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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
- abdominal pain
- acute generalized exanthematous pustulosis (AGEP)
- acute respiratory distress syndrome (ARDS)
- agitation
- agranulocytosis
- alopecia
- amblyopia
- amnesia
- anemia
- anorexia
- aplastic anemia
- apnea
- arthralgia
- asthenia
- azotemia
- bleeding
- bradycardia
- bronchospasm
- bullous rash
- cardiac arrest
- cataracts
- chills
- cholestasis
- confusion
- conjunctivitis
- constipation
- depression
- diaphoresis
- diarrhea
- disseminated intravascular coagulation (DIC)
- dizziness
- drowsiness
- Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
- dysgeusia
- dyspepsia
- dystonic reaction
- ecchymosis
- edema
- elevated hepatic enzymes
- eosinophilia
- epistaxis
- erythema multiforme
- exfoliative dermatitis
- fever
- flatulence
- flushing
- gastritis
- GI bleeding
- GI obstruction
- glomerulonephritis
- glycosuria
- gynecomastia
- headache
- heart failure
- hematuria
- hemolytic anemia
- hepatic failure
- hepatic necrosis
- hepatitis
- hepatomegaly
- hyperbilirubinemia
- hypercalcemia
- hyperglycemia
- hyperkalemia
- hyperlipidemia
- hypernatremia
- hyperphosphatemia
- hypertension
- hyperuricemia
- hypervolemia
- hypocalcemia
- hypokalemia
- hypomagnesemia
- hyponatremia
- hypotension
- hypotonia
- impotence (erectile dysfunction)
- infection
- infertility
- injection site reaction
- insomnia
- interstitial nephritis
- iritis
- jaundice
- lactic acidosis
- leukocytosis
- leukopenia
- libido decrease
- lichen planus-like eruption
- lymphadenopathy
- lymphocytosis
- maculopapular rash
- malaise
- metabolic acidosis
- muscle paralysis
- myalgia
- myoclonia
- myopathy
- nausea
- nephrolithiasis
- neuritis
- neutropenia
- oliguria
- onycholysis
- optic neuritis
- pancreatitis
- pancytopenia
- paresthesias
- pericarditis
- peripheral neuropathy
- pharyngitis
- phlebitis
- proctitis
- proteinuria
- pruritus
- pulmonary embolism
- purpura
- rash
- renal failure (unspecified)
- respiratory arrest
- rhinitis
- seizures
- splenomegaly
- Stevens-Johnson syndrome
- stomatitis
- stroke
- tachypnea
- thrombocytopenia
- tinnitus
- toxic epidermal necrolysis
- tremor
- tumor lysis syndrome (TLS)
- urticaria
- vasculitis
- ventricular fibrillation
- vertigo
- vomiting
- 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