Liraglutide

Indications

Liraglutide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus, to reduce the risk of major adverse cardiovascular events (cardiovascular death, non-fatal myocardial infarction, or non-fatal stroke) in adults with type 2 diabetes mellitus and established cardiovascular disease.

Pharmacology

Liraglutide is an acylated analog of human glucagon-like peptide 1 (GLP-1), an endogenous incretin hormone and acts as a GLP-1 receptor agonist. Activation of GLP-1 receptor stimulates insulin secretion and suppression of glucagon secretion in a glucose-dependent manner. It also delays gastric emptying thus reduces the rate of postprandial glucose present in the circulation. It has lowering effects of fasting, premeal and postprandial glucose; with a decrease in HbA1c by approx 1%.

Dosage And Administration

Inject Liraglutide subcutaneously once-daily at any time of day, independently of meals. Initiate Liraglutide with a dose of 0.6 mg per day for one week. The 0.6 mg dose is a starting dose intended to reduce gastrointestinal symptoms during initial titration, and is not effective for glycemic control. After one week at 0.6 mg per day, the dose should be increased to 1.2 mg. If the 1.2 mg dose does not result in acceptable glycemic control, the dose can be increased to 1.8 mg. If a dose is missed, resume the once-daily regimen as prescribed with the next scheduled dose. Do not administer an extra dose or increase in dose to make up for the missed dose.

If more than 3 days have elapsed since the last Liraglutide dose, reinitiate Liraglutide at 0.6 mg to mitigate any gastrointestinal symptoms associated with reinitiation of treatment. Upon reinitiation, Liraglutide should be titrated at the discretion of the prescriber.

 

Administration

  • Inspect visually prior to each injection. Only use if solution is clear, colorless, and contains no particles.
  • Inject Liraglutide subcutaneously in the abdomen, thigh or upper arm. No dose adjustment is needed if changing the injection site and/or timing.
  • When using Liraglutide with insulin, administer as separate injections. Never mix.
  • It is acceptable to inject Liraglutide and insulin in the same body region but the injections should not be adjacent to each other.

Interaction

Increased risk of hypoglycaemia when used w/ insulin secretagogues (e.g. sulfonylurea, meglitinide). May affect absorption of concomitantly administered oral drugs due to slow gastric emptying.

Contraindications

Personal or family history of medullary thyroid carcinoma (MTC). Patients with multiple endocrine neoplasia syndrome type 2; type 1 DM or diabetic ketoacidosis. Liraglutide is not a substitute for insulin.

Side Effects

Nausea, diarrhoea, vomiting, constipation, headache, dizziness, upper resp tract infection, influenza, sinusitis, nasopharyngitis, UTI, back pain, dehydration. Increased blood calcitonin, goitre, and thyroid neoplasms.

Pregnancy And Lactation

Pregnancy category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Precautions And Warnings

Patients with history of pancreatitis or alcoholism, inflammatory bowel disease, diabetic gastroparesis, pre-existing thyroid disease. Renal impairment. Pregnancy and lactation

Overdose Effects

Overdoses have been reported in clinical trials and post-marketing use of Liraglutide. Effects have included severe nausea and severe vomiting. In the event of overdosage, appropriate supportive treatment should be initiated according to the patient’s clinical signs and symptoms.

Therapeutic Class

GLP-1 receptor agonists.

Storage Conditions

Store between 2-8° C. Do not freeze. After initial use, it can be stored between 15-30° C for 30 days. Protect from heat and light.