THERAPEUTICS

Brands

• CellCept, Myfortic

Generic?

• Yes

Class

• Immunosuppressant

Commonly Prescribed for

(FDA approved in bold)

• Prophylaxis of organ rejection in patients with allogenic renal, cardiac, or hepatic transplants

• Myasthenia gravis (MG)

• Chronic inflammatory demyelinating polyneuropathy

• Neurosarcoidosis

• Multiple sclerosis (MS)

• Refractory uveitis

• Churg-Strauss syndrome

• Diffuse proliferative lupus nephritis

• Psoriasis

How the Drug Works

• Prodrug that is actively metabolized to mycophenolic acid, a selective inhibitor of inosine monophosphate dehydrogenase, an important enzyme in de novo synthesis of guanine nucleotide. This alters purine metabolism, which preferentially affects T and B lymphocytes, which depend on this pathway

• Inhibits proliferation of T and B lymphocytes and suppresses antibody formation

• May inhibit recruitment of leukocytes into sites of inflammation and graft rejection

• Does not affect production of interleukins

How Long Until It Works

• In as little as 2–3 weeks, and usually within 6 months

If It Works

• Usually used as a corticosteroid-sparing agent. May allow reduction in dose or discontinuation of corticosteroids. Most MG patients require long-term treatment, but occasionally may remit, allowing careful discontinuation

If It Doesn't Work

• Usually used as an adjunctive agent in conjunction with corticosteroids in MG. Azathioprine, cyclosporine, cyclophosphamide, plasma exchange, and IV immune globulin are alternative longterm treatments. Thymectomy may also be effective for selected patients

Best Augmenting Combos for Partial Response or Treatment-Resistance

• Generally combined with prednisone or other corticosteroids for treatment of MG, allowing eventual decrease in dose, and occasionally combined with other immunosuppressive agents

Tests

• Obtain a CBC when initiating treatment, then weekly in the first month, twice monthly in months 2–3, and monthly through the first year

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• Serious AEs are related to immunosupression and neutropenia

Notable AEs

• Diarrhea is most common. Other frequent AEs include abdominal pain, insomnia, nausea, peripheral edema, anxiety, back pain or headache, cough, and mild leukopenia. GI bleeding can also occur