Names and pronunciation
(mye-koe-phen′oh-late) CellCept mycophenolate acid Myfortic
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Drug reference
(mye-koe-phen′oh-late) CellCept mycophenolate acid Myfortic
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Func. class.: Immunosuppressant
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ACTION: Inhibits inflammatory responses that are mediated by the immune system
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USES: Prophylaxis for organ rejection in allogenic cardiac, hepatic, renal transplants
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Unlabeled uses: Nephrotic syndrome
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CONTRAINDICATIONS: Hyper- sensitivity to this product or mycopheno- lic acid
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Black Box Warning: Pregnancy Precautions: Breastfeeding, lympho- mas, neutropenia, renal disease, acci- dental exposure, anemia Black Box Warning: Infection, neoplastic disease; requires an experienced clini- cian and a specialized care setting Black Box Warning: Pregnancy/breast- feeding: pregnancy test within 1 wk be- fore initiation of treatment; confirm nega- tive pregnancy test; if patient becomes pregnant, enroll in Mycophenolate Preg- nancy Registry 1-800-617-8191; do not breastfeed during treatment and for 6 wk after final dose Black Box Warning: Requires a spe- cialized setting and experienced cli- nician: should be used by those experi- enced in the use of immunosuppressive therapy in a facility equipped for trans- plants Black Box Warning: Pregnancy/breast- feeding: to use 2 forms of contraception before, during, and for 6 wk after therapy; not to breastfeed during and for 6 wk af- ter final dose; that pregnancy test is re- quired the week before start of therapy and 8-10 days later M • To take at same time each day; not to crush, chew caps, or ext rel tab; swallow whole, take on empty stomach Black Box Warning: Infection: to report fever, chills, sore throat, fatigue; serious infections may occur; avoid crowds, per- sons with known infections Black Box Warning: Neoplastic dis- ease: lymphoma and other neoplastic diseases may occur, particularly skin cancer; limit UV exposure by wearing protective clothing, sunscreen HIGH ALERT
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SIDE EFFECTS CNS: Tremor, dizziness, insomnia, headache, fever, anxiety, pain, progres- leukoencephalopathy, sive multifocal asthenia, paresthesia CV: Hypertension, chest pain, hypoten- sion, edema GI: Diarrhea, constipation, nausea, vomiting, stomatitis, bleeding, GI abdominal pain, anorexia, dyspepsia GU: UTI, hematuria, renal tubular necro- sis, polyomavirus-associated nephropathy HEMA: Leukopenia, thrombocytopenia, anemia, pancytopenia, pure red cell apla- sia, neutropenia INTEG: Rash META: Peripheral edema, hypercholes- terolemia, hypophosphatemia, edema, hyperkalemia, hypokalemia, hypergly- cemia, hypocalcemia, hypomagnesemia MS: Arthralgia, muscle wasting, back pain, weakness RESP: Dyspnea, respiratory infection, increased cough, pharyngitis, bronchi- tis, pneumonia, plural effusion, pulmo- nary fibrosis SYST: Lymphoma, nonmelanoma skin carcinoma, sepsis
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INTERACTIONS Increase: bone marrow suppression— azaTHIOprine; do not use concurrently Increase: bleeding risk—anticoagulants, NSAIDs, thrombolytics, salicylates Increase: toxicity—acyclovir, ganciclovir, valACYclovir; monitor if used together Increase: effects of both products— phenytoin, theophylline Increase: mycophenolate levels—pro- benecid, immunosuppressives, salicy- lates; monitor for adverse reactions Decrease: mycophenolate levels—antac- ids (magnesium, aluminum), cholestyr- amine, cycloSPORINE, rifamycin; sepa- rate dosing times by several hours Decrease: protein binding of phenytoin, theophylline Decrease: effect of live attenuated vac- cines, oral contraceptives Drug/Herb Interference with immunosuppression: astragalus, cat’s claw, echinacea, melatonin Drug/Food Decrease: absorption if taken with food Drug/Lab Test Increase: serum creatinine, BUN, choles- terol, potassium, WBC
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DOSAGE AND ROUTES For kidney transplant rejection prophylaxis with or without antithymocyte induction • Adult: IV 1 g over at least 2 hr bid in combination with corticosteroids and cycloSPORINE; initial dose should be given within 24 hr of transplantation Oral dosage M The delayed-release tablets (mycopheno- late sodium) and the capsules, oral sus- pension, and tablets (mycophenolate mofetil) are not interchangeable on an mg basis • Adult: PO (regular release) 1 g myco- phenolate mofetil or PO (extended release) 720-mg mycophenolate sodium bid in combination with corticosteroids and cyclosporine • Child: PO (oral suspension) 600 mg/ m2 bid, max 2 g/day. Mycophenolate mofetil capsules may be given at dose of 750 mg bid for those with a body surface area (BSA) of 1.25-1.5 m2 or 1 g bid for those with a BSA >1.5 m2; mycopheno- late sodium delayed-release tablets 400 mg/m2 bid, max 720 mg bid • Infant ≥3 mo: PO (oral suspension) 600 mg/m2 bid, max 2 g/day For heart transplant rejection prophylaxis • Adult: IV 1.5 g over at least 2 hr bid in combination with corticosteroids and cy- cloSPORINE. The first dose may be admin- istered within 24 hr after transplantation • Adult: PO (regular release) (mycophe- nolate mofetil) 1.5 g bid in combination with corticosteroids and cycloSPORINE. Initial oral dose should be administered as soon as possible after transplantation For liver transplant rejection prophylaxis • Adult: IV 1 g over at least 2 hr bid in combination with corticosteroids and cy- cloSPORINE; the first dose may be admin- istered within 24 hr after transplantation • Adult: PO (mycophenolate mofetil) 1.5 g bid in combination with corticosteroids and cycloSPORINE; give initial dose as soon as possible after transplantation
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Available forms: Caps 250 mg; tabs 500 mg; inj (powder) 500 mg/20-mL vial; powder for oral susp 200 mg/mL: delayed rel tab (Myfortic) 180, 360 mg
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Administer: • May be given in combination with cor- ticosteroids, cycloSPORINE • Cytotoxic: Use safe handling proce- dures; avoid inhalation or direct contact with skin, mucous membranes; terato- genic in animals; wash skin if product comes in contact with skin PO route • Do not break, crush, or chew tabs; do not open caps • Give at same time each day • Oral susp: tap closed bottle several times to loosen powder; use 94 mL of water in graduated cylinder; add ½ total amount of water for reconstitution and shake the closed bottle; add remaining water and shake again; remove child- resistant cap; push adapter into neck of bottle; close tightly, may give by NG tube ≥8 French catheter • Give alone for better absorption Intermittent IV INFUSION route • Reconstitute each vial with 14 mL D5W; shake gently; further dilute to 6 mg/mL; dilute 1 g/140 mL D5W, 1.5 g/210 mL D5W; give by slow IV infusion ≥2 hr; never give by bolus or rapid IV inj • Do not give with other medications or sol, do not use if particulates are present Y-site compatibilities: Alemtuzumab, alfentanil, amikacin, anidulafungin, arg- atroban, bivalirudin, caspofungin, cefepime, DAPTOmycin, DOPamine, nor- epinephrine, octreotide, oxytocin, tacro- limus, tigecycline, tirofiban, vancomycin, zoledronic acid
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Assess: • Progressive multifocal leukoen- cephalopathy: may be fatal; ataxia, confusion, apathy, hemiparesis, visual problems, weakness; side effects should be reported to FDA • Pure red cell aplasia (PRCA): occurs when used in combination with other im- munosuppressants; assess for fatigue, pulmonary tachycardia; may cause graft rejection • Blood studies: CBC during treatment monthly, may monitor mycophenolate levels in those at high risk for organ re- jection • Hepatic studies: alk phos, AST, ALT, bilirubin • Renal studies: BUN, CCr, electrolytes
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Evaluate: • Therapeutic response: absence of graft rejection
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • About the need for repeated lab tests and follow-up exams
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PHARMACOKINETICS Rapidly and completely absorbed; meta bolized to active metabolite (MPA); excreted in urine, feces; protein binding (MPA) 97%; half-life (MPA) 17.9 hr
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• Child: PO (oral suspension) 600 mg/ m2 bid, max 2 g/day. Mycophenolate mofetil capsules may be given at dose of 750 mg bid for those with a body surface area (BSA) of 1.25-1.5 m2 or 1 g bid for those with a BSA >1.5 m2; mycopheno- late sodium delayed-release tablets 400 mg/m2 bid, max 720 mg bid
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