No

Antidiarrheal; Antisecretory Agent; Somatostatin Analog

Control of symptoms in patients with metastatic carcinoid and vasoactive intestinal peptide-secreting tumors (VIPomas); pancreatic tumors, gastrinoma, secretory diarrhea, acromegaly

B

Known hypersensitivity to octreotide or any component

Dosage adjustment may be required to maintain symptomatic control; insulin requirements may be reduced as well as sulfonylurea requirements; monitor patients for cholelithiasis, hyper- or hypoglycemia; use with caution in patients with renal impairment

1% to 10%:

Cardiovascular: Flushing, edema

Central nervous system: Fatigue, headache, dizziness, vertigo, anorexia, depression

Endocrine & metabolic: Hypoglycemia or hyperglycemia (1%), hypothyroidism, galactorrhea

Gastrointestinal: Nausea, vomiting, diarrhea, constipation, abdominal pain, cramping, discomfort, fat malabsorption, loose stools, flatulence

Hepatic: Jaundice, hepatitis, increase LFTs, cholelithiasis has occurred, presumably by altering fat absorption and decreasing the motility of the gallbladder

Local: Pain at injection site (dose-related)

Neuromuscular & skeletal: Weakness

<1%: Chest pain, hypertensive reaction, anxiety, fever, hyperesthesia, alopecia, wheal/erythema, rash, thrombophlebitis, leg cramps, Bell's palsy, muscle cramping, burning eyes, throat discomfort, rhinorrhea, shortness of breath

Symptoms of overdose include hypo- or hyperglycemia, blurred vision, dizziness, drowsiness, loss of motor function; well tolerated bolus doses up to 1000 mcg have failed to produce adverse effects

CYP2D6 (high dose) and 3A enzyme inhibitor

Octreotide is a clear solution and should be stored under refrigeration; ampuls may be stored at room temperature for up to 14 days when protected from light

Common diluent: 50-100 mcg/50 mL NS; common diluent for continuous I.V. infusion: 1200 mcg/250 mL NS

Minimum volume: 50 mL NS

Mimics natural somatostatin by inhibiting serotonin release, and the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide

Duration of action: 6-12 hours (S.C.)

Absorption: Oral: Absorbed but still under study; S.C.: Rapid

Bioavailability: S.C.: 100%

Distribution: V_d: 14 L; 65% bound to lipoproteins

Metabolism: Extensive by the liver

Half-life: 60-110 minutes

Elimination: 32% by the kidney

Adults: S.C.: Initial: 50 mcg 1-2 times/day and titrate dose based on patient tolerance and response

VIPomas: 200-300 mcg/day in 2-4 divided doses

Diarrhea: Initial: I.V.: 50-100 mcg every 8 hours; increase by 100 mcg/dose at 48-hour intervals; maximum dose: 500 mcg every 8 hours

Esophageal varices bleeding: I.V. bolus: 25-50 mcg followed by continuous I.V. infusion of 25-50 mcg/hour

Acromegaly, carcinoid tumors, and VIPomas (depot injection): Patients must be stabilized on subcutaneous octreotide for at least 2 weeks before switching to the long-acting depot: Upon switch: 20 mg I.M. intragluteally every 4 weeks for 2-3 months, then the dose may be modified based upon response

Dosage adjustment for acromegaly: After 3 months of depot injections the dosage may be continued or modified as follows:

GH less than or equal to 2.5 ng/mL, IGF-1 is normal, symptoms are controlled: Maintain octreotide LAR® at 20 mg I.M. every 4 weeks

GH >2.5 ng/mL, IGF-1 is elevated, or symptoms: Increase octreotide LAR® to 10 mg I.M. every 4 weeks

GH less than or equal to 1 ng/mL, IGF-1 is normal, symptoms controlled: Reduce octreotide LAR® to 10 mg I.M. every 4 weeks

Dosages >40 mg are not recommended

Dosage adjustment for carcinoid tumors and VIPomas: After 2 months of depot injections the dosage may be continued or modified as follows:

Increase to 30 mg I.M. every 4 weeks if symptoms are inadequately controlled

Decrease to 10 mg I.M. every 4 weeks, for a trial period, if initially responsive to 20 mg dose

Dosage >30 mg is not recommended

Schedule injections between meals to decrease GI effects

Vasoactive intestinal peptide: <75 ng/L; levels vary considerably between laboratories

May cause drowsiness, dizziness, or depression; may rarely cause anxiety

None reported

No information available to require special precautions

No effects or complications reported

Schedule injections between meals to decrease GI effects. May affect dietary fat and vitamin B₁₂. Consult prescriber about appropriate diet. Diabetic patients should monitor serum glucose closely (this drug may increase the effects of insulin or sulfonylureas); report abnormal glucose levels so appropriate adjustment can be made. You may experience skin flushing; nausea or vomiting (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); dizziness, fatigue, or drowsiness (use caution when driving or engaging in tasks that require alertness until response to drug is known). Report weight gain, swelling of extremities, or respiratory difficulty; acute or persistent GI distress (eg, diarrhea, vomiting, constipation, abdominal pain); muscle weakness or tremors or loss of motor function; chest pain or palpitations; blurred vision; pain, redness, or swelling at injection site; or emotional depression. Breast-feeding precautions: Do not breast-feed.

Do not use if solution contains particles or is discolored

Injection: 0.05 mg/mL (1 mL); 0.1 mg/mL (1 mL); 0.2 mg/mL (5 mL); 0.5 mg/mL (1 mL); 1 mg/mL (5 mL)

Injection, suspension, depot: 10 mg (5 mL); 20 mg (5 mL); 30 mg (5 mL)

Couper RT, Berzen A, Berall G, et al, "Clinical Response to the Long-Acting Somatostatin Analogue SMS 201-995 in a Child With Congenital Microvillus Atrophy," Gut, 1989, 30(7):1020-4.

Jaros W, Biller J, Greer S, et al, "Successful Treatment of Idiopathic Secretory Diarrhea of Infancy With the Somatostatin Analogue SMS 201-995," Gastroenterology, 1988, 94(1):189-93.

Jenkins SA, "Somatostatin in Acute Bleeding Oesophageal Varices. Clinical Evidence" Drugs, 1992, 44(Suppl 2):36-55.

Katz MD and Erstad BL, "Octreotide, A New Somatostatin Analogue," Clin Pharm, 1989, 8(4):255-73.