Octreox (Solution) Instructions for Use

Marketing Authorization Holder

Pharmasintez-Tyumen, LLC (Russia)

ATC Code

H01CB02 (Octreotide)

Active Substance

Octreotide (Rec.INN registered by WHO)

Dosage Forms

	Octreox	Solution for intravenous and subcutaneous administration 50 mcg/ml: 1 ml fl. 1, 2, 5, 6, 10, 20 or 30 pcs.
		Solution for intravenous and subcutaneous administration 100 mcg/ml: 1 ml fl. 1, 2, 5, 6, 10, 20 or 30 pcs.
		Solution for intravenous and subcutaneous administration 200 mcg/ml: 1 ml fl. 1, 2, 5, 6, 10, 20 or 30 pcs.
		Solution for intravenous and subcutaneous administration 300 mcg/ml: 1 ml fl. 1, 2, 5, 6, 10, 20 or 30 pcs.
		Solution for intravenous and subcutaneous administration 500 mcg/ml: 1 ml fl. 1, 2, 5, 6, 10, 20 or 30 pcs.
		Solution for intravenous and subcutaneous administration 600 mcg/ml: 1 ml fl. 1, 2, 5, 6, 10, 20 or 30 pcs.

Dosage Form, Packaging, and Composition

Solution for IV and SC administration transparent, colorless.

Excipients : lactic acid – 3.4 mg, mannitol – 45 mg, sodium bicarbonate – to pH 3.9 – 4.5, water for injections – to 1 ml.

1 ml – vials – carton packs.
1 ml – vials (2) – carton packs.
1 ml – vials (5) – carton packs.
1 ml – vials (6) – carton packs.
1 ml – vials (10) – carton packs.
1 ml – vials (20) – carton packs.
1 ml – vials (30) – carton packs.

Solution for IV and SC administration transparent, colorless.

Excipients : lactic acid – 3.4 mg, mannitol – 45 mg, sodium bicarbonate – to pH 3.9 – 4.5, water for injections – to 1 ml.

1 ml – vials – carton packs.
1 ml – vials (2) – carton packs.
1 ml – vials (5) – carton packs.
1 ml – vials (6) – carton packs.
1 ml – vials (10) – carton packs.
1 ml – vials (20) – carton packs.
1 ml – vials (30) – carton packs.

Solution for IV and SC administration transparent, colorless.

Excipients : lactic acid – 3.4 mg, mannitol – 45 mg, sodium bicarbonate – to pH 3.9 – 4.5, water for injections – to 1 ml.

1 ml – vials – carton packs.
1 ml – vials (2) – carton packs.
1 ml – vials (5) – carton packs.
1 ml – vials (6) – carton packs.
1 ml – vials (10) – carton packs.
1 ml – vials (20) – carton packs.
1 ml – vials (30) – carton packs.

Solution for IV and SC administration transparent, colorless.

Excipients : lactic acid – 3.4 mg, mannitol – 45 mg, sodium bicarbonate – to pH 3.9 – 4.5, water for injections – to 1 ml.

1 ml – vials – carton packs.
1 ml – vials (2) – carton packs.
1 ml – vials (5) – carton packs.
1 ml – vials (6) – carton packs.
1 ml – vials (10) – carton packs.
1 ml – vials (20) – carton packs.
1 ml – vials (30) – carton packs.

Solution for IV and SC administration transparent, colorless.

Excipients : lactic acid – 3.4 mg, mannitol – 45 mg, sodium bicarbonate – to pH 3.9 – 4.5, water for injections – to 1 ml.

1 ml – vials – carton packs.
1 ml – vials (2) – carton packs.
1 ml – vials (5) – carton packs.
1 ml – vials (6) – carton packs.
1 ml – vials (10) – carton packs.
1 ml – vials (20) – carton packs.
1 ml – vials (30) – carton packs.

Solution for IV and SC administration transparent, colorless.

Excipients : lactic acid – 3.4 mg, mannitol – 45 mg, sodium bicarbonate – to pH 3.9 – 4.5, water for injections – to 1 ml.

1 ml – vials – carton packs.
1 ml – vials (2) – carton packs.
1 ml – vials (5) – carton packs.
1 ml – vials (6) – carton packs.
1 ml – vials (10) – carton packs.
1 ml – vials (20) – carton packs.
1 ml – vials (30) – carton packs.

Clinical-Pharmacological Group

Somatostatin analogue. A drug for intensive care in gastroenterology

Pharmacotherapeutic Group

Somatostatin (synthetic analogue)

Pharmacological Action

Octreotide is a synthetic analogue of somatostatin, characterized by a longer duration of action. It inhibits the secretion of growth hormone by the anterior pituitary gland, as well as the secretion of thyroid-stimulating hormone.

It suppresses exocrine and endocrine (insulin, glucagon) secretion of the pancreas, as well as the secretion of gastrin, hydrochloric acid, cholecystokinin, secretin, digestive enzymes, vasoactive intestinal peptide and some other peptides and biologically active substances whose secretion is carried out by the gastroenteropancreatic system. It suppresses gastric and intestinal motility.

Pharmacokinetics

After SC injection, it is rapidly and completely absorbed into the systemic circulation. The C_max of the active substance in plasma is reached within 30 minutes. Plasma protein binding is 65%. Binding to blood cells is extremely insignificant. The V_d is 0.27 l/kg.

The total clearance is 160 ml/min. The T_1/2 after SC injection is 100 minutes. After IV administration, the elimination process occurs in 2 phases, with T_1/2 of 10 minutes and 90 minutes, respectively.

Indications

Acromegaly (with insufficient effectiveness of surgical treatment, radiotherapy, drug therapy with dopamine receptor agonists); tumors characterized by increased production of somatoliberin (growth hormone-releasing factor); relief of symptoms caused by the presence of secreting tumors of the gastroenteropancreatic system (including carcinoid tumors with carcinoid syndrome, glucagonomas, insulinomas, gastrinomas); prevention of complications after pancreatic surgery; diarrhea in AIDS patients refractory to other types of therapy.

For the purpose of stopping bleeding and preventing re-bleeding from esophageal varices in liver cirrhosis (in combination with endoscopic sclerosing therapy).

ICD codes

Dosage Regimen

Determine the dosage individually based on the specific disease, treatment goals, and clinical response.

Administer the solution via subcutaneous (SC) injection or intravenous (IV) infusion; the depot formulation is for deep intramuscular (IM) use only.

For acromegaly, initiate therapy with 50 mcg administered subcutaneously three times daily.

Titrate the dose based on growth hormone (GH) and insulin-like growth factor-1 (IGF-1) levels; the maximum recommended dose is 500 mcg subcutaneously three times daily.

For carcinoid tumors and other neuroendocrine tumors (NETs), initiate therapy with 50 mcg administered subcutaneously once or twice daily.

Gradually increase the dose to control symptoms; the usual therapeutic range is 150-500 mcg subcutaneously three times daily.

For acute bleeding from esophageal varices, administer a 50 mcg intravenous bolus injection followed by a continuous IV infusion at 50 mcg per hour for 2-5 days.

For prevention of postoperative pancreatic complications, administer 100 mcg subcutaneously three times daily for 7 consecutive days, starting preoperatively at least one hour before surgery.

For diarrhea in AIDS patients, administer a starting dose of 100 mcg subcutaneously as a single injection; titrate to a maximum of 500 mcg subcutaneously three times daily based on response.

Select the appropriate vial concentration (50, 100, 200, 300, 500, or 600 mcg/ml) to accurately measure the prescribed dose.

Rotate subcutaneous injection sites to minimize local reactions; avoid multiple injections in the same area.

For intravenous infusion, dilute the required dose in 50-200 ml of 0.9% Sodium Chloride or 5% Dextrose solution and infuse over 15-30 minutes.

Monitor blood glucose levels regularly, especially in patients with cirrhosis and variceal bleeding, due to the risk of hyperglycemia.

Perform ultrasound examination of the gallbladder before and periodically during long-term therapy to monitor for cholelithiasis.

Adverse Reactions

From the digestive system anorexia, abdominal pain, nausea, vomiting, bloating, diarrhea, steatorrhea; impaired glucose tolerance; rarely – severe pain in the epigastrium, tenderness on palpation, tension of the abdominal wall muscles, acute hepatitis, hyperbilirubinemia, increased activity of liver enzymes; with long-term use in some cases – formation of gallstones.

Local reactions pain, burning, itching, redness, swelling at the injection site.

Contraindications

Hypersensitivity to octreotide.

Use in Pregnancy and Lactation

Octreotide should be used during pregnancy and lactation only for strict indications.

Special Precautions

The drug should be used with caution in cholelithiasis, diabetes mellitus.

Before starting and during treatment, an ultrasound examination of the gallbladder is recommended. It should be borne in mind that Octreotide does not have antitumor activity.

During treatment, systematic monitoring of blood glucose concentration is necessary, especially in patients with bleeding from esophageal varices in liver cirrhosis, because there is an increased risk of hyperglycemia.

Drug Interactions

Somatostatin analogues may reduce the clearance of substances metabolized with the participation of cytochrome P450 isoenzymes, which may be due to the suppression of growth hormone.

With simultaneous use, the bioavailability of bromocriptine increases; with insulin – an enhancement of the hypoglycemic effect is possible; with cyclosporine – the absorption of cyclosporine decreases; with cimetidine – the absorption of cimetidine slows down.

Storage Conditions

Store at 2°C (36°F) to 8°C (46°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.