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Octreotide

Medically reviewed by Drugs.com. Last updated on Sep 10, 2020.

Pronunciation

(ok TREE oh tide)

Index Terms

  • Longastatin
  • Octreotide Acetate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule Delayed Release, Oral, as acetate:

Mycapssa: 20 mg

Kit, Intramuscular:

SandoSTATIN LAR Depot: 10 mg, 20 mg, 30 mg

Solution, Injection:

SandoSTATIN: 50 mcg/mL (1 mL); 100 mcg/mL (1 mL)

SandoSTATIN: 200 mcg/mL (5 mL [DSC]) [contains phenol]

SandoSTATIN: 500 mcg/mL (1 mL)

SandoSTATIN: 1000 mcg/mL (5 mL [DSC]) [contains phenol]

Generic: 50 mcg/mL (1 mL); 100 mcg/mL (1 mL); 200 mcg/mL (5 mL); 500 mcg/mL (1 mL); 1000 mcg/mL (5 mL)

Solution, Injection [preservative free]:

Generic: 100 mcg/mL (1 mL); 500 mcg/mL (1 mL)

Solution Pen-injector, Subcutaneous:

Bynfezia Pen: 2500 mcg/mL (2.8 mL) [contains phenol]

Brand Names: U.S.

  • Bynfezia Pen
  • Mycapssa
  • SandoSTATIN
  • SandoSTATIN LAR Depot

Pharmacologic Category

  • Antidiarrheal
  • Antidote
  • Somatostatin Analog

Pharmacology

Octreotide mimics natural somatostatin by inhibiting serotonin release and the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide. Decreases growth hormone (GH) and IGF-1 in acromegaly. Octreotide provides more potent inhibition of GH, glucagon, and insulin as compared to endogenous somatostatin. Also suppresses LH response to GnRH, secretion of thyroid-stimulating hormone and decreases splanchnic blood flow.

Absorption

SubQ (injection solution): Rapid and complete.

IM (LAR depot suspension): Released slowly (via microsphere degradation in the muscle).

Oral (delayed-release capsule): Limited; rate and extent of absorption decreased by 90% when taken with food.

Distribution

Vd: 13.6 L (21.6 ± 8.5 L in acromegaly).

Metabolism

Extensively hepatic.

Excretion

Urine (32% as unchanged drug); Clearance: Healthy adults: 7 to 10 L/hour; Adults with acromegaly: 18 L/hour; Decreased in patients with end-stage renal disease requiring dialysis.

Time to Peak

Plasma: SubQ (injection solution): 0.4 hours (0.7 hours acromegaly); IM (LAR depot suspension): Transient peak occurs 1 hour after injection, then steady plateau is reached after 2 to 3 weeks; Oral: 1.75 to 2.5 hours.

Duration of Action

SubQ (injection solution): 6 to 12 hours.

IM (LAR depot suspension): Following a single injection, a steady concentration is achieved within 2 to 3 weeks and maintained for an additional 2 to 3 weeks; steady-state levels are achieved after 3 injections administered at 4-week intervals.

Oral (delayed-release capsule): Complete elimination after ~48 hours in patients who achieve steady-state levels.

Half-Life Elimination

SubQ (injection solution): 1.7 to 1.9 hours; Increased in elderly patients; Cirrhosis: Up to 3.7 hours; Fatty liver disease: Up to 3.4 hours; Renal impairment: Up to 3.1 hours.

Oral (delayed-release capsule): Healthy adults: 2.7 hours; Adults with acromegaly: 3.2 to 4.5 hours; End-stage renal disease requiring dialysis: 7.09 hours.

Protein Binding

65%, primarily to lipoprotein (41% in acromegaly).

Special Populations: Renal Function Impairment

Elimination and clearance are prolonged; clearance may be reduced by about 50% in patients with severe renal failure.

Special Populations: Hepatic Function Impairment

Patients with liver cirrhosis showed prolonged elimination of the drug with t½ increasing and clearance decreasing after SubQ administration.

Special Populations: Elderly

There is a 46% increase in the half-life of the drug and a 26% decrease in clearance after SubQ administration.

Use: Labeled Indications

Acromegaly:

Delayed-release capsule: Long-term maintenance treatment of acromegaly in patients who have responded to and tolerated treatment with octreotide or lanreotide.

Injection solution: To reduce blood levels of growth hormone and insulin-like growth factor 1 in patients with acromegaly who have had inadequate response to or cannot be treated with surgical resection and/or pituitary irradiation.

LAR depot suspension: Long-term maintenance treatment of acromegaly in patients with an inadequate response to surgery and/or radiotherapy, or for whom surgery/radiotherapy is not an option.

The Endocrine Society and the Acromegaly Consensus Group suggest use of a first-generation, long-acting somatostatin analogue (eg, lanreotide, octreotide) as first-line therapy in patients with persistent disease despite surgical resection or in whom surgery is not appropriate. Alternative agents are suggested for patients with mild disease postoperatively. Preoperative use of somatostatin analogues is also suggested in select patients to reduce surgical risk from severe comorbidities, although there is conflicting evidence regarding the long-term benefit of this strategy (ACG [Melmed 2018]; ES [Katznelson 2014]).

Carcinoid syndrome:

Injection solution: Management of symptoms of carcinoid syndrome (diarrhea and flushing) in patients with metastatic gastroenteropancreatic neuroendocrine tumors (GEP-NETs).

LAR depot suspension: Long-term treatment of severe diarrhea and flushing episodes associated with carcinoid syndrome in patients with metastatic GEP-NETs.

Gastroenteropancreatic neuroendocrine tumors, functional, vasoactive intestinal peptide-secreting (VIPomas):

Injection solution: Treatment of profuse watery diarrhea associated with vasoactive intestinal peptide-secreting GEP-NETs (VIPomas).

LAR depot suspension: Long-term treatment of profuse watery diarrhea associated with VIPomas.

Limitations of use: According to the manufacturer's labeling, the effects of octreotide (injection solution and LAR depot suspension) on tumor size, growth rate, and development of metastases in patients with carcinoid syndrome and VIPomas have not been determined. However, according to the North American Neuroendocrine Tumor Society consensus guidelines for surveillance and medical management of midgut neuroendocrine tumors (NETs), somatostatin analogues (including octreotide LAR) are appropriate initial therapy in most patients with unresectable metastatic midgut NETs for inhibition of tumor growth based on demonstrated antiproliferative effects (NANETS [Strosberg 2017a]; Rinke 2009).

Off Label Uses

Carcinoid crisis, prevention and treatment

Clinical experience suggests octreotide may be of benefit in preventing carcinoid crisis prior to invasive procedures in patients with neuroendocrine tumors (NETs) and in the treatment of carcinoid crisis with hypotension [Oberg 2004].

Diarrhea associated with acute graft-versus-host disease

Clinical experience suggests octreotide may be of benefit in managing diarrhea associated with acute graft-versus-host disease (GVHD) [Kornblau 2000].

Diarrhea associated with chemotherapy, refractory

Clinical experience and a multidisciplinary expert panel suggest the utility of octreotide in managing refractory diarrhea associated with chemotherapy [Benson 2004], [Kornblau 2000].

Fistulas, high-output, gastroenteropancreatic

In a meta-analysis of trials evaluating the treatment of high-output enterocutaneous fistulas, the use of somatostatin analogues (including octreotide) was shown to be safe and effective for reducing time to fistula closure, need for repeat operation, and length of hospital stay [Coughlin 2012]. In a separate meta-analysis in this population, use of somatostatin analogues (including octreotide) was also associated with improvement in overall incidence of fistula closure [Rahbour 2012].

Gastroenteropancreatic neuroendocrine tumors, functional, gastrin-secreting (gastrinoma, Zollinger-Ellison syndrome), refractory

Data from a limited number of patients in an open-label study suggest octreotide may be of benefit in the treatment of progressive malignant gastrinoma (Zollinger-Ellison syndrome) [Shojamanesh 2002].

Gastroenteropancreatic neuroendocrine tumors, metastatic, tumor control

Data from a randomized, placebo-controlled, phase 3 study support the use of octreotide LAR in the management of well-differentiated metastatic midgut NETs [Rinke 2009]. Data from a randomized, phase 3 study support the use of octreotide LAR depot suspension in combination with lutetium Lu 177 dotatate for the treatment of well-differentiated metastatic NETs that originate in the midgut [Strosberg 2017b]. Clinical experience also suggests the utility of octreotide in managing metastatic gastroenteropancreatic NETs [Oberg 2004].

Based on the North American Neuroendocrine Tumor Society consensus guidelines for surveillance and medical management of midgut NETs, octreotide LAR is recommended as a first-line option for inhibition of tumor growth in most patients with unresectable metastatic midgut NETs [NANETS [Strosberg 2017a]].

Gastroesophageal variceal hemorrhage, acute

Data from a meta-analysis and controlled trial support the use of octreotide in conjunction with endoscopic treatment for the management of acute gastroesophageal variceal hemorrhage [Corley 2001], [Seo 2014].

Based on the American Association for the Study of Liver Diseases guidelines on the management of portal hypertensive bleeding in cirrhosis and the British Society of Gastroenterology guidelines on the management of variceal hemorrhage in cirrhotic patients, octreotide is recommended as a first-line option for management of acute variceal bleeding [AASLD [Garcia-Tsao 2017]], [BSG [Tripathi 2015]].

Hepatorenal syndrome

Data from a small, controlled trial in patients with type 1 hepatorenal syndrome (HRS) treated with midodrine, octreotide, and albumin showed significant improvement in renal plasma flow, GFR, and urinary sodium excretion [Angeli 1999]. Retrospective data also suggest improvement in 30-day mortality with the combination of midodrine, octreotide, and albumin [Esrailian 2007], [Skagen 2009].

Based on American Association for the Study of Liver Diseases clinical practice guidelines for the management of adult patients with ascites due to cirrhosis, octreotide in combination with midodrine and albumin should be considered for the treatment of type 1 HRS [AASLD [Runyon 2013]].

Hypoglycemia, sulfonylurea-induced

Data from a double-blind, placebo-controlled study support the use of octreotide in the treatment of sulfonylurea-induced hypoglycemia [Fasano 2008].

Malignant bowel obstruction

Data from a small, randomized study support the use of octreotide in managing GI symptoms due to malignant bowel obstruction in patients with advanced cancer [Mercadante 2000]. Data from a review and a systematic review also support the use of octreotide in managing symptoms caused by malignant bowel obstruction in patients with advanced cancer [Mercadante 2007], [Mercadante 2012].

Thymic epithelial malignancies, advanced

Data from a small, phase 2 study support the use of octreotide (with or without prednisone) in the treatment of advanced (invasive, recurrent, or metastatic) thymic epithelial malignancies, including thymic carcinoma and thymomas [Loehrer 2004].

Contraindications

Hypersensitivity to octreotide or any component of the formulation

Dosing: Adult

Acromegaly:

Note: For use in patients with persistent disease following surgery or in whom surgery is not appropriate (ACG [Melmed 2018]; ES [Katznelson 2014]). May use the long-acting IM depot formulation as initial therapy (ACG [Melmed 2018]; ES [Katznelson 2014]) or may consider 1 or 2 doses of SubQ octreotide to assess tolerability prior to starting the long-acting IM depot (AACE [Katznelson 2011]). If clinical and/or biochemical response is inadequate at maximum dosage of octreotide, consider alternative agents or starting combination therapy (ACG [Melmed 2018]; ES [Katznelson 2014]).

IM (depot): Initial: 20 mg intragluteally every 4 weeks for 3 months; after initial 3 months, adjust dose as necessary based on clinical response. Dosage titration example provided from the manufacturer's labeling:

Growth hormone (GH) ≤1 ng/mL, insulin-like growth factor 1 (IGF-1) normal, and symptoms controlled: Reduce octreotide depot to 10 mg every 4 weeks.

GH >1 to ≤2.5 ng/mL, IGF-1 normal, and symptoms controlled: Maintain octreotide depot at 20 mg every 4 weeks.

GH >2.5 ng/mL, IGF-1 elevated, and/or symptoms uncontrolled: Increase octreotide depot to 30 mg every 4 weeks. If GH, IGF-1, or symptoms remain uncontrolled, may increase dose to 40 mg every 4 weeks. Dosages >40 mg are not recommended by the manufacturer; however, in some cases, individualized doses up to 60 mg every 4 weeks have been used successfully in partial responders (Giustina 2017).

SubQ: Initial: 50 mcg 3 times daily; titrate to achieve target GH and IGF-1 levels. Usual effective dose: 100 mcg 3 times daily; range: 300 to 1,500 mcg/day. Doses above 300 mcg/day rarely result in additional benefit; if increased dose fails to provide additional benefit, the dose should be reduced.

Oral: Note: For long-term maintenance treatment in patients who respond to and tolerate treatment with injectable octreotide or lanreotide.

Initial: 20 mg twice daily; adjust dose in 20 mg/day increments every 2 to 4 weeks as necessary based on clinical response as follows (Melmed 2015; manufacturer's labeling):

60 mg/day: Administer as 40 mg every morning and 20 mg every evening.

80 mg/day: Administer as 40 mg twice daily (maximum: 80 mg/day).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Carcinoid crisis, prevention and treatment (off-label use):

IR octreotide solution:

Prevention:

Note: Consider use prior to invasive procedures in patients with carcinoid syndrome or metastatic midgut neuroendocrine tumors (NETs) and elevated urinary 5-hydroxyindoleacetic acid (5-HIAA) levels. Octreotide IR solution should be readily available during any surgical procedure in these patients (ENETS [Kaltsas 2017]; Mancuso 2011; Oberg 2004).

Patients controlled with octreotide IM (depot) 20 to 30 mg every 4 weeks: SubQ: 250 to 500 mcg within 1 to 2 hours prior to procedure (Oberg 2004).

Somatostatin analogue-naive patients (Oberg 2004):

IV bolus: 500 to 1,000 mcg 1 to 2 hours prior to procedure.

or

SubQ: 500 mcg 1 to 2 hours prior to procedure.

Treatment:

Intraoperative use for carcinoid crisis with hypotension: IV: 500 to 1,000 mcg bolus, repeat at 5-minute intervals until symptoms are controlled or 500 to 1,000 mcg bolus followed by 50 to 200 mcg/hour continuous infusion during the procedure (Oberg 2004).

Postoperative use for patients requiring intraoperative therapy: IV: 50 to 200 mcg/hour continuous infusion for 24 hours, followed by resumption of the preoperative treatment schedule (Oberg 2004).

Carcinoid syndrome:

Note: The North American Neuroendocrine Tumor Society (NANETS) guidelines suggest that the long-acting depot may be appropriate as initial therapy (ie, without prior SubQ octreotide as stated in the US labeling) (NANETS [Strosberg 2017a]). For patients experiencing breakthrough symptoms while taking the long-acting depot, supplementary doses of SubQ octreotide may be necessary.

IM (depot):

Initial: 20 mg intragluteally every 4 weeks (manufacturer's labeling) or 20 to 30 mg intragluteally every 4 weeks (Oberg 2004).

Titration: Dose may be modified based on response as follows:

May decrease to 10 mg every 4 weeks after 2 months if initially responsive to 20 mg dose.

Increase to 30 mg every 4 weeks if symptoms are inadequately controlled after 2 months. Note: The US labeling states that higher doses are not recommended; however, if frequent supplementary SubQ doses are needed (eg, ≥3 to 4 times/week), may consider further increasing the dose by 10 mg every 4 weeks, or maintaining the same dose and reducing the dosing interval to every 3 weeks, up to a maximum off-label dose of 60 mg every 4 weeks (Oberg 2004).

SubQ, IV: Initial: 100 to 600 mcg/day in 2 to 4 divided doses. If additional symptom control is needed, may increase by doubling the dose every 3 to 4 days until symptoms are controlled; usual range: 50 to 750 mcg/day. Experience with doses above 750 mcg/day is limited; however, may consider a continuous SubQ infusion of 1,000 to 2,000 mcg/day off label in patients who remain symptomatic on intermittent doses (Oberg 2004; manufacturer's labeling).

Diarrhea associated with acute graft-versus-host disease (off-label use):

Note: Use in combination with other appropriate agents (eg, corticosteroids) for the management of acute graft-versus-host disease (GVHD) (Kornblau 2000).

IV: 500 mcg every 8 hours; discontinue within 24 hours of diarrhea resolution to avoid ileus. Maximum duration of therapy if diarrhea is not resolved: 7 days (Kornblau 2000).

Diarrhea associated with chemotherapy, refractory (off-label use):

Low grade or uncomplicated, persistent: SubQ: 100 to 150 mcg 3 times daily (Benson 2004; Kornblau 2000).

Severe or complicated:

IV, SubQ: Initial: 100 to 150 mcg 3 times daily; may increase to 500 to 2,000 mcg IV or SubQ 3 times daily (Benson 2004; Kornblau 2000; Wadler 1995).

or

IV infusion: 25 to 50 mcg/hour (Benson 2004).

Duration of therapy: Discontinue therapy within 24 hours of resolution of diarrhea to reduce the risk of ileus (Barbounis 2001; Benson 2004).

Fistulas, high-output, gastroenteropancreatic (off-label use):

Note: Reserve use for patients with fistula output >1 to 1.5 L/day; in patients with enterocutaneous fistula, avoid use if barriers to spontaneous closure (eg, distal obstruction, Crohn disease) are present (Parli 2018; Stein 2020).

SubQ: 100 mcg 3 times daily; discontinue and consider alternative agents if fistula output does not decrease after 3 to 5 days (Parli 2018).

Gastroenteropancreatic neuroendocrine tumors, functional, gastrin-secreting (gastrinoma, Zollinger-Ellison syndrome), refractory (alternative agent) (off-label use):

Note: May be used to control symptoms of hormone hypersecretion (eg, ulcers, heartburn, diarrhea) refractory to first-line therapy. The NANETS guidelines suggest that the long-acting depot may be appropriate as initial therapy (ie, without prior SubQ octreotide) (NANETS [Strosberg 2017a]). For patients experiencing breakthrough symptoms while taking the long-acting depot, supplementary doses of SubQ octreotide may be necessary.

IM (depot):

Initial: 20 mg intragluteally every 4 weeks (manufacturer's labeling) or 20 to 30 mg intragluteally every 4 weeks (Oberg 2004).

Titration: Dose may be modified based on response as follows:

May decrease to 10 mg every 4 weeks after 2 months if initially responsive to 20 mg dose.

Increase to 30 mg every 4 weeks if symptoms are inadequately controlled after 2 months. Note: The US labeling states that higher doses are not recommended; however, if frequent supplementary SubQ doses are needed (eg, ≥3 to 4 times/week), may consider further increasing the dose by 10 mg every 4 weeks, or maintaining the same dose and reducing the dosing interval to every 3 weeks, up to a maximum off-label dose of 60 mg every 4 weeks (Oberg 2004).

SubQ: Initial: 100 mcg every 12 hours; may increase to 200 mcg every 12 hours (Shojamanesh 2002) or 100 to 500 mcg in 2 to 4 divided doses (usual dose: 150 mcg 3 times daily) (Oberg 2004). If additional symptom control is needed, may increase by doubling the dose every 3 to 4 days until symptoms are controlled; may also consider a continuous SubQ infusion of 1,000 to 2,000 mcg/day (Oberg 2004).

Gastroenteropancreatic neuroendocrine tumors, functional, vasoactive intestinal peptide-secreting (VIPomas):

Note: May be used to control symptoms of hormone hypersecretion (eg, diarrhea). The NANETS guidelines suggest that the long-acting depot may be appropriate as initial therapy (ie, without prior SubQ octreotide as stated in the US labeling) (NANETS [Strosberg 2017a]). For patients experiencing breakthrough symptoms while taking the long-acting depot, supplementary doses of SubQ octreotide may be necessary.

IM (depot):

Initial: 20 mg intragluteally every 4 weeks (manufacturer's labeling) or 20 to 30 mg intragluteally every 4 weeks (Oberg 2004).

Titration: Dose may be modified based on response as follows:

May decrease to 10 mg every 4 weeks after 2 months if initially responsive to 20 mg dose.

Increase to 30 mg every 4 weeks if symptoms are inadequately controlled after 2 months. Note: The US labeling states that higher doses are not recommended; however, if frequent supplementary SubQ doses are needed (eg, ≥3 to 4 times/week), may consider further increasing the dose by 10 mg every 4 weeks, or maintaining the same dose and reducing the dosing interval to every 3 weeks, up to a maximum off-label dose of 60 mg every 4 weeks (Oberg 2004).

SubQ, IV: Initial: 200 to 300 mcg/day in 2 to 4 divided doses. If additional symptom control is needed, may increase by doubling the dose every 3 to 4 days until symptoms are controlled; usual range: 150 to 450 mcg/day. Doses >450 mcg/day are rarely required; however, may consider a continuous SubQ infusion of 1,000 to 2,000 mcg/day off label in patients who remain symptomatic on intermittent doses (Oberg 2004; manufacturer's labeling).

Gastroenteropancreatic neuroendocrine tumors, metastatic, tumor control (off-label use):

Note: May be used to control tumor growth in patients with unresectable, metastatic, well-differentiated NETs with a high tumor burden (including thymus and lung NETs) (NANETS [Kunz 2013]; NANETS [Strosberg 2017a]). The NANETS guidelines suggest that the long-acting depot may be appropriate as initial therapy (ie, without prior SubQ therapy) (NANETS [Strosberg 2017a]). For patients with functional tumors who are experiencing breakthrough symptoms while taking the long-acting depot, supplementary doses of SubQ octreotide may be necessary.

IM (depot): 30 mg intragluteally every 4 weeks until tumor progression or death (Rinke 2009; Rinke 2017).

or

IM (depot):

Initial: 20 to 30 mg intragluteally every 4 weeks (Oberg 2004).

Titration: If frequent supplementary SubQ doses are needed (eg, ≥3 to 4 times/week), may increase the dose by 10 mg every 4 weeks, or maintain the same dose and reduce the dosing interval to every 3 weeks (Oberg 2004).

Dosage range: 20 to 60 mg every 4 weeks.

SubQ: Initial: 100 to 500 mcg in 2 to 4 divided doses (usual dose: 150 mcg 3 times daily). If additional symptom control is needed, may increase by doubling the dose every 3 to 4 days until symptoms are controlled; may also consider a continuous SubQ infusion of 1,000 to 2,000 mcg/day (Oberg 2004).

With lutetium Lu 177 dotatate treatment: IM (depot): 30 mg once following each lutetium Lu 177 dotatate dose (administer between 4 to 24 hours after the lutetium Lu 177 dotatate dose) for 4 doses and then continue 30 mg once a month after lutetium Lu 177 dotatate is completed (Strosberg 2017b). Rescue doses (dose not specified) of short-acting octreotide may be used in between for symptomatic management (for diarrhea or flushing), but discontinue at least 24 hours before each lutetium Lu 177 dotatate dose.

Gastroesophageal variceal hemorrhage, acute (off-label use):

Note: For use in patients with varices or at risk for varices who have upper GI bleeding; treatment should not be delayed pending confirmation of the source of bleeding. In patients with cirrhosis and active variceal bleeding, administer prophylactic antibiotics for up to 7 days (AASLD [Garcia-Tsao 2017]; Bajaj 2020).

IV: Initial: 50 mcg bolus, followed by continuous infusion of 50 mcg/hour for 2 to 5 days; may repeat bolus in first hour if hemorrhage is not controlled (AASLD [Garcia-Tsao 2017]; Bajaj 2020; BSG [Tripathi 2015]).

Hepatorenal syndrome (off-label use):

Note: For use as part of an appropriate combination regimen in patients who are not in an ICU (ie, cannot receive norepinephrine) (AASLD [Runyon 2013]; Runyon 2020).

SubQ: Initial: 100 mcg 3 times daily; may increase to 200 mcg 3 times daily (with a goal to increase mean arterial pressure by at least 15 mm Hg from baseline) (AASLD [Runyon 2013]; Angeli 1999; Esrailian 2007; Garcia-Tsao 2009).

IV: 50 mcg/hour as a continuous infusion (Runyon 2020). Note: Preferred to SubQ injections by some experts to achieve faster treatment response (Runyon 2020).

Duration of therapy: Discontinue therapy after 2 weeks if no response; may consider longer duration (eg, 4 weeks) if there is incomplete improvement in renal function after 2 weeks (Runyon 2020).

Hypoglycemia, sulfonylurea-induced (adjunct) (off-label use):

Note: Use in combination with IV dextrose for initial treatment of intentional overdose (Glatstein 2012); may also use for refractory, unintentional single-episode hypoglycemia occurring during therapeutic use (Chu 2020; Fasano 2008). The SubQ route is preferred over IV except in cases where peripheral circulation may be compromised (Smith 2019).

SubQ, IV: 50 to 100 mcg as a single dose; may repeat every 6 hours if needed (Dougherty 2010; Fasano 2008; Smith 2019). Note: In patients with recurrent hypoglycemia, a continuous IV infusion (eg, up to 125 mcg/hour) may be required (McLaughlin 2000). Usual duration is 24 hours; however, may need to be extended if hypoglycemia persists (Glatstein 2012; Smith 2019).

Malignant bowel obstruction (off-label use):

Note: For use in patients who are not candidates for surgery or who have inoperable obstruction (Mercadante 2007).

SubQ: 200 to 900 mcg/day in 2 to 3 divided doses (Mercadante 2007; Mercadante 2012) or 300 mcg/day by continuous SubQ infusion (Mercadante 2000). Note: Patients who respond to SubQ injections may be converted to IM depot injections (eg, 30 mg IM every 4 weeks) for maintenance therapy (Franke 2017; Laval 2012).

Thymic epithelial malignancies, advanced (off-label use):

SubQ: 500 mcg 3 times daily; evaluate after 2 months. Patients with remission (complete or partial) continued octreotide for up to a maximum of 12 months; patients with stable disease continued octreotide and also received prednisone for up to 12 months or until disease progression or unacceptable toxicity (Loehrer 2004).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Injection solution, LAR depot suspension: Refer to adult dosing. Elimination half-life is increased by 46% and clearance is decreased by 26%; dose adjustment may be required. Dosing should generally begin at the lower end of dosing range.

Delayed-release capsule: Refer to adult dosing.

Dosing: Pediatric

Note: Unless otherwise specified, all pediatric dosing based on use of the immediate-release injection solution (non-long-acting). Dosing is presented in multiple formats (eg, mcg/kg/hour, mcg/kg/day, mcg/kg/dose); use extra precaution.

Chylothorax, acquired (eg, postoperative): Limited data available; efficacy results variable; optimal dose not established (Church 2017): Infants and Children: Continuous IV infusion: Reported range: 1 to 4 mcg/kg/hour; in one report, octreotide was initiated and maintained at fixed rate of 3 mcg/kg/hour; other reports describe initiation of therapy at the lower end of a dosing range and titration; usual duration of therapy: 7 days (Landvoigt 2006; Mery 2014; Yeh 2013).

Diarrhea: Very limited data available; reported dosing highly variable: Note: In pediatric patients, octreotide has been used to manage refractory cases of diarrhea due to multiple etiologies including GVHD, chemotherapy induced, and congenital secretory syndromes; use has been described in a small trial, several case reports and by some centers. A dose-response relationship has not been established. SubQ administration is the usual route; however, the IV route has been used in some cases (Al-Hussaini 2012; Beckman 2000; Couper 1989; Jaros 1988; Pai 2011).

Infants, Children, and Adolescents:

Intermittent SubQ: Usual initial dose: 1 to 10 mcg/kg/dose every 8 to 12 hours; doses should begin at the low end of the range and be titrated to effect; reported range: 1 to 49 mcg/kg/day (Al-Hussaini 2012; Beckman 2000; Couper 1989; Jaros 1988; Pai 2011); a higher dose of 60 mcg/kg/day has been reported (Al-Hussaini 2012). In adults, a maximum dose of 500 mcg/dose has been recommended for GVHD (ASCO [Benson 2004]).

Continuous IV infusion: Note: Typically IV infusion reserved for patients failing intermittent dosing: Initial: 1 mcg/kg/hour (Beckman 2000); some patients may require titration; doses up to 49 mcg/kg/day have been reported (Pai 2011).

Esophageal varices; gastrointestinal bleed: Limited data available: Infants, Children, and Adolescents: IV: Initial: 1 to 2 mcg/kg bolus followed by 1 to 2 mcg/kg/hour continuous IV infusion; titrate infusion rate to response; taper dose by 50% every 12 hours when no active bleeding occurs for 24 hours; may discontinue when dose is 25% of initial dose (Al-Hussaini 2012; Eroglu 2004).

Hyperinsulinemic hypoglycemia: Limited data available: Note: Not first-line therapy (diazoxide suggested for initial management) (Shah 2017). Dosing should be individualized to patient response to achieve and maintain target serum glucose concentrations (typically >70 mg/dL) (Sperling 2014).

Daily dosing: Infants, Children, and Adolescents: SubQ:

Intermittent SubQ: Initial: 5 mcg/kg/day in divided doses every 6 to 8 hours; titrate to response, 5 mcg/kg/day increments have been used; usual reported effective range: 5 to 25 mcg/kg/day in divided doses; maximum daily dose: 35 mcg/kg/day (Demirbilek 2017; Shah 2017).

Continuous SubQ infusion: Initial: 5 mcg/kg/day delivered over 24 hours; titrate to response, 5 mcg/kg/day increments have been used; usual reported effective range: 5 to 25 mcg/kg/day; maximum daily dose: 35 mcg/kg/day (Demirbilek 2017; Hosokawa 2017; Shah 2017).

Monthly dosing: Long-acting depot formulation; conversion from SubQ (daily) to IM (monthly): Very limited data available:

Note: Not for initial management; for administration by a health care professional; in pediatric trials, initial doses (7) were administered in an inpatient facility. Due to the delayed onset of therapeutic levels with the long-acting IM formulation, overlap with SubQ octreotide therapy (intermittent or continuous infusion) along with IM therapy is necessary:

Children and Adolescents: Long-acting formulation (Sandostatin LAR): IM: Calculate patient's cumulative 31-day SubQ dose, which will equal the monthly IM dose; administer this dose every 4 weeks. Continue with SubQ octreotide therapy for 2 months after starting IM long-acting formulation (first 2 IM depot doses) then discontinue prior at the time of the third IM dose; monitor patient closely for hypoglycemia while receiving both IM (long-acting) and SubQ octreotide (Le Quan Sang 2012; Shah 2017).

Hypothalamic obesity (from cranial insult): Limited data available; efficacy results variable: Children ≥8 years of age and Adolescents: SubQ: Initial: 5 mcg/kg/day divided into 3 daily doses; dose may be increased bimonthly at 5 mcg/kg/day increments to a maximum of 15 mcg/kg/day divided into 3 daily doses; dosing based on small trials which showed insulin suppression, decreased caloric intake, and BMI stabilization or decrease; trials were limited to a 6 month duration; long-term effects are unknown (Lustig 1999; Lustig 2003; Lustig 2011).

Sulfonylurea overdose: Limited data available: Dosing in pediatric patients based on experience in adult patients; pediatric-specific reports are sparse (Glatstein 2010; Howland 2011). Infants, Children, and Adolescents: SubQ: 1 to 1.25 mcg/kg/dose every 6 hours; repeat as needed based upon blood glucose concentrations (Howland 2011); children generally need only a single dose (Dougherty 2013). Note: Although octreotide use is strongly advocated as a first-line therapy, indications and dosing for octreotide are not firmly established (Glatstein 2012).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Reconstitution

IV infusion: Dilute injection solution in 50 to 200 mL NS or D5W.

IM (LAR depot suspension): Allow vial and provided diluent-filled syringe to reach room temperature slowly (approximately 30 to 60 minutes). Reconstitute with provided diluent; refer to product labeling for detailed mixing instructions.

Administration

Delayed-release capsule: Oral: Take with a glass of water at least 1 hour before or 2 hours after a meal. Swallow capsules whole; do not crush or chew the capsules.

Injection solution:

Ampule, syringe, vial: SubQ, IV: Administer SubQ or IV; IV administration may be IV push (undiluted over 3 minutes), intermittent IV infusion (over 15 to 30 minutes), or continuous IV infusion (off-label route). In emergency situations (eg, carcinoid crisis), octreotide may be given as a rapid IV bolus. When administering SubQ use the concentration with smallest volume to deliver dose to reduce injection-site pain. Rotate injection site; may bring to room temperature prior to injection.

Prefilled pen: SubQ: Bring to room temperature ~20 to 30 minutes prior to administration. Administer SubQ into abdomen, front middle thigh, or back/outer area of upper arm. Rotate injection site; administer at least 2 inches away from previous injection site. Refer to manufacturer's labeling for additional administration instructions (including priming of pen).

LAR depot suspension: IM: Administer IM intragluteal (avoid deltoid administration); alternate gluteal injection sites to avoid irritation. For IM administration only; do not administer LAR depot suspension (Sandostatin LAR) IV or SubQ; must be administered immediately after mixing.

Dietary Considerations

Schedule injections between meals to decrease GI effects. Administer oral capsules at least 1 hour before or 2 hours after a meal. May alter absorption of dietary fats.

Storage

Delayed-release capsules: Until first use, store unopened wallets refrigerated at 2°C to 8°C (36°F to 46°F). Do not freeze. After first use, may be stored at 20°C to 25°C (68°F to 77°F) for up to 1 month.

Injection solution:

Ampule, syringe, vial: Store between 2°C and 8°C (36°F and 46°F). Protect from light. May be stored at room temperature of 20°C to 30°C (68°F and 86°F) for up to 14 days when protected from light. Stable as a parenteral admixture in NS or D5W for 24 hours. Discard multidose vials within 14 days after initial entry.

Prefilled pen: Store unused pen between 2°C and 8°C (36°F and 46°F). Protect from light. After first use may store refrigerated or at room temperature between 20°C and 25°C (68°F and 77°F) (excursions permitted to 15°C to 30°C [59°F to 86°F])] for up to 28 days.

LAR depot suspension: Prior to dilution, store at refrigerated temperatures between 2°C and 8°C (36°F and 46°F). Protect from light. Additionally, the manufacturer reports that octreotide suspension may be stored at room temperature of 20°C to 25°C (68°F and 77°F) for up to 10 days when protected from light (Novartis written communication 2011). Depot drug product kit may be at room temperature for 30 to 60 minutes prior to use. Use suspension immediately after preparation.

Drug Interactions

Androgens: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy

Antacids: May decrease the serum concentration of Octreotide. Monitor therapy

Antidiabetic Agents: May enhance the hypoglycemic effect of Hypoglycemia-Associated Agents. Monitor therapy

Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy

Bradycardia-Causing Agents: May enhance the bradycardic effect of other Bradycardia-Causing Agents. Monitor therapy

Bromocriptine: Somatostatin Analogs may increase the serum concentration of Bromocriptine. Somatostatin Analogs may also delay bromocriptine absorption and time to maximum plasma concentrations. Monitor therapy

Ceritinib: Bradycardia-Causing Agents may enhance the bradycardic effect of Ceritinib. Management: If this combination cannot be avoided, monitor patients for evidence of symptomatic bradycardia, and closely monitor blood pressure and heart rate during therapy. Consider therapy modification

Codeine: Somatostatin Analogs may decrease the metabolism of Codeine. The formation of two major codeine metabolites (morphine and norcodeine) may be impaired by somatostatin analogs. Monitor therapy

Copper Cu 64 Dotatate: Somatostatin Analogs may diminish the diagnostic effect of Copper Cu 64 Dotatate. Management: Imaging with copper Cu 64 dotatate positron emission tomography (PET) should be performed just prior to dosing with somatostatin analogs. If on somatostatin analogs, stop long-acting agents 28 days before, and short-acting agents 2 days before, imaging. Consider therapy modification

CycloSPORINE (Systemic): Somatostatin Analogs may decrease the serum concentration of CycloSPORINE (Systemic). Monitor therapy

Digoxin: Octreotide may enhance the bradycardic effect of Digoxin. Octreotide may increase the serum concentration of Digoxin. Monitor therapy

Fexinidazole [INT]: Bradycardia-Causing Agents may enhance the arrhythmogenic effect of Fexinidazole [INT]. Avoid combination

Gallium Ga 68 Dotatate: Somatostatin Analogs may diminish the diagnostic effect of Gallium Ga 68 Dotatate. Specifically, a false negative PET scan may occur if Gallium GA 68 Dotatate is used during treatment with somatostatin analogs. Management: Imaging with gallium Ga 68 dotatate positron emission tomography (PET) should be performed just prior to dosing with long-acting somatostatin analogs. Short-acting somatostatin analogs can be used up to 24 hours before imaging with gallium Ga 68 dotatate. Consider therapy modification

Gallium Ga 68 Dotatoc: Somatostatin Analogs may diminish the diagnostic effect of Gallium Ga 68 Dotatoc. Management: Imaging with gallium Ga 68 dotatoc positron emission tomography (PET) should be performed just prior to dosing with long-acting somatostatin analogs. Short-acting somatostatin analogs can be used up to 24 hours before imaging with gallium Ga 68 dotatoc. Consider therapy modification

Herbs (Hypoglycemic Properties): May enhance the hypoglycemic effect of Hypoglycemia-Associated Agents. Monitor therapy

Histamine H2 Receptor Antagonists: May decrease the serum concentration of Octreotide. Monitor therapy

Hormonal Contraceptives: Octreotide may decrease the serum concentration of Hormonal Contraceptives. Management: Women should use an alternative non-hormonal method of contraception or a back-up method when octreotide is combined with hormonal contraceptives. Consider therapy modification

Hypoglycemia-Associated Agents: May enhance the hypoglycemic effect of other Hypoglycemia-Associated Agents. Monitor therapy

Ivabradine: Bradycardia-Causing Agents may enhance the bradycardic effect of Ivabradine. Monitor therapy

Lacosamide: Bradycardia-Causing Agents may enhance the AV-blocking effect of Lacosamide. Monitor therapy

Lisinopril: Octreotide may increase the serum concentration of Lisinopril. Monitor therapy

Lutetium Lu 177 Dotatate: Somatostatin Analogs may diminish the therapeutic effect of Lutetium Lu 177 Dotatate. Specifically, the therapeutic effect of Lutetium Lu 177 Dotatate may be diminished if the timing of Somatostatin Analog administration is not carried out as recommended. Management: Discontinue long-acting somatostatin analogs at least 4 weeks and short-acting octreotide at least 24 hours prior to lutetium Lu 177 dotatate dose. Administer short and long-acting octreotide during treatment as recommended. See full interaction monograph Consider therapy modification

Macimorelin: Somatostatin Analogs may diminish the diagnostic effect of Macimorelin. Avoid combination

Maitake: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy

Midodrine: May enhance the bradycardic effect of Bradycardia-Causing Agents. Monitor therapy

Monoamine Oxidase Inhibitors: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy

Pegvisomant: Somatostatin Analogs may enhance the adverse/toxic effect of Pegvisomant. Specifically, this combination may increase the risk for significant elevations of liver enzymes. Monitor therapy

Pegvisomant: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy

Prothionamide: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy

Proton Pump Inhibitors: May decrease the serum concentration of Octreotide. Monitor therapy

Quinolones: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Quinolones may diminish the therapeutic effect of Agents with Blood Glucose Lowering Effects. Specifically, if an agent is being used to treat diabetes, loss of blood sugar control may occur with quinolone use. Monitor therapy

Ruxolitinib: May enhance the bradycardic effect of Bradycardia-Causing Agents. Management: Ruxolitinib Canadian product labeling recommends avoiding use with bradycardia-causing agents to the extent possible. Monitor therapy

Salicylates: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy

Selective Serotonin Reuptake Inhibitors: May enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects. Monitor therapy

Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Consider therapy modification

Siponimod: Bradycardia-Causing Agents may enhance the bradycardic effect of Siponimod. Management: Avoid coadministration of siponimod with drugs that may cause bradycardia. If combined, consider obtaining a cardiology consult regarding patient monitoring. Consider therapy modification

Telotristat Ethyl: Octreotide may decrease the serum concentration of Telotristat Ethyl. Management: Administer short-acting octreotide at least 30 minutes after administration of telotristat ethyl and monitor for decreased telotristat ethyl efficacy. Consider therapy modification

Terlipressin: May enhance the bradycardic effect of Bradycardia-Causing Agents. Monitor therapy

Tofacitinib: May enhance the bradycardic effect of Bradycardia-Causing Agents. Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Adverse reactions vary by route of administration and dosage form. Frequency of cardiac, endocrine, and gastrointestinal adverse reactions was generally higher in patients with acromegaly.

>10%:

Cardiovascular: Hypertension (≤13%), peripheral edema (16%), sinus bradycardia (19% to 25%)

Dermatologic: Alopecia (1% to 13%), hyperhidrosis (21%), pruritus (1% to 18%), skin rash (≤15%)

Endocrine & metabolic: Hyperglycemia (2% to 27%), hypothyroidism (≤12%)

Gastrointestinal: Abdominal distress (≤61%), abdominal pain (≤44%), biliary obstruction (duct dilatation: 12%), cholelithiasis (13% to 38%; length of therapy dependent), constipation (9% to 21%), diarrhea (≤61%), flatulence (≤38%), gallbladder sludge (24%; length of therapy dependent), nausea (≤61%), upper abdominal pain (8% to 11%), vomiting (4% to 21%)

Hematologic & oncologic: Anemia (≤15%)

Immunologic: Antibody development (≤25%; to octreotide; no efficacy change)

Local: Pain at injection site (2% to 50%)

Nervous system: Dizziness (5% to 20%), fatigue (1% to 32%), headache (6% to 33%), pain (4% to 15%)

Neuromuscular & skeletal: Arthralgia (1% to 26%), arthropathy (8% to 19%), asthenia (1% to 22%), back pain (1% to 27%), musculoskeletal pain (5% to 15%), myalgia (≤18%), osteoarthritis

Respiratory: Flu-like symptoms (1% to 20%), sinusitis (5% to 15%), upper respiratory tract infection (5% to 23%)

1% to 10%:

Cardiovascular: Bradycardia (2%), cardiac arrhythmia (≤9%), cardiac conduction disturbance (1% to 10%), edema (1% to 4%), flushing (1% to 4%), tachycardia (≤2%)

Endocrine & metabolic: Diabetes mellitus (1%), goiter (≤8%), hypoglycemia (2% to 4%)

Gastrointestinal: Abdominal distention (<10%), abnormal stools (<10%), cholecystitis (acute: 4%), dyspepsia (4% to 8%), fecal discoloration (4% to 6%), gastritis, gastrointestinal motility disorder, gastrointestinal reflux disease, intestinal polyps, malabsorption (fat: 1% to 4%), steatorrhea (4% to 6%), tenesmus (4% to 6%), xerostomia

Genitourinary: Pollakiuria (1% to 4%), urinary tract infection (1% to 4%)

Hematologic & oncologic: Bruise (1% to 4%)

Infection: Cold symptoms (1% to 4%), influenza (7%)

Local: Hematoma at injection site (1% to 4%)

Nervous system: Depression (1% to 4%)

Neuromuscular & skeletal: Tremor (1% to 4%)

Ophthalmic: Blurred vision (1% to 4%), visual disturbance (1% to 4%)

Respiratory: Epistaxis (1% to 4%), nasopharyngitis (7%)

<1%:

Cardiovascular: Cardiac failure, chest pain, hypertensive crisis, ischemia, orthostatic hypotension, palpitations, Raynaud's disease, syncope, thrombophlebitis

Dermatologic: Cellulitis, urticaria

Endocrine & metabolic: Adrenocortical insufficiency, amenorrhea, decreased libido, diabetes insipidus, galactorrhea not associated with childbirth, gynecomastia, infrequent uterine bleeding, iron deficiency, menstrual disease (polymenorrhea), pituitary apoplexy, weight loss

Gastrointestinal: Appendicitis, biliary obstruction, cholangitis (ascending), gastric ulcer, gastrointestinal hemorrhage, hemorrhoids, intestinal obstruction, pancreatitis, peptic ulcer

Genitourinary: Hematuria, vaginitis

Hematologic & oncologic: Basal cell carcinoma of skin, petechia, polyp (gallbladder)

Hepatic: Cholestatic hepatitis, hepatitis, increased liver enzymes, jaundice

Hypersensitivity: Hypersensitivity reaction

Nervous system: Amnesia, anxiety, Bell's palsy, neuritis, paranoid ideation, seizure, vertigo

Neuromuscular & skeletal: Arthritis, increased creatine phosphokinase in blood specimen, joint effusion

Ophthalmic: Increased intraocular pressure

Otic: Hearing loss, otitis

Renal: Nephrolithiasis

Respiratory: Dyspnea, pneumonia, status asthmaticus

Miscellaneous: Nodule (pulmonary)

Frequency not defined:

Cardiovascular: Pulmonary embolism

Hematologic & oncologic: Rectal hemorrhage

Hepatic: Ascites

Nervous system: Cerebrovascular disease, malignant hyperthermia

Respiratory: Pleural effusion

Postmarketing:

Cardiovascular: Acute myocardial infarction, aneurysm, arterial thrombosis (arm), atrial fibrillation, facial edema, prolonged QT interval on ECG, thrombosis (including retinal thrombosis)

Endocrine & metabolic: Cyanocobalamin deficiency

Gastrointestinal: Abdominal swelling

Hematologic & oncologic: Breast carcinoma, pancytopenia, thrombocytopenia

Hepatic: Liver steatosis

Hypersensitivity: Anaphylactic shock, nonimmune anaphylaxis

Nervous system: Aphasia, hemiparesis, intracranial hemorrhage, migraine, paresis, suicidal tendencies

Ophthalmic: Glaucoma, scotoma, visual field defect

Otic: Deafness, otalgia

Renal: Increased serum creatinine, renal failure syndrome, renal insufficiency

Respiratory: Pneumothorax (aggravated), pulmonary hypertension

Warnings/Precautions

Concerns related to adverse effects:

• Abnormal Schillings test: Chronic treatment has been associated with abnormal Schillings test; monitor vitamin B12 levels.

• Cholelithiasis and related complications: May impair gallbladder function (inhibits gallbladder contractility and decreases bile secretion); monitor patients for cholelithiasis. Cholelithiasis and complications of cholelithiasis (eg, cholecystitis, cholangitis, pancreatitis) requiring cholecystectomy have been reported; discontinue and treat appropriately if suspected. The incidence of gallbladder stone or biliary sludge increases with a duration of therapy of ≥12 months. Prophylactic cholecystectomy is recommended in patients with GI or pancreatic neuroendocrine tumors undergoing abdominal surgery if octreotide treatment is planned (Oberg 2004).

• Glucose regulation: Somatostatin analogs may affect glucose regulation. In type 1 diabetes, severe hypoglycemia may occur; in type 2 diabetes or patients without diabetes, hyperglycemia may occur. Insulin and other hypoglycemic medication requirements may change. Octreotide may worsen hypoglycemia in patients with insulinomas; use with caution.

• Local reactions: Mild to moderate injection-site pain (usually lasting 1 hour) may occur with the LAR depot suspension.

• Hypothyroidism: Suppresses secretion of TSH; monitor for hypothyroidism.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with heart failure or concomitant medications that alter heart rate or rhythm; bradycardia, conduction abnormalities, and arrhythmia have been observed in acromegalic and carcinoid syndrome patients. Cardiovascular medication requirements may change.

• Excessive GI fluid loss: In patients with conditions associated with excessive GI fluid loss receiving TPN, concomitant use of octreotide may reverse fluid losses and cause increases in serum zinc; monitor zinc levels (manufacturer's labeling).

• Hepatic impairment: Use caution in patients with hepatic impairment; dosage adjustment may be required in patients with established cirrhosis.

• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment may be required in patients receiving dialysis.

Concurrent drug therapy issues:

• QTc-prolonging agents: Octreotide may enhance the adverse/toxic effects of other QTc-prolonging agents.

Dosage form specific issues:

• LAR depot suspension: Do not use LAR depot suspension formulation for the treatment of sulfonylurea-induced hypoglycemia (Dougherty 2010).

• Vehicle used in LAR depot suspension (polylactide-co-glycolide microspheres): Has rarely been associated with retinal artery occlusion in patients with abnormal arteriovenous anastomosis (eg, patent foramen ovale).

Special populations:

• Elderly: Dosage adjustment may be necessary; significant increases in elimination half-life have been observed in older adults.

• Pediatric: Postmarketing cases of serious and fatal events, including hypoxia and necrotizing enterocolitis, have been reported with octreotide use in children (usually with serious underlying conditions), particularly in children <2 years of age. In studies with octreotide LAR depot suspension, the incidence of cholelithiasis in children is higher than the reported incidences for adults and efficacy was not demonstrated.

Other warnings/precautions:

• Radiolabeled diagnostic evaluations: Therapy with the octreotide injection solution formulation should be withheld 24 hours prior to administration of radiolabeled somatostatin analogs; the LAR depot suspension formulation should be withheld at least 2 months before administration of radiolabeled somatostatin analogs (Oberg 2004).

Monitoring Parameters

Acromegaly:

Initial:

Injection solution: Measure serum growth hormone (GH) every 1 to 4 hours for 8 to 12 hours post dose or a single measurement of serum insulin-like growth factor 1 (IGF-1) 2 weeks after initiation or dosage adjustment.

LAR depot suspension: Serum GH and IGF-1 at 3 months (prior to next dose).

Delayed-release capsule: Serum IGF-1 every 2 weeks initially and during dosage adjustment.

Maintenance:

Injection solution, LAR depot suspension: Serum GH and IGF-1 every 3 to 6 months.

Delayed-release capsule: Serum IGF-1 every month or as indicated.

Carcinoid: 5-HIAA, plasma serotonin and plasma substance P.

VIPomas: Vasoactive intestinal peptide.

Chronic therapy: Thyroid function (baseline and periodic); vitamin B12 level; blood glucose, glycemic control and antidiabetic regimen (patients with diabetes mellitus) should be assessed following initiation, then periodically or following dosage adjustments; cardiac function (heart rate, ECG); zinc level (patients with excessive GI fluid loss maintained on TPN); gallbladder monitoring if clinically indicated; routine gallbladder ultrasound is not considered necessary (ES [Katznelson 2014]).

Reproductive Considerations

Because normalization of insulin-like growth factor 1 and growth hormone may restore fertility in women with acromegaly, women of childbearing potential should use adequate contraception during treatment. The Endocrine Society suggests discontinuing long-acting formulations of somatostatin analogs approximately 2 months prior to a planned pregnancy; short-acting octreotide may be used until conception if needed (Endocrine Society [Katznelson 2014]). Pregnancy testing prior to administration of octreotide long-acting formulations is suggested to minimize potential fetal exposure (Abucham 2017).

Pregnancy Considerations

Octreotide crosses the placenta and can be detected in the newborn at delivery (Caron 1995; Fassnacht 2001; Maffei 2010).

Data concerning use in pregnancy are limited. In case reports of acromegalic women who received normal doses of octreotide during pregnancy, no congenital malformations were reported (Abucham 2017; manufacturer's labeling).

If treatment for acromegaly is required during pregnancy for worsening symptoms (eg, headaches or evidence of tumor growth), short-acting octreotide may be considered. Monitoring of insulin-like growth factor 1 and/or growth hormone (GH) is not recommended during pregnancy, as an active placental GH variant present in maternal blood limits the usefulness of the results (Endocrine Society [Katznelson 2014]).

Patient Education

What is this drug used for?

• It is used to treat diarrhea and flushing caused by cancer.

• It is used to treat acromegaly.

• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Abdominal pain

• Passing gas

• Nausea

• Vomiting

• Flu-like symptoms

• Headache

• Feeling dizzy, tired, or weak

• Muscle pain

• Joint pain

• Back pain

• Nose irritation

• Throat irritation

• Common cold symptoms

• Sweating a lot

• Constipation

• Diarrhea

• Hair loss

• Injection site pain

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• High blood sugar like confusion, fatigue, increased thirst, increased hunger, passing a lot of urine, flushing, fast breathing, or breath that smells like fruit

• Low blood sugar like dizziness, headache, fatigue, feeling weak, shaking, fast heartbeat, confusion, increased hunger, or sweating

• Low thyroid level like constipation; trouble handling heat or cold; memory problems; mood changes; or burning, numbness, or tingling feeling

• Gallstones like pain in the upper right abdominal area, right shoulder area, or between the shoulder blades; yellow skin or eyes; or fever with chills

• High blood pressure like severe headache or dizziness, passing out, or vision changes

• Urinary tract infection like blood in the urine, burning or painful urination, passing a lot of urine, fever, lower abdominal pain, or pelvic pain

• Pancreatitis like severe abdominal pain, severe back pain, severe nausea, or vomiting

• Chest pain

• Fast heartbeat

• Slow heartbeat

• Abnormal heartbeat

• Bloating

• Swelling

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.