Generic
Mycophenolate Mofetil
6 brands available in the market
At a glance
Mycophenolate Mofetil is an immunosuppressant used to prevent organ rejection after transplantation. It suppresses the immune system by inhibiting lymphocyte proliferation.
Description
Mycophenolate Mofetil is an immunosuppressive agent. It is an uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH). It inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation to DNA. Mycophenolic acid has cytostatic effects on lymphocytes. It has been shown to prevent acute rejection of kidney and heart allotransplantation and decreases antibody production.
Indications
- Prophylaxis of acute organ rejection in renal transplant
- Prophylaxis of acute organ rejection in cardiac transplant
- Prophylaxis of acute organ rejection in hepatic transplant
- Induction and maintenance therapy of Class III-V lupus nephritis
Therapeutic class
Immunological Chemotherapy, Immunosuppressant
Pharmacological class
IMPDH Inhibitor
Pharmacology
Mycophenolate mofetil is the 2-morpholinoethyl ester of mycophenolic acid (MPA). MPA is a potent, selective, uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis. MPA has more potent cytostatic effects on lymphocytes than on other cells because T- and B lymphocytes are critically dependent for their proliferation on de novo synthesis of purines.
Mechanism of action
Suppresses immune system by inhibiting lymphocyte proliferation and prevents organ rejection.
Dosage
Renal Transplant (Adult): 1 g twice daily (2 g daily dose)
Renal Transplant (Pediatric, 3 months-18 years): BSA 1.25-1.5 m²: 750 mg twice daily; BSA >1.5 m²: 1 g twice daily
Cardiac Transplant (Adult): 1.5 g twice daily (3 g daily dose)
Hepatic Transplant (Adult): 1.5 g twice daily (3 g daily dose)
Lupus Nephritis (Adult): Induction: 750 mg-1.5 g twice daily; Maintenance: 500 mg-1 g twice daily
Lupus Nephritis (Pediatric): Induction: 600 mg/m² twice daily (max 2 g/day); Maintenance: 300 mg/m² twice daily
Administration
- Take on an empty stomach (1 hour before or 2 hours after meals)
- Swallow tablet whole; do not crush, chew or break
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects (>10%):
- Diarrhea (21%)
- Leukopenia (34%)
- Nausea (23%)
- Vomiting
- Abdominal pain (27%)
- Sepsis
- Gastrointestinal candidiasis
- Urinary tract infection (34%)
- Hyperglycemia (44%)
- Hypertension (28%)
Serious: Opportunistic infections, lymphoma, skin cancers, GI bleeding
Precautions & warnings
- May increase new or reactive viral infections (hepatitis B/C, polyomaviruses)
- May cause blood dyscrasias (including pure red cell aplasia)
- May cause serious GI tract complications (bleeding, perforations, ulcers)
- May increase risk of lymphomas and other malignancies
- Avoid live vaccines
- Do not donate blood during therapy
- Use sunscreen to prevent skin cancer
Contraindications
- Hypersensitivity
- Pregnancy
- Lactation
- Rare hereditary deficiency of hypoxanthine-guanine phosphoribosyltransferase (HGPRT) including Kelley-Seegmiller or Lesch-Nyhan syndrome
Drug interactions
- Increased plasma levels with aciclovir, valaciclovir, ganciclovir, valganciclovir
- Reduced absorption with colestyramine, magnesium- and aluminium hydroxide-containing products
- Reduced plasma levels with ciclosporin, metronidazole, quinolones, rifamycins
- May reduce plasma levels of progestins and efficacy of oral contraceptives
- May reduce efficacy of live vaccines
Food interactions
Food may affect absorption; take on empty stomach.
Use in pregnancy
Use in Pregnancy: Mycophenolate Mofetil is highly unsafe during pregnancy (Category D); definite evidence of severe fetal harm. Can cause birth defects and abortion. Completely contraindicated.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Mycophenolate Mofetil is unsafe during breastfeeding; may cause toxicity to the baby. Do not use.
Pediatric use
Dose established for children aged 3 months to 18 years (renal transplant).
Geriatric use
Elderly patients have increased risk of infections, GI bleeding and pulmonary edema.
Renal / hepatic impairment
Renal Impairment: In severe renal impairment (GFR <25 mL/min/1.73m²), not to exceed 1 g twice daily.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed.
Overdose effects
Overdose may cause over suppression of immune system and increased risk of infections; if neutropenia develops, interrupt or reduce dose.
Storage conditions
Store below 30°C in a cool and dry place, away from light; keep out of reach of children.
Chemical structure
Mycophenolate Mofetil