Page 26 - RxExam's Naplex Theory Book Part 2

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Dose Special Notes

Sirolimus 6). The initial dose of Sirolimus (Rapamune) should be administered as
(Tablet) soon as possible after transplantation. Since Cyclosporine is a
(Oral solution) substrate and inhibitor of CYP3A4 and P-gp, it is recommended that
Sirolimus (Rapamune) be taken 4 hours after administration of
Cyclosporine.

7). St. John's Wort (hypericum perforatum) induces CYP3A4 and P-gp.
Since sirolimus is a substrate for both cytochrome CYP3A4 and P-gp,
there is the potential that the use of St. John’s Wort in patients
receiving Sirolimus (Rapamune) could result in reduced sirolimus
concentrations. Concurrent use should be strictly avoided.

8). The maintenance dose of Sirolimus (Rapamune) should be reduced
by approximately one third in patients with mild-to-moderate hepatic
impairment and by approximately one half in patients with severe
hepatic impairment. It is not necessary to modify Sirolimus
(Rapamune) loading dose in patients with mild, moderate, and severe
hepatic impairment.

9). Increased susceptibility to infections, hypersensitivity reactions,
exfoliative dermatitis, angioedema, hyperlipidemia, proteinuria and
decline in renal function are reported side effects of Sirolimus
(Rapamune).

Mycophenolic 1. Renal 1). Mycophenolic acid (Myfortic) delayed-release tablets are an enteric
Acid Transplant: formulation of Mycophenolate sodium that delivers the active moiety
(Tablet, DR) Mycophenolic acid (Myfortic). Mycophenolic acid is an uncompetitive
720 mg PO BID on and reversible inhibitor of inosine monophosphate dehydrogenase
DR = Delayed an empty stomach, (IMPDH), and therefore inhibits the de novo pathway of guanosine
Release one hour before nucleotide synthesis without incorporation to DNA. Because T- and B-
or two hours after lymphocytes are critically dependent for their proliferation on de novo
food intake. synthesis of purines, Mycophenolic acid (Myfortic) has potent
cytostatic effects on lymphocytes.

2). Mycophenolic acid (Myfortic) is indicated for the prophylaxis of
organ rejection in patients receiving allogeneic renal transplants,
administered in combination with cyclosporine and corticosteroids.

3). Mycophenolic acid (Myfortic) 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. Patients are to be instructed that Mycophenolic acid
(Myfortic) tablets should not be crushed, chewed, or cut prior to
ingesting.

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