Tirzepatide

An antidiabetic drug called tirzepatide is used to treat type 2 diabetes and aid in weight loss. Injections of tirzepatide are given subcutaneously or beneath the skin. It is marketed in the US under the names Zepbound for weight reduction and obstructive sleep apnea treatment and Mounjaro for diabetic treatment.

Tirzepatide is an agonist for the GLP-1 receptor and an analog of the gastric inhibitory polypeptide. Nausea, vomiting, diarrhea, decreased appetite, constipation, upper abdominal discomfort, and abdominal pain are among the most frequent adverse effects.

What is Tirzepatide?

Tirzepatide, a product of the Zepbound brand, is used to assist people in losing weight and keeping it off. By reducing hunger and delaying the passage of food from the stomach into the small intestine, tirzepatide helps people lose weight and may prolong feelings of fullness. Adults with obesity who suffer from moderate to severe obstructive sleep apnea (OSA) can also take the Zepbound brand of tirzepatide. Every week, tirzepatide is injected beneath the skin with an autoinjector pen.

The FDA has approved Zepbound (tirzepatide) to help adults who are obese or overweight and suffer from OSA or other weight-related medical conditions lose weight. Zepbound aids in weight loss and maintenance and is best used with diet and exercise.

For type 2 diabetes, tirzepatide (sold under the Mounjaro brand) is used to assist lower blood sugar levels. Tirzepatide lowers blood sugar levels in type 2 diabetes by slowing the passage of food through the intestines, reducing the amount of sugar the liver produces, and assisting in the release of insulin when blood sugar levels are elevated. Mounjaro should be used in conjunction with exercise and a healthy diet.

The FDA-approved medication Mounjaro (tirzepatide) is used in conjunction with diet and exercise to treat adults with type 2 diabetes. It can be taken alone or in combination with other diabetes medications such as metformin, SGLT2 inhibitors, or sulfonylureas.

The usage of tirzepatide in patients with a history of pancreatitis is unknown. Individuals with type 1 diabetes should not take tirzepatide.

Eli Lilly and Company manufactures Zepbound and Mounjaro, both of which contain the same active component, tirzepatide. Zepbound is available in single-dose pens in the following strengths: 2.5 mg, 5 mg, 7.5 mg, 10 mg, 12.5 mg, and 15 mg per 0.5 mL. It is also available in single-dose vials containing 2.5 mg and 5 mg per 0.5 mL.

Tirzepatide: How does it work?

Mechanism of Action

It has been demonstrated that tirzepatide’s dual agonist activity, which involves a higher affinity for GIP receptors than GLP-1 receptors, results in greater reductions of hyperglycemia than a selective GLP-1 receptor agonist. Tirzepatide replicates the effects of endogenous GIP at the GIP receptor, according to signal studies.

Yet, tirzepatide exhibits a preference for cAMP (a messenger linked to the control of lipid, sugar, and glycogen metabolism) production at the GLP-1 receptor as opposed to β-arrestin recruitment. Preference for the GIP receptor and unique signaling characteristics at GLP-1 indicate that this biased agonism raises insulin secretion. At the 10 mg dosage, tirzepatide has been shown to raise levels of adiponectin, an adipokine involved in the control of both glucose and lipid metabolism, by up to 26% from baseline after 26 weeks.

Structure

To maximize the compound’s absorption and metabolism, tirzepatide, a homolog of the human GIP hormone with a C20 fatty diacid component attached, is utilized. A glutamic acid and two (2-(2-aminoethoxy)ethoxy)acetic acid units connect the fatty-diacid portion (eicosanedioic acid) to the lysine residue’s side chain. Due to its high affinity for albumin, this arrangement enables a substantially longer half-life, increasing the interval between dosages.

Synthesis

In 2016, Eli Lilly and Company submitted patents that revealed the synthesis of tirzepatide for the first time. An allyloxycarbonyl protecting group on the lysine at position 20 of the linear chain of amino acids allows for a final set of chemical processes that derivatize the lysine’s sidechain amine with the lipid-containing fragment. This is accomplished using typical solid phase peptide synthesis.

There have been reports of extensive production of this substance.

On Zepbound, how much weight is lost?

After 72 weeks, patients using 5 mg of Zepbound (tirzepatide) per week dropped an average of 16.1 kg (35.5 lb). Over 72 weeks, the average weight reduction for Zepbound’s 10 mg weekly dose was 22.2 kg (48.9 lb), while for Zepbound’s 15 mg weekly dose, the average weight loss was 23.6 kg (52.0 lb). Over 72 weeks, those who took a placebo dropped 2.4 kg (5.3 lb).

What side effects can tirzepatide cause?

Common adverse effects of tirzepatide

Abdominal discomfort, burping, constipation, diarrhea, dyspepsia, exhaustion, gastroesophageal reflux disease, hair loss, hypersensitivity reactions, injection site reactions, nausea, and vomiting are among the most frequent adverse effects of tirzepatide, affecting at least 5% of patients.

Serious adverse effects from tirzepatide

Severe stomach issues, acute kidney damage, gallbladder disease, inflamed pancreas (acute pancreatitis), severe allergic reactions, hypoglycemia, diabetic retinopathy in type 2 diabetics, suicidal thoughts or behavior, and food or liquid entering the lungs during anesthesia or deep sedation are all examples of serious tirzepatide side effects.

Stop using this medication and seek immediate medical attention if you have:

• Indications of an allergic reaction, such as hives, lightheadedness, breathing difficulties, facial, lip, tongue, or throat swelling, or pancreatitis, which manifests as nausea, vomiting, and excruciating upper abdominal pain that travels to the back.

Make an immediate call to your physician if you have:

Severe digestive issues; adverse effects on the eyes or changes in eyesight, such as hazy or blurred vision;

• Symptoms of a thyroid tumor, such as a lump or swelling in your neck, difficulty swallowing, a hoarse voice, or shortness of breath; symptoms of a gallbladder issue, such as chalky stools, post-meal stomach pain, nausea, heartburn, bloating, and excruciating upper abdominal pain that could radiate to your back;
• The symptoms of low blood sugar can include headache, weakness, hunger, sweating, confusion, irritability, disorientation, a fast heartbeat, jitters, kidney difficulties with little to no urination, ankle or foot swelling, fatigue, and shortness of breath.

Warnings

Thyroid C-cell tumors may be caused by tirzepatide. If you or anybody in your family has a history of thyroid cancer or Multiple Endocrine Neoplasia (MEN) syndrome, you must inform your doctor. This syndrome results in the development of endocrine gland cancers. You should contact your doctor right away if you have any of the following symptoms: hoarseness, shortness of breath, swallowing difficulties, or a lump or swelling in your neck.

Keep all of your appointments with the lab, your doctor, and other medical specialists. To monitor how your body is reacting to this medication, your doctor could prescribe specific tests.

Before taking tirzepatide

• If you have an allergy to tirzepatide, any other drugs, or any of the substances in this medication, let your doctor and pharmacist know. A list of the medication’s ingredients can be found at the bottom of this page.
• If you are contemplating surgery or any other operation involving heavy sedation or anesthesia, let your healthcare provider know.
• Inform your physician of any digestive problems, such as difficulty digesting food, a history of diabetic retinopathy, or renal or pancreatic disease.
• If you plan to get pregnant, are presently pregnant, or are breastfeeding a kid, let your doctor know. You should notify your doctor if you become pregnant while using this medication.

How is tirzepatide to be used?

You should carefully read the instructions on your prescription label and ask your doctor or pharmacist to clarify any parts you don’t understand. This drug must be taken precisely as directed. Never take more or less of it or take it more frequently than your doctor has suggested.

Using a syringe and a single-dose vial or a pre-filled pen, tirzepatide is injected subcutaneously. Proper injection techniques should be taught to patients or caregivers. A 1 mL syringe that can measure a 0.5 mL dose must be used for dose administration when utilizing single-dose vials.

Usually, it is provided

• Every week.
• It can be taken with or without food, and at any time of day.
• It may be administered by injection into the upper arm, belly, or thigh.
• With every dose, you should switch up the injection locations.

Most likely, your doctor will start you on a modest dose that can be increased gradually but not more than once every four weeks.

As long as there are at least three days between doses, you are free to switch around the day of the week that you take tirzepatide.

Insulin and tirzepatide can be administered in the same location, however they shouldn’t be given adjacent to each other. It is recommended that insulin and tirzepatide be administered as distinct injections rather than together.

Type 2 diabetes is managed but not cured by Mounjaro. You might not experience the full benefits of this medication for at least four weeks. Keep taking this medication even if you feel better. Consult your doctor before ceasing to use this medication.

Information on tirzepatide dosage

Average Zepbound Dosage for Adult Weight Loss and OSA

The first dosage is 2.5 mg injected subcutaneously once a week.

After four weeks, the dosage needs to be raised to five milligrams injected once a week subcutaneously.

Additional dosage increases: The dosage may be raised in increments of 2.5 mg after the current dose has been taken for at least 4 weeks.

A weekly subcutaneous injection of 5 mg, 10 mg, or 15 mg is the indicated maintenance dose for weight loss.

For OSA, a weekly subcutaneous injection of 10 mg or 15 mg is advised as the maintenance dose.

Maximum dosage: once weekly, 15 mg subcutaneously.

Normal Mounjaro Dosage for Adults with Type 2 Diabetes

The first dosage is 2.5 mg injected subcutaneously once a week.

After four weeks, the dosage ought to be raised to five milligrams injected once a week subcutaneously.

After taking the current dosage for at least four weeks, the dosage should be increased in increments of 2.5 mg if further glycemic control is required.

Maximum dosage: once weekly, 15 mg subcutaneously.

Comments: The 2.5 mg dosage is not meant for glycemic management; rather, it is for the beginning of treatment. As long as there is a minimum of three days (72 hours) between the two doses, the weekly administration day may be altered if needed.

If I forget to take a dose, what should I do?

Take the missing dose of tirzepatide as soon as you remember to do so, preferably within four days of the missed dose. On the other hand, omit the missed dose and stick to your usual dosing plan if it has been more than four days since your last dose. Avoid administering two injections within three days of one another.

Discussions

Inform your physician and pharmacist of all the prescription and over-the-counter drugs, vitamins, nutritional supplements, and herbal products you now use or intend to take. Your doctor may need to adjust the dosages of your drugs or closely monitor you for any adverse effects since they may interact with tirzepatide.

While taking this medication, birth control pills may not function as effectively. Your doctor might advise you to take a different birth control method for four weeks following the beginning of tirzepatide and four weeks following any dose adjustment.

The risk of hypoglycemia may rise if tirzepatide is taken with other diabetes medications, such as insulin or sulfonylureas. Consult your physician and pharmacist about managing low blood sugar.

This list is not all-inclusive. Prescription and over-the-counter medications, vitamins, and herbal products are just a few of the numerous medications that may interact with Mounjaro.

Maintaining Storage

• Keep it refrigerated between 36°F and 46°F (2°C and 8°C).
• Avoid freezing. Avoid using if frozen.
• To keep the single-dose pens safe from light, keep them in their original carton until you’re ready to use them.
• Each single-dose pen can be kept for up to 21 days at room temperature, up to 86°F (30°C), if necessary.

FAQs

Reference

• Wikipedia contributors. (2025, February 23). Tirzepatide. Wikipedia. https://en.wikipedia.org/wiki/Tirzepatide
• 1mg. (n.d.). Tirzepatide: View Uses, side effects, and medicines | 1mg. https://www.1mg.com/generics/tirzepatide-510715
• Tirzepatide: Uses, Dosage, Side Effects & Warnings. (n.d.). Drugs.com. https://www.drugs.com/tirzepatide.html