Octreotide Acetate for Injection

Pharmacological action: Octreotide is a synthetic octapeptide compound and a 14-peptide human somatostatin analog. The pharmacological action of octreotide is similar to that of natural hormones, but its inhibitory effect on growth hormone, glucagon and insulin is stronger. Similar to somatostatin, octreotide can also inhibit the response of LH to GnRH, reduce visceral blood flow, and inhibit the secretion of 5-HT, gastrin, vasoactive intestinal peptide, chymotrypsin, motilin and glucagon. Toxicological study: Genetic toxicity: No genetic toxicity was found in laboratory studies. Reproductive toxicity: When rats and rabbits were given octreotide, the dose was equivalent to 16 times the highest human dose calculated based on body surface area, and no effect on fertility and fetuses was found. Carcinogenicity: Octreotide was administered to mice subcutaneously at a dose of up to 2 mg/kg/day (about 8 times the human exposure based on body surface area) for 85 to 89 weeks without any carcinogenicity. Octreotide was administered to rats subcutaneously at the highest dose of 1.25 mg/kg/day (about 10 times the human exposure based on body surface area), and sarcomas and squamous cell tumors were observed at the injection site. The incidence rates of male and female animals were 27% and 12%, respectively, and the incidence rate of the solvent control group was 8 to 10%. However, no tumors were observed at the injection site after continuous use of octreotide for 5 years. In the highest dose group, the incidence rate of uterine adenoma in female animals was 15%, while that in the saline group was 7% and that in the solvent control group was 0%. The occurrence of uterine adenoma in female animals may be related to the estrogen level in elderly animals.

The main ingredient of this product is: octreotide acetate, its chemical name is: D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophanyl-L-lysyl-L-threonyl-L-cysteinyl-L-threoninol (2→7) cyclic disulfide acetate. The auxiliary materials are lactic acid, mannitol, and sodium bicarbonate. Chemical structure: Molecular formula: C49H66N10O10S2·XC2H4O2X=1.5～2.4 Molecular weight: 1019.26·X60.02X=1.5～2.4

This product is white lump or powder.

Hemostatic drugs. Mainly used for bleeding caused by excessive primary fibrinolysis, including acute and chronic, localized or systemic hyperfibrinolytic bleeding, the latter of which is common in cancer, leukemia, gynecological accidents, severe liver disease bleeding, etc.

Before use, fully dissolve this product with 1 ml of water for injection or saline. 1. Continuous intravenous drip of 0.025 mg/hour for esophageal-gastric varicose bleeding. The maximum treatment period is 5 days. It can be diluted with saline or glucose solution. 2. To prevent complications after pancreatic surgery, 0.1 mg is injected subcutaneously 3 times a day for 7 days of continuous treatment. The first injection should be performed at least 1 hour before surgery. 3. The initial dose for gastrointestinal pancreatic endocrine tumors is 0.05 mg subcutaneously, once or twice a day, and then the dose can be gradually increased to 0.2 mg three times a day based on tolerance and efficacy. 4. The initial dose for acromegaly is 0.05-0.1 mg subcutaneously, once every 8 hours, and then the dose is adjusted based on monthly assessments of circulating GH concentrations, clinical responses and tolerance. The optimal dose for most patients is 0.2-0.3 mg/day, and the maximum dose should not exceed 1.5 mg/day. The dose can be reduced as appropriate after several months of treatment under the guidance of monitoring plasma GH levels. If the GH concentration does not decrease and the clinical symptoms do not improve after one month of treatment with this product, discontinuation of the drug should be considered.

1. Local reactions to injection, including pain, tingling or burning sensation at the injection site, accompanied by redness and swelling. These phenomena rarely last more than 15 minutes. Allowing the drug solution to reach room temperature before injection can reduce local discomfort. 2. Gastrointestinal reactions, including loss of appetite, nausea, vomiting, spasmodic abdominal pain, flatulence, loose stools, diarrhea, and steatorrhea. In rare cases, gastrointestinal reactions may resemble acute intestinal obstruction with progressive severe upper abdominal pain, abdominal tenderness, muscle tension, and abdominal distension. 3. Long-term use may lead to the formation of gallstones. 4. Because this product can inhibit the release of GH, glucagon, and insulin, it may cause blood sugar regulation disorders. Because it can reduce patients' postprandial glucose tolerance, a small number of long-term users may cause persistent hyperglycemia, and hypoglycemia has been observed. 5. Others: A few reports of acute pancreatitis may occur, which may gradually disappear after discontinuation of the drug. In rare cases, octreotide acetate treatment has been reported to cause hair loss in patients. Long-term use of this product and the development of gallstones may also lead to pancreatitis. Some patients may develop liver dysfunction, including slowly occurring hyperbilirubinemia with mild increases in alkaline phosphatase, γ-glutamyl transferase and transaminase.

Patients who are allergic to octreotide or any of the excipients in this product are contraindicated.

Precautions for children: There is limited experience with this product in children. Precautions for pregnancy and lactation: There is no experience with its use, and it should only be used when absolutely necessary. Precautions for the elderly: There is no evidence that elderly patients have a decreased tolerance to this product, so it is not necessary to reduce the dose when using this product.

This product can reduce the intestinal absorption of cyclosporine and delay the absorption of cimetidine.

Keep away from light and store at 2-8℃.

0.1mg

24 months

Guangdong Sunho Pharmaceutical Co., Ltd.

• Founded in:

  2005-06-13

• Address:

  No. 17, Jiankang Road, National Health Base, Zhongshan Torch Development Zone

• Tax NO.:

  914420007762231990

• Registered Funds:

  253.47694 million yuan

• Website:

  Log in to view

• Email:

  Log in to view