Anti-Inflammatory & Anti-Gout Medication Revised

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

NSAIDs have which type of properties?

Anti-inflammatory, Antipyretic, Analgesic

COX-1 function

Protects GI health

Inhibiting COX-1 results in

Increased risk of GI bleeding

COX-2 function

Activate pain & inflammation

COX-2 inhibition results in

Reduction in pain & inflammation

Aspirin is a platelet inhibitor. True or false?

True

Prodrug of salicylate

Acetylsalicylic acid (Aspirin)

Used for:

• First signs of MI

• Anti-inflammatory, anti-rheumatic (joints, muscles, CT), antipyretic action

Salicylate indication 

Contraindicated for:

• Conditions that place clients at risk for bleeding

• Children < 18 years have risk for Reye’s Syndrome (encephalopathy, hepatic damage)

Salicylate contraindications

• 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)

Adverse effects of Salicylates

What can lead to AERD?

Administering aspirin to patient who has rhinitis, asthma, or nasal polyps

Aspirin dosage for heart disease

81 mg

Aspirin dosage for pain

325 mg

When patient is taking aspirin, monitor for

S&S Bleeding:

• Petechiae, bruising, black & tarry stool, hematemesis

• Increased heart rate

• Tinnitus (ringing, buzzing, roaring), ototoxicity, hearing loss, dizziness, headache, confusion

• NVD

• Sweating, thirst, hyperventilation

Symptoms of aspirin toxicity

Procedures to treat aspirin overdose 

• Gastric lavage/hemodialysis or activated charcoal for acute ingestion

• Hemodialysis for severe cases or renal failure

Prodrug of propionic acid derivatives

Ibuprofen (Advil, Motrin)

Name the propionic acid derivatives

ibuprofen (Advil, Motrin) & Naproxen (Aleve)

Used for:

• Mild to moderate pain

• Fever

• Inflammation from arthritis and initial gout attacks

Propionic acid derivatives indication (ibuprofen/naproxen)

Name the acetic acid derivatives

Indomethacin & Ketorolac

MOA of NSAIDs

Blocks both COX-1 and COX-2; inhibits the synthesis of prostaglandins (except aspirin & COX-2 inhibitors)

Used for:

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

Indomethacin indication (acetic acid derivative)

Used for:

• Moderate to severe acute pain

• Powerful analgesic effects (comparable with opioids)

Ketorolac indication (acetic acid derivative)

NSAID with analgesic effect comparable to opioid

Ketorolac

Ketorolac BBW

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

Prodrug of enolic acid derivatives

Piroxicam (Feldene)

Name the enolic acid derivatives

Piroxicam (Feldene) & Meloxicam (Mobic) 

Used for:

• Mild to moderate pain

• Fever

• Inflammation from arthritis and initial gout attacks

Enolic acid derivatives indication & propionic acid derivatives

Name the COX-2 Inhibitors 

Celecoxib (Celebrex)

The first and only COX-2 inhibitor is

Celecoxib (Celebrex)

COX-2 Inhibitor MOA

• Selectively blocks COX-2

• Inhibits the synthesis of prostaglandins

Used for: OA, RA, acute pain symptoms, ankylosing spondylitis, and primary dysmenorrhea

COX-2 inhibitors indication

Patients taking sulfa drugs (TMP-SMX) or have sulfa allergies are contraindicated this drug

COX-2 inhibitors contraindication

NSAIDS HURT

H = hemostasis (systemic bleeding); heartburn; heart disease risk; hepatotoxicity

U = Ulcers/GI bleeding

R = Renal function (AERD for aspirin)

T = Tinnitus/hearing loss

Why do NSAIDs result in renal failure/exacerbate existing renal function?

Disruption of prostaglandin function by NSAIDs is sometimes strong enough to precipitate acute or chronic renal failure (afferent arteriole constriction due to decreased prostaglandins → decreased blood flow to kidney → renal failure)

NSAID adverse effects

• GI heartburn/bleeding/ulcers

• Increased risk of MI and stroke (cardiovascular events)

• Altered hemostasis (platelet dysfunction)

• Noncardiogenic pulmonary edema

• Tinnitus (roaring, dinging, buzzing in ears), hearing loss

• Skin eruption, sensitivity (allergic) reaction (rashes/urticaria)

• Hepatotoxicity

• Renal failure/dysfunction (acute/chronic)

NSAIDs can precipitate renal toxicity in patients with/undergoing:

• Dehydration

• Heart failure

• Liver dysfunction

• use of diuretics or (ACE) inhibitors (BP medication).

NSAID BBW

• All NSAIDs (except aspirin) increase risk of adverse cardiovascular thrombotic events (MI and stroke)

• NSAIDs may counteract the cardioprotective effects of aspirin.

Aspirin is the only NSAID that does not have a BBW for cardiovascular thrombotic events. True or false?

True

Contraindicated for

• GI lesions or peptic ulcer disease

• Bleeding disorders

• Heart disease

NSAID contraindications

What lab studies would be part of an assessment on whether a patient should take an NSAID or continue adherence to NSAIDs?

CBC, platelet count, cardiac, renal (CrCl), and liver function studies

What drug may be beneficial to help prevent GI bleeds caused by NSAIDs?

Misoprostol (Cytotec)

Condition that results from inappropriate uric acid metabolism

Gout

Gout can be caused by 

Underexcretion of uric acid or overproduction of uric acid

Gout medication drug classes

Mitotic Agents, Uricosuric Agents, Xanthine Oxidase Inhibitors

Prodrug of mitotic agents

Colchicine (Colcrys)

MOA of mitotic agents (Colchicine)

Stops WBC movement into areas with urate crystals; reduces inflammatory response to the deposits of urate crystals in joint tissue

Used for:

• Acute gout attacks

• Short-term management or prevention of gout

Colchicine indication

N/V, leukopenia, bleeding into GI & urinary tracts (watch for S&S of bleeding)

Colchicine (mitotic agents) adverse effects

Nursing implications for mitotic agents (colchicine)

• Monitor labs

• Monitor for S&S of bleeding (petechiae, black/tarry stool, hematuria, bruising)

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

Prodrug of Uricosuric Agents

Probenecid (Benemid)

Name the uricosuric agents

Probenecid (Benemid) & Lesinurad (Zurampic)

MOA of uricosuric agents

• Inhibits the reabsorption of uric acid in the kidney

• Increases uric acid excretion

• Treatment for chronic gout

• Management of hyperuricemia associated with certain cancers or chemotherapy

Uricosuric agents Indications (probenecid, lesinurad)

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

• NV, abd pain

• Headache, dizziness

Adverse effects of uricosuric agents (probenecid, lesinurad)-

Nursing implications for uricosuric agents

• Take with meals

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

• Monitor kidney functions and labs

Drugs to give with meals/foods

Salicylates, Xanthine Oxidase inhibitors, Uricosuric agents

Prodrug of Xanthine Oxidase Inhibitors

Allopurinol

Name the xanthine oxidase inhibitors

Allopurinol (Zyloprim) & Febuxostat (Uloric) 

MOA of xanthine oxidase inhibitors

• Reduces uric acid production by inhibiting xanthine oxidase

• Increases excretion of uric acid precursors

• Gout treatment

• Management of hyperuricemia associated with certain cancers or chemotherapy

Xanthine Oxidase Inhibitors Indications

Nursing implications for xanthine oxidase inhibitors 

• Take with meals

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

• Monitor kidney function and labs

• Agranulocytosis/aplastic anemia (bone marrow dysfunction)

• Serious skin conditions (exfoliative dermatitis, SJS)

• N/V

• Dizziness, drowsiness

• Kidney stones

Adverse effects of xanthine oxidase inhibitors

You can crush salicylates. True or false?

False

Drugs that can cause kidney stones

Uricosuric acid derivatives (probenecid & lesinurad) and xanthine oxidase inhibitors (allopurinol & febuxostat)

Drugs that can cause agranulocytosis/aplastic anemia

Xanthine oxidase inhibitors

Drugs that can cause leukopenia

Colchicine (Colcrys)

Why is colchicine given for acute gout attack but not long-term treatment?

Used for acute attacks due to its anti-inflammatory properties and the risk of adverse effects such as hepatotoxicity with long term treatment

Drug that can cause Reye’s syndrome in patients <18 years

Aspirin 

Discontinue ________ how many weeks prior to surgery?

Aspirin; 2

Drug used as an alternative to NSAIDs due to lack of GI effects

Acetaminophen 

Conditions that can precipitate renal failure when combined with NSAIDs

Dehydration, heart failure, liver dysfunction, or use of diuretics or ACE inhibitors (lower BP).

MOA of salicylates

• COX-1 & COX-2 inhibitor

• Inhibits the synthesis of prostaglandins that cause platelet aggregation 

NSAID interaction with ETOH

Increased GI bleeding

Drug that can cause SJS

Allopurinol