Octreotide-depot - Instructions For Use, Price, 30 Mg, 20 Mg, 10 Mg

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

Octreotide depot

Octreotide-depot: 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. In case of impaired renal function
11. 11. For violations of liver function
12. 12. Use in the elderly
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Octreotide-depo

ATX code: H01CB02

Active ingredient: octreotide (octreotide)

Manufacturer: Pharm-Sintez JSC (Russia); Deco company (Russia); Diamed (Russia)

Description and photo updated: 17.07.2018

Prices in pharmacies: from 26,000 rubles.

Buy

Octreotide depot is a drug that has a somatostatin-like effect.

Release form and composition

Dosage form - lyophilisate for preparing a suspension for intramuscular (i / m) administration of prolonged action: powder or porous mass, compacted into a tablet, white or yellowish-white. The drug is packaged at 10, 20 or 30 mg in 10 ml dark glass vials; in a blister strip packaging 1 bottle, 1 ampoule of solvent (colorless transparent liquid, 2 ml), a disposable syringe, 2 sterile needles and 2 alcohol swabs; in a cardboard box 1 blister strip and instructions for use of Octreotide-depot. The kit is designed for one injection.

The composition of the lyophilisate in 1 bottle:

• active substance: octreotide - 10, 20 or 30 mg;
• auxiliary components: D-mannitol, polysorbate-80, sodium carboxymethylcellulose, copolymer of DL-lactic and glycolic acids.

The composition of the solvent: solution for injection 0.8%, mannitol.

Pharmacological properties

Pharmacodynamics

The active ingredient of the drug is octreotide - a synthetic octapeptide. It is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but is characterized by a significantly longer duration of action. It is used in the pathogenetic therapy of tumors that actively express receptors for somatostatin.

Octreotide depot is a long-acting drug that maintains stable therapeutic concentrations of octreotide in the blood for 4 weeks.

Octreotide has the ability to suppress pathologically increased secretion of growth hormone (GH), serotonin and peptides produced in the gastroentero-pancreatic endocrine system.

In healthy volunteers, Octreotide Depot, like somatostatin, inhibits:

• GH secretion caused by insulin hypoglycemia, arginine and exercise;
• arginine-stimulated secretion of glucagon and insulin;
• the secretion of glucagon, insulin, gastrin and other peptides of the gastroentero-pancreatic endocrine system caused by food intake;
• the secretion of thyrotropin caused by thyroliberin.

Unlike somatostatin, octreotide inhibits GH secretion to a greater extent than insulin. The drug does not cause the development of the phenomenon of hormone hypersecretion by the mechanism of negative feedback.

In acromegaly, Octreotide-depot in most cases provides a persistent decrease in the concentration of GH and normalizes the concentration of IGF-1 [insulin-like growth factor 1 (somatomedin C)]. As a result, the severity of symptoms such as increased sweating, fatigue, headache, pain in bones and joints, paresthesia, and peripheral neuropathy is significantly reduced.

There are known cases of a decrease in tumor size during the use of the drug in patients with pituitary adenomas secreting GH.

Octreotide depot allows for constant control of the main symptoms of secreting endocrine tumors of the gastrointestinal tract (GIT) and pancreas.

The use of a dose of Octreotide-depot 30 mg once every 4 weeks slows down the growth of secreting and non-secreting widespread (metastatic) neuroendocrine tumors of the transverse colon, ascending colon, ileum, caecum, jejunum and vermiform appendix, as well as the growth of metastatic neuroendocrine tumors without primary identified.

Octreotide depot has been shown to be effective in increasing the period to progression of neuroendocrine tumors (both secreting and non-secreting).

In carcinoid tumors, octreotide may reduce symptoms, especially hot flashes and diarrhea. Clinical improvement is often accompanied by a decrease in plasma serotonin concentration and urinary excretion of 5-hydroxyindoleacetic acid.

In tumors characterized by overproduction of vasoactive intestinal peptide (VIPomas), Octreotide depot in most cases reduces the severe secretory diarrhea characteristic of this condition, which significantly improves the patient's quality of life. At the same time, concomitant electrolyte imbalances (eg, hypokalemia) are reduced, which makes it possible to discontinue enteral and parenteral administration of electrolytes and fluids. In some patients, computed tomography shows a slowing down or stopping of tumor progression, sometimes even its reduction in size, especially liver metastases. Clinical improvement is usually accompanied by a decrease (up to normalization) in plasma VIP concentration.

In most patients with glucagonomas, octreotide markedly reduces the necrotizing migratory rash associated with this condition. However, the drug does not affect the severity of diabetes mellitus, which is often diagnosed with glucagonomas, and does not reduce the need for insulin / oral hypoglycemic drugs. With diarrhea, Octreotide-depot reduces its severity, as a result of which the patient's body weight increases. The drug often contributes to a rapid decrease in plasma glucagon concentration, but this effect does not persist with prolonged use. At the same time, the improvement in the symptoms of the disease remains stable for a long time.

In Zollinger-Ellison syndrome (gastrinomas), Octreotide-depot, used as a single drug or in combination with proton pump inhibitors and H2-histamine receptor blockers, can reduce the formation of hydrochloric acid in the stomach and improve the patient's clinical condition, including diarrhea. At the same time, other symptoms (for example, hot flashes), probably associated with the synthesis of peptides by the tumor, may decrease. In some patients, the plasma concentration of gastrin decreases. In insulinomas, octreotide lowers the concentration of immunoreactive insulin in the blood. For operable tumors, Octreotide-depot can provide restoration and maintenance of normoglycemia in the preoperative period. In patients with inoperable tumors (benign and malignant), glycemic control can improve without a concomitant prolonged decrease in blood insulin levels.

In the case of hormone-resistant prostate cancer (HRPCa), there is an increase in the pool of neuroendocrine cells that express somatostatin receptors showing affinity for octreotide (SS2 and SS5 types), which explains the sensitivity of the tumor to the action of the latter. In more than 50% of such patients, the use of Octreotide-depot in combination with dexamethasone against the background of androgenic blockade (medical or surgical castration) restores sensitivity to hormonal therapy and helps to reduce prostate specific antigen (PSA). In patients with HRPCa and bone metastases, this therapy provides a pronounced and long-term analgesic effect. Moreover, in all patients who have a response to combination therapy with Octreotide-depot,the quality of life and median disease-free survival are significantly improved.

When treating patients diagnosed with rare tumors - somatoliberinomas (hyperproductive growth hormone releasing factor), Octreotide-depot reduces the severity of acromegaly. This is probably due to the suppression of the secretion of the releasing factor GH and GH itself. If the pituitary gland was enlarged before the start of treatment, it may decrease in the future.

Pharmacokinetics

Data on the pharmacokinetic parameters of Octreotide depot are not provided.

Indications for use

Octreotide depot is recommended for the treatment of acromegaly in the following cases:

• the symptoms of the disease are amenable to adequate control with octreotide in dosage forms for subcutaneous (s / c) administration;
• the period of preparation for surgical treatment;
• treatment between courses of radiation therapy to obtain a lasting effect;
• lack of sufficient effect from surgical and radiation therapy;
• inoperable forms of the disease.

The drug is used in the treatment of the following endocrine tumors of the pancreas and gastrointestinal tract:

• insulinomas;
• gastrinomas (Zollinger-Ellison syndrome);
• VIPomas;
• somatoliberinomas (tumors that overproduce growth hormone releasing factor);
• carcinoid tumors with symptoms of carcinoid syndrome;
• glucagonomas (for maintenance therapy and control of hypoglycemia in the preoperative period);
• secreting and non-secreting widespread (metastatic) neuroendocrine tumors of the transverse colon, ascending colon, ileum, cecum, jejunum and vermiform appendix, as well as metastatic neuroendocrine tumors without a primary focus.

Octreotide-depot is prescribed to prevent the development of acute postoperative pancreatitis during extensive surgical operations on the abdominal cavity and thoracoabdominal interventions, including for primary and secondary tumor lesions of the liver, cancer of the colon, esophagus, stomach and pancreas.

Also, the drug is used as part of the complex therapy of hormone-resistant prostate cancer against the background of androgenic blockade (medical or surgical castration).

Contraindications

Octreotide depot is strictly contraindicated only in the presence of known hypersensitivity to any of its components.

The drug should be used with caution in pregnant and breastfeeding women, in patients with diabetes mellitus and in patients with cholelithiasis.

Octreotide depot, instructions for use: method and dosage

Octreotide depot is intended for intramuscular administration.

The suspension is prepared by trained medical personnel immediately before injection. To dilute the lyophilisate, use the supplied solvent.

Rules for the preparation of the suspension and the administration of Octreotide-depot:

1. Remove the drug from the refrigerator and bring it to room temperature (this usually takes 30 to 50 minutes).
2. Holding the bottle strictly vertically, it is easy to knock on it so that the entire lyophilisate sinks to the bottom.
3. Open the package with a syringe and attach a needle with a pink pavilion 1.2x50 mm in size to it.
4. Open the ampoule with the solvent, draw all the contents into the syringe and set it to a dose of 2 ml.
5. Remove the plastic cap from the lyophilisate bottle, disinfect the stopper with an alcohol swab.
6. Insert the needle of the syringe with the solvent into the vial through the center of the stopper and carefully pour the solution along the inner wall of the vial, without touching the contents with the needle.
7. Remove the syringe and leave the vial stationary until the lyophilisate is completely saturated with the solvent and forms a suspension (approximately 3-5 minutes). Without turning the bottle over, check for the presence of dry lyophilisate at the bottom and at the walls. If dry residues of the powder are found, leave the bottle for a while until it is completely dissolved.
8. After making sure that there is no undissolved lyophilisate, gently mix the contents of the vial in a circular motion for 30-60 seconds so that the suspension becomes homogeneous. Do not shake or turn the bottle over, this can lead to the fall of flakes, which will make the drug unusable.
9. Quickly insert the syringe with the needle into the vial through the rubber stopper. Lower the needle cut down and slowly draw up the suspension at an angle of the bottle of 45 °. A small amount of suspension may remain on the bottom and sides of the bottle. This residue is provided, so you should not turn the bottle upside down when dialing the drug.
10. Replace the needle for the set with the needle for the introduction with the green pavilion (0.8x40 mm), gently turn the syringe and remove the air from it.
11. Disinfect the injection site with an alcohol swab.
12. Insert the needle deep into the gluteus muscle and pull the plunger back slightly to make sure the vessel is not damaged. If it enters a blood vessel, the needle should be replaced with another of the same diameter and the injection site should be changed.
13. Introduce the suspension by continuously pressing the syringe plunger.

The suspension prepared from the lyophilisate is homogeneous, white or yellowish-white in color.

With repeated injections, the right and left gluteus muscles should be alternated.

Octreotide depot should not be mixed in the same syringe with any other drugs.

The drug is always stored in the refrigerator, however, on the day of injection, the vial of lyophilisate and the ampoule with the solvent are allowed to be kept at room temperature.

Acromegaly therapy

For patients in whom the use of short-acting octreotide (for subcutaneous injections) provides adequate control of the symptoms of the disease, the administration of Octreotide-depot can be started the day after the last SC administration of octreotide. Treatment is started with a dose of 20 mg every 4 weeks, at this dosage, the drug is used for 3 months. In the future, the doctor adjusts the dose depending on the clinical manifestations of the disease and the concentration of GH and IGF-1 in the blood serum.

If within 3 months it is not possible to achieve an adequate response, both clinical and biochemical (in particular, if the GH level does not fall below 2.5 μg / L), the dose is increased to 30 mg every 4 weeks.

If, after 3 months of regular use of a dose of Octreotide-depot 20 mg, there is a persistent decrease in the concentration of GH in the serum below 1 μg / L, the concentration of IGF-1 is normalized, and the reversible symptoms of acromegaly disappear, a single dose may be reduced to 10 mg. Treatment should continue under close laboratory supervision.

For patients receiving a stable dose of the drug, the concentration of GH and IGF-1 can be determined once every six months.

When the appointment of Octreotide depot is required as a short-term treatment between courses of radiation therapy, as well as in patients in whom surgical and radiation therapy has been ineffective or insufficiently effective, it is recommended to conduct a trial course of treatment with short-acting octreotide (for SC administration) to evaluate it action and individual tolerance, and only then apply Octreotide-depot according to the scheme described above.

Therapy of endocrine tumors of the gastrointestinal tract and pancreas

For patients in whom the use of short-acting octreotide provides adequate control of the symptoms of the disease, the initial dose of the drug is 20 mg every 4 weeks. At the same time, after the start of the administration of Octreotide-depot, the use of SC octreotide is continued for another 2 weeks.

For patients who have not previously received SC octreotide, it is recommended to start treatment with the dosage form of the drug for SC administration at a dose of 0.1 mg 3 times a day for about 2 weeks. This is necessary in order to assess its effectiveness and individual tolerance. Only then can Octreotide-depot be used according to the scheme described above.

If after 3 months of treatment only partial improvement has been achieved, Octreotide Depot 30 mg is prescribed every 4 weeks. In cases where, within 3 months of therapy, it is possible to achieve adequate control of clinical manifestations and biological markers, the dose of the drug can be reduced to 10 mg every 4 weeks.

Against the background of the use of Octreotide-depot on certain days (mainly in the first 2 months of treatment, until the therapeutic plasma concentrations of the active substance are reached), the clinical manifestations characteristic of endocrine tumors of the gastrointestinal tract and pancreas may increase. Such patients are advised to additionally administer SC octreotide at a dose that was prescribed prior to the start of Octreotide Depot administration.

For secreting and non-secreting common neuroendocrine tumors of the transverse colon, ascending colon, ileum, blind, jejunum and vermiform appendix, as well as for metastases of neuroendocrine tumors without a primary identified focus, Octreotide depot is prescribed at a dose of 30 mg every 4 weeks. The therapy is continued until the tumor is controlled (until signs of its progression appear).

Prevention of acute postoperative pancreatitis

The drug is prescribed in a dose of 10 or 20 mg. The injection is done once, no earlier than 5 days and no later than 10 days before the proposed surgery.

Therapy for hormone-resistant prostate cancer

The initial recommended dose of Octreotide Depot is 20 mg every 4 weeks for 3 months. In the future, the doctor adjusts the dose depending on the clinical manifestations of the disease and the concentration of prostate specific antigen in the blood serum.

If, within 3 months of therapy, it is not possible to achieve adequate control of the clinical symptoms of the disease and biological markers (decrease in PSA), the dose is increased to 30 mg every 4 weeks.

Octreotide depot is used in combination with dexamethasone used in oral dosage form according to the following scheme: 4 mg / day for 1 month, then 2 mg / day for 2 weeks, then 1 mg / day.

In patients who have previously received drug antiandrogen therapy, the combination of Octreotide-depot + dexamethasone is combined with the use of a depot-form gonadotropin-releasing hormone analogue, which is injected once every 4 weeks.

PSA concentrations should be measured every month during therapy.

Side effects

• from the digestive system: excessive flatulence, bloating, abdominal cramping, diarrhea, loose stools, steatorrhea, nausea, vomiting, anorexia; rarely, phenomena resembling acute intestinal obstruction, such as severe pain in the epigastric region, progressive bloating and tension of the abdominal wall; with long-term treatment - the formation of stones in the gallbladder;
• from the liver: hyperbilirubinemia with an increase in alkaline phosphatase, gamma-glutamyl transpeptidase and other transaminases; in some cases - liver dysfunction, up to the development of acute hepatitis without cholestasis (transaminase indices are normalized after the abolition of Octreotide-depot);
• from the pancreas: in rare cases - acute pancreatitis in the first hours or days of using octreotide; rarely with long-term treatment - pancreatitis associated with cholelithiasis;
• on the part of metabolism: decreased glucose tolerance after a meal; rarely - hyperglycemia / hypoglycemia;
• local reactions: pain at the injection site; rarely - swelling and rashes at the injection site;
• others: in rare cases - temporary hair loss, skin rash, shortness of breath, tachycardia, bradycardia, hypersensitivity reactions.

Overdose

To date, no cases of octreotide overdose have been reported.

special instructions

Patients with GH-secreting pituitary tumors should be under close medical supervision during treatment, since the tumor may increase in size and develop such a serious complication as narrowing of the visual fields. In this case, the physician should consider alternative therapy.

Approximately 15–30% of patients who receive long-term short-acting (subcutaneous) octreotide develop gallstones. The prevalence in the general population (persons aged 40-60 years) is 5-20%. Clinical experience of long-term use of prolonged-release octreotide in patients with acromegaly, pancreatic and gastrointestinal tumors suggests that Octreotide-depot does not increase the incidence of gallbladder calculi. However, it is recommended to conduct an ultrasound examination of the gallbladder before starting the drug and repeat it every 6 months with long-term treatment. Gallstones (if they do form) are usually asymptomatic. In the presence of clinical symptoms, conservative treatment (for example, taking bile acid preparations) or surgery is carried out.

If stones in the gallbladder are formed while using Octreotide-depot, the doctor is guided by the following recommendations:

• there are no symptoms: depending on the benefit / risk ratio, the drug is canceled or continued to be used. In any case, no action is required other than surveillance;
• there are clinical symptoms: depending on the benefit / risk ratio, the drug is canceled or continued to be used. In any case, the patient requires the appointment of standard treatment for gallstone disease, accompanied by clinical manifestations. Drug therapy includes the appointment of combinations of bile acid preparations (for example, ursodeoxycholic and chenodeoxycholic acids in daily doses of 7.5 mg / kg). Ultrasonic testing is required until the stones disappear completely.

Currently, there is no data that would demonstrate the negative effect of the drug on the prognosis and course of the already existing cholelithiasis. If stones are found before starting treatment, the physician should weigh the expected benefits of the upcoming therapy against the possible risks of complications due to the presence of gallstones.

Against the background of drug therapy, it is possible to increase the excretion of fats from the body with feces, but until now there is no evidence that with prolonged use of Octreotide-depot can lead to the development of a deficiency of certain nutrients due to malabsorption (malabsorption).

The suppressive effect of octreotide is more pronounced on the secretion of GH and glucagon than insulin. At the same time, a shorter duration of the inhibitory effect on insulin secretion is noted. In this regard, Octreotide-depot may increase the severity and duration of hypoglycemia in patients with insulinomas. Patients should be under medical supervision.

In type 1 diabetes mellitus, Octreotide Depot may affect glucose metabolism, which reduces the need for insulin. In patients with type 2 diabetes mellitus and patients without concomitant disorders of carbohydrate metabolism, the use of short-acting octreotide in some cases leads to postprandial glycemia, in this regard, during the period of therapy with this drug, it is also recommended to control blood glucose levels and, if necessary, adjust hypoglycemic therapy.

Influence on the ability to drive vehicles and complex mechanisms

To date, there is no evidence of a negative effect of octreotide on human mental and motor functions, which could affect the ability to drive a car and work with complex mechanisms.

Application during pregnancy and lactation

There is no clinical experience of using Octreotide-Depot in pregnant and breastfeeding women. Therefore, the drug can only be prescribed in cases where the expected benefit clearly outweighs the potential risks.

It is recommended to refuse breastfeeding during the therapy period.

With impaired renal function

Octreotide depot can be used in case of impaired renal function according to the dosage regimen recommended by the doctor. There is no need to adjust the dose.

For violations of liver function

Octreotide depot for liver dysfunction can be used in accordance with the dosage regimen recommended by the doctor. There is no need to adjust the dose.

Use in the elderly

Elderly patients do not need a special dosage regimen of the drug.

Drug interactions

Octreotide depot, with simultaneous use, increases the bioavailability of bromocriptine, reduces the absorption of cyclosporine from the intestine, and slows down the absorption of cimetidine.

According to some literature data, somatostatin analogs can reduce the metabolic clearance of drugs that are metabolized with the participation of isoenzymes of the cytochrome P450 system, which may be caused by suppression of growth hormone. The likelihood of the development of such effects in octreotide cannot be ruled out, therefore, the drug should be used with caution in combination with agents metabolized by isoenzymes of this system and having a narrow therapeutic range (for example, simultaneously with terfenadine or quinidine).

Analogs

Octreotide-depot analogues are Octretex, Signifor, Somatulin, Somatulin Autogel.

Terms and conditions of storage

Store at a temperature of 2-8 ° C in a dry and dark place, out of reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Octreotide-depot

There are practically no reviews on Octreotide-depot on specialized medical sites and forums. This is probably due to the fact that the drug is mainly used for such serious indications as acromegaly, prostate cancer, pancreatic and gastrointestinal tumors, and patients do not particularly want to share their impressions of the therapy.

Price for Octreotide depot in pharmacies

Prices for Octreotide-depot depend on the dosage of the drug and are approximately (per set for one injection): 10 mg - 16,000–20,950 rubles, 20 mg - 26,000–27,000 rubles, 30 mg - 34,000–38,100 rub.

Octreotide depot: prices in online pharmacies

Drug name Price Pharmacy

Octreotide depot 20 mg lyophilisate for the preparation of a suspension for intramuscular administration of prolonged action 1 pc. RUB 26,000 Buy

Octreotide depot 30 mg lyophilisate for the preparation of a suspension for intramuscular administration of prolonged action 1 pc. RUB 34,900 Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, 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!