20)NSAIDs w/predominantly analgesic + antipyretic activity Flashcards
1
Q
NSAIDs w/predominantly analgesic + antipyretic activity
A
Aspirin, ibuprofen + paracetamol
- Most of these drugs inhibit synthesis of Prostaglandins ⇢ by inhibiting COZ enzymes near the site of injury
This question focuses on:
Analgesia ⇢ prevention of pain nerve ending sensitisation
Antipyresis ⇢ connected w/influence of thermoregulatory centre
2
Q
Classification
A
- Salicylic acid derivatives ⇢ Aspirin
- Analine derivatives ⇢ Paracetamol
- Propionic acid derivatives ⇢ Ibuprofen
3
Q
Mechanism of action
A
Analgesic activity
- Inhibition of prostaglandin synthesis
- Blocking of peripheral pain receptors
Antipyretic activity
- Inflammation = release of cytokines
- Cytokines ⇢ stimulate synthesis of prostaglandins in hypothalamus ⇢ ⇡ Body temperature
- Inhibition of prostaglandin production ⇢ hypothalamic thermostat is rested + heat is lost via sweating/vasodilation = ⇣ fever
4
Q
Pharmacokinetics - Aspirin
A
Administered orally
Aspirin
- Rapidly absorbed in GI tract
- Hydrolysed to salicylate
- ½ life = 20-30 minutes
5
Q
Pharmacokinetics - Paracetamol
A
- Well absorbed in small intestine
- Conjugated in liver
- Excreted in urine
- ½ life = approx 2 hours
6
Q
Pharmacokinetics - Ibuprofen
A
- Binds extensively to plasma proteins
- Metabolised in liver
- Excreted in urine
7
Q
Clinical uses
A
Aspirin
- Analgesic ⇢ headache, toothache, back pain
- Antipyretic ⇢ fever
Paracetamol
- Headache, myalgia + postpartum pain
In dentistry:
- Post-op pain
- Toothache ⇢ choline salicylate is active component in topical gel bonjela
- Paracetamol for treatment in teething
8
Q
Contraindication
A
Aspirin - dont give to those:
- Under 15
- Suffer from peptic ulcers
- Asthmatics
- Hypersensitivity history
9
Q
Side effects:
A
Aspirin has a high incidence of GI disturbances
Ulceration
Hypersensitivity issues
