Anti-inflammatory and Anti gout PDF

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Anti-inflammatory & Antigout Drugs Inflammation • Localized protective response stimulated by injury to tissues • Classic signs & symptoms: • Pain, fever, loss of function, redness, and swelling • Endogenous compounds, including proteins of the complement system, histamine, serotonin, bradykinin, leukotrienes, and prostaglandins

NSAIDs • • •

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One of the most commonly prescribed drugs in Canada A large and chemically diverse group of drugs that have/are used for their: Aspirin- additionally has antiplatelet effects Aspirin o Shown to reduce cardiac death after myocardial infarction (MI) o Should be administered at the first sign of MI o If aspirin is not given before the patient arrives at the emergency department, it is one of the first drugs given if there are no contraindications. Uses of NSAIDs o Relief of mild to moderate headaches o Relief of myalgia o Relief of neuralgia o Relief of arthralgia o Relief of postoperative pain o Relief of pain associated with arthritic disorders • such as rheumatoid arthritis, juvenile arthritis, ankylosing spondylitis, and osteoarthritis o Treatment of gout and hyperuricemia

Categories of NSAIDs Salicylates • Aspirin • Diflunisal Acetic Acid Derivatives • Diclofenac sodium (Voltaren) • Indomethacin sufindac

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Etodolac Ketorolac (Toradol) Mefenamic acid (Ponstan)

Cyclo-oxygenase (COX)-2 inhibitors • Celecoxib (Celebrex) Enolic acid derivatives • Nubumetone • Meloxicam • Piroxicam Propionic acid derivatives • Flurbiprophen • Ibuprophen (Motrin, Advil) • Ketoprophen (Apo-Keto-E) • Naxproxen (Naprolen, Naprosyn, Aleve) • Oxaprozin tiaprofenic acid Mechanism of Action • Inhibition of the leukotriene pathway, the prostaglandin pathway, or both • Blocking the chemical activity of the enzyme COX o COX-1 has a role in maintaining the gastrointestinal (GI) mucosa. o COX-2 promotes synthesis of prostaglandins involved in the inflammatory process. • aspirin o Irreversible inhibitor of COX-1 receptors within the platelets themselves o Reduced formation of thromboxane A2 o Other NSAIDs lack these antiplatelet effects. Contr Contraindica aindica aindications tions • Known drug allergy • Conditions that place the patient at risk for bleeding o Rhinitis o Vitamin K deficiency o Peptic ulcer disease • Patient currently experiencing hemorrhagic stroke • Not recommended for breastfeeding women • Can pass through breastmilk Adver Adverse se EEfffects • Heartburn to severe GI bleeding • Dyspepsia, heartburn, epigastric distress, nausea, vomiting, anorexia, abdominal pain • GI bleeding*

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• Mucosal lesions* (erosions or ulcerations) Acute kidney injury Cardiovascular - Noncardiogenic pulmonary edema Altered hemostasis Hepatotoxicity Skin eruption, sensitivity reaction Tinnitus (ringing in the ears), hearing loss

misopros misoprostol tol • Drug can be given with NSAIDS to reduce side effects • A synthetic prostaglandin E1 analogue: • inhibits gastric acid secretion and has a cytoprotective component • Helps to prevent GI bleeds • Mechanism of action: unclear • Not generally used in women of childbearing age NSAIDs and Kidney Function • Kidney function depends partly on prostaglandins. • Disruption of prostaglandin function by NSAIDs is sometimes strong enough to precipitate acute or chronic kidney injury or failure. • Use of NSAIDs can compromise existing kidney function. • Kidney toxicity can occur in patients with dehydration, heart failure, or liver dysfunction, or with the use of diuretics or angiotensin-converting enzyme inhibitors. NSAIDs: Health Canada W Warning arning • All NSAIDs (except aspirin) share a Health Canada warning regarding an increased risk of adverse cardiovascular thrombotic events, including fatal MI and stroke. • NSAIDs cause an increased risk of serious GI adverse events • Older adults are at greater risk.

Salicylates • • • •

acetylsalicylic acid (aspirin) the most common Oral (tablets, capsules), topical cream (Aspercreme®), oral liquids, rectal suppositories aspirin–antacid combinations (Alka-Seltzer®) Enteric-coated aspirin (Praxis ASA EC®)

aspirin • Daily tablet (81 mg or 325 mg): prophylactic therapy for adults who have strong risk factors for developing coronary artery disease or cardiovascular accident • Effective after MI • The 81- and 325-mg strengths appear to be equally beneficial for the prevention of thrombotic events. aspirin: Uses • Headache, neuralgia, myalgia, and arthralgia • Pain syndromes resulting from inflammation: arthritis, pleurisy, and pericarditis • Systemic lupus erythematosus: antirheumatic effects • Antipyretic action aspirin: Re Reye’ ye’ ye’ss Syndrome • Acute and potentially life-threatening condition involving progressive neurological deficits that can lead to coma and may also involve liver damage • Triggered by viral illnesses such as influenza, as well as by salicylate therapy itself in the presence of a viral illness. • Survivors of this condition may or may not have permanent neurological damage.

Salicylate intoxication (when chronic, known as salicylism) • Increased heart rate • Tinnitus, hearing loss, dimness of vision, headache, dizziness, mental confusion, drowsiness • Nausea, vomiting, diarrhea • Sweating, thirst, hyperventilation, hypoglycemia or hyperglycemia

Acetic Acid Derivatives indomethacin • Analgesic, anti-inflammatory, antirheumatic, and antipyretic properties • Uses: therapy for rheumatoid arthritis (RA), osteoarthritis (OA), acute bursitis or tendonitis, ankylosing spondylitis, acute gouty arthritis • Oral and rectal routes ketorolac tromethamine (Toradol) • Some anti-inflammatory activity • Used primarily for its powerful analgesic effects, which are comparable to those of narcotic drugs such as morphine sulphate • Indication: short-term use (up to 5 to 7 days) to manage moderate to severe acute pain • Adverse effects: kidney impairment, edema, GI pain, dyspepsia, and nausea

Propionic Acid Derivatives ibuprofen (Motrin, Advil) • Most commonly used NSAID • Common uses as analgesic in the management of: o Rheumatoid Arthritis, Osteoarthritis o primary dysmenorrhea o dental pain o musculoskeletal disorders • antipyretic actions naproxen • Second most commonly used NSAID • Somewhat better adverse effect profile than ibuprofen • Fewer drug interactions with angiotensin-converting enzyme inhibitors given for hypertension

Cyclo-oxygenase (COX)-2 inhibitors celecoxib (Celebrex®) • First and only remaining COX-2 inhibitor • Indicated for OA, RA, acute pain symptoms, ankylosing spondylitis, and primary dysmenorrhea • Adverse effects include headache, sinus irritation, diarrhea, fatigue, dizziness, lowerextremity edema, and hypertension • Little effect on platelet function • Not to be used in patients with known sulpha allergy

Enolic Acid derivatives • •

Used to treat mild to moderate OA, RA, and gouty arthritis nabumetone is better tolerated in terms of GI adverse events than are some other NSAIDs.

NSAIDs: Inter Interactions actions Serious interactions can occur when given with: • Alcohol • Anticoagulants • acetylsalicylic acid (ASA) • Biphosphonates • Corticosteroids and other ulcerogenic medications • Protein-bound drugs • Diuretics and angiotensin-converting enzyme inhibitors • Other drugs

Gout •

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A condition that results from inappropriate uric acid metabolism o Underexcretion of uric acid o Overproduction of uric acid Uric acid crystals are deposited in tissues and joints, resulting in pain Hyperuricemia

Antigout Drugs • • • • • •

NSAIDS are considered first-line therapy for most patients allopurinol (Zyloprim®) febuxostat (Uloric®) colchicine probenecid (Benuryl®) sulfinpyrazone

Indications allopurinol (Zyloprim) • Used to prevent uric acid production and to prevent acute tumour lysis syndrome • Severe adverse effects: exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis

probenecid (Benuryl) • Inhibits the reabsorption of uric acid in the kidneys and thus increases the excretion of uric acid colchicine • Oldest available therapy for gout o Considered second-line therapy (after NSAIDs) • Reduces the inflammatory response to the deposits of urate crystals in joint tissue • Powerful inhibitor of cell mitosis, and can cause short-term leukopenia • Prophylaxis of acute attacks in dosages of 0.6 mg once or twice a day

Herbal Products: Glucosamine and Chondroitin • Used to treat the pain of OA Adverse effects: Glucosamine: • GI discomfort • Drowsiness, headache, skin reactions Chondroitin: • GI discomfort (normally well tolerated) Drug interactions • Enhance the effects of warfarin • Glucosamine may increase insulin resistance

Nursing Implications: Antigout Drugs •

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Before beginning therapy, observe for and assess conditions that may be contraindications to therapy, especially, o GI lesions or peptic ulcer disease. o bleeding disorders. Observe for and assess conditions that require cautious use. Perform laboratory studies as indicated (cardiac, kidney, and liver function studies; complete blood count; platelet count). Perform a medication history to assess potential drug interactions. Do not give salicylates to children and teenagers because of the risk of Reye’s syndrome. Because these medications generally cause GI distress, they are often better tolerated if taken with food, milk, or an antacid to avoid irritation. Explain to patients that therapeutic effects may not be seen for 1 week or more. Educate patients about the various adverse effects of NSAIDs, and instruct them to notify their prescribers if these effects become severe or if bleeding or GI pain occurs. Instruct patients to watch closely for the occurrence of any unusual bleeding, such as in the stool. Advise patients that enteric-coated tablets should not be crushed or chewed. Monitor therapeutic effects, which vary according to the condition being treated. o Decrease in swelling, pain, stiffness, and tenderness of a joint or muscle area...