SANDOSTATIN LAR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SANDOSTATIN LAR (SANDOSTATIN LAR).
Synthetic octapeptide analog of somatostatin with greater metabolic stability and longer duration of action. Inhibits growth hormone (GH) secretion via binding to somatostatin receptors (SSTR2 and SSTR5) on pituitary somatotrophs. Also suppresses insulin-like growth factor-1 (IGF-1), glucagon, and insulin secretion. Reduces splanchnic blood flow and inhibits secretion of gastrointestinal hormones.
| Metabolism | Primarily metabolized in the liver via cytochrome P450 (CYP) enzymes, partly by CYP3A4. Approximately 32% of the dose is excreted unchanged in the urine. |
| Excretion | Renal: 32% as unchanged drug; biliary/fecal: 60-70% via feces as metabolites and unchanged drug. |
| Half-life | Terminal half-life: 12-14 days for subcutaneous octreotide LAR microspheres; clinical steady state achieved after 2-3 injections. |
| Protein binding | 65% bound primarily to albumin and to alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.2-0.4 L/kg, indicating limited extravascular distribution primarily in plasma and extracellular fluid. |
| Bioavailability | Subcutaneous: 100%; intramuscular LAR: 30% (due to slow release from microspheres). |
| Onset of Action | Subcutaneous immediate-release: 30 minutes; intramuscular LAR: gradual, therapeutic levels reached within 2 weeks. |
| Duration of Action | Subcutaneous: 6-12 hours; intramuscular LAR: 28 days (therapeutic effect maintained for 4 weeks). |
| Action Class | Somatostatin analogues |
| Brand Substitutes | Octride Depot 30mg Injection, Octride Depot 20mg Injection, Celostatin Lar 20mg Injection, Octride Depot 10mg Injection, Celostatin 10mg Injection |
Octreotide acetate 20 mg intramuscularly every 4 weeks for acromegaly; 20 mg intramuscularly every 4 weeks for neuroendocrine tumors; may initiate at 10 mg for symptom control of carcinoid syndrome and dose titrate based on response.
| Dosage form | INJECTABLE |
| Renal impairment | No formal dose adjustment recommended for renal impairment; use caution in severe renal impairment (CrCl <30 mL/min) as octreotide elimination is decreased. |
| Liver impairment | No formal dose adjustment recommended for hepatic impairment; use caution in Child-Pugh class C cirrhosis as octreotide clearance may be reduced. |
| Pediatric use | Safety and efficacy not established in pediatric patients; limited data in children with hypothalamic obesity: 5-20 mg intramuscularly every 4 weeks. |
| Geriatric use | No specific dose adjustment; start at the lower end of dosing range due to potential age-related decreased renal function and comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SANDOSTATIN LAR (SANDOSTATIN LAR).
| Breastfeeding | Octreotide is excreted in human milk; however, the M/P ratio is unknown. Caution should be exercised when administered to a nursing woman. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for Sandostatin LAR and any potential adverse effects on the breastfed infant from the drug or underlying maternal condition. |
| Teratogenic Risk | Pregnancy Category B. No evidence of teratogenicity in animal studies; however, no adequate and well-controlled studies in pregnant women. Octreotide crosses the placenta. Use only if clearly needed and potential benefit justifies potential risk to fetus. First trimester: theoretical risk of fetal growth restriction. Second/third trimesters: monitor fetal growth due to potential for decreased placental blood flow. |
■ FDA Black Box Warning
Not approved for treatment of carcinoid syndrome or VIPomas unless patient is intolerant or unresponsive to octreotide immediate-release. Cholelithiasis and complications of gallstones may occur. Do not administer intravenously or intra-arterially.
| Serious Effects |
["Hypersensitivity to octreotide or any component","Do not use for rapid control of acute symptoms (use immediate-release octreotide)"]
| Precautions | ["Gallbladder abnormalities: cholelithiasis, sludge, cholecystitis","Hypoglycemia or hyperglycemia due to altered insulin/glucagon secretion","Bradycardia, conduction abnormalities","Thyroid function monitoring (suppressed TSH)","Vitamin B12 deficiency","Withdrawal syndrome: severe GH rebound in acromegaly","Immunogenicity: antibodies may develop (rarely neutralizing)"] |
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| Fetal Monitoring | Monitor maternal blood glucose levels (octreotide may cause hypoglycemia or hyperglycemia). In pregnant women, assess fetal growth via ultrasound due to potential for intrauterine growth restriction. Monitor thyroid function (octreotide may suppress TSH). Check gallbladder ultrasound if symptoms of cholelithiasis occur. Monitor maternal heart rate and ECG in those with cardiac risk. |
| Fertility Effects | Octreotide may suppress growth hormone and IGF-1, potentially affecting ovulation and spermatogenesis. In acromegaly, improved fertility may occur with disease control. Reversible inhibition of gonadotropin secretion may occur. Animal studies showed no impairment of fertility at clinically relevant doses. |