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Azathioprine

Azathioprine Prescription
Generic Name: azathioprine (ay za THYE oh preen)
Brand Name: Azasan, Imuran
Physician reviewed azathioprine patient information - includes azathioprine description, dosage and directions.

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Azathioprine Drug Information:

Azathioprine weakens your body's immune system, to help keep it from "rejecting" a transplanted organ such as a kidney. Organ rejection happens when the immune system treats the new organ as an invader and attacks it. Azathioprine is used to prevent your body from rejecting a transplanted kidney. Azathioprine is also used to treat symptoms of rheumatoid arthritis. Azathioprine may also be used for purposes not listed in this medication guide. Azathioprine may cause a rare type of lymphoma (cancer) of the liver, spleen, and bone marrow that can be fatal. This has occurred mainly in teenagers and young men with Crohn's disease or ulcerative colitis. Learn more

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Azathioprine Side Effects

In Summary

Commonly reported side effects of azathioprine include: infection, nausea, leukopenia, and vomiting. See below for a comprehensive list of adverse effects.

For the Consumer

Applies to azathioprine: oral tablet

Other dosage forms:

  • intravenous powder for solution
Warning

Oral route (Tablet)

Chronic immunosuppression with azathioprine increases risk of malignancy in humans. Reports of malignancy include post-transplant lymphoma and hepatosplenic T-cell lymphoma (HSTCL) in patients with inflammatory bowel disease. Physicians using this drug should be very familiar with this risk as well as with the mutagenic potential to both men and women and with possible hematologic toxicities. Inform patients of the malignancy risks.

Side effects requiring immediate medical attention

Along with its needed effects, azathioprine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking azathioprine:

More common

  • Black, tarry stools
  • bleeding gums
  • blood in the urine or stools
  • chest pain
  • chills
  • cough
  • fever
  • hoarseness
  • lower back or side pain
  • painful or difficult urination
  • pinpoint red spots on the skin
  • sore throat
  • sores, ulcers, or white spots on the lips or in the mouth
  • swollen glands
  • unusual bleeding or bruising
  • unusual tiredness or weakness

Less common

  • Cloudy urine
  • fever sores on the skin
  • general feeling of illness
  • greatly decreased frequency of urination or amount of urine
  • skin rash
  • swelling of the feet or lower legs
  • weight loss
  • yellow skin or eyes

Rare

  • Bloating
  • clay-colored stools
  • constipation
  • dark urine
  • decreased appetite
  • diarrhea (severe)
  • fast heartbeat
  • fever (sudden)
  • headache
  • indigestion
  • itching
  • loss of appetite
  • muscle or joint pain
  • nausea (severe)
  • pains in the stomach, side, or abdomen, possibly radiating to the back
  • redness or blisters on the skin
  • stomach pain or tenderness
  • swelling of the feet or lower legs
  • unusual feeling of discomfort or illness (sudden)
  • vomiting (severe)

Incidence not known

  • Difficulty with breathing
  • difficulty with moving
  • fat in the stool
  • general feeling of illness
  • pale skin
  • sores on the skin
  • stomach cramps
  • sudden loss of weight
  • troubled breathing with movement
  • weight loss
Side effects not requiring immediate medical attention

Some side effects of azathioprine may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects.

Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Nausea (mild)
  • swollen joints
  • vomiting (mild)

Less common

  • Hair loss or thinning of the hair

For Healthcare Professionals

Applies to azathioprine: compounding powder, intravenous powder for injection, oral tablet

General

The principal and potentially serious toxic effects of azathioprine are hematologic and gastrointestinal. Risk of secondary infection and malignancy is also significant. Frequency and severity of side effects depend on dose and duration of azathioprine as well as on underlying disease or concomitant therapies. Hematologic toxicities and neoplasia were reported more often in renal homograft recipients than in patients using azathioprine for rheumatoid arthritis.

Hematologic

Very common (10% or more): Depression of bone marrow function, leukopenia

Common (1% to 10%): Anemia, thrombocytopenia

Rare (Less than 0.1%): Agranulocytosis, aplastic anemia, erythroid hypoplasia, megaloblastic anemia, pancytopenia

Frequency not reported: Bleeding, increased mean corpuscular volume and red cell hemoglobin content (reversible, dose-related)

Bone marrow suppression is dose related and is the most common cause for dosage reductions. Leukopenia (any degree) has been reported in greater than 50% of renal homograft recipients and 28% of rheumatoid arthritis patients. Leukopenia (less than 2500/mm3 [2.5 x 10(9)/L]) has been reported in 16% of renal homograft recipients and 5.3% of rheumatoid arthritis patients.

There are data to support an increased risk of bone marrow aplasia in patients with very low or absent thiopurine methyltransferase (TPMT) activity. In patients with low TPMT activity, there is an increase in 6-thioguanine nucleotide (6-TGN) concentrations, a cytotoxic metabolite which suppresses purine synthesis. Death associated with pancytopenia has been reported in patients with absent TPMT activity receiving azathioprine. Bone marrow aplasia has been reported in patients with normal TPMT activity.

A 55-year-old male with pompholyx and deficiency of erythrocyte thiopurine methyltransferase experienced pancytopenia coincident with azathioprine therapy. Ten weeks after starting azathioprine 100 mg per day, a full blood count (during routine monitoring) showed moderate pancytopenia. Azathioprine was discontinued. Ten days later he was admitted to the hospital with malaise, lethargy, and deterioration in blood count. He was treated with blood and platelet transfusions and discharged eight days later with modest improvement in peripheral blood count.

Gastrointestinal

Gastrointestinal side effects tend to be more problematic in the first few months of therapy. A 20-year-old man developed severe small-bowel villus atrophy and chronic diarrhea after starting azathioprine 50 mg per day. Diarrhea completely resolved within 2 weeks after azathioprine discontinuation. Mucosal biopsies at 4 months post azathioprine discontinuation showed complete reversal of severe duodenal villus atrophy.

Complications such as colitis, diverticulitis, and bowel perforation have been primarily reported in transplant patients, and may be related to concomitant high-dose corticosteroid therapy. Pancreatitis occurs most commonly in organ recipients and patients with Crohn's disease.

There have been case reports of patients with symptoms that imitate viral gastroenteritis (nausea, vomiting, diarrhea, and fever) occurring hours after a single dose of azathioprine.

Very common (10% or more): Nausea, vomiting

Uncommon (0.1% to 1%): Diarrhea, pancreatitis, steatorrhea

Rare (less than 0.1%): Colitis (transplant recipients), diverticulitis or intestinal perforation (transplant recipients), gastrointestinal ulcers (transplant recipients), intestinal hemorrhage (transplant recipients), necrosis (transplant recipients), severe diarrhea (inflammatory bowel disease patients)

Frequency not reported: Severe villus, sores in the mouth and on the lips

Oncologic

The increased risk of cancer may be more pronounced when azathioprine is used concomitantly with other immunosuppressive agents. Renal transplant patients may have a higher risk of developing lymphoproliferative disorders, lymphomas, and leukemia, as well as some solid tumors while receiving azathioprine.

Transplant patients as well as those with rheumatoid arthritis are often treated with multiple immunosuppressants; therefore, the true risk of neoplasia associated with azathioprine alone has yet to be determined.

A small increase in the risk of Epstein-Barr virus-positive lymphoma was seen in a study of patients with inflammatory bowel disease treated with azathioprine.

The majority of reported cases of hepatosplenic T-cell lymphoma have bee in patients with Crohn's disease or ulcerative colitis, and were adolescent and young adult males.

Common (1% to 10%): Cervical cancer, Kaposi's sarcoma, non-Hodgkin's lymphoma, squamous cell carcinoma of the skin, vulval cancer (renal homograft patients)

Uncommon (0.1% to 1%): Lymphoproliferative diseases after transplantation

Rare (0.01% to 0.1%): Melanoma, non-Kaposi's sarcoma

Very rare (less than 0.01%): Acute myeloid leukemia and myelodysplastic syndromes

Frequency not reported: Hepatosplenic T-cell lymphoma

Hepatic

Common (1% to 10%): Hepatic dysfunction (including cholestasis, destructive cholangitis, peliosis hepatitis, perisinusoidal fibrosis, nodular regenerative hyperplasia) (organ transplant recipients)

Uncommon (0.1% to 1%): Hepatotoxicity, including elevation of serum alkaline phosphatase, bilirubin, and/or serum transaminases

Rare (Less than 0.1%): Hepatic veno-occlusive disease, life-threatening hepatic damage

Frequency not reported: Acute focal hepatocellular necrosis, sinusoidal dilatation

Hepatotoxicity usually occurs within the first six months of therapy and is more common in patients requiring immunosuppression following transplant than in patients requiring therapy for rheumatoid arthritis.

Hepatotoxicity is often manifest as cholestasis and/or acute focal hepatocellular necrosis, and is generally reversible following discontinuation of azathioprine therapy. However, permanent hepatic damage associated with cirrhosis, perisinusoidal fibrosis, hepatic peliosis, sinusoidal dilatation, and veno-occlusive disease is also reported. Several cases of nodular regenerative hyperplasia of the liver and at least one case of destructive cholangitis have been reported.

Veno-occlusive disease of the hepatic veins is due to an unknown mechanism, may affect males more often, usually precedes portal hypertension, and carries a poor prognosis. Numerous fatalities have been reported. Permanent discontinuation of azathioprine therapy is indicated if hepatic veno-occlusive disease is suspected.

A 51-year-old man developed jaundice and diffuse abdominal pain two months after the start of azathioprine 1.4 mg/kg/day. Biopsy reports confirmed destruction of the bile ducts consistent with destructive cholangitis. After discontinuation of azathioprine, the abdominal pain disappeared within 2 days and liver function tests improved and returned to normal values 8 weeks later.

Hypersensitivity

Uncommon (0.1% to 1%): Hypersensitivity reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis

Very rare (less than 0.01%): Hypersensitivity reactions with fatal outcome

Idiosyncratic manifestations of hypersensitivity include general malaise, headache, dizziness, nausea, vomiting, diarrhea, fever, rigors, exanthema, rash, vasculitis, myalgia, arthralgia, hypotension, renal dysfunction, hepatic dysfunction, cardiac dysrhythmia, and cholestasis. Rhabdomyolysis has been reported as part of an azathioprine hypersensitivity syndrome.

At least 3 cases of erythema nodosum, 2 cases of pustules, and 1 case of contact dermatitis have been reported. Erythema nodosum and pustules may be related to the clinical activity of inflammatory bowel disease. Relapse of such lesions shortly after rechallenge should raise the hypothesis of hypersensitivity rather than pharmacological manifestations.

Azathioprine should be permanently withdrawn after occurrence of hypersensitivity reactions.

Cardiovascular

At least three cases of atrial fibrillation have been reported (one case involving a patient with ulcerative colitis), although causality is unknown. A 52-year-old male with steroid-dependent ulcerative colitis experienced atrial fibrillation coincident with azathioprine therapy. The drug had been started 3 years earlier, but discontinued after a few months because the patient reported palpitations, lipothymia, nausea, and vomiting. Upon a rechallenge with 50 mg of azathioprine, the patient showed general malaise, nausea, and vomiting. An ECG showed atrial fibrillation, and the patient reported that the symptoms were similar to those experienced previously.

Azathioprine-induced hypotension is independent of dose and may accompany signs and symptoms of hypersensitivity. Hypotension may be profound, although it is usually responsive to intravenous fluids and, if hypersensitivity is suspected, corticosteroids.

Rare (less than 0.01%): Hypotension, including cardiogenic shock

Frequency not reported: Atrial fibrillation

Dermatologic

Common (1% to 10%): Alopecia

Frequency not reported: Exacerbation of dermatomyositis, rash, Sweet's syndrome (acute febrile neutrophilic dermatosis)

Alopecia has been reported in patients on azathioprine monotherapy or in combination with other immunosuppressants. This side effect may resolve spontaneously despite ongoing therapy.

A female patient developed skin peeling syndrome eight months after the dosage of azathioprine was reduced to 25 mg daily. Skin lesions resolved 30 days after drug withdrawal.

Excess sun exposure, pale skin types, and duration of allograft seem to be important risk factors in the development of skin lesions.

Genitourinary

Rare (less than 0.1%): Hematuria secondary to azathioprine-induced crystalluria

Immunologic

Very common (10% or more): Viral, fungal, and bacterial infections (transplant recipients also receiving other immunosuppressants)

Common (1% to 10%): Susceptibility to infection in patients with inflammatory bowel disease

Uncommon (0.1% to 1%): Viral, fungal, and bacterial infections (other indications)

Frequency not reported: Protozoal and opportunistic infections, including reactivation of latent infections, increased susceptibility to varicella and herpes zoster progressive multifocal leukoencephalopathy

Metabolic

Very common (10% or more): Anorexia

Frequency not reported: Negative nitrogen balance

Musculoskeletal

Frequency not reported: Arthralgias, myalgias

Nervous system

Frequency not reported: Alterations in sense of smell or taste, exacerbation of myasthenia gravis, meningitis

Ocular

A patient with systemic lupus erythematosus and end-stage renal disease experienced CMV retinitis coincident with azathioprine therapy. It is theorized that immunosuppressive therapy may have a role in the development of CMV retinitis in this population. The patient responded to discontinuation of azathioprine, lowering of the corticosteroid dose, and systemic administration of ganciclovir.

Frequency not reported: CMV retinitis

Renal

Elevation in serum creatinine and BUN accompanied by oliguria are usually associated with hypotension, and normalize after treatment with intravenous hydration and steroids. Cases of hematuria secondary to azathioprine-induced crystalluria may be less common with high urine output.

A reduction in the incidence of chronic allograft nephropathy has been reported during the extended follow-up (greater than or equal to 10 years) of patients (n=128) participating in a randomized trial that examined the conversion from cyclosporine to azathioprine as early as three months after renal transplantation.

A 47-year-old female with Wegener's granulomatosis experienced rapid progression of renal failure within 10 days of starting azathioprine for vasculitis. Her creatinine was 119 mcmol/L at the time of presentation. Acute tubulointerstitial nephritis and no active glomerulonephritis were observed on renal biopsy. Her renal function started improving by day 6 post-admission and at one month post-admission her serum creatinine was 116 mcmol/L. She continued to have reasonable renal function and 16 months later had creatinine of 104 mcmol/L with no clinical evidence of recurrent interstitial nephritis.

Frequency not reported: Acute interstitial nephritis, chronic allograft nephropathy, elevation in serum creatinine and BUN accompanied by oliguria

Respiratory

Review of seven rare cases of azathioprine-associated interstitial pneumonitis revealed that the progression from alveolitis to pulmonary fibrosis may be dose-related.

Rare (less than 0.01%): Reversible interstitial pneumonitis

Other

There have been reports of fungal, protozoal, viral, and uncommon bacterial infections, some of which have been fatal, in patients who are receiving azathioprine.

Frequency not reported: Delayed wound healing, fatigue, fever, malaise, oral lesions

Editorial References and Review

Medically reviewed by USARx EDITORIAL TEAM Last updated on 1/1/2020.

Source: Drugs.com Azathioprine (www.drugs.com/mtm/azathioprine.html).