NURS 2535 - Anti-inflammatory and Antigout Drugs

What is Gout?

A condition that results from inappropriate uric acid metabolism

o Underexcretion of uric acid

o Overproduction of uric acid

Uric acid crystals are deposited in tissues and joints, resulting in pain

What do NSAIDs do?

1. Analgesic activities

2. Anti-inflammatory activities

3. Antipyretic activities

4. aspirin-platelet inhibition

Why use NSAIDs?

1. Relief of mild to moderate headaches

2. Relief of myalgia

3. Relief of neuralgia

4. Relief of arthralgia

5. Relief of postoperative pain

6. Relief of pain associated with arthritic disorders such as rheumatoid arthritis, juvenile arthritis, ankylosing spondylitis, and osteoarthritis

7. Treatment of gout and hyperuricemia

What is the mechanism of action for NSAIDs?

- Inhibition of the leukotriene pathway, the prostaglandin pathway, or both

- Blocking the chemical activity of the enzyme COX

What are the 2 types of Cox?

COX-1 and COX-2

Whats the difference between Cox 1&2?

COX-1 generates prostaglandins that are involved in the protection of gastrointestinal mucosa, while COX-2 generates prostaglandins that mediate inflammation and pain in sites throughout the body.

Role of COX-1

Cyclooxygenase-1 (COX-1) is the isoform of the enzyme that promotes the synthesis of prostaglandins

COX-1 has a role in maintaining the gastrointestinal (GI) mucosa.

Role of COX-2

COX-2 promotes synthesis of prostaglandins involved in the inflammatory process.

What are NSAIDs primarily used for?

NSAIDs are used primarily for their analgesic, anti-inflammatory, and antipyretic effects, and for platelet inhibition.

What are the NSAID Contraindications?

Known drug allergy

Conditions that place the patient at risk for bleeding

o Rhinitis

o Vitamin K deficiency

o Peptic ulcer disease

NSAID Adverse Effects?

Heartburn to severe GI bleeding

Acute kidney injury

Noncardiogenic pulmoterm-0nary edema

Altered hemostasis

Hepatotoxicity

Skin eruption, sensitivity reaction

Tinnitus, hearing loss

What is misoprostol?

Misoprostol is a synthetic prostaglandin medication used to prevent and treat stomach and duodenal ulcers, prevents GI bleeding, etc

Kidney function depends partly on ____________.

Kidney function depends partly on prostaglandins.

Disruption of prostaglandin function by NSAIDs can cause?

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

Which patients are more likely to experience kidney failure with the use of NSAIDs?

- dehydration

- heart failure

- liver dysfunction

- with the use of diuretics or angiotensin-converting enzyme inhibitors.

What are the 5 types of NSAIDs?

1. Salicylates

2. Propionic Acid Derivatives

3. Acetic Acid Derivatives

4. Cyclo-oxygenase-2 (COX-2) Inhibitor

5. Enolic Acid Derivatives

Space

Salicylates is most commonly known as

acetylsalicylic acid (aspirin)

Aspirin is the most commonly used of all salicylates. Although aspirin is available over the counter, many of the other salicylate drugs, such as diflunisal, do require a prescription

Aspirin uses

-Headache, neuralgia, myalgia, and arthralgia

-Pain syndromes resulting from inflammation: arthritis, pleurisy, and pericarditis

-Systemic lupus erythematosus: antirheumatic effects

-Antipyretic action

Aspirin is contraindicated in children with ______ _______ because the use of these drugs has been strongly associated with ______ ________

This drug class is contraindicated in children with flulike symptoms because the use of these drugs has been strongly associated with Reye's syndrome

Reye's syndrome can cause...?

Acute and potentially life-threatening condition involving progressive neurologic deficits that can lead to coma and may also involve liver damage.

What triggers Reye Syndrome?

- 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 _______ damage.

Survivors of this condition may or may not have permanent neurologic damage.

Salicylate intoxication (when chronic, known as ?)

salicylism

What are the 2 Acetic Acid Derivatives ?

indomethacin and ketorolac tromethamine (Toradol)

What is indomethacin used for and what are its properties?

- Analgesic, anti-inflammatory, antirheumatic, and antipyretic properties

- Uses: therapy for rheumatoid arthritis (RA), osteoarthritis (OA), acute bursitis or tendonitis, ankylosing spondylitis, acute gouty arthritis

How can you take indomethacin?

Oral and rectal routes

ketorolac tromethamine (Toradol) properties + uses:

- It has some anti-inflammatory activity

- Used primarily for its powerful analgesic effects, which are comparable to those of narcotic drugs such as morphine sulphate

Indications of ketorolac tromethamine (Toradol)

Indication: short-term use (up to 5 to 7 days) to manage moderate to severe acute pain

Adverse effects of ketorolac tromethamine (Toradol) ?

Adverse effects: kidney impairment, edema, GI pain, dyspepsia, and nausea

What are the 2 Propionic Acid Derivatives called:

ibuprofen (Motrin, Advil) & Naproxen

ibuprofen (Motrin, Advil) uses:

- Most commonly used NSAID

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

Naproxen is...

- Second most commonly used NSAID

- Somewhat better adverse effect profile than ibuprofen

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

Cyclo-oxygenase-2 (COX-2) Inhibitor was made to?

The COX-2 inhibitors were developed primarily to decrease the GI adverse effects characteristic of other NSAIDs because of their COX-2 selectivity. However, they are not totally devoid of GI toxicity.

Cyclo-oxygenase-2 (COX-2) Inhibitor:

celecoxib (Celebrex®)

celecoxib (Celebrex®)

- First and only remaining COX-2 inhibitor

- Indicated for OA, RA, acute pain symptoms, ankylosing spondylitis, and primary dysmenorrhea

Celecoxib adverse effects

Adverse effects include headache, sinus irritation, diarrhea, fatigue, dizziness, lower-extremity edema, and hypertension

Celecoxib has little effect on what function & what allergy should it not be used with?

- Little effect on platelet function

- Not to be used in patients with known sulpha allergy

What are the enolic acid derivatives?

piroxicam

meloxicam

nabumetone

Enolic Acid Derivatives uses?

- 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

What are antigout drugs?

Antigout medications, as their name implies, are medications used to treat gout, which is an overproduction or decreased excretion can often result in hyperuricemia (too much uric acid in the blood)

What are the 3 antigout drugs?

allopurinol, colchicine, probenecid

Uses of allopurinol?

allopurinol (Zyloprim)

o Used to prevent uric acid production and to prevent acute tumour lysis syndrome

o Also used for exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis

What is probenecid?

a second-line agent that promotes kidney uric acid excretion (uricosuric effect);

Inhibits the reabsorption of uric acid in the kidneys

What is colchicine?

o Oldest available therapy

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

o Powerful inhibitor of cell mitosis, and can cause short-term leukopenia

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