Expiration date: 07/2028

Method of administration and dosage

Always use this medication exactly as directed by your doctor. If in doubt, consult your doctor.

Your doctor will determine the dosage regimen and route of administration individually for you, depending on the indications, the severity of the disease, and your body's response.

Recommended dosage

• The starting dose of Tirzetta is 2.5 mg once a week for 4 weeks.
• After 4 weeks, your doctor will increase the dose to 5 mg once a week.
• If necessary, after 4 weeks the dose may be increased, but not by more than 2.5 mg. Thus, taking into account the increase, the dose should not exceed 7.5 mg once a week.
• Further increase of the dose is possible, but not more than 2.5 mg to the current dose every 4 weeks to doses of 10 mg, 12.5 mg, or 15 mg once weekly. In each case, your doctor will advise you to remain on a given dose for at least 4 weeks before moving to a higher dose.
• Recommended maintenance doses are 5 mg, 10 mg and 15 mg.

The maximum dose of Tirzetta that should not be exceeded is 15 mg once a week.

Do not change the dose yourself unless your doctor tells you to do so.

Use in children and adolescents

Safety and efficacy in children under 18 years of age have not yet been established. No data are available.

Route and (or) method of administration

The drug is injected subcutaneously into the abdomen, thigh, or upper arm. It can be administered at any time of day, with or without food. The injection site should be changed each time. If you also receive insulin injections, Tirzetta should be injected into a different site.

Duration of therapy

Your doctor will determine the duration of therapy depending on the severity of your condition. Use Tirzetta for as long as recommended by your doctor.

If you forget to use Tirzetta

If you forget to take Tirzetta, consult your doctor. Do not take a double dose to make up for a missed dose.

If a dose is missed, Tirzetta should be administered as soon as possible within 4 days of the scheduled dose. If more than 4 days have passed, skip the missed dose and administer the next dose on the scheduled day. You can then resume your regular weekly dosing schedule. If necessary, the weekly dosing day can be changed, provided that the interval between doses is at least 3 days.

If you have any questions about the use of Tirzetta, please talk to your doctor.

Indications

Tirzetta is used to treat adults aged 18 years and older with poorly controlled type 2 diabetes as an adjunct to diet and physical activity:

• as monotherapy if metformin is not suitable due to intolerance or contraindications;
• in addition to other drugs for the treatment of type 2 diabetes.

Tirzetta is indicated for use in adults aged 18 years and older as adjunctive therapy to a reduced-calorie diet and increased physical activity for weight management, including weight loss and maintenance in adults with a baseline body mass index (BMI):

• ? 30 kg/m2 (obesity);

or

• ? 27 kg/m2 to < 30 kg/m2 (overweight) in the presence of at least one weight-related comorbidity (eg, hypertension, dyslipidemia, obstructive sleep apnea, cardiovascular disease, prediabetes, or T2DM).

Compound

The drug Tirzetta contains

The active substance is tirzepatide.

Tirzetta, 2.5 mg, solution for subcutaneous administration

Each syringe/cartridge contains 2.5 mg tirzepatide in 0.5 ml solution (5 mg/ml).

Contraindications

Do not use Tirzetta:

• if you are allergic to tirzepatide or any other ingredients of this medicine (listed in section 6 of the leaflet);
• if you have a history of medullary thyroid cancer, including a family history;
• if you have been diagnosed with multiple endocrine neoplasia (MEN) type 2.

Special instructions

Before using Tirzetta, consult your doctor.

Be sure to tell your doctor if you have:

• severe problems with digestion or delayed gastric emptying (including severe gastroparesis);
• inflammatory disease of the pancreas (pancreatitis);
• signs and symptoms of low blood sugar, which may include dizziness or lightheadedness, sweating, confusion or drowsiness, headache, blurred vision, slurred speech, tremors, rapid heartbeat, anxiety, irritability, mood changes, hunger, weakness, nervousness;
• kidney dysfunction;
• disorders of the gallbladder;
• damage to the retina of the eye due to diabetes mellitus (diabetic retinopathy) or thickening of the retina associated with fluid accumulation (macular edema);
• thyroid diseases.

Conditions you need to monitor

Acute pancreatitis

You should use Tirzetta with caution if you have previously been diagnosed with pancreatitis.

Cases of acute pancreatitis have been reported in people taking tirzepatide.

If signs of acute pancreatitis such as acute, unbearable abdominal pain, nausea, vomiting, or fever occur, discontinue use of Tirzetta and consult your doctor.

Hypoglycemia

People receiving tirzepatide concomitantly with insulin secretagogues (e.g. sulfonylureas) or insulin may have an increased risk of hypoglycemia (see section 4 “Possible adverse reactions”).

Effect on the gastrointestinal tract

Tirzepatide may cause gastrointestinal (GI) adverse reactions, including nausea, vomiting, and diarrhea (see section 4, "Possible Adverse Reactions"). If you experience any of these adverse reactions, consult a doctor immediately. These adverse reactions can lead to dehydration, which can lead to deterioration of kidney function, including acute renal failure. This should be especially taken into account in elderly patients, who may be more susceptible to such complications.

Severe gastrointestinal diseases

Tirzepatide has not been studied in people with severe gastrointestinal diseases, including severe gastroparesis (delayed gastric emptying), and the drug is used with caution in such people.

Acute kidney injury

Tirzepatide causes gastrointestinal side effects, including nausea, vomiting, and diarrhea. These effects can lead to dehydration, which in severe cases can cause acute kidney injury.

Cases of acute kidney injury and worsening chronic renal failure have been reported in people taking GLP-1 receptor agonists (drugs like tirzepatide). Most of these events occurred in people experiencing nausea, vomiting, diarrhea, or dehydration. If you experience any of these symptoms, notify your doctor immediately.

Acute diseases of the gallbladder

Acute events of gallbladder disease, such as cholelithiasis or inflammatory gallbladder disease (cholecystitis), have been reported with the use of GLP-1 receptor agonists.

Acute gallbladder conditions have been associated with weight loss.

If you experience severe pain in the right hypochondrium or upper abdomen, you should immediately contact your doctor.

Diabetic retinopathy

Tirzepatide has not been studied in people with diabetic retinopathy (damage to the inner lining of the eye that occurs with diabetes) requiring emergency treatment or diabetic macular edema (thickening of the inner lining of the eye due to fluid accumulation) and should be used with caution and under appropriate medical supervision in these people.

If you experience any symptoms of vision changes, notify your doctor immediately.

Risk of developing thyroid tumors

It is unknown whether tirzepatide causes thyroid tumors, including thyroid cancer, in humans. In male and female rats, tirzepatide caused a dose- and duration-dependent increase in the incidence of thyroid tumors.

You should monitor for possible symptoms, such as swelling in the neck, hoarseness, difficulty swallowing, or shortness of breath. If you experience any of these symptoms, notify your doctor immediately.

Children and teenagers

Do not give this medicine to children under 18 years of age, as the safety and effectiveness of tirzepatide in this age group have not been established.

Tirzetta contains sodium.

This medicine contains less than 1 mmol (23 mg) sodium per dose, making it essentially sodium-free.

Packaging and release form

Solution for subcutaneous administration 5 mg/ml - 0.5 ml, syringe in a disposable single-dose autoinjector - 4 pieces (autoinjectors) with a package insert.

Side effects

Like all medicines, Tirzetta can cause side effects, although not everybody gets them.

It is important that you inform your doctor about any adverse reactions you experience so that he or she can take appropriate measures (for example, temporarily suspend or discontinue treatment, change the dose and duration of use of the drug, prescribe additional therapy).

Some adverse reactions may be serious and life-threatening.

Tell your doctor immediately if you experience any of the following side effects:

Uncommon (may affect up to 1 in 100 people):

• acute, unbearable pain in the abdomen, nausea, vomiting, increased body temperature (acute pancreatitis).

Rare (may affect up to 1 in 1,000 people):

• a severe allergic reaction that is accompanied by symptoms such as difficulty breathing, decreased blood pressure, a feeling of shortness of breath, a feeling of pressure and pain in the chest, rash, itching, swelling of the lips, tongue, face, sudden weakness or other signs of a sharp deterioration in health (anaphylactic reaction);
• rapidly developing and increasing swelling of the skin, face, neck, larynx, mucous membranes, difficulty breathing and swallowing (angioedema (Quincke's edema)).

The following are other side effects that may occur with Tirzetta:

Very common (may affect more than 1 in 10 people)

• decreased blood sugar levels (hypoglycemia) with the simultaneous use of drugs that stimulate insulin secretion (sulfonylurea drugs) or insulin
• nausea
• diarrhea

Common (may affect up to 1 in 10 people)

• allergic reactions (hypersensitivity reactions)
• decreased blood sugar levels (hypoglycemia) when used concomitantly with metformin and gliflozin (empagliflozin, dapagliflozin, etc.)
• loss of appetite
• dizziness
• increased heart rate
• regular or periodic increase in blood pressure above normal values, headache, nausea, weakness (hypertension)
• abdominal pain
• vomit
• dyspepsia
• constipation
• bloating
• belching
• flatulence
• reflux of stomach contents into the esophagus (gastroesophageal reflux disease)
• hair loss (alopecia)
• fatigue
• injection site reaction
• increased levels of lipase in the blood
• increased amylase levels in the blood

Uncommon (may affect up to 1 in 100 people)

• decreased blood sugar levels (hypoglycemia) when used concomitantly with metformin
• weight loss
• cholelithiasis
• inflammatory disease of the gallbladder (cholecystitis)
• pain at the injection site
• increased levels of calcitonin in the blood (determined by a blood test)

Reporting adverse reactions

If you experience any adverse reactions, consult your doctor. This includes any adverse reactions not listed in the package leaflet. You can also report adverse reactions directly (see below). By reporting adverse reactions, you help provide more information about the safety of this medicine.

Pharmacotherapeutic group

agents for the treatment of diabetes mellitus; other hypoglycemic agents, except insulins

Interaction with other drugs

Tell your doctor if you are taking, have recently taken, or might take any other medicines.

Your doctor will need to know about the medications you are taking to take into account any possible adverse reactions that may develop due to interactions between various medications and Tirzetta, and to possibly adjust the doses of the medications you are taking.

In particular, tell your doctor if you are taking any of the following medications:

• paracetamol (antipyretic drug);
• warfarin (used to treat and prevent blood clots);
• digoxin (used for chronic heart failure);
• oral contraceptives (used to prevent unwanted pregnancy).

Impact on the ability to drive a car and operate other machinery

Driving vehicles and operating machinery

Tirzepatide has little or no effect on the ability to drive or operate machinery. When used concomitantly with sulfonylureas or insulin, caution is recommended to prevent hypoglycemia when driving or operating machinery (see section "Special Warnings and Precautions").

Use during pregnancy and breastfeeding

Pregnancy, breastfeeding and fertility

If you are pregnant or breastfeeding, think you may be pregnant, or are planning a pregnancy, consult your doctor before using this medicine.

Pregnancy

There are no data on the use of tirzepatide in pregnant women. Do not use Tirzeta during pregnancy. Use effective contraception while taking Tirzeta.

Breast-feeding

It is unknown whether tirzepatide is excreted in breast milk. A risk to the newborn cannot be excluded. Your doctor may recommend discontinuing breastfeeding or discontinuing Tirzeta after assessing the benefit of breastfeeding for your baby and the benefit of therapy for you.

Fertility

The effect of tirzepatide on human fertility (the ability of a sexually mature organism to produce offspring) is unknown. Animal studies with tirzepatide have not revealed any direct harmful effects on fertility.

Pharmacodynamics

What is Tirzetta and what is it used for?

Tirzetta contains the active ingredient tirzepatide, which is used to treat type 2 diabetes mellitus (T2DM) and obesity as an adjunct to a low-calorie diet and physical activity.

Tirzepatide is a new class of dual-acting incretins (metabolic hormones that regulate insulin and glucose levels in the blood).

In clinical studies, tirzepatide's dual action has been shown to be effective in promoting weight loss, improving metabolism, and controlling blood sugar levels in people with type 2 diabetes.

Tirzepatide regulates appetite, which may help you eat less food and lose weight.

Tirzepatide, by improving insulin sensitivity, reduces elevated blood glucose levels, reduces body weight and restores normal lipid profile.

Tirzepatide has been associated with additional benefits, including reduced waist circumference, improved metabolism (lipid and glucose levels, etc.), improved cardiovascular parameters (blood pressure, pulse), and improved liver and kidney function and health. Obesity is a serious condition that increases the risk of cardiovascular complications. Weight loss while taking tirzepatide helps reduce the risk of various complications, such as cardiovascular disease, type 2 diabetes, and others. By losing weight, you reduce the risk of these complications and increase life expectancy.

Mode of action of Thirsetta

Tirzepatide acts similarly to natural hormones—physiological regulators of carbohydrate metabolism (insulin and glucose levels), as well as appetite and food intake. Tirzepatide is a long-acting receptor agonist (interacts with the receptor (target), causing a specific biological response) for glucose-dependent insulinotropic peptide (GIP) and glucagon-like peptide-1 (GLP-1). Both receptors are present on α- and β-endocrine cells of the pancreas, brain, heart, vascular system, immune cells, intestines, and kidneys. Influence on GLP-1 receptors, in addition to regulating carbohydrate metabolism, helps you feel full faster, maintain this feeling for a longer period, and control eating behavior. GIP receptors are also present on adipocytes (the type of cell that makes up adipose tissue). Influence on GLP-1 receptors may further contribute to the regulation of food intake. Thus, the drug's simultaneous action on two receptors (GIP and GLP-1) increases its effectiveness due to their complementary action.

In patients with type 2 diabetes, tirzepatide stimulates insulin production, reduces insulin resistance, and regulates carbohydrate metabolism. In addition to regulating carbohydrate metabolism, tirzepatide can help you consume less food, which contributes to a decrease in body fat for weight management and control.

If there is no improvement or you feel worse, you should consult a doctor.

Storage temperature

from 2℃ to 8℃

Dosage form

Solution for subcutaneous administration.

Transparent, colorless to slightly yellowish solution.

Overdose

If you use more Tirzetta than you should

Your doctor will monitor you to make sure you are getting the right dose of Tirzetta.

In case of a suspected overdose of Tirzetta, consult your doctor. If possible, show the doctor the package insert.

You will be prescribed supportive treatment based on your symptoms. Gastrointestinal side effects, including nausea, may occur.

Special storage conditions

Do not freeze.

If necessary, the drug in its original packaging (pack) may be stored at a temperature not exceeding 30 °C for no more than 21 days.

Do not store the medicine in the refrigerator after storage at 30°C.