SOMATULINE DEPOT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SOMATULINE DEPOT (SOMATULINE DEPOT).

How it works

Somatostatin analog; binds to somatostatin receptors (mainly SSTR2 and SSTR5) with high affinity, inhibiting the secretion of growth hormone (GH), insulin-like growth factor-1 (IGF-1), and various gastrointestinal hormones.

What the body does with it

Metabolism	Hepatic via CYP450 isoenzymes; primarily excreted unchanged in bile.
Excretion	Lanreotide is primarily excreted via the biliary-fecal route. After administration, approximately 78% of a radiolabeled dose is recovered in feces, with less than 5% excreted unchanged in urine. The remainder is metabolized and eliminated via bile.
Half-life	The terminal elimination half-life is approximately 23-29 days after subcutaneous injection of the depot formulation, supporting a monthly dosing interval.
Protein binding	88-90% bound primarily to alpha-1-acid glycoprotein (AAG), with minor binding to albumin.
Volume of Distribution	15-30 L, reflecting extensive tissue distribution. Given a typical body weight of 70 kg, this corresponds to approximately 0.21-0.43 L/kg.
Bioavailability	Subcutaneous injection: Approximately 80% (range 68-96%) relative to intravenous administration. The depot formulation provides sustained release over 28 days.
Onset of Action	Subcutaneous injection: Clinical suppression of growth hormone and IGF-1 levels is observed within 1-2 weeks after the first injection, with maximal effect by 4 weeks.
Duration of Action	Subcutaneous injection: The therapeutic effect persists for approximately 4 weeks after a single dose, consistent with the monthly dosing interval.

Classification & Brands

Dosing & administration

90 mg subcutaneously every 4 weeks for acromegaly; 120 mg subcutaneously every 4 weeks for neuroendocrine tumors (administered every 2 weeks if progression occurs). Adjust dose based on clinical response and growth hormone/IGF-1 levels.

Dosage form	SOLUTION
Renal impairment	No specific dose adjustment recommended for GFR ≥30 mL/min; for GFR <30 mL/min, use with caution and monitor for adverse effects due to limited data - consider dose reduction or interval prolongation.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose to 60 mg every 4 weeks; Child-Pugh C: not recommended (no data).
Pediatric use	Not approved for patients <18 years; safety and efficacy not established. No weight-based dosing guidelines available.
Geriatric use	No specific dose adjustment based on age alone; consider age-related renal function decline and monitor renal status; initiate at lower end of dosing range due to potential for 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 SOMATULINE DEPOT (SOMATULINE DEPOT).

Breastfeeding	No data available on presence in human milk, effects on breastfed infant, or milk production. Because many drugs are excreted in human milk and due to potential for serious adverse reactions, breastfeeding is not recommended during treatment.
Teratogenic Risk	Pregnancy Category X. Animal studies have shown embryotoxicity and teratogenicity. There is no adequate data in pregnant women; the drug is contraindicated during pregnancy due to risk of fetal harm. In first trimester, potential for major malformations; second and third trimesters may affect fetal growth and development.

Warnings & precautions

■ FDA Black Box Warning

Not applicable

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to lanreotide or any component","Concomitant use with St. John's wort"]

Clinical Precautions

Precautions

["Gallbladder abnormalities (gallstones)","Hypoglycemia/hyperglycemia","Cardiac conduction abnormalities","Pituitary apoplexy","Vitamin B12 deficiency","Thyroid function disturbances","Bradycardia"]

Clinical Tips & Counseling

Drug interactions

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SOMATULINE DEPOT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SOMATULINE DEPOT (SOMATULINE DEPOT).

How it works

What the body does with it

Metabolism	Hepatic via CYP450 isoenzymes; primarily excreted unchanged in bile.
Excretion	Lanreotide is primarily excreted via the biliary-fecal route. After administration, approximately 78% of a radiolabeled dose is recovered in feces, with less than 5% excreted unchanged in urine. The remainder is metabolized and eliminated via bile.
Half-life	The terminal elimination half-life is approximately 23-29 days after subcutaneous injection of the depot formulation, supporting a monthly dosing interval.
Protein binding	88-90% bound primarily to alpha-1-acid glycoprotein (AAG), with minor binding to albumin.
Volume of Distribution	15-30 L, reflecting extensive tissue distribution. Given a typical body weight of 70 kg, this corresponds to approximately 0.21-0.43 L/kg.
Bioavailability	Subcutaneous injection: Approximately 80% (range 68-96%) relative to intravenous administration. The depot formulation provides sustained release over 28 days.
Onset of Action	Subcutaneous injection: Clinical suppression of growth hormone and IGF-1 levels is observed within 1-2 weeks after the first injection, with maximal effect by 4 weeks.
Duration of Action	Subcutaneous injection: The therapeutic effect persists for approximately 4 weeks after a single dose, consistent with the monthly dosing interval.

Classification & Brands

Dosing & administration

Dosage form	SOLUTION
Renal impairment	No specific dose adjustment recommended for GFR ≥30 mL/min; for GFR <30 mL/min, use with caution and monitor for adverse effects due to limited data - consider dose reduction or interval prolongation.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose to 60 mg every 4 weeks; Child-Pugh C: not recommended (no data).
Pediatric use	Not approved for patients <18 years; safety and efficacy not established. No weight-based dosing guidelines available.
Geriatric use	No specific dose adjustment based on age alone; consider age-related renal function decline and monitor renal status; initiate at lower end of dosing range due to potential for 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 SOMATULINE DEPOT (SOMATULINE DEPOT).

Breastfeeding	No data available on presence in human milk, effects on breastfed infant, or milk production. Because many drugs are excreted in human milk and due to potential for serious adverse reactions, breastfeeding is not recommended during treatment.
Teratogenic Risk	Pregnancy Category X. Animal studies have shown embryotoxicity and teratogenicity. There is no adequate data in pregnant women; the drug is contraindicated during pregnancy due to risk of fetal harm. In first trimester, potential for major malformations; second and third trimesters may affect fetal growth and development.

Warnings & precautions

■ FDA Black Box Warning

Not applicable

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to lanreotide or any component","Concomitant use with St. John's wort"]

Clinical Precautions

Precautions

["Gallbladder abnormalities (gallstones)","Hypoglycemia/hyperglycemia","Cardiac conduction abnormalities","Pituitary apoplexy","Vitamin B12 deficiency","Thyroid function disturbances","Bradycardia"]

Clinical Tips & Counseling

Drug interactions

Loading safety data…