Aspirin given during viral infections
2) CHILDREN, young teens
(treat w/ Paracetamol Not aspirin)
3) Sudden severe HEPATITIS (liver inflam)
Cerebral oedema (Brain swelling); Confusion; Coma