Somatuline^® (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Ipsen Pharma (France)

Manufactured By

Ipsen Pharma Biotech (France)

ATC Code

H01CB03 (Lanreotide)

Active Substance

Lanreotide (Rec.INN registered by WHO)

Dosage Form

Somatuline®

Lyophilisate for the preparation of prolonged-release suspension for intramuscular administration 30 mg: fl. 1 pc. in a set with solvent, syringe and 2 needles

Dosage Form, Packaging, and Composition

Lyophilisate for the preparation of a prolonged-release suspension for intramuscular administration white or white with a creamy tint, dispersing in the supplied solvent to form a suspension of white or white with a creamy tint.

Excipients: copolymers (lactide-glycolide and lactide-glycolide), mannitol, sodium carboxymethylcellulose, polysorbate 80.

Solvent mannitol, water for injections (2 ml).

Glass vials (1) in a set with solvent (amp. 1 pc.) – blister packs (1) with a disposable polypropylene syringe, injection needles (2 pcs.) – cardboard packs.

Clinical-Pharmacological Group

Somatostatin analogue

Pharmacotherapeutic Group

Somatostatin (synthetic analogue)

Pharmacological Action

Synthetic peptide, which is an analogue of the natural hormone somatostatin.

Like natural somatostatin, Lanreotide suppresses pathologically increased secretion of growth hormone, as well as the secretion of many peptides and other biologically active substances produced in the gastroenteropancreatic endocrine system (including gastrin, insulin, glucagon, digestive enzymes, hydrochloric acid, vasoactive intestinal peptide, serotonin).

It has a more pronounced tropism for peripheral somatostatin receptors (pituitary and pancreatic) than for central ones. This determines its selectivity in relation to the secretion of growth hormone and the exocrine secretion of the pancreas and intestinal glands.

Pharmacokinetics

Absorption

The absorption of lanreotide is characterized by a first phase of rapid release of the peptide located on the surface of the microspheres, which is replaced by a slow second release phase. The C_max of the first phase, which is 6.8±3.8 µg/L, is noted after 1.4±0.8 h and the C_max of the second phase, which is 2.5±0.9 µg/L, is noted after 1.9±1.8 days. The absolute bioavailability is 46.1±16.7%.

Distribution

A study of the binding of lanreotide to blood components showed that such interaction is unlikely at this level.

In patients suffering from acromegaly and in healthy individuals, the pharmacokinetics are similar. At the same time, the concentrations of growth hormone and insulin-like growth factor (IGF-1) decrease for at least 14 days after a single administration of the drug. With constant administration of the drug for several months, no accumulation was noted.

Elimination

Mean residence time 8±1 days and T_1/2 5.2±2.5 days. These indicators confirm the prolonged release of the drug.

Indications

• Acromegaly;
• Carcinoid tumors (as symptomatic therapy).

ICD codes

Dosage Regimen

The use of Somatuline^® is possible only in specialized institutions. The drug is administered only intramuscularly.

Treatment begins with a test administration (in case of its ineffectiveness, further therapy is inappropriate) and the response is assessed (dynamics of growth hormone secretion, symptoms associated with carcinoid tumor).

The dosage regimen and duration of therapy are set individually.

The drug is prescribed intramuscularly at a dose of 30 mg once every 14 days. If the effectiveness is insufficient, the frequency of administration of the drug can be increased to 1 injection every 10 days.

Dissolution of the lyophilisate in the supplied solvent should be performed immediately before injection by gently shaking the contents of the vial until a homogeneous suspension of white or white with a creamy tint is obtained. The prepared suspension must not be mixed with other drugs.

Adverse Reactions

Local reactions itching, burning, moderate transient pain at the injection site, sometimes accompanied by redness.

From the digestive system diarrhea or soft stools, steatorrhea, abdominal pain, flatulence, nausea, vomiting; in rare cases, with prolonged use, the formation of gallstones (asymptomatic cholelithiasis) is possible.

From the metabolism in rare cases – increased blood glucose levels, change in glucose tolerance.

Contraindications

• Pregnancy;
• Lactation period (breastfeeding);
• Hypersensitivity to the components of the drug.

Use in Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and lactation.

Patients undergoing therapy with Somatuline^® should be warned about the possible impairment of reproductive function, as well as the advisability of using contraceptives during treatment with Somatuline^® and for 3 months after the end of treatment.

Use in Hepatic Impairment

In case of impaired liver function, the dose of the drug should be adjusted.

Use in Renal Impairment

In case of impaired renal function, the dose of the drug should be adjusted.

Special Precautions

When prescribing Somatuline^® to patients with diabetes mellitus (both type 1 and type 2), regular monitoring of blood glucose levels should be carried out and, if necessary, the dose of hypoglycemic drugs should be adjusted.

For gastrointestinal carcinoid tumors, treatment with Somatuline^® is prescribed after elimination of the existing intestinal obstruction by the tumor.

When treating acromegaly, careful monitoring of the condition of the pituitary gland is necessary.

During long-term treatment, an ultrasound of the gallbladder should be performed every 6 months.

In case of impaired liver or kidney function, the dose of the drug should be adjusted.

When co-administered with cyclosporine (orally), it is necessary to adjust the dose of cyclosporine.

Overdose

Symptoms possible intensification of manifestations of side effects from the digestive system, electrolyte disturbances.

Treatment symptomatic therapy is carried out.

Drug Interactions

With simultaneous use with insulin, its hypoglycemic effect is enhanced, which requires correction of the insulin dose.

Storage Conditions

List B. The drug should be stored out of the reach of children at a temperature from 2°C (35.6°F) to 8°C (46.4°F) (in the refrigerator).

Shelf Life

Shelf life – 2 years.

The shelf life of the prepared suspension is 6 hours when stored at room temperature.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.