Tirzepatide, sold under the brand name Mounjaro®, is used primarily for the treatment of type 2 diabetes and weight loss. Its dosing schedule involves a gradual increase to help manage potential side effects and optimize its effectiveness. Here’s a breakdown of the common dosing regimen for tirzepatide when used for weight loss.

Initial Dosing and Titration

• Starting Dose: 2.5 mg injected subcutaneously (under the skin) once a week.
• First Increase: After 4 weeks, increase to 5 mg once weekly.
• Subsequent Increases: Depending on the individual’s response and tolerability, the dose can be increased every 4 weeks:
  • From 5 mg to 7.5 mg once weekly.
  • Then from 7.5 mg to 10 mg once weekly.
  • And potentially to 15 mg once weekly as the maximum dose.

Considerations:

• The titration schedule is designed to minimize gastrointestinal side effects, common with GLP-1 receptor agonists like tirzepatide. Possible side effects include nausea, diarrhea, and vomiting.
• The dose may be adjusted based on the patient's glycemic response and is not necessarily increased to the maximum unless needed for better blood sugar control/ weight loss.
• It's important to administer tirzepatide on the same day each week to maintain consistent blood levels of the medication.

Tirzepatide, marketed under the brand names Mounjaro® and Zepbound®, are injectable medications that have been gaining attention for their effectiveness in treating type 2 diabetes and their significant potential in weight loss. While it's primarily approved by the FDA for use in type 2 diabetes, many clinical trials and studies have highlighted its benefits for weight loss, leading to expectations of its approval for this specific use.

Mechanism of Action

Tirzepatide mimics the action of two incretin hormones, GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic polypeptide). These hormones play crucial roles in regulating blood sugar levels, appetite, and energy intake. The dual action of tirzepatide not only helps to reduce blood glucose levels but also suppresses appetite, which contributes to weight loss.

Weight Loss Efficacy

Studies have shown that tirzepatide can lead to significant weight loss. In clinical trials, participants using tirzepatide experienced notable reductions in body weight. Results vary based on the dose and individual factors, but some participants lost up to 20% of their body weight over the course of the studies, which is comparatively higher than results typically seen with other weight loss medications currently on the market.

For Type 2 Diabetes Ozempic®

• Starting Dose: 0.25 mg once weekly for 4 weeks; this dose is intended for treatment initiation and is not effective for glycemic control.
• Maintenance Dose: After the initial 4 weeks, increase to 0.5 mg once weekly. If additional glycemic control is needed, the dose may be increased after at least 4 weeks to 1.0 mg once weekly, and potentially further to 2.0 mg once weekly based on efficacy and tolerability.

For Weight Loss Wegovy®

• Starting Dose: 0.25 mg once weekly for 4 weeks.
• Incremental Increases: The dose is then increased every 4 weeks through a step-wise approach:
  • Increase to 0.5 mg once weekly for 4 weeks.
  • Then to 1.0 mg once weekly for 4 weeks.
  • Followed by 1.7 mg once weekly for 4 weeks.
  • And finally, to 2.4 mg once weekly.

The gradual increase in dosing for both uses is designed to improve gastrointestinal tolerability, as semaglutide can cause side effects such as nausea and diarrhea, particularly when treatment is initiated or doses are increased.

It is essential that semaglutide be administered on the same day each week, and it can be taken at any time of day, with or without meals. If a dose is missed, it should be taken as soon as possible within 5 days after the missed day. If more than 5 days have passed, the missed dose should be skipped, and the next dose should be taken on the regularly scheduled day.

Semaglutide is primarily available as an injectable medication under the brand names Ozempic®, and Wegovy®, used for the treatment of type 2 diabetes and weight loss. However, for those seeking non-injectable options, semaglutide is also available in an oral form:

Rybelsus® is the oral form of semaglutide. It was the first oral glucagon-like peptide-1 (GLP-1) receptor agonist approved for use. Rybelsus® is taken as a daily tablet and is used for the treatment of type 2 diabetes. It offers an alternative for patients who are not comfortable with injections or who prefer a pill-based treatment. While the oral form is effective for managing blood sugar levels in type 2 diabetes, its use for weight loss is not as well-established as the injectable forms, which have been more prominently studied and utilized in weight management.

Compounded semaglutide is also available in an oral form with similar active ingredients to Rybelsus® for those who prefer the convenience of a daily medication vs a weekly injection. The oral for has the added benefit of being shelf stable at room temperature where the injectable needs to be refrigerated.

Semaglutide sold under brand names Ozempic® and Wegovy®, is used for both for type 2 diabetes management and weight loss, can have several potential side effects. Common side effects often relate to the gastrointestinal system but there are other considerations as well. Here’s a detailed look:

Common Side Effects

1. Gastrointestinal Issues: The most frequently reported side effects are gastrointestinal in nature, including nausea, vomiting, diarrhea, abdominal pain, and constipation. These symptoms are generally mild to moderate and often decrease over time as the body adjusts to the medication.
2. Appetite Changes: Decreased appetite is a common effect that contributes to weight loss in patients using semaglutide.

Less Common but Serious Side Effects

1. Pancreatitis: There is a risk of inflammation of the pancreas, which is a serious condition that requires immediate medical attention. Symptoms can include severe abdominal pain that may radiate to the back.
2. Kidney Problems: In some cases, semaglutide can affect kidney function, leading to kidney injury or worsening of pre-existing kidney disease.
3. Gallbladder Issues: There have been reports of gallbladder-related problems, such as gallstones and inflammation of the gallbladder, particularly in patients losing weight rapidly.
4. Hypoglycemia: When used with other medications for diabetes that can lower blood sugar, such as insulin or sulfonylureas, semaglutide can increase the risk of hypoglycemia (low blood sugar).

Wegovy® vs Zepbound® are both effective medications used for weight management, but they work in slightly different ways and have different profiles that might make one more suitable than the other depending on individual health conditions and goals.

Wegovy® (Semaglutide) works by mimicking a hormone that targets areas of the brain involved in regulating appetite and food intake. It has been widely used for diabetes treatment and more recently for weight loss. The effectiveness of semaglutide for weight loss has been well-documented, with patients experiencing significant reductions in body weight.

Zepbound® (Tirzepatide), on the other hand, combines the actions of two hormones (GLP-1 and GIP) which are also involved in appetite regulation and insulin secretion. This dual action not only helps in reducing appetite but also improves glucose control more effectively. Early studies and clinical trials have shown that tirzepatide may lead to even greater weight loss than semaglutide.

Weight regain after stopping Wegovy® or Ozempic® can vary depending on individual factors such as diet, exercise habits, and overall lifestyle. Semaglutide, used in the treatment of type 2 diabetes and for weight loss, works by regulating appetite and calorie intake, helping people to reduce their body weight while they are on the medication.

Research indicates that when individuals discontinue Wegovy® or Ozempic®, there is a tendency to regain some of the weight that was lost. This is primarily because the physiological effects that reduced appetite and calorie intake are no longer active. The amount of weight regained can be influenced by whether the person adopts long-term changes to their eating habits and physical activity levels.

Studies have shown that weight regain can start within weeks of stopping the medication. However, adopting a healthy diet and maintaining physical activity can help manage weight gain after discontinuing Wegovy® or Ozempic®. It's important for individuals considering stopping Wegovy® or Ozempic® to consult with healthcare providers, who can offer strategies to maintain weight loss or recommend alternative treatments.