SANDOSTATIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SANDOSTATIN (SANDOSTATIN).

How it works

Synthetic octapeptide analog of somatostatin with longer half-life. Inhibits growth hormone (GH), glucagon, and insulin secretion. Reduces splanchnic blood flow and suppresses serotonin release from neuroendocrine tumors.

What the body does with it

Metabolism	Metabolized by peptidases; not extensively hepatic; 32% excreted unchanged in urine; metabolites inactive; half-life ~1.7 hours.
Excretion	Renal: ~32% unchanged; biliary/fecal: ~66% as metabolites; total clearance ~160 mL/min.
Half-life	Terminal elimination half-life: 1.7–1.9 hours (subcutaneous); prolonged in hepatic impairment (up to 2.6 h). After intravenous bolus, biphasic elimination with t½ α ~0.2 h and t½ β ~1.5 h.
Protein binding	~65% bound primarily to alpha-1 acid glycoprotein and, to a lesser extent, albumin.
Volume of Distribution	Apparent Vd: 0.2–0.4 L/kg (total, ~30 L). Indicates distribution mainly into extracellular fluid with limited tissue binding.
Bioavailability	Subcutaneous: ~100% (almost complete); intramuscular (long-acting): slow release with absolute bioavailability ~50% of total dose delivered over 4 weeks; intravenous: 100%.
Onset of Action	Subcutaneous: acromegaly symptom improvement and GH suppression within 1–2 hours; intravenous: immediate; intramuscular (long-acting depot): reaches therapeutic levels after 2–3 weeks.
Duration of Action	Subcutaneous: GH suppression lasts 6–8 hours; intravenous: 4–6 hours; intramuscular (depot): 4 weeks (for acromegaly, repeat injection every 4 weeks).

Classification & Brands

Dosing & administration

Subcutaneous: 50-100 mcg every 8-12 hours. Intravenous bolus: 50 mcg, then continuous infusion 25-100 mcg/hour for acute variceal bleeding.

Dosage form	INJECTABLE
Renal impairment	No adjustment required for mild to moderate impairment. For severe renal impairment (GFR < 30 mL/min), reduce dose by 50% and monitor for toxicity.
Liver impairment	No specific Child-Pugh based guidelines. Caution in severe hepatic impairment; monitor liver function and adjust dose based on response.
Pediatric use	0.5-1 mcg/kg subcutaneously every 8-12 hours. Maximum 50 mcg per dose. For continuous IV infusion, 0.5-1 mcg/kg/hour.
Geriatric use	No specific dose adjustment required. Use lower end of dosing range due to potential age-related renal impairment and increased sensitivity.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for SANDOSTATIN (SANDOSTATIN).

Breastfeeding	Unknown if excreted in human milk. M/P ratio not available. Caution advised due to potential for growth inhibition in nursing infant. Consider alternative if possible.
Teratogenic Risk	Pregnancy Category B. No evidence of teratogenicity in animal studies; limited human data. Use only if clearly needed. Risks in first trimester: unlikely but unknown. Second/third trimester: potential for fetal growth restriction due to maternal vasoconstriction, though not reported. Advise caution.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to octreotide or any component of the formulation","Not for use in patients with severe hepatic impairment (Child-Pugh C) due to lack of data"]

Clinical Precautions

Precautions

["Gallbladder abnormalities (biliary sludge, cholelithiasis) due to inhibition of gallbladder contraction and bile secretion","Hyperglycemia or hypoglycemia due to altered glucose metabolism","Bradycardia, conduction abnormalities (monitor ECG)","Hypothyroidism (suppression of TSH)","Intestinal obstruction (rare, due to mesenteric fibrosis in carcinoid patients)"]

Clinical Tips & Counseling

Drug interactions

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SANDOSTATIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SANDOSTATIN (SANDOSTATIN).

How it works

What the body does with it

Metabolism	Metabolized by peptidases; not extensively hepatic; 32% excreted unchanged in urine; metabolites inactive; half-life ~1.7 hours.
Excretion	Renal: ~32% unchanged; biliary/fecal: ~66% as metabolites; total clearance ~160 mL/min.
Half-life	Terminal elimination half-life: 1.7–1.9 hours (subcutaneous); prolonged in hepatic impairment (up to 2.6 h). After intravenous bolus, biphasic elimination with t½ α ~0.2 h and t½ β ~1.5 h.
Protein binding	~65% bound primarily to alpha-1 acid glycoprotein and, to a lesser extent, albumin.
Volume of Distribution	Apparent Vd: 0.2–0.4 L/kg (total, ~30 L). Indicates distribution mainly into extracellular fluid with limited tissue binding.
Bioavailability	Subcutaneous: ~100% (almost complete); intramuscular (long-acting): slow release with absolute bioavailability ~50% of total dose delivered over 4 weeks; intravenous: 100%.
Onset of Action	Subcutaneous: acromegaly symptom improvement and GH suppression within 1–2 hours; intravenous: immediate; intramuscular (long-acting depot): reaches therapeutic levels after 2–3 weeks.
Duration of Action	Subcutaneous: GH suppression lasts 6–8 hours; intravenous: 4–6 hours; intramuscular (depot): 4 weeks (for acromegaly, repeat injection every 4 weeks).

Classification & Brands

Dosing & administration

Subcutaneous: 50-100 mcg every 8-12 hours. Intravenous bolus: 50 mcg, then continuous infusion 25-100 mcg/hour for acute variceal bleeding.

Dosage form	INJECTABLE
Renal impairment	No adjustment required for mild to moderate impairment. For severe renal impairment (GFR < 30 mL/min), reduce dose by 50% and monitor for toxicity.
Liver impairment	No specific Child-Pugh based guidelines. Caution in severe hepatic impairment; monitor liver function and adjust dose based on response.
Pediatric use	0.5-1 mcg/kg subcutaneously every 8-12 hours. Maximum 50 mcg per dose. For continuous IV infusion, 0.5-1 mcg/kg/hour.
Geriatric use	No specific dose adjustment required. Use lower end of dosing range due to potential age-related renal impairment and increased sensitivity.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for SANDOSTATIN (SANDOSTATIN).

Breastfeeding	Unknown if excreted in human milk. M/P ratio not available. Caution advised due to potential for growth inhibition in nursing infant. Consider alternative if possible.
Teratogenic Risk	Pregnancy Category B. No evidence of teratogenicity in animal studies; limited human data. Use only if clearly needed. Risks in first trimester: unlikely but unknown. Second/third trimester: potential for fetal growth restriction due to maternal vasoconstriction, though not reported. Advise caution.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to octreotide or any component of the formulation","Not for use in patients with severe hepatic impairment (Child-Pugh C) due to lack of data"]