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Tesamorelin – Effects, Uses & Side Effects

Tesamorelin is a synthetic analogue of growth hormone-releasing hormone (GHRH) used to treat HIV-associated lipodystrophy in adults.

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Things worth knowing about "Tesamorelin"

Tesamorelin is a synthetic analogue of growth hormone-releasing hormone (GHRH) used to treat HIV-associated lipodystrophy in adults.

What is Tesamorelin?

Tesamorelin is a synthetically produced peptide hormone that closely resembles the naturally occurring human growth hormone-releasing hormone (GHRH). It consists of 44 amino acids and is administered as a subcutaneous injection. In clinical medicine, tesamorelin is marketed under the brand name Egrifta.

Indication

Tesamorelin is approved for the treatment of HIV-associated lipodystrophy in adults. This condition is a metabolic complication frequently observed in HIV-positive patients receiving antiretroviral therapy, characterized by unwanted accumulation of visceral adipose tissue (abdominal fat). Tesamorelin is specifically indicated to reduce this excess visceral fat.

Mechanism of Action

Tesamorelin binds to GHRH receptors in the anterior pituitary gland, stimulating the release of growth hormone (GH). The released growth hormone promotes lipolysis, the breakdown of fat tissue, particularly in the abdominal region. Unlike direct administration of growth hormone, tesamorelin mimics the physiological mechanism of growth hormone secretion, supporting a more natural regulation of growth hormone levels.

Dosage and Administration

The recommended dose is 2 mg of tesamorelin administered once daily as a subcutaneous injection into the abdominal area. Injections should ideally be given at the same time each day. Patients may self-administer the injection after appropriate training. Regular medical monitoring is required throughout treatment.

Side Effects

Like all medications, tesamorelin can cause side effects. Commonly reported side effects include:

Injection site reactions (redness, swelling, pain)
Joint pain (arthralgia)
Fluid retention (peripheral edema)
Carpal tunnel syndrome
Elevated blood glucose levels (hyperglycemia)
Nausea and gastrointestinal discomfort

Patients with diabetes or pre-diabetes should be closely monitored, as tesamorelin may influence insulin resistance.

Contraindications

Tesamorelin must not be used in patients with:

Hypersensitivity to the active substance or any of the excipients
Active malignancies (cancerous tumors)
Pituitary diseases or pituitary tumors
Pregnancy or breastfeeding
Individuals under 18 years of age

Drug Interactions

Tesamorelin may interact with several medications. Particular caution is advised with:

Corticosteroids: These may reduce the effectiveness of tesamorelin.
Insulin sensitizers and antidiabetic agents: Dose adjustments may be necessary.
Antiretroviral medications: Interactions may influence the metabolism of tesamorelin.

Clinical Context and Evidence

In clinical trials, tesamorelin demonstrated a significant reduction in visceral adipose tissue in HIV-infected patients with lipodystrophy. Treatment not only improved cosmetic aspects but also metabolic parameters such as triglyceride levels. However, the effect is sustained only with continued therapy; visceral fat may return after discontinuation of treatment.

References

Falutz J et al. - Metabolic effects of a growth hormone-releasing factor in patients with HIV. N Engl J Med. 2007;357(23):2359-2370.
European Medicines Agency (EMA) - Egrifta (Tesamorelin) Product Information, 2015.
Grinspoon SK, Carr A. - Cardiovascular risk and body-fat abnormalities in HIV-infected adults. N Engl J Med. 2005;352(1):48-62.

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