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Linagliptin

Dipeptidyl peptidase-4 (DPP-4) inhibitor (gliptin) · Antidiabetic

Also known as Trajenta

START
5 mg PO once daily (no titration; no renal/hepatic adjustment)
TYPICAL MAX
5 mg/day (fixed)
STOP IF
Acute pancreatitis, severe hypersensitivity (angioedema/SJS), bullous pemphigoid, disabling arthralgia
WATCH
Pancreatitis symptoms, severe joint pain, skin (pemphigoid), HbA1c; hypoglycaemia if with sulfonylurea/insulin
CDSCO approvedSchedule HATC A10BH05
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo dose adjustment at any eGFR (non-renal elimination)90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1hONSET1.5hPEAK12h1dDURATION
ONSET
1h · DPP-4 inhibition
PEAK
1.5h · Cmax
12h · effective t½
DURATION
1d · once-daily
EXCRETION
~80% biliary/faecal; <5% renal
route + CYP
INTERACTIONS
3 major
SEVERE in our sources
PREGNANCY
Avoid — limited data; insulin preferred in pregnancy
FDA category + note
Top interactionssee all 7
  • BexaroteneSevereDatabaseDDInter
  • GatifloxacinSevereDatabaseDDInter
  • SulfonylureasSevereDatabaseKimi deep-research + Cla
Available in India

15 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Inhibits DPP-4, prolonging endogenous incretins (GLP-1, GIP) → glucose-dependent insulin secretion and reduced glucagon; weight-neutral, low intrinsic hypoglycaemia risk; uniquely non-renally eliminated.

Indications

Type 2 diabetes mellitus (monotherapy or add-on to metformin, sulfonylurea, insulin, etc.)

Dosing

Adult
5 mg PO once daily (with or without food).
Pediatric
Not established.
Renal adjustment
No dose adjustment at any level of renal impairment (primarily biliary/enterohepatic elimination).
Hepatic adjustment
No dose adjustment (limited severe-impairment data).
Geriatric
No specific adjustment.
Max dose
5 mg/day (fixed)

Pharmacokinetics

Onset
DPP-4 inhibition within ~1 h; glycaemic effect over weeks
Peak effect
Cmax ~1.5 h
Duration
~24 h (long DPP-4 occupancy)
Half-life
Effective ~12 h (terminal long due to target binding)
Bioavailability
~30%
Protein binding
Concentration-dependent (high, saturable)
Metabolism
Minimal (mostly unchanged)
Excretion
Predominantly biliary/faecal (~80%); <5% renal

Contraindications

  • Type 1 diabetes / diabetic ketoacidosis
  • History of serious hypersensitivity to linagliptin (angioedema, anaphylaxis, SJS)

Side effects

Common
NasopharyngitisHypoglycaemia (with sulfonylurea/insulin)HeadacheArthralgia (class)
Serious
  • Acute pancreatitis
  • Severe hypersensitivity (angioedema, anaphylaxis, SJS)
  • Severe disabling arthralgia (DPP-4 class)
  • Bullous pemphigoid
  • Possible heart-failure hospitalisation signal (class — agent-variable)

Pregnancy & lactation

Pregnancy

Avoid — limited data; insulin preferred in pregnancy

Lactation

Avoid (excreted in animal milk)

Drug interactions

Bexarotene
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Gatifloxacin
Severe
Database

Clinical effect not specified

Source: DDInter

Sulfonylureas
Severe
Database

Additive hypoglycaemia

Reduce sulfonylurea/insulin dose; monitor glucose

Source: Kimi deep-research + Cla

Ace Inhibitors
Moderate
Database

Possible additive angioedema risk (DPP-4 class)

Monitor for angioedema

Source: Kimi deep-research + Cla

Glp 1 Receptor Agonists
Moderate
Database

Overlapping incretin mechanism — no added benefit, possible GI/pancreatitis additive

Avoid combining DPP-4 inhibitor with GLP-1 agonist

Source: Kimi deep-research + Cla

Rifampicin
Moderate
Database

Reduced glucose-lowering efficacy

Monitor glucose. Consider alternative DPP-4i.

Source: DDInter

Strong Cyp3a4 + P Gp Inducers
Moderate
Database

Reduced linagliptin exposure → loss of efficacy

Consider alternative agent if chronic rifampicin

Source: Kimi deep-research + Cla

5 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.

Related guidelines

Other Dipeptidyl peptidase-4 (DPP-4) inhibitor (gliptin) drugs

Ask House about Linagliptin

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19