Nabumetone

Nabumetone Brand Names- Relafen | Relafen DS

What is Nabumetone

Nabumetone is an oral nonsteroidal anti-inflammatory drug (NSAID) of the acetic acid chemical class.

Nabumetone is a nonacidic prodrug that requires conversion to an active metabolite (6-MNA) for its anti-inflammatory, analgesic, and antipyretic activity.

Nabumetone is the only NSAID of the acetic acid class with a half-life long enough to support once daily administration.

Other NSAIDs that can be given as a single daily dose include piroxicam (enolic acid derivative) and oxaprozin (propionic acid derivative). Because the metabolites of 6-MNA are weak inhibitors of the COX enzyme and are renally excreted, nephrotoxicity of nabumetone relative to other NSAIDs is hypothesized to be less.

However, current data do not conclusively support or refute this hypothesis; more data are needed.

Nabumetone appears to inhibit cyclooxygenase-2 preferentially at low doses, but the preferential inhibition of cyclooxygenase-2 is diminished at higher doses.

All NSAIDs including nabumetone cause an increased risk of serious gastrointestinal adverse effects including bleeding, ulceration, and perforation of the stomach or intestines and may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke.

The lowest effective nabumetone dose for the shortest possible duration is recommended, as the risk for adverse effects may increase with duration of use.

Nabumetone was approved by the FDA in December 1991.

Indications

1. ankylosing spondylitis
2. osteoarthritis
3. rheumatoid arthritis

For the acute and chronic treatment of rheumatoid arthritis or osteoarthritis

Side Effects

1. abdominal pain
2. acne vulgaris
3. agitation
4. agranulocytosis
5. alopecia
6. anaphylactoid reactions
7. anemia
8. angina
9. angioedema
10. anorexia
11. anxiety
12. aplastic anemia
13. appetite stimulation
14. arrhythmia exacerbation
15. aseptic meningitis
16. asthenia
17. azotemia
18. blurred vision
19. bullous rash
20. chills
21. confusion
22. constipation
23. cough
24. cystitis
25. depression
26. diaphoresis
27. diarrhea
28. dizziness
29. dysgeusia
30. dyspepsia
31. dysphagia
32. dyspnea
33. dysuria
34. edema
35. elevated hepatic enzymes
36. eosinophilic pneumonia
37. eructation
38. erythema multiforme
39. esophageal stricture
40. esophageal ulceration
41. esophagitis
42. fatigue
43. fever
44. flatulence
45. gastritis
46. GI bleeding
47. GI perforation
48. gingivitis
49. glossitis
50. headache
51. heart failure
52. hematuria
53. hemolytic anemia
54. hepatic failure
55. hepatic necrosis
56. hepatitis
57. hyperglycemia
58. hyperkalemia
59. hypertension
60. hyperuricemia
61. hypokalemia
62. hyponatremia
63. impotence (erectile dysfunction)
64. infertility
65. insomnia
66. interstitial nephritis
67. jaundice
68. leukopenia
69. malaise
70. melena
71. myocardial infarction
72. nausea
73. nephrolithiasis
74. nephrotic syndrome
75. neutropenia
76. nightmares
77. odynophagia
78. oliguria
79. palpitations
80. pancreatitis
81. paresthesias
82. peptic ulcer
83. photosensitivity
84. platelet dysfunction
85. pneumonitis
86. polyuria
87. proteinuria
88. pruritus
89. pseudoporphyria
90. purpura
91. pyrosis (heartburn)
92. rash
93. renal failure (unspecified)
94. renal papillary necrosis
95. Stevens-Johnson syndrome
96. stomatitis
97. stroke
98. syncope
99. thrombocytopenia
100. thromboembolism
101. tinnitus
102. toxic epidermal necrolysis
103. tremor
104. urticaria
105. vaginal bleeding
106. vasculitis
107. vertigo
108. visual impairment
109. vomiting
110. weight gain
111. weight loss
112. xerostomia

Monitoring Parameters

• blood pressure
• serum creatinine/BUN

Contraindications

• acute bronchospasm
• acute myocardial infarction
• alcoholism
• anemia
• angina
• anticoagulant therapy
• asthma
• bone marrow suppression
• breast-feeding
• cardiac arrhythmias
• cardiac disease
• cerebrovascular disease
• chemotherapy
• children
• coagulopathy
• coronary artery bypass graft surgery (CABG)
• coronary artery disease
• corticosteroid therapy
• dehydration
• dental disease
• dental work
• diabetes mellitus
• geriatric
• GI bleeding
• GI disease
• GI perforation
• heart failure
• hematological disease
• hemophilia
• hepatic disease
• hypertension
• hypovolemia
• immunosuppression
• infertility
• intramuscular injections
• jaundice
• labor
• myocardial infarction
• nasal polyps
• neutropenia
• NSAID hypersensitivity
• obstetric delivery
• peptic ulcer disease
• peripheral edema
• peripheral vascular disease
• pregnancy
• renal disease
• renal failure
• renal impairment
• reproductive risk
• rheumatoid arthritis
• salicylate hypersensitivity
• stroke
• surgery
• systemic lupus erythematosus (SLE)
• tachycardia
• thrombocytopenia
• thromboembolism
• tobacco smoking
• ulcerative colitis
• urticaria

Interactions

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