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Mycophenolic Acid information from DrugsUpdate  

See Available Brands of Mycophenolic Acid in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation
FI - Food *

Mycophenolic acid mycophenolate is an immunosuppressant drug used to prevent rejection in organ transplantation. It was initially marketed as the prodrug mycophenolate mofetil (MMF) to improve oral bioavailability. More recently, the salt mycophenolate sodium has also been introduced. Mycophenolic acid is commonly marketed under the trade names CellCept (mycophenolate mofetil; Roche) and Myfortic (mycophenolate sodium; Novartis).

Pharmacodynamics

Pharmacokinetics

Mycophenolic acid acts by blocking purine synthesis of human lymphocytes through reversible inhibition of inosine monophosphate dehydrogenase. It also inhibits proliferation of both T- and B- lymphocytes.

Absorption
Mycophenolate mofetil/mycophenolate sodium: Both extensively absorbed from the GI tract.

Distribution
Mycophenolic acid (MPA): 97% bound to plasma proteins.

Metabolism

Mycophenolate is converted to active MPA, which undergoes enterohepatic recirculation. MPA is metabolised by glucuronidation to the inactive glucuronide.

Excretion
Via urine (as the glucuronide and negligible amounts of MPA); via faeces (about 6% of a dose). Mean half-life of MPA: 17.9 hours (as oral mycophenolate mofetil) and 16.6 hours (as IV mycophenolate mofetil); 12 hours (as mycophenolate sodium).

Mycophenolic Acid Indications / Mycophenolic Acid Uses

Information Not Available

Mycophenolic Acid Adverse Reactions / Mycophenolic Acid Side Effects

Diarrhoea, vomiting, GI haemorrhage and perforation; leucopenia; asthenia, pain, headache, anaemia, thrombocytopenia, renal tubular necrosis, haematuria, BP changes, hyperglycaemia, disturbances of electrolytes and blood lipids, peripheral oedema, dyspnoea, cough, acne, rash, alopecia, dizziness, insomnia, paraesthesia, tremor, hypersensitivity reactions, pancreatitis, hepatitis.

Potentially Fatal: Angioedema, anaphylaxis, fatal pulmonary fibrosis.

Precautions

Warnings
Administer under the supervision of a health care provider experienced in immunosuppressive therapy and management of organ transplantation and in an equipped facility. Increased risk of lymphoma and increased susceptibility to infection may be related to immunosuppression.

Administration is associated with increased risk of pregnancy loss and congenital malformations. Women of childbearing potential must use contraception.

Monitor

Perform CBCs weekly during the first month, twice monthly during the second and third months, then monthly through the first year. Monitor patient for signs and symptoms of bacterial, viral, or fungal infections, and for signs and symptoms of organ rejection.

Overdosage
No reported cases. At plasma levels >100 mcg/ml, small amounts of the inactive metabolite may be removed by haemodialysis. Excretion of MPA may be enhanced by bile acid sequestrants (e.g. colestyramine).

Special Precautions

Teratogenic in animals; avoid inhalation or direct skin contact. Monitor patients for lymphoproliferative disorders; advise patient to limit exposure to sunlight/UV light. Active peptic ulcer disease. Severe renal impairment. Mycophenolate mofetil and mycophenolate sodium are not interchangeable. Perform CBCs; monitor for neutropenia.

Other Drug Interactions

Increased plasma levels of both drugs when combined with aciclovir, valaciclovir, ganciclovir and valganciclovir. Reduced absorption with colestyramine, magnesium- and aluminium hydroxide-containing products, sevelamer and other calcium-free phosphate binders. Reduced plasma levels with ciclosporin, metronidazole, quinolones, rifamycins. May reduce plasma levels of progestins; may reduce efficacy of oral contraceptives. Increased plasma levels with probenecid. May reduce efficacy of live vaccines.

Other Interactions

Food Interaction
Food reduces MPA peak serum levels by 40% and 33% following mycophenolate mofetil and mycophenolate sodium admin, respectively. Extent of absorption is not affected. Avoid cat's claw and echinacea as they have immunostimulant effects.

Dosage

Oral
Prophylaxis of acute renal graft rejection
Adult: As mycophenolate mofetil: 1 g bid starting within 72 hours of transplantation. Max: 2 g/day. As mycophenolic acid: 720 mg bid.
Child: As mycophenolate mofetil: 2-18 years: 600 mg/m2 bid. Max: 1 g bid. BSA 1.25-1.5 m2: 750 mg bid; >1.5 m2: 1 g bid. As mycophenolic acid: 5-16 yr: 400 mg/m2 bid (max: 720 mg bid). BSA 1.19-1.58 m2: 540 mg bid (max: 1,080 mg); >1.58 m2: 720 mg bid (max: 1,440 mg).
Elderly: As mycophenolic acid: Max: 720 mg bid.
Renal impairment: Severe chronic renal impairment (GFR <25 ml/min/1.73 m2): Avoid >1 g bid of mycophenolate mofetil.

Oral
Prophylaxis of cardiac graft rejection
Adult: As mycophenolate mofetil: 1.5 g bid starting within 5 days after transplantation.

Intravenous
Prophylaxis of acute renal graft rejection
Adult: As mycophenolate mofetil: 1 g bid by IV infusion over 2 hours starting within 24 hours after transplantation for up to 14 days, convert to oral therapy as soon as possible.
Renal impairment: Severe chronic renal impairment (GFR <25 ml/min/1.73 m2): Avoid >1 g bid of mycophenolate mofetil.

Intravenous
Prophylaxis of hepatic transplant rejection
Adult: As mycophenolate mofetil: 1 g bid by IV infusion over 2 hours for the first 4 days (up to a max of 14 days) following transplantation. To be started within 24 hours of transplantation. Subsequently, convert to oral admin at 1.5 g bid as soon as possible.

Intravenous
Prophylaxis of cardiac graft rejection
Adult: As mycophenolate mofetil: 1.5 g bid starting within 5 days after transplantation, convert to oral admin as soon as possible.

Reconstitution
Reconstitute in glucose 5% to a final concentration of 6 mg/ml mycophenolate mofetil.

Food(before/after)

Information Not Available

List of Contraindications

Mycophenolic Acid and Pregnancy

Contraindicated in pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Mycophenolic Acid and Lactation

Contraindicated in lactation

Mycophenolic Acid and Children

CellCept
Safety and efficacy in cardiac or hepatic transplants not established.

Myfortic
Safety and efficacy not established; however, there are limited pharmacokinetic data available for the safety and efficacy of Myfortic use in children 5 to 16 years of age who are stable pediatric renal transplant patients.

Mycophenolic Acid and Geriatic

Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Mycophenolic Acid and Other Contraindications

Pregnancy, lactation. Rare hereditary deficiency of hypoxanthine-guanine phosphoribosyltransferase (HGPRT), including Kelley-Seegmiller or Lesch-Nyhan syndrome.

Storage

Intravenous
Store vials and reconstituted solution at 15-30°C (59-86°F). Begin infusion within 4 hours of reconstitution.

Oral

Store at 15-30°C (59-86°F). Protect tablet from light. Do not freeze oral suspension.

Lab interference

Intravenous
Store vials and reconstituted solution at 15-30°C (59-86°F). Begin infusion within 4 hours of reconstitution.

Oral

Store at 15-30°C (59-86°F). Protect tablet from light. Do not freeze oral suspension.

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