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Octreotide

Digestive system drugs Dosage and administration Category Toxicity grading Acute toxicity Flammability hazard characteristics storage properties Extinguishing media
Octreotide
Octreotide
CAS No.
79517-01-4
Chemical Name:
Octreotide
Synonyms
OCTREOTIDE;SMS-201-995;SANDOSTATIN;SMS 201-995ac;Sandostatin LAR;r*))-(racetate(salt);Octreotide (SMS 201-995);M.W. 1019.24 C49H66N10O10S2;OCTREOTIDE (SMS 201-995), ACETATE;FCFWKTCT-OL (DISULFIDE BRIDGE: 2-7)
CBNumber:
CB0279552
Molecular Formula:
C49H66N10O10S2
Formula Weight:
1019.24
MOL File:
79517-01-4.mol

Octreotide Properties

Melting point:
153-156°C
alpha 
D20 -42° (c = 0.5 in 95% acetic acid)
storage temp. 
−20°C
solubility 
H2O: soluble
InChIKey
XQEJFZYLWPSJOV-XJQYZYIXSA-N
CAS DataBase Reference
79517-01-4
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
WGK Germany  3
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning P264, P280, P305+P351+P338,P337+P313P
Precautionary statements:
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Octreotide price More Price(2)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich PHR1880 Octreotide Acetate Pharmaceutical Secondary Standard; Certified Reference Material 79517-01-4 10mg $219 2018-11-23 Buy
Sigma-Aldrich 1477604 Octreotide acetate 79517-01-4 4.37mg $1254.4 2018-11-20 Buy

Octreotide Chemical Properties,Uses,Production

Digestive system drugs

Octreotide belongs to digestive system drugs, which is an artificially synthetic cyclic octapeptide compound, and is a homolog of natural somatostatin. It contains the pharmacological activity of a natural somatostatin, and has long-lasting effects (the half-lifetime of this product is 1.5-hour, while it is 2 to 3 minutes of natural somatostatin). The product selectively inhibited the secretion of growth hormone, glucagon and insulin, and the effect is stronger than natural. It is proved by animal experiments: intravenous this product for 15 minutes, the inhibition of growth hormone release is 70 times higher than the natural somatostatin, and the inhibition of insulin release is 3 times than the natural somatostatin. It has also the inhibition effect to thyrotropin, adrenocorticotropic hormone, gastrin, cholecystokinin, vasoactive intestinal polypeptide. As well as it can inhibit the secretion of gastric acid, pancreatic amylase, lipase and pepsin. It can slow down pass through time of gastrointestinal tract, which promotes the absorption of water and electrolytes. It has the contract effect of visceral blood vessels, which can reduce splanchnic blood flow, and reduce the blood flow of liver. Thus, it reduces the portal pressure and portal blood flow, and reduces excessive secretion of intestinal tract, and it may enhance the intestinal absorption of water and the Na+.
The amino acids of 1,4,8 positon is unnatural amino acids on the chemical structure of the product, so it is less susceptible to enzyme hydrolysis, and it has more longer half-lifetime. It is absorbed rapidly and completely by subcutaneous injection of the product. The time to peak plasma concentration is 0.5-hour, and the volume of distribution is 0.27 L/kg. The half-lifetime is 1.5-hour, and the metabolic clearance rate is 160 ml/min. It is biphasic elimination as intravenous injection of this product, the half-lifetime of α phase and β phase are 10 minutes and 90 minutes, respectively. The plasma protein binding rate is 65%.
Octreotide is clinically used for the treatment of esophageal varices caused by portal hypertension, acromegaly, gastrointestinal bleeding including cirrhosis, esophageal varices bleeding, peptic ulcer bleeding and stress ulcer bleeding, pancreatic diseases including heavy acute pancreatitis, pancreatic trauma, or pancreatic fistula after surgery, and prevention of complications after pancreas surgery. It is also used for gastrointestinal fistula, digestive endocrine tumors such as vasoactive intestinal peptide tumors, gastrinoma, glucagon tumors, ectopic ACTH syndrome, carcinoid syndrome, and it is used for acromegaly, exophthalmus hyperthyroidism disease, after the removal of the entire colon appearing persistent and intractable diarrhea, AIDS-related diarrhea. Intrathecal injection of this product can treat cancer pain.

Dosage and administration

1. prevention of complications of pancreatic surgery: one hour before surgery, subcutaneous injection of 0.1mg octreotide; then 0.1mg subcutaneously 3 times a day for seven days.
2. treatment of varices caused by esophagus portal hypertension: 0.1mg intravenous injection, then 0.5mg, every two hours by intravenous drip.
3. stress ulcers and gastrointestinal bleeding: 0.1mg subcutaneously 3 times a day.
4. severe pancreatitis: 0.1mg subcutaneous injection, 4 times a day for 3 to 7 days; pancreatic injury or pancreatic fistula after surgery, subcutaneous injection, each 0.1mg, every 8 hours for 7 to 14 days.
5. gastrointestinal fistula and digestive tract endocrine system of cancer adjuvant therapy: subcutaneous 0.1mg, 3 times a day, a course for10 to 14 days.
6. digestive system endocrine tumors, Graves' disease, acromegaly and AIDS-related diarrhea: subcutaneous 0.1mg, 3 times a day, acromegaly treatment for 10 to 14 days. There are injection site pain or tingling, and it is usually ease after 15 minutes.
Gastrointestinal adverse reactions include anorexia, nausea, vomiting, diarrhea, abdominal cramps. Occasionally it will appear hyperglycemia, cholelithiasis, abnormal glucose tolerance, and liver function abnormalities (γ-glutamyl transferase increased and transaminase slightly increased) and others. Patients with dysfunction of kidney and pancreatic, and cholelithiasis should be used with caution. Pregnant women, lactating women and children are prohibition.
The above information is edited by the chemicalbook of Kui Ming.

Category

toxic substances

Toxicity grading

highly toxic

Acute toxicity

intravenous-rat LD50: 18.1 mg/kg; intravenous-mouse LD50: 72.3 mg/kg

Flammability hazard characteristics

combustible; fire decomposition of toxic nitrogen oxide compounds, sulfur oxide fumes

storage properties

cold warehouse, ventilated and dry; and separately stored with food raw materials

Extinguishing media

water, carbon dioxide, dry power, sandy soil

Chemical Properties

Colourless to off-white lyophilised solid

Uses

Octapeptide analog of Somatostatin. A gastric antisecretory agent. Used in treatment of acromegaly

Uses

natural hormone somatostatin

brand name

Sandostatin (Novartis).

Octreotide Preparation Products And Raw materials

Raw materials

Preparation Products


Octreotide Suppliers

Global( 124)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22080 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20795 55
Rixing Chemical CO.,LTD
13237129059
- info@rixingchemi.com CHINA 235 55
Hangzhou Peptide Biochem Co.,Ltd 18668118770
86-0571-89197072 linda@peptide-china.com China 229 56
Cellmano Biotech Limited +86-551-65326643
+86-551-65326641 info@cellmano.com China 1028 55
Shanghai Boyle Chemical Co., Ltd. 86-15221043597
86-21-57758967 sales@boylechem.com China 2930 55
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833
+86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96815 76
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
86-21-50328109 3bsc@sina.com China 15940 69
GL Biochem (Shanghai) Ltd 86-21-61263452 (tel), 86-13641803416(mobile)
86-21-61263399 ymbetter@glbiochem.com China 9721 64
Shanghai Hanhong Scientific Co.,Ltd. 021-54306202,021-54308259
+86-21-54291107 info@hanhonggroup.com China 43423 64

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