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

Name of the NSAIDS Drugs- Enolic Acids

  • Piroxicam
  • Meloxicam

1. Piroxicam

Piroxicam
Availability
Capsules: 10 mg, 20 mg
Indications and dosages
➣ Inflammatory disorders (such as arthritis)
 Adults: 20 mg P.O. daily as a single dose or in two divided doses
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 blocking cyclooxygenase activity and inhibiting prostaglandins, this NSAID reduces inflammatory symptoms and pain

Pharmacokinetics
  • Half-life: 14-158 hr (average 50 hr)
  • Onset: 15-30 min (single 20 mg dose); 1 hr (multiple 20 mg doses)
  • Protein Bound: 99.3% (with plasma concentrations 5-30 mcg/mL)
  • Metabolism: hydroxylation at the 5 position of the pyridyl side chain; conjugation by cyclodehydration, hydrolysis of: amide linkage, decarboxylation, ring contraction, N-demethylation
  • Excretion: urine, feces
Administration
  • Give with milk, antacids, or food to minimize GI upset.
Adverse reactions
  • CNS: headache, drowsiness, dizziness
  • CV: Edema, hypertension, vasculitis, tachycardia, arrhythmias
  • EENT: blurred vision, tinnitus
  • GI: nausea, vomiting, diarrhoea, constipation, abdominal pain, flatulence, dyspepsia, anorexia, severe GI bleeding
  • GU: proteinuria, renal failure Hematologic: anaemia, blood dyscrasias Hepatic: jaundice, hepatitis
  • Skin: rash
  • Other: allergic reactions including anaphylaxis
Contraindications
  • Hypersensitivity to drug or other NSAIDs (including aspirin)
  • Active GI bleeding or ulcer disease
  • Third trimester of pregnancy
Precautions:
  • renal impairment, severe cardiovascular or hepatic disease
  • history of ulcer disease
  • pregnant patients in first or second trimester
  • breastfeeding patients (not recommended)
  •   children (safety not established).
Patient monitoring
  • Monitor vital signs and cardiovascular status. Stay alert for hypertension and arrhythmias.
  • Monitor kidney and liver function tests, hearing, and CBC.
  • Watch for signs and symptoms of drug-induced hepatitis and GI toxicity, including ulcers and bleeding.
  • Monitor for signs and symptoms of infection, which drug may mask.
Patient teaching
  • Advise patient to take with milk, antacids, or food to minimize GI upset.
  • Tell patient drug may mask signs and symptoms of infection. Instruct him to contact prescriber if he suspects he has an infection.
  • Teach patient to recognize and immediately report signs and symptoms of allergic reaction or GI bleeding.
  • Inform patient that many herbs increase the risk of GI bleeding. Caution him not to use herbs without prescriber’s approval.
  • Instruct patient to drink plenty of fluids and to report decreased urination.
  • Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
  • Tell female patient to inform prescriber if she is pregnant or breastfeeding.
  • 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

  • Administer piroxicam with food to decrease GI upset.
  • Use piroxicam with extreme caution in patients with a history of ulcer disease or GI bleeding because NSAIDs such as piroxicam increase risk of GI bleeding and ulceration. Expect to use piroxicam 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 piroxicam 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 drug 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 level and hematocrit because drug may worsen anemia.
  • Assess patient’s skin routinely for rash or other signs of hypersensitivity reaction because piroxicam 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.

2.Meloxicam

Meloxicam
Availability
Oral suspension: 7.5 mg/5 ml Tablets: 7.5 mg, 15 mg
Indications and dosages
➣ Osteoarthritis; rheumatoid arthritis
Adults: 7.5 mg P.O. once daily; may increase to 15 mg/day
➣ Juvenile arthritis
 Children ages 2 and older: 0.125 mg/kg P.O. once daily, up to a maximum of 7.5 mg
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.

Pharmcokinetics
  • 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, paresthesia, 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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