Clinical Pharmacology Details


Leflunomide


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Indications & Dose:

Adult and Child <18 yr


• Rheumatoid arthritis: Loading dose 100 mg qd for 3 days; Maintenance dose 20 mg daily (10 mg qd if side effects intolerable); Drug elimination procedure: cholestyramine 8 g tid x 11 days (consecutive days not necessary); without these extra measures, nondetectable plasma levels would take <2 years, after during disocntinuation


Activepsoriaticarthritis(specialistuseonly)



Adult: Initially100mg once daily for 3 days, then reduced to 20mg once daily. 

Contraindications:

Preexisting liver impairment 

Side Effects:

Cautions:

Precautions:

Hepatotoxicity, renal insufficiency, immunodeficiency, bone-marrow dysplasia, sever infections (potential for immunosuppression) 

Interaction:

Drugs


Cholestyramine,Coadministration results in rapid and significant decrease in active metabolite


Nonsteroidal antiinflammatory drugs: Inhibition of CYP 2C9 , decreases the metabolism of many NSAIDS
Rifampin: Leflunomide levels increased 40%.


 

Warnings:

Adverse Effects:

Lactations:

Pregnancy category X; amount of excretion into breast milk unknown; use of leflunomide by nursing mothers is not recommended since the potential risk of nursing infant is considered serious 

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

CNS: Headache, dizziness, paresthesia
CV:
Hypertension
GI: Diarrhea, nausea, abdominal pain, hepatitis, abnormal liver enzymes
GU: Polyurea, dysuria
METAB: Weight loss
RESP: Respiratory infection, bronchitis
SKIN:
Alopecia, rash, pruritis 

Patient And Carer Advice: