Description overdue on 02.02.2013

Somatotropin derivative   synthetic origin. The pharmacological effect of the active substance similar to the hormone somatostatin effect, but has a prolonged effect. The drug has a spasmolytic, antithyroid effects, reduces the secretion of hormone TSH, growth hormone, slows gastrointestinal motility and reduces the production of gastric juice, inhibits pathological hypersecretion of growth hormone, serotonin, and peptides that are produced in gastroenteritis pakreaticheskom-section of the endocrine system. Octreotide normally able to reduce production growth hormone   under stress, the action of arginine, when insulin-induced hypoglycemia .

The medicament reduces secretion of gastrin, glucagon, insulin and other peptide-pakreaticheskogo gastroenteritis card endocrine mealtime. The drug decreases the secretion of glucagon and insulin action arginine ; reduces secretion thyrotropin   under the influence of tireoliberina. Octreotide can achieve greater suppression of growth hormone secretion than somatostatin, insulin. With the introduction of the drug is not registered the phenomenon of hormone hypersecretion on a "negative feedback."

Patients with acromegaly marked reduction somatomidina A and / or growth hormone in plasma. A significant reduction in growth hormone levels (2 times or more) recorded in almost all patients, stabilization and normalization of growth hormone levels occurs in 50% of patients. The appointment of the drug Octreotide at carcinoid tumors   It leads to a decrease in the severity of symptoms of the underlying disease ("tide" of blood flow to the skin of the face, diarrhea syndrome). Positive dynamics is confirmed by a decrease in the level of serotonin in the blood and excretion of 5-HIAA in the urine. When the diagnosis of tumors, which are characterized by increased production of VIP ( vasoactive intestinal peptide ) During therapy marked improvement in the quality of life for patients by reducing the severity of symptoms of secretory diarrhea characteristic of the disease. At the same time recorded a decrease of severity of comorbidities electrolyte balance   (eg, hypoglycemia), which allows you to cancel the background of the therapy, parenteral and enteral administration of fluid and electrolytes.

Octreotide can not only slow down, but to completely stop the process of tumor progression that leads to a reduction in their size, slowing down the process of metastasis. Confirmation of positive clinical dynamics is the reduction and normalization of VIP. When glucagonomas noted a marked decrease in the severity of necrotizing migrans rash, but use of the drug Octreotide does not influence the severity of diabetes. Patients with diarrhea drug suppresses its symptoms, which leads to an increase in body weight, reduction in blood levels of glucagon. But against the background of long-term therapy, this effect is not preserved, despite the long-lasting symptomatic improvement.

With Zollinger-Ellison syndrome ( gastrinoma ) Medicament can be used alone or in combination with proton pump inhibitors and H2 receptor blockers, leading a reduction of acid secretion in the stomach .  In some patients, a decrease in the blood concentration of gastrin on background therapy .  In patients with insulinomas Octreotide is able to reduce the concentration of immunoreactive insulin (the effect may last for a short time, no more than 2 hours) .  In patients with operable tumors medication can achieve and maintain normoglycemia in the preoperative .  Patients with rare forms of tumors - somatoliberinomami, which are characterized by overproduction releasing factor growth hormone, the drug can reduce the severity of symptoms of acromegaly .  This effect is attributed to the suppression of growth hormone and its releasing factor .  Subsequently, there may be a reduction of hypertrophic pituitary .

Octreotide significantly reduces the severity of Peripheral neuropathy , Pain in the joints and bones, fatigue, paresthesia, rash, headaches. In patients with pituitary adenomas, which are characterized by hypersecretion of growth hormone, there is a decrease in tumor size in the background of the therapy. Octreotide depot is a long-acting drug, it is administered 1 to 4 times a week. The microspheres contain a polymer matrix, which is a carrier core material. Intramuscular injection of the drug provides a gradual release of the active component at the expense of long-term destruction of the microspheres in the muscle tissue. Octreotide is available in powder form and the solution is injected intramuscularly, subcutaneously, intravenously.

Indications:

Instructions for use of the drug Octreotide appoint him in acromegaly (in case of failure of radiotherapy, dopamine agonist treatment, after surgery, for inoperable patients). The drug relieves the symptoms of gastroenteritis-pancreatic tumors department endocrine system ( Zollinger-Ellison , Glucagonomas, gastrinoma, VIP Ohms, carcinoid tumors with carcinoid syndrome) somatoliberin   (tumor hypersecretion somatoliberin), insulin, persistent diarrhea in patients with AIDS. The drug is indicated for the prevention and control of bleeding in cirrhosis of the varicose veins of the esophagus (compared to endoscopic sclerotherapy). The drug is indicated for prevention of postoperative complications following surgical interventions on the pancreas.

Contraindications:

Octreotide is not indicated in case of intolerance of the basic substance. When gestation pregnancy, cholelithiasis, breast feeding, diabetes drug is prescribed with caution.

Side effect:

Abdominal pain, spastic nature, loss of appetite, stearrhea   (no malabsorption), diarrhea, flatulence, vomiting, nausea, alopecia, acute pancreatitis , Increased levels of liver enzymes, hyperbilirubinemia . With prolonged use may develop persistent hyperglycemia, reactive pancreatitis, cholelithiasis , Hypoglycemia, allergies, impaired glucose tolerance. The site of administration of the medicament possible swelling, itching, redness of the skin, burning sensation.

Overdose:

Manifested by nausea, abdominal pain of spastic origin, "tides" of blood to the face, decrease in heart rate, feeling of emptiness in the stomach. Treatment is carried out posindromno.

Mode of application:

Octreotide is administered intravenously, subcutaneously. If acromegaly   the medicament is administered subcutaneously in an initial dosage of 0, 05-0, 1 mg 8-12ch intervals. Further correction mode on the basis of monthly definitions of growth hormone levels, total portability, the analysis of clinical symptoms. The average daily dosage is 0, 2-0, 3 mg. Do not exceed the recommended maximum daily dose of 1, 5 mg. In the absence of positive dynamics within 3 months of improved clinical symptoms and reduce the required level of growth hormone treatment is stopped.

In endocrine tumors gastroenteritis-pancreatic system   Octreotide is administered subcutaneously at a dose of 0, 05 mg 1-2 times a day. Further tactics determined tolerated medication, assessment of the dynamics of changes in the level of the hormone produced by the tumor. If persistent diarrhea in patients with AIDS   preparation is administered three times a day subcutaneously in an amount of 0 1 mg. If within a week to stabilize the chair, the dose was increased to 0 and 25 mg 3 times per day. Absent further positive dynamics of octreotide treatment is stopped. After surgery on the pancreas drug indicated for the prevention of complications in a dose of 0, 1 mg 3 times a day for a week. In some cases the drug is administered 1 hour before surgery. When bleeding from the varices of the esophagus Octreotide is administered intravenously at a rate of 0, 025 mg per hour, therapy is designed for 5 days. Octreotide Depot is administered by deep intramuscular injection, alternating places for injections.

If acromegaly drug is administered 1 time per month at a dose of 20 mg, therapy is designed for 3 months. Further correction is carried out depending on the level of growth hormone IFR1, clinical symptoms. Intramuscular administration is carried out after a course of subcutaneous injections. In the absence of adequate biochemical and clinical response within three months the amount of drug increased up to 30 mg (one dose of 1 every 4 weeks). When registering a persistent decrease in serum concentrations of growth hormone at least 1mkg / l, with the disappearance of symptoms of acromegaly, with normalization of IFR1 within 3 months of therapy may reduce the dosage to 10 mg. These patients require careful monitoring. Determining the level of IFR1 held 1 time in 6 months.

The initial dosage for endocrine tumors of the gastrointestinal tract and pancreas is 20 mg (1 per month). Subcutaneous administration of the medicament is continued for 2 weeks after the initial injection. Upon reaching adequate results in terms of biological markers of the disease, the number of clinical symptoms of the drug is reduced to 10 mg (1 per month). When failure amount of drug increased up to 30 mg (one per month). During treatment, some days may increase the severity of symptoms characteristic of endocrine tumors of the pancreas, and the digestive tract. In such cases, additional intradermal medication at a dose equal to the initial one. Such phenomena are observed in the first 2 months of therapy and explains the gradual achievement of therapeutic concentrations of the active substance in the blood plasma.

Special instructions:

Patients with pituitary tumors require more careful monitoring for the early detection of tumor growth, diagnosis narrowing visual fields . For these patients require correction of treatment. Rarely during therapy Gastroenteritis-pancreatic endocrine tumors observed sudden recurrence of the underlying disease. Patients diagnosed with insulinomas during treatment may increase the duration and severity hypoglycemia . With the introduction of the drug in the bedtime or between meals severity of side effects from the gastrointestinal tract is less pronounced.

Long-term treatment of acromegaly require regular ultrasound state gallbladder . Cholelithiasis in most cases are asymptomatic, rarely resort to surgery. It is not recommended to inject at short intervals in the same place. Solution prior to administration to warm to room temperature. The use of medication during breastfeeding and gestation pregnancy only if absolutely indicated.

During treatment requires regular monitoring of blood sugar indicator, to be more careful observation, patients with cirrhosis, bleeding from varicose veins of the esophagus. Reduce blood sugar fluctuations can be more frequent administration of the drug in small doses. Octreotide Depot should not be administered intravenously. The drug is injected deep into the gluteal muscle. In case of contact with a blood vessel requires the replacement of the needle, the injection site. Octreotide can buy at any pharmacy network without a special medical form.

Drug Interactions:

Octreotide is able to slow down the rate of absorption cimetidine , Reduce the absorption cyclosporine . If necessary, therapy glucagon pereoralnymi hypoglycemic agents, diruteticheskimi medicines, BCCI, beta-blockers , Insulin requires a mandatory correction mode octreotide. The drug is able to increase the bioavailability of bromocriptine   while treatment. It is believed that somatostatin analogues slow down the metabolism of drugs that need to activate the enzyme cytochrome P450 (explained by the suppression of growth hormone). That is why the drugs with a narrow therapeutic range of doses and metabolized by cytochrome P450 with the help prescribe with caution.