Somatulin

General characteristics. Structure:

Active agent: a lanreotida acetate of 40 mg that corresponds to the maintenance of a lanreotid of 30 mg

Excipients: copolymers (lactide glycolide and laktik-glikolik), Mannitolum, sodium carboxymethylcellulose, polysorbate 80.

Solvent: Mannitolum, water for and (2 ml).

Pharmacological properties:

The synthetic peptide which is an analog of natural hormone of somatostatin.
Like natural somatostatin, ланреотид suppresses patholologically growth hormone hypersecretion, and also secretion of many peptides and other biologically active agents produced in gastro-entero-pancreatic endocrine system (including gastrin, insulin, a glucagon, digestive enzymes, hydrochloric acid, vazointestinalny peptide, serotonin).
Possesses more expressed tropnost to peripheral somatostatinovy receptors (pituitary and pancreatic), than to central. It caused its selectivity concerning secretion of a growth hormone and exocrine secretion of a pancreas and glands of intestines.

Pharmacokinetics. Absorption. Absorption of a lanreotid is characterized by the first phase of bystry release of the peptide which is on a surface of microspheres which is replaced by a slow second phase of release. Cmax of the first phase making 6.8±3.8 mkg/l is noted in 1.4±0.8 h and Cmax of the second phase making 2.5±0.9 mkg/l is noted in 1.9±1.8 days. Absolute bioavailability makes 46.1±16.7%.

Distribution. Studying of binding of a lanreotid components of blood showed that similar interaction is improbable at such level.
At the patients having an acromegalia and at healthy faces the pharmacokinetics is similar. At the same time concentration of a growth hormone and an insulinopodobny growth factor (IFR-1) decrease during, at least, 14 days after one-time administration of drug. At constant administration of drug within several months cumulation is noted.

Removal. Average time of deduction of 8±1 days and T1/2 5.2±2.5 days. These indicators confirm the prolonged drug release.

Indications to use:

— acromegalia;
— carcinoid tumors (as symptomatic therapy).

Route of administration and doses:

Somatulin's use is possible only in specialized institutions. The drug is administered only by in oil.
Treatment is begun with trial introduction (in case of its inefficiency further therapy is inexpedient) and estimate response (dynamics of secretion of growth of a growth hormone, the symptoms connected with a carcinoid tumor).
The mode of dosing and duration of therapy establish individually.

Drug appoint in oil in a dose of 30 mg of 1 times in 14 days. At insufficient efficiency it is possible to increase the frequency of administration of drug to 1 injection each 10 days.
Dissolution of lyophilisate in the enclosed solvent should be carried out just before an injection by smooth agitation of contents of a bottle before receiving homogeneous suspension of color, white or white with a creamy shade. The prepared suspension cannot be mixed with other drugs.

Features of use:

At Somatulin's appointment patients with a diabetes mellitus (both type 1, and type 2) should carry out regular control of level of glucose to blood and, if necessary, to carry out dose adjustment of hypoglycemic drugs.
At carcinoid tumors of a GIT treatment by Somatulin is appointed after elimination of the existing intestinal obstruction a tumor.
At treatment of an acromegalia careful observation of a condition of a hypophysis is necessary.
At prolonged treatment each 6 months it is necessary to make ultrasonography of a gall bladder.
At an abnormal liver function or kidneys it is necessary to adjust a drug dose.
At co-administration with cyclosporine (orally), it is necessary to carry out cyclosporine dose adjustment.

Side effects:

Local reactions: an itch, burning, the moderate passing pain in the place of an injection which sometimes is followed by a hyperemia.
From the alimentary system: diarrhea or soft chair, steatorrhea, abdominal pain, meteorism, nausea, vomiting; in rare instances at prolonged use formation of stones in a gall bladder (an asymptomatic cholelithiasis) is possible.
From a metabolism: in rare instances - increase in level of glucose in blood, change of tolerance to glucose.

Interaction with other medicines:

At simultaneous use with insulin its hypoglycemic action amplifies that demands insulin dose adjustment.

Contraindications:

— pregnancy;
— period of a lactation (breastfeeding);
— hypersensitivity to drug components.

Use of the drug SOMATULIN® at pregnancy and feeding by a breast
Drug is contraindicated to use at pregnancy and in the period of a lactation.
Patients to whom therapy by Somatulin is carried out have to be warned about possible disturbance of reproductive function, and also about expediency of use of contraceptives during treatment by Somatulin and within 3 months after the end of treatment.

Use at abnormal liver functions
At an abnormal liver function it is necessary to adjust a drug dose.

Use at renal failures
At a renal failure it is necessary to adjust a drug dose.

Overdose:

Symptoms: strengthening of manifestations of side effects from the alimentary system is possible, electrolytic disturbances.
Treatment: carry out symptomatic therapy.

Storage conditions:

List B. It is necessary to store drug in the place, unavailable to children, at a temperature from 2 ° to 8 °C (in the refrigerator).

Issue conditions:

According to the recipe

Packaging:

Lyophilisate for пригот. сусп. for introduction in oil пролонгир. actions of 30 mg: фл. 1 pieces in set. with solvent, the syringe and 2 needles.