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SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES › HYPOTHALAMIC HORMONES › Somatostatin and analogues
vapreotide
H01CB04
Forms & Strengths
- Injectable solution: 50 mcg/mL, 100 mcg/mL, 250 mcg/mL
Adult Dosing
- Esophageal variceal bleeding: 50 mcg IV bolus followed by 50 mcg/hour continuous IV infusion for up to 5 days
- Carcinoid syndrome and VIPomas: 50 to 100 mcg subcutaneously every 8 to 12 hours, titrated based on clinical response
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Management of acute bleeding from esophageal varices in cirrhosis
- Symptomatic treatment of neuroendocrine tumors such as carcinoid tumors and vasoactive intestinal peptide-secreting tumors (VIPomas)
Mechanism of Action
- Synthetic cyclic octapeptide analogue of natural somatostatin
- Binds to somatostatin receptors (SSTR subtypes 2 and 5) with high affinity
- Inhibits the release of growth hormone, serotonin, gastrin, vasoactive intestinal peptide, insulin, and glucagon
- Reduces splanchnic blood flow and portal venous pressure, decreasing variceal hemorrhage
Contraindications
- Known hypersensitivity to vapreotide or any component of the formulation
- Pregnancy and lactation due to potential risks of hormonal disruption
Adverse Reactions
- Cardiovascular: Bradycardia, flushing, transient hypotension or hypertension
- Gastrointestinal: Abdominal pain, nausea, diarrhea, steatorrhea, flatulence
- Metabolic: Hyperglycemia or hypoglycemia due to altered insulin and glucagon regulation
- Local: Pain, erythema, or burning sensation at the subcutaneous injection site
Drug Interactions
- Insulin and oral hypoglycemic agents: May require dose adjustment due to altered glucose homeostasis
- Beta-blockers and calcium channel blockers: Potential for additive bradycardia or blood pressure reduction
- Cyclosporine: Vapreotide may decrease serum concentration and absorption of cyclosporine
- Drugs metabolized by cytochrome P450 enzymes: Potential indirect effects through altered endocrine regulation
Curated Content: Needs Vetting Before Put to Clinical Use