Octra

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

Octra is only released on presentation of a prescription from a doctor.

Indications Octra

• for the treatment of acromegaly - to relieve the main signs of the disease and reduce the amount of somatotropin and IGF-1 in the bloodstream, especially those patients who do not have the expected effect of surgical and radiation treatment;
• for the treatment of acromegaly, if there is no opportunity to conduct surgical intervention to the patient, and also as an intercourse supportive treatment;
• to alleviate the symptoms associated with neoplasms of the endocrine system of the digestive tract: with carcinoid neoplasms, Vipoma, glucagonomas, gastrinomas, insulinomas, etc. Meanwhile, Octra does not belong to anti-tumor drugs and does not directly eliminate the tumor itself;
• for treatment with somatoliberin (neoplasms accompanied by hyperproduction of hypothalamic growth hormones);
• for the prevention of adverse effects after surgery in the pancreas;
• to stop bleeding and prevent the recurrence of bleeding from the esophageal vessels affected by varicose veins (in combination with sclerosing treatment).

Release form

The drug is issued in ampoules of 1 ml, in a cardboard bundle or blister pack, with a nested annotation for medicinal use.

Each ampoule contains:

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

 Octra is a liquid without color and sediment, transparent.

Pharmacodynamics

The active ingredient of the drug is an analog of the releasing factor inhibiting the synthesis of pituitary hormones, with similar pharmacotherapeutic characteristics, but with prolonged (prolonged in time) action.

Octra retards excessively increased production of somatotropin, as well as substances that are produced in the digestive endocrine apparatus.

In the normal state, the active substance is capable of suppressing the synthesis of growth hormone triggered by arginine, physical exertion or a state of hypoglycemia. Injections of the drug are not accompanied by hormonal hypersecretion in the negative reciprocal connection type.

Patients with acromegaly by administration of the drug achieve a steady decrease in the amount of growth hormone and stabilize the content of IGF-1 (somatomedin C).

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

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

With neoplasms flowing with excessive production of VIP, the use of Octr makes it possible to 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 exchange disorders, for example, a low potassium content in the blood, is achieved. This makes it possible to avoid additional introduction of liquid and electrolytic mixtures. According to tomographic data, in many patients inhibition of tumor growth is observed, or even its regression, in particular of metastatic foci in the liver. Relief of clinical manifestations may be accompanied by stabilization of VIP in the blood.

The use of Octra in the treatment with glucagon can lead to the elimination of the rash, although the drug itself has no effect on the course of diabetes mellitus. Correction of insulin and hypoglycemic agents is not required. Simultaneously with elimination of symptoms of diarrhea, the body weight may increase. Improvement of the condition is usually lasting and stable.

With the treatment of gastrinoma, Octra can reduce the production of gastric juice, which, in turn, will affect the functioning of the intestine. Sometimes there may be a decrease in the level of gastrin in the blood.

When treating insulinoma, Octra lowers the level of IRI in the blood. In preparation for surgery, the drug can facilitate the recovery and stabilization of blood sugar levels.

Octra facilitates the symptoms of acromegaly, while not eliminating the disease itself.

[1]

Pharmacokinetics

With subcutaneous injection, the assimilation of the active ingredient occurs quickly and fully. 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 amounts.

The total clearance is within 160 ml per minute. Half-life is 100 minutes. The main amount of the drug is excreted with feces, about 32% is unchanged in urine. With intravenous injection, the drug is withdrawn in two stages, which corresponds to 10 and 90 minutes.

In the elderly, the clearance may decrease, and the half-life duration may increase. In chronic severe kidney lesions, as well as with liver cirrhosis, the clearance may be halved. 

[2]

Dosing and administration

Octra can be administered in the form of subcutaneous or intravenous injections.

The initial dosage is prescribed in the amount of 1 ml per day (subcutaneously). Further, 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. More 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. Further, the dosage is determined depending on the results of hormonal studies, changes in clinical symptoms, and the patient's condition. More often, the daily amount of the drug can be 0.3 mg. The limiting amount is 1.5 mg per day. Treatment is terminated if the expected effect is not achieved after three months.

For the treatment of endocrine neoplasms of the digestive tract, Octra is used subcutaneously, initially at 0.05 mg up to 2 times a day. Further, the dosage can 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 μg three times a day after surgery (within a week). In some situations, dosage is reviewed on an individual basis.

If the maximum allowable dosage does not have the desired effect for a week, the treatment is canceled.

In order to stop bleeding from the affected esophagus with varicose veins, Octra is used intravenously, by dropping, for 5 days. The rate of administration is 50 μg per hour, continuously.

[4], [5]

Use Octra during pregnancy

Unfortunately, at present there is insufficient practical experience of using Octra by pregnant women. In relation to the potential danger to the future child, the medicine belongs to category B. Thus, Octra can be prescribed during pregnancy only in situations where the expected effect for a woman is assessed higher than the possible risk for a future baby.

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 Octr is planned for the treatment of lactating women. 

Contraindications

It is necessary to avoid prescribing this drug if the patient is inclined to allergic reactions to the active substance of the drug.

It is very cautious and under the mandatory supervision of a specialist, Octra is used during pregnancy, breast feeding, as well as in patients with diabetes and cholelithiasis. 

Side effects Octra

The hormonal agent can have a number of side effects:

• weight loss, bouts of vomiting and nausea, painful spasms in the epigastric region, increased gas formation, diarrhea, the formation of stones in the biliary system;
• inflammatory reaction in the pancreas, cholelithiasis, disorders of the liver (inflammation of the hepatic parenchyma without stagnation of bile), hyperbilirubinemia;
• slowing the rhythm of cardiac activity;
• latent diabetes mellitus, sometimes - stable hyperglycemia, less often - hypoglycemia, glucose metabolism disorder;
• allergic manifestations (rashes, redness of the skin, swelling);
• at the injection site - soreness in the zone of drug administration, edema, burning sensation, hyperemia;
• rarely - deterioration of the hair, their loss.

[3]

Overdose

The use of Octra in significant dosages can cause the following symptoms:

• slowing heart rate, facial hyperemia, abdominal pain and cramps, diarrhea, nausea, hunger.

The listed symptoms completely self-eradicated during the day after the introduction of a single overestimated dose of the drug.

The introduction of high doses was not accompanied by reactions that pose a danger 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.

[6]

Interactions with other drugs

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

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

With simultaneous administration with diuretics, ß-adrenoblockers, calcium channel blockers, as well as with hypoglycemic agents, insulin, glucagon, dosage adjustment is required.

Combination with drugs that are metabolized with the participation of cytochrome P150 isoenzymes should be applied with extreme caution. To such undesirable combinations should be attributed drugs quinidine and terfenadine. 

[7], [8]

Storage conditions

Storage of the drug should be provided in a darkened dry place, preferably in a special refrigerator, at temperatures ranging from + 2 ° C to + 8 ° C. Children should not be allowed to store medicines. 

Shelf life

Shelf life - up to 2 years, after which the medical product should be discarded.