Brand names: SandoSTATIN, SandoSTATIN LAR Depot, Mycapssa
Drug class: Somatostatin Agonists

Medically reviewed by Drugs.com on Jun 10, 2024. Written by ASHP.

Introduction

Synthetic polypeptide that is pharmacologically related to somatostatin; somatostatin analog.

Uses for Octreotide Acetate

Carcinoid Tumors

Symptomatic treatment to suppress or inhibit severe diarrhea and flushing associated with carcinoid tumors. Designated an orphan drug by FDA for this use.

Available in various preparations for this use, including immediate-release injection formulations for sub-Q or IV administration, and a long-acting release (LAR) injectable IM suspension for long-term treatment in patients who have responded to and tolerated the immediate-release formulation.

Potential effect on the underlying disease process remains to be elucidated; some tumor regression reported occasionally.

Effect on tumor size, rate of growth and development of metastases not determined.

Also has been used for acute management of potentially life-threatening hypotension associated with carcinoid crisis.

Has been administered prophylactically for carcinoid crisis; however, effectiveness of this strategy has been questioned.

Vasoactive Intestinal Peptide-Secreting Tumors

Management of severe diarrhea associated with vasoactive intestinal peptide (VIP)-secreting tumors.

Available in various preparations for this use, including immediate-release injection formulations for sub-Q or IV administration, and a long-acting release (LAR) injectable IM suspension for long-term treatment in patients who have responded to and tolerated the immediate-release formulation.

Effect on tumor size, rate of growth and development of metastases not determined.

Acromegaly

Treatment to reduce growth hormone (GH) and insulin-like growth factor 1 (IGF-1) blood concentrations in patients with acromegaly who have had inadequate responses to or are not candidates for surgical resection, pituitary irradiation, and bromocriptine mesylate (at maximally tolerated doses).

Available in various preparations for this use, including immediate-release injection formulations for sub-Q or IV administration and a long-acting release (LAR) injectable IM suspension for long-term treatment in patients who have responded to and tolerated the immediate-release formulation; an oral preparation (delayed-release capsules) is also available for use in patients who have responded to and tolerated treatment with octreotide or lanreotide.

Acromegaly is caused by excess circulating levels of GH and IGF-1, typically from a pituitary adenoma; surgical resection of the adenoma is generally first-line treatment of choice. Octreotide LAR or lanreotide injection generally recommended as first-line medical treatment of choice in patients with persistent disease after surgery. Switching to oral octreotide is a suitable option for patients who have demonstrated complete or partial biochemical response to these injectable agents.

Variceal bleeding† [off-label]

Has been used in adults and pediatric patients for treatment of acute variceal bleeding.^{† [off-label]} Generally administered as a continuous IV infusion for this use, with or without an initial bolus injection. Experts recommend initation of IV vasoactive drugs (e.g., octreotide, vasopressin, terlipressin) as soon as acute variceal bleeding is suspected.

Hyperinsulinaemic Hypoglycemia† [off-label]

Has been used in adults and children for treatment of hyperinsulinaemic hypoglycemia^{† [off-label]}.

Has been used for treatment of sulphonylurea-induced severe hypoglycemia^{† [off-label]} in children and adults.

Hepatorenal Syndrome†

Has been used for treatment of hepatorenal syndrome^† in combination with albumin and/or midodrine to increase effective circulating blood volume and renal blood flow in adults and children. The American Association for the Study of Liver Diseases (AASLD) states that a trial of octreotide in combination with oral midodrine may be considered when more effective alternatives (i.e., terlipressin, norepinephrine) not available.

Autosomal Dominant Polycystic Liver or Kidney Disease†

Has been used for treatment of autosomal dominant polycystic kidney or liver disease^† (designated an orphan drug by FDA for autosomal dominant polycystic liver disease). Some evidence suggests that such treatment may decrease total liver or kidney volume.

Enterocutaneous Fistulas†

Has been used for treatment of enterocutaneous fistulas^†. Somatostain analogs, including octreotide, have been shown to reduce time to fistula closure.

Gastrointestinal Angiodysplastic Lesions†

Has been used for treatment of gastrointestinal angiodysplastic lesions^†. Experts recommend use of somatostatin analogs, including octreotide, in refractory patients.

Octreotide Acetate Dosage and Administration

General

Pretreatment Screening

• Acromegaly (Sandostatin injection and generic equivalents): Obtain a baseline serum IGF-1 level.

• Acromegaly (Sandostatin LAR): For patients not currently receiving octreotide, maintain these patients on the sub-Q injection for at least 2 weeks to determine tolerance to the drug prior to switching to the LAR formulation. Patients considered to be responders based on growth hormone (GH) and IGF-1 levels and who can tolerate the drug can then be switched to the LAR formulation.

• Obtain baseline thyroid function tests (thyroid stimulating hormone [TSH], total and/or free T₄) in patients receiving chronic therapy.

Patient Monitoring

• Acromegaly (Sandostatin injection and generic equivalents): Monitor IGF-1 levels every 2 weeks after initiation of therapy or dosage changes. Response also may be evaluated by monitoring GH levels at 1–4 hour intervals for 8–12 hours post dose.

• Acromegaly (Sandostatin LAR): Monitor GH and IGF-1 levels every 3 months after drug initiation or dosage changes.

• Acromegaly (Mycapssa): Monitor IGF-1 levels and patient's signs and symptoms every 2 weeks after drug initiation, during dose titration, or as indicated. Once maintenance dosage is achieved, monitor monthly or as indicated.

• Perform periodic thyroid function tests (TSH, total and/or free T₄) during chronic therapy.

• Monitor periodically for signs and symptoms of biliary disorders.

• Monitor glucose levels periodically, when treatment is initiated, or when dosage is altered; adjust antihyperglycemic treatment as needed.

• Monitor vitamin B₁₂levels during treatment.

Administration

Administer by sub-Q, IV, IM, or oral route depending on specific use.

Administer immediate-release octreotide injection by sub-Q injection or by IV injection or infusion for symptom control in patients with acromegaly, carcinoid tumors, or VIP tumors. Sub-Q injection is the usual route of administration; IV administration generally reserved for emergency situations (e.g., acute management of carcinoid crisis).

Also available as a long-acting release (LAR) injectable suspension for IM administration in patients with acromegaly, carcinoid tumors, or VIP tumors who have responded to and tolerated the immediate-release injection; do not administer LAR formulation sub-Q or IV.

Also available as delayed-release capsules for long-term maintenance treatment of acromegaly in patients who have responded to and tolerated treatment with octreotide or lanreotide.

Sub-Q Administration

Administer immediate-release injection by sub-Q route.

To minimize pain, administer smallest volume that will deliver the desired dose; rotate injection sites in a systematic manner. Avoid multiple injections at the same site within short periods of time.

Instruct patients and/or their caregivers on proper sub-Q injection technique.

IM Administration

Administer LAR injectable suspension IM into the gluteal muscle. Alternate injection sites to minimize irritation. Injection into the deltoid muscle may cause severe discomfort and is not recommended.

IM administration of the LAR formulation may be used after tolerance established with at least 2 weeks of therapy with immediate-release injection.

Must be given under the supervision of a clinician.

Commercially available as a powder for suspension; must be reconstituted with supplied diluent prior to administration.

Prior to reconstitution, remove from refrigerator and allow drug to remain at room temperature for 30–60 minutes. Do not inject provided diluent without preparing suspension. Closely follow mixing instructions provided in the prescribing information.

IV Administration

Immediate-release injection may be diluted in 50–200 mL of 0.9% sodium chloride or 5% dextrose injection and infused over 15–30 minutes or administered by IV push over 3 minutes; such solutions are stable for 24 hours.

In emergency situations (e.g., carcinoid crisis), may be administered by rapid, direct IV (bolus) injection.

Standardize 4 Safety

Standardized concentrations for octreotide have been established through Standardize 4 Safety (S4S), a national patient safety initiative to reduce medication errors, especially during transitions of care. Because recommendations from the S4S panels may differ from the manufacturer’s prescribing information, caution is advised when using concentrations that differ from labeling, particularly when using rate information from the label. For additional information, see [Web].

Oral Administration

Administer octreotide capsules with a glass of water at least 1 hour before a meal or at least 2 hours after a meal.

Swallow intact (whole); do notcrush or chew the capsules.

Total daily dosage of 60 mg: Administer 40 mg in the morning and 20 mg in the evening.

Total daily dosage of 80 mg: Administer 40 mg twice daily.

Dosage

Available as octreotide acetate; dosage expressed in terms of octreotide.

Pediatric Patients

Variceal Bleeding†

IV

In pediatric patients^†, continuous IV infusion of 1–5 mcg/kg per hour of octreotide appears to be effective, but may require an initial bolus dose.

Adults

Carcinoid Tumors

Sub-Q

Suggested dosage during first 2 weeks of therapy is 100–600 mcg daily, given in 2–4 divided doses using the immediate-release formulation.

Median maintenance dosage (immediate-release injection) in clinical studies was approximately 450 mcg daily; however, clinical and biochemical benefits were obtained with as little as 50 mcg daily in some patients, while others required dosages up to 1500 mcg daily. Experience with dosages >750 mcg daily is limited.

If switching to the LAR injectable suspension, continue sub-Q injections with the immediate-release formulation for at least 2 weeks; thereafter, patients who tolerate and respond to the drug may be switched to the LAR formulation. Because a certain period of time is needed to reach therapeutic levels following initial injection of the LAR formulation, sub-Q therapy (immediate-release injection) should be continued for at least 2 weeks at the same dosage; some patients may require 3–4 weeks of such therapy to prevent exacerbation of disease symptoms.

IM

Patients who have responded well to at least 2 weeks of therapy with the immediate-release injection may be switched to the LAR injection administered IM at a dosage of 20 mg once every 4 weeks for 2 months. After 2 months, increase dosage to 30 mg once every 4 weeks if necessary for adequate symptom control. Dosage may be decreased to 10 mg every 4 weeks if satisfactory symptom relief is achieved with the 20-mg dose.

Safety and efficacy of LAR doses >30 mg not evaluated and not recommended.

Carcinoid Crisis (Treatment)

IV

Doses of 50–500 mcg (using immediate-release injection), repeated as necessary, have been administered by rapid IV injection.

Alternatively, IV infusions of 50 mcg/hour (using immediate-release injection) for 8–24 hours have been administered.

VIP-secreting Tumors

Sub-Q

Initiate therapy with 200–300 mcg (range 150–750 mcg) daily using the immediate-release injection, given in 2–4 divided doses, for at least 2 weeks. Individualize dosage during this period, but dosages >450 mcg daily usually not required.

If switching to the LAR injectable suspension, continue sub-Q injections with the immediate-release formulation for at least 2 weeks; thereafter, patients who tolerate and respond to the drug may be switched to the LAR formulation. Because a certain period of time is needed to reach therapeutic levels following initial injection of the LAR formulation, sub-Q therapy (immediate-release injection) should be continued for at least 2 weeks at the same dosage; some patients may require 3–4 weeks of such therapy to prevent exacerbation of disease symptoms.

IM

Patients who have responded well to at least 2 weeks of therapy with the immediate-release injection may be switched to the LAR injection administered IM at a dosage of 20 mg once every 4 weeks for 2 months. After 2 months, increase dosage to 30 mg once every 4 weeks if necessary for adequate symptom control. Dosage may be decreased to 10 mg every 4 weeks if satisfactory symptom relief is achieved with the 20-mg dose.

Safety and efficacy of LAR doses >30 mg not evaluated and not recommended.

Acromegaly

Sub-Q

Initiate therapy with 50 mcg (immediate-release injection) 3 times daily. Initiation with a low dosage promotes tolerance to adverse GI effects during titration.

Titrate dosage by tolerance, clinical effect, and evaluation of multiple GH levels. Adjust dosage based on GH levels measured at 1- to 4-hour intervals for 8–12 hours after sub-Q injection or alternatively, based on a single IGF-1 level measured 2 weeks after initiation of therapy or a dosage change.

300–600 mcg (immediate-release injection) daily given in 3 divided doses generally results in maximum effect; up to 1500 mcg daily given in 3 divided doses may be needed in some patients. Doses >300 mcg/day seldom result in additional biochemical benefit; reduce dosage if an increase in dose fails to provide additional benefit.

If patient has received pituitary irradiation, withdraw therapy for approximately 4 weeks each year to assess disease activity. If GH or IGF-1 levels increase and symptoms recur, resume therapy.

IM

Patients responding well to immediate-release injection based on GH and IGF-1 levels and who tolerate the drug may be switched to the LAR injection administered by IM injection at an initial dose of 20 mg once every 4 weeks for 3 months.

Subsequent dosage of the LAR injection is determined based on GH and IGF-1 concentrations and clinical response (see Table 2).

GH and IGF-1 measurements may be made after 3 monthly IM injections. Adjust dosage based on the GH levels taken 4 weeks after the last injection of long-acting suspension or a single IGF-1 level measured 4 weeks after the last injection of long-acting suspension.

If clinical and biochemical control is not obtained at a dosage of 30 mg once every 4 weeks, dosage may be increased to 40 mg once every 4 weeks; doses >40 mg are not recommended.

If patient has received pituitary irradiation, withdraw therapy yearly for approximately 8 weeks to assess disease activity. If GH or IGF-1 levels increase and symptoms recur, resume therapy.

Oral

Initially 20 mg twice daily.

Subsequent oral doses are determined based on IGF-1 concentrations and clinical response monitored every 2 weeks.

Titrate in increments of 20 mg daily.

For dosages of 60 mg daily, administer as 40 mg in the morning and 20 mg in the evening; the 80 mg daily dosage should be administered as 40 mg twice daily.

Maximum recommended total daily dosage is 80 mg.

If IGF-1 levels remain >ULN after treatment with the maximum recommended dosage or patient cannot tolerate treatment, consider discontinuance and switching to another somatostatin analog.

Variceal Bleeding†

IV

Has been administered as an initial IV bolus dose of 50 mcg, followed by a continuous IV infusion of 50 mcg/hour for 2 to 5 days. May give a second bolus within the first hour if bleeding is ongoing.

In randomized controlled trials, IV bolus dose has ranged from 0–100 mcg and IV infusion rates have ranged from 25–50 mcg/hour. Duration has ranged from 8 hours to 7 days.

Special Populations

Hepatic Impairment

Patients with liver cirrhosis receiving LAR injectable suspension: Initial dosage 10 mg every 4 weeks; may be titrated.

Patients with hepatic impairment receiving immediate-release injection or oral preparations: No dosage recommendations at this time.

Renal Impairment

Patients with renal failure requiring dialysis receiving LAR injectable suspension: Initial dosage should be 10 mg every 4 weeks; may titrate. In other patients with renal impairment, initial dosage should be similar to a nonrenal patient (i.e., 20 mg every 4 weeks).

Patients with renal failure requiring dialysis receiving immediate-release injection: Maintenance dosage may require adjustment.

Patients with end-stage renal disease receiving oral capsules: Initial dosage 20 mg once daily; may titrate.

Geriatric Patients

Immediate-release injection: Initiate at the low end of the dosage range.

LAR injectable suspension: Initiate at the low end of the dosage range.

Oral capsules: No dosage recommendations at this time.

Cautions for Octreotide Acetate

Contraindications

• Known hypersensitivity to octreotide or any ingredient in the formulation.

Warnings/Precautions

Warnings

Biliary Effects

Biliary abnormalities (e.g., cholelithiasis, sludge, and dilatation) occur commonly. Acute cholecystitis, ascending cholangitis, biliary obstruction, cholestatic hepatitis, and pancreatitis have been reported. Incidence related to duration of therapy; incidence not apparently related to age, sex, or dose.

Monitor periodically; discontinue and treat appropriately if complications of cholelithiasis suspected.

General Precautions

Endocrine Effects

Hypoglycemia or hyperglycemia can occur as a result of altered balance between the counter-regulatory hormones (e.g., insulin, glucagon, growth hormone). Hypoglycemia, sometimes severe, reported in patients with type 1 diabetes mellitus. Hyperglycemia reported in patients without diabetes patients and those with type 2 diabetes mellitus. Monitor blood glucose levels; adjust diabetes treatment accordingly.

Hypothyroidism may result from suppression of secretion of thyroid stimulating hormone (TSH). Perform baseline and periodic assessment of thyroid function (e.g., TSH, total and/or free thyroxine [T₄]).

Cardiovascular Effects

Higher degree or complete antrioventricular block reported following intravenous administration during surgical procedures; doses exceeded recommendations and/or were administered by continuous IV infusion. Safety of continuous IV infusion not established; consider cardiac monitoring.

Sinus bradycardia, conduction abnormalities, and arrhythmias reported in patients with acromegaly or carcinoid syndrome. ECG changes (e.g., QT prolongation, axis shifts, early repolarization, low voltage, R/S transition, early R-wave progression, and nonspecific ST-T-wave changes) reported. Dose adjustments in drugs with bradycardic effects (e.g., β-adrenergic blocking agents) may be required.

Risk of Pregnancy

Growth hormone and insulin-like growth factor-1 (IGF-1) normalization may lead to improved fertility and unintended pregnancy in female patients with acromegaly; advise female patients of child-bearing potential.

Dietary Abnormalities

Decreases in serum vitamin B₁₂ concentrations and abnormal Shilling’s test results reported; monitor vitamin B₁₂ concentrations.

Alterations in GI absorption of dietary fats reported.

Excessive increases in serum zinc concentrations may occur if octreotide is used to reduce excessive fluid loss^† from the GI tract in patients with conditions producing such a loss. Periodically monitorzinc levels in patients receiving concomitant total parenteral nutrition (TPN) and octreotide.

Immunogenicity

Up to 25% of patients develop antibodies to octreotide.

Antibodies to octreotide do not affect clinical response; some evidence from clinical studies indicates that antibodies to octreotide immediate-release injection may be associated with prolonged duration of GH suppression.

Specific Populations

Pregnancy

Limited available human data.. Animal data do not reveal harm to the fetus; growth retardation observed, possibly a consequence of growth hormone suppression. Use during pregnancy only when clearly needed.

Lactation

No data on the presence of octreotide in human milk. Consider benefits of breast-feeding and importance of octreotide to the woman along with the potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.

Females and Males of Reproductive Potential

Growth hormone and insulin-like growth factor-1 normalization may lead to improved fertility and unintended pregnancy; advise female patients of child-bearing potential.

Pediatric Use

Safety and efficacy of immediate-release, long-acting suspension, and oral preparation in pediatric patients not established. Controlled safety and effectiveness trials of immediate-release injection in pediatric patients < 6 years of age not performed. Serious adverse events, including hypoxia, necrotizing enterocolitis, and death reported postmarketing with use in children, most notably in children <2 years of age. The majority of these patients had serious underlying co-morbid conditions; relationship of such adverse events to octreotide has not been established.

Long-acting suspension investigated in pediatric patients 6–17 years of age with hypothalamic obesity^† secondary to cranial insult; efficacy not demonstrated, but new cholelithiasis reported in 33% of children.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger adults. Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.

Dcreased clearance and increased elimination half-life.

Hepatic Impairment

Prolonged half-life of immediate-release injection in patients with liver cirrhosis or fatty liver disease.

Long-acting suspension formulation has not been studied in patients with hepatic impairment; the manufacturer recommends an initial dose of 10 mg.

Renal Impairment

Half-life of immediate-release injection increased. Dosage adjustment may be necessary in patients with renal failure requiring dialysis.

Long-acting suspension formulation has not been studied in patients with renal impairment; the manufacturer recommends an initial dose of 10 mg in patients with renal failure requiring dialysis.

The manufacturer recommends 20 mg once daily as the initial dosage of the oral preparation (Mycapssa) in patients with end stage renal disease.

Common Adverse Effects

Carcinoid Syndrome

Common adverse effects (≥20%) in patients receiving LAR suspension: Back pain, fatigue, headache, abdominal pain, nausea, and dizziness.

Acromegaly

Common adverse effects (≥10%) in patients receiving immediate-release injection: Biliary tract abnormalities (gallstones, biliary sludge, duct dilatation), diarrhea, loose stools, nausea, abdominal discomfort, sinus bradycardia, hyperglycemia, and biochemical hypothryroidism.

Common adverse effects (≥20%) in patients receiving LAR injectable suspension: Diarrhea, cholelithiasis, abdominal pain, flatulence.

Common adverse effects (≥10%) in patients receiving oral capsules: Nausea, diarrhea, headache, arthralgia, asthenia, hyperhidrosis, peripheral swelling, blood glucose increased, vomiting, abdominal discomfort, dyspepsia, sinusitis, and osteoarthritis.

Drug Interactions

Not known to be metabolized by CYP isoenzymes or other drug metabolizing enzymes.

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Substrates of CYP isoenzyymes: Potential pharmacokinetic interaction (decreased substrate clearance). Caution advised if used concomitantly with CYP3A4 substrates with a low therapeutic index (e.g., quinidine); increased monitoring may be required.

Drugs Affecting Gastric Acidity

Oral preparation (Mycapssa): Potential for reduced octreotide systemic exposure. Increased dosages may be required in patients treated with drugs that alter upper gastrointestinal tract pH (e.g., proton pump inhibitors, histamine H₂-receptor antagonists, and antacids).

Drugs Associated with Bradycardia

Possible additive effect on heart rate reduction; dosage adjustment of the concomitantly administered drug may be necessary.

Effects on GI Absorption of Drugs

Possible decreased absorption of concomitant drugs.

Specific Drugs

Octreotide Acetate Pharmacokinetics

Absorption

Bioavailability

Following sub-Q injection, immediate-release formulation is rapidly and completely absorbed; peak concentrations are attained in 0.4 hours. Sub-Q and IV doses of immediate-release formulation are bioequivalent.

After IM administration of the long-acting suspension, peak plasma concentration is attained initially within 1 hour, progressively declines to a nadir within 3–5 days, and then slowly increases to a dose proportional peak concentration about 2–3 weeks post injection.

The relative bioavailability of the long-acting suspension given IM compared to the immediate-release injection given sub-Q is 60–63%. Following multiple IM injections of long-acting suspension given every 4 weeks, steady-state octreotide concentrations are achieved after the third injection.

Oral capsules: Methacrylate (Acryl-EZE) enteric-coated capsule with Transient Permeability Enhancer (TPE) technology disintegrates in the small intestine where the octreotide-TPE formulation is released into the lumen. Peak concentration attainined in 1.67–2.5 hours; metabolism and excretion expected to be identical to immediate-release sub-Q injection.

Food

Oral capsules: Rate and extent of absorption decreased 90% when administered with food.

Duration

Duration of action of immediate-release injection is variable but extends up to 12 hours depending upon the type of tumor.

Following administration of long-acting suspension, plateau plasma concentrations are maintained over a period of 2–3 weeks.

Special Populations

In patients with acromegaly, the time to peak plasma concentration is 0.7 hours following administration of immediate-release formulation.

In patients with acromegaly, plasma concentrations are dose proportional; peak plasma concentrations were lower following administration of the oral preparation.

Distribution

Extent

It is not known whether the drug is distributed into breast milk.

Plasma Protein Binding

Approximately 65% bound to plasma proteins, mainly to lipoprotein and, to a lesser extent, albumin.

Special Populations

In patients with acromegaly, plasma protein binding is 41.2%.

Elimination

Elimination Route

Approximately 32% excreted in urine as unchanged drug.

Half-life

Apparent elimination half-life is 1.7–1.9 hours.

Apparent elimination half-life is 3.2–4.5 hours following administration of the oral preparation in patients with acromegaly.

Special Populations

Following administration of the immediate-release injection, elimination half-life of 2.4, 3, or 3.1 hours reported in patients with mild renal impairment (Cl_cr 40–60 mL/minute), moderate impairment (Cl_cr 10–39 mL/minute), or severe impairment (Cl_cr <10 mL/minute), respectively.

In patients with severe renal failure requiring dialysis, clearance of immediate-release injection is decreased by approximately 50% compared with healthy individuals.

Long-acting suspension has not been studied in patients with renal or hepatic impairment.

Elimination of immediate-release injection prolonged in patients with liver cirrhosis; half-life increased to 3.7 hr. Half-life increased to 3.4 hr in patients with fatty liver disease.

In geriatric individuals, the half-life is prolonged by 46%, and the clearance is decreased by 26%.

In patients with acromegaly, disposition and elimination half-life following sub-Q injection (immediate-release preparation) are similar to healthy individuals.

Oral capsules: In patients with eGFR 15–19 mL/minute per 1.73 m², AUC and half-life increased, but not to the same extent as those requiring dialysis. In patients requiring dialysis, clearance reduced 46%, AUC increased 87%, and half-life increased 85% compared to healthy subjects.

Stability

Storage

Oral

2–8°C unopened in the original package; do not freeze.

After first-use, store opened package at 20–25°C for up to 1 month.

Parenteral

Injection

2–8°C; protect from light.

May store at 20–30°C for up to 14 days if protected from light.

May allow to come to room temperature before administration; do not warm artificially.

Open ampuls or prepare single-dose vials and syringes just prior to administration; discard unused drug.

Multiple-dose vials should be discarded within 14 days.

Diluted solutions are stable for ≥24 hours.

LAR Suspension

2–8°C; protect from light.

Product kit should remain at room temperature for 30–60 minutes before preparation of the suspension.

Actions

• Synthetic octapeptide pharmacologically related to the natural hormone somatostatin; also known as a somatostatin analog.

• More potent inhibitor of GH, glucagon, and insulin than somatostatin.

• Suppresses luteinizing hormone (LH) response to gonadotropin-releasing hormone (GnRH), decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide.

• Decreases concentrationsof GH and/or IGF-1 in patients with acromegaly.

Advice to Patients

• Advise patients and caregivers to refer to the instructions for use that accompanies the octreotide preparation.

• Advise patients and caregivers of proper sterile subcutaneous injection technique.

• Advise patients that octreotide can cause gallstones and/or complications of gallstones (e.g., cholecystitis, cholangitis, and pancreatitis) and to immediately report any signs or symptoms to their healthcare provider.

• Advise patients with carcinoid tumors or vasoactive intestinal polypeptide-secreting tumors to closely follow return visit reinjection schedule in order to minimize exacerbation of symptoms.

• Advise patients with acromegaly that growth hormone (GH) and insulin-like growth factor-1 (IGF-1) levels will be assessed periodically.

• Advise patients with acromegaly to closely follow return visit reinjection schedule in order to maintain steady control of GH and IGF-1 levels.

• Advise patients that octreotide may affect glucose regulation and to report hyperglycemia or hypoglycemia to their healthcare provider.

• Advise patients that thyroid function will be assessed periodically.

• Advise patients that bradycardia and conduction abnormalities may occur and to report an irregular heartbeat to their healthcare provider.

• Advise patients that vitamin B₁₂ levels may be monitored during treatment.

• Advise patients that hypersensitivity reactions (anaphylaxis and angioedema) are possible, and to seek prompt medical attention if an allergic reaction occurs.

• Advise patients taking the oral preparation of octreotide (Mycapssa) to take it with a glass of water on an empty stomach at least 1 hour before a meal or at least 2 hours after a meal. Swallow the capsules whole; do not crush or chew the capsules before swallowing.

• Inform female patients that treatment with octreotide may result in unintended pregnancy and to use adequate contraception during drug treatment. Advise patients taking the oral preparation of octreotide (Mycapssa) and oral contraceptives to use an alternative non-hormonal method of contraception or a back-up method.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

• Importance of informing patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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