Non –steroidal anti-inflammatory drugs (NSAIDS)-Acetic acids

Muscloskeletal Drugs

Name of the NSAIDS Drugs- Acetic Acids

  • Etodolac
  • Indomethacin
  • Ketorolac
  • Nabumetone
  • Sulindac
  • Tolmelin

1.Etodolac

Etodolac
Availability
Capsules: 200 mg, 300 mg Tablets: 400 mg, 500 mg Tablets (extended release): 400 mg, 500 mg, 600 mg
Indications and dosages
 ➣ Osteoarthritis; rheumatoid arthritis
Adults: 300 mg P.O. two or three times daily; or 400 mg, 500 mg, or 600 mg P.O. b.i.d.; or 400 to 1,000 mg P.O. (extended-release tablets) once daily
➣ Mild to moderate pain
Adults: 200 to 400 mg P.O. q 6 to 8 hours, not to exceed 1,200 mg/day
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 extendedrelease 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.

2.Indomethacin

Indomethacin
Availability
Capsules: 25 mg, 50 mg Capsules (sustained release): 75 mg Oral suspension: 25 mg/5 ml
Indications and dosages
 ➣ Rheumatoid arthritis; osteoarthritis; ankylosing spondylitis
Adults: 25 to 50 mg P.O. two or three times daily, not to exceed 200 mg daily; or one 75-mg sustained-release capsule P.O. once or twice daily
➣ Acute gouty arthritis
Adults: 50 mg P.O. t.i.d. until pain is tolerable; then reduce dosage rapidly and, finally, discontinue drug. Don’t give sustained-release form.
➣ Acute bursitis or tendinitis of shoulder
Adults: 75 to 150 mg P.O. daily in three or four divided doses. Discontinue once inflammation is controlled.
Mechanism of Action

Blocks activity of cyclooxygenase, the enzyme needed to synthesize prostaglandins, which mediate inflammatory response and cause local vasodilation, swelling, and pain. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID reduces inflammatory symptoms and helps relieve pain

Pharmacokinetics
  • Bioavailability: ~100%
  • Peak plasma time: 0.5-2 hr; 1.67 hr (Tivorbex)
  • Protein bound: 99%
  • Metabolized in liver
  • Half-life: 4.5 hr (prolonged in neonates)
  • Excretion: Urine (60%), feces (>33%)
Administration
  • Give with food, full glass of water, or antacids to reduce GI upset.
  • Don’t open or crush capsules.
  • For arthritis, give up to 100 mg of daily dose at bedtime as needed to reduce nighttime pain and morning stiffness.
  • Don’t give sustained-release form to patients with gouty arthritis.
Adverse reactions
  • CNS: headache, dizziness, drowsiness, fatigue, vertigo, depression, seizures
  • EENT: tinnitus
  • GI: nausea, vomiting, diarrhea, constipation, abdominal pain or cramps, dyspepsia, ulcers, GI bleeding
  • Other: allergic reactions including anaphylaxis
Contraindications
  • Hypersensitivity to drug, its components, or other NSAIDs
  • Active GI bleeding
  • Concurrent diflunisal use
Precautions :
  • Severe cardiovascular, renal, or hepatic disease
  • History of ulcer disease
  • Elderly patients
  • Pregnant or breastfeeding patients
  • Children ages 14 and younger (efficacy not established)
Patient monitoring
  • Assess for dizziness, drowsiness, headache, fatigue, and exacerbation of depression, epilepsy, or parkinsonism.
  • Monitor for drug efficacy, indicated by improved joint mobility, pain relief, and decreased inflammation.
  • Monitor urine output for marked reduction.
  • Watch for signs and symptoms of GI bleeding and ulcers.
Patient teaching
  • Tell patient to take with food, full glass of water, or antacid to reduce GI upset.
  • Advise patient not to open or crush capsules.
  • Inform breastfeeding patient that indomethacin enters breast milk and may cause seizures in infant. Advise her to use a different infant feeding method during therapy.
  • Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, balance, and alertness.
  • As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

Nursing Considerations

  • Use indomethacin with extreme caution in patients with history of ulcer disease or GI bleeding because NSAIDs such as indomethacin 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 oral indomethacin with food, a full glass of water (not suspension), or an antacid to reduce GI distress.
  • If GI distress occurs, withhold drug and notify prescriber immediately.
  • Use indomethacin cautiously in patients with hypertension, and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
  • Shake suspension well before giving it.
  • For arthritis, give up to 100 mg of daily dose (not E.R. capsules) at bedtime to reduce nighttime pain and morning stiffness.
  • Make sure suppository stays in rectum at least 1 hour to improve absorption.
  • To reconstitute I.V. form, add 1 to 2 ml of preservative-free sodium chloride for injection or preservative-free sterile water to vial. Solution made with 1 ml diluent contains 100 mcg (0.1 mg) indomethacin/0.1 ml. Solution made with 2 ml diluent contains 50 mcg (0.05 mg) indomethacin/0.1 ml. Use solution immediately because it contains no preservatives. Discard unused portion.
  • Be aware that scheduled I.V. doses may be withheld if infant or neonate has anuria or a significant decrease in urine output (less than 0.6 ml/kg/hr).
  • When using I.V. form, avoid extravasation to protect surrounding tissue.
  • Anticipate a second course (3 more doses) of I.V. indomethacin if patent ductus arteriosus fails to close or reopens. After two courses, surgery may be performed.
  • Monitor patient—especially if he’s elderly or receiving long-term indomethacin 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, 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, those taking diuretics or ACE inhibitors, and those 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 signs of rash or other hypersensitivity reaction because indomethacin 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.
  • Because indomethacin causes sodium retention, monitor weight and blood pressure, especially if patient has hypertension.
  • When drug is used to treat gouty arthritis, expect its action to peak in 24 to 36 hours and significant swelling to gradually disappear over 3 to 5 days.
  • Be aware that E.R. form shouldn’t be used to treat gouty arthritis.
  • Expect to use suppositories for patients who can’t swallow oral form.
  • To evaluate drug effectiveness, assess for reduced pain and inflammation and improved joint mobility.
  • Expect patient to have intermittent checkups during long-term therapy and an ophthalmologic examination if vision changes

3.Ketorolac

Ketorolac
Availability
Injection: 15 mg/ml in 1-ml preloaded syringes, 30 mg/ml in 1- and 2-ml preloaded syringes Ophthalmic solution: 0.4%, 0.5% Tablets: 10 mg
Indications and dosages
➣ Moderately severe acute pain
Adults younger than age 65: Initially, 30 mg I.V. or 60 mg I.M. as a single dose, or 30 mg I.M. or I.V. q 6 hours, not to exceed 120 mg/day. To switch to P.O. therapy, give 20 mg P.O. initially for patients who received single 30-mg I.V. or 60-mg I.M. dose, followed by 10 mg P.O. q 4 to 6 hours as needed (not to exceed 40 mg/day or 5 days). Children ages 2 to 16: 1 mg/kg I.M. as a single dose, to a maximum of 30 mg; or one dose of 0.5 mg/kg I.V., to a maximum of 15 mg
➣ Ocular itching caused by seasonal allergic conjunctivitis
Adults and children ages 3 and older: One drop of 0.5% ophthalmic solution (Acular) instilled into affected eye q.i.d.
➣ Postoperative ocular inflammation related to cataract extraction
Adults and children ages 3 and older: One drop of 0.5% ophthalmic solution (Acular) instilled into operative eye q.i.d., starting 24 hours after surgery and continuing for 2 weeks
 ➣ To reduce ocular pain, burning, or stinging after corneal refractive surgery
Adults and children ages 3 and older: One drop of 0.4% ophthalmic solution (Acular LS) instilled into operative eye q.i.d. for up to 4 day
Mechanism of Action

Blocks cyclooxygenase, an enzyme needed to synthesize prostaglandins. Prostaglandins mediate inflammatory response and cause local vasodilation, swelling, and pain. They also promote pain transmission from periphery to spinal cord. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID reduces inflammation and relieves pain

Pharmcokinetics
  • Bioavailability: 80-100%
  • Peak serum time: 1-3 min (IV); 30-60 min (IM); ~1 hr (PO)
  • Protein bound: >99%
  • Metabolized in liver
  • Half-life: 2-6 hr
  • Excretion: Urine (91%), feces (6%)
Adverse reactions
  • CNS: drowsiness, headache, dizziness
  • CV: hypertension EENT: tinnitus GI: nausea, vomiting, diarrhea, constipation, flatulence, dyspepsia, epigastric pain, stomatitis
  • Hematologic: thrombocytopenia
  • Skin: rash, pruritus, diaphoresis
  • Other: excessive thirst, edema, injection site pain
Contraindications
  • Hypersensitivity to drug, its components, aspirin, or other NSAIDs
  • Concurrent use of aspirin, other NSAIDs, or probenecid
  • Peptic ulcer disease
  • GI bleeding or perforation
  • Advanced renal impairment, risk of renal failure
  • Increased risk of bleeding, suspected or confirmed cerebrovascular bleeding, hemorrhagic diathesis, incomplete hemostasis
  • Prophylactic use before major surgery, intraoperative use when hemostasis is critical
  • Labor and delivery
  • Breastfeeding
Precautions :
  • Mild to moderate renal impairment, cardiovascular disease
  • Elderly patients
  • Pregnant patients
  • Children.
Patient monitoring
  • Monitor for adverse reactions, especially prolonged bleeding time and CNS reactions.
  • Check I.M. injection site for hematoma and bleeding.
  • Monitor fluid intake and output
Patient teaching
  • Inform patient that drug is meant only for short-term pain management.
  • Tell patient to immediately report bleeding and adverse CNS reactions.
  • Advise patient to minimize GI upset by eating small, frequent servings of healthy foods.
  • Instruct patient to avoid aspirin products and herbs during therapy.
  • Teach patient how to use eye drops, if prescribed.
  • Caution female patient not to take drug if she is breastfeeding.
  • Advise patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
  • As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

4.Nabumetone

Nabumetone
Availability
Tablet 500mg (generic),750mg (generic),1,000mg (Relafen DS)
Indications and dosages
Osteoarthritis
1000 mg orally once daily initially; maintenance: 1000-2000 mg/day orally in single daily dose or divided every 12 hours; not to exceed 2000 mg/day
Rheumatoid arthritis
1000 mg orally once daily initially; maintenance: 1000-2000 mg/day orally in single daily dose or divided every 12 hours; not to exceed 2000 mg/day
Mechanism of Action

Inhibits synthesis of prostaglandins in body tissues by inhibiting at least 2 cyclooxygenase (COX) isoenzymes, COX-1 and COX-2. May inhibit chemotaxis, alter lymphocyte activity, decrease proinflammatory cytokine activity, and inhibit neutrophil aggregation; these effects may contribute to anti-inflammatory activity

Pharmacokinetics
  • Peak serum time: 2-4 hr (PO)
  • Protein bound: >99%
  • Metabolized in liver
  • Half-life: 24 hr (6-MNA)
  • Dialyzable: No
  • Excretion: Urine (80%), feces (9%)
Administration

Oral Administration

May take with or without food

Contraindications
  • Absolute: Aspirin allergy, severe renal impairment; perioperative   pain in the setting of coronary artery bypass graft (CABG) surgery
  • Relative: duodenal /gastric/peptic ulcer, stomatitis, systemic lupus erythematosus, ulcerative colitis , late pregnancy (may cause premature closure of ductus arteriosus)
Cautions
  • Use caution in asthma (bronchial), bleeding disorders, cardiac disease, hepatic impairment, hypertension, and renal impairment
  • May not be sufficiently activated in patients with hepatic dysfunction; use with caution
  • Long-term administration of nonsteroidal anti-inflammatory drugs (NSAIDs) may result in renal papillary necrosis and another renal injury; patients at greatest risk include elderly individuals, those with impaired renal function, hypovolemia, heart failure, liver dysfunction, or salt depletion, and those taking diuretics, angiotensin-converting enzyme inhibitors, or angiotensin-receptor blockers
  • Risk of serious gastrointestinal (GI) toxicity, including bleeding, ulcers, and perforation
  • May cause drowsiness, dizziness, blurred vision, and other neurologic effects
  • May decrease platelet adhesion and aggregation, prolonging bleeding time; monitor closely patients with a history of coagulation disorders
  • May increase risk of hyperkalaemia
  • May cause photosensitivity reactions
  • Severe skin reactions may occur; discontinue use at the first sign of rash

5.Sulindac

Sulindac
Availability
Tablet 150mg,200mg
Indications and Dosages
To decrease pain and inflammation in ankylosing spondylitis, acute attacks of gout or pseudogout, bursitis, moderately painful arthralgia, osteoarthritis, rheumatoid arthritis, and tendinitis
TABLETS Adults and adolescents over age 14. Initial: 150 to 200 mg b.i.d., adjusted based on patient’s response. Maximum: 200 mg b.i.d
To relieve symptoms of acute gouty arthritis, acute subacromial bursitis, and supraspinatus tendinitis
 TABLETS Adults and adolescents over age 14. 200 mg b.i.d. for 7 to 14 days; decreased to lowest effective dosage after satisfactory response
Mechanism of Action

May block the activity of cyclooxygenase, an enzyme needed to synthesize prostaglandins, which mediate the inflammatory response and cause local vasodilation, swelling, and pain. By blocking cyclooxygenase and inhibiting prostaglandins, this NSAID reduces inflammatory symptoms and pain.

Pharmacokinetics
  • Half-life: Sulindac (8 hr); sulfide metabolite (16.4 hr)
  • Peak Plasma Time: 2 hr (sulindac); 5-6 hr (sulfide metabolites)
  • Concentration: 3-6 mcg/mL
  • Excretion: Urine (50%); feces (25%)
  • Bioavailability: 90%
  • Protein Bound: Approx 93% (sulindac); approx 98% (sulfide metabolite)
  • Metabolism: Hepatic reduction; significant enterohepatic circulation
  • Enzymes inhibited: Cyclooxygenase
Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria induced by aspirin, iodides, or other NSAIDs

Adverse Reactions
  • CNS: Aseptic meningitis, cerebral hemorrhage, chills, drowsiness, fever, headache, ischemic stroke, malaise, nervousness, transient ischemic attack
  • CV: Deep vein thrombosis, edema, heart failure, hypertension, MI, palpitations, peripheral edema, vasculitis
  • EENT: Tinnitus
  • ENDO: Hypoglycemia
  • GI: Abdominal cramps or pain, anorexia, constipation, diarrhea, esophageal irritation, flatulence, gastritis, gastrointestinal bleeding or ulceration, hepatic failure, hepatitis, hepatotoxicity, indigestion, jaundice, liver failure, nausea, perforation of stomach or intestines, vomiting
  • GU: Acute renal failure, decreased urine output, interstitial nephritis, nephrotic syndrome, polyuria, proteinuria
  • HEME: Agranulocytosis, aplastic anemia, leukopenia, pancytopenia
  • RESP: Bronchial spasm, dyspnea, pulmonary edema, wheezing
  • SKIN: Diaphoresis, erythema multiforme, exfoliative dermatitis, maculopapular rash, pruritus, purpura, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria
  • Other: Anaphylaxis, angioedema, facial edema, hypersensitivity syndrome

Nursing Considerations

  • Use sulindac with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as sulindac increased risk of GI bleeding and ulceration. Expect to use sulindac for the 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. If GI distress occurs, withhold drug and notify prescriber at once
  • Use sulindac cautiously in patients with hypertension and monitor blood pressure closely throughout therapy. Drug may cause hypertension or worsen it.
  • If patient has systemic lupus erythematosus and mixed connective tissue disease, monitor him closely because sulindac increases the risk of aseptic meningitis.
  • Especially if patient is elderly or taking sulindac long-term, watch for less common but serious adverse GI reactions, including anorexia, constipation, diverticulitis, dysphagia, esophagitis, gastritis, gastroenteritis, gastroesophageal reflux disease, haemorrhoids, hiatal hernia, melena, stomatitis, and vomiting.
  • Monitor liver function test results because, in rare cases, elevated levels may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.
  • Watch BUN and serum creatinine levels in elderly patients; those with heart failure, impaired renal function, or hepatic dysfunction; and those taking diuretics or ACE inhibitors, because drug may cause renal failure.
  • Monitor CBC for decreased haemoglobin and haematocrit because drug may worsen anemia.
  • Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction because sulindac 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.
  • Expect patient to undergo audiometric examinations before and periodically during prolonged therapy, as ordered.
  • Monitor patient for evidence of hypersensitivity syndrome, which could become life-threatening. Report multiple occurring and multi-organ adverse reactions to prescriber and expect drug to be discontinued. Be prepared to provide emergency supportive care, as ordered.
Patient Teaching
  • Instruct patient to take sulindac exactly as prescribed. Explain that higher doses don’t increase effectiveness and may increase risk of adverse reactions.
  • Advise patient to crush tablet and mix with food, if needed, to aid in swallowing.
  • Instruct patient to take drug with or immediately after meals to decrease GI distress, to take with a full glass of water, and to remain upright for 20 to 30 minutes after administration to prevent drug from lodging in esophagus and causing esophageal irritation.
  • Urge patient to notify prescriber immediately of chills, fever, rash, or sweating, which may indicate hypersensitivity.
  • Advise patient to consult prescriber before using acetaminophen, alcohol, aspirin, other NSAIDs, or any OTC drugs during sulindac therapy.
  • Caution patient to avoid hazardous activities until drug’s CNS effects are known.
  • Explain the need for periodic physical examinations and laboratory tests during prolonged therapy to monitor drug effectiveness.
  • Inform patient that sulindac may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.
  • Tell patient that sulindac also may increase the risk of serious adverse GI reactions; stress the need to seek immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.
  • Alert patient to the possibility of rare but serious hypersensitivity reactions. Urge him to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity
Cautions
  • Use caution in asthma (bronchial), cardiac disease, congestive heart failure, hepatic impairment, hypertension, renal impairment.
  • Long-term administration of NSAIDs may result in renal papillary necrosis and other renal injury; patients at greatest risk include the elderly, or those with impaired renal function, hypovolemia, heart failure, liver dysfunction, salt depletion, and individuals taking diuretics, ACE inhibitors, or ARBs.

6.Tolmetin

Tolmetin
Availability
Tablet 600mg Capsule 400mg
Indications and Dosages
To relieve moderate pain from rheumatoid arthritis and osteoarthritis
CAPSULES, TABLETS Adults. Initial: 400 mg t.i.d. Maintenance: 600 to 1,800 mg daily in divided doses t.i.d. or q.i.d. Maximum: 2,000 mg daily for rheumatoid arthritis, 1,600 mg daily for osteoarthritis.
To treat juvenile rheumatoid arthritis
CAPSULES, TABLETS Children over age 2. Initial: 20 mg/kg daily in divided doses t.i.d. or q.i.d. Maintenance: 15 to 30 mg/kg daily in divided doses. Maximum: 30 mg/kg daily.
Mechanism of Action

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

Pharmacokinetics
  • Peak Plasma Time: 30-60 min
  • Onset of action: 1-2hr
  • Half-life elimination: 1 hr
  • Protein Bound: 99%
  • Metabolism: Liver oxidation
  • Excretion: Urine (approx 100%)
Contraindications

Angioedema, asthma, bronchospasm, nasal polyps, rhinitis, or urticaria caused by aspirin, iodides, or other NSAIDs

Cautions
  • Use caution in asthma (bronchial), cardiac disease, CHF, hepatic impairment, HTN, renal impairment
  • Long-term administration of NSAIDs may result in renal papillary necrosis and other renal injury; patients at greatest risk include the elderly, or those with impaired renal function, hypovolemia, heart failure, liver dysfunction, salt depletion, and individuals taking diuretics, ACE inhibitors, or ARBs
  • Strong cross-sensitivity may exist for ASA allergic patients
  • Food reduces bioavailability
  • Heart Failure (HF) risk
  • NSAIDS have the potential to trigger HF by prostaglandin inhibition that leads to sodium and water retention, increased systemic vascular resistance, and blunted response to diuretics
  • NSAIDS should be avoided or withdrawn whenever possible
  • AHA/ACC Heart Failure Guidelines; Circulation. 2016; 134
Adverse Reactions
  • CNS: Aseptic meningitis, cerebral hemorrhage, ischemic stroke, depression, dizziness, drowsiness, fatigue, headache, transient ischemic attack, weakness
  • CV: Chest pain, deep vein thrombosis, edema, hypertension, MI, peripheral edema
  • EENT: Tinnitus
  • ENDO: Hypoglycemia
  • GI: Abdominal pain; constipation; diarrhea; elevated liver function test results; flatulence; gastritis; GI bleeding, perforation, or ulceration; hepatitis; indigestion; jaundice; liver failure; nausea; peptic ulcer disease; vomiting
  • GU: Acute renal failure, dysuria, elevated BUN level, hematuria, interstitial nephritis, nephrotic syndrome, nephrotoxicity, proteinuria, UTI
  • HEME: Agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, pancytopenia, prolonged bleeding time
  • SKIN: Erythema multiforme, exfoliative dermatitis, maculopapular rash, Stevens Johnson syndrome, toxic epidermal necrolysis, urticaria
  • Other: Anaphylaxis, angioedema, weight gain or loss

Nursing Considerations

  • Give tolmetin with food or milk to reduce adverse GI reactions.
  • Assess patient for improvement within 7 days and progressive improvement over several successive weeks.
  • Use tolmetin with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as tolmetin increase the risk of GI bleeding and ulceration. Expect to use tolmetin for the 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. If GI distress occurs, withhold drug and notify prescriber at once.
  • Use tolmetin 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 tolmetin 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 because, rarely, elevated levels may progress to severe hepatic reactions, including fatal hepatitis, liver necrosis, and hepatic failure.
  • Monitor BUN and serum creatinine levels in patients with heart failure, impaired renal function, or hepatic dysfunction; those taking diuretics or ACE inhibitors; and elderly patients because drug may cause renal failure.
  • Monitor CBC for decreased hemoglobin and hematocrit because drug may worsen anemia.
  • Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction because tolmetin 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.
  • Assess invasive sites or wounds for bleeding and bruising from drug’s effects on platelets.
Patient Teaching
  • Tell patient to take drug with food or milk.
  • Urge patient to limit sodium intake because drug may cause fluid retention.
  • Tell patient to avoid alcohol during therapy.
  • Teach patient how to perform proper oral hygiene and advise her to have needed dental work done before tolmetin therapy starts because of the increased risk of bleeding.
  • Explain that tolmetin may increase the risk of serious adverse cardiovascular reactions; urge patient to seek immediate medical attention if signs or symptoms arise, such as chest pain, shortness of breath, weakness, and slurring of speech.
  • Tell patient that tolmetin also may increase the risk of serious adverse GI reactions; stress the need to seek immediate medical attention for such signs and symptoms as epigastric or abdominal pain, indigestion, black or tarry stools, or vomiting blood or material that looks like coffee grounds.
  • Alert patient to the possibility of rare but serious skin reactions. Urge her to seek immediate medical attention for rash, blisters, itching, fever, or other indications of hypersensitivity

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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