Lanreotide Acetate

Trade Names:
Somatuline Depot
- Injection, solution, extended-release 60 mg
- Injection, solution, extended-release 90 mg
- Injection, solution, extended-release 120 mg

Pharmacology

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Similar to the natural hormone somatostatin. Suppresses secretion of serotonin and gastroenteropancreatic peptides (eg, gastrin, glucagon, insulin, motilin, secretin). Also suppresses growth hormone (GH).

Pharmacokinetics

Absorption

After subcutaneous administration, bioavailability ranges from approximately 69% to 78%, depending on the dose. C _max ranges from 4.3 to 8.4 ng/mL during the first day. At steady state, C _max ranges from 3.8 to 7.7 ng/mL, increasing linearly with the dose. The steady-state trough serum concentration ranges from 1.8 to 3.8 ng/mL, depending on the dose. Mean serum concentration is greater than 1 ng/mL throughout 28 days with the 90 mg dose and greater than 0.9 ng/mL with 60 mg.

Elimination

The t _½ is 23 to 30 days.

Onset

Less than 5% is excreted in urine and less than 0.5% is recovered unchanged in feces, indicating some biliary excretion.

Special Populations

In patients with moderate to severe renal function impairment, reduce the starting dose to 60 mg. In patients with end-stage renal disease, there is approximately a 2-fold decrease in total serum Cl of lanreotide, with a consequent 2-fold increase in t _½ and AUC.

A 30% reduction in Cl is observed in patients with moderate to severe hepatic function impairment.

Compared with healthy young subjects, elderly subjects showed an 85% increase in t _½ and a 65% increase in mean residence time.

Indications and Usage

Long-term treatment of acromegaly in patients who have had an inadequate response to surgery and/or radiotherapy, or for whom surgery and/or radiotherapy is not an option.

Contraindications

None known.

Dosage and Administration

Subcutaneous Start with 90 mg deep subcutaneously at 4-wk intervals for 3 months. After 3 months, the dose may be adjusted as follows.

maintain dose at 90 mg every 4 wk.

Increase dose to 120 mg every 4 wk. GH 1 ng/mL or less with IGF-1 normal and clinical symptoms controlled: reduce dose to 60 mg every 4 wk.

Thereafter, adjust dose according to response of patient as judged by reduction in serum GH and/or IGF-1 levels, and/or changes in acromegaly symptoms.

Subcutaneous In patients with moderate to severe hepatic or renal function impairment, start with 60 mg at 4 wk intervals for 3 months then adjust dose as described above.

General Advice

• Administer via deep subcutaneous injection in the superior external quadrant of the buttock.
• Insert needle perpendicular to the skin, rapidly and to its full length; do not fold skin.
• Alternate between right and left side.
• Remove from refrigerator 30 minutes prior to administration and allow to come to room temperature.

Storage/Stability

Store under refrigeration at 36° to 46°F. Protect from light.

Drug Interactions

There may be an additive effect on reduction of heart rate associated with lanreotide, necessitating dosage adjustment of concurrent medication.

Availability may be increased by lanreotide.

Cyclosporine bioavailability may be reduced, necessitating cyclosporine dosage adjustments.

Cl may be reduced by lanreotide. Use drugs that have a low therapeutic index (eg, quinidine) with caution.

Insulin and glucagon secretion may be inhibited, necessitating adjustments in antidiabetic treatment.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Bradycardia (18%); hypertension (5%); sinus bradycardia (3%).

CNS

Headache (7%).

GI

Diarrhea (57%); abdominal pain (37%); nausea (11%); constipation (8%); flatulence, vomiting (7%); loose stools (6%).

Hematologic-Lymphatic

Anemia (14%).

Hepatic

Cholelithiasis and gallbladder sledge (20%).

Local

Injection-site induration, inflammation, mass, nodule, pain, or pruritus (9%).

Metabolic-Nutritional

Diabetes/hyperglycemia/hypoglycemia (14%); decreased weight (11%).

Musculoskeletal

Arthralgia (7%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Reduce starting dose in patients with moderate to severe renal function impairment.

Hepatic Function

Reduce starting dose in patients with moderate to severe hepatic function impairment.

CV abnormalities

In patients with acromegaly, the most common adverse reactions are bradycardia, sinus bradycardia, and hypertension. In patients suffering from cardiac disorders prior to treatment, sinus bradycardia may occur. Use with caution in patients with bradycardia.

Cholelithiasis

Gallbladder motility may be reduced, leading to gallstone formation; periodically monitor gallbladder function.

Hyperglycemia or hypoglycemia

Serum glucose control may be altered because of inhibition of insulin and glucagon secretion.

Latex allergy

The prefilled syringe needle cover contains rubber.

Thyroid function

Slight decreases in thyroid function have been seen during treatment in patients with acromegaly.

Overdosage

Symptoms

There are no confirmed cases of overdose that were serious or led to an adverse reaction.

Patient Information

• Advise patient to read the patient information leaflet.
• Advise patients to consult with health care provider as soon as possible if an injection is missed.
• Instruct patients to report severe pain in the right upper area of the stomach (abdomen), along with nausea and vomiting, or any other bothersome or persistent adverse reactions to health care provider.

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