TesamorelinPA study guide

Why they happen and how to manage them

Edema, arthralgia, carpal tunnel syndrome

Growth hormone causes sodium and water retention and increases tissue turgor. Management: Usually transient; resolves on stopping. Ask about swelling and hand numbness.

Hyperglycemia and new diabetes

Growth hormone opposes insulin action in liver, muscle, and fat. Management: Check glucose before and during treatment and adjust diabetes medicines; reconsider therapy if there is no fat response.

Tumor growth or recurrence

Growth hormone and IGF-1 are growth factors for many tissues. Management: Screen the cancer history before starting and stop for any recurrence.

Injection site reactions

Local irritation from a daily peptide injection. Management: Rotate sites across the abdomen.

Hypersensitivity

Immune response to a synthetic peptide. Management: Stop at the first sign of rash, hives, or flushing.

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Common and serious

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Narrow therapeutic index

The label does not describe a narrow therapeutic index or direct dosing by measured blood levels of the drug.

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Blood glucose

Why

Glucose intolerance or diabetes

When

Before starting and periodically during treatment

Act on

Consider stopping if glucose intolerance or diabetes develops without a clear fat response

Normal

Fasting 70 to 99 mg/dL.

Sources: [1][2]

Hemoglobin A1c

Why

Development of diabetes, defined in trials as an A1c of 6.5% or higher

When

Periodically during treatment

Normal

Below 5.7% is normal and 6.5% or higher indicates diabetes. Many people with diabetes aim for below 7%.

Sources: [1][2]

IGF-1 (insulin-like growth factor 1)

Why

Growth hormone response and overexposure

When

During therapy

Act on

Consider stopping for persistent elevation above 3 SDS, especially without a clear fat response

Sources: [1]

Adult dose

Egrifta SV (2 mg vial)

1.4 mg (0.35 mL of reconstituted solution) subcutaneously once daily into the abdomen.

Egrifta WR (11.6 mg vial)

1.28 mg (0.16 mL of reconstituted solution) subcutaneously once daily; one reconstituted vial provides 7 daily doses.

Sources: [1][2]

Renal adjustment

Not studied. Pharmacokinetics in renal impairment have not been established.

Sources: [1]

Hepatic adjustment

Not studied. Pharmacokinetics in hepatic impairment have not been established.

Sources: [1]

Boxed warning

None. The Egrifta labels carry no boxed warning.

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Contraindications

• Disruption of the hypothalamic-pituitary axis (hypophysectomy, hypopituitarism, pituitary tumor or surgery, head irradiation, head trauma)
• Active malignancy
• Known hypersensitivity to tesamorelin or excipients
• Pregnancy

Sources: [1]

Key interactions

Drugs metabolized by CYP450 enzymes (corticosteroids, sex steroids, anticonvulsants, cyclosporine)

Growth hormone may change their clearance; monitor for interactions. Simvastatin and ritonavir exposure changed little in studies.

Glucocorticoid replacement for adrenal insufficiency

Growth hormone blocks the enzyme that activates cortisone and prednisone, so maintenance or stress doses may need to rise.

Sources: [1][2]

Antidote or reversal

No specific antidote, and the label has no overdosage section. Stop the drug and give supportive care.

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Pregnancy

Contraindicated. Modifying visceral fat offers no benefit in pregnancy, and rats exposed during organogenesis had offspring with hydrocephaly at about 2 and 4 times the clinical exposure. Stop the drug if pregnancy occurs.

Sources: [1][2]

Lactation

Mothers with HIV in the United States are advised not to breastfeed, and there are no data on tesamorelin in human milk. Do not breastfeed while using it.

Sources: [1]

Pediatric

Not established. In children with open growth plates it could accelerate linear growth, and it is not indicated for children with open or closed epiphyses.

Sources: [1]

Geriatric

No information on use in patients over 65.

Sources: [1]