Drug reference

Tacrolimus

Immunosuppressant

Also known as ADOPORT, ENVARSUS MODIFIED-RELEASE TABLETS

Immunosuppressant

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

Manufacturer advises use only if potential

FDA category + note

Top interactionssee all 12 →

Live VaccinesContraindicatedDatabase
AcyclovirSevereDatabaseDDInter
AdalimumabSevereDatabaseDDInter
AmikacinSevereDatabaseDDInter

Mechanism

Tacrolimus is a calcineurin inhibitor. Although not chemically related to ciclosporin, it has a similar mode of action.

Indications

Prophylaxis of graft rejection following liver transplantationtransplant rejection prophylaxistransplant rejection rescue therapysevere, acute, steroid-resistant IBDrefractory Crohn’s disease

Pharmacokinetics

Bioavailability

25 ± 10%

Protein binding

75–99%

Metabolism

CYP3A

Excretion

<1%

Side effects

Common

nephrotoxicityneurotoxicitygi complaintshypertensionglucose intolerancediabetes mellitus

Serious

Neurotoxicity
Cardiomyopathy
Disturbance of glucose metabolism

Pregnancy & lactation

Pregnancy

Manufacturer advises use only if potential

Drug interactions

Live Vaccines

Contraindicated

Database

Risk of disseminated infection from the live vaccine due to immunosuppression.

Live vaccines are contraindicated in patients receiving tacrolimus. Inactivated vaccines should be considered, but the immune response may be attenuated.

Acyclovir

Severe

Database

Drug interaction classified as: synergy.

Source: DDInter

Adalimumab

Severe

Database

Drug interaction classified as: synergy.

Source: DDInter

Amikacin

Severe

Database

Increased risk of acute kidney injury and elevated tacrolimus levels due to impaired renal clearance.

Avoid concomitant use. If unavoidable, monitor renal function and tacrolimus trough levels very closely. Adjust tacrolimus dose as needed. Consider alternative antibiotics.

Source: DDInter

Amiloride

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Amiodarone

Severe

Database

Increased tacrolimus blood concentrations, leading to increased risk of nephrotoxicity and neurotoxicity.

Monitor tacrolimus trough levels closely and adjust tacrolimus dose as needed. Consider a dose reduction of tacrolimus.

Source: DDInter