Octreotide | Octretex ampoules 0.1 mg / ml 1 ml, 5 pcs.
Special Price
$48.76
Regular Price
$62.00
In stock
SKU
BID470644
Release form
Solution for infusion and subcutaneous injection
Packaging
5 ampoules
Pharmacological action
Octreotide - a synthetic analogue of somatostatin. It is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but a significantly longer duration of action. Octreotide suppresses the secretion of growth hormone (GH), both pathologically increased and caused by arginine, physical activity and insulin hypoglycemia. The drug also suppresses the secretion of insulin, glucagon, gastrin, serotonin, as pathologically increased, and that caused by food intake also inhibits the secretion of insulin and glucagon, stimulated by arginine. Octreotide inhibits thyrotropin secretion caused by thyroliberin.
Unlike somatostatin, octreotide suppresses the secretion of GH to a greater extent than the secretion of insulin, and its administration is not accompanied by subsequent hypersecretion of hormones (for example, GH in patients with acromegaly). In patients with acromegaly, octreotide reduces the concentration of GR and insulin-like growth factor (IGF-1) in blood plasma. A decrease in the concentration of GR by 50% or more is observed in 90% of patients, while the concentration of GR less than 5 ng / ml is achieved in about half of the patients. In most patients with acromegaly, octreotide reduces the severity of headache, soft tissue swelling, hyperhidrosis, joint pain and paresthesia. In patients with large pituitary adenomas, treatment with octreotide can lead to some reduction in tumor size.
In case of secreting tumors of the gastroenteropancreatic endocrine system in cases of insufficient effectiveness of the therapy (surgery, embolization of the hepatic artery, chemotherapy, including streptozotocin and fluorouracil), the administration of octreotide can lead to an improvement in the course of the disease. So, with carcinoid tumors, the use of octreotide can lead to a decrease in the severity of sensation of flushing of the face, diarrhea, which in many cases is accompanied by a decrease in the concentration of serotonin in the plasma and excretion of 5-hydroxyindoleacetic acid by the kidneys. In tumors characterized by hyperproduction of a vasoactive intestinal peptide (VIP), the use of octreotide in most patients leads to a decrease in severe secretory diarrhea and, accordingly, to an improvement in the quality of life of the patient. At the same time, there is a decrease in concomitant disturbances in the electrolyte balance, for example, hypokalemia, which allows you to cancel the enteral and parenteral administration of fluid and electrolytes. In some patients, the progression of the tumor slows down or stops, and its size decreases, as well as the size of the liver metastases. Clinical improvement is usually accompanied by a decrease in the concentration of VIP in plasma or its normalization. With glucagonomas, the use of octreotide leads to a decrease in migratory erythema. Octreotide does not have any significant effect on the severity of hyperglycemia in diabetes mellitus, however, the need for insulin or oral hypoglycemic drugs usually remains unchanged. The drug causes a decrease in diarrhea, which is accompanied by an increase in body weight. Although the decrease in plasma glucagon concentration under the influence of octreotide is transient in nature, clinical improvement remains stable throughout the entire period of drug administration.
In patients with gastrinomas / Zollinger-Ellison syndrome, when using octreotide as a monotherapy or in combination with proton pump inhibitors or H2 histamine receptor blockers, it is possible to reduce hypersecretion of hydrochloric acid in the stomach, the concentration of gastrin in the blood plasma, as well as a decrease in the severity of diarrhea and hot flashes . In patients with insulinomas, octreotide reduces the level of immunoreactive insulin in the blood (this effect can be short-term - about 2 hours). In patients with operable tumors, octreotide can ensure the restoration and maintenance of normoglycemia in the preoperative period. In patients with inoperable benign and malignant tumors, glycemic control may improve without a simultaneous prolonged decrease in insulin concentration in the blood.
In patients with rare tumors that hyper-produce releasing factor GH (somatoliberinomas), octreotide reduces the severity of acromegaly symptoms. This is due to the suppression of secretion of the releasing factor of GR and GR itself. In the future, pituitary hypertrophy may decrease. In case of refractory diarrhea in AIDS patients, the use of octreotide leads to complete or partial normalization of stool in approximately 1/3 of patients suffering from diarrhea that is not controlled by adequate antimicrobial and / or antidiarrheal therapy.
In patients who are scheduled for pancreatic surgery, the use of octreotide during and after surgery reduces the incidence of typical postoperative complications (e.g., pancreatic fistula, abscesses, sepsis, postoperative acute pancreatitis).
When bleeding from varicose veins of the esophagus and stomach in patients with cirrhosis of the liver, the use of octreotide in combination with specific treatment (for example, sclerotherapy) leads to a more effective stop of bleeding and early rebleeding, reduce transfusion volume and improve 5-day survival. It is believed that the mechanism of action of octreotide is associated with a decrease in organ blood flow through the suppression of vasoactive hormones such as VIP and glucagon.
Pharmacokinetics
Absorption
After s / c administration, octreotide is rapidly and completely absorbed. Tmax of octreotide in blood plasma - within 30 minutes.
Distribution of
Communication with plasma proteins is 65%. The binding of octreotide with blood cells is extremely small. Vd is 0.27 L / kg.
Excretion of
T1 / 2 after sc administration of octreotide is 100 min. After iv administration, the excretion of octreotide is carried out in 2 phases, with T1 / 2 10 and 90 min, respectively. Most of octreotide is excreted through the intestines, about 32% - unchanged by the kidneys. The total clearance is 160 ml / min. In elderly patients, the clearance of octreotide decreases, and T1 / 2 increases. In severe chronic renal failure, clearance decreases by 2 times.
Indications
acromegaly (in the absence of a sufficient effect from surgical treatment, radiation therapy (in the intervals between courses of radiation therapy until its full effect), treatment of dopamine receptor agonists in inoperable patients, as well as in patients who refuse surgical treatment)
stopping symptoms of secreting tumors of the gastroenteropancreatic endocrine system (carcinoid tumors with carcinoid syndrome, VIP, glucagon, gastrinoma / Zollinger-Ellie syndrome sleep), insulinoma, srdolkp somatoliberinoma refractory diarrhea in AIDS patients
prevention of complications after pancreatic operations
stopping bleeding and preventing recurrence of bleeding from the varicose veins of the esophagus and stomach with cirrhosis (in combination with endoscopic sclerotherapy).
Contraindications
hypersensitivity to octreotide or other components of the drug
children under 18 years of age.
Precautions: cholelithiasis (cholelithiasis) diabetes mellitus pregnancy and lactation (see. "Use during pregnancy and lactation").
Pregnancy and lactation
Experience with octreotide in pregnant women is limited. Octretex should be used during pregnancy only if the intended benefit to the mother outweighs the potential risk to the fetus.
It is not known whether the drug passes into breast milk, so if you use the drug during lactation, you should refuse to breast-feed.
Composition of
1 ampoule contains:
Active ingredient: octreotide acetate (in terms of octreotide) 0.1 mg
Excipients: lactic acid - 3.4 mg mannitol - 45 mg sodium bicarbonate - up to pH 3.9–4, 5 water for injection - up to 1 ml
Dosage and administration
s / i, drip.
Acromegaly: s / c, in an initial dose of 0.05-0.1 mg at intervals of 8 or 12 hours Further dose selection is based on monthly definitions GH blood concentration (target concentration of GR <2.5 ng / ml IGF-1 within the normal range) analysis of clinical symptoms and tolerance to the drug. In most patients, the optimal daily dose is 0.2-0.3 mg. Do not exceed the maximum dose of 1.5 mg / day. In patients receiving octreotide in a stable dose, the determination of the concentration of GR should be carried out every 6 months. If after 3 months of treatment with octreotide there is not a sufficient decrease in the concentration of GR and an improvement in the clinical picture of the disease, therapy should be discontinued.
Tumors of the gastroenteropancreatic endocrine system: sc, at an initial dose of 0.05 mg 1-2 times / day. Subsequently, depending on the achieved clinical effect, the effect on the concentration of hormones produced by the tumor (in the case of carcinoid tumors - the effect on the excretion of 5-hydroxyindoleacetic acid by the kidneys) and tolerance, the dose of the drug can be gradually increased to 0, 1–0.2 mg 3 times / day. In exceptional cases, higher doses may be required. Maintenance doses of the drug should be selected individually. In carcinoid tumors, if octreotide therapy in the maximum tolerated dose for 1 week was not effective, treatment should not be continued.
Refractory diarrhea in AIDS patients: sc, at an initial dose of 0.1 mg 3 times / day. If after 1 week of treatment the diarrhea does not subside, the dose is increased individually (subject to normal tolerance), to 0.25 mg 3 times / day. If during the week of treatment with octreotide (at a dose of 0.25 mg 3 times a day) no improvement occurs, therapy should be discontinued.
Prevention of complications after pancreatic surgery: s / c, the first dose of 0.1 mg 1 hour before laparotomy, after surgery - 0.1 mg 3 times / day for 7 consecutive days.
Bleeding from varicose veins of the esophagus and stomach: iv drip at a rate of 0.025 mg / h for 5 days.
Special patient groups
Elderly patients. Currently, there is no data that would indicate that elderly people have reduced octreotide tolerance and require a change in dosing regimen.
Impaired liver function. Correction of the maintenance dose in patients with impaired liver function is recommended.
Impaired renal function. In patients with impaired renal function, correction of the dosage regimen of octreotide is not required.
Children. Experience with octreotide in children is limited.
Terms of use of the drug
SC administration. Patients who independently conduct sc administration of octreotide should receive detailed instructions from a doctor or nurse: Before administration, warm the solution to room temperature - this helps to reduce discomfort at the injection site. Do not administer the drug at the same place with short periods of time. Ampoules should be opened immediately before drug administration. Unused amount of solution should be discarded.
IV drip. If necessary, iv drip of octreotide, the contents of one ampoule containing 0.1 mg of the active substance should be diluted in 60 ml of 0.9% sodium chloride solution. Octreotide at a temperature below 25 РC for 24 hours maintains physical and chemical stability in a sterile 0.9% sodium chloride solution or 5% dextrose solution in water. However, since octreotide can affect glucose metabolism, a 0.9% sodium chloride solution is preferred. Before iv administration, the ampoule should be carefully examined for a change in the color of the solution and the presence of foreign particles.
To avoid microbial contamination, diluted solutions should be used immediately after preparation. If the solution is not to be used immediately, it should be stored at 2–8 РC. Before administration, the solution should be warmed to room temperature. The total time between dilution, storage in the refrigerator and the end of the solution should not exceed 24 hours.
Side effects of the
From the gastrointestinal tract: very often - diarrhea, abdominal pain, nausea, constipation, bloating, cholelithiasis often - dyspepsia, vomiting, a feeling of heaviness in the abdomen, mild consistency of the stool, discoloration of the stool, anorexia, cholecystitis, violation colloidal stability of bile (formation of microcrystals of cholesterol), hyperbilirubinemia, increased activity of hepatic transaminases, steatorrhea (without malabsorption phenomena). Although the excretion of fat with feces may increase, To date, there is no evidence that prolonged treatment with octreotide can lead to nutritional deficiency due to malabsorption (malabsorption) rarely - symptoms resembling acute intestinal obstruction: progressive bloating, severe pain in the epigastric region, tension of the abdominal wall, decreased glucose tolerance (due to suppression of insulin secretion), persistent hyperglycemia, hypoglycemia, acute pancreatitis (in the first hours or days of treatment with the drug).
From the side of the liver and biliary tract: in some cases, acute hepatitis without cholestasis, hyperbilirubinemia, increased activity of hepatic transaminases (after the cancellation of octreotide, the activity of hepatic transaminases in the blood serum is normalized), alkaline phosphatase, GGT. With prolonged use, the formation of stones in the gallbladder is possible, development of reactive pancreatitis. The frequency of side effects from the gastrointestinal tract can be reduced by increasing the time intervals between meals and the administration of octreotide (see "Special Instructions").
From the nervous system: very often - headache often - dizziness.
From the endocrine system: very often - hyperglycemia often - hypothyroidism / thyroid dysfunction (decreased TSH concentration, total and free T4) hypoglycemia, impaired glucose tolerance.
On the part of the CCC: in some cases - bradycardia.
Local reactions: very often - pain, a sensation of itching or burning, redness and swelling at the site of p / injection (usually disappear within 15 minutes). The severity of local reactions can be reduced, if you use a solution of room temperature or enter a smaller volume of a more concentrated solution.
Other: rarely - skin allergic reactions in some cases - anaphylactic reactions, transient alopecia.
Drug Interaction
Reduces cyclosporine absorption, slows cimetidine absorption.
Correction of dosage regimen for simultaneous use of diuretics, -adrenoblockers, BPC, oral hypoglycemic drugs, glucagon is necessary.
The combined use of octreotide and bromocriptine increases the bioavailability of bromocriptine.
Reduces the metabolism of substances metabolized by cytochrome P450 enzymes (may be due to GR suppression). As such effects of octreotide cannot be ruled out, caution should be exercised when prescribing drugs metabolised by the cytochrome P450 system and having a narrow range of therapeutic concentrations (eg quinidine, terfenadine).
overdose
Symptoms: short-term heart rate, blood tides to the face, spastic abdominal pain, diarrhea, nausea, feeling of emptiness in the stomach.
Treatment: symptomatic.
Storage conditions
In the dark place, at a temperature of 2–8 РC (do not freeze).
Expiration
2 Year
Active substance Octreotide at
Pharmacy
Prescription
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