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Tirzepatide 20mg/mL Injection Solution
Tirzepatide is a peptide that exhibits multiple actions in the body resulting in up to 20% weight loss, reduction in insulin resistance with corresponding reduction of associated risk factors, positive effects on dyslipidemia and beneficial effects on bone density.
GLP-1 (Glucagon-like Peptide-1) Receptor agonist
• GLP-1-R acts in pancreatic Beta islet cells and GI tract causing incretin activity (increased insulin secretion) and
slows gastric emptying/transit
• Reduces plasma Glucagon levels, a well-known risk marker for T2D (diabetes)
• Decreases hunger through Satiety pathways:
– Effects on Melanocortin System (esp Hypothalamus and Brain Stem- brain hub for appetite)
– increases A-Melanocyte Stimulating hormone which reduces hunger
• Up-modulates fat utilization
• Increase of Leptin hormone in brain causing hunger reduction through the:
– Increase in hunger-reducing POMC (Anorexigenic Pro-Opiomelanocortin)
– Reduction in hunger hormones AgRP (Agouti Related Peptide) and NPY (Neuropeptide Y)
• Reduction of Ghrelin levels in stomach/gut
• Gut-brain signaling via several pathways including Vagal feedback to HP/brain stem.
GIP (Glucose Dependent Insulinotropic Polypeptide, also known as Gastric Inhibiting Polypeptide) agonist.
• The main incretin hormone- insulinotropic effect in response to food intake
• If used alone- Increases glucagon secretion- risky for T2D but when used in combination with GLP-1 R- down
regulates glucagon levels.
• In combo with GLP-1R- enhanced appetite suppression and improved WAT (white adipose tissue) health and
storage capacity, thereby reducing lipid ‘spillover’ ectopic fat accumulation (around organs- heart, liver, kidneys
etc)
Indication and Usage
Tirzepatide indicated in combination with a reduced calorie diet and increased physical activity:
• to reduce the risk of major adverse cardiovascular events (cardiovascular death, non-fatal myocardial infarction,
or non-fatal stroke) in adults with established cardiovascular disease and either obesity or overweight.
• to reduce excess body weight and maintain weight reduction long term in:
• Adults and pediatric patients aged 12 years and older with obesity
• Adults with overweight in the presence of at least one weight-related comorbid condition
Common side effects include:
Nausea, diarrhea, vomiting, constipation, abdominal pain, dyspepsia, injection site reactions, fatigue, hypersensitivity reactions, eructation, hair loss, gastroesophageal reflux disease.
Warnings & Precautions:
1. Risk of Thyroid C-Cell Tumors (A mass in the neck, dysphagia, dyspnea, or persistent hoarseness)
2. Acute Pancreatitis (Severe and persistent abdominal pain, may or may not have nausea)
3. Acute gallbladder disease
4. Hypoglycemia especially with the use of other diabetic medications like sulfonylureas and insulin
5. Acute kidney injury
6. Severe Gastrointestinal Disease
7. Hypersensitivity
8. Diabetic Retinopathy Complications in Patients with Type 2 Diabetes Mellitus 5
9. Suicidal behavior and ideation
Who should not take Tirzepatide? Given the theoretical risk, Tirzepatide should be avoided in those with a personal or family history of medullary thyroid carcinoma. Patients with a history of MEN 2 (multiple endocrine neoplasia syndrome type-2) should also avoid Tirzepatide. Furthermore, patients who experience a hypersensitivity reaction should avoid using Tirzepatide any further. Other relative contraindications also exist, such as gallbladder disease or diabetic retinopathy.
Dosage and Administration:
Tizepatide is a potent medication, and it is extremely important to adhere to the prescribed dosing schedules. Your
body needs time to adjust to the medication. It is not a race to get to the last dosing. If your patient needs to stay at
a lower dose, then that is acceptable.
Tirzepatide 20mg/mL Inj. Solution
Weeks 1-4: Inject 0.13 mL Subcutaneously once weekly
Weeks 5-8: Inject 0.25 mL Subcutaneously once weekly
Weeks 9-12: Inject 0.5 mL Subcutaneously once weekly
Weeks 13 & Thereafter: Inject 0.75mL Subcutaneously once weekly.
Tirzepatide is administered subcutaneously in the abdomen, thigh, or upper arm once weekly on the same day each week, at any time of the day with or without food. Do not inject intramuscularly or intravenously. Rotate the sites of injection weekly and do not inject into an area where the skin is tender, swollen, bruised, red or hard. Avoid injecting into areas with scars or stretch marks.
Missed Dose: If a dose is missed, you may administer the missed dose as soon as possible, within 4 days (96 hours) after the missed dose. If more than 4 days have passed, skip the missed dose and administer the next dose on the regularly scheduled day. In each case, patients can then resume their regular once weekly dosing schedule. The day of weekly administration can be changed, if necessary, as long as the time between the two doses is at least 3 days (72 hours)