Allopurinol

Allopurinol Brand Names- Aloprim | Zyloprim

What is Allopurinol

Allopurinol is a structural analog of the natural purine base, hypoxanthine and is a xanthine oxidase inhibitor (XOI), a type of uric acid-lowering therapy (ULT).

Allopurinol is used in the prevention of gout, renal calculi due to either uric acid or calcium oxalate, and in the prophylaxis and treatment of uric acid nephropathy.

In addition, allopurinol is indicated for the prophylaxis of hyperuricemia and its complications associated with radiation and chemotherapy treatment of leukemia, lymphoma, other myeloproliferative disorders, and some solid tumors.

For chronic gout management, the American College of Rheumatology (ACR) and the European League Against Rheumatism (EULAR) guidelines recommend ULT to achieve a target serum uric acid (sUA) level of less than 6 mg/dL to prevent the formation of crystals and to eliminate crystal deposition, thereby dissolving tophi; a lower target (less than 5 mg/dL) is recommended for patients with severe disease.

Allopurinol is usually the first-line treatment agent due to effectiveness and cost considerations, unless contraindications exist. ULTs such as allopurinol are considered more effective than probenecid at achieving treatment goals and are considered less likely to promote uric acid nephrolithiasis.

Allopurinol and febuxostat appear relatively similar as monotherapy in lowering serum urate concentrations and reducing gout flares with long-term (more than 1 year) of use.

Treatment guidelines recommend combination therapy with a uricosuric (e.g., lesinurad) plus a xanthine oxidase inhibitor (XOI) when treatment goals are not met with an XOI alone; use of pegloticase is usually reserved for severe, refractory chronic gout.

The most common adverse event with allopurinol is rash, and fatal hypersensitivity reactions have been reported. Persons with the HLA-B*5801 haplotype, which is prevalent in some Asian populations, are more likely to experience serious side effects with the drug.

Allopurinol can also be quite toxic if doses are not adjusted for renal dysfunction.

Indications

  • gout
  • gouty arthritis
  • hyperuricemia
  • nephrolithiasis
  • renal calculus
  • uric acid nephropathy

For the treatment of signs and symptoms of primary or secondary gout (i.e., acute attacks, tophi, gouty arthritis or joint destruction, uric acid lithiasis, and/or uric acid nephropathy)

Side Effects

  1. abdominal pain
  2. acute generalized exanthematous pustulosis (AGEP)
  3. acute respiratory distress syndrome (ARDS)
  4. agitation
  5. agranulocytosis
  6. alopecia
  7. amblyopia
  8. amnesia
  9. anemia
  10. anorexia
  11. aplastic anemia
  12. apnea
  13. arthralgia
  14. asthenia
  15. azotemia
  16. bleeding
  17. bradycardia
  18. bronchospasm
  19. bullous rash
  20. cardiac arrest
  21. cataracts
  22. chills
  23. cholestasis
  24. confusion
  25. conjunctivitis
  26. constipation
  27. depression
  28. diaphoresis
  29. diarrhea
  30. disseminated intravascular coagulation (DIC)
  31. dizziness
  32. drowsiness
  33. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
  34. dysgeusia
  35. dyspepsia
  36. dystonic reaction
  37. ecchymosis
  38. edema
  39. elevated hepatic enzymes
  40. eosinophilia
  41. epistaxis
  42. erythema multiforme
  43. exfoliative dermatitis
  44. fever
  45. flatulence
  46. flushing
  47. gastritis
  48. GI bleeding
  49. GI obstruction
  50. glomerulonephritis
  51. glycosuria
  52. gynecomastia
  53. headache
  54. heart failure
  55. hematuria
  56. hemolytic anemia
  57. hepatic failure
  58. hepatic necrosis
  59. hepatitis
  60. hepatomegaly
  61. hyperbilirubinemia
  62. hypercalcemia
  63. hyperglycemia
  64. hyperkalemia
  65. hyperlipidemia
  66. hypernatremia
  67. hyperphosphatemia
  68. hypertension
  69. hyperuricemia
  70. hypervolemia
  71. hypocalcemia
  72. hypokalemia
  73. hypomagnesemia
  74. hyponatremia
  75. hypotension
  76. hypotonia
  77. impotence (erectile dysfunction)
  78. infection
  79. infertility
  80. injection site reaction
  81. insomnia
  82. interstitial nephritis
  83. iritis
  84. jaundice
  85. lactic acidosis
  86. leukocytosis
  87. leukopenia
  88. libido decrease
  89. lichen planus-like eruption
  90. lymphadenopathy
  91. lymphocytosis
  92. maculopapular rash
  93. malaise
  94. metabolic acidosis
  95. muscle paralysis
  96. myalgia
  97. myoclonia
  98. myopathy
  99. nausea
  100. nephrolithiasis
  101. neuritis
  102. neutropenia
  103. oliguria
  104. onycholysis
  105. optic neuritis
  106. pancreatitis
  107. pancytopenia
  108. paresthesias
  109. pericarditis
  110. peripheral neuropathy
  111. pharyngitis
  112. phlebitis
  113. proctitis
  114. proteinuria
  115. pruritus
  116. pulmonary embolism
  117. purpura
  118. rash
  119. renal failure (unspecified)
  120. respiratory arrest
  121. rhinitis
  122. seizures
  123. splenomegaly
  124. Stevens-Johnson syndrome
  125. stomatitis
  126. stroke
  127. tachypnea
  128. thrombocytopenia
  129. tinnitus
  130. toxic epidermal necrolysis
  131. tremor
  132. tumor lysis syndrome (TLS)
  133. urticaria
  134. vasculitis
  135. ventricular fibrillation
  136. vertigo
  137. vomiting
  138. water intoxication

Monitoring Parameters

  • CBC with differential
  • LFTs
  • serum creatinine/BUN
  • serum uric acid

Contraindications

  • anticoagulant therapy
  • bone marrow suppression
  • breast-feeding
  • driving or operating machinery
  • hepatic disease
  • hepatotoxicity
  • infants
  • pregnancy
  • renal disease
  • renal failure
  • renal impairment
  • serious rash

Interactions

  • Aluminum Hydroxide
  • Aluminum Hydroxide; Magnesium Carbonate
  • Aluminum Hydroxide; Magnesium Hydroxide
  • Aluminum Hydroxide; Magnesium Hydroxide; Simethicone
  • Aluminum Hydroxide; Magnesium Trisilicate
  • Amoxicillin
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amoxicillin; Clavulanic Acid
  • Ampicillin
  • Ampicillin; Sulbactam
  • Azathioprine
  • Capecitabine
  • Chlorpropamide
  • Colchicine; Probenecid
  • Cyclosporine
  • Diazoxide
  • Dichlorphenamide
  • Didanosine, ddI
  • Floxuridine
  • Fluorouracil, 5-FU
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Mercaptopurine, 6-MP
  • Methotrexate
  • Methoxsalen
  • Omeprazole; Amoxicillin; Rifabutin
  • Pegloticase
  • Pexidartinib
  • Probenecid
  • Pyrazinamide, PZA
  • Riluzole
  • Sulfinpyrazone
  • Theophylline, Aminophylline
  • Thiazide diuretics
  • Uricosuric Agents
  • Warfarin
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