Classifications: biologic response modifier; immunosuppressant; Therapeutic:immunosuppressant
Pregnancy Category: C
0.5 mg, 1 mg, 5 mg capsules; 5 mg/mL injection; 0.1%, 0.03% ointment
Inhibits helper T-lymphocytes by selectively inhibiting secretion of interleukin-2, interleukin-3, and interleukin-gamma;
thus reduces transplant rejection.
Inhibits antibody production (thus subduing immune response) by creating an imbalance in favor of suppressor T-lymphocytes.
Liver rejection prophylaxis; rejection prophylaxis for other organ transplants (kidney, heart, bone marrow, pancreas, small
bowel), moderate to severe atopic dermatitis (e.g., eczema).
Acute organ transplant rejection, severe plaque-type psoriasis.
Hypersensitivity to tacrolimus or castor oil; pregnancy (category C), lactation.
Renal or hepatic insufficiency, hyperkalemia, QT prolongation; CHF; diabetes mellitus, gout, history of seizures, hypertension.
Route & Dosage
Adult: PO 0.150.2 mg/kg/d in 2 divided doses q12h, start no sooner than 6 h after transplant; give first oral dose 812
h after discontinuing IV therapy IV 0.010.05 mg/kg/d as continuous IV infusion, start no sooner than 6 h after transplant, continue until patient can
take oral therapy
Child: PO 0.150.2 mg/kg/d IV 0.030.05 mg/kg/d
Adult: Topical Apply thin layer to affected area b.i.d., continue until clearing of symptoms
Child (215 y): Topical Apply thin layer of 0.03% ointment to affected area b.i.d., continue until clearing of symptoms
Severe Plaque-Type Psoriasis
Adult: PO Start with 0.05 mg/kg/d, increase to 0.1 mg/kg/d at week 3 and to 0.15 mg/kg/d at week 6 if necessary
Start with lower dose.
Hemodialysis: Supplementation not necessary
- Discontinue cyclosporine at least 24 h before the first dose of tacrolimus.
- Convert patient from IV to oral therapy as soon as possible.
- Give first oral dose 812 h after discontinuing IV infusion.
- Ensure that skin is clean and completely dry before application.
- Apply a thin layer to the affected area and rub in gently and completely.
- Do not apply occlusive dressing over the site.
PREPARE: IV Infusion: Dilute 5 mg/mL ampules with NS or D5W to a concentration of 0.0040.02 mg/mL; use a less concentrated solution for
ADMINISTER: IV Infusion: Give as continuous IV.
INCOMPATIBILITIES Y-site: Phenytoin.
- Store ampules between 5° and 25° C (41° and 77° F); store capsules at room temperature, 15°30°
C (59°86° F).
- Store the diluted infusion in glass or polyethylene containers and discard after 24 h.
Adverse Effects (≥1%)CNS: Headache, tremors, insomnia, paresthesia, hyperesthesia
and/or sensations of warmth, circumoral numbness. CV: Mild to moderate hypertension. Endocrine:
Hirsutism, hyperglycemia, hyperkalemia, hypokalemia, hypomagnesemia,
hyperuricemia, decreased serum
cholesterol. GI: Nausea, abdominal pain, gas,
appetite changes, vomiting, anorexia, constipation, diarrhea
, ascites. Hematologic: Anemia, leukocytosis, thrombocytopenia purpura. Urogenital:
UTI, oliguria, nephrotoxicity. Respiratory: Pleural effusion, atelectasis, dyspnea. Special Senses:
Blurred vision, photophobia. Skin: Flushing, rash, pruritus, skin irritation, alopecia
, folliculitis, hyperesthesia, exfoliative dermatitis,
hirsutism, photosensitivity, skin discoloration, skin ulcer, sweating. Body as a Whole: Pain, fever, peripheral edema, increased risk of cancer.
Use with cyclosporine
increases risk of nephrotoxicity. Erythromycin, metoclopramide
may increase levels; caspofungin, rifampin
may decrease levels. nsaid
s may lead to oliguria or anuria. Herbal: St. John's wort
. Food: Grapefruit juice
(>1 qt/d) may increase plasma
concentrations and adverse effects.
Erratic and incompletely from GI tract; absolute bioavailability approximately 1425%; absorption reduced by food. Peak:
PO 14 h. Duration: IV
12 h. Distribution:
, tacrolimus is found primarily in lipoprotein-deficient fraction; 7597% protein bound; distributed
into red blood cells; blood:plasma ratio reported >4; animal studies have demonstrated high concentrations of tacrolimus
in lung, kidney, heart, and spleen; distributed into breast milk. Metabolism:
Extensively in liver (CYP3A4). Elimination:
Metabolites primarily in bile. Half-Life:
Assessment & Drug Effects
- Lab tests: Monitor serum electrolytes, blood glucose, uric acid, BUN, and creatinine clearance periodically.
- Monitor kidney function closely; report elevated serum creatinine or decreased urinary output.
- Monitor for neurotoxicity, and report tremors, changes in mental status, or other signs of toxicity.
- Monitor cardiovascular status and report hypertension.
Patient & Family Education
- Learn complete dosing instructions.
- Be aware of potential adverse effects.
- Minimize exposure to natural or artificial sunlight while using the ointment.
- Notify physician of S&S of neurotoxicity.