Non steroidal Antiinflammatory Drugs (NSAIDs)

Pharmacist Dr.Dilan Zakaria H.

Non steroidal anti-inflammatory drugs

Non steroidal anti-inflammatory drugs (NSAIDs) are medications used to relieve pain and reduce inflammation. They are one of the most commonly used medications.

Pharmacological Effects
Analgesic (CNS and peripheral effect) may involve non-PG related effects Antipyretic (CNS effect) Anti-inflammatory due mainly to PG inhibition Pain relief starts soon after taking the first dose and a full analgesic effect should normally be obtained within a week, whereas an Anti-inflammatory effect may not be achieved for up to 3 weeks. Dental and orofacial pain Most mild to moderate dental pain and inflammation is effectively relieved by NSAIDs. Those used for dental pain include ibuprofen and diclofenac .

Choice Of NSAIDs
Differences in anti-inflammatory activity between NSAIDs are small, About 60% of patients will respond to any NSAID; NSAID should be chosen on the basis of the incidence of gastro-intestinal and other side effects There is no best NSAID for all patients

NSAIDs
Aspirin the prototype of the salicylates is employed for mild to moderate pain of
varied origin. Aspirin and other NSAIDs have been combined with opioid analgesics for treatment of cancer pain. High-dose is effective for treatment of rheumatic fever, rheumatoid arthritis, and other inflammatory joint conditions. Aspirin decreases the incidence of transient ischemic attacks, unstable angina, coronary artery thrombosis with myocardial infarction, and thrombosis after coronary artery bypass grafting Epidemiologic studies suggest that long-term use of aspirin at low dosage is associated with a lower incidence of colon cancer, possibly related to its COXinhibiting effects.

NSAIDs
Ibuprofen has anti inflammatory, analgesic, and antipyretic properties. It
has fewer side-effects than other non-selective NSAIDs but its antiinflammatory properties are weaker. The concomitant administration of ibuprofen antagonizes the irreversible platelet inhibition induced by aspirin. Thus, treatment with ibuprofen in patients with increased cardiovascular risk may limit the cardioprotective effects of aspirin.

Naproxen is one of the first choices because it combines good efficacy

with a low incidence of side-effects (but more than ibuprofen)

Indomethacin has an action equal to or superior to that of naproxen,

but with a high incidence of side-effects including headache, dizziness, and gastro-intestinal disturbances

NSAIDs

Mefenamic acid has minor anti-inflammatory properties. It has

occasionally been associated with diarrhea and hemolytic anemia which require discontinuation of treatment. Mefenamic acid is probably less effective than aspirin as an anti-inflammatory agent and is clearly more toxic. It should not be used for longer than 1 week and should not be given to children , It is rarely used today. Diclofenac is relatively nonselective as a COX inhibitor. Adverse effects occur in approximately 20% of patients and include gastrointestinal distress, occult gastrointestinal bleeding, and gastric ulceration. Diclofenac at a dosage of 150 mg/d appears to impair renal blood flow and glomerular filtration rate. Elevation of serum aminotransferases may occur more commonly with this drug than with other NSAIDs.

NSAIDs Diclofenac continue . . . . . . . A 0.1% ophthalmic preparation is recommended for prevention of postoperative ophthalmic inflammation and can be used after intraocular lens implantation . A topical gel containing 3% diclofenac is effective for solar keratoses. Diclofenac in rectal suppository form can be considered a drug of choice for preemptive analgesia . In Europe, diclofenac is also available as an oral mouthwash .

COX Inhibitors
The selective inhibitors of cyclo-oxygenase-2, etoricoxib and celecoxib, are as effective as non-selective NSAIDs such as diclofenac and naproxen. Short-term data indicate that the risk of serious upper gastro-intestinal events is lower with selective inhibitors compared to non-selective NSAIDs. Cyclo-oxygenase-2 selective inhibitors are associated with an increased risk of thrombotic events (e.g. myocardial infarction and stroke) and should not be used in preference to non-selective NSAIDs except when specifically indicated (i.e. for patients at a particularly high risk of developing gastroduodenal ulceration or bleeding) and after assessing their cardiovascular risk. Celecoxib and etoricoxib are licensed for the relief of pain in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis; etoricoxib is also licensed for the relief of pain from acute gout.

Common adverse Effects

Gastritis and peptic ulceration with bleeding Acute Renal Failure in susceptible Sodium + water retention and edema Prolongation of gestation and inhibition of labor Hypersenstivity (not immunologic but due to PG inhibition )

NSAIDs
In patients not at high risk for cardiac events who are undergosing a noncardiac procedure, it is recommended that aspirin and aspirin-containing medications be stopped seven to 10 days before surgery. Nonaspirin, nonselective NSAIDs (and probably COXIBs) should be discontinued five half-lives before surgery.60 A list of these medications appears in TABLE

NSAIDs
Owing to the increased susceptibility of the elderly to the side-effects of NSAIDs the following recommendations are made: for osteoarthritis, soft-tissue lesions, and back pain, first try measures such as weight reduction (if obese), warmth, exercise, and use of a walking stick; for osteoarthritis, soft-tissue lesions, back pain, and pain in rheumatoid arthritis, paracetamol should be used first and can often provide adequate pain relief; alternatively, a low-dose NSAID (e.g. ibuprofen up to 1.2 g daily) may be given; for pain relief when either drug is inadequate, paracetamol in a full dose plus a low-dose NSAID may be given; if necessary, the NSAID dose can be increased or an opioid analgesic given with paracetamol; do not give two NSAIDs at the same time.

Thank You