18 Questions
What is the brand name for Methyl Salicylate?
Salonpas
Which medication is classified as a Phenylbutazone derivative?
Butazolidin
What is the generic name for Pepto Bismol?
Bismuth Subsalicylate
Which drug is a Selective COX-2 Inhibitor?
Celebrex
What is the brand name for Paracetamol?
Tylenol
Which medication was withdrawn due to safety concerns?
Valdecoxib
What is the primary reason why NSAIDs are contraindicated for people with hypertension?
Increase in blood volume
What is a common risk factor that contributes to NSAID-induced gastrointestinal ulceration?
Concurrent use of steroids
Which NSAID has a long-half life of 50 hours and a higher risk for peptic ulcer disease?
Piroxicam (Feldene)
Why are aspirin and tolmetin contraindicated in individuals with gout?
They increase serum urate levels
What is the mechanism of action of opioids?
Activation of opioid receptors to reduce cAMP concentration
Which NSAID category includes Bismuth subsalicylate, which is used for peptic ulcer disease?
Salicylates
Which NSAID was withdrawn from the market due to bone marrow suppression and Steven-Johnson syndrome?
Rofecoxib (Vioxx)
What is the primary effect of NSAIDs on vasodilation during inflammatory processes?
Increase in vasodilation
Which category of NSAID includes Paracetamol (Tylenol) as a weak anti-inflammatory agent?
Para-aminophenols
What is the primary mechanism through which NSAIDs induce gastrointestinal ulceration?
Inhibition of COX-1 and PGE production
Which NSAID has the advantage of lesser risk for NSAID-induced peptic ulcer disease but a disadvantage of acute thrombotic events like stroke and myocardial infarction?
Celecoxib (Celebrex)
What is the major pathway of metabolism for Paracetamol (Tylenol)?
Sulfation and glucuronidation
Study Notes
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)
- A sharp decline in fever within 24 hours directs the workup away from infection and suggests a neoplastic disorder
- Tolmetin (Tolectin ®) is contraindicated in patients with gout
- Pyrazolone derivatives include phenylbutazone (Butazolidine ®) and oxiphenbutazone
Categories of NSAIDs
- Non-Selective COX Inhibitors:
- Salicylates: methyl salicylate (Salonpas ®), bismuth subsalicylate (Pepto-bismol ®)
- Indole derivatives: indomethacin (Indocin ®)
- Oxicam derivatives: piroxicam (Feldene ®)
- Phenylacetic acid derivatives: diclofenac (Voltaren ®)
- Pyrolealkanoic acid derivatives: tolmetin (Tolectin ®)
- Selective COX-2 Inhibitors:
- Oxicam derivatives: meloxicam (Mobic ®)
- Phenylacetic acid derivatives: etodolac (Lodine ®)
- Coxibs: celecoxib (Celebrex ®), etoricoxib (Arcoxia ®)
Mechanism of Action of NSAIDs
- Inhibit COX, leading to decreased PGE production
- Non-selective COX inhibitors inhibit both COX-1 and COX-2
- Selective COX-2 inhibitors inhibit only COX-2
Side Effects and Adverse Effects of NSAIDs
- Gastrointestinal ulceration (inhibition of COX-1, PGE production)
- Sodium and water retention (inhibition of PG-induced inhibition of renal chloride reabsorption)
- Reversible inhibition of GFR
- Nephrotoxic effects
- Hypersensitivity reactions (asthma-induced allergy)
Paracetamol (Acetaminophen)
- Has analgesic and antipyretic activity, but weak anti-inflammatory activity
- Mechanism of action: weak peripheral inhibitor of COX at peripheral circulation
- Metabolism: major pathway is sulfation and glucuronidation; minor pathway is GSH conjugation
- Toxic metabolite: N-acetyl para-benzoquinone imine
- Non-toxic metabolite: mercapturic acid
- Maximum dose: 4000mg or 8 tablets
Test your knowledge on NSAIDs with questions about their indications, contraindications, and adverse effects. Learn about specific NSAIDs such as Tolmetin, Phenybutazone, and Piroxicam.
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