Learn More About Tizepatide

Tirzepatide is a novel medication approved by the US Food and Drug Administration (FDA) for treating type 2 diabetes mellitus(T2DM). This medication also demonstrates efficacy in weight loss, leading to its off-label use for obesity treatment. Tirzepatide is administered once weekly via subcutaneous injection with incremental dosage adjustments.

What is Tirzepatide?

Tirzepatide is a dual agonist for the glucagon-likepeptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)receptors. The drug leads to significantly improved glycemic control and weight reduction in patients with T2DM, maximizing benefits similar to GLP-1medications such as Semaglutide. Tirzepatide is a synthetic polypeptide dual agonist for GLP-1 and GIP. Tirzepatide, "twincretin," exhibits distinct characteristics from GLP-1 receptor agonists. The medication comprises 39 amino acids and is an analog of the gastric inhibitory polypeptide. Functionally, Tirzepatide stimulates insulin release from the pancreas and reduces hyperglycemia (high blood sugar in blood).

Among patients without diabetes, administering Tirzepatide once weekly for managing obesity led to remarkable reductions in body weight. The subcutaneous injection is administered once weekly, making Tirzepatide offer a competitive advantage over other drugs used to manage diabetes and overweight, which may require several daily doses. Clinical trials have determined that this drug reduces glycosylated hemoglobin (HbA1c) levels and reduces body weight. 

Tirzepatide also encourages weight loss by slowing gastric emptying through its activation of GLP-1 receptors. This action causes food to remain in the stomach longer, extending the feeling of fullness and reducing overall appetite. By delaying the movement of food into the intestines, the Tirzepatide weight loss injection ensures a steadier absorption of nutrients and glucose, contributing to more stable blood sugar levels. The prolonged satiety and decreased hunger help reduce calorie intake, making Tirzepatide an effective tool for weight management.

Pharmacokinetics

Absorption: Tirzepatide has a bioavailability of approximately 80%. The time it takes to reach peak serum levels can range from8 to 72 hours.

Distribution: The mean steady-state volume of distribution (Vd) of Tirzepatide is approximately 10.3 L. Tirzepatide is highly bound to plasma albumin (99%).

Metabolism: When injected, the peptide structure undergoes proteolytic cleavage. In addition, the C20 fatty diacid composition undergoes β-oxidation and amide hydrolysis. Being a modified polypeptide, Tirzepatide undergoes metabolism into individual amino acids in various tissues, including the liver.[6]

Elimination: Tirzepatide has a half-life of 5days, facilitating weekly dosing, and is cleared in urine and feces as metabolites.

Standard dosing is once weekly; prescribed doses can be increased on follow-up visits based on efficacy, as defined by HbA1clevels, body weight, and adverse effects. The patient's ability to tolerate adverse effects plays a significant role in dosing titration.

Side effects

Based on available data, most users do not experience significant adverse drug reactions. The primary adverse effects are gastrointestinal-related, but other side effects have also been infrequently reported. Decreased appetite is frequently reported, though this is a potential contributory etiology of intentional weight loss. The most common side effects include:

• Constipation

• Diarrhea

• Decreased appetite

• Indigestion

• Stomach pain

• Vomiting

• Nausea

  
  

Strategies for reducing or managing side effects include a slow titration(which means adjusting the dose), adequate hydration and use of medication for symptom control as needed. Sometimes, the temperature of food can affect nausea. Cold or room temperature meals might be more tolerable than hot meals, as they often have less aroma, which can trigger nausea. Ginger is a natural remedy that has been shown to reduce nausea. Consider adding ginger supplements or incorporating ginger into your diet.

Serious adverse effects include:

• Pancreatitis (inflammation of the pancreas)

• Changes in vision

• Low blood sugar

• Kidney problems or kidney failure

• Serious allergic reactions

• Gallbladder problems

If you are taking Tirzepatide and experience any of the following symptoms, you should reach out to your health care provider immediately or seek emergency medical care:

• Ongoing pain starting in the upper left or middle of the abdomen that spreads to the back, with or without vomiting

• Rash, itchiness, swelling of the eyes, face, mouth, tongue or throat and difficulty breathing/swallowing

• Decreased urine output or edema (swelling of legs, ankles or feet)

• Changes in vision

• Dizziness and/or fainting

• Upper abdominal pain, fever, jaundice or clay-colored stool

• Rapid heartbeat

Contraindications

Tirzepatide comes with a safety warning that it may cause tumors in the thyroid, including thyroid cancer. Tirzepatide is also contraindicated in multiple endocrine neoplasia syndrome type-2 (MEN-2 a genetic disorder of the endocrine glands). The FDA has identified intestinal blockage as a potential safety issue for all drugs targeting GLP-1receptors, including Tirzepatide.

Tirzepatide has the potential to affect the absorption of other medications because it delays gastric emptying. Be sure to check with your healthcare provider before taking Tirzepatide and describe all the medications you are taking. This will help you avoid any possible medication interactions.

Additionally, if you’re taking Tirzepatide in addition to other medications to lower your blood glucose levels, your dose may need to be lowered (or increased) when starting Tirzepatide to prevent hypoglycemia (very low glucose levels). Tirzepatide, and other anti-obesity medications, are FDA-approved for long-term weight management because obesity is a chronic disease, just like hypertension (high blood pressure) and type 2diabetes

After initiating therapy with Tirzepatide, clinicians are likely to follow up with patients in set intervals as early as 4 weeks or as late as 12 weeks, depending on the dosage and the local standard of care for weight management.

What’s the Difference Between Tirzepatide and Semaglutide?

The drug may sound similar to another related type 2diabetes and weight loss drug, Semaglutide, which is a glucagon-like peptide-1(GLP-1) receptor agonist. Similar to Tirzepatide, Semaglutide mimics the hormone GLP-1 and triggers the body to make more insulin when blood sugar levels rise after eating. Tirzepatide is different from Semaglutide because it also mimics the GIP hormone, so it not only affects stomach emptying and appetite, but also affects how fat is deposited in the body.

Tirzepatide appears to be exceptionally effective for weight loss in people with and without type 2 diabetes, according to the results of two clinical trials that tested its effectiveness for that use.

Nearly every participant in a study published last year who received Tirzepatide injections in conjunction with diet and exercise lost weight.

Beneficial effects on systolic blood pressure (a measure of how much pressure is exerted against your artery walls when your heart is beating) have been found across the series of trials that studied Tirzepatide in people with type 2 diabetes. Systolic pressure dropped by between 4.2millimeters of mercury (mmHg) and 12.6 mmHg after 40 to 42 weeks in participants receiving Tirzepatide, mostly attributed to the effect of weight loss.

 

Administration of Tirzepatide

Tirzepatide is administered as a once-weekly, on the same day, subcutaneous injection under the skin of your abdomen, thigh, or upper arm. The doses of Tirzepatide may vary based on the patient’s response, with a dose-dependent reduction in HbA1c and body weight observed in trials. Tirzepatide has to be titrated (adjusted) when it is started, meaning a gradual dose increase happens over many months, to allow the body to adjust to the medication and lower the risk of side effects.

For patients concurrently taking other anti hyperglycemic agents like insulin secretagogues or insulin, dose adjustments may be necessary. Therefore, it’s crucial to follow guidelines about potential interactions and necessary dose adjustments to optimize the safety and efficacy of Tirzepatide.

What if I miss a dose?

If you miss a dose, take it as soon as you can unless it is more than 4 days (96 hours) late. If it is more than 4 days late, skip the missed dose. Take the next dose at the normal time. Do not take 2 doses within3 days of each other.

What should I know about storage and disposal of this medication?

Keep this medication in the container it came in and out of reach of children. Store it away from light and heat. Store unused Tirzepatide in the refrigerator (36°F to 46°F [2°C to 8°C]) Do not freeze. Do not use Tirzepatide if it has been frozen. When traveling, store your medication in a cold container with ice packs to ensure maintenance of adequate temperature, put it in the refrigerator as soon as one becomes available. Do not leave medication in a car, glove compartment or any other hot place.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. 

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Dispose of needles and syringes in puncture resistant containers to avoid accidental puncture and always keep them out of the reach of children.

Diet and Lifestyle Changes

Tirzepatide does not give license to ditch a healthy diet and lifestyle. These medications are less likely to work without changes to underlying habits and lifestyle. Tirzepatide offers a promising path to weight loss, especially when combined with balanced dietary choices and an active lifestyle. Every patient’s experience with weight loss varies, so there is no set timeframe that applies to everyone. How quickly you lose weight depends on factors like lifestyle habits, diet, activity level, age, and other medications you may be taking.

The Takeaway

Tirzepatide is a recently approved medication that shows promise in managing type 2 diabetes and aiding significant weight loss by mimicking key gut hormones. It’s an injectable drug that can help you better control your blood sugar levels and potentially achieve substantial weight reduction when combined with a healthy lifestyle. By understanding what to eat, managing side effects, and incorporating consistent lifestyle changes, you can navigate your weight loss journey with absolute confidence. 

 

References

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