NSAIDS Flashcards
What does NSAID stand for?
Non-Steroidal Anti-Inflammatory Drugs
What are the primary indications for anti-inflammatory analgesic drugs?
- Rheumatoid arthritis
- Osteoarthritis
- Acute gouty arthritis
- Ankylosing spondylitis
- Dysmenorrhea
- Other inflammatory conditions
Name the three isoforms of COX enzymes.
- COX-1
- COX-2
- COX-3
What is the primary function of COX-1?
Housekeeping or homeostatic functions
What type of gastric injury is reported by 30-40% of NSAID users?
Gastric injury, including erosion, bleeding, or ulcer
List the common structural features of most NSAIDs.
- An acidic center
- Aromatic or heteroaromatic ring
- Additional center of lipophilicity (alkyl chain or another aromatic ring)
What is the pKa range for most NSAIDs?
3.0–5.0
What are salicylates derived from?
Derivatives of 2-hydroxybenzoic acid (salicylic acid)
What is the historical significance of salicylic acid?
Discovered in 1838 from willow bark
What is the common name for acetylsalicylic acid?
Aspirin
What are the characteristics of arylalkanoic acids?
Strong organic acids with a pKa of 3.0 – 5.0
What is the prototype member of the ‘Profens’ group?
Ibuprofen
What is the structure of phenylbutazone?
1-aryl-3,5-pyrazolidinedione
What is the mechanism of action for acetaminophen?
Inhibition of PGs at CNS (COX-3)
What are the potential dangers of acetaminophen overdose?
Hepatotoxic potentials leading to acute liver injury and death
What are the classes of drugs used for rheumatoid arthritis (RA)?
- NSAIDs
- Gold compounds
- Aminoquinolines
- Immunosuppressants
- Sulphasalazine
- Biological disease modifying antirheumatic drugs
What is the mechanism of action of gold compounds?
Inhibition of lysosomal enzymes (glucuronidase, acid phosphatase, collagenase and acid hydrolyase)
Name a biological disease modifying antirheumatic drug.
- Etanercept
- Infliximab
- Adalimumab
- Tocilizumab
- Abatacept
What is gout?
Increased levels of uric acid due to increased synthesis, decreased excretion, or both
What is the pKa range of uric acid?
5.7 and 10.3
What are the two methods to correct high uric acid levels?
- Inhibition of biosynthesis (xanthine oxidase inhibitor)
- Increasing excretion (uricosuric agents)
What is the mechanism of action for allopurinol?
Inhibit xanthine oxidase enzyme, preventing uric acid synthesis
Fill in the blank: Acetaminophen is also known as _______.
Paracetamol
True or False: Meloxicam is marketed as a selective COX-2 inhibitor.
True
What is the primary structure of anilides?
Simple acetamides of aniline, which may contain a 4-hydroxy or 4-alkoxy group
