Tacrolimus

DEA Class; Rx

Common Brand Names; Prograf, Astagraf XL, Hecoria, Envarsus XR, Protopic

• Immunosuppressants; 
• Calcineurin Inhibitors

Hypersensitivity to tacrolimus or any component of the formulation, including castor oil (Prograf)

• Tremor (54%)
• Hypertension (50%)
• Hypophosphatemia (49%)
• Increased creatinine (45%)
• Infection (45%)
• Headache (44%)
• Diarrhea (44%)
• Nausea (38%)
• Peripheral edema (36%)
• Constipation (35%)
• Urinary tract infection (34%)
• Hypomagnesemia (34%)
• Asthenia (34%)
• Abdominal pain (33%)
• Pain (32%)
• Insomnia (32%)
• Hyperlipemia (31%)
• Hyperkalemia (31%)
• Anemia (30%)
• Vomiting (29%)
• Dyspepsia (28%)
• Fever (29%)
• Arthralgia (25%)
• Back pain (24%)
• Diabetes mellitus (24%)
• Paresthesia (23%)
• Hypokalemia (22%)
• Hyperglycemia (22%)
• Dyspnea (22%)
• Dizziness (19%)
• Chest Pain (19%)
• Increased cough (18%)
• Edema (18%)
• Skin rash (17%)
• Pruritus (15%)
• Leukopenia (15%)

Hypersensitivity reactions, including anaphylaxis reported with injection formulation, which contains polyoxyl 60 hydrogenated castor oil (HCO-60), a castor oil derivative; limit IV use to patients unable to take orally; monitor patient for 30 min after initiation of infusion and then at frequent intervals; discontinue infusion if anaphylaxis occurs; transition patient from IV to oral dosing as soon as patient can tolerate oral administration

Increased risk of infections and lymphoma, including latent virus activation (eg, BK virus-induced nephropathy)

Patients receiving immunosuppressants are at increased risk of developing bacterial, viral, fungal, and protozoal infections, including opportunistic infections; these infections may lead to serious, including fatal, outcomes; serious viral infections reported include, cytomegalovirus infections; CMV seronegative transplant patients who receive an organ from a CMV seropositive donor are at higher risk of developing CMV viremia and CMV disease; monitor for the development of infection and adjust the immunosuppressive regimen to balance the risk of rejection with the risk of infection (see Black Box Warnings)

Medication errors (eg, substitution and dispensing errors, between tacrolimus immediate-release products and tacrolimus extended-release products) reported outside the U.S; which led to serious adverse reactions such as graft rejection, or other adverse reactions due to under-or over-exposure to tacrolimus; not interchangeable or substitutable for tacrolimus extended-release tablets, tacrolimus immediate-release capsules or tacrolimus for oral suspension; changes between tacrolimus immediate-release and extended-release dosage forms must occur under physician supervision

Hypertension may occur; may treat with antihypertensives that are non-potassium-sparing diuretics; concurrent use of calcium channel blockers may require tacrolimus dosage adjustment

There is a pregnancy registry that monitors pregnancy outcomes in women exposed to drug during pregnancy

Controlled lactation studies have not been conducted in humans; however tacrolimus has been reported to be present in human milk

Maximum dosage for systemic formulations is dependent on indication, route of therapy, and tacrolimus serum concentrations; 2 applications/day topically.

Maximum dosage for systemic formulations is dependent on indication, route of therapy, and tacrolimus serum concentrations; 2 applications/day topically.

Maximum dosage for systemic formulations is dependent on indication, route of therapy, and tacrolimus serum concentrations; 2 applications/day topically.

Maximum dosage for systemic formulations is dependent on indication, route of therapy, and tacrolimus serum concentrations; 2 applications/day topically.

capsule, immediate-release (Prograf, Hecoria)

• 0.5mg
• 1mg
• 5mg

capsule, extended-release (Astagraf XL)

• 0.5mg
• 1mg
• 5mg

tablet, extended-release (Envarsus XR)

• 0.75mg
• 1mg
• 4mg

injectable solution (Prograf)

• 5mg/mL

granules for oral suspension (Prograf)

• 0.2mg/packet
• 1mg/packet

ointment

• 0.03%
• 0.1%