octreotide

IM:

REMS

IV: SC: Treatment of the following:
- Symptoms (flushing and diarrhea) associated with metastatic carcinoid tumors;
- Profuse, watery diarrhea associated with vasoactive intestinal peptide tumors (VIPomas);
- Acromegaly in patients who have had inadequate response to or cannot be treated with surgical resection, pituitary irradiation, and bromocriptine at maximally tolerated doses.
PO: Long-term maintenance treatment of acromegaly in patients who have responded to and tolerated treatment with octreotide or lanreotide.

Unlabeled Use:

Management of diarrhea associated with chemotherapy or graft-versus-host disease.
Gastroesophageal variceal hemorrhage.

Action ⬆ ⬇

Suppresses secretion of serotonin and gastroenterohepatic peptides.
Increases absorption of fluid and electrolytes from the GI tract and increases transit time.
Decreases levels of serotonin metabolites.
Also suppresses growth hormone, insulin, and glucagon.

Therapeutic effects:

Normalization of growth hormone (GH) and insulin-like growth factor-1 (IGF-1) levels and maintenance of these levels.
Control of severe flushing and diarrhea associated with metastatic carcinoid tumors and VIPomas.

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability. Well absorbed following SUBQ administration and IM administration of depot form. Food reduces rate and extent of oral absorption.

Distribution: Some distribution to extravascular tissues.

Metabolism/Excretion: Extensive hepatic metabolism; 32% excreted unchanged in urine.

Half-Life: 1.5 hr.

Time/Action Profile ⬆ ⬇

(control of symptoms)

ROUTE	ONSET	PEAK	DURATION
SUBQ, IV	unknown	unknown	up to 12 hr
IM (LAR depot)	unknown	2 wk	up to 4 wk
PO	unknown	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity.

Use Cautiously in:

Gallbladder disease (↑ risk of stone formation);
Renal impairment (dose ↓ may be necessary);
Hyperglycemia or hypoglycemia (changes in blood glucose may occur);
Fat malabsorption (may be aggravated);
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Rep: Premenopausal women (may fertility and risk of pregnancy);
Pedi: Safety and effectiveness of depot injection and oral formulation not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, QT interval prolongation, atrioventricular block, bradycardia, hypertension, orthostatic hypotension, palpitations

Derm: ↑sweating, flushing

EENT: sinusitis, visual disturbances

Endo: hyperglycemia, hypoglycemia, hypothyroidism

GI: abdominal pain, cholelithiasis, diarrhea, nausea, vomiting, abdominal bloating, cholecystitis, fat malabsorption, flatulence, ILEUS, PANCREATITIS, steatorrhea, stool discoloration

GU: urinary tract infection

Local: injection-site pain

Metab: weight loss

MS: arthralgia

Neuro: headache, dizziness, drowsiness, fatigue, weakness.

Misc: ↓vitamin B₁₂ levels

Interactions ⬆ ⬇

Drug-drug:

May alter requirements for insulin or oral hypoglycemic agents.
May ↓ levels of cyclosporine and digoxin; closely monitor levels and adjust dose of cyclosporine and digoxin as needed.
Beta blockers, digoxin, diltiazem, ivabradine, and verapamil may ↑ risk of bradycardia.
Proton pump inhibitors, H2 receptor antagonists, and antacids may ↓ absorption and levels of orally administered octreotide; may need to ↑ dosage of oral octreotide.
May ↑ levels of lisinopril; closely monitor BP.
May ↓ levels of levonorgestrel; advise patient to use nonhormonal contraceptive or a backup method while receiving octreotide.
May ↑ levels of bromocriptine; may need to ↓ dose of bromocriptine.
May ↓ effectiveness of lutetium Lu 177 dotatate; discontinue long-acting octreotide ≥4 wk and short-acting octreotide ≥24 hr prior to each dose of lutetium Lu 177 dotatate.

Route/Dosage ⬆ ⬇

Carcinoid Tumors

SC IV (Adults ): 100–600 mcg/day in 2–4 divided doses during first 2 wk of therapy (range 50–1500 mcg/day).
IM (Adults ): Sandostatin LAR: 20 mg every 4 wk for 2 mo; dose may be further adjusted.

VIPomas

SC IV (Adults ): 200–300 mcg/day in 2–4 divided doses during first 2 wk of therapy (range 150–750 mcg/day).
IM (Adults ): Sandostatin LAR: 20 mg every 2 wk for 2 mo; dose may be further adjusted.

Acromegaly

SC IV (Adults ): 50–100 mcg 3 times daily; titrate to achieve GH levels <5 ng/mL or IGF-1 levels <1.9 units/mL (males) or <2.2 units/mL (females) (usual effective dose = 100–200 mcg 3 times daily).
IM (Adults ): Sandostatin LAR: 20 mg every 4 wk for 3 mo, then adjusted on the basis of GH levels.
PO (Adults ): 20 mg twice daily initially; titrate based on IGF-1 levels obtained every 2 wk by 20 mg/day. If maintenance dose = 60 mg/day, administer as 40 mg in am and 20 mg in pm; if maintenance dose = 80 mg/day, administer as 40 mg twice daily (not to exceed 80 mg/day).

Renal Impairment

PO (Adults ): End-stage renal disease: 20 mg once daily initially; titrate based on IGF-1 levels obtained every 2 wk by 20 mg/day. If maintenance dose = 40 mg/day, administer as 20 mg twice daily; if maintenance dose = 60 mg/day, administer as 40 mg in am and 20 mg in pm; if maintenance dose = 80 mg/day, administer as 40 mg twice daily (not to exceed 80 mg/day).

Diarrhea Associated With Chemotherapy (off-label)

SC IV (Adults ): 100–150 mcg SUBQ every 8 hr; may ↑ to 500–1500 mcg SUBQ or IV every 8 hr for severe diarrhea.
SC (Children ): 1–10 mcg/kg every 8–12 hr.

Diarrhea Associated With Graft-Versus-Host Disease (off-label)

IV (Adults ): 500 mcg every 8 hr; do not continue for longer than 7 days (discontinue within 24 hr of diarrhea resolution).
SC (Children ): 1–10 mcg/kg every 8–12 hr.

Gastroesophageal Variceal Hemorrhage (off-label)

IV (Adults ): 25–100 mcg bolus (may repeat in 1st hr if hemorrhage uncontrolled), followed by continuous infusion of 25–50 mcg/hr for 2–5 days.
IV (Children ): 1–2 mcg/kg bolus, followed by continuous infusion of 1–2 mcg/kg/hr; taper dose by 50% every 12 hr when no active bleeding for 24 hr; discontinue when dose is 25% of initial dose.

Availability ⬆ ⬇

(Generic available)

Delayed release capsules (Mycapssa): 20 mg
Solution for IV or SUBQ injection (Sandostatin): 50 mcg/mL; 100 mcg/mL; 200 mcg/mL; 500 mcg/mL; 1000 mcg/mL
Suspension for IM injection (depot) (Sandostatin LAR): 10 mg/6 mL; 20 mg/6 mL; 30 mg/6 mL

Assessment ⬆ ⬇

Assess frequency and consistency of stools and bowel sounds during therapy.
Monitor for steatorrhea (excess fat in stool), abdominal bloating, and weight loss.If new occurrence or worsening of these symptoms occurs,evaluate for pancreatic exocrine insufficiency and provide appropriate medical management.
Monitor BP and HR prior to and periodically during therapy.
Assess patient’s fluid and electrolyte balance and skin turgor for dehydration.
Monitor patients with diabetes for signs of hypoglycemia. May require ↓ in requirements for insulin and sulfonylureas and treatment with diazoxide.
Assess for right upper quadrant or radiating pain, and monitor gallbladder and bile duct ultrasound prior to and periodically during prolonged therapy.

Lab Test Considerations:

Monitor GH and IGF-1 in patients with acromegaly; 5-HIAA (urinary 5-hydroxyindoleacetic acid), plasma serotonin, and plasma substance P in patients with carcinoid tumors; plasma VIP in patients with VIPoma; and free T₄ and serum glucose concentrations prior to and periodically during therapy in all patients taking octreotide.
- Monitor quantitative 72-hr fecal fat and serum carotene determinations periodically for possible drug-induced aggravations of fat malabsorption.
- May cause a slight ↑ in liver enzymes.
- Monitor vitamin B12 during therapy (may ↓ levels).
- Monitor glycemic control for all patients with diabetes and adjust antidiabetic treatment as needed.

Implementation ⬆ ⬇

Do not confuse Sandostatin with Sandimmune. If a dose is missed, administer as soon as possible, then return to regular schedule. Do not double doses.
PO: Administer with water on an empty stomach, ≥1 hr before a meal or ≥2 hr after a meal. DNC: Swallow capsules whole; do not open, crush, or chew.
SC: Solution is clear and colorless; do not use if cloudy, discolored, or contains particulates. Ampules should be refrigerated but may be stored at room temperature for the days they will be used. Discard unused solution.Administer the smallest volume needed to achieve required dose to prevent pain at injection site. Rotate injection sites at least 2 inches away from last site; avoid multiple injections in same site within short periods of time. Preferred injection sites are the hip, thigh, or abdomen.
- Administer injections between meals and at bedtime to avoid GI side effects.
IM: Should be administered by a health care professional. Mix IM solution by adding diluent included in kit. Administer immediately after mixing into the gluteus maximus. Avoid using deltoid due to pain of injection.
- Patients with carcinoid tumors and VIPomas should continue to receive SUBQ dose for 2 wk following switch to IM depot form to maintain therapeutic level.

IV Administration:

Diluent: May be administered undiluted.
Rate: Administer over 3 min.
Intermittent Infusion: Diluent: Dilute in 50–200 mL of 0.9% NaCl or D5W.Concentration: 1.5–250 mcg/mL. Store ampules in refrigerator and keep in outer carton to protect from light.
Rate: Infuse over 15–30 min.

Patient/Family Teaching ⬆ ⬇

Explain purpose of octreotide to patient and instruct patient using injection form in correct technique, care, and disposal of equipment. Advise all patients to read Medication Guide prior to using and with each Rx refill, in case of changes.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
May cause dizziness, drowsiness, or visual disturbances. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to change positions slowly to minimize orthostatic hypotension.
Advise patient to notify health care professional if signs and symptoms of gallstones, hyperglycemia, hypoglycemia, thyroid dysfunction, or irregular heartbeat occur.
Advise patient to notify health care professional if they experience new or worsening symptoms of fat in their stool, stool discoloration, loose stools, abdominal bloating, or weight loss.
Rep: Inform females of reproductive potential that therapy with octreotide may result in improved fertility. Caution patient to use nonhormonal contraception to prevent unintended pregnancy. Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇