Octreotide-long FS - Instructions For Use, Reviews, Price, Analogues

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

Octreotide-Long FS

Octreotide-long FS: 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-Long FS

ATX code: H01CB02

Active ingredient: octreotide (Octreotide)

Manufacturer: Pharmstandard-UfaVITA, JSC (Russia); Nativa, OOO (Russia)

Description and photo update: 2018-27-11

Octreotide-long FS is a drug for intensive care in gastroenterology, a synthetic analogue of the peptide hormone somatostatin.

Release form and composition

Octreotide-long FS is available in the form of microspheres for the preparation of a suspension for intramuscular (i / m) administration, prolonged action: a porous mass of white / white color with a slight yellow tinge, compacted into a tablet or in the form of a lyophilized powder (brittle lyophilisate). The reconstituted suspension (microspheres are combined with a solvent) after shaking is a homogeneous suspension of white / white color with a slight yellow tint; at rest, the solution precipitates, but when shaken is easily resuspended. It should freely pass into the syringe through a needle No. 0840 [10, 20 or 30 mg in dark glass vials with a volume of 10 ml; 1 bottle each complete with one ampoule of solvent (2 ml in glass ampoules), one disposable syringe (volume 5 ml), needle for solvent, needle for suspension, needle for injection,alcohol wipes (2 pcs.), ampoule knife (or without it) in contour plastic packaging, in a cardboard box 1 package and instructions for use of Octreotide-Long FS].

1 bottle contains:

• active substance: octreotide acetate (in terms of octreotide) - 10, 20 or 30 mg;
• auxiliary components: polysorbate-80, DL-lactic and glycolic acid copolymer, sodium carmellose, D-mannitol.

1 ml of a solvent for the preparation of a suspension (clear, colorless liquid) contains: D-mannitol - 8 mg, water for injection.

Pharmacological properties

Pharmacodynamics

Octreotide-long FS is a drug that has a long-term somatostatin-like effect. It provides in the blood for 28 days the maintenance of stable therapeutic concentrations of the active substance - octreotide, which is a synthetic analogue of the natural hormone somatostatin, which has similar but longer pharmacological effects. The action of octreotide is aimed at suppressing the pathologically increased secretion of growth hormone (GH), and peptides and serotonin produced in the gastroenteropancreatic endocrine system.

Administration of the drug to healthy individuals causes suppression of GH secretion caused by exercise, arginine and insulin hypoglycemia. Like somatostatin, octreotide suppresses the secretion of peptides of the gastroenteropancreatic endocrine system, which is potentiated by food intake, including insulin, glucagon, gastrin. It has an inhibitory effect on the secretion of insulin and glucagon, stimulated by arginine, as well as on the secretion of thyrotropin caused by thyroliberin. In contrast to somatostatin, the severity of the suppressive effect of octreotide affects GH secretion to a much greater extent than insulin secretion. The use of octreotide is not accompanied by the phenomenon of hormone hypersecretion by the mechanism of negative feedback.

In acromegaly, the administration of octreotide provides a persistent decrease in the level of GH and normalization of the concentration of IGF-1 (insulin-like growth factor 1) in the vast majority of patients. Against the background of the introduction of Octreotide-Long FS, there is a significant decrease in the severity of acromegaly symptoms, including headache, peripheral neuropathy, increased sweating, fatigue, pain in the joints and bones, paresthesia.

The use of octreotide in a pituitary adenoma, secreting GH, helps to reduce the size of the tumor.

In patients with carcinoid tumors, clinical improvement is manifested by a decrease in the severity of symptoms of the disease, primarily hot flashes and diarrhea, a decrease in the concentration of serotonin in the blood plasma, and a decrease in the excretion of 5-hydroxyindoleacetic acid in the urine.

The use of octreotide in tumors with overproduction of VIP (vasoactive intestinal peptide) leads to a decrease in the severity of severe secretory diarrhea, which is characteristic of this condition. Together with the improvement of the patient's quality of life, this contributes to a simultaneous decrease in concomitant electrolyte disturbances, including hypokalemia, and allows the abolition of parenteral and enteral administration of electrolytes and fluids. The results of computed tomography indicate a slowdown or arrest of the progression of tumor growth, in some cases - a decrease in its size, liver metastases. Clinical improvement is confirmed by a decrease in the concentration of VIP in plasma down to normal values.

Administration of octreotide in glucagonomas markedly reduces the necrotizing migratory rash characteristic of this condition. The use of the drug does not have a significant effect on the severity of diabetes mellitus, which is often observed with glucagonomas, does not lead to a decrease in the need for insulin or hypoglycemic drugs for oral administration. Octreotide-long FS reduces the severity of severe diarrhea and increases the patient's body weight. Against the background of the use of octreotide, a rapid decrease in plasma glucagon concentration occurs, but with prolonged therapy this effect is lost. Symptomatic improvement remains stable for a long time.

In gastrinomas (Zollinger-Ellison syndrome), the use of Octreotide-Long FS is indicated as monotherapy or in combination with proton pump inhibitors and H2-histamine receptor blockers. Clinical improvement occurs as a result of a decrease in the formation of hydrochloric acid in the stomach and a decrease in diarrhea. It is characterized by a decrease in the severity of symptoms associated with the production of peptides by the tumor, including hot flashes, in some cases - a decrease in the concentration of gastrin in plasma.

In patients with insulinomas, Octreotide-Long FS helps to reduce the level of immunoreactive insulin in the blood.

In the preoperative period of operable tumors, octreotide is used to restore and maintain normoglycemia. With inoperable benign and malignant neoplasms, glycemic control can be improved even without simultaneous measures for a prolonged decrease in the concentration of insulin in the blood.

In somatoliberinoma (a tumor that overproduces GH-releasing factor), octreotide suppresses the secretion of growth hormone releasing factor and GH itself, reducing the symptoms of acromegaly. This contributes to the subsequent reduction in the size of the pituitary gland, increased before the start of treatment.

The sensitivity of the GR PCa tumor (hormone-resistant prostate cancer) to the drug is determined by an increase in the pool of neuroendocrine cells that express the SS2 and SS5 somatostatin receptors affinity for octreotide.

Against the background of androgenic blockade (medical or surgical castration), the use of octreotide in patients with HH PC as part of combination therapy with dexamethasone restores the sensitivity to hormone therapy and reduces prostate specific antigen (PSA) in more than 50% of patients. In patients with bone metastases, this treatment improves the quality of life, providing a pronounced and long-term analgesic effect.

Indications for use

The use of Octreotide-Long FS has been shown as a means of pathogenetic therapy for tumors actively expressing somatostatin receptors.

When treating acromegaly, the appointment of octreotide is advisable in the following cases:

• the required adequate control of the manifestations of the disease is provided by subcutaneous administration of octreotide;
• there is no sufficient effect of radiation therapy and surgery;
• the period of preparation for surgery;
• treatment between courses of radiotherapy to ensure the development of a lasting effect;
• inoperability of the patient.

In the treatment of endocrine tumors of the pancreas and gastrointestinal tract (GIT), the use of Octreotide-Long FS is indicated for such neoplasms:

• carcinoid tumors with concomitant carcinoid syndrome;
• gastrinomas (Zollinger-Ellison syndrome);
• insulinomas;
• VIPomas (Werner-Morrison syndrome);
• glucagonomas (to control hypoglycemia in the preoperative period and as a maintenance treatment);
• somatoliberinomas (characterized by overproduction of the tumor releasing factor GR).

In patients with hormone-resistant prostate cancer, octreotide is used as part of a combination therapy against the background of surgical or medical castration.

Contraindications

The use of Octreotide-Long FS for the treatment of patients with individual intolerance to the drug components is contraindicated.

With caution, Octreotide-Long FS should be prescribed for cholelithiasis, diabetes mellitus, during pregnancy and breastfeeding.

Octreotide-long FS, instructions for use: method and dosage

The reconstituted suspension is intended for deep injection exclusively into the gluteus muscle. For repeated injections, the left and right sides should be alternated.

The procedure should only be carried out by specially trained medical personnel.

On the day of the procedure, the vial with the drug and the ampoule with the solvent can be stored at room temperature or taken out of the refrigerator 0.5-1 hour before injection.

The suspension should be prepared immediately before injection, using the solvent supplied with the microspheres.

While holding the vial with the lyophilisate in a strictly vertical position, lightly knock on its walls in order to shed the entire drug onto the bottom of the vial.

Having opened the package, you should take out a syringe and attach a needle to it for taking a solvent (0.8 mm by 40 mm). Take all the contents from the ampoule with the solvent into the syringe and set the plunger to the 2 ml mark. Having removed the plastic cap from the vial with microspheres and disinfected the rubber stopper with an alcohol swab from the packaging, it is necessary to insert the needle into the vial through the center of the stopper, avoiding its contact with the microspheres. On the inner wall, the solvent is carefully injected into the vial, then the syringe with the needle is removed and the microspheres are left until they are completely saturated with the solvent, which occurs over a period of 2 to 5 minutes. During a visual check for the presence of a dry residue, the bottle should not be turned over, the drug is examined carefully. If necessary, leave the bottle for some time to soak. After ascertaining the fact of complete soaking of the entire mass in the vial, it is slowly rotated for 0.5-1 minutes until a homogeneous suspension is formed.

Do not flip or shake the bottle!

For the procedure, a needle is attached to the syringe to set the suspension (1.2 mm by 50 mm). It is inserted through the stopper into the vial and the needle cut is lowered down, the vial is tilted at an angle of 45 degrees and the suspension is taken slowly. Even if a small amount of the drug remains on the walls and bottom, the bottle should not be turned over, this consumption is taken into account.

Suspension Octreotide-Long FS should be injected immediately after preparation, therefore, immediately after taking the drug from the vial, the needle on the syringe is replaced with a needle for injecting the drug (1.1 mm by 40 mm) and the syringe is gently turned over and air is removed from it. After disinfecting the injection site, the needle is inserted deep into the gluteus muscle. By slightly pulling the syringe plunger towards you, you should make sure that the blood vessel is not damaged, after which you can slowly inject the drug. If the needle enters the capillary, the injection site and needle must be changed.

For repeated injections, alternate the left and right buttock.

Do not mix the suspension with another drug in the same syringe.

If the needle is clogged, it must be replaced with another.

For long-term use of Octreotide-Long FS in acromegaly, it is recommended to establish the individual tolerance and efficacy of the drug by preliminary testing for three days with subcutaneous (SC) administration of octreotide at a dose of 0.3 mg per day. The absence of signs of intolerance and a decrease in the concentration of IGF-1 in the blood of more than 60% from the initial level is an indication of a good prospect for using the drug as a long-term primary or secondary pharmacotherapy. In patients with less sensitivity to the drug, the starting dose should be increased. It is advisable for patients in the resistant group to undergo surgery. In non-radical adenomectomy, a three-day test with subcutaneous administration increases sensitivity to subsequent drug therapy.

The recommended dosage for the treatment of acromegaly in patients with adequate control of the manifestations of the disease, established as a result of subcutaneous tests: the initial dose is 20 mg 1 time in 28 days. The duration of the course is 3 injections. You can start an intramuscular injection the next day after the last subcutaneous injection. Each subsequent dose of Octreotide-Long FS should be adjusted based on clinical symptoms, serum IGF-1 and GH concentrations.

If, after three injections, an adequate clinical and biochemical effect cannot be achieved, a single dose can be increased to 30 mg.

When, against the background of initial therapy at a dose of 20 mg after three injections, there is a normalization of the IGF-1 concentration, a steady decrease in the serum concentration of GH below 0.001 mg / L and the absence of reversible symptoms of acromegaly, subsequent treatment can be carried out at a dose of 10 mg 1 time in 28 days under careful control of disease symptoms, serum concentrations of GH and IGF-1.

While receiving a stable dose of Octreotide-Long FS, studies to determine the concentration of GH and IGF-1 should be performed every 180 days.

For the treatment of endocrine tumors of the gastrointestinal tract and pancreas, the use of the drug should be started with s / c administration of octreotide at a dose of 0.1 mg 3 times a day for 14 days. This will allow assessing the overall individual tolerance and effectiveness of the drug.

The recommended dosage for patients in whom SC administration of octreotide provides adequate control of the manifestations of the disease: the initial dose is 20 mg 1 time in 28 days. Subcutaneous administration should be continued within 14 days from the day of the first administration of the drug.

If therapy for 84 days provides adequate control of biological markers and clinical manifestations of the disease, a single dose for subsequent procedures can be reduced to 10 mg, while maintaining their original frequency.

When, after three injections of initial therapy, sufficient improvement has not been achieved, a single dose can be increased to 30 mg.

If, against the background of therapy with Octreotide-Long FS, there is an increase in clinical manifestations that are characteristic of endocrine tumors of the gastrointestinal tract and pancreas, it is recommended to additionally introduce a subcutaneous dose that was used before the start of the course therapy. Such conditions occur mainly during the first 60 days of treatment until therapeutic plasma octreotide concentrations are reached.

The recommended dosage for the treatment of GH PCa: the initial dose is 20 mg 1 time in 28 days. The duration of the course is 84 days. Then it is necessary to adjust the single dose taking into account the dynamics of the concentration of PSA in the serum and clinical symptoms.

If after 84 days of therapy an adequate clinical and biochemical effect is not achieved (lowering PSA is not enough), the dose can be increased to 30 mg, keeping the frequency of administration. The use of Octreotide-Long FS is combined with dexamethasone, which is administered orally according to the scheme: during the first 30 days - 4 mg once a day, then within 14 days - 2 mg once a day, then as a maintenance dose - according to 1 mg daily. Against the background of preliminary drug antiandrogen therapy, the drug is prescribed in combination with an analogue of gonadotropin-releasing hormone (GnRH). In this case, the injection of a prolonged form of GnRH analog is done once every 28 days. Treatment is accompanied by control of PSA concentrations, which is carried out once every 30 days.

Side effects

• on the part of the cardiovascular system: sometimes - tachycardia, bradycardia;
• from the digestive system: often - bloating, excessive gas formation, cramping abdominal pain, diarrhea, loose stools; sometimes - cholecystitis; rarely - nausea, vomiting, formation of stones in the gallbladder, steatorrhea (an increase in the excretion of fats with feces is possible, but there is no information that long-term treatment can lead to malabsorption), symptoms of acute intestinal obstruction (severe pain in the epigastric region, progressive bloating, tension in the abdominal wall); very rarely - acute pancreatitis (in cases of subcutaneous administration of octreotide), against the background of long-term therapy - pancreatitis (associated with cholelithiasis), liver dysfunction in the form of acute hepatitis without cholestasis (after the abolition of octreotide, transaminase values normalize themselves),hyperbilirubinemia (slow development is accompanied by an increase in gamma-glutamyl transferase, alkaline phosphatase);
• from the respiratory system: very rarely - shortness of breath;
• local reactions: often - pain; rarely - rashes and swelling at the injection site (are of a short, mild character);
• allergic reactions: rarely - rash, hypersensitivity reactions; very rarely - anaphylaxis;
• from the endocrine system: rarely - hypoglycemia, development of persistent hyperglycemia;
• others: rarely - temporary hair loss.

Overdose

Symptoms: against the background of a single intravenous bolus injection of octreotide at a dose of 1 mg, an adult patient showed the appearance of short-term bradycardia, spastic abdominal pain, flushing of the face, diarrhea, feeling of emptiness in the stomach, nausea. During the first 24 hours after the administration of Octreotide-Long FS, all the described phenomena were resolved.

Treatment: symptomatic.

special instructions

Treatment of GH-secreting pituitary tumors should be closely monitored because of the possible enlargement of the tumor, leading to the development of serious complications, including narrowing of the visual fields. An increase in the size of the tumor is the basis for transferring the patient to the use of other methods of therapy.

There is a risk (in 15-30% of patients) of the appearance of stones in the gallbladder on the background of prolonged SC administration of octreotide. An increase in the incidence of calculus formation in the gallbladder with the use of long-acting octreotide for long-term treatment of patients with neuroendocrine tumors of the gastrointestinal tract and pancreas or acromegaly, in comparison with short-acting octreotide, was not observed. However, ultrasound examination of the gallbladder is recommended both before starting treatment with the drug, and regularly (once every 6 months) during therapy. Most often, stone formation in the gallbladder is asymptomatic. In the presence of clinical symptoms, the patient should receive therapy for gallstone disease, and the feasibility of prescribing Octreotide-long FS is assessed individually,taking into account the balance of benefits and risks.

In type 1 diabetes mellitus, the effect of Octreotide-Long FS on glucose metabolism is possible, this should be taken into account, and the dose of insulin administered should be reduced. In type 2 diabetes mellitus and in patients without concomitant disorders of carbohydrate metabolism, SC injections of octreotide may cause postprandial glycemia. In this connection, in this category of patients, it is recommended to regularly monitor the blood glucose concentration for the timely correction of hypoglycemic therapy.

The use of octreotide in patients with insulinomas may cause an increase in the severity or duration of hypoglycemia, due to its less inhibitory effect on insulin secretion than on the secretion of GH and glucagon, as well as a shorter duration of the inhibitory effect on insulin secretion.

Octreotide-long FS can interfere with the absorption of fats in the intestine, cause a decrease in the content of cyanocobalamin (vitamin B ₁₂) and a deviation of the cyanocobalamin absorption test (Schilling test) from the norm. If a patient has a history of vitamin B ₁₂ deficiency during treatment with octreotide, it is recommended to control the cyanocobalamin content.

Influence on the ability to drive vehicles and complex mechanisms

There is no information on the negative effect of Octreotide-Long FS on the ability to concentrate and the speed of psychomotor reactions, which allows performing potentially dangerous types of work during therapy.

Application during pregnancy and lactation

With caution, only if absolutely necessary, the use of Octreotide-Long FS is indicated during gestation and breastfeeding.

Pediatric use

Experience with the use of Octreotide-Long FS for the treatment of children is limited.

With impaired renal function

No dosage adjustment is required.

For violations of liver function

No dosage adjustment is required.

Use in the elderly

Elderly patients do not need to adjust the dosage regimen of Octreotide-Long FS.

Drug interactions

• cyclosporin: the degree of absorption of cyclosporin from the intestine decreases;
• cimetidine: the rate of absorption of cimetidine from the intestine slows down;
• bromocriptine: increases the bioavailability of bromocriptine;
• quinidine, terfenadine and other drugs, the metabolism of which is due to enzymes of the cytochrome P450 system and has a narrow therapeutic dose range: a decrease in the metabolic clearance of these drugs is possible, therefore, they should be prescribed in combination with octreotide with caution.

Analogs

The analogues of Octreotide-Long FS are Octreotide, Octreotid Kabi, Octreotid San, Octreotid-Actavis, Octreotid-depot, Octretex, Genfastat, Sandostatin, Serakstal, etc.

Terms and conditions of storage

Keep out of the reach of children.

Store at 2-8 ° C in a dark place.

Shelf life: microspheres - 2 years, solvent - 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews of Octreotide-Long FS

The few reviews about Octreotide-Long FS are positive. Pointing to the high therapeutic efficacy of the drug, patients, among other things, attribute a much lower cost to its advantages compared to imported counterparts.

Price for Octreotide-Long FS in pharmacies

The price of Octreotide-Long FS for one package containing 1 bottle with 10 mg of microspheres can be from 27 324 rubles, 20 mg - from 33 264 rubles, 30 mg - from 51 084 rubles.

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!