DIQTA 1.0: Drug-Induced QT Prolongation Atlas

TACROLIMUS

DIR Classification Postmarketing Surveillance Drug Property Information Reference

DIR Classification

Classification:Most-DIQT concern

Severity Score:4.0

Description in Drug Labeling: View Full Labeling: SPL in DailyMed | PDF

WARNINGS AND PRECAUTIONS
QT Prolongation
Tacrolimus may prolong the QT/QTc interval and may cause Torsade de Pointes. Avoid tacrolimus in patients with congenital long QT syndrome. In patients with congestive heart failure, bradyarrhythmias, those taking certain antiarrhythmic medications or other medicinal products that lead to QT prolongation, and those with electrolyte disturbances such as hypokalemia, hypocalcemia, or hypomagnesemia, consider obtaining electrocardiograms and monitoring electrolytes (magnesium, potassium, calcium) periodically during treatment.
When co-administering tacrolimus with other substrates and/or inhibitors of CYP3A4 that also have the potential to prolong the QT interval, a reduction in tacrolimus dose, frequent monitoring of tacrolimus whole blood concentrations, and monitoring for QT prolongation is recommended. Use of tacrolimus with amiodarone has been reported to result in increased tacrolimus whole blood concentrations with or without concurrent QT prolongation [see Drug Interactions (7)].
DRUG INTERACTIONS
Effects of Other Drugs on Tacrolimus
ADVERSE REACTIONS
Postmarketing Adverse Reactions
The following adverse reactions have been reported from worldwide marketing experience with tacrolimus. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Decisions to include these reactions in labeling are typically based on one or more of the following factors: (1) seriousness of the reaction, (2) frequency of the reporting, or (3) strength of causal connection to the drug.
Cardiovascular: Atrial fibrillation, atrial flutter, cardiac arrhythmia, cardiac arrest, electrocardiogram T wave abnormal, flushing, myocardial infarction, myocardial ischemia, pericardial effusion, QT prolongation, Torsade de Pointes, venous thrombosis deep limb, ventricular extrasystoles, ventricular fibrillation, myocardial hypertrophy [see Warnings and Precautions (5.13)].
PATIENT PACKAGE INSERT
Tacrolimus capsules may cause serious side effects, including:
changes in the electrical activity of your heart (QT prolongation).

Postmarketing Surveillance

Contingency Table:

Current Drug

Other Drugs

QT Prolongation

24042

Other ADRs

135842

38245745

Odds Ratio = 0.586

Drug Property Information

ATC Code(s):

L04AD02 - tacrolimus

L04AD - Calcineurin inhibitors
L04A - IMMUNOSUPPRESSANTS
L04 - IMMUNOSUPPRESSANTS
L - ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

D11AH01 - tacrolimus

D11AH -
D11A - OTHER DERMATOLOGICAL PREPARATIONS
D11 - OTHER DERMATOLOGICAL PREPARATIONS
D - DERMATOLOGICALS

Active Ingredient:TACROLIMUS

Active Ingredient UNII:WM0HAQ4WNM

Drugbank ID:DB00864

PubChem Compound:445643

CTD ID:D016559

PharmGKB:PA451578

CAS Number:104987-11-3

Dosage Form(s):capsule

Route(s) Of Administrator:oral

Daily Dose:

5.0 mg/day L04AD02

Chemical Structure:

SMILE Code:
CO[C@@H]1C[C@@H](CC[C@H]1O)\C=C(/C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@H](C[C@@H](C)C\C(C)=C\[C@@H](CC=C)C(=O)C[C@H](O)[C@H]1C)OC

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