Mycophenolate

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Contraindications 4 Dosage 5 Adverse-effects 6 Drug-interactions 7 Mechanism-of-action 8 More General Terms 9 Internet Database 10 References

Introduction

• Mycophenolate mofetil. Antibiotic substance produced by Penicillium brevi-compactum, P. stoloniferum & related species.

• Medication Guide to be distributed to every patient who fills a CellCept prescription. [7]

Indications

• maintenance of immunosuppression after organ transplantation & for treatment of refractory rejection
• used in conjunction with corticosteroids & cyclosporine
• use in suppressing need for azathioprine

Contraindications

• pregnancy [4,6]
• women of childbearing potential should have a negative serum or urine pregnancy test with a sensitivity of at least 25 mIU/mL within one week prior to beginning therapy
• women of childbearing potential taking mycophenolate must

• receive contraceptive counseling
• use effective contraception

• begin using 2 chosen methods of contraception 4 weeks prior to starting mycophenolate therapy, unless abstinence is the chosen method
• contraceptives should be used during & for 6 weeks after stopping mycophenolate
  

• pregnancy category = x

Dosage

• 1 g PO BID
• take on an empty stomach
• do not crush or chew capsules
• dose should be decreased or stopped in patients with neutropenia < 1300/ mm3

• Tabs: 250 mg. Myfortic: enteric coated Dosage adjustment with renal failure:

• doses > 2 g/day are not recommended

Adverse-effects

• commmon > 10%

• general

• abdominal pain, fever, headache, infection from immunosuppression, asthenia, chest pain, back pain hypertension

• central nervous system

• tremor, insomnia, dizziness

• dermatology

• acne, rash

• gastrointestinal

• diarrhea, constipation, dyspepsia, nausea/vomiting

• hematologic

• hypochromic anemia, leukopenia, thrombocytopenia, leukocytosis
• pure red cell aplasia [9,10]

• metabolic

• peripheral edema, hypercholesterolemia, hypophosphatemia, edema, hypokalemia, hyperkalemia, hyperglycemia

• respiratory

• dyspnea, cough, pharyngitis, bronchitis, pneumonia

• urogenital

• UTI, hematuria, renal tubular necrosis

• progressive multifocal leukoencephalopathy ? [5]
• congenital anomalies following exposure to mycophenolate mofetil during pregnancy, including microtia, cleft lip & cleft palate [6]
• BK virus-associated nephropathy in renal transplant patients [8]

• Caution:

• avoid inhalation or direct contact with skin or mucous membranes of powder in capsules; wash with soap & water if occurs
• capsules should not be opened or crushed
• teratogenic [6]
  
• drug adverse effects of immunosuppressive agents

Drug-interactions

• antacids decrease absorption
• cholestyramine decreases absorption
• mycophenolate may increase levels of

• acyclovir
• ganciclovir

• iron supplements may increase mycophenolate levels
• probenecid may increase mycophenolate levels
• salicylates may increase free fraction of mycophenolate
  
• drug interaction(s) of antibiotics with warfarin

Mechanism-of-action

• immunosuppressive agent
• inhibits purine metabolism

More General Terms

• immunosuppressive agent
• carboxylate
• phenol
• alkene; olefin
• ester
• other antibiotic
• antineoplastic agent (chemotherapeutic agent)
• disease-modifying antirheumatic agent (DMARD)

Internet Database

PubChem: 31839
PubChem: 5281078
PubChem: 4272
PubChem: 4271
PubChem: 198011
PubChem: 162230

References

1. Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
3. Department of Veterans Affairs, VA National Formulary
4. Prescriber's Letter 14(12): 2007 Pregnancy Category Change for Mycophenolate Motefil (CellCept) Detail-Document#: [1] (subscription needed) [2]
5. FDA MedWatch [3]
6. FDA MedWatch [4]
7. FDA MedWatch [5]
8. FDA Medwatch [6]
9. FDA Medwatch [7]
10. FDA MedWatch [8]
11. Myfortic: Novartis at (888) 669-6682

mycophenolate (Cellcept, Myfortic)