Mycophenolic Acid Pharmacology

Mycophenolic Acid

About Mycophenolic Acid
Anti metabolite, Purine synthesis inhibitor, Immunosuppressant.
Mechanism of Action of Mycophenolic Acid
Mycophenolic acid is a potent, selective, uncompetitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation into DNA. Because T- and B-lymphocytes are critically dependent for their proliferation on de novo synthesis of purines, whereas other cell types can utilize salvage pathways, mycophenolic acid has potent cytostatic effects on lymphocytes. Mycophenolic acid inhibits proliferative responses of T- and B-lymphocytes to both mitogenic and allospecific stimulation. Addition of guanosine or deoxyguanosine reverses the cytostatic effects of mycophenolic acid on lymphocytes. Mycophenolic acid also suppresses antibody formation by B-lymphocytes. Mycophenolic acid prevents the glycosylation of lymphocyte and monocyte glycoproteins that are involved in intercellular adhesion to endothelial cells and may inhibit recruitment of leukocytes into sites of inflammation and graft rejection.
Pharmacokinets of Mycophenolic Acid
Absorption- Well absorbed after oral and intravenous administration
Distribution- 97% bound to the plasma proteins
Metabolism- They undergo presystemic metabolism completely into active metabolite mycophenolic acid.
Excretion- Excreted via urine and feces
Onset of Action for Mycophenolic Acid
N/A
Duration of Action for Mycophenolic Acid
7 to 18 hours
Half Life of Mycophenolic Acid
17.9 hr (as oral mycophenolate mofetil) and 16.6 hr (as IV mycophenolate mofetil); 12 hr (as mycophenolate sodium).
Side Effects of Mycophenolic Acid
1. Fever
2. Chills
3. Body aches
4. Flu symptoms
5. Bruising
6. Weakness
7. Cough
8. Vomit
9. Bloody, black, or tarry stools
10. Painful or difficult urination
11. Tingly feeling
12. Upset stomach
13. Diarrhea
14. Constipation
15. Tremor
16. Anxiety
17. Insomnia
18. Swelling of the feet or lower legs
19. Skin rash

Contra-indications of Mycophenolic Acid
Rare hereditary deficiency of hypoxanthine-guanine phosphoribosyltransferase (HGPRT), including Kelley-Seegmiller or Lesch-Nyhan syndrome.
Special Precautions while taking Mycophenolic Acid
1. Stomach ulcer or other stomach disease
2. Viral, bacterial, or fungal infection
3. Hereditary deficiency of hypoxanthine-guanine phosphoribosyl-transferase (HGPRT) e.g.Lesch-Nyhan and Kelley-Seegmiller syndrome
4.Teratogenic in animals; avoid inhalation or direct skin contact
5.Monitor patients for lymphoproliferative disorders; advise patient to limit exposure to sunlight/UV light. Active peptic ulcer disease
6.Severe renal impairment


Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Mycophenolic Acid
1. Organ transplantation rejection
2. Autoimmune skin disorders
3.Immunoglobulin- A nephropathy
4.Small vessel vasculitis
5.Psoriasis
6.Lupus nephritis
Interactions for Mycophenolic Acid
1.Increased plasma levels of both drugs when combined with aciclovir, valaciclovir, ganciclovir and valganciclovir
2.Reduced absorption with colestyramine, magnesium- and aluminium hydroxide-containing products, sevelamer and other calcium-free phosphate binders
3.Reduced plasma levels with ciclosporin, metronidazole, quinolones, rifamycins
4.May reduce plasma levels of progestins; may reduce efficacy of oral contraceptives
5.Increased plasma levels with probenecid
6.May reduce efficacy of live vaccines
Typical Dosage for Mycophenolic Acid
Adults-

Prophylaxis of acute renal graft rejection
Adult: As mycophenolate mofetil: 1 g bid starting within 72 hr of transplantation. Max: 2 g/day. As mycophenolic acid: 720 mg bid.
Child: As mycophenolate mofetil: 2-18 yr: 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.


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 hr starting within 24 hr 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 hr for the first 4 days (up to a max of 14 days) following transplantation. To be started within 24 hr 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
Schedule of Mycophenolic Acid
N/A
Storage Requirements for Mycophenolic Acid
Store at room temperature. Protect from light and heat. Keep out of the reach of children.
Intravenous: Store vials and reconstituted solution at 15-30?C (59-86?F). Begin infusion within 4 hr of reconstitution.
Oral: Store at 15-30?C (59-86?F). Protect tablet from light. Do not freeze oral suspension.
Effects of Missed Dosage of Mycophenolic Acid
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Mycophenolic Acid
Give symptomatic and supportive treatment. Use bile acid sequestrants to increase the drug excretion.

Home Delivery for Mycophenolic Acid in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including mycophenolic acid.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for mycophenolic acid and other medicines and health products. Home delivery services for mycophenolic acid may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take mycophenolic acid only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for mycophenolic acid before they complete the sale. You can get this information while placing the order for mycophenolic acid with the pharmacy.

Mycophenolic Acid is a generic medicine name and there are several brands available for it. Some of the brands for mycophenolic acid might be better known than mycophenolic acid itself. If the pharmacy that's willing to deliver medicines to your home doesn't have mycophenolic acid in stock, you can ask for one of the branded alternatives for mycophenolic acid.