Tesamorelin is a synthetic peptide analogue of the growth hormone-releasing hormone (GHRH). It's primarily used as a treatment for HIV-associated lipodystrophy, a condition characterized by abnormal distribution of body fat.

Tesamorelin works by stimulating the pituitary gland to produce and release growth hormone. By increasing growth hormone levels, tesamorelin helps to reduce visceral adipose tissue (fat around the organs) in HIV-infected patients with lipodystrophy.

Tesamorelin stimulates the secretion of endogenous growth hormone by binding to pituitary growth hormone-releasing factor receptors. It thus acts as a lipolytic and has anabolic properties.

It is indicated in patients with HIV-associated lipodystrophy for the Reduction of excess abdominal fat.

Tesamorelin Dose in Adult

Tesamorelin Dose in the treatment of HIV-associated lipodystrophy:  

• Tesamorelin is usually given as a 2 mg shot under the skin once every day.
• This helps reduce the abnormal fat distribution that can happen with HIV infection.

Tesamorelin Dose in Children

Not recommended in children

Pregnancy Risk factor: X

• If someone is pregnant, they shouldn't use tesamorelin because it can be harmful to the baby.
• When a person is pregnant, their body naturally stores more fat around their organs, and tesamorelin works to reduce this fat.
• But if someone takes it while pregnant, it might hurt the developing baby.
• If someone becomes pregnant while using tesamorelin, they should stop using it right away.

Tesamorelin use during breastfeeding:

• We're not sure if tesamorelin is found in breast milk, so it's best for women with HIV to avoid breastfeeding entirely.
• This helps lower the risk of passing HIV to their baby. It's a recommendation from the
• Department of Health and Human Services to prevent HIV transmission from mother to child.

Tesamorelin Dose in Renal Disease:

• The manufacturer's instructions don't include any adjustments to the dosage of tesamorelin for people with kidney problems because it hasn't been studied yet in those individuals.

Tesamorelin dose in Liver Disease:

• The manufacturer's instructions for tesamorelin don't offer any changes to the dosage for people with liver issues because it hasn't been studied in those cases.

Beyond 26 weeks, the incidence of adverse reactions generally decreases with continued treatment.

Common Side Effects of Tesamorelin Include:

• Immunologic:
  • Antibody development
• Local:
  • Injection site reaction
• Neuromuscular & skeletal:
  • Arthralgia

Less Common Side Effects of Tesamorelin Include:

• Cardiovascular:
  • Peripheral Edema
  • Chest Pain
  • Flushing
  • Hypertension
  • Palpitations
• Central Nervous System:
  • Paresthesia
  • Hypoesthesia
  • Carpal Tunnel Syndrome
  • Depression
  • Pain
  • Insomnia
• Dermatologic:
  • Injection Site Pruritus
  • Skin Rash
  • Urticaria At Injection Site
  • Pruritus
  • Night Sweats
  • Rash At Injection Site
  • Urticaria
• Gastrointestinal:
  • Vomiting
  • Dyspepsia
  • Abdominal Pain
• Hematologic & Oncologic:
  • Elevated Glycosylated Hemoglobin
  • Local Hemorrhage
• Hypersensitivity:
  • Hypersensitivity Reaction
• Local:
  • Erythema At Injection Site
  • Pain At Injection Site
  • Irritation At Injection Site
  • Swelling At Injection Site
• Neuromuscular & Skeletal:
  • Limb Pain
  • Myalgia
  • Increased Creatine Phosphokinase In Blood Specimen
  • Muscle Rigidity
  • Musculoskeletal Pain
  • Joint Stiffness
  • Joint Swelling
  • Muscle Spasm
  • Muscle Strain

Contraindications to Tesamorelin Include:

• People should avoid using tesamorelin if they're allergic to it or any of its ingredients, or if they have conditions like hypophysectomy, hypopituitarism, pituitary tumor/surgery, head irradiation, or head trauma that can disrupt the hypothalamic-pituitary axis.
• Active malignancy and pregnancy are also contraindications for its use.

Warnings and precautions

Hypersensitivity reactions

• Some people might have hypersensitivity reactions to tesamorelin, showing symptoms like itching, redness, flushing, hives, or a rash.
• If someone experiences signs of hypersensitivity, it's important to stop using tesamorelin and advise them to seek medical help right away.

Fluid retention:

• Taking tesamorelin might lead to fluid retention, which can show up as swelling in the arms, legs, or other body parts.
• This can make the skin feel tight and cause discomfort in muscles and bones.
• Sometimes, this swelling might go away on its own or when the treatment is stopped.

Injection-site reactions:

• Some people might experience reactions at the injection site when using tesamorelin, like redness, itching, pain, irritation, or bruising.
• Rotating where the injection is given on different parts of the abdomen can help lower the chance of these reactions happening.

Diabetes:

• Using tesamorelin could raise the risk of developing diabetes because it might lead to problems with glucose tolerance.
• Before starting treatment, it's important to check a person's glucose levels and keep an eye on them regularly for any changes in how their body handles glucose.
• For people who already have diabetes, it's crucial to watch out for any signs of diabetic retinopathy getting worse because tesamorelin can increase levels of IGF-1, which might affect the eyes.

Malignancy

• The release of natural growth hormone and the rise in IGF-1 levels due to tesamorelin might increase the chance of developing new cancers or existing ones returning.
• People with active cancers shouldn't use tesamorelin, and treatment should only begin once any prior cancer treatment is finished.
• Throughout treatment, it's crucial to keep an eye on IGF-1 levels, and if they stay high, it might be necessary to stop the treatment.
• If there's any sign of cancer coming back, tesamorelin should be stopped immediately.

Acute critical illness

• In cases of acute critical illness, using growth hormone like tesamorelin might raise the risk of death, especially after surgeries like open-heart or abdominal surgery, trauma, or acute respiratory failure.
• It's worth thinking about stopping tesamorelin treatment for patients who are critically ill.

Tesamorelin: Drug Interaction

Monitor:

• Serum IGF-1 Levels: Keep an eye on IGF-1 levels before starting tesamorelin and during treatment. Elevated IGF-1 levels might increase the risk of cancer, so it's important to watch for this.
• Serum Glucose: Check glucose levels before starting treatment and regularly afterward. Tesamorelin might affect how the body handles glucose, which can lead to changes in metabolism.
• Retinopathy: Patients with diabetes should be monitored for any changes in retinopathy, especially since tesamorelin can raise IGF-1 levels, which might affect the eyes.
• Visceral Adipose Tissue: Measure visceral fat using waist circumference or CT scans to monitor how tesamorelin is working.
• Fluid Retention: Keep an eye out for signs of fluid retention, like swelling, while using tesamorelin.

How to administer Tesamorelin?

Subcutaneous Injection Site Guidelines

• Preferred Site: Inject tesamorelin into the abdomen, as it's the preferred location for administration.
• Rotate Injection Site: Rotate the injection site within the abdomen to prevent irritation or discomfort.
• Avoid Scar Tissue, Bruises, or Navel: Do not inject into areas with scar tissue, bruises, or the navel, as this can cause pain or complications.

Mechanism of action of Tesamorelin:

• Tesamorelin works by binding to receptors called pituitary growth hormone-releasing factor (GRF) receptors.
• This binding prompts the release of natural growth hormone in the body.
• Growth hormone has two main effects: it helps build tissues (anabolic effect) and it breaks down fats (lipolytic effect).
• Growth hormone interacts with specific receptors on different types of cells, like bone-building cells (osteoblasts), muscle cells (myocytes), liver cells (hepatocytes), and fat cells (adipocytes).
• This interaction triggers a reduction in overall fat mass.
• The main player in these effects is a substance called IGF-1, which is produced in the liver and in various tissues throughout the body.

Distribution:

• In healthy adults, the volume of distribution (V) is approximately 9.4 liters per kilogram (L/kg), with some variability. In HIV-infected patients, this volume is slightly higher, around 10.5 L/kg.

Bioavailability:

• When tesamorelin is given as a subcutaneous injection (SubQ), less than 4% of the dose is absorbed into the bloodstream in healthy adults.

Half-life Elimination:

• The half-life of tesamorelin, which is the time it takes for half of the drug to be eliminated from the body, is around 26 minutes in healthy adults. In HIV-infected patients, this half-life is slightly longer, approximately 38 minutes.

Time to Peak:

• Tesamorelin reaches its peak concentration in the bloodstream around 9 minutes after administration.

International Brands of Tesamorelin:

• Egrifta

Tesamorelin Brands in Pakistan:

No brands available in Pakistan.