Oktra

Octra is a hormonal agent, a representative of the pharmacological series of hypothalamic hormones for systemic use. Refers to octreotide derivatives. ATC code H01C B02.

Octra is available only upon presentation of a doctor's prescription.

Indications Oktra

• for the treatment of acromegaly - to alleviate the main symptoms of the disease and reduce the amount of somatotropin and IGF-1 in the bloodstream, especially in those patients who do not have the expected effect from surgical and radiation treatment;
• for the treatment of acromegaly if it is not possible to perform surgical intervention on the patient, as well as for inter-course maintenance treatment;
• to relieve symptoms associated with neoplasms of the endocrine system of the digestive tract: carcinoid neoplasms, VIPomas, glucagonomas, gastrinomas, insulinomas, etc. Meanwhile, Octra does not belong to antitumor drugs and does not directly eliminate the tumor itself;
• for the treatment of somatoliberin (neoplasms accompanied by hyperproduction of hypothalamic growth hormones);
• to prevent adverse effects after surgery in the pancreas;
• to stop bleeding and prevent recurrence of bleeding from esophageal vessels affected by varicose veins (in combination with sclerosing treatment).

Release form

The medicine is available in 1 ml ampoules, in a cardboard box or blister pack, with enclosed instructions for medicinal use.

Each ampoule contains:

• octreotide 0.1 mg/ml;
• Additional ingredients: mannitol, sodium bicarbonate, lactic acid, water for injection.

Octra is a colorless, sediment-free, transparent liquid.

Pharmacodynamics

The active ingredient of the drug is an analogue of a releasing factor that inhibits the synthesis of pituitary hormones, with similar pharmacotherapeutic characteristics, but with a prolonged (extended in time) effect.

Octra slows down the excessively increased production of somatotropin, as well as substances that are produced in the digestive endocrine system.

In a normal state, the active substance is able to suppress the synthesis of growth hormone, provoked by arginine, physical exercise or hypoglycemia. Injections of the drug are not accompanied by hormonal hypersecretion by the type of negative feedback.

Patients with acromegaly achieve a stable decrease in the amount of somatotropin and stabilization of the IGF-1 (somatomedin C) content by administering the drug.

In a significant number of patients, Octra reduces the severity of symptoms such as headaches, hyperhidrosis, numbness of the body and limbs, arthralgia, neuropathy, apathy. In some cases, injections of the drug contributed to a decrease in the size of neoplasms.

In carcinomas, the use of the drug can alleviate symptoms such as dyspepsia and hot flashes. In most patients, the relief is combined with a decrease in the level of serotonin in the blood and the excretion of 5-hydroxyindoleacetic acid by the kidneys.

In neoplasms with excessive VIP production, the use of Octra helps reduce the manifestations of intestinal hypersecretion, which significantly improves the patient's quality of life. At the same time, a reduction in the number of electrolyte metabolism disorders is achieved, for example, low potassium levels in the blood. This makes it possible to avoid additional administration of fluid and electrolytic mixtures. According to tomographic data, many patients experience inhibition of tumor growth, or even its regression, especially metastatic foci in the liver. Alleviation of clinical manifestations may be accompanied by stabilization of VIP in the blood.

The use of Octra in glucagon therapy can lead to the elimination of the rash, although the drug has no effect on the course of diabetes itself. No adjustment of insulin or hypoglycemic agents is required. Along with the elimination of diarrhea symptoms, body weight may increase. The improvement in the condition is usually long-lasting and stable.

When treating gastrinoma, Octra may reduce the production of gastric juice, which in turn will affect bowel function. Sometimes, a decrease in the level of gastrin in the blood may be observed.

When treating insulinoma, Octra reduces the level of IRI in the blood. When preparing for surgery, the drug can facilitate the restoration and stabilization of blood sugar levels.

Octra alleviates the symptoms of acromegaly without eliminating the disease itself.

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Pharmacokinetics

With subcutaneous injection, the active ingredient is absorbed quickly and completely. The maximum content in the blood is observed after half an hour.

The connection with plasma proteins is about 65%, with blood cells – in small quantities.

Total clearance rates are within 160 ml per minute. Half-life is 100 minutes. The main amount of the drug is excreted with feces, approximately 32% is excreted unchanged with urine. When administered intravenously, the drug is excreted in two stages, which corresponds to 10 and 90 minutes.

In old age, clearance may decrease and half-life may increase. In chronic severe kidney disease, as well as in liver cirrhosis, clearance may decrease by half.

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Dosing and administration

Octra can be administered as subcutaneous or intravenous injections.

The initial dosage is 1 ml per day (subcutaneously). Then the frequency of injections and dosage may increase, which is determined by the tolerability of the drug, the clinical effect and the positive dynamics of treatment. Most often, injections are prescribed up to 3 times a day.

For the treatment of acromegaly, the solution is used subcutaneously from 0.5 to 1 ml every 8-12 hours. Then the dosage is determined depending on the results of hormonal studies, changes in clinical symptoms, and the patient's condition. Most often, the daily amount of the drug can be 0.3 mg. The maximum amount is 1.5 mg per day. Treatment is stopped if the expected effect is not achieved after three months.

For the treatment of endocrine neoplasms of the digestive tract, Octra is administered subcutaneously, initially at 0.05 mg up to 2 times a day. The dosage can then be revised upwards, to 0.1 or 0.2 mg, up to 3 times a day.

To prevent postoperative complications, the solution is administered subcutaneously: 0.1 mg 60 minutes before laparotomy, and 100 mcg three times a day after surgery (for a week). In some situations, the dosage is revised individually.

If the maximum permissible dosage does not produce the desired effect within a week, treatment is discontinued.

In order to stop bleeding from esophageal vessels affected by varicose disease, Octra is administered intravenously, by drip, for 5 days. The rate of administration is 50 mcg per hour, continuously.

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Use Oktra during pregnancy

Unfortunately, there is currently insufficient practical experience of using Octra in pregnant women. In terms of potential danger to the unborn child, the drug belongs to category B. Thus, Octra can be prescribed during pregnancy only in situations where the expected effect for the woman is assessed as higher than the possible risk to the unborn child.

There is also no reliable information about whether the active ingredient of the drug penetrates into breast milk. For this reason, caution should be exercised if Octra is planned for use in nursing women.

Contraindications

This drug should be avoided if the patient is prone to allergic reactions to the active substance of the drug.

Octra should be used with extreme caution and under the mandatory supervision of a specialist during pregnancy, breastfeeding, and in patients with diabetes and gallstone disease.

Side effects Oktra

The hormonal agent may have a number of side effects:

• weight loss, bouts of vomiting and nausea, painful spasms in the epigastric region, increased gas formation, diarrhea, formation of stones in the biliary system;
• inflammatory reaction in the pancreas, cholelithiasis, liver disorders (inflammation of the liver parenchyma without bile stasis), hyperbilirubinemia;
• slowing of the heart rate;
• latent diabetes mellitus, sometimes persistent hyperglycemia, less often hypoglycemia, glucose metabolism disorder;
• allergic reactions (rashes, skin redness, swelling);
• at the injection site – pain in the area of drug administration, swelling, burning sensation, hyperemia;
• rarely – deterioration of hair condition, hair loss.

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Overdose

The use of Octra in significant doses may cause the following symptoms:

• slowing of the heart rate, flushing of the face, pain and spasms in the abdominal cavity, diarrhea, bouts of nausea, feeling of hunger.

The listed symptoms completely disappeared within 24 hours after the administration of a single, high dose of the drug.

Administration of excessive doses was not accompanied by reactions that posed a threat to the patient's viability.

In case of accidental administration of large doses of the drug, symptomatic treatment may be prescribed. Hemodialysis is not required.

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Interactions with other drugs

Octra may decrease the rate of absorption of cyclosporines and cimetidine.

The combined use of the drug leads to an increase in the bioavailability of bromocriptine.

When taken simultaneously with diuretics, ß-blockers, calcium channel blockers, as well as hypoglycemic agents, insulin, glucagon, dosage adjustment is required.

Combination with drugs that are metabolized with the participation of cytochrome P150 isoenzymes should be used with extreme caution. Such undesirable combinations include the drugs quinidine and terfenadine.

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Storage conditions

The medicine should be stored in a dark, dry place, preferably in a special refrigerator, at temperatures from +2°C to +8°C. Children should not be allowed near the places where the medicine is stored.

Shelf life

The shelf life is up to 2 years, after which the medicine should be discarded.