Non-steroidal anti-inflammatory drugs (NSAIDS)-Diary heterocyclics Sulphonamides
- Celecoxib
1.Celecoxib
| Celecoxib |
| Availability Capsules: 50 mg, 100 mg, 200 mg, 400 mg |
| Indications and dosages ➣ Ankylosing spondylitis, osteoarthritis Adults: 200 mg/day P.O. as a single dose or 100 mg P.O. b.i.d. ➣ Rheumatoid arthritis Adults: 100 to 200 mg P.O. b.i.d. ➣ Adjunctive treatment in familial adenomatous polyposis to decrease the number of adenomatous colorectal polyps Adults: 400 mg P.O. b.i.d. ➣ Acute pain or primary dysmenorrhea Adults: 400 mg P.O. once, plus one additional 200 mg-dose as needed on first day; then 200 mg b.i.d. as needed ➣ Juvenile rheumatoid arthritis Children age 2 and older weighing 10 to 25 kg (22 to 55 lb): 50 mg P.O. b.i.d. Children age 2 and older weighing 25 kg or more: 100 mg P.O. b.i.d. |
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, diarrhoea, 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.
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
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