Product Name Octreotide Acetate
CAS No 83150-76-9
Sequence
Purity (HPLC) 98.0%min.
Molecular Formula C49H66N10O10S2
Molecular Weight 1019.28
Appearance White powder
Single Impurity (HPLC) 1.0%max
Amino Acid Composition ±10% of theoretical
Peptide Content (N%) ≥80.0%
Water Content(Karl Fischer) ≤7.0%
Acetate Content(HPIC) ≤12.0%
Specific Rotation (20/D) -45.0～-50.0°(c=0.5 95%HAc)
Use
Octreotide is used to treat severe watery diarrhea and sudden reddening of the face and neck caused by certain types of tumors (such as carcinoid tumors, vasoactive intestinal peptide tumors) that are found usually in the intestines and pancreas. The symptoms occur when these tumors make too much of certain natural substances (hormones). This medication works by blocking the production of these hormones. By decreasing watery diarrhea, octreotide helps to reduce the loss of body fluids and minerals.Octreotide is also used to treat a certain condition (acromegaly) that occurs when the body makes too much of a certain natural substance called growth hormone. Treating acromegaly helps reduce the risk of serious problems such as diabetes and heart disease. Octreotide works by decreasing the amount of growth hormone to normal levels.This drug is not a cure for these conditions. This medication is usually used with other treatment (such as surgery, radiation, other drugs).
How This Drug Is Given:
- Octreotide has two formulations. For purposes of clarity, trade names will be used for discussion. Sandostatin® is a short acting version and Sandostatin LAR is a long acting version.
- Sandostatin is given by subcutaneous injection (S.C. - the layer of tissue between the skin and the muscle). It may be necessary to take the shot several times a day. The injection sites should be rotated regularly. This medication may also be given intravenously.
- Sandostatin LAR® is given by intramuscular injection (IM - into the muscle) under a doctor's supervision. This medication is generally given once every 4 weeks. The preferred site for injection is the hip, because it is painful given into the arm. Sandostatin LAR® should NOT be given by S.C. or IV routes.
- If short acting Sandostatin® is to be replaced by long-acting Sandostatin LAR®, short acting Sandostatin® should be continued for at least two weeks to maintain therapeutic doses in patients with carcinoid tumors or VIPomas.
- Short acting Sandostatin® may also be used to control breakthrough syptoms in carcinoid.
- The amount of octreotide that you will receive depends on many factors, including your height and weight, your general health or other health problems, and the type of cancer or condition being treated. Your doctor will determine your dose and schedule.
Mechanism of action
Octreotide binds to somatostatin receptors coupled to phospholipase C through G proteins and leads to smooth muscle contraction in the blood vessels. Downstream effects that stimulate phospholipase C, the production of 1, 4,5-inositol triphosphate, and action on the L-type calcium channels lead to the inhibition of growth hormone, treating the various growth-hormone and metabolic effects of acromegaly.
Octreotide's suppression of luteinizing hormone (LH), reduction in splanchnic blood flow, and inhibition of serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide provide relief for the gastrointestinal and flushing symptoms of carcinoid and/or VIPoma tumors.
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