Tacrolimus oral and injection

Tacrolimus lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats the new organ as an invader.

Tacrolimus is used together with other medicines to prevent your body from rejecting a heart, liver, or kidney transplant.

The Astragraf XL and Envarsus XR brands of tacrolimus is generally not used for liver transplants.

Tacrolimus may also be used for purposes not listed in this medication guide.

Tacrolimus may increase your risk of developing serious infection, lymphoma, or other cancers. Talk with your doctor about the risks and benefits of using this medicine.

Call your doctor right away if you have any signs of infection, such as fever, chills, body aches, skin warmth or redness, or flu symptoms.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Applies to tacrolimus: intravenous solution, oral capsule, oral capsule extended release, oral tablet extended release

General

Some of the most commonly reported side effects include hypertension, diarrhea, hyperglycemia, anemia, headache, tremor, insomnia, pain, and asthenia.[Ref]

Cardiovascular

Very common (10% or more): Hypertension (up to 89%), peripheral edema (up to 36%), chest pain (up to 19%), pericardial effusion (up to 15%)
Frequency not reported: Angina pectoris, bradycardia, cardiac fibrillation, cardiomyopathy, cardiopulmonary failure, deep thrombophlebitis, ECG abnormalities, echocardiogram abnormalities, heart rate decreased, hemorrhage, hypotension, myocardial hypertrophy, peripheral vascular disorder, phlebitis, QT prolongation, tachycardia, thrombosis, Torsade de Pointes, vasodilation[Ref]

Gastrointestinal

Very common (10% or more): Diarrhea (up to 72%), nausea (up to 46%), constipation (up to 36%), vomiting (up to 29%), dyspepsia (up to 28%)
Frequency not reported: Abdomen enlarged, duodenitis, dysphagia, esophagitis, flatulence, gastritis, gastroesophagitis, gastrointestinal (GI) hemorrhage, GI perforation, ileus, oral moniliasis, pancreatic pseudocyst, peritonitis, rectal disorder, stomatitis, ulcerative esophagitis[Ref]

Metabolic

Very common (10% or more): Hyperglycemia (up to 70%), hypophosphatemia (up to 49%), hypomagnesemia (up to 48%), hyperkalemia (up to 45%), anorexia (up to 34%), hyperlipidemia (up to 34%), hypokalemia (up to 29%)
Frequency not reported: Abnormal healing, acidosis, alkalosis, appetite increased, bicarbonate decreased, dehydration, gout, hypercalcemia, hypercholesterolemia, hyperphosphatemia, hyperuricemia, hypervolemia, hypocalcemia, hypoglycemia, hyponatremia, hypoproteinemia, lactic dehydrogenase increased, weight gain[Ref]

Hematologic

Very common (10% or more): Anemia (up to 65%), leukopenia (up to 48%), leukocytosis (up to 32%), thrombocytopenia (24%)
Frequency not reported: Coagulation disorder, ecchymosis, hematocrit increased, hemoglobin abnormal, hypochromic anemia, polycythemia, prothrombin decreased, serum iron decreased
Postmarketing reports: Agranulocytosis, disseminated intravascular coagulation, hemolytic anemia, hemolytic-uremic syndrome, neutropenia, pancytopenia, pure red cell aplasia, thrombocytopenic purpura, thrombotic thrombocytopenic purpura[Ref]

Nervous system

Very common (10% or more): Headache (up to 64%), tremor (up to 56%), paresthesia (up to 40%), dizziness (up to 19%), fatigue (up to 16%)
Frequency not reported: Amnesia, aphasia, convulsion, encephalopathy, hemorrhagic stroke, hypertonia, incoordination, monoparesis, myoclonus, nerve compression, nervousness, neuralgia, neuropathy, paralysis flaccid, psychomotor skills impaired, quadriparesis, seizures, somnolence, vertigo, writing impaired
Postmarketing reports: Coma, dysarthria, posterior reversible encephalopathy syndrome (PRES), progressive multifocal leukoencephalopathy (PML)[Ref]

Psychiatric

Very common (10% or more): Insomnia (up to 64%)
Frequency not reported: Abnormal dreams, agitation, anxiety, confusion, crying, depression, emotional lability, hallucinations, mental status changes, mood elevated, nightmares, psychosis, thinking abnormal
Postmarketing reports: Mutism[Ref]

Other

Very common (10% or more): Pain (up to 63%), asthenia (up to 54%), fever (up to 48%)
Frequency not reported: Abscess, accidental injury, chills, ear pain, fall, feeling abnormal, generalized edema, hernia, otitis media, sepsis, temperature intolerance, tinnitus, ulcer[Ref]

Renal

Very common (10% or more): Serum creatinine increased (up to 45%), BUN increased (up to 30%)
Frequency not reported: BK nephropathy, hydronephrosis, renal failure, toxic nephropathy, tubular necrosis[Ref]

Respiratory

Very common (10% or more): Pleural effusion (up to 36%), dyspnea (up to 29%), atelectasis (up to 28%), cough increased (18%), bronchitis (17%)
Frequency not reported: Asthma, emphysema, hiccups, lung disorder, pharyngitis, pneumonia, pneumothorax, pulmonary edema, rhinitis, sinusitis, voice changes
Postmarketing reports: Interstitial lung disease[Ref]

Hepatic

Very common (10% or more): Liver function tests abnormal (up to 36%)
Frequency not reported: Cholangitis, cholestatic jaundice, GGT increased, granulomatous hepatitis, hepatitis, jaundice[Ref]

Dermatologic

Very common (10% or more): Pruritus (up to 36%), rash (up to 24%)
Frequency not reported: Alopecia, cellulitis, hirsutism, photosensitivity, sweating[Ref]

Genitourinary

Very common (10% or more): Urinary tract infection (up to 34%), oliguria (up to 19%)
Frequency not reported: Albuminuria, bladder spasm, cystitis, dysuria, hematuria, nocturia, pyuria, urge incontinence, urinary frequency, urinary incontinence, urinary retention, vaginitis[Ref]

Immunologic

Very common (10% or more): Cytomegalovirus infection (up to 12%)
Frequency not reported: Flu syndrome[Ref]

Oncologic

Postmarketing reports: Epstein-Barr virus associated lymphoproliferative disorder, hepatosplenic T-cell lymphoma, leukemia, lymphoma, melanoma, post-transplant lymphoproliferative disorder (PTLD)[Ref]

Musculoskeletal

Frequency not reported: Arthralgia, generalized spasm, joint disorder, leg cramps, mobility decreased, myasthenia, myalgia, osteoporosis
Postmarketing reports: Rhabdomyolysis[Ref]

Hypersensitivity

Frequency not reported: Allergic reaction[Ref]

Ocular

Frequency not reported: Abnormal vision, amblyopia[Ref]

Some side effects of tacrolimus may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

LIVER TRANSPLANT:
IMMEDIATE RELEASE:
-Initial dose: 0.075 to 0.1 mg/kg orally every 12 hours

Comments:
-Should be taken consistently either with or without food because the presence and composition of food decreases the bioavailability.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or mycophenolate mofetil (MMF)

INTRAVENOUS:
-Initial dose: 0.03 to 0.05 mg/kg/day as a continuous IV infusion

Comments:
-Pediatric patients without pre-existing renal or hepatic dysfunction have required and tolerated higher doses than adults to achieve similar blood concentrations.
-IV administration should be reserved only for initiation in patients unable to take oral therapy.
-Convert to oral therapy as soon as it can be tolerated, usually within 2 to 3 days.

Use: Prophylaxis of organ rejection in patients receiving allogeneic liver, kidney or heart transplants; use concomitantly with adrenal corticosteroids; in kidney and heart transplant, use in conjunction with azathioprine or MMF

Severe liver impairment (Child-Pugh 10 or greater): May require lower doses

LIVER TRANSPLANT:
Patients experiencing post-transplant hepatic impairment may be associated with an increased risk of developing renal insufficiency related to high blood levels of this drug. Monitor closely and consider dose adjustments.

Data not available