Anti-inflammatory and Anti-gout Drugs

Inflammation

Protective response stimulated by injury to tissues, which serves to destroy, dilute, or wall off (sequester) both the injurious agent and the injured tissue

Complement system proteins involved in inflammation are:

Histamine, serotonin, bradykinin, leukotrienes, and prostaglandins

excessive or prolonged inflammation can lead to tissue damage and various pathological conditions. True or false?

True

Non-steroidal anti-inflammatory drugs (NSAIDs)

• Anti-inflammatory

• Antipyretic (reduce fever)

• Analgesic

Aspirin

Induces platelet inhibition

NSAIDs types

• Salicylate

• Propionic acid derivatives

• Acetic acid derivatives

• Enolic acid derivatives

• COX-2 Inhibitors

Salicylate prototype drug

Acetylsalicylic acid (Aspirin)

• Blocks both COX-1 and COX-2

• Inhibits the synthesis of prostaglandins that cause platelet aggregation

MOA of salicylates

Salicylates are indicated for

• First signs of myocardial infarction (MI)

• Anti-inflammatory, anti-rheumatic, anti-pyretic action

Salicylates are contraindicated for

• Conditions that place clients at risk for bleeding

• Children < 18 years

  • Risk for Reye’s Syndrome

Adverse effects of salicylates

• GI: N/V, stomach pain, increased risk for ulcers/GI bleeding

• Hematological: increased risk for bleeding

• GU: risk for acute kidney injury

• Resp: bronchospasms (in patients with asthma)

Which NSAID may cause Reye’s syndrome in children with viral illnesses of fever?

Salicylates (Aspirin)

Aspirin triad

Contraindicated for patients with asthma, rhinitis, nasal polyps; Can lead to aspirin-exacerbated respiratory disease (AERD)

At ______ mg, aspirin improves ______

81; cardiac risk reduction (e.g. thrombus, stroke, MI prevention)

At ______ mg, aspirin is used to treat __________

325; mild to moderate pain

What should be monitored when a patient takes aspirin?

Risk for bleeding

S&S for bleeding (aspirin)

Petechiae, bruising, black or tarry stools, vomiting blood

Aspirin should be taken with water 6-8 oz water, and should not be crushed. True or false.

True

how much time before surgeries should aspirin be discontinued?

at least 2 weeks

Salicylate toxicity effect on CV

Increased heart rate

Salicylate toxicity effect on CNS

Tinnitus, hearing loss, dizziness, headache, confusion

Salicylate toxicity effect on GI

NV, diarrhea

Metabolic effects of salicylate toxicity

Sweating, thirst, hyperventilation

Managing salicylate activit

• Gastric lavage or activated charcoal for acute ingestion

• Hemodialysis for severe cases or renal failure

What should be done if a patient is overdosing on aspirin?

Administer activated charcoal or perform gastric lavage

A patient presents with renal failure after taking aspirin. What should be done?

Hemodialysis

When should hemodialysis be used to treat salicylate overdose?

In severe cases or renal failure

Propionic acid derivative prototype drug

Ibuprofen (Advil, Motrin)

Propionic acid derivative

Naproxen (Aleve)

MOA of Propionic acid derivatives

• Blocks both COX-1 and COX-2

• Inhibits the synthesis of prostaglandins

What are propionic acid derivatives indicated for?

• Mild to moderate pain

• Fever

• Inflammation from arthritis and initial gout attacks

Acetic acid derivatives

Ketorolac (Toradol), Indomethacin

MOA of acetic acid derivatives

• Blocks both COX-1 and COX-2

• Inhibits the synthesis of prostaglandins

Indomethacin is indicated for

RA, OA, ankylosing spondylitis, acute gouty arthritis, children with PDA, and treatment of preterm labor

Ketorolac (Toradol) is indicated for

• Moderate to severe acute pain

• Powerful analgesic effects (comparable with opioids; useful for opiate addicts)

BBW for Ketorolac

Use limited to no more than 5 days in a row due to high risk of kidney and GI problems

Enolic acid derivatives

Indomethacin and Ketorolac have the same MOA (inhibit COX-1 & COX-2 and synthesis of prostaglandins). True or false?

True

Enolic acid derivative prototype drug

Piroxicam (Feldene)

Enolic acid derivatives

Meloxicam (Mobic)

MOA of enolic acid derivatives

• Blocks both COX-1 and COX-2

• Inhibits the synthesis of prostaglandins

Acetic acid derivatives and enolic acid derivatives have different MOAs. True or false?

False

Enolic acid derivatives are indicated for

• Mild to moderate pain

• Fever

• Inflammation from arthritis and initial gout attacks

Ibuprofen and Piroxicam have the same indications. True or false?

True

COX-2 Inhibitor prototype drug

Celecoxib (Celebrex)

MOA of COX-2 inhibitors

• Selectively blocks COX-2

• Inhibits the synthesis of prostaglandins

NSAIDs broadly inhibit prostaglandin synthesis. True or false?

True. Aside from salicylates that inhibit prostaglandins involved with platelet aggregation

COX-2 inhibitors are indicated for

OA, RA, acute pain symptoms, ankylosing spondylitis, and primary dysmenorrhea

What are COX-2 inhibitors contraindicated for?

Sulfa allergy

NSAID adverse effects

• GI: heartburn to severe GI bleeding

• Acute renal failure 

• Noncardiogenic pulmonary edema

• Increased risk of MI and stroke

• Altered hemostasis

• Hepatotoxicity

• Skin eruption, sensitivity reaction

• Tinnitus, hearing loss

Acute renal failure from NSAIDs

Renal function depends partly on prostaglandins.

• Disruption of prostaglandin function by NSAIDs is sometimes strong enough to precipitate acute or chronic renal failure.

• Use of NSAIDs can compromise existing renal function.

• Renal toxicity can occur in patients with dehydration, heart failure, liver dysfunction, or use of diuretics or angiotensin-converting enzyme (ACE) inhibitors.

NSAIDs are contraindicated for

Patients with dehydration, heart failure, liver dysfunction, or use of diuretics or angiotensin-converting enzyme (ACE) inhibitors.

All NSAIDs increase risk of adverse cardiovascular thrombotic events (MI and stroke). True or false?

False

BBWs for NSAIDs except aspirin

Increase risk of adverse cardiovascular thrombotic events (MI and stroke)

• NSAIDs may counteract the cardioprotective effects of aspirin.

What are S&S are NSAIDs broadly contraindicated for?

• GI lesions or peptic ulcer disease

• Bleeding disorders

Nursing implications for NSAIDs

• Perform laboratory studies as indicated (cardiac, renal, and liver function studies; complete blood count; platelet count).

• Inform 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.

Misoprostol (Cytotec)

NSAID that may be beneficial to prevent GI bleeds

It is safe to be chew or crush NSAIDs. True or false?

False

Gout (hyperuricemia)

Condition that results from inappropriate uric acid metabolism

• Underexcretion of uric acid

• Overproduction of uric acid

How does gout cause pain?

Uric acid crystals are deposited in tissues and joint, which cause pain

Mitotic agents prototype drug

Colchicine (Colcrys)

MOA of mitotic agents

• Stops WBC movement (chemotaxis) into areas with urate crystals

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

Mitotic agents are indicated for

• Acute gout attacks

• Short-term management or prevention of gout

Adverse effects of mitotic agents

• GI: N/V

• Leukopenia

• Bleeding into the GI or urinary tracts

Nursing implications for mitotic agents

• Monitor lab values

• Monitor for signs and symptoms of bleeding

• Educate patients on S&S of bleeding and when to seek medical care

Uricosuric agents prototype drug

Probenecid (Benemid)

Uricosuric agents

lesinurad (Zurampic)

MOA of uricosuric agents

• Inhibits the reabsorption of uric acid in the kidney

• Increases uric acid excretion

Uricosuric agents are indicated for

• Treatment for chronic gout

• Management of hyperuricemia associated with certain cancers or chemotherapy

Adverse effects of uricosuric agents

• Increased risk for kidney stones (Esp. during initial therapy)

• GI: N/V, abdominal pain

• Headache, dizziness

Nursing implications of uricosuric agents

• Take with meals

• Stay well hydrated (3L of fluid/day)

• Monitor kidney functions and labs

Xanthine oxidase inhibitors prototype drug

Allopurinol (Zyloprim)

Xanthine oxidase inhibitors

Febuxostat (Uloric)

MOA of xanthine oxidase inhibitors

• Reduces uric acid production by inhibiting xanthine oxidase

• Increases excretion of uric acid precursors

Xanthinin oxidase inhibitors are indicated for

• Gout treatment

• Management of hyperuricemia associated with certain cancers or chemotherapy

Adverse effects of xanthinin oxidase inhibitors

• Agranulocytosis/aplastic anemia

• Serious skin conditions (exfoliative dermatitis, Stevens-Johnson syndrome)

• GI: N/V

• Dizziness, drowsiness

• Kidney stones

Nursing implications for xanthin oxidase inhibitors

• Take with meals

• Stay well hydrated (3L of fluid/day)

• Monitor kidney function and labs

Xanthinin oxidase inhibitors and uricosuric agents both have the same nursing implications (take with meals, stay well hydrated, monitor kidney function and labs). True or false?

True

What drug class is acetylsalicylic acid (aspirin)

Salicylate

What drug class is Ibuprofen (Advil, Motrin)

Propionic acid derivative

Naproxen (Aleve)

Propionic acid derivative

What drug class is indomethacin?

Acetic acid derivative

What drug class is Piroxicam (Feldene)

Enolic acid derivative

What drug class is Meloxicam (Mobic)

Enolic acid derivative

What drug class is Celecoxib (Celebrex)

COX-2 inhibitors (only drug in class)

What drug class is colchicine (Colcrys)

Mitotic agent

What drug class is probenecid (Benemid)

Uricosuric acid

What drug class is lesinurad (Zurampic)

Uricosuric acid

What drug class is allopurinol (Zyloprim)

Xanthine Oxidase Inhibitor

What drug class is febuxostat (Uloric)

Xanthine Oxidase Inhibitor