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Octreotide - instructions for use, analogs, reviews and release forms (injections in ampoules for injection Depot, Long PS 10 mg, 20 mg and 30 mg) drugs for the treatment of pancreatitis, bleeding in gastrointestinal ulcers in adults, children and pregnancy. Composition

Octreotide - instructions for use, analogs, reviews and release forms (injections in ampoules for injection Depot, Long PS 10 mg, 20 mg and 30 mg) drugs for the treatment of pancreatitis, bleeding in gastrointestinal ulcers in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Octreotide. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Octreotide in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Octreotide analogues in the presence of existing structural analogues. Use for the treatment of pancreatitis, bleeding with ulcers of the gastrointestinal tract in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

 

Octreotide - synthetic analogue of somatostatin, which has similar pharmacological effects, but significantly longer duration of action.

 

The drug inhibits the secretion of growth hormone, both pathologically elevated, and caused by arginine, exercise and insulin hypoglycemia. The drug also inhibits the secretion of insulin, glucagon, gastrin, serotonin, both pathologically elevated, and caused by eating; also suppresses the secretion of insulin and glucagon stimulated with arginine. Octreotide suppresses the secretion of thyrotropin, caused by thyroidiberin.

 

In patients who are scheduled to undergo pancreatic surgery, the use of octreotide before surgery, during and after it reduces the incidence of typical postoperative complications (eg, pancreatic fistula, abscesses, sepsis, acute postoperative 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, sclerosing and haemostatic therapy) leads to more effective stopping of bleeding and prevention of rebleeding.

 

Octreotide Depot is a long-acting octreotide dosage form for intramuscular administration that maintains stable therapeutic octreotide concentrations in the blood for 4 weeks. Octreotide is a pathogenetic therapy for tumors that actively express somatostatin receptors. Octreotide is a synthetic octapeptide, which is a derivative of the natural hormone somatostatin and has similar pharmacological effects, but a much longer duration of action. The drug suppresses the pathologically increased secretion of growth hormone (GH), as well as peptides and serotonin produced in the gastrointestinal pancreatic endocrine system.

 

Composition

 

Octreotide + excipients.

 

Pharmacokinetics

 

After subcutaneous administration, Octreotide is rapidly and completely absorbed. Binding to plasma proteins is 65%. The binding of Octreotide to the shaped elements of blood is very insignificant. After intravenous administration octreotide removal is carried out in 2 phases with half-lives of 10 minutes and 90 minutes, respectively.Most of the octreotide is excreted through the intestine, about 32% is excreted unchanged by the kidneys.

 

Indications

  • treatment of acute pancreatitis;
  • stop bleeding with peptic ulcer of the stomach and duodenum;
  • stop bleeding and prevent bleeding from varicose veins of the esophagus in patients with cirrhosis;
  • prevention of complications after operations on the pancreas;
  • Diarrhea in patients with AIDS, refractory to other types of therapy.

 

In the therapy of acromegaly:

  • when adequate control of manifestations of the disease is due to subcutaneous administration of octreotide;
  • in the absence of sufficient effect from surgical treatment and radiation therapy;
  • for preparation for surgical treatment;
  • for treatment between radiotherapy courses before the development of a persistent effect;
  • in inoperable patients.

 

In the therapy of endocrine tumors of the gastrointestinal tract and pancreas:

  • carcinoid tumors with the phenomena of carcinoid syndrome;
  • insulinomas;
  • VIPoms;
  • gastrinomas (Zollinger-Ellison syndrome);
  • glucagonomes (for the control of hypoglycemia in the preoperative period, as well as for maintenance therapy);
  • somatoliberynoma (tumors characterized by hyperproduction of growth hormone releasing factor);
  • treatment of patients with secreting and non-secretive widespread (metastatic) neuroendocrine tumors of the lean, iliac, blind, ascending colon, transverse colon and appendix, or metastases of neuroendocrine tumors without a primary focus.

 

In the treatment of hormone-resistant prostate cancer:

  • in the combination therapy on the background of surgical or drug castration.

 

In the prevention of acute postoperative pancreatitis:

  • with extensive surgical operations on the abdominal cavity and thoracoabdominal interventions (including for cancer of the stomach, esophagus, colon, pancreas, primary and secondary tumor lesions of the liver).

 

Forms of release

 

A solution for intravenous and subcutaneous administration of 50 μg and 100 μg.

 

Solution for injection 0.01% (Octreotide Phsynthesis).

 

Solution for infusion and subcutaneous administration (Octreotide Actavis).

 

Lyophilizate for the preparation of a suspension for intramuscular administration of a prolonged action of 10 mg, 20 mg and 30 mg (Octreotide Depot).

 

Lyophilizate for the preparation of a solution for intramuscular administration of prolonged action (microspheres) 20 mg (Octreotide Long).

 

Instructions for use and dosage

 

The dose is set individually, depending on the nature of the disease, the regimen of treatment, and also on the dosage form used.

 

Octreotide in the form of a dosage form with the usual duration of action is applied subcutaneously and intravenously drip (in the form of a dropper), in the form of a depot form - deeply intramuscular.

 

For the treatment of acute pancreatitis, the drug is administered subcutaneously in a dose of 100 μg 3 times a day for 5 days. It is possible to administer up to 1200 micrograms per day using the intravenous route of administration.

 

To stop ulcers bleeding administered intravenously in a dose of 25-50 mkg / h in the form of intravenous infusions for 5 days.

 

To stop bleeding from the varicose veins of the esophagus is administered IV in a dose of 25-50 μg / h in the form of prolonged IV infusions for 5 days.

 

In elderly patients, there is no need to reduce the dose of Octreotide.

 

To prevent complications after operations on the pancreas, the first dose of 100-200 μg is administered subcutaneously 1-2 hours before laparotomy; then after the operation, enter sc to 100-200 μg 3 times a day for 5-7 consecutive days.

 

Depot

 

The drug Octreotide Depot should be administered only deep intramuscularly (IM), in the gluteal muscle. With repeated injections, the left and right sides should alternate. Suspension should be prepared immediately before injection. On the day of injection, the vial with the preparation and the ampoule with the solvent can be kept at room temperature.

 

In the treatment of acromegaly in patients for whom the octreotide administration provides adequate control of the manifestations of the disease, the recommended initial dose of Octreotide Depot is 20 mg every 4 weeks for 3 months. Start treatment with the drug Octreotide Depot can be the day after the last SC administration octreotide. In the future, the dose is adjusted taking into account the concentration in the serum of GH and IGF-1, as well as clinical symptoms. If after 3 months of treatment an adequate clinical and biochemical effect could not be achieved (in particular, if the GH concentration remains above 2.5 μg / L), the dose can be increased to 30 mg administered every 4 weeks.

 

In those cases when, after 3 months of treatment with Octreotide Depot at a dose of 20 mg, there is a persistent decrease in serum GH concentration below 1 μg / L,normalization of IGF-1 concentration and disappearance of reversible symptoms of acromegaly, it is possible to reduce the dose of Octreotide Depot to 10 mg. However, in these patients receiving a relatively small dose of Octreotide Depot, serum concentrations of GH and IGF-1, as well as the symptoms of the disease, should be carefully monitored.

 

For patients receiving a stable dose of Octreotide Depot, the determination of GH and IGF-1 concentrations should be performed every 6 months.

 

Patients in whom surgical treatment and radiotherapy are not effective or generally ineffective, as well as patients who need short-term treatment between the radiotherapy courses and the time of its full effect, it is recommended that a trial of subcutaneous octreotide therapy be conducted to assess its effectiveness and of general tolerability, and only after this go on to use the drug Octreotide Depot according to the above scheme.

 

In the treatment of endocrine tumors of the gastrointestinal tract and pancreas in patients to whom SC administration of octreotide provides adequate control of the manifestations of the disease, the recommended initial dose of Octreotide Depot is 20 mg every 4 weeks.SC administration of octreotide should continue for another 2 weeks after the first administration of Octreotide Depot.

 

In patients who did not receive octreotide earlier, it is recommended to start treatment with SC administration of octreotide at a dose of 0.1 mg 3 times a day for a relatively short period of time (approximately 2 weeks) in order to evaluate its effectiveness and overall tolerability. Only after this, the drug Octreotide Depot is prescribed according to the above scheme.

 

In the case when therapy with Octreotide Depot for 3 months provides adequate control of clinical manifestations and biological markers of the disease, it is possible to reduce the dose of Octreotide Depot to 10 mg, administered every 4 weeks. In cases where after 3 months of treatment with Octreotide Depot, only partial improvement was achieved, the dose of the drug can be increased to 30 mg every 4 weeks. Against the background of treatment with Octreotide Depot on certain days, it is possible to increase the clinical manifestations characteristic of endocrine tumors of the gastrointestinal tract and pancreas. In these cases, additional SC administration of octreotide is recommended in the dose used before the start of treatment with Octreotide Depot.This can occur mainly in the first 2 months of treatment, until the therapeutic concentrations of octreotide in plasma are reached.

 

Secreting and nonsecreting advanced (metastatic) tumor, neuroendocrine jejunum, ileum, caecum, the ascending colon, transverse colon, and the appendix, or metastasis of neuroendocrine tumors with no identified primary chamber: The recommended dose of the drug Octreotide Depot is 30 mg every 4 weeks. The drug therapy should continue until signs of tumor progression.

 

In the treatment of hormone-resistant prostate cancer, the recommended initial dose of Octreotide Depot is 20 mg every 4 weeks for 3 months. In the future, the dose is corrected taking into account the dynamics of serum PSA concentration, as well as clinical symptoms. If after 3 months of treatment failed to achieve an adequate clinical and biochemical effect (PSA reduction), the dose can be increased to 30 mg, administered every 4 weeks.

 

Treatment with Octreotide Depot combine with dexamethasone, which is prescribed orally as follows: 4 mg per day for 1 month, followed by 2 mg per day for 2 weeks followed by 1 mg per day (the maintenance dose).

 

Treatment with Octreotide Depot and Dexamethasone in patients who had previously undergone drug and anti-androgen therapy are combined with the use of a gonadotropin-releasing hormone (GnRH) analogue. In this case, an injection of the GnRH analogue (depot form) is carried out once every 4 weeks.

 

For patients receiving Octreotide Depot, the determination of PSA concentrations should be performed every month.

 

In patients with impaired renal, hepatic and elderly patients, there is no need to correct the dosage regimen of Octreotide Depot.

 

For the prevention of acute postoperative pancreatitis, Octreotide Depot in a dose of 10 or 20 mg is administered only once, not more than 5 days and no later than 10 days before the proposed surgical intervention.

 

Rules for the preparation of suspension and drug administration

 

The drug Octreotide Depot is administered only intramuscularly. The suspension for the IM injection is prepared with the help of the applied solvent immediately before administration. The drug should be prepared and administered only by specially trained medical personnel.

 

Before the injection, the ampoule with the solvent and the vial with the drug should be removed from the refrigerator and brought toroom temperature (30-50 minutes is required). Keep the bottle with Octreotide Depot strictly vertically. Tapping lightly on the vial, make sure that all the lyophilizate is on the bottom of the vial.

 

Open the package with a syringe and attach a 1.2 mm x 50 mm needle to the syringe to collect the solvent. Open the ampoule with the solvent and draw into the syringe all the contents of the ampoule with the solvent, install the syringe for a dose of 2.0 ml. Remove the plastic cap from the vial containing the lyophilizate. Disinfect the rubber stopper of the vial with an alcohol swab. Insert the needle into the vial with the lyophilizate through the center of the rubber stopper and carefully insert the solvent into the inner wall of the vial without touching the needle with the contents of the vial.

 

Remove the syringe from the vial. The bottle must remain stationary until the solvent is fully saturated with the lyophilisate and a suspension is formed (for about 3-5 minutes). After that, without turning the bottle, you should check the presence of dry lyophilizate at the walls and bottom of the vial. If a dry residue of the lyophilizate is found, leave the vial until it is completely soaked.

 

After you are convinced of the absence of residues of dry lyophilizate,the contents of the vial should be gently stirred in a circular motion for 30-60 seconds until a uniform suspension is formed. Do not overturn or shake the bottle, this can lead to flocculation and the unfitness of the suspension.

 

Quickly insert the needle through the rubber stopper into the vial. Then cut the needle down and, tilting the vial at an angle of 45 degrees, slowly put the suspension in the syringe completely. Do not flip the bottle when typing. A small amount of the drug can remain on the walls and bottom of the vial. The consumption of the residue on the walls and the bottom of the vial is taken into account.

 

Immediately after dialing the suspension, replace the needle with the pink pavilion on the needle with the green pavilion (0.8 x 40 mm), gently flip the syringe and remove the air from the syringe.

 

Suspension of Octreotide Depot should be administered immediately after preparation. Suspension of Octreotide Depot should not be mixed with any other drug in one syringe.

 

Using an alcohol sponge, disinfect the injection site. Insert the needle deep into the gluteus muscle, then gently pull the plunger of the syringe backward to make sure that there is no damage to the vessel.Insert the suspension intramuscularly slowly with constant pressure on the syringe plunger.

 

If you get into a blood vessel, you need to change the injection site and the needle. When clogging the needle, replace it with another needle of the same diameter.

 

With repeated injections, the left and right sides should alternate.

 

Side effect

  • anorexia;
  • nausea, vomiting;
  • abdominal cramps;
  • severe pain in the epigastric region;
  • tension of the abdominal wall;
  • sensation of bloating;
  • excessive gassing;
  • loose stools;
  • diarrhea;
  • steatorrhea;
  • In rare cases, there may be phenomena reminiscent of acute intestinal obstruction;
  • Hyperbilirubinemia in combination with an increase in the activity of alkaline phosphatase, GGT and, to a lesser extent, other transaminases
  • formation of stones in the gallbladder;
  • arrhythmia;
  • bradycardia;
  • tachycardia;
  • dyspnea;
  • a violation of glucose tolerance after meals (due to the suppression of insulin secretion by the drug);
  • hypoglycemia;
  • In rare cases, long-term treatment may develop persistent hyperglycemia;
  • at the injection site, pain, itching or burning sensation, redness, swelling (usually within 15 minutes);
  • allergic reactions;
  • skin rash;
  • alopecia.

 

Contraindications

  • children's age till 18 years;
  • hypersensitivity to octreotide or other components of the drug.

 

Application in pregnancy and lactation

 

The use of Octreotide and Octreotide Depot and Long in pregnancy has not been studied. The drug should be used during pregnancy only if the intended benefit to the mother exceeds the potential risk to the fetus.

 

It is not known whether the drug enters the breast milk, so when using the drug during lactation, breastfeeding should be abandoned.

 

Use in children

 

Contraindicated in children and adolescents under the age of 18 years.

 

Application in elderly patients

 

In elderly patients, there is no need to reduce the dose of Octreotide.

 

special instructions

 

In diabetic patients receiving insulin, Octreotide may reduce the need for insulin.

 

When tumors of the pituitary gland secreting GH, careful monitoring of the patients is necessary, because it is possible to increase the size of tumors with the development of such serious complications as narrowing of the visual fields. In these cases, consideration should be given to the need for other treatments.

 

If the stones in the gallbladder are identified before the treatment, the question of the use of Octreotide is decided individually, depending on the ratio of the potential therapeutic effect of the drug and the possible risk factors associated with the presence of gallstones.

 

Gastrointestinal side effects can be reduced if Octreotide injections are done in between meals or at bedtime.

 

To reduce the phenomena of discomfort at the injection site, it is recommended to bring the drug solution before introducing it to room temperature and introduce a smaller volume of the drug. Several injections should be avoided in the same place at short intervals.

 

Impact on the ability to drive vehicles and manage mechanisms

 

Some of the side effects of Octreotide can adversely affect the ability to drive vehicles and other mechanisms that require increased concentration and speed of psychomotor reactions.

 

Drug Interactions

 

Octreotide reduces the absorption of cyclosporine, slows the absorption of cimetidine.

 

It is necessary to correct the dosage regimen of concomitant diuretics, beta-blockers,blockers of "slow" calcium channels, insulin, oral hypoglycemic drugs.

 

With the simultaneous use of Octreotide and bromocriptine, the bioavailability of the latter increases.

 

There is evidence that somatostatin analogues can reduce the metabolic clearance of substances metabolized by cytochrome P450 isoenzymes, which may be caused by GH suppression. Since it is impossible to exclude such effects of Octreotide, drugs metabolized by isoenzymes of the cytochrome P450 system and having a narrow therapeutic range (quinidine and terfenadine) should be administered with caution.

 

Analogues of the drug Octreotide

 

Structural analogs for the active substance:

  • Genfastat;
  • Octreotide Cabi;
  • Octreotide San;
  • Octreotide Aktavis;
  • Octreotide Depot;
  • Octreotide Long;
  • Octreotide Long FS;
  • Octreotide Phsynthesis;
  • Octreotide acetate;
  • Octretex;
  • Octrid;
  • Serakstal;
  • Sandostatin.

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