Tacrolimus Administration, Monitoring Parameters and Chemical Structure
Oral Administration
- Administer at approximately the same time each day. To minimize variations in bioavailability, administer consistently with or without food. Administration with food or within 1 hour of a meal, especially high-fat meals, results in significantly decreased absorption.
- Do not administer with grapefruit juice.
- To convert an oral dose to an IV dose, take the total daily oral dose and give 25% to 33% of the dose by a continuous intravenous infusion (personal communication, Astellas Pharma, Inc.). When converting to oral therapy from intravenous treatment, the first oral dose should be given 8 - 12 hours following discontinuation of the IV infusion.
- Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F).
Extemporaneous compounding preparation † :
- A 0.5 mg/ml suspension can be made by mixing the contents of six-5 mg tacrolimus capsules with equal amounts of Ora-Plus® and Simple Syrup, NF to make a final volume of 60 ml. When stored at room temperature in either glass or plastic amber bottles, the suspension is stable for 56 days. Shake well before each use.
Intravenous Administration
- Because of the risk of hypersensitivity reactions (see Contraindications/Precautions), IV administration should be reserved for patients who cannot take tacrolimus orally. Oral therapy should replace IV therapy as soon as possible.
- Observe patients for 30 minutes after beginning the infusion and frequently thereafter for possible hypersensitivity reactions.
- Visually inspect parenteral products for particulate matter and discoloration prior to administration whenever solution and container permit.
- Due to chemical instability, tacrolimus should not be mixed or infused with solutions with a pH >= 9 (e.g., acyclovir or ganciclovir).
Dilution:
- The concentrate for injection must be diluted with NS or D5W injection to a final concentration of 4 - 20 mcg/ml.
- Prepare solutions in polyethylene or glass containers to allow storage for 24 hours. Do not use polyvinyl chloride (PVC) containers because stability is decreased and the polyoxyl 60 hydrogenated castor oil in the formulation may leach phthalates from PVC containers.
Intravenous infusion:
- Administer through non-PVC tubing to minimize the potential for drug adsorption onto the tubing.
- Infuse the required daily dose of the diluted IV solution over 24 hours. As an alternative, the daily dose may be divided equally into two doses and infused over 4 hours.
Topical Administration
- Apply as a thin layer and rub in gently and completely. Before applying the ointment after a bath or shower, make sure the skin is completely dry.
- Avoid the eyes and surrounding area.
- Do not use with occlusive dressings. Use of occlusive dressings may promote systemic absorption.
- Store ointment at room temperature, 15 - 30 degrees C (59 - 86 degrees F).
† non-FDA approved
[ Last revised: 4/25/2006 4:32:00 PM ]
References
. Jacobson PA, Johnson CE, West NJ, et al. Stability of tacrolimus in an extemporaneously compounded oral liquid. Am J Health Syst Pharm 1997;54:178 - 80.
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Tacrolimus Monitoring Parameters
- blood glucose: systemic therapy
- CBC: systemic therapy
- LFTs: systemic therapy
- serum creatinine/BUN: systemic therapy
- serum electrolytes: systemic therapy
- serum lipid profile: systemic therapy
- serum potassium: systemic therapy
- serum tacrolimus concentrations: systemic therapy
- serum uric acid: systemic therapy
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Chemical Structure For: Tacrolimus
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