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Diabetes Mellitus: Non Insulin Injectable Agents!

PHARMACOTHERAPY

 NON-INSULIN INJECTABLE AGENTS

1.GLUCAGON-LIKE PEPTIDE 1 AGONSIT:

  • GLP-1 Agonists enhance glucose dependent insulin secretion while suppressing inappropriately high glucagon secretion in the presence of elevated glucose, which results in reduced hepatic glucose production.
  • Exenatide and Liraglutide are both indicated for the treatment of T2 DM to improve glycemic control.

Pharmacokinetics:

  • Plasma concentrations are detected up to 10hrs after injection, although pharmacodynamics action lasts for approximately 6hrs.

Mechanism of Action:

  • GLP-1 agonists lower blood glucose levels by producing glucose dependent insulin secretion, reducing post meal glucose secretion, which decreases post meal glucose output, increasing satiety which decreases food intake and regulating gastric emptying which allows nutrients to be absorbed into the circulation more smoothly.

Clinical uses:

  • In a 26 weeks head-to-tail trial in patients with T2DM with a baseline A1c between 7%-11% who were taking metformin, sulfonylurea, or both; Exenatide lowered A1c levels to 0.8% and Liraglutide lowered A1c levels greater than 1.1%.
  • Both drugs produced similar weights loss, with an average reduction of 3.24kg for liraglutide and 2.87kg for exenatide.

Dose:

  • Exenatide is recommended for twice daily dosing in its intermediate release.
  • As exenatide is excreted renally, it is not recommended for patients with renal impairment.
  • Liraglutides half-life is 13hrs, making it suitable for once daily dosing. No specific dose adjustments are required for liraglutide in renal impairment patients.

Adverse Effects:

  • An increased risk of hypoglycemia occurs when GLP-1 agonists are used in combination with sulfonylurea.
  • Nausea
  • Vomiting
  • Diarrhea
  • GLP-1 Agonists delay absorption of other medications, so it is best to take concomitant medications 1hr. before or 3hr. after a GLP-1 agonist if rapid absorption of concomitant medication is required.
  • Acute pancreatitis

Contraindications:

  • They are contraindicated in pt. with a personal or family history of medullary thyroid cancer and in history of multiple endocrine tumors.


2.AMYLIN

Mechanism of Action:

  • Pramlintide acetate is a synthetic analog of human amylin, which is naturally occurring neuroendocrine peptide that is co-secreted by the Beta cells of the pancreas in response to food.
  • The secretion of Amylin is completely deficient in patients with T1DM and relatively deficient in patients with T2 DM.
  • Pramlintide slower the gastric emptying without altering absorption of nutrients. suppresses glucagon secretion and leads to reduction in food intake by increasing satiety. By slowing the gastric emptying, the normal initial post meal spike in blood glucose is reduced.

Administration and Dose:

  • Pramlintide is given by SC injection before meals to lower the postprandial blood glucose elevations.
  • A disposable pen formulation is now on the market and available as SmylinPen 60 for patients with T1 DM and SmylinPen 120 for people with T2 DM.

  • The no. of days the pen will last will vary depending on the daily dose.

  • The amount of medication is 1.5mL in the SmylinPen and 2.7mL in the SmylinPen 120

When rapid absorption is needed for the efficacy of an agent, pramlintide should be administered 2hrs before or 1hr after this drug.

Clinical Uses:

  • Pramlintide generally results in an average weight loss of 1-2kg.
  • It is injected as a combination therapy with insulin in patients with T1 or T2 DM.
  • It has been shown to decrease A1c levels by 0.4-0.5%

Adverse Effects:

  • Hypoglycemia
  • Nausea
  • Vomiting

Contraindication:

  • It is contraindicated in patients receiving medications that alter GI mobility, such as Acetylcholine agents, or drugs that slower the absorption of nutrients such as a-glucosidase inhibitors.

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