Octreotide - Instructions For Use, Price, Reviews, Drug Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Octreotide

Octreotide: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Octreotide

ATX code: H01CB02

Active ingredient: octreotide (octreotide)

Producer: F-Sintez, CJSC (Russia), Pharmstandard-UfaVITA (Russia), Nativa, LLC (Russia), Deco company (Russia), ALTAIR (Russia)

Description and photo update: 2019-02-09

Prices in pharmacies: from 999 rubles.

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Octreotide is a somatostatin-like drug.

Release form and composition

Dosage form - solution for intravenous and subcutaneous administration: transparent, colorless, odorless [1 ml in ampoules: at a dose of 50 and 100 mcg / ml - 5 ampoules in blisters, in a cardboard box 1 or 2 packages; at a dose of 300 and 600 mcg / ml - 1, 2 or 5 ampoules in blisters, in a carton pack 1 (1, 2 or 5 ampoules) or 2 (5 ampoules) packaging; each pack also contains instructions for the use of Octreotide].

The active ingredient is octreotide (in the form of acetate), its content in 1 ml of solution is 50, 100, 300 or 600 mcg.

Inactive ingredients: sodium chloride and injection water.

Pharmacological properties

Pharmacodynamics

Octreotide is a synthetic analogue of somatostatin, has pharmacological effects similar to it, but a long duration of action is observed.

Octreotide helps to suppress the secretion of the following substances:

• Growth hormone: pathologically elevated or induced by exercise, arginine and insulin hypoglycemia;
• Insulin, glucagon, gastrin, serotonin: pathologically elevated or caused by food intake;
• Insulin, glucagon: stimulated with arginine;
• Thyrotropin: caused by thyroliberin.

The use of octreotide before, during and after pancreatic surgery can reduce the incidence of typical postoperative complications, in particular abscesses, sepsis, pancreatic fistulas, and acute postoperative pancreatitis.

With bleeding from varicose veins of the stomach and esophagus and with cirrhosis of the liver, due to the use of octreotide in combination with specific therapy (in particular with hemostatic and sclerosing treatment), a more effective stopping of bleeding is observed. Octreotide is also used to prevent re-bleeding.

Pharmacokinetics

Octreotide is rapidly and completely absorbed after subcutaneous administration. C _max (maximum concentration of the substance) of octreotide in blood plasma is reached in 30 minutes.

The level of binding to plasma proteins is 65%. The substance binds to the formed elements of the blood to an extremely insignificant extent. V _d (volume of distribution) - 0.27 l / kg.

T _1/2 (half-life) after subcutaneous administration is 100 minutes. Excretion of octreotide after intravenous administration is carried out in two phases with T _{1/2 of} 10 minutes (first phase) and 90 minutes (second phase). Most of the substance is excreted through the intestines, approximately 32% of the dose is excreted by the kidneys unchanged. The total clearance is 160 ml / min.

In elderly patients, clearance decreases, and T _1/2 increases.

In patients with severe renal failure, clearance is reduced by 2 times.

Indications for use

• Stopping bleeding from varicose veins of the esophagus and stomach in patients with liver cirrhosis and prevention of recurrence (in combination with endoscopic sclerotherapy or other specific therapeutic measures);
• Acromegaly - to control the symptoms of the disease and reduce insulin-like growth factor-1 (IGF-1) and growth hormone in blood plasma in cases where the effect of radiation or surgical treatment is not enough; for the treatment of the disease in cases where the patient has refused the operation or has contraindications to its conduct; for short-term treatment in the intervals between courses of radiation therapy until the effect of its implementation is obtained;
• Secreting endocrine tumors of the pancreas and gastrointestinal tract (to control symptoms): glucagonomas, somatoliberinomas, VIPomas, carcinoid tumors with carcinoid syndrome, insulinomas (for maintenance therapy, as well as for the control of hypoglycemia in the preoperative period), gastrinomas and syndrome Ellison (usually in combination with histamine H ₂ receptor blockers and proton pump inhibitors);
• Treatment of acute pancreatitis;
• Treatment and prevention of complications after surgical interventions on the abdominal organs;
• Stopping bleeding in case of gastric ulcer and duodenal ulcer.

Contraindications

The use of Octreotide is strictly contraindicated in children and adolescents under 18 years of age, as well as in all patients who have hypersensitivity to any component of the drug.

The drug must be used with caution in the treatment of patients with diabetes mellitus and cholelithiasis (cholelithiasis).

The effect of the drug on the course of pregnancy has not been studied, so its use is possible only in extreme cases, if the intended benefits outweigh the possible risks.

It is not known whether octreotide penetrates into breast milk; therefore, it is recommended to stop breastfeeding during treatment.

Octreotide, instructions for use: method and dosage

Octreotide is intended for subcutaneous (subcutaneous) and intravenous (iv) administration.

Prescribed dosage regimens depending on indications and purpose of use:

• Treatment of acute pancreatitis: 100 mcg s / c 3 times a day for 5 days. In some cases, the doctor may advise the intravenous administration of the drug in a daily dose of up to 1200 mcg;
• Prevention of complications after surgery on the pancreas: 100-200 mcg sc. The first dose is administered 1-2 hours before laparotomy, after surgery - 3 times a day for 5-7 days;
• Stopping ulcerative bleeding: 25-50 mcg / hour as an intravenous infusion, course - 5 days;
• Stopping bleeding from varicose veins of the esophagus and stomach: 25-50 mcg / hour as a continuous intravenous infusion, the course of treatment is 5 days;
• Acromegaly: The initial dose is 50-100 mcg s / c every 8 or 12 hours. In case of ineffectiveness (the target concentration of growth hormone is less than 2.5 ng / ml, and the IGF-1 index is within the normal range), a single dose is increased to 300 μg. The maximum allowable daily dose is 1500 mcg. In patients receiving a stable dose of octreotide, growth hormone levels should be measured every 6 months. If after 3 months of treatment there is no sufficient decrease in this indicator and an improvement in the clinical course of the disease, Octreotide should be canceled;
• Tumors of the gastroenteropancreatic endocrine system: the initial dose is 50 mcg 1-2 times a day, if necessary, it is gradually increased to 100-200 mcg 3 times a day s / c. In case of ineffectiveness (assessed on the basis of data on the achieved clinical effect, the concentration of hormones that produce the tumor, and the tolerability of the drug), the dose is increased to 300 μg s / c 1-2 times a day. In exceptional cases, an even greater dose increase is possible - up to 300-600 mcg 3 times a day. The doctor selects the maintenance doses for each patient individually. If therapy in the maximum tolerated dose is ineffective for 1 week with carcinoid tumors, Octreotide is discontinued.

Patients with impaired liver function require maintenance dose adjustment.

Rules for subcutaneous administration of Octreotide:

• Carefully inspect the ampoule for the presence of impurities in the solution and color changes;
• Heat the ampoule to room temperature;
• Open the ampoule just before administration;
• Throw away the unused amount of solution;
• Do not inject in the same place at short intervals.

Intravenous drip rules:

• Carefully inspect the ampoule for the presence of impurities and discoloration;
• Heat the solution to room temperature;
• For dilution, use 0.9% sodium chloride (for example, 1 ampoule of 600 μg is diluted with 60 ml of saline);
• Prepare an injection solution immediately before administration;
• If necessary, store no more than 24 hours after reconstitution in a refrigerator (at a temperature of 2 to 8 ºС).

Side effects

Criteria for assessing the incidence of side effects: very often - not more often than in 1 case out of 10, often - ≥1 / 100, but <1/10, sometimes - ≥1 / 1000, but <1/100.

Adverse reactions identified during clinical trials of Octreotide:

• From the digestive system: very often - diarrhea or constipation, bloating, nausea, abdominal pain; often - steatorrhea, stool discoloration, feeling of fullness or heaviness in the abdomen, soft stool consistency, dyspeptic disorders, anorexia, vomiting;
• From the hepatobiliary system: stones in the gallbladder (cholelithiasis); often - increased activity of hepatic transaminases, cholecystitis, hyperbilirubinemia, the formation of cholesterol microcrystals due to a violation of the colloidal stability of bile;
• From the side of the cardiovascular system: often - bradycardia; sometimes - tachycardia;
• From the endocrine system: very often - hyperglycemia; often - hypoglycemia, impaired glucose tolerance, hypothyroidism, dysfunction of the thyroid gland (manifested by a decrease in the levels of thyroid-stimulating hormone, total and free thyroxine);
• From the respiratory system: often - shortness of breath;
• From the nervous system: very often - headache; often - dizziness;
• Dermatological reactions: often - rash, itching, hair loss;
• Local reactions: very often - pain at the injection site;
• Others: sometimes - dehydration.

The causal relationship of the following side effects with the use of Octreotide has not been established:

• From the hepatobiliary system: cholestasis, jaundice, cholestatic hepatitis, acute hepatitis without cholestasis, cholestatic jaundice, acute pancreatitis, increased levels of gamma-glutamyltransferase and alkaline phosphatase;
• From the immune system: hypersensitivity reactions, anaphylactic reactions;
• From the side of the cardiovascular system: arrhythmias;
• Dermatological reactions: urticaria.

Overdose

The main symptoms: a feeling of flushing of the face, a short-term decrease in the heart rate, spastic abdominal pain, a feeling of emptiness in the stomach, nausea, diarrhea.

Therapy: symptomatic.

special instructions

Women of childbearing age with acromegaly should use reliable contraceptive methods during therapy. with a decrease in the level of growth hormone and normalization of the level of IGF-1 under the influence of octreotide, it is possible to restore fertility.

With long-term treatment, it is necessary to monitor the function of the thyroid gland.

In patients with a history of vitamin B ₁₂ deficiency, it is necessary to monitor the content of cobalamin in the body.

Before prescribing Octreotide, patients should be referred for ultrasound examination of the gallbladder. If stones are found, the drug can be prescribed after a careful assessment of the expected benefits of therapy and the possible risks. Re-examinations should be carried out every 6-12 months during treatment.

If stones are detected during treatment:

• Asymptomatic: you can discontinue the drug or continue therapy after assessing the benefit / risk ratio. There is no need to take any action, more frequent observation is required;
• With clinical symptoms: you can cancel the drug or continue treatment after assessing the benefit / risk ratio. Patients need standard therapy for gallstone disease (including bile acid preparations) and regular ultrasound monitoring.

Patients with growth hormone-secreting pituitary tumors require close medical supervision during treatment, as the drug can increase the size of the tumor and develop a serious complication such as narrowing of the visual fields. If this happens, it is necessary to consider the use of other methods of treatment.

Octreotide can interfere with the absorption of fats in the intestines.

With the development of bradycardia, it is necessary to consider the possibility of reducing the dose of calcium channel blockers, beta-blockers or drugs that affect the water-electrolyte balance.

It should be remembered that Octreotide is not an antineoplastic agent, therefore it does not contribute to the healing of secreting endocrine tumors of the pancreas and gastrointestinal tract.

In the treatment of endocrine tumors of the gastrointestinal tract and pancreas, in some cases, a sudden relapse is possible. With the development of insulinoma during the use of octreotide, an increase in the duration and severity of hypoglycemia is possible. Such patients should be closely monitored, especially with each change in the dose of the drug.

Octreotide affects blood glucose concentration. It is possible to reduce fluctuations due to the more frequent administration of the drug in lower doses. In type 1 diabetes mellitus, the drug can reduce the need for insulin, in type 2 diabetes (with partially preserved insulin secretion) and in patients without diabetes, it can lead to the development of postprandial hyperglycemia. For this reason, patients with diabetes mellitus need control of blood glucose levels and antidiabetic therapy.

Patients also need to control the concentration of glucose in the blood after bleeding from varicose veins of the stomach or esophagus, since in this case the risk of developing type 1 diabetes mellitus increases.

Influence on the ability to drive vehicles and complex mechanisms

Due to the risk of developing side effects from the central nervous system, it is recommended to be careful when driving a car and performing any work that requires increased attention and speed of reactions.

Application during pregnancy and lactation

• Pregnancy: the use of Octreotide is possible only for strict indications after assessing the ratio of the expected benefit with the possible risk;
• Lactation period: therapy is contraindicated.

Pediatric use

Octreotide is not prescribed for patients under 18 years of age.

With impaired renal function

There is no need to adjust the dose of Octreotide in patients with impaired renal function.

For violations of liver function

Correction of the maintenance dose of Octreotide is recommended for patients with impaired hepatic function.

Use in the elderly

Elderly patients do not require dosage adjustment.

Drug interactions

Care should be taken to simultaneously use drugs that are metabolized by the cytochrome P _{450 system} and have a narrow range of therapeutic concentrations (for example, quinidine or terfenadine), because the likelihood of developing side effects increases.

Octreotide reduces the absorption of cyclosporine, increases the bioavailability of bromocriptine, slows down the absorption of cimetidine, and reduces the metabolism of drugs that are metabolized with the participation of enzymes of the cytochrome P _{450 system}.

In the case of the simultaneous use of the following drugs, their doses must be adjusted: insulin, oral hypoglycemic drugs, glucagon, calcium channel blockers, beta-blockers and diuretics.

Analogs

Analogs of Octreotide are: Octreotide Fsintez, Octrid, Octretex, Sandostatin, Somatostatin, Differelin, Sermorelin.

Terms and conditions of storage

Store out of the reach of children and protected from light, in a temperature range of 8-25 ºС.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews of Octreotide

Reviews of Octreotide are few. Most of them characterize the drug positively. It is indicated to be highly effective and well tolerated. The solution is used both in inpatient and outpatient settings. The cost of the funds is assessed as high.

Price for Octreotide in pharmacies

The approximate price for Octreotide (5 ampoules) is: 50 μg / ml - 635-1031 rubles, 100 μg / ml - 1510-1827 rubles, 300 μg / ml - 5947-6382 rubles, 600 μg / ml - 12 532 –13887 rubles.

Octreotide: prices in online pharmacies

Drug name Price Pharmacy

Octreotide 50 μg / ml solution for intravenous and subcutaneous administration 1 ml 5 pcs. 999 RUB Buy

Octreotide 50 μg / ml solution for intravenous and subcutaneous administration 1 ml 5 pcs. 1049 RUB Buy

Octreotide 100 μg / ml solution for intravenous and subcutaneous administration 1 ml 5 pcs. 1298 RUB Buy

Octreotide 100 μg / ml solution for intravenous and subcutaneous administration 1 ml 5 pcs. 1786 RUB Buy

Octreotide solution for intravenous and subcutaneous injection. 100 mcg / ml amp. 1ml 5 pcs 1981 RUB Buy

Octreotide 50 μg / ml solution for intravenous and subcutaneous administration 1 ml 10 pcs. 2649 RUB Buy

Octreotide 100 μg / ml solution for intravenous and subcutaneous administration 1 ml 10 pcs. RUB 3119 Buy

Octreotide solution for intravenous and subcutaneous injection. 0.01% 1ml 10 pcs. 3383 RUB Buy

Octreotide 100 μg / ml solution for intravenous and subcutaneous administration 1 ml 10 pcs. 3889 RUB Buy

Octreotide 300 mcg / ml solution for intravenous and subcutaneous administration 1 ml 5 pcs. RUB 5879 Buy

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Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!