Allopurinol Injection

Name: Allopurinol Injection

What do I need to tell my doctor BEFORE I take Allopurinol Injection?

  • If you have an allergy to allopurinol or any other part of allopurinol injection.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take Allopurinol Injection?

  • Tell all of your health care providers that you take allopurinol injection. This includes your doctors, nurses, pharmacists, and dentists.
  • Avoid driving and doing other tasks or actions that call for you to be alert until you see how this medicine affects you.
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • This medicine may affect how much of some other drugs are in your body. If you are taking other drugs, talk with your doctor. You may need to have your blood work checked more closely while taking allopurinol injection with your other drugs.
  • Follow the diet and workout plan that your doctor told you about.
  • Talk with your doctor before you drink alcohol.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine while you are pregnant.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How do I store and/or throw out Allopurinol Injection?

  • If you need to store this medicine at home, talk with your doctor, nurse, or pharmacist about how to store it.

Allopurinol Injection Description

Allopurinol sodium for injection is a xanthine oxidase inhibitor. It is available in vials as the sterile lyophilized sodium salt of allopurinol sodium equivalent to 500 mg of allopurinol. Allopurinol sodium for injection contains no preservatives.

The chemical name for allopurinol sodium is 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one monosodium salt. It is a white amorphous mass with a molecular weight of 158.09 and molecular formula C5H3N4NaO. The structural formula is

The pKa of allopurinol sodium is 9.31.

Indications and Usage for Allopurinol Injection

Allopurinol Sodium for Injection is indicated for the management of patients with leukemia, lymphoma, and solid tumor malignancies who are receiving cancer therapy which causes elevations of serum and urinary uric acid levels and who cannot tolerate oral therapy.

Contraindications

Patients who have developed a severe reaction to allopurinol should not be restarted on the drug.

Warnings

ALLOPURINOL SHOULD BE DISCONTINUED AT THE FIRST APPEARANCE OF SKIN RASH OR OTHER SIGNS WHICH MAY INDICATE AN ALLERGIC REACTION. In some instances with oral allopurinol, a skin rash may be followed by more severe hypersensitivity reactions such as exfoliative, urticarial, and purpuric lesions as well as Stevens-Johnson syndrome (erythema multiforme exudativum), and/or generalized vasculitis, irreversible hepatotoxicity and, on rare occasions, death.

In patients receiving mercaptopurine or azathioprine, the concomitant administration of 300 to 600 mg of allopurinol sodium for injection per day will require a reduction in dose to approximately one-third to one-fourth of the usual dose of mercaptopurine or azathioprine. Subsequent adjustment of doses of mercaptopurine or azathioprine should be made on the basis of therapeutic response and the appearance of toxic effects (see PRECAUTIONS- Drug Interactions).

A few cases of reversible clinical hepatotoxicity have been noted in patients taking oral allopurinol, and in some patients asymptomatic rises in serum alkaline phosphatase or serum transaminase have been observed. If anorexia, weight loss, or pruritus develop in patients on allopurinol, evaluation of liver function should be part of their diagnostic workup. In patients with pre-existing liver disease, periodic liver function tests are recommended during the early stages of therapy.

Due to the occasional occurrence of drowsiness, patients should be alerted to the need for due precaution when engaging in activities where alertness is mandatory.

The occurrence of hypersensitivity reactions to allopurinol may be increased in patients with decreased renal function receiving thiazides and allopurinol concurrently. Thus, in patients with decreased renal function, such combinations should be administered with caution.

Adverse Reactions

In an uncontrolled, compassionate plea protocol, 125 of 1,378 patients reported a total of 301 adverse reactions while receiving allopurinol sodium for injection. Most of the patients had advanced malignancies or serious underlying diseases and were taking multiple concomitant medications. Side effects directly attributable to allopurinol sodium for injection were reported in 19 patients. Fifteen of these adverse experiences were allergic in nature (rash, eosinophilia, local injection site reaction). One adverse experience of severe diarrhea and one incidence of nausea were also reported as being possibly attributable to allopurinol sodium for injection. Two patients had serious adverse experiences (decreased renal function and generalized seizure) reported as being possibly attributable to allopurinol sodium for injection.

A listing of the adverse reactions regardless of causality reported from clinical trials follows:

 

Incidence Greater Than 1%:

 
 

Cutaneous/Dermatologc:

 

rash (1.5%)

 

Genitourinary:

 

renal failure/insufficiency (1.2%)

 

Gastrointestinal:

 

nausea (1.3%), vomiting (1.2%)

 

Incidence Less Than 1%:

 
 

Body as Whole:

 

fever, pain, chills, alopecia, infection, sepsis, enlarged abdomen, mucositis/pharyngitis, blast crisis, cellulitis, hypervolemia

 

Cardiovascular:

 

heart failure, cardiorespiratory arrest, hypertension, pulmonary embolus, hypotension, decreased venous pressure, flushing, headache, stroke, septic shock, cardiovascular disorder, ECG abnormality, hemorrhage, bradycardia, thrombophlebitis, ventricular fibrillation

 

Cutaneous/Dermatologic:

 

urticaria, pruritus, local injection site reaction

 

Gastrointestinal:

 

diarrhea, gastrointestinalbleeding, hyperbilirubinemia, splenomegaly, hepatomegaly, intestinal obstruction, jaundice, flatulence, constipation, liver failure, proctitis

 

Genitourinary:

 

hematuria, increased creatinine, oliguria, kidney function abnormality, urinary tract infection

 

Hematologic:

 

leukopenia, marrow aplasia, thrombocytopenia, eosinophilia,neutropenia, anemia, pancytopenia, ecchymosis, bone marrow suppression, disseminated intravascular coagulation

 

Metabolic:

 

hypocalcemia, hyperphosphatemia, hypokalemia, hyperuricemia, electrolyte abnormality, hypercalcemia, hyperglycemia, hypernatremia, hyponatremia, metabolic acidosis, edema, glycosuria, hyperkalemia, lactic acidosis, water intoxication, hypomagnesemia

 

Neurologic:

 

seizure, status epilepticus, myoclonus, twitching, agitation, mental status changes, cerebral infarction, coma, dystonia, paralysis, tremor

 

Pulmonary:

 

respiratory failure/insufficiency, ARDS, increased respiration rate, apnea

 

Musculoskeletal:

 

arthralgia

 

Other:

 

hypotonia, diaphoresis, tumor lysis syndrome

The most frequent adverse reaction to oral allopurinol is skin rash. Skin reactions can be severe and sometimes fatal. Therefore, treatment with allopurinol sodium for injection should be discontinued immediately if a rash develops (see WARNINGS). For further details on hypersensitivity reactions to treatment with oral allopurinol, refer to the package insert for allopurinol tablets.

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