Supresta

Supresta Uses, Dosage, Side Effects, Food Interaction and all others data.

Supresta delayed-release tablets are enteric coated formulation of mycophenolate sodium that delivers the active moiety mycophenolic acid. It is an immunosuppressive agent. It is an uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH). Therefore, it inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation to DNA. Supresta has cytostatic effects on lymphocytes. It has been shown to prevent the occurrence of acute rejection of kidney and heart allotransplantation. It also decreases antibody production.

Supresta is an antibiotic substance derived from Penicillium stoloniferum. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase. Supresta is important because of its selective effects on the immune system. It prevents the proliferation of T-cells, lymphocytes, and the formation of antibodies from B-cells. It also may inhibit recruitment of leukocytes to inflammatory sites.

Trade Name Supresta
Generic Mycophenolic acid
Mycophenolic acid Other Names Acide mycophenolique, Acido micofenolico, Acidum mycophenolicum, Micofenolico acido, Mycophenolate, Mycophenolic acid, Mycophenolsäure
Type
Formula C17H20O6
Weight Average: 320.3371
Monoisotopic: 320.125988372
Protein binding

>98%

Groups Approved
Therapeutic Class Immunosuppressant
Manufacturer
Available Country Russia
Last Updated: September 19, 2023 at 7:00 am
Supresta
Supresta

Uses

Prophylaxis of organ rejection in kidney transplant: Supresta is used for the prophylaxis of organ rejection in adult patients receiving a kidney transplant. It is used for the prophylaxis of organ rejection in pediatric patients 5 years of age and older who are at least 6 months post kidney transplant.

Supresta is also used to associated treatment for these conditions: Kidney Transplant Rejection

How Supresta works

Supresta 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. Supresta 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. Supresta also suppresses antibody formation by B-lymphocytes. Supresta 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.

Dosage

Supresta dosage

Dosage in adult kidney transplant patients: The recommended dose of Supresta is 720 mg administered twice daily (1440 mg total daily dose).

Dosage in pediatric kidney transplant patients: The recommended dose of Supresta in conversion (at least 6 months post-transplant) pediatric patients age 5 years and older is 400 mg/m2 body surface area (BSA) administered twice daily (up to a maximum dose of 720 mg administered twice daily). Pediatric patients with a BSA of 1.19 to 1.58 m2 may be dosed either with three Supresta 180 mg tablets, or one 180 mg tablet plus one 360 mg tablet twice daily (1080 mg daily dose). Patients with a BSA of >1.58 m2 may be dosed either with four Supresta 180 mg tablets, or two Supresta 360 mg tablets twice daily (1440 mg daily dose).

Supresta tablets should be taken on an empty stomach, 1 hour before or 2 hours after food intake. Tablets should not be crushed, chewed, or cut prior to ingesting. The tablets should be swallowed whole in order to maintain the integrity of the enteric coating.

Side Effects

The most common adverse reactions (≥20%) associated with the administration of Supresta are anemia, leukopenia, constipation, diarrhea, vomiting, dyspepsia, urinary tract infection, CMV infection, insomnia, and postoperative pain.

Toxicity

Oral (LD50): Acute: 352 mg/kg [Rat], 1000 mg/kg [Mouse], and >6000 mg/kg Rabbit. Possible signs and symptoms of acute overdose could include the following: hematological abnormalities such as leukopenia and neutropenia, and gastrointestinal symptoms such as abdominal pain, diarrhea, nausea and vomiting, and dyspepsia.

Precaution

Supresta tablets are used with caution because it-

  • Can cause embryofetal toxicity
  • Can increase new or reactive viral infections
  • Can cause blood dyscrasias including pure red cell aplasia
  • Can cause serious GI tract complications (gastrointestinal bleeding, perforations and ulcers)
  • May increase the risk of developing lymphomas and other malignancies, particularly of the skin
  • Use of live vaccine should be avoided during treatment with Supresta

Interaction

Caution should be exercised with concomitant administration of Antacids, Azathioprine, Cyclosporin, Rifampin, Sevelamer, Cholestyramine, Acyclovir, Metronidazole, Hormonal contraceptives as these medicines may decrease Supresta concentration.

Food Interaction

  • Take on an empty stomach. Take mycophenolic acid at least 1 hour before or 2 hours after eating.

Volume of Distribution

  • 54 ± 25 L

Elimination Route

Bioavailability following oral administration of Myfortic delayed-release tablet ranges from 70-95%

Half Life

The mean elimination half-life for mycophenolic acid ranges from 8-16 hours, while that of the MPAG metabolite ranges from 13-17 hours.

Clearance

  • 140 +/- 30 mL/min [Stable renal transplant patients]

Pregnancy & Breastfeeding use

Pregnancy Category D. Can cause fetal harm.

Lactation: Discontinue Supresta or discontinue nursing while on treatment or within 6 weeks after stopping therapy. Take into consideration the importance of the drug to the mother.

Contraindication

Supresta delayed-release tablets and Mycophenolate mofetil tablets and capsules should not be used interchangeably without physician supervision because the rate of absorption following the administration of these two products is not equivalent.

Acute Overdose

No data are available with regard to overdose.

Storage Condition

Store at 25° C and Keep out of reach of children.

Innovators Monograph

You find simplified version here Supresta

Supresta contains Mycophenolic acid see full prescribing information from innovator Supresta Monograph, Supresta MSDS, Supresta FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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