Liraglutide
Mechanism :
Analogue of human glucangon-like peptide 1 (GLP-1) which is a type of incretin - hormones released after eating that play a role in decreasing the blood glucose. Thus, Liraglutide acts by increasing insulin secretion after a meal, delaying gastric emptying to decrease postprandial glucose and also decreases glucagon secretion. GLP-1 is an important receptor in glucose homeostasis. Liraglutide bind and activates GLP-1 that increases insulin secreation in patients with type 2 Diabetes from pancreatic beta cells in presence of high levels of glucose
Indication :
- Type 2 Diabetes Mellitus: As an adjunctive theraoy after lifestyle modification in patients above 10 years age.
- Obesity: As an adjunctive therapy after lifestyle modifcation in patients above 12 years age
- For reduction of cardiovascular mortality in patients with cardiovasaulate disease
Contraindications :
• Hypersensitivity to the drug or its components
• Personal or family history of medullary thyroid carcinoma
• Multiple Endocrine Neoplasia syndrome type 2
• Pancreatitis
• Hypoglycemia
• Renal failure
• Gallbladder disease
Dosing :
Available as multidose pen for subcutaneous administration of 18 mg/3mL solution.
Which delivers doses of 0.6 mg, 1.2 mg or 1.8 mg.
Type 2 DM (Victoza)
In patients >10 years old as an add-on drug to improve glycaemic control.
0.6 mg SC per day which may increased to 1.2 mg SC per day after 1 week, which may then be further increased to 1.8 mg SC per day after 1 week if glycaemic control not achieved.
Obesity (Saxenda)
In patients >12 years as an adjunctive therapy after lifestyle modification for chronic weight management.
0.6 mg SC per day for 1 week, increased by 0.6 mg/day weekly till maintenance dose of 3 mg/day achieved .
Assess change in BMI after 12 weeks of maintenance therapy.
Adverse Effect :
• Nausea, vomiting, diarrhea
• Hypoglycaemia
• Headache
• Injection site reactions
• Dizziness
• Dyspepsia
• Decrease in appetite
• Gastroesophageal reflux disease
• Urinary tract infection
• Abdominal pain
• Insomnia
• Dryness of mouth
• Anxiety
Interaction :
• Liraglutide may cause delayed gastric emptying and thus can alter the absorption of co-administered drugs.
• Risk of hypoglycaemia with concomitant use of antidiabetic drugs such as sulfonylureas and insulin
• Contraindicated:
o Cidofovir: Concomitant use may increase cidofovir levels thus increasing risk of myelosuppresion, nephrotoxicity and other adverse effects. Liraglutide should be discontinued a week before starting Cidofovir
• Caution advised, hence avoid:
o Amikacin, Gentamicin, Streptomycin: May increase amikacin levels, risk of ototoxicity
o Bumetanide: May decrease efficacy of Liraglutide
o Clofarbine: May increase levels of clofarbine, risk of myelosuppression
o Foscarnet: May increase levels of Foscarnet, risk of myelosuppression
o Ganciclovir, Valganciclovir: May increase levels and hence risk of myelosuppresion
o Mannitol: May increase mannitol levels, risk of nephrotoxicity, neurotoxicity
o Pentamidine: Increased risk of hyperglycaeimia or severe hypoglycaemia
o Tenofovir: May increase tenofovir levels, risk of nephrotoxicity
o Polymyxin B: Increased risk of nephrotoxicity
Lactation :
Hepatic Dose :
Caution advised, no specific guidelines available