Octreotide
Drug Info:
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Octreotide
Brand names: Sandostatin LAR®, Sandostatin®
Chemical formula:
- Drug Forms:
- Octreotide Acetate Solution for injection (below)
- Octreotide Acetate Suspension for injection
- Espa�ol:
- Acetato de octreotida, Solución para inyección
- Acetato de octreotida, Suspensión para inyección
Octreotide Acetate Solution for injection
What is this medicine?
OCTREOTIDE (ok TREE oh tide) is used to reduce blood levels of growth hormone in patients with a condition called acromegaly. This medicine also reduces flushing and watery diarrhea caused by certain types of cancer.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•gallbladder disease
•kidney disease
•liver disease
•an unusual or allergic reaction to octreotide, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
This medicine is for injection under the skin or into a vein (only in emergency situations). It is usually given by a health care professional in a hospital or clinic setting.
If you get this medicine at home, you will be taught how to prepare and give this medicine. Allow the injection solution to come to room temperature before use. Do not warm it artificially. Use exactly as directed. Take your medicine at regular intervals. Do not take your medicine more often than directed.
It is important that you put your used needles and syringes in a special sharps container. Do not put them in a trash can. If you do not have a sharps container, call your pharmacist or healthcare provider to get one.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What may interact with this medicine?
Do not take this medicine with any of the following medications:
•cisapride
•droperidol
•general anesthetics
•grepafloxacin
•perphenazine
•thioridazine
This medicine may also interact with the following medications:
•bromocriptine
•cyclosporine
•diuretics
•medicines for blood pressure, heart disease, irregular heart beat
•medicines for diabetes, including insulin
•quinidine
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress.
To help reduce irritation at the injection site, use a different site for each injection and make sure the solution is at room temperature before use.
This medicine may cause increases or decreases in blood sugar. Signs of high blood sugar include frequent urination, unusual thirst, flushed or dry skin, difficulty breathing, drowsiness, stomach ache, nausea, vomiting or dry mouth. Signs of low blood sugar include chills, cool, pale skin or cold sweats, drowsiness, extreme hunger, fast heartbeat, headache, nausea, nervousness or anxiety, shakiness, trembling, unsteadiness, tiredness, or weakness. Contact your doctor or health care professional right away if you experience any of these symptoms.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•changes in blood sugar
•changes in heart rate
•severe stomach pain
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•diarrhea or constipation
•gas or stomach pain
•nausea, vomiting
•pain, redness, swelling and irritation at site where injected
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children.
Store in a refrigerator between 2 and 8 degrees C (36 and 46 degrees F). Protect from light. Allow to come to room temperature naturally. Do not use artificial heat. If protected from light, the injection may be stored at room temperature between 20 and 30 degrees C (70 and 86 degrees F) for 14 days. After the initial use, throw away any unused portion of a multiple dose vial after 14 days. Throw away unused portions of the ampules after use.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Oxford A-Z of Medicinal Drugs:
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octreotide
A long-acting analogue of somatostatin, a hormone that is produced in the brain, gastrointestinal tract, and pancreas and inhibits the release of growth hormone. It is used for the treatment of acromegaly (a conditon due to excessive secretion of growth hormone by a tumour in the pituitary gland), either in the short term for patients awaiting pituitary surgery and for the long-term treatment of those individuals with acromegaly who do not respond to surgery, dopamine antagonists, or radiotherapy. It may also be used until radiotherapy is effective. Octreotide is also used to inhibit the secretions (and thus relieve the symptoms) of hormone-secreting tumours of the gastrointestinal tract. It is available as a solution for injection on prescription only.
Side effects:
include pain, stinging, and swelling at the injection site and gastrointestinal upsets, such as loss of appetite, nausea, vomiting, and abdominal pain; gallstones may develop with long-term treatment.
Precautions:
octreotide should be used with caution in women who are pregnant or breastfeeding. Diabetic patients may need to reduce their dosage of insulin or oral antidiabetic drugs. Gall bladder function should be monitored throughout treatment. The drug should be stopped gradually at the end of treatment.
Interactions with other drugs:
Antidiabetic drugs: doses of these may need to be reduced (see Precautions).
Ciclosporin: octreotide reduces the plasma concentration of ciclosporin.
Cimetidine octreotide may delay the absorption of cimetidine.
Proprietary preparations:
Sandostatin; Sandostatin Lar (depot injection).
| octafonium chloride, obesity, Ovysmen | |
| oedema, oestrogen antagonists, oestrogens |
Oxford Dictionary of Biochemistry:
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octreotide
a synthetic octapeptide analogue of somatostatin, with which it shares four residues essential for activity. It has a much longer half-life in vivo (1 — 2 h) than somatostatin (1 — 2 min) and has been used in the therapy of breast, ovarian, prostatic, gut, endocrine, and pituitary tumours.
| octose, octopinic acid, octopine | |
| octulose, octyl, octyl glucoside |
Saunders Veterinary Dictionary:
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octreotide
A somatostatin analog used in the treatment of endocrine disorders of the pituitary and pancreas.
Wikipedia on Answers.com:
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Octreotide
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| Systematic (IUPAC) name | |
| (4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19- [[(2R)-2-amino-3-phenyl-propanoyl]amino]-16- benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-7- (1-hydroxyethyl)-13-(1H-indol-3-ylmethyl)-6,9,12, 15,18-pentaoxo-1,2-dithia-5,8,11,14,17- pentazacycloicosane-4-carboxamide |
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| Clinical data | |
| Trade names | Sandostatin |
| AHFS/Drugs.com | monograph |
| Pregnancy cat. | B (US) |
| Legal status | ℞ Prescription only |
| Routes | Subcutaneous, intramuscular, intravenous |
| Pharmacokinetic data | |
| Bioavailability | 100%; I.M.: 60% to 63% of subcutaneous dose |
| Protein binding | 65% |
| Metabolism | Hepatic |
| Half-life | 1.7–1.9 hours |
| Identifiers | |
| CAS number | 83150-76-9  79517-01-4 (acetate) 135467-16-2 (pamoate) |
| ATC code | H01CB02 |
| PubChem | CID 54373 |
| DrugBank | DB00104 |
| ChemSpider | 10482007 |
| UNII | RWM8CCW8GP |
| KEGG | D00442  |
| ChEMBL | CHEMBL1680 |
| Chemical data | |
| Formula | C49H66N10O10S2 |
| Mol. mass | 1019.24 g/mol |
| SMILES | eMolecules & PubChem |
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Octreotide (brand name Sandostatin, Novartis Pharmaceuticals) is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone. It was first synthesized in 1979 by the chemist Wilfried Bauer.
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Contents
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Uses
Approved uses
The Food and Drug Administration (FDA) has approved the usage of a salt form of this peptide, octreotide acetate, as an injectable depot formulation for the treatment of acromegaly, gigantism, thyrotropinoma, diarrhea and flushing episodes associated with carcinoid syndrome, and diarrhea in patients with vasoactive intestinal peptide-secreting tumors (VIPomas).
Radiolabelling
Further information: Octreotide scan
Octreotide is used in nuclear medicine imaging by labelling with indium-111 (Octreoscan) to noninvasively image neuroendocrine and other tumours expressing somatostatin receptors.[1] More recently, it has been radiolabelled with gallium-68, enabling imaging with positron emission tomography (PET), which provides higher resolution and sensitivity.
Octreotide can also be labelled with a variety of radionuclides, such as yttrium-90 or lutetium-177, to enable peptide receptor radionuclide therapy (PRRT) for the treatment of unresectable neuroendocrine tumours.
Off-label and experimental uses
Octreotide has also been used off-label for the treatment of severe, refractory diarrhea from other causes. It is used in toxicology for the treatment of prolonged recurrent hypoglycemia after sulfonylurea and possibly meglitinides overdose. It has also been used with varying degrees of success in infants with nesidioblastosis to help decrease insulin hypersecretion.
In patients with suspected oesophageal varices, octreotide can be given to help decrease bleeding.[2] It has been investigated for patients with pain from chronic pancreatitis,[3] and it may be useful in the treatment of thymic neoplasms.[citation needed]
The drug has been used off-label, injected subcutaneously, in the management of hypertrophic pulmonary osteoarthropathy (HPOA) secondary to non-small cell lung carcinoma. Although its mechanism is not known, it appears to reduce the pain associated with HPOA.[citation needed]
It has been used in the treatment of malignant bowel obstruction.[4]
Octreotide may be used in conjunction with midodrine to partially reverse peripheral vasodilation in the hepatorenal syndrome. By increasing systemic vascular resistance, these drugs reduce shunting and improve renal perfusion, prolonging survival until definitive treatment with liver transplant.[5]
While successful treatment has been demonstrated in case reports,[6][7] larger studies have failed to demonstrate efficacy in treating chylothorax.[8]
A small study has shown that octreotide may be effective in the treatment of idiopathic intracranial hypertension.[9][10]
Contraindications
Octreotide has not been adequately studied for the treatment of children, pregnant and lactating women. The drug is given to these groups of patients only if a risk-benefit analysis is positive.[11][12]
Adverse effects
The most frequent adverse effects (more than 10% of patients) are headache, hypothyroidism, cardiac conduction changes, gastrointestinal reactions (including cramps, nausea/vomiting and diarrhoea or constipation), gallstones, reduction of insulin release, hyperglycemia[13] or hypoglycemia, and (usually transient) injection site reactions. Slow heart rate, skin reactions such as pruritus, hyperbilirubinemia, hypothyroidism, dizziness and dyspnoea are also fairly common (more than 1%). Rare side effects include acute anaphylactic reactions, pancreatitis and hepatitis.[11][12]
Some studies reported alopecia in patients who were treated by octreotide.[14] Rats which were treated by octreotide experienced erectile dysfunction in a 1998 study.[15] A prolonged QT interval has been observed in patients, but it is uncertain whether this is a reaction to the drug or part of the patients' illnesses.[11]
| Identifiers | |
|---|---|
| Symbol | |
| OPM superfamily | 167 |
| OPM protein | 1soc |
Pharmacokinetics
Octreotide is absorbed quickly and completely after subcutaneous application. Maximal plasma concentration is reached after 30 minutes. The elimination half-life is 100 minutes (1.7 hours) on average when applied subcutaneously; after intravenous injection, the substance is eliminated in two phases with half-lives of 10 and 90 minutes, respectively.[11][12]
Pharmacological effects
Since octreotide resembles somatostatin in physiological activities, it can:
- inhibit secretion of many hormones, such as gastrin, cholecystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, TSH, and vasoactive intestinal peptide,
- reduce secretion of fluids by the intestine and pancreas,
- reduce gastrointestinal motility and inhibit contraction of the gallbladder,
- inhibit the action of certain hormones from the anterior pituitary,
- cause vasoconstriction in the blood vessels, and
- reduce portal vessel pressures in bleeding varices.
It has also been shown to produce analgesic effects, most probably acting as a partial agonist at the mu opioid receptor.[16][17]
Interactions
Octreotide can reduce the intestinal resorption of ciclosporin, possibly making it necessary to increase the dose.[18] Patients with diabetes mellitus might need less insulin or oral antidiabetics when treated with octreotide. The bioavailability of bromocriptine is increased;[12] besides being an antiparkinsonian, bromocriptine is also used for the treatment of acromegaly.
See also
- Octreotate, a closely related peptide
References
- ^ Medscape: Octreoscan review
- ^ Abid S, Jafri W, Hamid S, et al. (March 2009). "Terlipressin vs. octreotide in bleeding oesophageal varices as an adjuvant therapy with endoscopic band ligation: a randomized double-blind placebo-controlled trial". Am. J. Gastroenterol. 104 (3): 617–23. doi:10.1038/ajg.2008.147. PMID 19223890.
- ^ Uhl W, Anghelacopoulos SE, Friess H, Büchler MW (1999). "The role of octreotide and somatostatin in acute and chronic pancreatitis". Digestion 60 Suppl 2: 23–31. doi:10.1159/000051477. PMID 10207228.
- ^ Shima Y, Ohtsu A, Shirao K, Sasaki Y (May 2008). "Clinical efficacy and safety of octreotide (SMS201-995) in terminally ill Japanese cancer patients with malignant bowel obstruction". Japanese Journal of Clinical Oncology 38 (5): 354–9. doi:10.1093/jjco/hyn035. PMID 18490369. http://jjco.oxfordjournals.org/cgi/pmidlookup?view=long&pmid=18490369.
- ^ Skagen C, Einstein M, Lucey MR, Said A (Feb 2009). "Combination Treatment With Octreotide, Midodrine, and Albumin Improves Survival in Patients With Type 1 and Type 2 Hepatorenal Syndrome.". J Clin Gastroenterol. 43 (7): 680–5. doi:10.1097/MCG.0b013e318188947c. PMID 19238094.
- ^ Dalokay Kilic, MD, Ekber Sahin, MD, Oner Gulcan, MD, Bulent Bolat, MD, Riza Turkoz, MD, Ahmet Hatipoglu, MD (2005). "Octreotide for Treating Chylothorax after Cardiac Surgery". Texas Heart Institute Journal 32 (3): 437–39. PMC 1336729. PMID 16392238. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1336729.
- ^ Marcia L. Buck, Pharm.D., FCCP (2004). "Octreotide for the Management of Chylothorax in Infants and Children". Pediatric Pharmacotherapy 10 (10). http://www.medscape.com/viewarticle/494653.
- ^ Chan, Emily, Russell, Jennifer MD, Williams, William MD, Van Arsdell, Glen MD, Coles, John MD, McCrindle, Brian MD (2005). "Postoperative Chylothorax After Cardiothoracic Surgery in Children". Annals of Thoracic Surgery 80 (11): 1864–71. PMID 16242470.
- ^ Greek Researchers Investigate Octreotide Hypertension Research Foundation, accessed 2011-01-02
- ^ G. N. Panagopoulos, S. N. Deftereos, G. A. Tagaris, M. Gryllia, T. Kounadi, O. Karamani, D. Panagiotidis, E. Koutiola-Pappa, C. E. Karageorgiou, G. Piadites (2007-07-10). "Octreotide: A therapeutic option for idiopathic intracranial hypertension". Neurology, Neurophysiology and Neuroscience. http://www.neurojournal.com/article/view/1120. Retrieved 2011-01-02.
- ^ a b c d Haberfeld, H, ed. (2009) (in German). Austria-Codex (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 3-85200-196-X.
- ^ a b c d Dinnendahl, V, Fricke, U, ed. (2010) (in German). Arzneistoff-Profile. 8 (23 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.
- ^ Hovind, P; Simonsen, L; Bülow, J (2010). "Decreased leg glucose uptake during exercise contributes to the hyperglycaemic effect of octreotide.". Clinical physiology and functional imaging 30 (2): 141–5. doi:10.1111/j.1475-097X.2009.00917.x. PMID 20132129.
- ^ Van Der Lely, AJ; De Herder, WW; Lamberts, SW (1997). "A risk-benefit assessment of octreotide in the treatment of acromegaly". Drug safety : an international journal of medical toxicology and drug experience 17 (5): 317–24. PMID 9391775.
- ^ Kapicioglu, S; Mollamehmetoglu, M; Kutlu, N; Can, G; Ozgur, GK (1998). "Inhibition of penile erection in rats by a long-acting somatostatin analogue, octreotide (SMS 201-995)". British journal of urology 81 (1): 142–5. PMID 9467491.
- ^ Maurer R, Gaehwiler BH, Buescher HH, Hill RC, Roemer D. Opiate antagonistic properties of an octapeptide somatostatin analog. Proceedings of the National Academy of Sciences USA. 1982 Aug;79(15):4815-7. PMID 6126877
- ^ Allen MP, Blake JF, Bryce DK, Haggan ME, Liras S, McLean S, Segelstein BE. Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands. Bioorganic and Medicinal Chemistry Letters. 2000 Mar 20;10(6):523-6. PMID 10741545
- ^ Klopp, T, ed. (2010) (in German). Arzneimittel-Interaktionen (2010/2011 ed.). Arbeitsgemeinschaft für Pharmazeutische Information. ISBN 978-3-85200-207-1.
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Oxford A-Z of Medicinal Drugs
Market University Press. © 2000, 2003, 2010 An A-Z of Medicinal Drugs. All rights reserved.
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Oxford Dictionary of Biochemistry
Oxford University Press. Oxford Dictionary of Biochemistry and Molecular Biology © 1997, 2000, 2006 All rights reserved.
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Saunders Veterinary Dictionary
Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.
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