Tirzepatide is a once-weekly GIP (glucose-dependent insulinotropic polypeptide) receptor and GLP-1 (glucagon-like peptide-1) receptor agonist, representing a new class of medicines studied for the treatment of obesity.
Tirzepatide is sold under the brand name Mounjaro. It is a single peptide that triggers the body's receptors for GIP and GLP-1, two natural incretin hormones.
It is a first-in-class medication that activates both GLP-1 and GIP receptors leading to improved blood sugar control. This medication was approved for medical use in the United States in May 2022.
The glucose-dependent insulinotropic peptide is a hormone released from the small intestine that enhances the release of insulin after eating.
So, how does it work?
The GLP-1 stimulates insulin secretion, inhibits glucagon secretion at pancreatic alpha cells, and has an extrapancreatic influence as slowing gastric emptying which increases the feeling of satiety (“fullness”).
GIP is the main hormone in healthy people, causative of most of the incretin effects, but the insulin response after GIP secretion in Type 2 DM patients is strongly reduced. In the past, GIP has been considered an unappealing therapeutic target for Type 2 DM. This conception has been changing in recent years since it has been reported that resistance to GIP can be reversed and its effectiveness restored by improving glycemic control.
GIP has decreased food intake and increased energy expenditure, resulting in weight reductions. Combined with a GLP-1 receptor agonist, it has a more significant effect on glucose and body weight effects:
· Substantial A1C reductions.
· Boosted weight loss.
· Improvements in cardiometabolic measures.
· Reduce appetite.
What is the difference from Semaglutide?
Tirzepatide has a greater affinity to GIP receptors than the GLP-1 receptors and this dual agonist behavior has been shown to produce greater reductions of hyperglycemia compared to the selective GLP-1 receptor agonist.
The study from SURMOUNT-1 clinical trial in April 2022, showed overweight or obese participants who had at least one additional comorbidity (but not diabetes) lost up to 52 lbs or 22.5% of their body weight during the 72-week duration of the Mounjaro (Tirzepatide) clinical trial.
Common side effects:
- Nausea
- Vomiting
- Diarrhea
- Decreased appetite
- Constipation
- Upper abdominal discomfort
- Abdominal pain
Serious Side effects
· Inflammation of the pancreas
o Severe pain in the stomach area that will not go away with or without vomiting. Pain may be felt from the abdomen to the back.
· Low blood sugar (hypoglycemia)
o Higher risk is Tirzepatide is used with other medications that can cause low blood sugar such as sulfonylurea or insulin.
o Signs and symptoms of low blood sugar may include, dizziness or light-headedness, sweating, confusion, or drowsiness, headache, blurred vision, slurred speech, shakiness, fast heartbeat, anxiety, irritability or mood changes, hunger, weakness, and feeling jittery.
Serious Allergic Reactions
· Swelling of the face, lips, tongue, and throat, problems breathing or swallowing
· Severe rash or itching, fainting or feeling dizzy
· Very rapid heartbeat
· Kidney problems (kidney failure)
o In patients who have kidney problems, diarrhea, nausea, and vomiting may cause a loss of fluids (dehydration), which may cause kidney problems to get worse. It is essential to drink fluids to help reduce the chance of dehydration.
· Changes in vision
· Gallbladder problems
o Pain in your upper stomach
o Fever
o Yellowing of skin or eyes (jaundice)
o Clay-colored stools
Please call us at 731-882-7373 for a free phone consultation with one of our Nurse Practitioners if Tirzepatide Plus is the right pharmacological therapy for you for weight management in addition to a healthy lifestyle and habits.
References:
Do GLP-1–Based Therapies Increase Cancer Risk?: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3920789
Glucose-dependent insulinotropic polypeptide (Gastric Inhibitory Polypeptide; GIP)
https://pubmed.ncbi.nlm.nih.gov/19251046/
Tirzepatide Once Weekly for the Treatment of Obesity: https://www.nejm.org/doi/full/10.1056/NEJMoa2206038
The Role of GIP Receptor in the CNS for the Pathogenesis of Obesity: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8576424/
Therapy in the Early Stage: Incretins: https://pubmed.ncbi.nlm.nih.gov/21525466/
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