Company: Novo Nordisk
Pharmacologic class: Antidiabetic (glucagon-like peptide-1 [GLP-1] receptor agonist)
Active ingredient: Liraglutide (rDNA origin) 6 mg/mL; solution for subcutaneous injection
Indication: As adjunct to diet and exercise, to improve glycemic control in type 2 diabetes
Pharmacology: Liraglutide is an analogue of human GLP-1 that acts as an agonist at GLP-1 receptors. Its properties differ from those of the native protein in that it has a longer half-life, enabling it to be dosed once daily. Its actions include increasing intracellular cyclic adeno-sine monophosphate, resulting in insulin release in the presence of increased glucose concentrations. This insulin secretion subsides as glucose levels normalize. Liraglutide also decreases glucagon secretion and delays gastric emptying, both of which contribute to its therapeutic effect. It has been shown to reduce fasting, premeal, and postprandial glucose throughout the day.
Clinical trials: Five double-blind, randomized, controlled clinical trials were conducted to assess the efficacy of liraglutide in the management of type 2 diabetes. In a 52-week monotherapy trial, 746 patients were randomized to liraglutide 1.2 mg or 1.8 mg or glimepiride 8 mg. Treatment with liraglutide resulted in significant reductions in hemoglobin (Hb) A1c compared with glimepiride.
A 26-week study involving 1,091 patients compared three doses of liraglutide (0.6 mg, 1.2 mg, and 1.8 mg), glimepiride 4 mg, and placebo as add-on therapy to metformin. The addition of liraglutide 1.2 mg and 1.8 mg resulted in a significant mean HbA1c reduction compared with placebo and a similar mean HbA1c reduction compared to glimepiride.
In a 26-week study in 1,041 patients that compared three doses of liraglutide (0.6 mg, 1.2 mg, and 1.8 mg), rosiglitazone 4 mg, and placebo as add-on therapy to glimepiride, treatment with liraglutide 1.2 mg and 1.8 mg resulted in a significant reduction in mean HbA1c compared with placebo as add-on to glimepiride.
A 26-week study in 581 patients compared liraglutide 1.8 mg, placebo, and insulin glargine as add-on therapy with metformin and glimepiride. Treatment with liraglutide as add-on to metformin and glimepiride resulted in significant mean reduction in HbA1c compared with placebo add-on to metformin and glimepiride.
Lastly, a 26-week trial compared liraglutide 1.2 mg, liraglutide 1.8 mg, and placebo as add-on therapy to metformin 2 g and rosiglitazone 8 mg. Treatment with liraglutide as add-on to metformin plus rosiglitazone resulted in a significant reduction in mean HbA1c compared with placebo.
Adults: Give by subcutaneous injection in abdomen, thigh, or upper arm once daily. Initially 0.6 mg/day for one week, then 1.2 mg/day; may increase to 1.8 mg/day.
Children: <18yrs: not recommended.
Contraindications: History (personal or family) of medullary thyroid carcinoma. Multiple endocrine neoplasia syndrome type 2.
Precautions: Not for treating type 1 diabetes or ketoacidosis. Not recommended for first-line treatment in patients inadequately controlled on diet and exercise. Pancreatitis; monitor for signs/symptoms. Renal or hepatic dysfunction. Gastroparesis. Inform patients of thyroid cancer risk and symptoms. Pregnancy (Cat. C). Nursing mothers: not recommended.
Interactions: Concomitant insulin (insufficient data). Hypoglycemia with insulin secretagogues (consider reducing their doses). May affect absorption of other drugs (delayed gastric emptying). Monitor digoxin.
Adverse reactions: Headache, GI upset, antibody formation, immunogenicity reactions (e.g., urticaria), constipation, anorexia; rare: pancreatitis (discontinue if occurs), papillary thyroid carcinoma.
How supplied: Multi-dose, prefilled pen (3mL)—2, 3
For more information, call 877.484.2869 or visit www.Victoza.com.