Antiinflammatory Agents and Nonsteroidal Antiinflammatory Drugs (NSAIDs)

NSAIDs Large and chemically diverse group of drugs with the following properties: Analgesic Antiinflammatory Antipyretic

Large and chemically diverse group of drugs with the following properties:

Analgesic

Antiinflammatory

Antipyretic

NSAIDs: Mechanism of Action Activation of the arachidonic acid pathway causes: pain headache fever inflammation

Activation of the arachidonic acid pathway causes:

pain

headache

fever

inflammation

Instructors may wish to use EIC Image #107: Arachidonic Acid Pathway

NSAIDs: Mechanism of Action Analgesia—treatment of headaches and pain Block the undesirable effects of prostaglandins, which cause headaches

Analgesia—treatment of headaches and pain

Block the undesirable effects of prostaglandins, which cause headaches

NSAIDs: Mechanism of Action Antipyretic: reduce fever Inhibit prostaglandin E 2 within the area of the brain that controls temperature

Antipyretic: reduce fever

Inhibit prostaglandin E 2 within the area of the brain that controls temperature

NSAIDs: Mechanism of Action Relief of inflammation Inhibit the leukotriene pathway, the prostaglandin pathway, or both

Relief of inflammation

Inhibit the leukotriene pathway, the prostaglandin pathway, or both

NSAIDs Six structurally related groups: Acetic acids Carboxylic acids Propionic acids Enolic acids Fenamic acids Nonacidic compounds

Six structurally related groups:

Acetic acids

Carboxylic acids

Propionic acids

Enolic acids

Fenamic acids

Nonacidic compounds

NSAIDs: Acetic Acid diclofenac sodium (Voltaren) diclofenac potassium (Cataflam) etodolac (Lodine) indomethacin (Indocin) sulindac (Clinoril) tolmetin (Tolectin)

diclofenac sodium (Voltaren)

diclofenac potassium (Cataflam)

etodolac (Lodine)

indomethacin (Indocin)

sulindac (Clinoril)

tolmetin (Tolectin)

NSAIDs: Carboxylic Acids Acetylated aspirin (ASA) choline magnesium salicylate (Trilisate) diflunisal (Dolobid) Nonacetylated salicylamide salsalate (Disalcid) sodium salicylate

Acetylated

aspirin (ASA)

choline magnesium salicylate (Trilisate)

diflunisal (Dolobid)

Nonacetylated

salicylamide

salsalate (Disalcid)

sodium salicylate

NSAIDs: Propionic Acids fenoprofen (Nalfon) flurbiprofen (Ansaid) ibuprofen (Motrin, others) ketoprofen (Orudis) ketorolac (Toradol) naproxen (Naprosyn) oxaprozin (Daypro)

fenoprofen (Nalfon)

flurbiprofen (Ansaid)

ibuprofen (Motrin, others)

ketoprofen (Orudis)

ketorolac (Toradol)

naproxen (Naprosyn)

oxaprozin (Daypro)

NSAIDs: Other Agents Enolic acids phenylbutazone (Butazolidin) piroxicam (Feldene) Fenamic acids meclofenamic acid (Meclomen) mefenamic acid (Ponstel) Nonacidic compounds nabumetone (Relafen)

Enolic acids

phenylbutazone (Butazolidin)

piroxicam (Feldene)

Fenamic acids

meclofenamic acid (Meclomen)

mefenamic acid (Ponstel)

Nonacidic compounds

nabumetone (Relafen)

NSAIDs: Other Agents COX-2 Inhibitors celecoxib (Celebrex) rofecoxib (Vioxx)

COX-2 Inhibitors

celecoxib (Celebrex)

rofecoxib (Vioxx)

NSAIDs: Drug Effects Analgesic (mild to moderate) Antigout Antiinflammatory Antipyretic Relief of vascular headaches Platelet inhibition (ASA)

Analgesic (mild to moderate)

Antigout

Antiinflammatory

Antipyretic

Relief of vascular headaches

Platelet inhibition (ASA)

NSAIDs: Therapeutic Uses Relief of mild to moderate pain Acute gout Various bone, joint, and muscle pain Osteoarthritis Rheumatoid arthritis Juvenile rheumatoid arthritis Dysmenorrhea Fever

Relief of mild to moderate pain

Acute gout

Various bone, joint, and muscle pain

Osteoarthritis

Rheumatoid arthritis

Juvenile rheumatoid arthritis

Dysmenorrhea

Fever

NSAIDs: Specific Agents salicylates (aspirin) More potent effect on platelet aggregation and thermal regulatory center in the brain analgesic antipyretic antiinflammatory Antithrombotic effect: used in the treatment of MI and other thromboembolic disorders

salicylates (aspirin)

More potent effect on platelet aggregation and thermal regulatory center in the brain

analgesic

antipyretic

antiinflammatory

Antithrombotic effect: used in the treatment of MI and other thromboembolic disorders

NSAIDs: Specific Agents phenylbutazone (Butazolidin) Greater effects on uric acid production and excretion, in addition to antiinflammatory effects More commonly used for treatment of gout

phenylbutazone (Butazolidin)

Greater effects on uric acid production and excretion, in addition to antiinflammatory effects

More commonly used for treatment of gout

NSAIDs: Side Effects Gastrointestinal dyspepsia, heartburn, epigastric distress, nausea **GI bleeding **mucosal lesions (erosions or ulcerations) Misoprostol (Cytotec) can be used to reduce these dangerous effects.

Gastrointestinal

dyspepsia, heartburn, epigastric distress, nausea

**GI bleeding

**mucosal lesions (erosions or ulcerations)

Misoprostol (Cytotec) can be used to reduce these dangerous effects.

NSAIDs: Side Effects Renal reductions in creatinine clearance acute tubular necrosis with renal failure

Renal

reductions in creatinine clearance

acute tubular necrosis with renal failure

NSAIDs: Side Effects Cardiovascular noncardiogenic pulmonary edema

Cardiovascular

noncardiogenic pulmonary edema

NSAIDs: Salicylate Toxicity Adults: tinnitus and hearing loss Children: hyperventilation and CNS effects Effects arise when serum levels exceed 300  g/mL. Metabolic acidosis and respiratory alkalosis may be present.

Adults: tinnitus and hearing loss

Children: hyperventilation and CNS effects

Effects arise when serum levels exceed 300  g/mL.

Metabolic acidosis and respiratory alkalosis may be present.

NSAIDs: Nursing Implications Before beginning therapy, assess for conditions that may be contraindications to therapy, especially: GI lesions or peptic ulcer disease Bleeding disorders Assess also for conditions that require cautious use. Perform lab studies as indicated (cardiac, renal, liver studies, CDC, platelet count).

Before beginning therapy, assess for conditions that may be contraindications to therapy, especially:

GI lesions or peptic ulcer disease

Bleeding disorders

Assess also for conditions that require cautious use.

Perform lab studies as indicated (cardiac, renal, liver studies, CDC, platelet count).

NSAIDs: Nursing Implications Perform a medication history to assess for potential drug interactions. Several serious drug interactions exist: alcohol heparin phenytoin oral anticoagulants steroids sulfonamides

Perform a medication history to assess for potential drug interactions.

Several serious drug interactions exist:

alcohol

heparin

phenytoin

oral anticoagulants

steroids

sulfonamides

NSAIDs: Nursing Implications Salicylates are NOT to be given to children under age 12 because of the risk of Reye’s syndrome. Because these agents generally cause GI distress, they are often better tolerated if taken with food, milk or an antacid to avoid GI irritation. Explain to patients that therapeutic effects may not be seen for 3 to 4 weeks.

Salicylates are NOT to be given to children under age 12 because of the risk of Reye’s syndrome.

Because these agents generally cause GI distress, they are often better tolerated if taken with food, milk or an antacid to avoid GI irritation.

Explain to patients that therapeutic effects may not be seen for 3 to 4 weeks.

NSAIDs: Nursing Implications Educate patients about the various side effects of NSAIDs, and to notify their physician if these effects become severe or if bleeding or GI pain occur. Patients should watch closely for the occurrence of any unusual bleeding, such as in the stool. Enteric-coated tablets should not be crushed or chewed.

Educate patients about the various side effects of NSAIDs, and to notify their physician if these effects become severe or if bleeding or GI pain occur.

Patients should watch closely for the occurrence of any unusual bleeding, such as in the stool.

Enteric-coated tablets should not be crushed or chewed.

NSAIDs: Nursing Implications Monitor for therapeutic effects, which vary according to the condition being treated: decrease in swelling, pain, stiffness, and tenderness of a joint or muscle area

Monitor for therapeutic effects, which vary according to the condition being treated:

decrease in swelling, pain, stiffness, and tenderness of a joint or muscle area