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Astagraf XL Dosage

Generic name: TACROLIMUS 0.5mg
Dosage form: capsule, coated, extended release

The information at Drugs.com is not a substitute for medical advice. Always consult your doctor or pharmacist.

Administration Instructions

Take ASTAGRAF XL consistently every morning at the same time (to ensure consistent and maximum possible drug exposure) on an empty stomach at least 1 hour before a meal or at least 2 hours after a meal [see Clinical Pharmacology (12.3)].
Swallow ASTAGRAF XL capsules whole with liquid; do not chew, divide, or crush the capsules.
If a dose is missed, take the dose up to 14 hours after the scheduled time (i.e., for a missed 8:00 AM dose, take by 10:00 PM). Beyond the 14-hour time frame, wait until the usual scheduled time the following morning to take the next regular daily dose.
Avoid eating grapefruit or drinking grapefruit juice or alcoholic beverage while taking ASTAGRAF XL [see Drug Interactions (7.2)].

Recommended Starting Dosage

Table 1 includes the recommended starting ASTAGRAF XL dosages. Due to the reduced clearance and prolonged half-life, patients with severe hepatic impairment (Child-Pugh ≥ 10) may require a lower starting dosage of ASTAGRAF XL [see Clinical Pharmacology (12.3)].

Table 1: Recommended Starting Dosage of ASTAGRAF XL with or without Basiliximab Induction
Concomitant Medications Starting Dosages of ASTAGRAF XL
MMF = mycophenolate mofetil

With MMF, steroids, and basiliximab induction

Administer 0.15 to 0.2 mg/kg prior to reperfusion or within 48 hours of the completion of the transplant procedure (timing may be delayed until renal function has recovered).

With MMF and steroids;

Without basiliximab induction

First Dose (pre-operative): Administer 0.1 mg/kg as a single dose within 12 hours prior to reperfusion.
Second Dose (post-operative): Administer 0.2 mg/kg at least 4 hours after the pre-operative dose and within 12 hours after reperfusion.

Dosage Adjustments

Titrate the ASTAGRAF XL dosage based on clinical assessments of rejection and tolerability and to achieve target trough concentration ranges (see Table 2) [see Dosage and Administration (2.4) and Warnings and Precautions (5.6, 5.7, 5.11)].

African-American patients, compared to Caucasian patients, may need to be titrated to higher ASTAGRAF XL dosages to attain comparable trough concentrations [see Clinical Pharmacology (12.3) and Clinical Studies (14)].

Table 2: Recommended Target Tacrolimus Whole Blood Trough Concentrations in Kidney Transplant Patients
For observed tacrolimus concentrations see Clinical Studies (14).

Time Period Post Transplant

Tacrolimus Target Whole Blood Trough Concentrations

During Month 1

7 to 15 ng/mL (with basiliximab induction)

10 to 15 ng/mL (without basiliximab induction)

Months 2 to 6

5 to 15 ng/mL

> 6 Months

5 to 10 ng/mL

Therapeutic Drug Monitoring

Measure tacrolimus whole blood trough concentrations at least two times on separate days during the first week after initiation of dosing and after a change in dosage, after a change in co-administration of CYP3A4 inducers and/or inhibitors, or after a change in renal or hepatic function. When interpreting measured concentrations, consider that the time to achieve tacrolimus steady state is approximately 7 days after initiating or changing the ASTAGRAF XL dose.

Monitor tacrolimus whole blood trough concentrations using a validated assay [e.g., immunoassays or high-performance liquid chromatography with tandem mass spectrometric detection (HPLC/MS/MS)]. The immunosuppressive activity of tacrolimus is mainly due to the parent drug rather than to its metabolites. Immunoassays may react with metabolites as well as the parent drug. Therefore, whole blood tacrolimus trough concentrations obtained with immunoassays may be numerically higher than concentrations obtained with an assay using HPLC/MS/MS. Comparison of the whole blood tacrolimus trough concentrations of patients to those described in the prescribing information and other published literature must be made with knowledge of the assay method(s) employed.

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