Tesamorelin (Egrifta) - Treats HIV associated 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 Adults

Dose in the treatment of HIV-associated lipodystrophy:

  • 2 mg subQ once a day.

Tesamorelin Dose in Children

Not recommended in children

Pregnancy Risk factor: X

  • It is contraindicated in pregnant females.
  • Due to hormonal and metabolic changes, pregnancy causes an increase in the deposition of visceral fat tissue.
  • Tesamorelin reduces visceral adipose tissues deposition, which could potentially cause harm to the unborn foetus.
  • Treatment should be stopped if pregnancy occurs during treatment.

Tesamorelin use during breastfeeding:

  • It is unknown if the drug can be absorbed into breast milk.
  • HIV-positive women should not breastfeed to reduce the risk of contracting the virus.

Tesamorelin Dose in Renal Disease:

  • It has not been studied in patients with renal disease.
  • The manufacturer has not recommended any dose adjustment in patients with renal impairment.

Tesamorelin dose in Liver Disease:

  • It has not been studied in patients with liver disease.
  • The manufacturer has not recommended any dose adjustment in patients with liver disease.

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:

  • Allergy to tesamorelin and any component of the formulation
  • Disruption of the hypothalamic-pituitary-axis due to hypophysectomy, hypopituitarism, head irradiation, pituitary tumor or surgery, or head trauma
  • Active malignancy
  • Pregnancy.

Warnings and precautions

  • Hypersensitivity reactions
    • Allergy reactions can include pruritus and flushing, erythema and urticaria.
    • If you suspect an allergic reaction, it is best to stop treatment immediately and seek medical attention.
  • Fluid retention:
    • Treatment may cause temporary body swelling or peripheral oedema, which may disappear upon discontinuation.
  • Injection-site reactions:
    • There may be reactions at the injection site such as erythema and pain, pruritus or irritation.
    • Rotating the injection site can help to avoid local reactions.
  • Diabetes:
    • Growth hormones may increase the risk of diabetes and glucose intolerance.
    • Before starting therapy, it is important to monitor blood glucose levels.
    • Patients with diabetes who have been prescribed growth hormone must be closely monitored for any signs or symptoms that might indicate a worsening or new-onset of retinopathy.
  • Malignancy
    • A persistent elevation in IGF-1 and growth hormone levels may increase the likelihood of developing or reactivating malignancies.
    • Patients suffering from active malignancies should not use growth hormones.
    • During treatment, IGF-1 levels must be closely monitored
    • Patients with elevated IGF-1 levels should stop taking therapy.
    • Any evidence of recurrent malignancy should be stopped.
  • Acute critical illness
    • Because of the higher mortality rates, patients with acute critical illness, such as those who have had open-heart surgery, trauma or abdominal surgery, should not take growth hormones.
    • Critically ill patients should not be treated.

Tesamorelin: Drug Interaction

Risk Factor D (Consider therapy modification)

Cortisone

Tesamorelin may decrease serum concentrations of the active metabolite(s) of Cortisone.

PredniSONE

Tesamorelin may decrease serum concentrations of the active metabolite(s) of PredniSONE.

Risk Factor X (Avoid combination)

Macimorelin

Growth Hormone Products may diminish the diagnostic effect of Macimorelin.

Monitor:

  • Serum IGF-1 levels at baseline and during therapy ( The risk of malignancy is potentially increased in patients with sustained elevation of IGF-1 levels).
  • Serum glucose before initiating therapy. Treatment for diabetes may need adjustment.
  • Monitor blood sugars periodically and retinopathy in patients with diabetes.
  • Monitor visceral adipose tissue (by measuring waist circumference).
  • Monitor the patient for fluid retention.

How to administer Tesamorelin?

  • It is administered SubQ preferably in the abdomen. The injection site should be rotated.
  • It should not be injected into scar tissues, bruises, or the navel.

Mechanism of action of Tesamorelin:

It stimulates endogenous growth hormone secretion by binding to pituitary hormone-releasing factor receptors. It acts as an anabolic agent and a lipolytic. IGF-1 is produced in the liver and peripheral tissues by growth hormone. IGF-1 binding to osteoblasts, myocytes and hepatocytes leads to a reduction in total fat.

After the bioavailabilitySubQ administration in healthy adults is lower than 4% Half-life elimination for HIV-infected people, it takes 38 minutes to get healthy adults and 26 minutes for HIV-infected individuals. The peak effect time is observed in9 minutes    

International Brands of Tesamorelin:

  • Egrifta

Tesamorelin Brands in Pakistan:

No brands available in Pakistan.