pharmacological features, side effects and uses of aspirin (2011)
Describe mechanism of action, pharmacological features, side effects and uses of aspirin
(Aug, 2013)
Write short note on aspirin (2012)
Classify analgesics. Describe mechanism of action, pharmacological features, uses, side
effects and contraindications of morphine (Aug, 2015, 2013)
Classification of analgesic
Algesia (pain): - defined as unpleasant sensation, usually evoked by external or internal noxious
stimuli.
Analgesis: - are agents used to abolish algesia
They are divided into two types:
1. Nonopioid Analgesics (NSAIDs)
2. Narcotic Analgesics
Classification of nonsteroidal anti-inflammatory drugs (based on COX selectivity)
Nonselective Irreversible Inhibitors of COX: Aspirin
Nonselective Reversible Inhibitors of COX: Ibuprofen, Diclofenac
Preferential COX-2 Inhibitors (10 to 20 fold COX-2 selective): Meloxicam, Etodolac,
Nabumetone
Selective COX-2 Inhibitors (> 50 fold COX-2 selective): Rofecoxib, Celecoxib,
Valdecoxib, Etoricoxib
COX-3 Inhibitors (?): Paracetamol
Weak Inhibitors of COX-1 & COX-2 + Other MOA (5 to 10 fold COX-2 selective):
Nimesulide
NSAIDs which do not inhibit COX: Nefopam
, Aspirin
Nonselective Irreversible Inhibitors of COX
Mechanism of action
Prostaglandins, prostacyclin (PGI2) and thromboxane A2 (TXA2) are produced from
arachidoic acid by the enzyme cyclooxygenase which exist in a constitutive (COX – 1)
and an inducible (COX-2) Isoforms.
COX-2 normally present in minute quantities, is induced by cytokines and other signal
molecules at the sites of inflammation leading to the generation of PGs locally which
mediate many of the inflammatory changes and produce pain.
Aspirin inhibits COX irreversibly by acetylating one of its serine residues.