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SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES › ANTERIOR PITUITARY LOBE HORMONES AND ANALOGUES › Other anterior pituitary lobe hormones and analogues
pegvisomant
H01AX01
Forms & Strengths
- Lyophilized powder for reconstitution: 10 mg, 15 mg, 20 mg, 25 mg, and 30 mg single-dose vials
Adult Dosing
- Acromegaly: Loading dose of 40 mg subcutaneously under healthcare provider supervision
- Acromegaly maintenance: 10 mg to 30 mg subcutaneously once daily
- Dose adjustments in 5 mg increments based on serum IGF-I concentrations every 4-6 weeks
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of acromegaly in patients who have had an inadequate response to surgery or radiation, or for whom these therapies are not appropriate
Mechanism of Action
- Highly selective growth hormone (GH) receptor antagonist
- Binds to GH receptors on cell surfaces, blocking the binding of endogenous GH and inhibiting downstream intracellular signaling, leading to decreased serum IGF-I concentrations
Contraindications
- Known hypersensitivity to pegvisomant or any of its excipients
Adverse Reactions
- Injection site reactions (pain, erythema, lipohypertrophy)
- Elevated liver transaminases (ALT, AST)
- Flu-like syndrome, fatigue, nausea, diarrhea
- Lipohypertrophy at injection sites
- Potential increase in pituitary tumor size (requires periodic MRI monitoring)
Drug Interactions
- Insulin and oral hypoglycemic agents: May require dose reduction due to improved insulin sensitivity
- Opioid analgesics: May require higher doses of opioids to achieve pain control due to decreased GH/IGF-I signaling
- Hepatotoxic drugs: Concurrent use may increase the risk of liver enzyme elevations
Curated Content: Needs Vetting Before Put to Clinical Use