Universal reference book for medicines
Product name: OCTRIDE (OCTRIDE)

Active substance: octreotide

Type: Somatostatin analogue.
The drug for intensive care in gastroenterology
Manufacturer: Sun Pharmaceutical Industries (India)
Composition, form of production and packaging
The solution for the / in and / or the introduction of a
transparent, colorless.

1 ml

octreotide acetate 64 μg,

which corresponds to the content of octreotide 50 μg

Excipients: acetic acid ice - 2 mg, sodium acetate trihydrate - 2 mg, sodium chloride - 7 mg, water d / and - up to 1 ml.

1 ml - ampoules of colorless glass (1) - plastic pallets (1) - cardboard boxes.

The solution for the / in and / or the introduction of a transparent, colorless.

1 ml

octreotide acetate 128 μg,

which corresponds to the content of octreotide 100 μg

Excipients: acetic acid ice - 2 mg, sodium acetate trihydrate - 2 mg, sodium chloride - 7 mg, water d / and - up to 1 ml.

1 ml - ampoules of colorless glass (1) - plastic pallets (1) - cardboard boxes.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Somatostatin analogue.
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, as well as peptides and serotonin produced in the gastro-entero-pancreatic endocrine system.

In healthy individuals, octreotide, like somatostatin, suppresses the secretion of growth hormone caused by arginine, exercise and insulin hypoglycemia;
secretion of insulin, glucagon, gastrin and other peptides of the gastro-entero-pancreatic endocrine system caused by food intake, as well as the secretion of insulin and glucagon stimulated with arginine; secretion of thyrotropin, caused by thyroidiberin.
The suppressing effect on the secretion of growth hormone in octreotide, in contrast to somatostatin, is expressed to a much greater extent than on the secretion of insulin.
The introduction of octreotide is not accompanied by the phenomenon of hypersecretion of hormones by the mechanism of negative feedback.
In patients with acromegaly, the administration of octreotide provides, in the vast majority of cases, a persistent decrease in the level of growth hormone and the normalization of the concentration of insulin-like growth factor 1 / somatomedin C (IGF-1).

In most patients with acromegaly, octreotide significantly reduces the severity of such symptoms as headache, increased sweating, paresthesia, fatigue, pain in the bones and joints, peripheral neuropathy.
It was reported that treatment with octreotide of individual patients with pituitary adenomas, secreting growth hormone, led to a decrease in the size of the tumor.
In carcinoid tumors, the use of octreotide can lead to a decrease in the severity of the symptoms of the disease, primarily such as hot flashes and diarrhea.
In many cases, clinical improvement is accompanied by a decrease in plasma serotonin concentration and excretion of 5-hydroxyindoleacetic acid in the urine.
In tumors characterized by hyperproduction of the vasoactive intestinal peptide (WIPO), the use of octreotide in most patients reduces the severe secretory diarrhea that is characteristic of this condition, which in turn leads to an improvement in the quality of life of the patient.
At the same time, there is a decrease in associated electrolyte imbalance, for example, hypokalemia, which allows to cancel enteral and parenteral administration of fluid and electrolytes. According to computed tomography, in some patients, the progression of the tumor slows or stops, and even the decrease in its size, especially the metastases to the liver. Clinical improvement is usually accompanied by a decrease (up to normal values) of the concentration of vasoactive intestinal peptide (VIP) in plasma.
With glucagonomes, the use of octreotide in most cases leads to a marked decrease in the necrotizing migrating rash that is characteristic of this condition.
Octreotide does not have any significant effect on the severity of diabetes mellitus, often observed with glucagonomes, and usually does not lead to a decrease in the need for insulin or oral hypoglycemic drugs. Patients suffering from diarrhea, octreotide causes it to decrease, which is accompanied by an increase in body weight. When octreotide is used, there is often a rapid decrease in plasma glucagon concentration, but this effect does not persist with long-term treatment. At the same time, symptomatic improvement remains stable for a long time.
In gastrinomas / Zollinger-Ellison syndrome, octreotide, used as a monotherapy or in combination with histamine H 2 receptor blockers and proton pump inhibitors, can reduce the formation of hydrochloric acid in the stomach and lead to clinical improvement, incl.
and in relation to diarrhea. It is also possible to reduce the severity and other symptoms likely associated with the synthesis of peptides by the tumor, incl. tides. In some cases, a decrease in the concentration of gastrin in the plasma.
In patients with insulinomas, octreotide reduces the level of immunoreactive insulin in the blood.
In patients with operable tumors, octreotide can provide restoration and maintenance of normoglycemia in the preoperative period. In patients with inoperable benign and malignant tumors, glycemic control may improve without a simultaneous prolonged decrease in insulin levels in the blood.
In patients with rare tumors, hyper-growth hormone releasing factor (somatoliberinomas), octreotide reduces the severity of the symptoms of acromegaly.
This, apparently, is due to the suppression of the secretion of the releasing factor of growth hormone and the growth hormone itself. In the future, it is possible to reduce the size of the pituitary gland, which were increased before the treatment.
PHARMACOKINETICS

Suction

After sc administration, the drug is quickly and completely absorbed.
T max in blood plasma (5.2 mg / ml at a dose of 0.1 mg) is 30 minutes.
Distribution

Binding to plasma proteins - 65%, with shaped elements of blood - is extremely insignificant.
V d is 0.27 l / kg.
Excretion

The total clearance is 160 ml / min.
T 1/2 is 100 minutes. Most of the drug is excreted through the intestine, about 32% are excreted unchanged by the kidneys. After intravenous administration, excretion is carried out in 2 phases, T 1/2 is 10 and 90 minutes, respectively.
Pharmacokinetics in special clinical cases

In elderly patients, clearance of octreotide decreases, and T 1/2 increases.

In chronic renal failure of severe severity, the clearance decreases by a factor of 2.

INDICATIONS

- Acromegaly (when adequate control of the 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);

- therapy of endocrine tumors of the gastrointestinal tract and pancreas: carcinoid tumors with the phenomena of carcinoid syndrome;
insulinomas; VIPoms;gastrinomas (Zollinger-Ellison syndrome);
- Glukagonomy (for the control of hypoglycemia in the preoperative period, as well as for maintenance therapy);

- somatoliberynomas (tumors characterized by hyperproduction of growth hormone releasing factor);

- prevention of complications after operations on the pancreas;

- stop bleeding and prevent bleeding from varicose veins of the esophagus with cirrhosis of the liver (in combination with endoscopic sclerosing therapy);

- Treatment of acute pancreatitis.

DOSING MODE

The drug is intended for p / to and / in the introduction.

The initial dose is 50 mcg / day p / k 1 or 2 times / day.
After that, the number of injections and the dose can be gradually increased, based on the tolerability, clinical response and effects on the levels of hormones produced by the tumor (in the case of carcinoid tumors - the effect on the excretion of urinary 5-hydroxyindoleacetic acid). The drug is usually used 2-3 times / day.
In acromegaly, the drug is given SC at an initial dose of 50-100 μg, at intervals of 8 or 12 hours. Subsequently, the dose selection is based on the results of a monthly monitoring of the growth hormone concentration in the blood, the analysis of clinical symptoms and the tolerability of the drug.
In most cases, the daily dose is 200-300 μg. The maximum dose is 1500 mcg / day. If after 3 months of treatment there is no sufficient reduction of growth hormone and an improvement in the clinical picture of the disease, therapy should be discontinued.
With endocrine tumors of the gastroenteropancreatic system, the drug is administered SC in the initial dose of 50 μg 1-2 times / day.
Further, depending on the effect achieved, the effect on the concentration of hormones produced by the tumor (in the case of carcinoid tumors - the effect on the release of 5-hydroxyindoleacetic acid in the urine) and tolerability, the dose can be gradually increased to 100-200 μg 3 times / day.
To prevent complications after operations on the pancreas, the drug is given SC, the first dose is 100 μg for 1 hour before laparotomy, after surgery - 100 μg 3 times / day, for 7 consecutive days.
In exceptional cases, higher doses may be required. Supportive doses of the drug should be selected individually.
In the event that therapy in the maximum tolerated dose is not effective within 1 week, therapy should be discontinued.

To stop bleeding from varicose veins of the esophagus, the drug is injected intravenously at a rate of 25 μg / h for 5 days.

For the treatment of acute pancreatitis, the drug is administered SC in a dose of 100 μg 3 times / day for 5 days.
It is possible to appoint up to 1200 mcg / day using an intravenous route.
The rules of injection

With n / k introduction, multiple injections of the drug should be avoided in the same place for a short time.

When iv administration of the drug immediately before use, the contents of the single-use vial or reusable vial should be diluted in physiological saline.
The dilution volume will depend on the infusion system used, and it should be modified to ensure continuous administration of octreotide at the recommended rate. After the drug has been diluted, the resulting solution should be used within 24 hours. It is necessary to destroy the unused solution.
Before / in the introduction of the solution, it must be checked for transparency, presence of particles, sediment, discoloration and leakage, in all cases when the solution and material of the package permit.
Do not use the drug if it is cloudy, contains particles, sediment, if its color has changed or traces of streaks are visible.
SIDE EFFECT

On the part of the digestive system: anorexia, nausea, vomiting, abdominal cramps, bloating, excessive gas formation, loose stools, diarrhea, steatorrhea;
with prolonged use, the formation of stones in the gallbladder.
Although the release of fat with feces may increase, to date, there is no evidence that prolonged treatment with octreotide can lead to malnutrition due to malabsorption (malabsorption).
In rare cases, phenomena that resemble acute intestinal obstruction are possible: progressive bloating, severe pain in the epigastric region, and stress of the abdominal wall. The frequency of side effects from the gastrointestinal tract can be reduced by increasing the time intervals between meals and the administration of octreotide.
There have been reports of rare cases of acute pancreatitis that developed during the first hours or days of octreotide.
With prolonged use, there have been cases of pancreatitis associated with cholelithiasis.
There are separate reports on the development of violations of liver function (acute hepatitis without cholestasis with normalization of transaminases after octreotide abolition);
slow development of hyperbilirubinemia, accompanied by an increase in the parameters of alkaline phosphatase, GGT, to a lesser extent, other transaminases.
From the side of the cardiovascular system: in some cases - bradycardia.

From the side of metabolism: a decrease in glucose tolerance after eating;
with prolonged use of SC in some cases, persistent hyperglycemia may develop; sometimes - the state of hypoglycemia. Octreotide can affect glucose metabolism, as it inhibits the formation of GH.
Allergic reactions: rarely skin manifestations;
in some cases - anaphylactic reactions.
Local reactions: pain, itching, or burning, redness or swelling at the site of the injection are possible (usually within 15 minutes).
The severity of local reactions can be reduced by using a room temperature solution, or by introducing a smaller volume of a more concentrated solution.
Other: in rare cases - temporary hair loss.

CONTRAINDICATIONS

- Hypersensitivity to the components of the drug.

With caution should apply the drug for cholelithiasis, diabetes, pregnancy and lactation.

PREGNANCY AND LACTATION

Clinical experience with octreotide in pregnancy is limited.
Octreotide 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 octreotide is excreted in breast milk, so care should be taken with octreotide for the treatment of nursing mothers.

APPLICATION FOR FUNCTIONS OF THE LIVER

Currently, there is no data that would indicate the need to adjust the dose of the drug in patients with impaired renal function.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Since there is evidence of an increase in T 1/2 octreotide in patients with liver cirrhosis, correction of the maintenance dose in patients with impaired hepatic function is recommended .

APPLICATION FOR CHILDREN

The experience with octreotide in children is limited.

SPECIAL INSTRUCTIONS

When tumors of the pituitary gland secreting GH, careful monitoring of the patient 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. In 15-30% of patients receiving octreotide c / k for a long time, gallstones may appear in the gall bladder. The prevalence in the general population (age 40-60 years) is 5-20%.
The experience of long-term treatment with octreotide prolonged action of patients with acromegaly and tumors of the gastrointestinal tract and pancreas suggests that octreotide prolonged action, in comparison with short-acting octreotide, does not lead to an increase in the incidence of gallbladder stones.

In patients with type 1 diabetes, octreotide can affect glucose metabolism and, therefore, reduce the need for injected insulin.
For patients with type 2 diabetes mellitus and patients without concomitant disturbance of carbohydrate metabolism, octreotide injections can lead to postprandial glycemia. In this regard, it is recommended to regularly monitor the level of glycemia and, if necessary, correct hypoglycemic therapy.
In patients with insulinomas, an increase in the severity and duration of hypoglycemia may occur in patients with insulinomas (this is associated with a more pronounced inhibitory effect on GH and glucagon secretion than on insulin secretion, and also with a shorter duration of inhibitory effect on insulin secretion).
A systematic observation of these patients is shown.
Before the appointment of octreotide, the initial ultrasound of the gallbladder should be performed in all patients.
During treatment with octreotide, repeated ultrasound of the gallbladder should be performed, preferably at intervals of 6-12 months. Stones in the gallbladder, if they are found, are usually asymptomatic. In the presence of clinical symptoms conservative treatment (for example, administration of bile acid preparations) or surgical intervention is indicated.
If gallbladder stones are found even before the start of treatment, it is necessary to evaluate the potential benefits of octreotide therapy in comparison with the possible risk associated with the presence of gallstones.

At present, there is no evidence that octreotide adversely affects the course or prognosis of an already existing cholelithiasis.

Management of patients whose gallstones are formed during treatment with octreotide

a) Asymptomatic gallstones: the use of octreotide can be discontinued or continued - according to the benefit / risk ratio estimate.
In any case, no other measures are required, except to continue inspections, making them, if necessary, more frequent.
b) Stones of the gallbladder with clinical symptoms: the use of octreotide can be stopped or continued - according to the benefit / risk ratio estimate.
In any case, the patient should be treated in the same way as in other cases of cholelithiasis with clinical manifestations. Drug treatment includes the use of combinations of bile acid preparations (for example, chenodeoxycholic acid at a dose of 7.5 mg / kg / day in combination with ursodeoxycholic acid in the same dose) under ultrasound control until the stones disappear completely.
Currently, there is no data that would indicate the need for dose adjustment in patients
elderly age and in patients with impaired renal function.
Since there is evidence of an increase in T 1/2 octreotide in patients with cirrhosis of the liver, correction of the maintenance dose in
patients with impaired liver function.
Use in Pediatrics

The experience with octreotide in children is limited.

Impact on the ability to drive vehicles and manage mechanisms

There is no data on the effect of Oktyr's drug on the ability to drive vehicles and to work with mechanisms.

OVERDOSE

Doses up to 2000 mg of octreotide in the form n / k injection 3 times over several months were well tolerated.
Symptoms: maximum single dose at / in an adult patient bolus of 1 mg. It is noted symptoms such as a decrease in heart rate, flushing, abdominal pain, spastic nature, diarrhea, nausea, a feeling of emptiness in the stomach. These symptoms resolved within 24 hours from the time of drug administration.
One patient by continuous infusion dose excess octreotide was introduced in error (250 g / h instead of 25 g / h), which is not accompanied by side effects.
In cases of acute overdose has not been observed any life-threatening reactions.
Treatment: symptomatic therapy.

DRUG INTERACTION

Octreotide decreases absorption of cyclosporin slows absorption cimetidine.
With simultaneous application of octreotide and bromocriptine increases the bioavailability of the latter.
Requires correction dosing regimen used simultaneously diuretics, beta-blockers, calcium channel blockers slow, insulin, oral hypoglycemic drugs, glucagon.
There is evidence that somatostatin analogs can reduce the metabolism of drugs metabolized by cytochrome P450 (may be due to suppression of GH). Since it is impossible to eliminate such effects of octreotide, drugs metabolized by this enzyme system and have a narrow therapeutic range of doses should be administered with caution.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children, protected from light at a temperature of 2 ° to 8 ° C.
Shelf life - 3 years.
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