Tesamorelin (Egrifta / Egrifta SV) Medical Information Sheet
1. Indications and Usage
Tesamorelin is a synthetic peptide analog of Growth Hormone Releasing Hormone (GHRH). It is officially indicated for:
- Reduction of excess abdominal fat (visceral adiposity) in HIV-infected patients with lipodystrophy.
Important Limitation: The long-term cardiovascular safety and potential long-term cardiovascular benefit of Tesamorelin treatment have not been studied and are not known. It is not indicated for weight loss management in the general population.
2. Mechanism of Action
Tesamorelin functions as a Growth Hormone Releasing Factor (GRF) analog that mimics the action of the naturally occurring GHRH produced in the hypothalamus.
- Pituitary Stimulation: Tesamorelin binds to and activates the GHRH receptors on the pituitary somatotroph cells in the brain.
- Endogenous Growth Hormone (GH) Release: This binding stimulates the synthesis and pulsatile release of the patient’s own endogenous Growth Hormone (GH).
- IGF-1 Increase: The increased GH, in turn, stimulates the production of Insulin-like Growth Factor-1 (IGF-1) and IGF-Binding Protein-3 (IGFBP-3) in the liver.
- Metabolic Effect: The subsequent GH and IGF-1 increase leads to a reduction of visceral adipose tissue (VAT), the deep fat around the organs in the abdomen, which is characteristic of HIV-associated lipodystrophy.
3. Dosage and Administration
Tesamorelin is administered as a subcutaneous injection once daily.
| Aspect | Details |
|---|---|
| Standard Dose | 1.4 mg or 2 mg injected once daily, depending on the specific formulation (e.g., Egrifta SV is 1.4 mg). Always follow the exact dosage and formulation prescribed by your doctor. |
| Route | Subcutaneous injection (under the skin). |
| Injection Site | Administer into the abdomen. Rotate the injection site daily to reduce the risk of injection site reactions (e.g., redness, itching). Do not inject into the navel, scar tissue, or bruised areas. |
| Preparation | The medication is supplied as a lyophilized (freeze-dried) powder and must be reconstituted (mixed) with the provided diluent (Sterile Water for Injection) immediately before use. |
| Mixing Instruction | Direct the diluent toward the sides of the vial. Roll the vial gently between the hands for about 30 seconds until the powder is completely dissolved. DO NOT SHAKE. |
| Missed Dose | If a dose is missed, take it as soon as possible. If it is almost time for the next dose, skip the missed dose and return to the regular schedule. Do not double doses. |
4. Storage and Handling
A. Unopened Vials and Diluent
| Component | Storage Condition | Instructions |
|---|---|---|
| Unopened Tesamorelin Vials | Room Temperature (20°C to 25°C or 68°F to 77°F) | Store in the original box to protect from light. Do not freeze. |
| Diluent, Syringes, Needles | Controlled Room Temperature | Store away from excessive heat and moisture. |
B. Reconstituted Solution
- Must be used IMMEDIATELY following reconstitution.
- Discard any unused solution immediately after injection.
- Do not refrigerate or freeze the reconstituted solution.
⚠️ Important Contraindications and Warnings
- Active Malignancy: Should not be used in patients with an active malignancy (cancer). Any pre-existing malignancy should be inactive and its treatment complete before initiating Tesamorelin therapy.
- Hypersensitivity: Contraindicated in patients with a known hypersensitivity to Tesamorelin or any of its components.
- Pituitary Dysfunction: Contraindicated in patients with disruption of the hypothalamic-pituitary axis due to hypophysectomy, hypopituitarism, pituitary tumor/surgery, head irradiation, or head trauma.
- Pregnancy: Contraindicated in pregnant women (Pregnancy Category X).
- Glucose Intolerance: Tesamorelin stimulates GH production, which can increase the risk of glucose intolerance or worsen pre-existing diabetes. Careful monitoring of blood glucose and HbA1c levels is required during therapy.
