Somatuline Depot

Generic Name: Lanreotide Acetate
Class: Other Miscellaneous Therapeutic Agents
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

Introduction

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

Uses for Somatuline Depot

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

Somatuline Depot 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

Table 1. Adjustment of Lanreotide Dosage According to Response in Adults with Acromegaly

Response	Dosage Adjustment
GH concentration >1 to 2.5 ng/mL, normal IGF-1 concentration, and controlled clinical symptoms	Maintain dosage at 90 mg once every 4 weeks1
GH concentration ≤1 ng/mL, normal IGF-1 concentration, and controlled clinical symptoms	Reduce dosage to 60 mg once every 4 weeks1
GH concentration >2.5 ng/mL, elevated IGF-1 concentration, and/or uncontrolled clinical symptoms	Increase dosage to 120 mg once every 4 weeks1

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 Somatuline Depot

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 Somatuline Depot

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

Drug	Interaction	Comments
Antidiabetic therapy	Possible hypoglycemia or hyperglycemia1	Monitor blood glucose concentrations when lanreotide is initiated or dose altered; adjust dose of insulin and/or antidiabetic agent as necessary1
β-Adrenergic blocking agents	Possible additive bradycardia1	Dosage adjustment of β-blocker may be necessary 1
Bromocriptine	Increased bioavailability of bromocriptine1
Cyclosporine	Possible decreased cyclosporine concentrations1	Adjust cyclosporine dosage as required1
Quinidine	Possible increased quinidine concentrations1	Use with caution1
Vitamin K	No effect on vitamin K absorption1

Somatuline Depot 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

ActionsActions

• 
  

  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.

Lanreotide Acetate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	Injection, extended-release	60 mg (of lanreotide)	Somatuline Depot (available in disposable prefilled syringe)	Tercica
		90 mg (of lanreotide)	Somatuline Depot (available in disposable prefilled syringe)	Tercica
		120 mg (of lanreotide)	Somatuline Depot (available in disposable prefilled syringe)	Tercica

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions May 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Tercica. Somatuline Depot (lanreotide) injection prescribing information. Brisbane, CA; 2007 Aug.

2. Food and Drug Administration. Orphan designations pursuant to Section 526 of the Federal Food and Cosmetic Act as amended by the Orphan Drug Act (P.L. 97-414). Rockville, MD; 2007 Oct 3. From FDA web site. Accessed 2008 Jan 25

3. AACE Acromegaly Guidelines Task Force. AACE medical guidelines for clinical practice for the diagnosis and treatment of acromegaly. Endocr Pract. 2004; 10:213-25. [PubMed 15382339]

4. Chanson P, Barson-Chazott, Kuhn JM et al. Control of IGF-I levels with titrated dosing of lanreotide autogel over 48 weeks in patients with acromegaly. Clin Endocrinol (OXF). 2008; 69:299-305. [PubMed 18248639]

5. Ipsen Pharma Biotech. Somatuline Depot (lanreotide) injection patient labeling. Signes, France; 2007 Aug.

6. Croxtall JD, Scott LJ. Lanreotide Autogel: a review of its use in management of acromegaly. Drugs. 2008; 68:711-23. [PubMed 18370450]

7. Murray RD, Melmed S. A critical analysis of clinically available somatostatin analog formulations for therapy of acromegaly. Clin Endocrinol Metab. 2008; 93:2957-68.

8. Croxtall JD, Scott LJ. Spotlight on lanreotide autogel in acromegaly. Biodrugs. 2008; 22:275-7. [PubMed 18611070]

9. Melmed S. Acromegaly. N Engl J Med. 2006; 355:2558-73. [PubMed 17167139]

10. Terica, Brisbane, CA: Personal communication.

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