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Anti-inflammatory Drugs Part I: (NSAIDs)
Terms in this set (22)
main anti-inflammatory agents are
A. The Glucocorticoids
B. The Non-Steroidal Anti-Inflammatory Drugs (NSAIDs).
Features of NSAIDS
• Non narcotic, Non-opioid
• Weaker analgesic
• Do not depress CNS
• Do not produce physical dependence
• No abuse liability
• Analgesic, anti-pyretic and anti-inflammatory actions
Pharmacological Effects of NSAIDs(Analgesic)
- Refers to the relief of pain (for example, headache).
- Produce a mild degree of analgesia which is much less than the analgesia produced by opioid analgesics such as morphine.
Pharmacological Effects of NSAIDs(Anti-inflammatory)
These drugs are used to treat inflammatory diseases (rheumatoid disorders).
Pharmacological Effects of NSAIDs(Antipyretic)
- Reduce fever; lower elevated body temperature by their action on the hypothalamus.
Pharmacological Effects of NSAIDs(Antiplatelet)
Inhibit platelet aggregation, prolong bleeding time; have anticoagulant effects
The analgesic and antipyretic properties of NSAIDs
Reduce prostaglandins synthesis by
inhibiting cyclooxygenase (COX) enzyme in the periphery and centrally (CNS), thus decreasing the formation of pain mediators.
The anti-inflammatory properties of NSAIDs
Reduce Prostaglandins synthesis at the site of injury in the periphery.
(constitutive) acts in physiological conditions
(inducible) is induced in inflammatory cells by pathological stimulus.
Inhibition of it is responsible for their GIT toxicity.
nonselective for COX-1 and COX-2.
selective COX-2 inhibitors
-GIT side effects are decreased by ~50% and less renal problems.
Shared Toxicities of NSAIDs
1. Gastric mucosal damage
2. Bleeding: (All NSAIDS except COX-2 inhibitors)
3. Limitation of renal blood flow
4. Hypertension and cardiovascular problem(due to COX-2 inhibition)
4. Delay / prolongation of labour
5. Asthma and anaphylactoid reactions
have little or no anti-inflammatory action(has only analgesic and antipyretic p)
metabolized to salicylic acid, which is an irreversible inhibitor of COX.
Indication of Aspirin (acetylsalicylic acid)
- Analgesic, antipyretic and anti-inflammatory
- Antiplatelets: suppress platelet aggregation
• Due to inhibition of thromboxane A2 synthesis responsible for platelet aggregation.
Side effects of aspirin
• Gastrointestinal symptoms
• CNS toxicity
• Allergic reaction (urticaria, angioneurotic edema, aspirin asthma,
occasionally anaphylactic shock)
• Salicylate reaction (CNS reaction)
• Renal damage
• Hematologic effects
• Because low dose of aspirin decrease excretion of uric acid, it should not be used in gout.
** NSAIDS are category C and D in the last trimester of pregnancy.
can occur with repeated ingestion of fairly large doses of salicylate (dose >5g/day
• It is a syndrome consisting of tinnitus (a high-pitched buzzing noise in the ears), vertigo, decreased hearing and sometimes also nausea and vomiting.
-Rescure: i.v. NaHCO3
Aspirin, if given to children with febrile viral infections.
linked with an encephalitis (Reye's syndrome: liver and brain damage)
- Hepatic damage
Risk factors for NSAIDs GI toxicity
• Older age
• Rheumatoid arthritis
• History of peptic ulcer disease
• Higher dose NSAIDs.
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