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. Last updated on Nov 17, 2020.

• Overview
• Side Effects
• Dosage
• Professional
• Interactions
• More

Introduction

Synthetic octapeptide pharmacologically related to somatostatin.^{1 6 8}

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).^{1 2}

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

Improves certain manifestations of acromegaly (asthenia, joint pain, swelling of extremities, excessive perspiration, headache).⁴

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.^{1 9}

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.^{1 5}

Allow product to reach room temperature by removing sealed pouch from refrigerator 30 minutes prior to administration.¹ Keep pouch sealed until time of administration.¹

Insert the needle rapidly to its full length at an angle perpendicular to the skin; the skin should not be folded prior to administration.¹

Dosage

Available as lanreotide acetate; dosage expressed in terms of lanreotide.¹

Adults

Acromegaly

Sub-Q

Initially, 90 mg once every 4 weeks for 3 months.¹

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

Renal Impairment

Acromegaly

Sub-Q

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

Geriatric Patients

Dosage adjustments not required.¹

Cautions for Lanreotide

Contraindications

• None.¹

Warnings/Precautions

Sensitivity Reactions

Latex Sensitivity

The needle cover of the prefilled syringe contains dry natural rubber (latex).¹

Biliary Effects

Biliary abnormalities (e.g., cholelithiasis, biliary sludge) occur commonly,¹ possibly due to decreased gallbladder motility, inhibited gallbladder contractility, and decreased bile secretion.¹ Incidence may be related to dose and duration of therapy.¹ Perform gallbladder studies periodically.¹

Endocrine Effects

Hypoglycemia or hyperglycemia can occur as a result of inhibition of insulin and glucagon secretion.¹ Monitor blood glucose concentrations when lanreotide therapy is initiated or dosage adjusted in patients with diabetes mellitus.^{1 10} Adjust dose of antidiabetic agents as necessary.¹ (See Interactions.)

Slight decreases in thyroid function possible; hypothyroidism reported rarely.¹ Assess thyroid function when indicated.¹

Cardiovascular Effects

Sinus bradycardia, bradycardia, and hypertension reported.¹ Exercise care when initiating therapy in patients with bradycardia.¹

Specific Populations

Pregnancy

Category C.¹

Lactation

Not known whether lanreotide is distributed into milk. ¹ Discontinue nursing or the drug. ¹

Pediatric Use

Safety and efficacy not established.¹

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.¹

Hepatic Impairment

Clearance may be decreased; dosage adjustment recommended for patients with moderate to severe hepatic impairment.¹ (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.¹ (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.¹

Interactions for Lanreotide

Drugs Metabolized by Hepatic Microsomal Enzymes

Substrates of CYP isoenzyymes: Potential pharmacokinetic interaction (decreased substrate clearance).¹ Caution advised if used concomitantly with CYP3A4 substrates with a low therapeutic index.¹

Drugs Associated with Bradycardia

Possible additive effect on heart rate reduction; dosage adjustment of the concomitantly administered drug may be necessary.¹

Effects on GI Absorption of Drugs

Possible decreased absorption of concomitant drugs.¹

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.¹ A drug depot is formed at the injection site allowing for sustained release.¹

Peak levels obtained during the first day following sub-Q administration.¹

Duration

Serum concentrations slowly decline over 28 days with low peak to trough fluctuation noted at steady state.¹

Distribution

Extent

Not known whether lanreotide is distributed into milk. ¹

Elimination

Elimination Route

<5% excreted in urine; <0.5% recovered unchanged in feces, indicating some biliary excretion.¹

Half-life

23–30 days following single-dose administration to healthy subjects.¹

Special Populations

In healthy geriatric individuals, half-life was increased by 85%.¹

End-stage renal disease requiring dialysis decreases clearance twofold and doubles half-life.¹ (See Renal Impairment under Dosage and Administration.)

Moderate to severe hepatic impairment reduces clearance by 30%.¹ (See Hepatic Impairment under Dosage and Administration.)

Stability

Storage

Parenteral

Injection

2–8°C in original package; protect from light.¹

Actions

• Decreases the concentration of GH and IGF-1.^{1 8}

• Inhibits basal secretion of several gastric enzymes (e.g., motilin, gastric inhibitory peptide, pancreatic polypeptide) and postprandial secretion of pancreatic polypeptide, gastrin, and cholecystokinin.^{1 8}

• Has high affinity for somatostatin receptors (SSTR) 2 and 5 in the anterior pituitary and pancreas.^{1 6 8}

Advice to Patients

• Provide copy of manufacturer’s patient information.¹

• 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.⁵

• Importance of informing clinician if allergy to latex exists.⁵

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.^{1 5}

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. ^{1 5}

• Importance of informing patients of other important precautionary information.¹ (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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