Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 0.05mg/mL
- 0.1mg/mL
- 0.2mg/mL
- 0.5mg/mL
- 1mg/mL
depot injection
- 10mg/kit
- 20mg/kit
- 30mg/kit
injectable solution
- 2500mcg/mL (single-patient-use pen)
Acromegaly
Indicated to reduce blood levels of growth hormone (GH) and insulin-like growth factor 1 (IGF-1) [somatomedin C] in adults with acromegaly who have had inadequate response to or cannot be treated with surgical resection, pituitary irradiation, and bromocriptine mesylate at maximally tolerated doses
Solution: 50 mcg SC q8hr initially; titrate up to 500 mcg SC q8hr if necessary; after successful treatment with solution for 2 weeks, initiate treatment with suspension (depot injection)
Suspension (depot IM injection)
-
Patients not currently receiving octreotide
- Begin therapy with solution as listed above
- Maintain on SC solution for at least 2 weeks to determine tolerance to octreotide
- Patients who responds to the drug, based on GH and IGF-1 levels and who tolerate the drug, then switch to octreotide suspension
-
Patients currently receiving octreotide
- Switch to octreotide suspension 20 mg IM (gluteal) q4Weeks for 3 months; titrate up or down to 10-30 mg IM q4Weeks, depending on response; not to exceed 40 mg
- After 3 months, dosage may be adjusted as follows:
- GH ≤2.5 ng/mL, IGF-1 normal, and clinical symptoms controlled: Maintain octreotide suspension at 20 mg q4Weeks
- GH >2.5 ng/mL, IGF-1 elevated, and/or clinical symptoms uncontrolled: Increase octreotide suspension to 30 mg q4Weeks
- GH ≤1 ng/mL, IGF-1 normal, and clinical symptoms controlled: Reduce octreotide suspension to 10 mg q4Weeks
- If GH, IGF-1, or symptoms are not adequately controlled at a dose of 30 mg, the dose may be increased to 40 mg q4Weeks
- In patients who have received pituitary irradiation, withdraw yearly for ~8 weeks to assess disease activity; if GH or IGF-1 levels increase and signs and symptoms recur, resume therapy
Dosing Considerations
- Monitor IGF-1 levels q2Weeks to guide titration; goal: GH levels <5 ng/mL or IGF-1 levels <1.9 units/mL (men) and <2.2 units/mL (women)
- Monitor IGF-1 or GH levels every 6 months
- Withdraw drug yearly for 4 weeks (solution) or 8 weeks (suspension) from patients who have undergone irradiation to assess
Carcinoid Tumor
Solution: 100-600 mcg/day SC divided q6-12hr; may titrate to 1500 mcg/day; after successful treatment with solution for 2 weeks, initiate treatment with suspension (depot injection)
Suspension (depot IM injection): 20 mg IM q4Weeks for 2 months then modify dose based on response; may increase to 30mg q4Weeks if symptoms are inadequately controlled; decrease to 10 mg IM q4Weeks for trial period if initially responsive to 20 mg dose; dose >30 mg not recommended
VIPoma
Solution: 200-300 mcg/day SC divided q6-12hr; after successful treatment with solution for 2 weeks, initiate treatment with suspension (depot injection)
Suspension (depot IM injection): Patients must be stabilized on subcutaneous octreotide for at least 2 weeks before switching to long-acting depot; upon switch, administer 20 mg IM intragluteally every 4 weeks for 2 months; continue solution for first 2 weeks; titrate suspension up or down to 10-30 mg IM q4Weeks
Esophageal Variceal Bleeding (Off-label)
Solution: 25-100 mcg IV bolus (usual bolus dose: 50 mcg); follow by continuous IV infusion of 25-50 mcg/hr for 2-5 days; may repeat bolus in first hr if hemorrhage not controlled
GI or Pancreatic Fistula (Off-label)
Solution: 50-200 mcg SC q8hr for 2-12 days
AIDS-Related Diarrhea (Off-label)
Solution: 100-500 mcg SC q8hr
Ileostomy-Related Diarrhea (Off-label)
Solution: 25 mcg/hr IV or 50 mcg SC q12hr
Chemotherapy-Related Diarrhea (Off-label)
Low-grade or uncomplicated: Solution: 100-150 mcg SC q8hr for 1-30 days
Complicated: Solution: 100-150 mcg SC q8hr or 25-50 mcg/hr IV; may increase to 500 mcg q8hr until controlled
Severe: Solution: 100-150 mcg SC q8hr; may increase to 500-1500 mcg SC/IV q8hr
Dumping Syndrome (Off-label)
Solution: 50-150 mcg/day IV; may adjust to 25-600 mcg/day dose range
Suspension (depot injection): 10-20 mg/month IM
Chylothorax (Off-label)
Solution: 50-100 mcg SC q8hr
Dosage Modifications
Renal impairment
-
Solution and suspension
- Mild-to-severe without dialysis: No dosage adjustment necessary
- With dialysis: 10 mg IM q4Weeks initially, then titrate to effect
-
Autoinjector pen
- Patients on dialysis: Half-life of octreotide may increase, may require dosage adjustment on maintenance dose
Hepatic impairment
- Cirrhosis: 10 mg IM q4Weeks initially, then titrate to effect
Neuroendocrine Tumors (Orphan)
Orphan indication sponsor
- Novartis Pharmaceuticals Corporation, One Health Plaza, East Hanover, NJ 07936-1080
Dosage Forms & Strengths
injectable solution
- 0.05mg/mL
- 0.1mg/mL
- 0.2mg/mL
- 0.5mg/mL
- 1mg/mL
Safety and efficacy not established
GI Bleeding (Off-label)
1 mcg/kg bolus, then 1 mcg/kg/hr infusion; taper by 50% when no active bleeding for 24 hours
Diarrhea (Off-label)
Chylothorax (Off-label)
0.3-4 mcg/kg/hr SC/IV, depending on nature of chylothorax
Hyperinsulinemia/Hypoglycemia of Infancy (Off-label)
2-10 mcg/kg/day SC/IV divided q12hr; increase on basis of response
Sulfonylurea Overdose (Off-label)
1 mcg/kg SC/IV q12hr OR 25 mcg once; monitor blood glucose concentrations
Acromegaly
Solution: 50 mcg SC q8-12hr initially; titrate up to 500 mcg SC q8hr if necessary; after successful treatment with solution for 2 weeks, initiate treatment with suspension (depot injection)
Suspension (depot injection): 20 mg IM intragluteally every 4 weeks for 3 months; titrate up or down to 10-30 mg IM every 4 weeks, depending on response; not to exceed 40 mg
Dosing Considerations
Dose adjustment may be necessary; clearance may decrease by 26% and half-life by 46%
Monitor IGF-1 levels every 2 weeks to guide titration; goal: GH levels <5 ng/mL or IGF-1 levels <1.9 units/mL (men) and <2.2 units/mL (women)
Monitor IGF-1 or GH levels every 6 months
Withdraw drug yearly for 4 weeks (solution) or 8 weeks (suspension) from patients who have undergone irradiation to assess
Carcinoid Tumor
Solution: 100-600 mcg/day SC divided q6-12hr; may titrate to 1500 mcg/day; after successful treatment with solution for 2 weeks, initiate treatment with suspension (depot injection)
Suspension (depot injection): 20 mg IM every 4 weeks if regular injection well tolerated
VIPoma
Solution: 200-300 mcg/day SC divided q6-12hr; after successful treatment with solution for 2 weeks, initiate treatment with suspension (depot injection)
Suspension (depot injection): 20 mg IM (gluteal) every 4 weeks for 2 months; continue solution for first 2 weeks; titrate suspension up or down to 10-30 mg IM every 4 weeks
Esophageal Variceal Bleeding (Off-label)
Solution: 50 mcg IV bolus, then 25-50 mcg/hr for 1-5 days
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Gallbladder problems (>60%): Decreased gallbladder contractility, gallstones, cholecystitis, cholestatic hepatitis
Dysglycemia (25%)
Hypothyroidism (25%)
Bradycardia (25%)
1-10%
ECG changes (10%)
Arrhythmia (9%)
Pancreatitis
Upper respiratory tract infection
Fatigue
Headache
Malaise
Rash
Diarrhea
Nausea
Vomiting
Pain at injection site
Joint pain
Blurred vision
Postmarketing Reports
Pediatric Patients
- No formal controlled clinical trials have been performed to evaluate the safety and effectiveness of octreotide depot injection in children younger than 6 years
- Serious adverse events, including hypoxia, necrotizing enterocolitis, and death, have been reported in children (mostly in those younger than 2 years)
- The relation of these events to octreotide has not been established, because the majority of these pediatric patients had serious underlying comorbid conditions
Warnings
Contraindications
Hypersensitivity
Cautions
Use caution in patients with hepatic impairment; patients with established cirrhosis may necessitate dosage adjustment
Use caution in patients with renal impairment; patients receiving dialysis may necessitate dosage adjustment
May alter fat absorption in some patients (monitor for pancreatitis)
Monitor for cholelithiasis; may impair gallbladder function; incidence of gallbladder stone or biliary sludge increases with duration of therapy exceeding 12 months; prophylactic cholecystectomy recommended if octreotide treatment is planned in in patients with gastrointestinal or pancreatic neuroendocrine tumors
May decrease vitamin B12 levels (monitor)
Monitor for hypothyroidism (octreotide suppresses secretion of TSH)
Use caution when giving drug to patients with cardiovascular disease
May enhance toxicity of QTc-prolonging agents
Use caution in patients with heart failure or concomitant medications that may alter heart rate or rhythm; arrhythmia, conduction abnormalities, and bradycardia reported in acromegalic and carcinoid syndrome patients; cardiovascular medications requirements may change
Depot formulation, not for treatment of sulfonylurea-induced hypoglycemia
Somatostatin analogs may affect glucose regulation; severe hypoglycemia may occur in type 1 diabetes patients; hyperglycemia may occur in type 2 diabetes or patients without diabetes; therapy may worsen hypoglycemia in patients with insulinomas; use with caution
Dosage adjustments may be necessary in the elderly
Females of childbearing age should use adequate contraception because the treatment may restore fertility
In patients maintained on total parenteral nutrition (TPN), monitoring for elevations in zinc levels recommended
May reduce excessive fluid loss in patients with conditions that cause fluid losses
Drug interaction overview
- Coadministration with cyclosporine may decrease blood levels of cyclosporine and result in transplant rejection
- Octreotide inhibits the secretion of insulin and glucagon; monitor blood glucose levels upon initiation or dose adjustment; patients with diabetes mellitus may require dose adjustments of insulin or other antidiabetic agents
- Coadministration with bromocriptine increases the availability of bromocriptine
- Patients receiving beta blockers, calcium channel blockers, or agents to control fluid and electrolyte balance, may require dose adjustments of these therapeutic agents
- Octreotide has been associated with alterations in nutrient absorption, so it may have an effect on absorption of orally administered drugs
- Limited published data indicate that somatostatin analogs might decrease the metabolic clearance of compounds known to be metabolized by cytochrome P450 enzymes, which may be due to the suppression of growth hormones
Pregnancy & Lactation
Pregnancy
Limited data in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage
Reproductive potential
- Discuss potential for unintended pregnancy with premenopausal women as therapeutic benefits of a reduction in growth hormone (GH) levels and normalization of insulin-like growth factor 1 (IGF-1) concentration in acromegalic females treated with drug may lead to improved fertility
Animal data
- In animal reproduction studies, no-adverse- developmental-effects were observed with intravenous administration of drug to pregnant rats and rabbits during organogenesis at doses 7 and 13-times, respectively the maximum recommended human dose (MRHD) of 1500 mcg/day based on body surface area
- Transient growth retardation, with no impact on postnatal development, was observed in rat offspring from a pre- and post-natal study of octreotide at intravenous doses below the MRHD based on body surface area
Lactation
There is no information available on presence of drug in human milk, effects on breastfed infant, or on milk production; studies show that drug administered subcutaneously passes into milk of lactating rats
Consider developmental and health benefits of breastfeeding along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Somatostatin analog; decreases GH secretion, secretion of gastrin, VIP, glucagon, secretin, serotonin release and pancreatic polypeptide; in acromegaly, octreotide decreases growth hormone and IGF-1 secretion; suppresses LH response to GnRH secretion and decreases splanchnic blood flow
Absorption
Absorption rapid and complete (SC)
Bioavailability: SC, 100%; IM, 60%
Peak plasma time: IV, immediately after injection; SC, 15-30 min; PO, 90-120 min; IM, 60 min
Distribution
Protein bound: 65% binds to lipoprotein
Vd: 13.6 L
Metabolism
Metabolized by liver
Elimination
Half-life: 1.7 hr
Total body clearance: 10 L/hr
Excretion: Urine (32%)
Administration
IV Incompatibilities
Fat emulsion 10%
IV Preparation
Common diluent: 50-100 μg/50 mL NS
Common diluent for continuous IV infusion: 1200 μg/250 mL NS
Minimum volume: 50 mL NS
Administration
IM
- Administer suspension (depot injection) immediately after reconstitution; inject into gluteal muscle, avoiding deltoid
IV
- IV administration may be IVP, IVPB, or continuous infusion
- Regular injection only: IVP should be administered undiluted over 3 minutes
- IVPB: Administer over 15-30 minutes
- Continuous infusion: 25-50 μg/hr for treatment of esophageal variceal bleeding
- Do not use if solution contains particles or is discolored
SC
- Rotate SC injection sites in a systematic manner
Storage
Protect from light
Suspension
- Unopened pens: Refrigerate at 2-8ºC (36-46ºF) in the carton
Solution multidose vials
- Unopened pens: Refrigerate at 2-8ºC (36-46ºF) in the carton
- After first use, store at room temperature at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF) for up to 14 days; discard vial after 14 days
Autoinjector pen
- Unused pens: Refrigerate at 2-8ºC (36-46ºF) in the carton
- After first use, store at controlled room temperature at 20-25°C (68-77°F); excursions permitted to 15-30ºC (59-86ºF) for up to 28 days
- Discard pen 28 days after first use
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Patient Handout
Formulary
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