Generic Name

Linagliptin

Precaution

Concomitant use w/ sulphonylureas which are known to cause hypoglycemia; dose reduction of sulphonylureas may be considered. May affect ability to drive or operate machinery. Childn. Elderly >75 yr. Pregnancy & lactation. Lactation: Unknown whether distributed in breast milk; caution advised

Indication

Type 2 Diabetes Mellitus

Contra Indication

Patients with a history of a hypersensitivity reaction to linagliptin, such as urticaria, angioedema, or bronchial hyperreactivity. Type 1 DM. Treatment of diabetic ketoacidosis.

Dose

N/A

Side Effect

1-10% Nasopharyngitis (4.3%),Hyperlipidemia (2.8%; with pioglitazone),Cough (2.4%; with metformin and sulfonylurea),Hypertriglyceridemia (2.4%; with sulfonylurea),Weight gain (2.3%; with pioglitazone), Hypoglycemia 7.6% overall incidence, 22.9% incidence compared with placebo plus metformin and a sulfonylurea Incidence similar to placebo with monotherapy or combined with metformin or pioglitazone

Pregnancy Category

Mode of Action

Dipeptidyl peptidase 4 (DPP-4) inhibitor; increases and prolongs incretin hormone activity which is inactivated by DPP-4 enzyme. Incretins regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and reducing glucagon secretion from pancreatic alpha cells .

Interaction

Increased risk of hypoglycaemia when used w/ an insulin secretagogue (e.g. sulfonylurea) or insulin. Plasma concentration of linagliptin may be decreased by strong inducers of P-glycoprotein (e.g. rifampicin) and may be increased by strong P-glycoprotein inhibitors (e.g. ritonavir).

Pregnancy Category Note

Pregnancy The limited data in pregnant women are not sufficient to inform of drug-associated risk for major birth defects and miscarriage; there are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy In animal reproduction studies, no adverse developmental effects were observed when linagliptin was administered to pregnant rats during period of organogenesis at doses similar to maximum recommended clinical dose, based on exposure Poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, pre-eclampsia, and delivery complications; poorly controlled diabetes increases fetal risk for major birth defects, still birth, and macrosomia related morbidity Lactation There is no information regarding presence of linagliptin in human milk, the effects on breastfed infant, or effects on milk production; however, linagliptin is present in rat milk; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy or from underlying maternal condition

Adult Dose

Oral Type 2 diabetes mellitus Adult: 5 mg once daily. Indicated for adults with diabetes mellitus type II along with diet and exercise to lower blood sugar; may be used as monotherapy or in combination with other common antidiabetic medications including metformin, sulfonylurea, pioglitazone, or insulin. Elderly: No dose adjustment is necessary based on age. Hepatic or renal impairment: No dosage adjustment required.

Child Dose

Safety and efficacy not established

Renal Dose

Renal Impairment: No dose adjustment.

Administration

May administer with or without food