- March 15, 2022
- Newsletter
- 617-430-5616
Menu
Brand Name :
Zyloprim, Aloprim
Synonyms :
Allopurinol
Class :
Xanthine oxidase inhibitors, Antigout agents
Dosing forms and strengths
Tablet
(100 mg)
(300 mg)
Dosage forms and strengths
Tablet
(100 mg)
(300 mg)
Refer adult Dosing
Interaction with allopurinol may enhance the allergic reaction to ampicillin.
may diminish the serum concentration when combined
aluminum hydroxide/magnesium carbonate
may diminish the serum concentration of Aluminum Hydroxide
allopurinol enhances the effects of warfarin by anti-coagulation
allopurinol increases the effect of anticoagulation of vitamin K antagonists
allopurinol increases the effect of anticoagulation of vitamin K antagonists
allopurinol increases the effect of anticoagulation of vitamin K antagonists
allopurinol increases the effect of anticoagulation of vitamin K antagonists
allopurinol increases the effect of anticoagulation of vitamin K antagonists
increases the risk of myelosuppression by decreasing the metabolism of azathioprine
may reduce the plasma concentration of allopurinol
ACE Inhibitors may enhance the potential for allergic or hypersensitivity reactions to allopurinol
ACE Inhibitors may enhance the potential for allergic or hypersensitivity reactions to allopurinol
ACE Inhibitors may enhance the potential for allergic or hypersensitivity reactions to allopurinol
ACE Inhibitors may enhance the potential for allergic or hypersensitivity reactions to allopurinol
ACE Inhibitors may enhance the potential for allergic or hypersensitivity reactions to allopurinol
loop diuretics may increase the risk of adverse effect of allopurinol
loop diuretics may increase the risk of adverse effect of allopurinol
loop diuretics may increase the risk of adverse effect of allopurinol
may increase the allergic or hypersensitivity reactions to thiazide diuretics
may increase the allergic or hypersensitivity reactions to thiazide diuretics
may increase the allergic or hypersensitivity reactions to thiazide diuretics
may increase the allergic or hypersensitivity reactions to thiazide diuretics
may have an increased allergic or hypersensitivity reactions when combined with allopurinol
may have an increased allergic or hypersensitivity reactions when combined with allopurinol
may have an increased allergic or hypersensitivity reactions when combined with allopurinol
may have an increased allergic or hypersensitivity reactions when combined with allopurinol
may have an increased allergic or hypersensitivity reactions when combined with allopurinol
It may enhance the adverse effects when combined with pegloticase
allopurinol: they may increase the potential for allergic or hypersensitivity reactions to amoxicillin
meticrane has the potential to enhance the rate of excretion of allopurinol; this can potentially lead to decreased levels of serum, possibly diminishing its effectiveness
it may diminish the excretion rate when combined with antibiotics, resulting in an enhanced serum level
it may diminish the excretion rate when combined with antibiotics, resulting in an enhanced serum level
it may diminish the excretion rate when combined with antibiotics, resulting in an enhanced serum level
the toxicity of cyclophosphamide increases by decreasing metabolism.
the metabolism is decreased by allopurinol, and the activity of mercaptopurine is increased risk of infection increases on administering both the drugs simultaneously
lansoprazole amoxicillin and clarithromycin
when amoxicillin combines with allopurinol it decreases the effects of the drug by resulting hypersensitivity reaction
amoxicillin and clavulanate potassium
when amoxicillin combines with allopurinol it decreases the effects of the drug by resulting hypersensitivity reaction
omeprazole amoxicillin and clarithromycin
when both drugs are combined, there may be a decreased effect of the drug's action by decreasing renal clearance
when both drugs are combined, there may be a decreased effect of the drug's action by decreasing renal clearance
it may diminish the excretion rate when combined with xanthine derivatives, resulting in an enhanced serum level
it may diminish the excretion rate when combined with xanthine derivates, resulting in an enhanced serum level
it may diminish the excretion rate when combined with xanthine derivates, resulting in an enhanced serum level
it may diminish the excretion rate when combined with xanthine derivates, resulting in an enhanced serum level
it may diminish the excretion rate when combined with zinc compounds, resulting in an enhanced serum level
it may diminish the excretion rate when combined with zinc compounds, resulting in an enhanced serum level
it may diminish the excretion rate when combined with zinc compounds, resulting in an enhanced serum level
it may diminish the excretion rate when combined with zinc compounds, resulting in an enhanced serum level
it may diminish the excretion rate when combined with zinc compounds, resulting in an enhanced serum level
When bacampicillin combines with allopurinol, there may be chance of increased risk of rash on skin.
Actions and Spectrum:
allopurinol works on enzyme inhibition mechanism. By inhibiting xanthine oxidase, allopurinol reduces the production of uric acid, leading to lower levels of uric acid in the blood and decreased formation of urate crystals that cause gouty attacks.
The Spectrum of Activity: allopurinol effectively lowers uric acid levels in the blood and prevents acute gout attacks in patients with hyperuricemia. It also manages uric acid overproduction associated with certain conditions, such as Lesch-Nyhan syndrome and tumor lysis syndrome.
Frequency defined
Adults
1-10%
Renal failure (1.2%)
Vomiting (1.2%)
Rash (1.5%)
Nausea (1.3%)
Frequency not defined
1-10%
Macular retinitis
Malaise
Neuritis
Pharyngitis
Ecchymosis
Electrolyte abnormalities
Epistaxis
Foot drop
Haematuria
Pruritus
Skin edema
Black Box Warning:
allopurinol is associated with severe and potentially life-threatening skin reactions (SJS).
allopurinol can also cause other hypersensitivity reactions, including fever, rash, eosinophilia, and other systemic symptoms.
allopurinol should be used cautiously as these conditions may enhance the risk of severe skin reactions and hypersensitivity disorders.
Contraindication/Caution:
Hypersensitivity: allopurinol is contraindicated in individuals with known hypersensitivity or allergic reactions to allopurinol or its components.
Severe Liver or KidneyDisease: allopurinol is restricted in disorders associated with liver and kidney, as it may further impair liver or kidney function.
Concurrent Use with azathioprine or Mercaptopurine: allopurinol is contraindicated in patients receiving azathioprine or mercaptopurine, as it can inhibit the metabolism of these medications and increase their toxicity.
Children Under 6 Years of Age: allopurinol is restricted under this age group, as safety and efficacy in this age group have not been established.
Pregnancy and Breastfeeding: allopurinol should be used with caution in pregnant or breastfeeding individuals.
Pregnancy warnings:
Pregnancy category: N/A
Lactation: Excreted into human milk is unknown
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
<b>Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
xanthine oxidase inhibitors play a crucial role in reducing the production of uric acid in the body.
Pharmacodynamics:
allopurinol is a xanthine oxidase inhibitor that exerts its pharmacodynamic effects by reducing the production of uric acid, a waste product of purine metabolism. allopurinol is a prodrug converted to its active metabolite, oxypurinol, which is responsible for its pharmacological actions.
MOA:
The mechanism of action of allopurinol involves its conversion into the active metabolite, oxypurinol, which is a potent xanthine oxidase inhibitor. oxypurinol competes with hypoxanthine and xanthine for the active site of xanthine oxidase, inhibiting the enzyme’s activity.
Pharmacokinetics:
Absorption
allopurinol is well absorbed from the gastrointestinal tract after oral administration. However, food may delay its absorption, so it is recommended to take allopurinol on an empty stomach for optimal absorption.
Distribution
allopurinol is widely distributed throughout the body, with a volume of distribution of approximately 1.6 L/kg. It is highly protein-bound (over 90%) to plasma proteins, primarily albumin.
Metabolism
allopurinol undergoes extensive hepatic metabolism in the liver, primarily by the enzyme xanthine oxidase, to its active metabolite, oxypurinol (alloxanthine). oxypurinol is responsible for the majority of the pharmacological effects of allopurinol.
Elimination and Excretion
allopurinol and its metabolites are primarily excreted in the urine. Approximately 20% of the administered dose is excreted unchanged in the urine, while most are excreted as oxypurinol. The elimination half-life of allopurinol is approximately 1-2 hours, while the elimination half-life of oxypurinol is more prolonged, ranging from 13 to 30 hours
Administration:
allopurinol is available in oral tablet form and should be taken as a healthcare professional prescribes.
Taking allopurinol with food or immediately after a meal is recommended to minimize the risk of stomach upset.
For patients with kidney impairment, the dosage of allopurinol may need to be adjusted to prevent the accumulation of the medication in the body.
Patient information leaflet
Generic Name: allopurinol
Why do we use allopurinol?
allopurinol is a medication commonly used to manage hyperuricemia; a condition characterized by elevated uric acid levels in the blood. It is primarily indicated for the prevention and treatment of gout.
By reduces the production of uric acid, allopurinol preventing the formation of uric acid crystals in the joints and reducing the risk of gout attacks.
allopurinol is also used in some instances of hyperuricemia associated with other medical conditions, such as kidney stones or certain types of cancer, where elevated uric acid levels may pose a risk to the patient’s health.