ِ ق َوال تَ ْعَجلْ بِا ْلقُ ْر ِ آن ح ل ا ك فَتَ َعالَى اللَّهُ ا ْل َمل ُ ْ َ ُّ ِ ِ ِ َ ك َو ْحيُهُ َوقُلْ َرب ي ل إ ى ض ق ي ن أ ل ب ق ن م ْ َْ ْ ُ ْ َ َ ْ َ ِ دنِي ِعْلما ز ْ صدق هلل العلي العظيم سورة طه االيه 114 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 Phospholipids Phospholipase A2 Arachidonic Acid Lipoxygenase Leukotrienes COX-1 (Constitutive) COX-2 (Inducible) Inflammation, Swelling, Pain Stomach Intestine Kidney Platelets 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) Thank you