alogliptin, Nesina

 Indications

Adjunct to diet and exercise to improve glycemic control

in type 2 diabetes mellitus.

Action

Acts as a competitive inhibitor of dipeptidyl peptidase-4

(DPP-4) which slows the inactivation of incretin hormones,

thereby increasing their concentrations and reducing

fasting and postprandial glucose concentrations.

Therapeutic Effects: Improved control of

blood glucose.

Pharmacokinetics

Absorption: Completely absorbed following oral administration

(100%).

Distribution: Well distributed into tissues.

Metabolism and Excretion: Not extensively metabolized,

76% excreted unchanged in urine.

Half-life: 21 hr.

TIME/ACTION PROFILE (inhibition of DPP-4)

ROUTE ONSET PEAK† DURATION

PO unknown 1–2 hr 24 hr

†Multiple dosing.

Contraindications/Precautions

Contraindicated in: Type 1 diabetes; Diabetic ketoacidosis;

Previous severe hypersensitivity reactions.

Use Cautiously in: Hepatic impairment; Renal impairment

(doseprequired if CCr 60 mL/min); HF or

renal impairment (qrisk for worsening HF); Geri: May

haveqsensitivity to effects; Lactation: Use cautiously;

OB: Use during pregnancy only if clearly needed; Pedi:

Safety and effectiveness not established.

Adverse Reactions/Side Effects

CNS: headache. CV: HF. Derm: STEVENS-JOHNSON

SYNDROME, bullous pemphigoid. GI: HEPATOTOXICITY,

PANCREATITIS,qliver enzymes. MS: arthralgia. Misc:

HYPERSENSITIVITY REACTIONS (including anaphylaxis or

angioedema).

Interactions

Drug-Drug:qrisk of hypoglycemia with sulfonylureas

and insulin; dose adjustments may be necessary.

Route/Dosage A

PO (Adults): 25 mg once daily.

Renal Impairment

PO (Adults): CCr 30–59 mL/min—12.5 mg once

daily; CCr 15–29 mL/min—6.25 mg once daily; CCr

15 mL/min or requiring hemodialysis—6.25 mg

once daily.

Availability

Tablets: 6.25 mg, 12.5 mg, 25 mg. In combination

with: metformin (Kazano), pioglitazone (Oseni).