Page 22 - RxExam's Naplex Theory Book Part 2

www.pharmacyexam.com Krisman

A). Calcineurin Inhibitors

Dose Special Notes

Cyclosporine Please Refer To Page 334 (Part 1) of Chapter 36-Rheumatoid Arthritis.

Tacrolimus 1. Kidney 1). Tacrolimus (Prograf) binds to an intracellular protein, FKBP-12. A
(Capsule) Transplant: complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is
(Injection) 0.1 to 0.2 mg/kg then formed and the phosphatase activity of calcineurin inhibited. This
per day given as effect may inhibit T-lymphocyte activation (i.e. immunosuppression).
two divided doses.
2). Tacrolimus (Prograf) is indicated for the prophylaxis of organ
2. Heart rejection in patients receiving allogeneic kidney, heart or liver
Transplant: transplants. It is recommended that Tacrolimus be used concomitantly
0.075 mg/kg per with azathioprine or mycophenolate mofetil (MMF) and adrenal
day given as two corticosteroids.
divided doses.
3). It is important to take Tacrolimus (Prograf) capsules consistently
3. Liver every day either with or without food because the presence and
Transplant: composition of food decreases the bioavailability of Tacrolimus
0.1 to 0.15 mg/kg (Prograf). Patients should not eat grapefruit or drink grapefruit juice in
per day given as combination with Tacrolimus (Prograf).
two divided doses.
4). Tacrolimus should NOT be used simultaneously with Cyclosporine.

5). With a given dose of mycophenolic acid, exposure to mycophenolic
acid is higher with Tacrolimus co-administration than with
cyclosporine co-administration because cyclosporine interrupts the
enterohepatic recirculation of mycophenolic acid while tacrolimus
does not. Clinicians should be aware that there is also a potential for
increased mycophenolic acid exposure after crossover from
cyclosporine to Tacrolimus (Prograf) in patients concomitantly
receiving mycophenolic acid-containing products.

6). Coadministration with magnesium and aluminum hydroxide
antacids increase Tacrolimus (Prograf) whole blood concentrations.
Monitoring of whole blood concentrations and appropriate dosage
adjustments of tacrolimus are recommended when these drugs and
Tacrolimus (Prograf) are used concomitantly.

7). Due to its potential for nephrotoxicity, consideration should be
given to dosing Tacrolimus (Prograf) at the lower end of the
therapeutic dosing range in patients who have received a liver or heart
transplant and have pre-existing renal impairment.

8). Serious infections, nephrotoxicity, neurotoxicity, hyperkalemia,
hypertension myocardial hypertrophy and pure red cell aplasia are commonly
reported side effects of Tacrolimus (Prograf).

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