II. Indications
- See Tacrolimus Ointment for use in Atopic Dermatitis
- FDA Approved indications
- Allogenic Organ Transplant (Kidney, Liver, Heart)
- Used in combination with other immunosupressants (e.g. Mycophenolate)
- Allogenic Organ Transplant (Kidney, Liver, Heart)
- Other Non-FDA approved indications
- Other organ transplant (Cornea, Pancreas, Kidney)
- Lupus Nephritis
- Crohns Disease
- Membranous Glomerulonephritis
- Myasthenia Gravis
III. Mechanism
- See Calcineurin Inhibitor
- Tacrolimus is a Macrolide isolated from the Bacteria Streptomyces tsukubaensis
- Tacrolimus is a Calcineurin Inhibitor via binding the FKBP 12 Protein
IV. Medications
- Tacrolimus capsules: 0.5 mg, 1 mg, 5 mg
- Tacrolimus extended release capsules (Astagraf XL): 0.5 mg, 1 mg, 5 mg
- Tacrolimus extended release tablets (Envarsus XR): 0.75 mg, 1 mg, 4 mg
V. Dosing
- See other references for specific dosing regimens per indication
- Prescribers are typically specialists knowledgeable about the risks and monitoring of Tacrolimus
- Decrease dose in renal dysfunction, and adjust doses based on serum levels
VI. Adverse Effects
- Nephrotoxicity
- Hepatotoxicity
- Cardiovascular adverse effects
- Hypertension
- QTc Prolongation
- Myocardial hypertrophy
- Neurologic adverse effects
- Gastrointestinal (more prominent than Cyclosporine)
- Secondary Malignancy
- Squamous cell cancer
- Lymphoproliferative disorders
- Miscellaneous adverse effects
- Hyperkalemia
- Diabetes Mellitus
- Alopecia
- Serious infections (Bacterial, viral, fungal)
VII. Safety
- Pregnancy Category C
- Avoid in Lactation per drug label
- However thought to be safe in Lactation based on registry data
- https://pubmed.ncbi.nlm.nih.gov/30000743/
- Monitoring
VIII. Pharmacokinetics
- Hepatic Metabolism (CYP3A4)
- Biliary excretion (95%)
IX. Drug Interactions
- See Calcineurin Inhibitor
-
Nephrotoxic Drugs (e.g. Aminoglycosides, Amphotericin B)
- Avoid in combination with Tacrolimus (combination increases nephrotoxicity)
- Numerous Drug Interactions (see other references)
- Tacrolimus is CYP3A4 metabolized
- Many medications alter Tacrolimus absorption and serum levels
X. Efficacy
- Similar efficacy and more potent than Cyclosporine in Solid Organ Transplant
XI. Resources
- Tacrolimus Capsules (DailyMed)
- Calcineurin Inhibitors (Stat Pearls)
Images: Related links to external sites (from Bing)
Related Studies
| tacrolimus (on 11/2/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| TACROLIMUS 0.03% OINTMENT | Generic | $0.73 per gram |
| TACROLIMUS 0.1% OINTMENT | Generic | $1.91 per gram |
| TACROLIMUS 0.5 MG CAPSULE (IMMEDIATE RELEASE) | Generic | $0.19 each |
| TACROLIMUS 1 MG CAPSULE (IMMEDIATE RELEASE) | Generic | $0.28 each |
| TACROLIMUS 5 MG CAPSULE (IMMEDIATE RELEASE) | Generic | $1.55 each |
| prograf (on 1/12/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| PROGRAF 0.5 MG CAPSULE | Generic | $0.19 each |
| PROGRAF 1 MG CAPSULE | Generic | $0.28 each |
| astagraf xl (on 1/12/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| ASTAGRAF XL 1 MG CAPSULE | $4.96 each | |
| envarsus xr (on 12/23/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| ENVARSUS XR 1 MG TABLET | $6.19 each | |