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Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
Introduction
Non-steroidal anti-inflammatory drugs (NSAIDs) have been used widely to
treat pain and inflammation for many years. For the majority of patients, these
drugs are effective and well tolerated. However, their use is associated with a
risk gastrointestinal (GI) complications including mucosal erosion, bleeding,
ulceration or perforation, and rarely, renal complications.
Uses:
- relieve mild to moderate pain caused by: headach , toothache, pain after
surgery, sports injuries
- reduce inflammation.
- lower a high temperature.
- Aspirin is used to inhibit the clotting of blood and prevent strokes and heart
attacks
- anticancer agents.
- In veterinary medicine approved veterinary NSAIDs are used to control the
pain of osteoarthritis and postoperative in dogs.
- Pain relief in acute renal colic
- Chronic inflammatory disorders including
rheumatoid
osteoarthritis and chronic back pain .arthritis ,
Mechanism of action
Prostaglandins are produced within the body's cells by the enzyme
cyclooxygenase (COX). There are two COX enzymes, COX-1 and COX-2
Nonsteroidal antiinflammatory drugs (NSAIDs) block the COX enzymes and
reduce prostaglandins throughout the body. As a consequence, ongoing
inflammation, pain, and fever are reduced. Since the prostaglandins that
protect the stomach and support platelets and blood clotting also are reduced,
NSAIDs can cause ulcers in the stomach and promote bleeding.
Prostaglandins are a family of chemicals that are produced by the cells of
the body and have several important functions:
1 - promote inflammation, pain, and fever
2 - support the blood clotting function of platelets
3 - protect the lining of the stomach from the
damaging effects of acid.
Traditional NSAIDs
Aspirin
Ibuprofen (Motrin®, Advil®)
Ketoprofen (Orudis®)
Naproxen (Naprosyn®)
COX-2 Inhibitors
Celecoxib (Celebrex®)
Meloxicam (Mobic®)
Rofecoxib (Vioxx®)
Differences between NSAIDs:
 NSAIDs vary in their potency and duration of action
 COX-1 inhibitors cause ulcers and promote bleeding, more an NSAID
blocks COX-1 (e.g. aspirin is NSAID that inhibits the clotting of blood
for a prolonged period . Most NSAIDs inhibit the clotting of blood for
only a few hours.
 COX-2 inhibitors cause less bleeding and fewer ulcers than other
NSAIDs(e.g. Coxibs Celebrex)
 COX-1 activity promotes prostaglandins necessary to maintaining a
healthy gastric mucosa and platelet initiated clotting.
 COX-2 activity promotes prostaglandins mediating pain and
inflammation
How to take NSAIDs?
• mouth (orally) as tablets, capsules or liquid (You should take oral with
or after food or milk, will cause stomach problems).
•
injections
•
suppositories
• . creams and gels for joint or muscle pain.
•
NSAIDs for children a liquid (Suspension) form of ibuprofen,
containing 100mg of the medicine per 5ml, can be given to children
over three months old if they weigh at least 5kg (11 pounds). It may
also be given to
younger babies. Most other NSAIDs shouldn't be given to children under
12 years.
Cautions
• Asthma
• Are over 65 years
• Renal insufficiency
• Get indigestion or stomach or duodenal ulcer GI bleeding
• Pregnant or breastfeeding (but some NSAIDs e.g. ibuprofen, diclofenac ,
relatively safe as secreted in very small quantities
• CV disease or risk factors
• Hepatic and cardiac failure
•
Hypertension
• Concurrent use of drugs that increase risk of bleeding e.g .warfarin,
corticosteroids
Side-effects of NSAIDs
 The following side-effects, especially over 65. These include:
 indigestion
 heartburn
 feeling sick or vomiting
 diarrhoea
 bleeding and ulceration in the stomach
 Other, less common, side-effects of NSAIDs include:
 ankle swelling
 headache
 dizziness (vertigo)
 ringing in the ears (tinnitus)
 bleeding
Selecting a NSAID
 Differences between NSAIDs' anti-inflammatory activities are small systematic reviews have found no important differences in their efficacy
for the symptoms of musculo-skeletal disorders.
 Individuals vary in their response to a NSAID - where they fail to
respond to one NSAID, a switch to an alternative may produce a good
response .
 Differences in NSAIDs' tolerability are large. Non-selective NSAIDs
vary in their risk of GI toxicity.
Interactions of NSAIDs with other medicines
some NSAIDs increase the blood-thinning effects of a medicine called
warfarin, which is used for treating heart problems.
Names of common NSAIDs
Examples of the main types of NSAIDs are shown in the tables.
- diclofenac sodium
Voltarol Emugel, Pennsaid
- felbinac
Traxam
- ibuprofen
Ibuspray, Mentholatum
- ketoprofen
Oruvail,
- - piroxicam
Feldene P Gel
- aspirin
- celecoxib
Celebrex (COX-2)
- meloxicam
Mobic
- mefenamic acid
Ponstan
- rofecoxib (COX-2)