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

Endogenous compounds, including proteins of the complement system, histamine, serotonin, bradykinin, leukotrienes, and prostaglandins

Question 2

Inflammation symptoms

Answer 2

Pain, fever, loss of function, redness, and swelling

Question 3

Nonsteroidal Anti-inflammatory Drugs (NSAIDs) four functions

Answer 3

A large and chemically diverse group of drugs that have:
-Analgesic activities
-Anti-inflammatory activities
-Antipyretic activities
-aspirin-platelet inhibition

Question 4

Indications of NSAIDs

Answer 4

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 5

Properties all NSAIDs share:

Answer 5

Antipyretic properties
Analgesic properties
Anti-inflammatory properties

Question 6

NSAIDs: Salicylates

Answer 6

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 7

NSAIDs: Acetic acid derivatives

Answer 7

diclofenac sodium (Voltaren®)
indomethacin sulindac
ketorolac (Toradol®)

Question 8

NSAIDs
Cyclo-oxygenase (COX)-2 inhibitors

Answer 8

-celecoxib (Celebrex®)

Question 9

Enolic acid derivatives

*DNTK

Answer 9

nabumetone
meloxicam (Mobicox®)
piroxicam

Question 10

NSAIDs: Propionic acid derivatives

Answer 10

ibuprofen (Motrin®, Advil®)
naproxen (Naprolen®, Naprosyn®, Aleve®)

Question 11

Aspirin is shown to reduce?
should be administred at the first sign of?

Answer 11

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 12

NSAIDs: Two Mechanism of Action
COX 1 VS 2

Answer 12

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.

Question 13

Three Conditions that place the patient at risk for bleeding

Answer 13

Known drug allergy

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

Question 14

NSAIDs: Adverse Effects

Answer 14

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

Question 15

misoprostol

Answer 15

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 16

NSAIDs and Kidney Function

Kidney toxicity can occur in patients with

Meds that can increase toxicity if given with NSAIDs

Answer 16

Kidney function depends partly on prostaglandins (P increases renal blood flow and GFR)

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 17

NSAIDs: Health Canada Warning

Answer 17

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 18

Salicylates

Answer 18

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®)

Question 19

acetylsalicylic acid (aspirin)

inhibits?
has ____ and ____ effects
which patients population may benefit from aspirin?

Answer 19

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 20

aspirin: usual dosage for prophylactic therapy

Answer 20

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 21

aspirin: Uses

Answer 21

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

Question 22

aspirin: Reye’s Syndrome

Answer 22

Acute and potentially life-threatening condition involving progressive neurological deficits that can lead to coma and may also involve liver damage (increasepressure within brain and fat accumulation in liver; vomiting, disorientation, delirium, convulsion, LOC)

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 23

Salicylate intoxication symptoms (when chronic, known as salicylism)

Answer 23

Increased heart rate
Tinnitus, hearing loss, dimness of vision, headache, dizziness, mental confusion, drowsiness
Nausea, vomiting, diarrhea
Sweating, thirst, hyperventilation, hypoglycemia or hyperglycemia

Question 24

Acetic Acid Derivatives: indomethacin

Answer 24

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

Question 25

Acetic Acid Derivatives: ketorolac tromethamine (Toradol)

Answer 25

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 26

Propionic Acid Derivatives: ibuprofen (Motrin, Advil)

Answer 26

Most commonly used NSAID

Uses: analgesic effects in the management of RA, OA, primary dysmenorrhea, dental pain, musculoskeletal disorders; antipyretic actions

Question 27

Propionic Acid Derivatives: naproxen
AEs
Fewer drug interactions with?

Answer 27

Second most commonly used NSAID

Somewhat better adverse effect profile than ibuprofen

Fewer drug interactions with angiotensin-converting enzyme inhibitors given for hypertension

Question 28

Cyclo-oxygenase-2 (COX-2) Inhibitor: celecoxib (Celebrex®)

What enzyme does it inhibit?
Indicated for
AEs
little effect on?
do not use in pts with _____ allergy

Answer 28

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 29

Enolic Acid Derivatives

**DNTK

Answer 29

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.

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 30

NSAIDs: Adverse Effects

Answer 30

GI:

Dyspepsia, heartburn, epigastric distress, nausea, vomiting, anorexia, abdominal pain
GI bleeding*
Mucosal lesions* (erosions or ulcerations)

*Misoprostol can be used to reduce these dangerous effects

Renal
Reductions in creatinine clearance
Acute tubular necrosis with acute kidney injury

Cardiovascular
Noncardiogenic pulmonary edema

Question 31

NSAIDs: Serious interactions can occur when given with:

Answer 31

Alcohol
Anticoagulants
acetylsalicylic acid (ASA)
Biphosphonates(protect bones; slows osteoclats)
Corticosteroids and other ulcerogenic medications
Protein-bound drugs
Diuretics and angiotensin-converting enzyme inhibitors
Other drugs

Question 32

Gout

Answer 32

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 33

Antigout Drugs

Answer 33

allopurinol (Zyloprim®)
colchicine
probenecid (Benuryl®)

Question 34

allopurinol (Zyloprim)

Answer 34

Used to prevent uric acid production and to prevent acute tumour lysis syndrome (cancer cells die and release substances in blood reuslting in hyperurecemia, hyperkalemia, hyperhosphatemia, hypocalcemia)

Side effects: exfoliative dermatitis, Stevens-Johnson syndrome (severe skin disorder; blister rash), and toxic epidermal necrolysis (severe skin disorder; blister and peeling of skin)

Question 35

probenecid (Benuryl)

Answer 35

Inhibits the reabsorption of uric acid in the kidneys and thus increases the excretion of uric acid

Question 36

colchicine

Answer 36

Oldest available therapy

Reduces the inflammatory response to the deposits of urate crystals in joint tissue

Powerful inhibitor of cell mitosis (cell division), and can cause short-term leukopenia (decreased WBC)

Prophylaxis of acute attacks in dosages of 0.6 mg once or twice a day

Question 37

Herbal Products: Glucosamine and Chondroitin

Answer 37

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 38

Nursing Implications

Answer 38

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.

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.

Question 39

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

Answer 39

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