Skip to main content

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.

Labels:

Comments

Post a Comment

Popular posts from this blog

Diabetes Mellitus: Clinical Presentation and Diagnosis!

 CLINICAL PRESENTATION AND DIAGNOSIS OF DM 2. SCREENING American Diabetes Association (ADA) recommends routine screening for T2 DM every 3 years in all adults starting at 45 years of age. Testing of T2 DM should be considered in any adult, regardless of their age, who have a BMI greater than or equal to 25kg/m2. The ADA does not currently recommend widespread screening for T1 DM because of the relatively low incidence in the general population, although measurement of Islet antibodies may be appropriate for high-risk individuals. 3.GESTATIONAL DIABETES: "Gestational diabetes is the glucose intolerance in women during pregnancy". All pregnant women who have risk factors for T2 DM should be screened for undiagnosed T2 DM at their first prenatal visit using standard diagnostic criteria.  Any women found to have diabetes in the early point at pregnancy is considered to have T2 DM or GDM. All other pregnant women, not currently known to have DM should be screened for GDM with a 75...
Post a Comment
Read more

Hospital Acquired Pneumonia- Definition, Predisposing Factors, Clinical Features and Management!

 HOSPITAL ACQUIRED PNEUMONIA Definition: "HAP refers to a new episode of pneumonia occurring at least 2 days after the administration to hospital. It is the most common Hospital Acquired Infection (HAI) and leading cause of HAI-associated death". Predisposing factors: Aspiration of nasopharyngeal secretion Bacteria introduced into the lower GIT. Bacteriaemia Old age Mode of Spread:  Droplet infection Infecting agent: Bacteria: S.pneumonia , S.aureus , H.influenza Virus: Adenovirus, Corona virus, Herpes Simplex Clinical Features: Purulent sputum New radiological infiltrates Temperature > 38 degree Celsius Leukocytosis Investigations: Chest Pain:  to confirm the diagnosis and exclude complication. Pulse Oximetry : to monitor response to oxygen therapy, if SaO2 < 93% features of sever pneumonia, identify ventilatory failure or acidosis. Cell count:  ESR, Neutrophil leukocytosis Microbiological studies:  for severe CAP and those that do not respond to ...
Post a Comment
Read more

Management of H.pylori and NSAID-associated ulcers Eradication!

MANAGEMENT FOR H.PYLORI ERADICATION It is known that H.pylori infection is associated with over 90% of duodenal ulcers and 80% of Gastric Ulcers. Antibiotics alone or acid-suppressing agents alone, do not eradicate H.pylori . Both therapies act synergistically as growth of the organism occurs at elevated pH and antibiotics efficacy is enhanced during growth. Additionally, increasing intragastric pH may enhance antibiotic absorption. High eradication rates are achieved by a short course of Triple Therapy consisting of:            1 .PPI                                         2. Clarithromycin                         3. Amoxicillin/Metronidazole          in a twice recommended simultaneous regimen. First-Line Therapy :  European Guidelines recommended 1 we...
Post a Comment
Read more