AZATHIOPRINE

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naratriptan

GENERIC NAME: Azathioprine


PHARMACOLOGICAL CLASS: Immunosuppressant Agent
ATC CODE: L04AX01
PRACTICE INSIGHTS:

Patients with intermediate TPMT activity may be at risk for increased


myelosuppression & low or absent TPMT activity receiving conventional
azathioprine doses are at risk for developing severe, life-threatening
myelotoxicity.
Dosage reductions are recommended for patients with reduced TPMT activity
I.V. dose is equivalent to oral dose

DOSE
ADULT:
Kidney transplantation (Prevention of transplant rejection)
Oral, I.V.

Initial, 3-5 mg/kg/day given as a single daily dose


To be given on day of transplantation or 3 days prior to transplantation
Maintenance, 1-3 mg/kg/day

Rheumatoid arthritis
Oral

Initial, 1 mg/kg/day OD or bid for 6-8 weeks


May increase by 0.5 mg/kg every 4 weeks until response or
Maximum initial dose, 2.5 mg/kg/day to a minimum of 12 weeks
Maintenance, reduce dose by 0.5 mg/kg every 4 weeks until lowest effective
dose is reached

Chronic refractory thrombocytopenic purpura (Off-label use)


Oral

Maintenance, 100-200 mg/day

Crohns disease (Off-label use)


Oral

2-3 mg/kg/day OD

Dermatomyositis/polymyositis(Off-label use)
Oral

50 mg/day in conjunction with prednisone

Increase by 50 mg/week
Total dose, 2-3 mg/kg/day

Lupus nephritis (Off-label use)


Oral

Initial, 2 mg/kg/day with/without corticosteroids


May reduce to 1.5 mg/kg/day after 1 month or
Target dose, 2 mg/kg/day

Ulcerative colitis (Off-label use)


Oral

1.5-2.5 mg/kg/dayOD

PEDIATRIC:
Juvenile Idiopathic Arthritis
Oral, I.V.

Initial, 1 mg/kg/day OD or bid 0.5 mg/kg/day after 6-8 weeks


Maximum initial dose, 2.5 mg/kg/day
Maintenance, 0.5 mg/kg every 4 weeks until lowest effective dose is reached

Transplantation, Prevention of transplant rejection (Off-label use)


Oral, I.V.

Initial, 3-5 mg/kg/day on day of transplant or 3 days before transplant


Maintenance, 1-3 mg/kg/day

Lupus Nephritis (Off-label use)


Oral

<12 years: Safety and efficacy not established

>12 years: 2 mg/kg/day with or without low-dose corticosteroids

DOSE ADJUSTMENT
Hepatic impairment

No dosage adjustment provided in manufacturers labeling

Renal impairment

No dosage adjustment provided in manufacturers labeling

INDICATIONS (OPTIONAL):
PREGNANCY & LACTATION:

Category D
Enters breast milk/not recommended

MODE OF ACTION:Azathioprine is purine anti-metabolite that may inhibit synthesis


of DNA, RNA, and proteins. It may also interfere with cellular metabolism and inhibit
mitosis.
ADVERSE DRUG REACTIONS:
1-10%

Dizziness,drowsiness,fatiguenausea, pain/pressure sensation,


paresthesias,throat/neck symptoms

<1%

Coronary artery vasospasm in pts with CAD risk factors, myocardial infarction

DRUG INTERACTIONS:
CONTRAINDICATIONS & WARNINGS:

Contraindicated in
o Hypersensitivity to azathioprine or any component of the formulation
o Pregnancy, lactation
o Patients with rheumatoid arthritis
o History of treatment with alkylating agents
Risk of
o Neoplasia
o Hematologic toxicities
o Post-transplant lymphoma
o Hepatosplenic T-cell lymph
o Infection
o Hepatotoxicity
Use caution in
o Inflammatory bowel disease

DIETARY & GENERAL CONSIDERATIONS:

Advise patient to take with food


Warn patient to avoid smoking & alcohol
Advise female patients to avoid pregnancy

MONITORING PARAMETERS:

Monitor:
o CBC with differential, platelets
o Hepatic & renal function
o TPMT genotyping or phenotyping
o Symptoms of infection, malignancy

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