DIQTA 1.0: Drug-Induced QT Prolongation Atlas

SITAGLIPTIN

DIR Classification Postmarketing Surveillance Drug Property Information Reference

DIR Classification

Classification:Ambiguous

Severity Score:1.0

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

ADVERSE REACTIONS
Clinical Trials Experience
No clinically meaningful changes in vital signs or in ECG (including in QTc interval) were observed in patients treated with JANUVIA.
CLINICAL PHARMACOLOGY
Pharmacodynamics
Cardiac Electrophysiology
In a randomized, placebo-controlled crossover study, 79 healthy subjects were administered a single oral dose of sitagliptin 100 mg, sitagliptin 800 mg (8 times the recommended dose), and placebo. At the recommended dose of 100 mg, there was no effect on the QTc interval obtained at the peak plasma concentration, or at any other time during the study. Following the 800 mg dose, the maximum increase in the placebo-corrected mean change in QTc from baseline was observed at 3 hours postdose and was 8.0 msec. This increase is not considered to be clinically significant. At the 800 mg dose, peak sitagliptin plasma concentrations were approximately 11 times higher than the peak concentrations following a 100-mg dose.
In patients with type 2 diabetes mellitus administered sitagliptin 100 mg (N=81) or sitagliptin 200 mg (N=63) daily, there were no meaningful changes in QTc interval based on ECG data obtained at the time of expected peak plasma concentration.

Postmarketing Surveillance

Contingency Table:

Current Drug

Other Drugs

QT Prolongation

24076

Other ADRs

71411

38310176

Odds Ratio = 0.357

Drug Property Information

ATC Code(s):

A10BH01 - sitagliptin

A10BH0 -
A10BH - Dipeptidyl peptidase 4 (DPP-4) inhibitors
A10B - "BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS"
A10 - DRUGS USED IN DIABETES
A - ALIMENTARY TRACT AND METABOLISM

A10BD07 - sitagliptin

A10BD0 -
A10BD - Combinations of oral blood glucose lowering drugs
A10B - "BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS"
A10 - DRUGS USED IN DIABETES
A - ALIMENTARY TRACT AND METABOLISM

A10BD12 - sitagliptin

A10BD - Combinations of oral blood glucose lowering drugs
A10B - "BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS"
A10 - DRUGS USED IN DIABETES
A - ALIMENTARY TRACT AND METABOLISM

A10BD24 - sitagliptin

A10BD - Combinations of oral blood glucose lowering drugs
A10B - "BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS"
A10 - DRUGS USED IN DIABETES
A - ALIMENTARY TRACT AND METABOLISM

A10BH51 - sitagliptin

A10BH - Dipeptidyl peptidase 4 (DPP-4) inhibitors
A10B - "BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS"
A10 - DRUGS USED IN DIABETES
A - ALIMENTARY TRACT AND METABOLISM

Active Ingredient:SITAGLIPTIN PHOSPHATE

Active Ingredient UNII:TS63EW8X6F

Drugbank ID:DB01261

PubChem Compound:4369359

CTD ID:

PharmGKB:PA164748978

CAS Number:486460-32-6

Dosage Form(s):tablet, film coated

Route(s) Of Administrator:oral

Daily Dose:

100.0 mg/day A10BH01

Chemical Structure:

SMILE Code:
N[C@@H](CC(=O)N1CCN2C(C1)=NN=C2C(F)(F)F)CC1=CC(F)=C(F)C=C1F

Reference

N/A