Mycophenolate Mofetil

BRAND NAMES:

Myfenax – It contains the active ingredient of mycophenolate mofetil. It consists of compositions of ciclosporin and corticosteroids. It is available in the form of film-coated oral tablets used for prophylaxis of acute transplant rejection in patients receiving allogeneic transplantation of renal, cardiac, and hepatic organs. 

Myhibbin – It contains the active ingredients of mycophenolate mofitil. It is available in the form of oral suspension.

Cellcept – It contains the active ingredients of mycophenolate mofitil. It is available in the form of oral suspension and tablets. It is taken combination therapy with immunosuppressive drugs.

MECHANISM OF ACTION:

Mycophenolate mofetil is an immunosuppressant drug. It inhibits the formation of T cells and B cells by converting to its active form, mycophenolic acid. This, in turn, reduces immunological and antibody responses, as well as the synthesis of inflammatory mediators, thus limiting inflammation and graft rejection. It is frequently used in combination with other immunosuppressive medications.

PHARMACOKINETICS:

Absorption: Mycophenolate mofetil is quickly absorbed in the small intestine. The highest concentration of its active metabolite, MPA, is achieved 60 to 90 minutes after an oral dose. Food does not interfere with the absorption of mycophenolate mofetil.

Distribution: Mycophenolate mofetil is administered at a volume of 3.6 to 4.0 L/kg.

Metabolism: Administration can be done orally or intravenously. Mycophenolate mofetil is entirely metabolized by liver carboxylesterases 1 and 2 to mycophenolic acid, the active parent medicine. It is then metabolised by the enzyme glucuronyl transferase, producing the inactive phenolic glucuronide MPA.

Excretion: When mycophenolate mofetil was given orally in a pharmacokinetics study, it was found to be 93% excreted in urine and 6% excreted in feces.

PHARMACODYNAMICS:

Mycophenolate mofetil is a mycophenolic acid derivative. MPA, the active form of mycophenolate, inhibits immune cell growth and antibiotic synthesis, both of which cause transplant rejection. Therefore the mentioned benefits result in high rates of successful transplantation, preventing the catastrophic effects of graft rejection. 

DOSAGE AND ADMINISTRATION:

Mycophenolate is available in several forms, including capsules, tablets, delayed-release tablets, and oral suspension. It is typically taken twice a day on an empty stomach. Mycophenolate is available in tablets, capsules, oral suspension, injectable powder, and delayed-release tablets. 

• Capsules – 250mg

• Tablet – 500mg

• Oral suspension- 200mg/ml

• Powder for injection – 500mg/vial

• Tablet- delayed release – 180mg and 360mg

DRUG INTERACTIONS:

Drug interactions of Mycophenolate mofetil may interact with an 

• Immunosuppressant – azathioprine

• Anti-viral medications – acyclovir and ganciclovir

• Tuberculosis – rifampicin

• Antibiotic – norfloxacin+metronidazole

CONTRAINDICATIONS:

Contraindications include hypersensitivity to mycophenolate mofetil, mycophenolic acid, or any component of the drug product. When combined with other immunosuppressive treatments, patients treated with mycophenolate are more likely to develop lymphomas and other malignancies, particularly those of the skin.

SIDE EFFECTS:

Mycophenolate may cause side effects.

• Constipation

• Nausea

• Vomiting

• Difficulty falling asleep 

• Pain, especially in the back, muscle or joints

• Headache

• Tremor

Some side effects can be serious

• Sudden severe stomach pain, stomach pain or diarrhea

• Difficulty breathing

• Chest pain

• Rash

• Itching

• Dizziness

• Fever

• Muscle pain

OVERDOSE:

Symptoms of overdose may include

• Sudden severe stomach pain

• Difficulty breathing

• Rash

• Itching

• Dizziness, fainting, pale skin, and fast heartbeat

• Lack of energy

• Vomiting or spitting up blood

• Tarry stools

• joint stiffness or pain

TOXICITY:

Acute overdose symptoms may include hematological abnormalities, such as leukopenia, as well as gastrointestinal problems.