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Sitagliptin (Januvia)

Antidiabeticprescriptionoral · inferred

Dipeptidyl peptidase-4 (DPP-4) inhibitor that prevents incretin hormone (GLP-1, GIP) degradation, enhancing glucose-dependent insulin secretion and suppressing glucagon. Weight-neutral with low hypoglycemia risk. ~87% oral bioavailability, primarily renally eliminated unchanged (79%). Dose-adjust in renal impairment. Well-tolerated first-line add-on to metformin. Does not cause the GI side effects seen with GLP-1 agonists.

Projected serum levels — 100 mg, once daily

Sitagliptin (Januvia)
Sitagliptin (Januvia) modeled serum levels, 100 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 25 50 75 100 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1
Sitagliptin (Januvia) modeled serum levels with a loading dose of 122 mg, then 100 mg once daily The first dose is larger so levels approach steady state faster. 0 25 50 75 100 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule

Maintenance schedule: 100 mg once daily (oral).

Loading schedule: 122 mg on day 1, then 100 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~1 days: peak ≈ 90.4 mg, trough ≈ 19.5 mg body load. Population-based estimate over 15 days for a 100 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Antidiabetic
Route modeled
Oral
Model confidence
inferred
Half-life
12 h
Common dose
100 mg
Suggested maximum
100 mg/day
Reference dose range
50–100 mg (single dose)
Suggested cadence
once daily
Validated against
100 mg oral — Cmax 0.95 mg/L at 2.5 h

Documented interactions

  • contraindicated
    Efavirenz (Sustiva) + Sitagliptin (Januvia) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Sitagliptin (Januvia) AUC by ~0.18x

  • contraindicated
    Rifampin + Sitagliptin (Januvia) CYP induction

    Rifampin inducer of CYP3A4 predicted to change Sitagliptin (Januvia) AUC by ~0.18x

  • danger
    Carbamazepine (Tegretol) + Sitagliptin (Januvia) CYP induction

    Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Sitagliptin (Januvia) AUC by ~0.27x

  • danger
    Clarithromycin (Biaxin) + Sitagliptin (Januvia) CYP inhibition

    Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Sitagliptin (Januvia) AUC by ~2.50x

  • danger
    Dasatinib (Sprycel) + Sitagliptin (Januvia) CYP inhibition

    Dasatinib (Sprycel) time_dependent_inhibitor of CYP3A4 predicted to change Sitagliptin (Januvia) AUC by ~2.14x

  • danger
    Diltiazem + Sitagliptin (Januvia) CYP inhibition

    Diltiazem mechanism_based of CYP3A4 predicted to change Sitagliptin (Januvia) AUC by ~2.50x

Serum checks 86 modeled interaction pairings for sitagliptin (januvia) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Efficacy and safety of sitagliptin when added to ongoing metformin therapy in patients with type 2 diabetes Charbonnel B et al. · Diabetes Care, 2006 DOI

    Pivotal RCT (701 patients) demonstrating sitagliptin 100 mg added to metformin reduced HbA1c by an additional 0.65% versus placebo, with weight neutrality and no increased hypoglycemia.

  2. Effect of sitagliptin on cardiovascular outcomes in type 2 diabetes (TECOS trial) Green JB et al. · New England Journal of Medicine, 2015 DOI

    Large CV safety trial (14,671 patients, median 3 years) confirming sitagliptin is non-inferior to placebo for MACE, with no increased heart failure risk, establishing cardiovascular safety of DPP-4 inhibitors.

2 published studies referenced in the app, each with a plain-language summary.