DRUG INFORMATION QUERY -6

LINAGLIPITIN:
Adult Dosing
Type 2 diabetes mellitus
 5 mg orally once daily with or without food
Pediatric Dosing
General Dosage Information
 Safety and effectiveness have not been established in pediatric
patients.
Dose Adjustments
 Renal impairment: No adjustment is necessary.
 Hepatic impairment: No adjustment is necessary.
 Geriatrics: No adjustment is necessary.
 Concomitant use with insulin or insulin secretagogue (eg,
sulfonylurea): Dose reduction of insulin or insulin secretagogue
may be required.
Indications
FDA-Labeled Indications
Type 2 diabetes mellitus
Contraindications
History of hypersensitivity to linagliptin, or any component of the
product (eg, anaphylaxis, angioedema, exfoliative skin conditions,
urticaria, or bronchial hyperreactivity)
Precautions
 Angioedema: History of angioedema to another dipeptidyl
peptidase-4 (DPP-4) inhibitor; use with caution
  Cardiovascular: Heart failure may occur; monitoring
recommended and consider discontinuation
 Dermatologic: Bullous pemphigoid, requiring hospitalization,
has been reported; discontinue use if suspected and treatment
may be necessary
 Endocrine and metabolic: Concomitant use of insulin or an
insulin secretagogue (eg, sulfonylurea) may increase the risk of
hypoglycemia, especially with combined insulin therapy in
patients with severe renal impairment; dose adjustment of
insulin or insulin secretagogue may be required.
 Gastrointestinal: Acute pancreatitis, including fatalities, has
been reported; monitoring recommended and if suspected,
immediately discontinue use
 Immunologic: Serious hypersensitivity reactions have been
reported, including anaphylaxis, angioedema, and exfoliative
skin conditions; discontinue use if suspected, and use with
caution in patients with history of angioedema to another
dipeptidyl peptidase-4 inhibitor.
 Musculoskeletal: Severe and persistent joint pain has been
reported with dipeptidyl peptidase-4 (DPP-4) inhibitors with
onset occurring from 1 day to years after initiation; may require
discontinuation, and symptoms may reoccur when rechallenged
with same drug or with another DPP-4 inhibitor
Pregnancy Category
Fetal risk cannot be ruled out. (MDX)
Breast Feeding
Micromedex: Infant risk cannot be ruled out
ADVERSE EFFECTS
Common
Endocrine metabolic: Hypoglycemia (Monotherapy, up to 14.6%;
combination therapy, up to 19.8%)
Gastrointestinal: Diarrhea (Monotherapy; up to 7%; combination
therapy, 2.2% to 6.6%)
Respiratory: Cough (2.1% to 6.1%), Nasopharyngitis (Monotherapy,
5.9% to 31.6%; combination therapy, 3% to 8.4%)
Serious
Cardiovascular: Heart failure
Dermatologic: Bullous pemphigoid (0.2%)
Gastrointestinal: Pancreatitis (Monotherapy, Less than 1%;
combination therapy, 0.3% to 0.7%)
Immunologic: Anaphylaxis, Hypersensitivity reaction (Up to 2.4%)
Musculoskeletal :Arthralgia (Monotherapy, 2% to 8%; combination
therapy, 0% to 8.1%)
Other: Angioedema
PHARMACOKINETICS
Absorption
Tmax: 1.5 hours
Bioavailability, oral: 30%
Effect of food: not clinically relevant
Distribution
Vd: 1110 L
Protein binding: 70% to 99%
Metabolism
limited
Excretion
Renal clearance: 70 mL/min
Renal excretion: 5% to less than 7%
Bile: 80%
Extracorporeal: no (hemodialysis), no (peritoneal dialysis)
Elimination Half Life
greater than 100 hours