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Indications ⬇

REMS

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

Noted primarily for PO and IV use.

CV: hypertension, peripheral edema, QT interval prolongation

Derm: pruritus, rash, alopecia, herpes simplex, hirsutism, impaired wound healing, photosensitivity, sweating

EENT: abnormal vision, amblyopia, sinusitis, tinnitus

Endo: hyperglycemia, hyperlipidemia

F and E: hyperkalemia, hypomagnesemia, hyperphosphatemia, hypocalcemia, hyponatremia, hypophosphatemia, metabolic acidosis, metabolic alkalosis

GI: ↑liver enzymes, abdominal pain, anorexia, ascites, constipation, diarrhea, dyspepsia, nausea, vomiting, cholangitis, cholestatic jaundice, dysphagia, flatulence, GI BLEEDING, GI PERFORATION, oral thrush, peritonitis

GU: nephrotoxicity, urinary tract infection, ↓fertility

Hemat: anemia, leukocytosis, leukopenia, thrombocytopenia, coagulation defects, pure red cell aplasia, thrombotic microangiopathy (including hemolytic uremic syndrome and thrombotic thrombocytopenia purpura)

Local: topicalburning, stinging

Metab: ↑appetite

MS: arthralgia, hypertonia, leg cramps, muscle spasm, myalgia, myasthenia, osteoporosis

Neuro: dizziness, headache, insomnia, paresthesia, tremor, abnormal dreams, agitation, anxiety, confusion, depression, emotional lability, hallucinations, neuropathy, POSTERIOR REVERSIBLE ENCEPHALOPATHY SYNDROME (PRES), psychoses, SEIZURES, somnolence

Resp: cough, pleural effusion, asthma, bronchitis, pharyngitis, pneumonia, pulmonary edema

Misc: generalized pain, chills, fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), INFECTION (INCLUDING ACTIVATION OF LATENT VIRAL INFECTIONS SUCH AS BK VIRUS-ASSOCIATED NEPHROPATHY), MALIGNANCY (INCLUDING LYMPHOMA AND SKIN CANCER)

Interactions ⬆ ⬇

Noted primarily for PO and IV use, but should be considered for topical use.

Availability ⬆ ⬇

(Generic available)

Route/Dosage ⬆ ⬇

Kidney Transplantation

Liver Transplantation

Heart Transplantation

Lung Transplantation

Atopic Dermatitis

US Brand Names ⬆ ⬇

tacrolimus (oral, IV): Astagraf XL, Envarsus XR, Prograf,

tacrolimus (topical): Protopic

Action ⬆ ⬇

  • Inhibit T-lymphocyte activation.
Therapeutic effects:
  • Prevention of transplanted organ rejection.
  • Improvement in signs/symptoms of atopic dermatitis.

Classifications ⬆ ⬇

Therapeutic Classification: Immunosuppressant agents

Pharmacokinetics ⬆ ⬇

Absorption: Absorption following oral administration is erratic and incomplete (bioavailability ranges 5–67%); minimal amounts absorbed following topical use.

Distribution: Widely distributed to tissues.

Protein Binding: 99%.

Metabolism/Excretion: 99% metabolized by the liver; <1% excreted unchanged in the urine.

Half-Life: Liver transplant patients: 11.7 hr; healthy volunteers: 21.2 hr.

Canadian Brand Names ⬆ ⬇

tacrolimus (oral, IV): Advagraf, Envarsus PA

Time/Action Profile ⬆ ⬇

( immunosuppression)

ROUTEONSETPEAKDURATION
POrapid1.3–3.2 hr*12 hr
PO-ERunknownunknown24 hr
IVrapidunknown8–12 hr
Topical‡unknown1–2 wkunknown

* Blood level.

‡Improvement in atopic dermatitis.

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆ ⬇

ta-KROE-li-mus

Code ⬆

NDC Code