Oktrayd

Octraide is a medicinal product, a representative of the pharmacotherapeutic series of hypothalamic hormones of systemic use. Refers to octreotide derivatives. 

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

Indications Oktrayd

For the treatment of acromegaly (increased production of growth hormone) - if the effectiveness of surgical treatment was insufficient, as well as to support the body between therapeutic courses, or if it is impossible to conduct an operation to the patient;

• for the treatment of oncological pathologies of the endocrine system (digestive tract), namely carcinoma, insulin, VIP, gastrin, glucagon;
• 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).

[1], [2]

Release form

The medicine is released in ampoules of 1 ml, in a cardboard box, with a nested annotation to the drug use.

Each ampoule contains:

• octreotide acetate (analogue of octreotide) 100 μg;
• additional ingredients: 2 mg of acetic acid, 2 mg of sodium acetate trihydrate, 7 mg of sodium chloride, water for injection up to 1 ml.

Octread is a clear, colorless liquid. The ampoule has a blue dot for tampering and an orange rim in place of the cleavage. 

[3], [4]

Pharmacodynamics

The active component of the drug is analogous to the releasing factor inhibiting the production of pituitary hormones, with similar pharmacotherapeutic properties, but with prolonged (prolonged in time) action.

Okkrayd brakes 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 able to inhibit 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 administering 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, Octread reduces the severity of such symptoms as headaches, hyperhidrosis, numbness of the 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, Octreeid treatment allows 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 Octread 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 itself. Correction of insulin and hypoglycemic agents is not required. Simultaneously with eliminating the symptoms of diarrhea, body weight may increase. Improvement of the condition is usually lasting and stable.

When treating gastrinom, Octreeid 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 insulin, Octread reduces the level of IRI in the blood. In preparation for surgery, the drug can facilitate the recovery and stabilization of blood sugar levels.

Okkrayd facilitates the symptoms of acromegaly, suppressing the production of somatotropin, peptides and serotonin. At the same time the level of IGF-1 is normalized.

[5]

Pharmacokinetics

1. With subcutaneous injection, the assimilation of the active component occurs easily. The maximum content in the blood is observed after half an hour.

2. The connection with plasma proteins is about 65%, with blood cells - in small amounts.

3. The indicators of total clearance - 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.

4. In the senile age, the clearance may decrease, and the half-life duration may increase. In chronic severe renal lesions, clearance may be halved.

[6]

Dosing and administration

Okkrayd is prescribed in the form of subcutaneous or intravenous injections.

The initial dosage is prescribed in the amount of 50 mcg per day (subcutaneously 1-2 times). 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 drug is administered subcutaneously from 50 to 100 μg 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 from 200 to 300 μg. The limit is 1500 μg per day. Treatment is terminated if the expected effect is not achieved after three months.

For the treatment of endocrine neoplasm of the digestive tract Oktrayd is used subcutaneously, initially 50 mcg up to 2 times a day. Further, the dosage can be revised upwards, up to 100 or 200 μg, up to 3 times a day.

To prevent postoperative complications, the solution is administered subcutaneously: 100 μg 60 minutes before laparotomy, and 100 μg three times a day - after the operation (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, Octread is administered intravenously, by dropping, for 5 days. The rate of administration is 25 μg per hour.

[9], [10]

Use Oktrayd during pregnancy

To date, there is insufficient practical experience with the use of Octraide by pregnant women. In relation to the potential danger to the future child, the drug belongs to the B category. Thus, it is recommended that Octrides be administered 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 no reliable information about whether the active component of the drug penetrates into breast milk. For this reason, caution should be exercised if Octrides is to be used in a nursing woman. 

Contraindications

It should avoid the prescription of the drug with the patient's inclination to an allergic reaction to the active substance of the drug.

Extremely cautious and under the mandatory supervision of a doctor, Octread is used during pregnancy, breastfeeding, as well as in patients with diabetes and cholelithiasis. 

Side effects Oktrayd

The medicine can have a number of side effects:

• emaciation, attacks of vomiting and nausea, painful spasms in the epigastric region, increased gas formation, diarrhea, the formation of stones in the biliary system;
• acute inflammation of the pancreas, cholelithiasis, disorders of the liver (inflammation of the hepatic parenchyma without stagnation of bile), hyperbilirubinemia;
• slowing of the heart rate;
• latent diabetes mellitus, sometimes - stable hyperglycemia, less often - hypoglycemia, glucose metabolism disorder;
• allergic manifestations (rashes, redness of the skin, swelling);
• local - soreness in the zone of drug administration, edema, burning sensation, hyperemia;
• rarely - transient alopecia.

[7], [8]

Overdose

Tests of the dose in the amount of 2000 micrograms subcutaneously three times during 2-3 months were transferred by patients without problems.

Use in more significant dosages may cause the following symptoms:

• reduction in heart rate, facial hyperemia, abdominal pain and cramps, diarrhea, nausea, "empty stomach" feeling.

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. 

[11]

Interactions with other drugs

Octward reduces 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. This includes drugs such as quinidine and terfenadine. 

[12],

Storage conditions

The drug is stored in dark, dry places, preferably in a special refrigerator, at temperatures ranging from + 2 ° C to + 8 ° C. Children should not be allowed to store medicines.

[13],

Shelf life

Shelf life - up to 3 years, after which the medicine should be discarded.

[14]