Selective NSAIDs Drugs

Name of the Selective NSAIDs Drugs

• Celecoxib
• Diclofenac
• Etodolac
• Meloxicam

1.Celecoxib

Mechanism of Action

Selectively inhibits the enzymatic activity of cyclooxygenase-2 (COX-2), the enzyme needed to convert arachidonic acid to prostaglandin. Prostaglandins are responsible for mediating the inflammatory response and causing local vasodilation, swelling, and pain. Prostaglandins also play a role in peripheral pain transmission to the spinal cord. By inhibiting COX-2 activity and prostaglandin production, this NSAID reduces inflammatory symptoms and relieves pain. Celecoxib’s mechanism of action in reducing the number of colorectal polyps is unknown.

Pharmacokinetics

• Bioavailability: Undetermined
• Peak plasma time: ≤3 hr (capsule); 1 hr (oral solution)
• Protein bound: 97% (principally to albumin; to a lesser extent, to alpha1-acid glycoprotein)
• Metabolized in liver by CYP2C9
• Half-life: Mild hepatic impairment, 11 hr; chronic renal insufficiency or moderate hepatic impairment, 13.1 hr
• Clearance: 500 mL/min
• Excretion: Feces (57%), urine (27%)

Administration

• When administering doses higher than 200/mg daily, give with food or milk to improve drug absorption.

Adverse reactions

• CNS: dizziness, drowsiness, headache, insomnia, fatigue,stroke
• CV: angina, tachycardia, peripheral edema, myocardial infarction
• EENT: ophthalmic effects, tinnitus, epistaxis, pharyngitis, rhinitis, sinusitis
• GI: nausea, diarrhea, constipation, abdominal pain, dyspepsia, flatulence, dry mouth, GI bleeding
• GU: menorrhagia,renal failure
• Hematologic: eosinophilia, ecchymosis, neutropenia, leukopenia, pancytopenia, thrombocytopenia, agranulocytosis, granulocytopenia, aplastic anemia, bone marrow depression
• Hepatic: hepatotoxicity
• Metabolic: hyperchloremia, hypophosphatemia
• Musculoskeletal: back pain, leg cramps
• Respiratory: upper respiratory tract infection
• Skin: rash
• Other: anaphylaxis

Contraindications

• Hypersensitivity to drug, sulfonamides, or other NSAIDs
• Advanced renal disease
• Severe hepatic impairment
• Sensitivity precipitated by aspirin
• Third trimester of pregnancy
• Breastfeeding

Precautions:

• Renal insufficiency, hypertension
• History of asthma, urticaria, renal disease, hepatic dysfunction, heart failure
• Patients on long-term NSAID therapy
• Elderly patients
• Pregnant patients in first or second trimester
• Children younger than age 18 (safety not established).

Patient monitoring

• Monitor CBC, electrolyte levels, creatinine clearance, occult fecal blood test, and liver function test results every 6 to 12 months.
• Patient teaching
• Advise patient to immediately report bloody stools, vomiting of blood, or signs or symptoms of liver damage (nausea, fatigue, lethargy, pruritus, yellowing of eyes or skin, tenderness in upper right abdomen, or flulike symptoms).
• Instruct patient to take drug with food or milk.
• Tell patient to avoid aspirin and other NSAIDs (such as ibuprofen and naproxen) during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

Nursing Considerations

• Use celecoxib with extreme caution in patients who have a history of ulcer disease or GI bleeding because NSAIDs, such as celecoxib, increase the risk of GI bleeding and ulceration. In these patients, drug should be used for shortest time possible.
• Be aware that serious GI tract ulceration and bleeding, as well as perforation of stomach or intestine, can occur without warning or symptoms. Elderly patients are at greatest risk. To minimize risk, give celecoxib with food. If patient develops GI distress, withhold celecoxib and notify prescriber immediately.
• Use celecoxib cautiously in patients with hypertension and monitor blood pressure closely throughout therapy because drug can start or worsen hypertension.
• Use celecoxib cautiously in children with systemic onset juvenile rheumatoid arthritis because serious adverse reactions can occur, including disseminated intravascular coagulation.
• Use celecoxib cautiously in patients known to be poor CYP2C9 metabolizers based on history or experience with other CYP2C9 substrates, such as warfarin or phenytoin. Dosage should start at half the lowest recommended amount. For patients with juvenile rheumatoid arthritis who are also poor CYP2C9 metabolizers, alternative management should be considered.
• Monitor patient—especially if elderly or receiving long-term celecoxib therapy— for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.
• Monitor liver function test results because, in rare cases, elevation may progress to severe hepatic reaction, including fatal hepatitis, hepatic necrosis, and hepatic failure.
• Monitor BUN and serum creatinine levels in elderly patients; patients taking diuretics, ACE inhibitors, or angiotensin II receptor antagonists; and patients with heart failure, impaired renal function, or hepatic dysfunction because drug may cause renal failure.
• Monitor CBC for decreased hemoglobin level and hematocrit because drug may worsen anemia.
• Assess patient’s skin regularly for signs of rash or other hypersensitivity reaction because celecoxib is a sulfur drug and may cause serious skin reactions without warning, even in patients with no history of sensivitity to sulfur. At first sign of reaction, stop drug and notify prescriber.
• Avoid using celecoxib with a non-aspirin NSAID, regardless of the dose, because celecoxib reduces inflammation and fever, which may mask signs of infection.

2.Diclofenac

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate inflammatory response and cause local pain, swelling, and vasodilation. By blocking cyclooxygenase and inhibiting prostaglandins, diclofenac reduces inflammatory symptoms. This mechanism also relieves pain because prostaglandins promote pain transmission from periphery to spinal cord.

Pharmacokinetics

• Bioavailability: 55%
• Peak plasma time: 1 hr
• Protein bound: >99%
• Half-life: ~2 hr
• Excretion:Urine (~65%); bile (~35%)

Administration

• Give on empty stomach 1 hour before or after a meal.
• If drug causes GI upset, give with milk or meals. Mix and give oral powder with 30 to 60 ml of water only.
• Make sure patient swallows extendedrelease and delayed-release forms whole without chewing or crushing.
• Know that oral powder isn’t indicated for prophylactic migraine therapy or cluster headaches.
• Know that oral powder formulation isn’t interchangeable with other oral forms.
• Don’t apply patch to damaged or nonintact skin.
• Avoid contact of patch with eyes and mucosa. If eye contact occurs, immediately wash eyes with water or saline solution

Contraindications

• Hypersensitivity to drug or its components, other NSAIDs, or aspirin
• Active GI bleeding or ulcer disease
• Aspirin-sensitive asthma, urticaria
• Use as perioperative analgesia in coronary artery bypass graft surgery
• Use on nonintact or damaged skin (patch)

Precautions:

• Severe cardiovascular (including patients taking diuretics or ACE inhibitors, patients with fluid retention, hypertension, or congestive heart failure), renal, or hepatic disease; bleeding tendency; dehydration
• Advanced renal disease (not recommended)
• History of porphyria or preexisting asthma
• Concurrent methotrexate or anticoagulant use; concurrent use of drugs known to be potentially hepatotoxic (such as acetaminophen, anti-infectives, or antiepileptics)
• Concurrent use of aspirin (not recommended)
• Concurrent use with oral NSAIDs (avoid use)
• Elderly patients
• Pregnant or breastfeeding patients
• Children (safety and efficacy not established)

Adverse reactions

• CNS: dizziness, drowsiness, headache, paresthesia
• CV: hypertension, thrombosis
• EENT: tinnitus
• GI: dyspepsia, diarrhea, abdominal pain, dyspepsia, heartburn, peptic ulcer, GI bleeding, GI perforation
• GU: dysuria, frequent urination, hematuria, proteinuria, nephritis, acute renal failure
• Hepatic: liver failure
• Hematologic: prolonged bleeding time
• Hepatic: hepatotoxicity
• Skin: eczema, photosensitivity, rash, contact dermatitis, dry skin, exfoliation; application-site reactions, including pruritus, dermatitis, burning (with patch); exfoliative dermatitis,Stevens-Johnson syndrome, toxic epidermal necrolysis Other: dysgeusia, pain and redness allergic reactions (including edema), anaphylaxis

Patient monitoring

• Monitor hepatic and renal function.
• Observe for and report signs and symptoms of bleeding.
• Assess for hypertension.
• Monitor sodium and potassium levels in patients receiving potassiumsparing diuretics.
• Discontinue drug if rash or other signs of local skin reaction occur.
• Discontinue drug immediately if abnormal liver test values persist or worsen.
• Weigh patient to detect fluid retention. Report gain of more than 2 lb in 24 hours

Patient teaching

• Instruct patient to take drug on empty stomach 1 hour before or after a meal.
• Advise patient not to lie down for 15 to 30 minutes after taking oral drug, to minimize esophageal irritation.
• Instruct patient to mix oral powder in 1 to 2 ounces of water only before taking.
• Tell patient to measure proper amount of gel using measuring dosing card supplied and to gently massage gel into skin of entire affected foot, knee, or ankle.
• Instruct patient to apply 10 drops of topical solution to clean, dry skin and to spread evenly around front, back, and sides of knee; then repeat this procedure until 40 drops have been applied and knee is completely covered with solution.
• Instruct patient not to apply gel, patch, or topical solution to open wounds and to avoid contact with eyes and mucous membranes.
• Advise patient to avoid exposing treated sites to bath water and sunlight, external heat, occlusive dressings or clothing, sunscreens, cosmetics, lotions, moisturizers, insect repellants, or other topical drugs.
• Instruct patient to wash hands thoroughly after applying topical solution, patch, or gel except when gel is applied to the hand. If gel is applied to a hand, advise patient to avoid washing treated hands for at least 1 hour after application.
• Tell patient to discard used patches out of the reach of children and pets.
• Instruct patient to stop drug and immediately report wheezing and signs or symptoms of hypersensitivity reactions (rash, swelling of face or throat, shortness of breath) or liver impairment (unusual tiredness, weakness, nausea, yellowing of skin or eyes, tenderness on right upper side of abdomen, flulike symptoms).
• Instruct patient to stop taking drug and contact prescriber promptly if he experiences ringing or buzzing in ears, dizziness, GI discomfort, or bleeding.
• Inform patient that drug may cause serious CV side effects and to immediately report such signs and symptoms as unexplained weight gain, chest pain, shortness of breath, weakness, or slurred speech.
• Caution patient not to take over-thecounter analgesics during diclofenac therapy.
• Advise female patient to avoid pregnancy while taking this drug.
• Advise breastfeeding patient that she should decide whether to discontinue breastfeeding or discontinue drug, taking into account importance of drug for her treatment.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above

Nursing Considerations

• Use diclofenac with extreme caution and for shortest possible time in patients with a history of GI bleeding or ulcer disease because NSAIDs increase risk of GI bleeding and ulceration.
• Don’t substitute one form of oral diclofenac for another. Different formulations aren’t bioequivalent.
• Be aware that serious GI tract ulceration and bleeding, as well as perforation of stomach or intestine, can occur without warning or symptoms. Elderly patients are at greater risk. Monitor patient for signs of GI irritation and ulceration, especially if patient has a predisposing condition (such as a history of GI bleeding); takes an oral corticosteroid, anticoagulant, or NSAID (long-term); smokes; is an alcoholic; is over age 60; has poor general health; or tests positive for Helicobacter pylori. To minimize risk, give diclofenac with food. If patient develops GI distress, withhold drug and notify prescriber immediately.
• Use diclofenac cautiously in patients with hypertension, and monitor blood pressure closely; drug can cause or worsen hypertension.
• Assess patient for hypotension. If patient takes a potassium-sparing diuretic, check for elevated serum potassium level.
• Report signs of bleeding, such as bleeding gums, bloody or cloudy urine, ecchymoses, melena, and petechiae.
• Monitor BUN and serum creatinine levels in elderly patients, patients taking ACE inhibitors or diuretics, and patients with heart failure or impaired renal or hepatic function. These patients may have an increased risk of renal failure.
• Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction; drug may cause serious skin reactions without warning. At first sign of reaction, stop drug and notify prescriber.
• Because severe hepatic reactions may occur during diclofenac therapy, monitor liver function test results and serum uric acid level. Liver enzyme elevations usually occur within 2 months of starting drug and should be reported promptly because dosage may need adjustment. Also monitor patient for evidence of hepatic dysfunction (diarrhea, fatigue, flulike symptoms, jaundice, lethargy, nausea, pruritus, right upper quadrant tenderness).
• Report weight gain of more than 1 kg (2 lb) in 24 hours because it suggests fluid retention

3.Etodolac

Mechanism of Action

Blocks the activity of cyclooxygenase, the enzyme needed for prostaglandin synthesis. Prostaglandins, important mediators of the inflammatory response, cause local vasodilation with swelling and pain. By inhibiting cyclooxygenase and prostaglandins, this NSAID causes inflammatory symptoms and pain to subside.

Pharmacokinetics

• Bioavailability: 80-100%
• Peak plasma time: Immediate release, 1-2 hr (adults); extended release, 5-7 hr (children)
• Protein bound: ≥99%
• Metabolism: Hepatic
• Half-life: Immediate release, 5-8 hr (adults); extended release, 12 hr (children)
• Excretion: Urine (73%), feces (16%)

Administration

• Give with food or antacids to reduce GI upset.
• Make sure patient swallows extended-release tablets whole without crushing or chewing.
• Withhold drug several days before invasive surgery, as ordered.

Adverse reactions

• CNS: dizziness, malaise, weakness, depression, nervousness
• CV: hypertension
• EENT: blurred vision, tinnitus
• GI: nausea, vomiting, constipation, diarrhea, flatulence, dyspepsia, peptic ulcer, duodenitis, intestinal ulceration, gastritis, melena
• GU: dysuria, urinary frequency, polyuria,renal failure
• Hematologic: thrombocytopenia
• Hepatic: cholestatic jaundice, cholestatic hepatitis, hepatic necrosis
• Skin: rash, skin peeling, cutaneous vasculitis with purpura, hyperpigmentation
• Other: fluid retention, chills, fever, allergic reaction

Contraindications

• Hypersensitivity to drug or its components
• Concurrent use of other NSAIDs
• Active GI bleeding or ulcer disease

Precautions:

• Severe cardiovascular, renal, or hepatic disease
• Elderly patients
• Breastfeeding patients
• Children (safety not established).

Patient monitoring

• Monitor CBC, liver function tests, BUN, creatinine level, and coagulation studies.
• Assess for GI bleeding and gastric upset. Administer antacids as needed and prescribed.
• Know that drug may cause falsepositive urine bilirubin and urine ketone test results
• Monitor patient for signs and symptoms of thrombocytopenia and increased bleeding time.
• Assess for fluid retention and weigh patient daily.
• Watch for decreased blood pressure control in hypertensive patients

Patient teaching

• Instruct patient to take with meals if possible.
• Tell patient to swallow extended-release tablets whole without crushing or chewing.
• Instruct patient to immediately report unusual bleeding or bruising, change in urination pattern, unusual tiredness, or yellowing of skin or eyes
• Advise patient to avoid activities that can cause injury.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

Nursing Considerations

• Assess patient’s hydration status and rehydrate, if needed and as ordered, before starting etodolac therapy.
• Use etodolac with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs increase the risk of GI bleeding and ulceration. Expect to use etodolac for the shortest time possible in these patients. Also use with extreme caution in patients with advanced renal disease because etodolac is eliminated mainly by the kidneys.
• Be aware that serious GI tract ulceration, bleeding, and perforation may occur without warning symptoms. Elderly patents are at greater risk. To minimize risk, give drug with food. If GI distress occurs, withhold drug and notify prescriber immediately.
• Use etodolac cautiously in patients with hypertension and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it
• Especially if patient is elderly or taking etodolac long-term, watch for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.
• Monitor liver function test results. Rarely, elevated levels may progress to severe hepatic reactions, including fatal hepatitis, hepatic necrosis, and hepatic failure.
•  Monitor BUN and serum creatinine levels in patients with heart failure, hepatic dysfunction, or impaired renal function; those taking diuretics or ACE inhibitors; and elderly patients because drug may cause renal failure.
• Monitor CBC for decreased hemoglobin level and hematocrit because drug may worsen anemia.
• Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction because etodolac and other NSAIDs may cause serious skin reactions without warning, even in patients with no history of NSAID hypersensitivity Stop drug at first sign of reaction and notify prescriber.
• If patient also takes acetaminophen, monitor fluid intake and output and BUN and serum creatinine levels for signs of adverse renal reactions.

4.Meloxicam

Mechanism of Action

Blocks cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. By inhibiting prostaglandins, the NSAID meloxicam reduces inflammatory symptoms. It also relieves pain because prostaglandins promote pain transmission from the periphery to the spinal cord.

Pharmacokinetics

• Bioavailability: 89%
• Peak plasma concentration: 1221.9 ng/mL (tablet)
• Protein bound: 99.4%; primarily to albumin
• Metabolized in liver by CYP2C9 (major) and CYP3A4 (minor)
• Half-life: 15-20 hr (PO)
• Excretion: Equally excreted in urine and feces, mostly as metabolites

Administration

• Before starting therapy, ask patient about aspirin sensitivity and allergies to other NSAIDs. If patient is dehydrated, provide adequate fluids.

Adverse reactions

• CNS: headache, dizziness, syncope, malaise, fatigue, asthenia, depression, confusion, nervousness, drowsiness, insomnia, vertigo, tremor, paraesthesia, anxiety, seizures
• CV: hypertension, hypotension, palpitations, angina, vasculitis, heart failure, arrhythmias, MI
• EENT: abnormal vision, conjunctivitis, hearing loss, tinnitus, pharyngitis
• GI: nausea, vomiting, diarrhea, constipation, colitis, GI ulcers with perforation, abdominal pain, dyspepsia, gastroesophageal reflux, esophagitis, flatulence, ulcerative stomatitis, dry mouth, pancreatitis, GI hemorrhage
• GU: urinary frequency, urinary tract infection, albuminuria, hematuria, renal failure
• Hematologic: anemia, purpura, leukopenia, thrombocytopenia
• Hepatic: hepatitis
• Musculoskeletal: joint pain, back pain Metabolic: dehydration Respiratory: upper respiratory infection, dyspnea, coughing, asthma, bronchospasm
• Skin: rash, urticaria, pruritus, bullous eruption, sweating, alopecia, photosensitivity, angioedema
• Other: altered taste, increased appetite, weight gain or loss, hot flashes, fluid retention and edema, masking of infection symptoms, hypersensitivity reactions including anaphylaxis

Contraindications

• Hypersensitivity to drug, its components, or other NSAIDs

Precautions:

• Bleeding disorders, GI or cardiac disorders, severe renal impairment, severe hepatic disease, asthma, peptic ulcer disease
• Concurrent aspirin, oral anticoagulant, or corticosteroid therapy
• Elderly or debilitated patients
• Pregnant or breastfeeding patients.

Patient monitoring

• Closely monitor patient with aspirin-sensitivity asthma, because of risk of severe bronchospasm. 
• In prolonged therapy, monitor CBC and kidney and liver function tests. 
• Assess for cardiovascular disorders and hepatotoxicity.
• Monitor patient for fluid retention and weight gain.

Patient teaching

• Instruct patient to immediately report signs and symptoms of hepatotoxicity, including right upper quadrant pain, nausea, fatigue, lethargy, pruritus, and jaundice.
• Tell patient to report abdominal pain, blood in stool or emesis, or black tarry stools.
• Instruct patient to avoid alcohol and smoking.
• Caution pregnant patient to avoid drug, especially during third trimester.
• Tell patient to consult prescriber before taking over-the-counter preparations.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.

Nursing Considerations

• Use meloxicam with extreme caution in patients with history of ulcer disease or GI bleeding because NSAIDs such as meloxicam increase risk of GI bleeding and ulceration. Expect to use drug for shortest time possible in these patients.
• Be aware that serious GI tract ulceration, bleeding, and perforation may occur without warning symptoms. Elderly patients are at greater risk. To minimize risk, give drug with food and a full glass of water. If GI distress occurs, withhold drug and notify prescriber immediately.
• Use meloxicam cautiously in patients with hypertension and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
• Monitor patient—especially if elderly or taking meloxicam long-term—for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, hemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.
• Monitor liver function test results because, rarely, elevations may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.
•   Monitor BUN and serum creatinine levels in elderly patients; patients taking diuretics, angiotensin II receptor antagonists, or ACE inhibitors; and patients with heart failure, impaired renal function, or hepatic dysfunction; drug may cause renal failure.
• Monitor CBC for decreased hemoglobin and hematocrit. Drug may worsen anemia.
• Assess patient’s skin regularly for rash or other hypersensitivity reaction because meloxicam is an NSAID and may cause serious skin reactions without warning, even in patients with no history of NSAID sensitivity. At first sign of reaction, stop drug and notify prescriber.
• Monitor patient for adequate hydration before beginning meloxicam therapy to decrease risk of renal dysfunction.

REFERENCES

1. Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
2. McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
3. April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
4. Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
5. Nursebro.com, Search – Nursebro

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