Tacrolimus
PROGRAF
Pronunciation: ta-KROE-li-mus (PROE-graf)
“Tacky lima’s Pro graphing”
What it isCalcineurin inhibitor that suppresses T-cell signaling; prevention of transplant rejection.
Why this oneIt prevents rejection more effectively than cyclosporine and avoids that drug's hirsutism and gingival overgrowth.
What limits itNarrow index with trough monitoring, nephrotoxicity, tremor and post-transplant diabetes. CYP3A4 makes interactions constant.
FDA-approved for
- transplant immunosuppression (1994)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Kidney transplant rejection prophylaxis (with azathioprine) | Adults | 0.2 mg/kg/day ÷ q12h | Trough mo 1-3: 7-20 ng/mL; mo 4-12: 5-15 ng/mL | Per trough level |
| Kidney transplant rejection prophylaxis (with MMF/IL-2 antagonist) | Adults | 0.1 mg/kg/day ÷ q12h | Trough mo 1-12: 4-11 ng/mL | Per trough level |
| Liver transplant rejection prophylaxis (with corticosteroids) | Adults | 0.10-0.15 mg/kg/day ÷ q12h | Trough mo 1-12: 5-20 ng/mL | Per trough level |
| Heart transplant rejection prophylaxis (with azathioprine or MMF) | Adults | 0.075 mg/kg/day ÷ q12h | Trough mo 1-3: 10-20 ng/mL; mo ≥4: 5-15 ng/mL | Per trough level |
| Liver transplant rejection prophylaxis | Pediatric | 0.15-0.2 mg/kg/day ÷ q12h | Trough mo 1-12: 5-20 ng/mL | Per trough level |
Renal Pre-existing renal impairment (liver/heart tx): dose at lower end of range; further reductions may be needed (nephrotoxicity risk)
Hepatic Severe (Child-Pugh ≥10): may require lower doses; monitor blood concentrations closely
Instructions
- Take capsules consistently with or without food (same way each time)
- IV route for patients unable to tolerate oral
- Therapeutic drug monitoring of whole-blood trough recommended
- Avoid grapefruit / grapefruit juice
- Not interchangeable/substitutable with extended-release tacrolimus products
- African-American patients may require higher doses
Available strengths
- cap 0.5, 1, 5 mg
- ER cap 0.5, 1, 5 mg
- ER tab 0.75, 1, 4 mg
- susp 0.2, 1 mg/packet
- ointment 0.03, 0.1 %
- inj 5 mg/mL
Cautions
- New-onset diabetes after transplant — monitor glucose
- Nephrotoxicity (acute/chronic) — caution with other nephrotoxic drugs
- Neurotoxicity incl. PRES; hyperkalemia; hypertension
- Anaphylaxis with IV formulation; not recommended with sirolimus (liver/heart); myocardial hypertrophy
- Medication errors — not interchangeable with ER products
Adverse reactions
- Abnormal renal function
- Hypertension
- Diabetes mellitus/hyperglycemia
- Tremor
- Infections (incl. CMV, UTI, bronchitis)
- Headache
- Insomnia
- Paresthesia
- Peripheral edema
- GI (nausea, diarrhea, constipation, abdominal pain)
- Anemia/leukopenia
- Hyperkalemia
- Hypomagnesemia
- Hyperlipemia
Pregnancy Can cause fetal harm; associated with prematurity, birth defects, low birth weight, fetal distress
Lactation Undefined
Cost
| Strength | #/mo | generic $/mo | CostPlus | |
|---|---|---|---|---|
| 0.5 mg | cap | 60 BID | $7.36 | offered |
| 1 mg | cap | 60 BID | $9.21 | offered |
| 5 mg | cap | 60 BID | $41.28 | offered |
Other forms: Tacrolimus ointment (PROTOPIC)
Generic entry2009
⚠ BOXED WARNING
- Malignancies and serious infections
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityNephrotoxicity, neurotoxicity, hypertension, diabetes and extensive interaction/level-monitoring burden.
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