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Clinician’s Corner: NCRETIN MIMETICS (GLP-1 receptor agonists)

How they work: mimics natural physiology to provide self-regulating glycemic control by enhancing insulin secretion only in the presence of high blood sugar (hyperglycemia).  GLP-1 stimulates the pancreas to INCREASE insulin and DECREASE glucagon secretion.

Insulin secretion decreases as blood glucose concentrations approach normal.

Brand Name Generic Manufacturer Year released Dose
Byetta® exanatide Astra-Zeneca 2005 5mcg-10mcg twice daily, before meals
Victoza® liraglutide Novo-Nordisk 2010 0.6-1.8mg /day any time
Bydureon®BCise exenatide -er Astra-Zeneca 2012 2mg once a week
Trulicity® dulaglutide Lilly 2014 .75- 1.5mg/week
Ozempic® semaglutide Novo-Nordisk 2017 .25-1mg/week

All of the incretin mimetics (GLP-1 agonists) are additional therapy to improve glycemic control in Type 2 diabetics who are taking metformin, a sulfonylurea or a combination, and not having adequate control.

2017: AACE (American Association of Clinical Endocrinologists) recommends incretins as first add on in Type-2 diabetes, after established metformin therapy.

Many endocrinologists are using the GLP-1 agonists along with a long acting insulin to decrease the need for mealtime “log” insulins three times daily.

In clinical trials, most patients lost weight. Proposed weight-loss mechanisms include:

  • Incretins bind to the GLP-1 receptor in the brain suppressing appetite.
  • Incretins delay gastric emptying, which may cause patients to feel full faster and longer.

Byetta dosage (exantide):      ($750.00/month)           

  • 5mcg/ dose given twice daily, anytime during the 60 minute period before morning and evening meal. Do NOT give AFTER a meal.
  • Dose can be increased to 10mcg twice daily after one month based on glycemic response and tolerability
  • NOT recommended in patients with kidney disease
  • Supplied as 30 day prefilled pens.

Victoza dosage (liraglutide):   ($950.00/month)

  • 1 pen available. You dial up dose on pen for 0.6mg or 1.2mg or 1.8mg.
  • Administered once daily any time of day without regard for meals
  • Start 0.6mg daily for 1 week. After 1 week increase dose to 1.2mg.  If not acceptable glycemic control may increase to 1.8mg. Use abdomen, thigh or upper arm.
  • Reduce both CV risk and death

Bydureon dosage BCise (Exantide-extended)   ($725.00/month)

  • 2mg once a week, every 7 days.
  • Comes as 4 syringe/vials per tray (one month supply)
  • NOT recommended in patients with kidney disease

Trulicity dosage (dolaglutide)     ($785.00/month)    0.75mg and 1.5mg pens

  • Initiate at 0.75 mg subcutaneously once weekly. Dose can be increased to 1.5 mg once weekly for additional glycemic control
  • Amazing delivery device. Auto injector.

Ozempic dosage (semaglutide)     ($800/month) 

  • Initiate with 0.25 mg subcutaneously once weekly for 4 weeks, then 0.5 mg for at least another 4 weeks.  May be escalated to a max dose 1 mg.
  • Carries warning for diabetic retinopathy.

INCRETIN MIMETICS – general prescribing rules:

  • Careful if existing stomach disease.  Careful if pancreatitis risk. Caution in renal failure.
    • Do not administer incretin mimetics & DPP-4’s together – pancreatitis risk!
  • Other diabetic medicines may increase the risk of low blood sugars with these agents
  • No additional glucose monitoring is required to determine dose.
  • No additional dose planning around meal size or amount of exercise is required.
  • Risk of Thyroid C-cell tumors (black box warning- seen in rodents)

Storage requirements: Keep under 77 degrees, do not freeze.  Keep refrigerate until first use.

Remember to write for pen needles for these devices.

Insulin/Incretin combos

Glargine & lixisenatide Soliqua® 100/33 Long acting insulin + incretin Inject once daily, within one hour of first meal of the day. Use alternative treatments if doses below 15 Units or above 60 Units are required.
Degludec & liraglutide Xultophy® 100/3.6 Long acting insulin + incretin Dose 10-50 units (max) same time each day; with or without food.

This class of drugs is one of the “smartest” classes of diabetes therapy.  Unlike the sulfonylureas, they push out insulin only when blood sugars are high.  Therefore, they have a very low risk of hypoglycemia (low blood sugar).  Unlike sulfonylureas that cost around $8.00 per month, these drugs cost 100 times more!!

Your Thompson Pharmacist is a great resource for affordable therapy for Type-2 diabetes.  Go ahead and ask…at Thompson Pharmacy it’s all for YOU!