lanreotide (Rx)

>10%

Abdominal pain (19%)

Cholelithiasis (20%)

Diarrhea (57%)

Nausea (11%)

Bradyarrhythmia (5% to 18% )

Injection site reaction (subcutaneous depot, 6% to 22% ; intramuscular, up to 50% )

Flatulence (up to 14% )

Anemia (3% to 14% )

1-10%

Arthralgia (7%)

Constipation (8%)

Headache (7%)

Loose stools (6%)

Vomiting (7%)

Hyper-/hypoglycemia/diabetes (7%)

Sinus bradycardia (3%)

<1%

Injection site pruritus

Steatorrhea

Aortic valve regurgitation

Allergic skin reaction

Mitral valve regurgitation

Pancreatitis

Postmarketing Reports

Angioedema

Anaphylaxis

Gastrointestinal disorders: Abdominal pain, diarrhea, and steatorrhea

Hepatobiliary disorders: Cholecystitis, pancreatitis

General disorders and administration site conditions: Injection site reactions

Cardiac: Hypertension

Injection site reacsions: Injection site abscess

Contraindications

Hypersensitivity to lanreotide

Cautions

Risk of reducing gallbladder motility, which could lead to gallstone formation; monitor periodically

Inhibition of insulin and glucagon secretion; may affect glucose regulation, which can lead to hyper-hypoglycemia; glucose monitoring is recommended; adjust antidiabetic treatment accordingly

Decreases in thyroid function reported; thyroid function tests are recommended where clinically indicated

Bradycardia, hypertension, and sinus bradycardia reported; use with caution in at-risk patients; initiate appropriate medical management in patients who develop symptomatic bradycardia

Pharmacological gastrointestinal effects of lanreotide may reduce the intestinal absorption of concomitant drugs; lanreotide may decrease the relative bioavailability of cyclosporine; concomitant administration of lanreotide and cyclosporine may necessitate the adjustment of cyclosporine dose to maintain therapeutic levels

Cholelithiasis (gallstones) resulting in complications, including cholecystitis, cholangitis, and pancreatitis, and requiring cholecystectomy reported; if complications of cholelithiasis are suspected, discontinue therapy and treat appropriately

Use caution in renal/hepatic impairment, diabetes

Pregnancy

Limited available data based on postmarketing case reports, use in pregnant women are not sufficient to determine a drug-associated risk of adverse developmental outcomes

A reproductive study in pregnant rats given 30 mg/kg of lanreotide by subcutaneous injection every 2 weeks (5 times the human dose, based on body surface area comparisons) resulted in decreased embryo/fetal survival

Lactation

There is no information available on presence of lanreotide in human milk, effects of drug on breastfed infant, or on milk production; studies show that lanreotide acetate administered subcutaneously passes into the milk of lactating rats; due to specifies-specific differences in lactation physiology, animal data may not reliably predict drug levels in human milk

Because of potential for serious adverse reactions in breastfed infants, including effects on glucose metabolism and bradycardia, advise women not to breastfeed during treatment and for 6 months (6 half-lives) following the last dose

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Analog of somatostatin, which is a peptide inhibitor of multiple endocrine, neuroendocrine, and exocrine mechanisms

Absorption

Peak plasma concentration (single dose): 3.8 ng/mL (60 mg-dose); 5.7 ng/mL (90 mg-dose); 7.7 ng/mL (120 mg-dose)

Peak plasma time: 7-12 hr

Distribution

Protein binding: 79-83%

Vd: 0.2 L/kg

Bioavailability: ~69-83%

Metabolism

Half-Life: 23-36 days

Excretion: Urine (<5%); feces (<0.5%)

SC Preparation

Remove lanreotide from refrigerator 30 minutes prior to administration; allow to come to room temperature

Visually inspect injection for particulate matter and discoloration

Do not administer if particulate matter or discoloration is observed

SC Administration

Administer as a deep SC injection only in the superior external quadrant of the buttock

Alternate the injection site between the right and left sides from one injection to another

Storage

Store in refrigerator at 2-8°C (36- 46°F)

Protect from light

Store in the original package