Lanreotide

Class: Somatostatin Agonists
- Somatostatin Analogs
Chemical Name: [cyclo S-S]-3-(2-naphthyl)-d-alanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-lysyl-l-valyl-l-cysteinyl-l-threoninamide acetate (salt)
CAS Number: 127984-74-1
Brands: Somatuline Depot

Medically reviewed by Drugs.com on Nov 17, 2021. Written by ASHP.

• Uses
• Dosage
• Cautions
• Interactions
• Pharmacokinetics
• Patient advice
• Preparations

Introduction

Synthetic octapeptide pharmacologically related to somatostatin.

Uses for Lanreotide

Acromegaly

Long-term treatment of acromegaly in patients who have had inadequate responses to or are not candidates for surgical resection and/or radiotherapy (designated an orphan drug by FDA for this use).

Goal of therapy is to normalize concentrations of growth hormone (GH) and insulin-like growth factor 1 (IGF-1).

Improves certain manifestations of acromegaly (asthenia, joint pain, swelling of extremities, excessive perspiration, headache).

Lanreotide Dosage and Administration

General

• Individualize dosage based on patient’s response (GH and IGF-1 levels, clinical symptoms); monitor serum GH and IGF-1 concentrations and adjust dosage accordingly.

Administration

Sub-Q Administration

Administer by deep sub-Q injection into the upper outer quadrant of the buttock; alternate injection sites every 4 weeks between the right and left buttock.

Allow product to reach room temperature by removing sealed pouch from refrigerator 30 minutes prior to administration. Keep pouch sealed until time of administration.

Insert the needle rapidly to its full length at an angle perpendicular to the skin; the skin should not be folded prior to administration.

Dosage

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

Adults

Acromegaly

Sub-Q

Initially, 90 mg once every 4 weeks for 3 months.

After 3 months, adjust subsequent dosages based on response (GH and IGF-1 concentrations and clinical response) (see Table 1).

Special Populations

Hepatic Impairment

Acromegaly

Sub-Q

In patients with moderate to severe hepatic impairment, initially, 60 mg once every 4 weeks for 3 months. Subsequent dosages are determined based on GH and IGF-1 concentrations and clinical response.

Renal Impairment

Acromegaly

Sub-Q

In patients with moderate to severe hepatic impairment, initially, 60 mg once every 4 weeks for 3 months. Subsequent dosages are determined based on GH and IGF-1 concentrations and clinical response.

Geriatric Patients

Dosage adjustments not required.

Cautions for Lanreotide

Contraindications

• None.

Warnings/Precautions

Sensitivity Reactions

Latex Sensitivity

The needle cover of the prefilled syringe contains dry natural rubber (latex).

Biliary Effects

Biliary abnormalities (e.g., cholelithiasis, biliary sludge) occur commonly, possibly due to decreased gallbladder motility, inhibited gallbladder contractility, and decreased bile secretion. Incidence may be related to dose and duration of therapy. Perform gallbladder studies periodically.

Endocrine Effects

Hypoglycemia or hyperglycemia can occur as a result of inhibition of insulin and glucagon secretion. Monitor blood glucose concentrations when lanreotide therapy is initiated or dosage adjusted in patients with diabetes mellitus. Adjust dose of antidiabetic agents as necessary. (See Interactions.)

Slight decreases in thyroid function possible; hypothyroidism reported rarely. Assess thyroid function when indicated.

Cardiovascular Effects

Sinus bradycardia, bradycardia, and hypertension reported. Exercise care when initiating therapy in patients with bradycardia.

Specific Populations

Pregnancy

Category C.

Lactation

Not known whether lanreotide is distributed into milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.

Hepatic Impairment

Clearance may be decreased; dosage adjustment recommended for patients with moderate to severe hepatic impairment. (See Hepatic Impairment under Dosage and Administration and see Special Populations under Pharmacokinetics.)

Renal Impairment

Clearance may be decreased; dosage adjustment recommended for patients with moderate to severe renal impairment. (See Renal Impairment under Dosage and Administration and see Special Populations under Pharmacokinetics.)

Common Adverse Effects

Diarrhea, abdominal pain, nausea, constipation, flatulence, vomiting, cholelithiasis, injection site reactions, arthralgia, headache.

Interactions for Lanreotide

Drugs 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.

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

Lanreotide Pharmacokinetics

Absorption

Bioavailability

Mean bioavailability was 73.4, 69, and 78.4% following sub-Q administration of single 60-, 90-, and 100-mg dosages, respectively. A drug depot is formed at the injection site allowing for sustained release.

Peak levels obtained during the first day following sub-Q administration.

Duration

Serum concentrations slowly decline over 28 days with low peak to trough fluctuation noted at steady state.

Distribution

Extent

Not known whether lanreotide is distributed into milk.

Elimination

Elimination Route

<5% excreted in urine; <0.5% recovered unchanged in feces, indicating some biliary excretion.

Half-life

23–30 days following single-dose administration to healthy subjects.

Special Populations

In healthy geriatric individuals, half-life was increased by 85%.

End-stage renal disease requiring dialysis decreases clearance twofold and doubles half-life. (See Renal Impairment under Dosage and Administration.)

Moderate to severe hepatic impairment reduces clearance by 30%. (See Hepatic Impairment under Dosage and Administration.)

Stability

Storage

Parenteral

Injection

2–8°C in original package; protect from light.

Actions

• Decreases the concentration of GH and IGF-1.

• Inhibits basal secretion of several gastric enzymes (e.g., motilin, gastric inhibitory peptide, pancreatic polypeptide) and postprandial secretion of pancreatic polypeptide, gastrin, and cholecystokinin.

• Has high affinity for somatostatin receptors (SSTR) 2 and 5 in the anterior pituitary and pancreas.

Advice to Patients

• Provide copy of manufacturer’s patient information.

• Importance of advising patients to closely adhere to the schedule for return visits and lanreotide injections in order to maintain steady control of GH and IGF-1 levels.

• Importance of informing clinician if allergy to latex exists.

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

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

• Importance of informing patients of other important precautionary information. (See Cautions.)

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.

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