chapter 49 anti inflammatory and antigout drugs

Question 1

inflammation

Answer 1

Localized protective response stimulated by injury to tissues, which serves to destroy, dilute, or wall off (sequester) both the injurious agent and the injured tissue
Pain, fever, loss of function, redness, and swelling
Endogenous compounds, including proteins of the complement system, histamine, serotonin, bradykinin, leukotrienes, and prostaglandins

Question 2

NSAIDs uses

Answer 2

Uses of NSAIDs
Relief of mild to moderate headaches
Relief of myalgia
Relief of neuralgia
Relief of arthralgia
Relief of postoperative pain
Relief of pain associated with arthritic disorders such as rheumatoid arthritis, juvenile arthritis, ankylosing spondylitis, and osteoarthritis
Treatment of gout and hyperuricemia

Question 3

properties of Nsaids

Answer 3

Properties all NSAIDs share:
Antipyretic properties
Analgesic properties
Anti-inflammatory properties

Question 4

aspirin

Answer 4

Shown to reduce cardiac death after myocardial infarction (MI)
Should be administered at the first sign of MI
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.

Question 5

NSAIDs mechanism of action

Answer 5

Inhibition of the leukotriene pathway, the prostaglandin pathway, or both
Blocking the chemical activity of the enzyme COX
COX-1 has a role in maintaining the gastrointestinal (GI) mucosa.
COX-2 promotes synthesis of prostaglandins involved in the inflammatory process.

aspirin
Irreversible inhibitor of COX-1 receptors within the platelets themselves
Reduced formation of thromboxane A2, a substance that normally promotes platelet aggregation (also known as antiplatelet activity)
Other NSAIDs lack these antiplatelet effects.

Question 6

NSAIDs: Contraindications

Answer 6

Known drug allergy
Conditions that place the patient at risk for bleeding
Rhinitis
Vitamin K deficiency
Peptic ulcer disease

Question 7

NSAIDs: Adverse Effects

Answer 7

Heartburn to severe GI bleeding
Acute kidney injury
Noncardiogenic pulmonary edema
Altered hemostasis
Hepatotoxicity
Skin eruption, sensitivity reaction
Tinnitus, hearing loss

Question 8

misoprostol

Answer 8

Many of the adverse effects of NSAIDs are secondary to their inactivation of protective prostaglandins that help maintain the normal integrity of the stomach lining.
Prevents GI bleed
A synthetic prostaglandin E1 analogue: inhibits gastric acid secretion and has a cytoprotective component
Mechanism of action: unclear

Question 9

NSAIDs and Kidney Function

Answer 9

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.

Question 10

NSAIDs: Health Canada Warning

Answer 10

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.

Question 11

Salicylates

Answer 11

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®)
acetylsalicylic acid (aspirin)
Inhibits platelet aggregation
Antithrombotic effect: used in the treatment of MI and other thromboembolic disorders
Reye’s syndrome
Patients with systemic lupus erythematosus may benefit from aspirin therapy because of its antirheumatic effects.

Question 12

aspirin: Forms

Answer 12

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.

Question 13

aspirin: Uses

Answer 13

Headache, neuralgia, myalgia, and arthralgia
Pain syndromes resulting from inflammation: arthritis, pleurisy, and pericarditis
Systemic lupus erythematosus: antirheumatic effects
Antipyretic action

Question 14

aspirin: Reye’s Syndrome

Answer 14

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.

Question 15

Salicylates

Answer 15

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

Question 16

Acetic Acid Derivatives

Answer 16

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

Question 17

Propionic Acid Derivatives

Answer 17

ibuprofen (Motrin, Advil)
Most commonly used NSAID
Uses: analgesic effects in the management of RA, OA, primary dysmenorrhea, dental pain, 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

Question 18

Cyclo-oxygenase-2 (COX-2) Inhibitor

Answer 18

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, lower-extremity edema, and hypertension
Little effect on platelet function
Not to be used in patients with known sulpha allergy

Question 19

Enolic Acid Derivatives

Answer 19

piroxicam
meloxicam
nabumetone
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.

Question 20

NSAIDs: Adverse Effects

Answer 20

GI
Dyspepsia, heartburn, epigastric distress, nausea, vomiting, anorexia, abdominal pain
GI bleeding*
Mucosal lesions* (erosions or ulcerations)
Renal
Reductions in creatinine clearance
Acute tubular necrosis with acute kidney injury
Cardiovascular
Noncardiogenic pulmonary edema
*Misoprostol can be used to reduce these dangerous effects.

Question 21

Gout

Answer 21

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

Question 22

Antigout Drugs

Answer 22

allopurinol (Zyloprim®)
febuxostat (Uloric®)
colchicine
probenecid (Benuryl®)
sulfinpyrazone

Question 23

Antigout Drugs: Indications

Answer 23

allopurinol (Zyloprim)
Used to prevent uric acid production and to prevent acute tumour lysis syndrome
Also used for 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
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

Question 24

Herbal Products: 
Glucosamine and Chondroitin

Answer 24

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

Question 25

nursing implications - salicylates

Answer 25

Before beginning therapy, observe for and assess conditions that may be contraindications to therapy, especially,
GI lesions or peptic ulcer disease.
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.
Several serious drug interactions exist.
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.
Do not give salicylates to children and teenagers because of the risk of Reye’s syndrome
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.
Decrease in swelling, pain, stiffness, 
and tenderness of a joint or muscle area