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Identification
NameOctreotide
Accession NumberDB00104  (BTD00088, BIOD00088)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Octreotide is the acetate salt of a cyclic octapeptide. It is a long-acting octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin.

Structure
Thumb
Synonyms
Octreotida
Octreotidum
Octrotide
External Identifiers
  • SMS 201-995
  • SMS-201-995
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ocphylsolution500 mcgintravenous; subcutaneousPendopharm Division Of De Pharmascience Inc2014-05-12Not applicableCanada
Ocphylsolution100 mcgintravenous; subcutaneousPendopharm Division Of De Pharmascience Inc2014-05-12Not applicableCanada
Ocphylsolution50 mcgintravenous; subcutaneousPendopharm Division Of De Pharmascience Inc2014-05-12Not applicableCanada
Octreotide Acetateinjection, solution500 ug/mLintravenous; subcutaneousSandoz Inc2014-02-04Not applicableUs
Octreotide Acetateinjection, solution100 ug/mLintravenous; subcutaneousSandoz Inc2014-02-04Not applicableUs
Octreotide Acetateinjection, solution50 ug/mLintravenous; subcutaneousSandoz Inc2014-02-04Not applicableUs
Octreotide Acetateinjection, solution200 ug/mLintravenous; subcutaneousSandoz Inc1988-10-21Not applicableUs
Octreotide Acetateinjection, solution1000 ug/mLintravenous; subcutaneousSandoz Inc1988-10-21Not applicableUs
Octreotide Acetate Injection - 100mcg/mlsolution100 mcgintravenous; subcutaneousSandoz Canada IncorporatedNot applicableNot applicableCanada
Octreotide Acetate Injection - 200mcg/mlsolution200 mcgintravenous; subcutaneousSandoz Canada IncorporatedNot applicableNot applicableCanada
Octreotide Acetate Injection - 500mcg/mlsolution500 mcgintravenous; subcutaneousSandoz Canada IncorporatedNot applicableNot applicableCanada
Octreotide Acetate Injection - 50mcg/mlsolution50 mcgintravenous; subcutaneousSandoz Canada IncorporatedNot applicableNot applicableCanada
Octreotide Acetate Omega 100mcg/mlsolution100 mcgintravenous; subcutaneousOmega Laboratories Ltd2004-02-26Not applicableCanada
Octreotide Acetate Omega 200mcg/mlsolution200 mcgintravenous; subcutaneousOmega Laboratories Ltd2004-03-11Not applicableCanada
Octreotide Acetate Omega 500mcg/mlsolution500 mcgintravenous; subcutaneousOmega Laboratories Ltd2004-02-26Not applicableCanada
Octreotide Acetate Omega 50mcg/mlsolution50 mcgintravenous; subcutaneousOmega Laboratories Ltd2004-02-26Not applicableCanada
Octreotide Injectionsolution50 mcgintravenous; subcutaneousTeva Canada Limited2014-04-18Not applicableCanada
Octreotide Injectionsolution500 mcgintravenous; subcutaneousTeva Canada Limited2008-03-06Not applicableCanada
Octreotide Injectionsolution200 mcgintravenous; subcutaneousTeva Canada Limited2008-03-06Not applicableCanada
Octreotide Injectionsolution100 mcgintravenous; subcutaneousTeva Canada Limited2008-03-06Not applicableCanada
Sandostatininjection, solution50 ug/mLintravenous; subcutaneousNovartis Pharmaceuticals Corporation1988-10-21Not applicableUs
Sandostatininjection, solution1000 ug/mLintravenous; subcutaneousNovartis Pharmaceuticals Corporation1988-10-21Not applicableUs
Sandostatininjection, solution200 ug/mLintravenous; subcutaneousNovartis Pharmaceuticals Corporation1998-10-21Not applicableUs
Sandostatininjection, solution500 ug/mLintravenous; subcutaneousNovartis Pharmaceuticals Corporation1988-10-21Not applicableUs
Sandostatininjection, solution100 ug/mLintravenous; subcutaneousNovartis Pharmaceuticals Corporation1988-10-21Not applicableUs
Sandostatin 100mcg/mlsolution100 mcgintravenous; subcutaneousNovartis Pharmaceuticals Canada Inc1989-12-31Not applicableCanada
Sandostatin 200mcg/mlsolution200 mcgintravenous; subcutaneousNovartis Pharmaceuticals Canada Inc1996-12-31Not applicableCanada
Sandostatin 500mcg/mlsolution500 mcgintravenous; subcutaneousNovartis Pharmaceuticals Canada Inc1989-12-31Not applicableCanada
Sandostatin 50mcg/mlsolution50 mcgintravenous; subcutaneousNovartis Pharmaceuticals Canada Inc1989-12-31Not applicableCanada
Sandostatin Lar 10mgpowder10 mgintramuscularNovartis Pharmaceuticals Canada Inc1999-01-27Not applicableCanada
Sandostatin Lar 20mgpowder20 mgintramuscularNovartis Pharmaceuticals Canada Inc1999-01-27Not applicableCanada
Sandostatin Lar 30mgpowder30 mgintramuscularNovartis Pharmaceuticals Canada Inc1999-01-27Not applicableCanada
Sandostatin Lar DepotkitNovartis Pharmaceuticals Corporation2015-02-01Not applicableUs
Sandostatin Lar DepotkitNovartis Pharmaceuticals Corporation1988-11-01Not applicableUs
Sandostatin Lar DepotkitNovartis Pharmaceuticals Corporation1988-11-01Not applicableUs
Sandostatin Lar DepotkitNovartis Pharmaceuticals Corporation1988-11-01Not applicableUs
Sandostatin Lar DepotkitNovartis Pharmaceuticals Corporation2015-02-01Not applicableUs
Sandostatin Lar DepotkitNovartis Pharmaceuticals Corporation2015-02-01Not applicableUs
Sandostatin Lar Depot Demonstration KitkitNovartis Pharmaceuticals Corporation1988-11-01Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Octreotideinjection, solution1000 ug/mLintravenous; subcutaneousFresenius Kabi USA, LLC2006-03-14Not applicableUs
Octreotideinjection, solution200 ug/mLintravenous; subcutaneousFresenius Kabi USA, LLC2006-03-14Not applicableUs
Octreotideinjection, solution500 ug/mLintravenous; subcutaneousFresenius Kabi USA, LLC2006-03-14Not applicableUs
Octreotideinjection, solution100 ug/mLintravenous; subcutaneousFresenius Kabi USA, LLC2006-03-14Not applicableUs
Octreotideinjection, solution50 ug/mLintravenous; subcutaneousFresenius Kabi USA, LLC2006-03-14Not applicableUs
Octreotide Acetateinjection, solution500 ug/mLintravenous; subcutaneousSun Pharmaceutical Industries Limited2007-08-14Not applicableUs
Octreotide Acetateinjection500 ug/mLintravenous; subcutaneousWockhardt Limited2011-05-11Not applicableUs
Octreotide Acetateinjection, solution50 ug/mLintravenous; subcutaneousTeva Parenteral Medicines, Inc.2005-11-14Not applicableUs
Octreotide Acetateinjection, solution500 ug/mLintravenous; subcutaneousSagent Pharmaceuticals2013-12-15Not applicableUs
Octreotide Acetateinjection200 ug/mLintravenous; subcutaneousWockhardt USA LLC.2011-05-11Not applicableUs
Octreotide Acetateinjection, solution1000 ug/mLintravenous; subcutaneousSun Pharmaceutical Industries Limited2007-08-14Not applicableUs
Octreotide Acetateinjection, solution200 ug/mLintravenous; subcutaneousSagent Pharmaceuticals2013-12-15Not applicableUs
Octreotide Acetateinjection, solution100 ug/mLintravenous; subcutaneousSagent Pharmaceuticals2013-12-15Not applicableUs
Octreotide Acetateinjection100 ug/mLintravenous; subcutaneousWockhardt USA LLC.2011-05-11Not applicableUs
Octreotide Acetateinjection, solution200 ug/mLintravenous; subcutaneousSun Pharmaceutical Industries Limited2007-08-14Not applicableUs
Octreotide Acetateinjection200 ug/mLintravenous; subcutaneousWockhardt Limited2011-05-11Not applicableUs
Octreotide Acetateinjection, solution100 ug/mLintravenous; subcutaneousSun Pharmaceutical Industries Limited2007-08-14Not applicableUs
Octreotide Acetateinjection100 ug/mLintravenous; subcutaneousWockhardt Limited2011-05-11Not applicableUs
Octreotide Acetateinjection, solution50 ug/mLintravenous; subcutaneousSagent Pharmaceuticals2013-12-15Not applicableUs
Octreotide Acetateinjection1000 ug/mLintravenous; subcutaneousWockhardt USA LLC.2011-05-11Not applicableUs
Octreotide Acetateinjection, solution50 ug/mLintravenous; subcutaneousSun Pharmaceutical Industries Limited2007-08-14Not applicableUs
Octreotide Acetateinjection1000 ug/mLintravenous; subcutaneousWockhardt Limited2011-05-11Not applicableUs
Octreotide Acetateinjection, solution500 ug/mLintravenous; subcutaneousMylan Institutional LLC2013-04-25Not applicableUs
Octreotide Acetateinjection, solution500 ug/mLintravenous; subcutaneousSun Pharmaceutical Industries Limited2012-08-31Not applicableUs
Octreotide Acetateinjection, solution1000 ug/mLintravenous; subcutaneousTeva Parenteral Medicines, Inc.2005-11-23Not applicableUs
Octreotide Acetateinjection, solution100 ug/mLintravenous; subcutaneousMylan Institutional LLC2013-04-25Not applicableUs
Octreotide Acetateinjection, solution100 ug/mLintravenous; subcutaneousSun Pharmaceutical Industries Limited2012-08-31Not applicableUs
Octreotide Acetateinjection, solution200 ug/mLintravenous; subcutaneousTeva Parenteral Medicines, Inc.2005-11-23Not applicableUs
Octreotide Acetateinjection, solution50 ug/mLintravenous; subcutaneousMylan Institutional LLC2013-04-25Not applicableUs
Octreotide Acetateinjection, solution50 ug/mLintravenous; subcutaneousSun Pharmaceutical Industries Limited2012-08-31Not applicableUs
Octreotide Acetateinjection, solution500 ug/mLintravenous; subcutaneousTeva Parenteral Medicines, Inc.2005-11-14Not applicableUs
Octreotide Acetateinjection50 ug/mLintravenous; subcutaneousWockhardt USA LLC.2011-05-11Not applicableUs
Octreotide Acetateinjection, solution1000 ug/mLintravenous; subcutaneousSagent Pharmaceuticals2013-12-15Not applicableUs
Octreotide Acetateinjection50 ug/mLintravenous; subcutaneousWockhardt Limited2011-05-11Not applicableUs
Octreotide Acetateinjection, solution100 ug/mLintravenous; subcutaneousTeva Parenteral Medicines, Inc.2005-11-14Not applicableUs
Octreotide Acetateinjection500 ug/mLintravenous; subcutaneousWockhardt USA LLC.2011-05-11Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Sandostatin LARNovartis Pharmaceuticals
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Octreotide acetate
79517-01-4
Thumb
  • InChI Key: XQEJFZYLWPSJOV-XJQYZYIXSA-N
  • Monoisotopic Mass: 1078.461610082
  • Average Mass: 1079.3
DBSALT000130
Categories
UNIIRWM8CCW8GP
CAS number83150-76-9
WeightAverage: 1019.25
Monoisotopic: 1018.440480713
Chemical FormulaC49H66N10O10S2
InChI KeyDEQANNDTNATYII-OULOTJBUSA-N
InChI
InChI=1S/C49H66N10O10S2/c1-28(61)39(25-60)56-48(68)41-27-71-70-26-40(57-43(63)34(51)21-30-13-5-3-6-14-30)47(67)54-37(22-31-15-7-4-8-16-31)45(65)55-38(23-32-24-52-35-18-10-9-17-33(32)35)46(66)53-36(19-11-12-20-50)44(64)59-42(29(2)62)49(69)58-41/h3-10,13-18,24,28-29,34,36-42,52,60-62H,11-12,19-23,25-27,50-51H2,1-2H3,(H,53,66)(H,54,67)(H,55,65)(H,56,68)(H,57,63)(H,58,69)(H,59,64)/t28-,29-,34-,36+,37+,38-,39-,40+,41+,42+/m1/s1
IUPAC Name
(4R,7S,10S,13R,16S,19R)-19-[(2R)-2-amino-3-phenylpropanamido]-10-(4-aminobutyl)-16-benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-7-[(1R)-1-hydroxyethyl]-13-[(1H-indol-3-yl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide
SMILES
[H][C@]1(NC(=O)[[email protected]](CCCCN)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)[[email protected]](CC2=CC=CC=C2)NC(=O)[[email protected]](CSSC[[email protected]](NC1=O)C(=O)N[[email protected]](CO)[C@@H](C)O)NC(=O)[[email protected]](N)CC1=CC=CC=C1)[C@@H](C)O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentOligopeptides
Alternative Parents
Substituents
  • Alpha-oligopeptide
  • Cyclic alpha peptide
  • Phenylalanine or derivatives
  • Macrolactam
  • N-acyl-alpha amino acid or derivatives
  • Alpha-amino acid amide
  • Alpha-amino acid or derivatives
  • Amphetamine or derivatives
  • 3-alkylindole
  • Indole
  • Indole or derivatives
  • Aralkylamine
  • Benzenoid
  • Substituted pyrrole
  • Monocyclic benzene moiety
  • Fatty amide
  • Fatty acyl
  • Pyrrole
  • Heteroaromatic compound
  • Amino acid or derivatives
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Secondary alcohol
  • Lactam
  • Organic disulfide
  • Organoheterocyclic compound
  • Azacycle
  • Primary amine
  • Amine
  • Hydrocarbon derivative
  • Organic oxygen compound
  • Carbonyl group
  • Organic nitrogen compound
  • Primary alcohol
  • Primary aliphatic amine
  • Alcohol
  • Organic oxide
  • Organonitrogen compound
  • Organooxygen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor treatment of acromegaly and reduction of side effects from cancer chemotherapy
PharmacodynamicsOctreotide exerts pharmacologic actions similar to the natural hormone, somatostatin. It is an even more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Like somatostatin, it also suppresses leuteinizing hormone (LH) response to GnRH, decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide. Octreotide has been used to treat the symptoms associated with metastatic carcinoid tumors (flushing and diarrhea), and Vasoactive Intestinal Peptide (VIP) secreting adenomas (watery diarrhea). Octreotide substantially reduces and in many cases can normalize growth hormone and/or IGF-1 (somatomedin C) levels in patients with acromegaly.
Mechanism of actionOctreotide binds to somatostatin receptors. These receptors are coupled via pertussis toxin sensitive G proteins which lead to inhibition of adenylyl cyclase. Octreotide binding to these receptors also stimulates phosphotyrosine phosphatase and activation of the Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 13.6 L [healthy volunteers]
  • 21.6±8.5 L [patients with acromegaly]
Protein bindingNot Available
MetabolismNot Available
Route of eliminationAbout 32% of the dose is excreted unchanged into the urine.
Half lifeNot Available
Clearance
  • 7 – 10 L/hr [healthy after 100-mcg SC injection]
  • 18 L/hr [patients with acromegaly after 100-mcg SC injection]
  • 8.8 L/hr [mild renal impairment after 100-mcg SC injection]
  • 7.3 L/hr [moderate renal impairment after 100-mcg SC injection]
  • 7.6 L/hr [severe renal impairment after 100-mcg SC injection]
  • 4.5 L/hr [severe renal failure requiring dialysis after 100-mcg SC injection]
  • 5.9 L/hr [Patients with liver cirrhosis after 100-mcg SC injection]
  • 8.2 L/hr [patients with fatty liver disease after 100-mcg SC injection]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9239
Blood Brain Barrier-0.8738
Caco-2 permeable-0.7824
P-glycoprotein substrateSubstrate0.8557
P-glycoprotein inhibitor INon-inhibitor0.9599
P-glycoprotein inhibitor IINon-inhibitor0.969
Renal organic cation transporterNon-inhibitor0.8506
CYP450 2C9 substrateNon-substrate0.8205
CYP450 2D6 substrateNon-substrate0.7632
CYP450 3A4 substrateNon-substrate0.5268
CYP450 1A2 substrateNon-inhibitor0.7975
CYP450 2C9 inhibitorNon-inhibitor0.7743
CYP450 2D6 inhibitorNon-inhibitor0.8449
CYP450 2C19 inhibitorNon-inhibitor0.7355
CYP450 3A4 inhibitorNon-inhibitor0.8236
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.708
Ames testNon AMES toxic0.6448
CarcinogenicityNon-carcinogens0.8761
BiodegradationNot ready biodegradable0.9943
Rat acute toxicity2.6174 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9693
hERG inhibition (predictor II)Inhibitor0.6064
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Sun pharmaceutical industries ltd
  • Teva parenteral medicines inc
  • Novartis pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
Injectionintravenous; subcutaneous100 ug/mL
Injectionintravenous; subcutaneous1000 ug/mL
Injectionintravenous; subcutaneous200 ug/mL
Injectionintravenous; subcutaneous50 ug/mL
Injectionintravenous; subcutaneous500 ug/mL
Solutionintravenous; subcutaneous100 mcg
Solutionintravenous; subcutaneous500 mcg
Solutionintravenous; subcutaneous50 mcg
Injection, solutionintravenous; subcutaneous100 ug/mL
Injection, solutionintravenous; subcutaneous1000 ug/mL
Injection, solutionintravenous; subcutaneous200 ug/mL
Injection, solutionintravenous; subcutaneous50 ug/mL
Injection, solutionintravenous; subcutaneous500 ug/mL
Solutionintravenous; subcutaneous200 mcg
Powderintramuscular10 mg
Powderintramuscular20 mg
Powderintramuscular30 mg
Kit
Prices
Unit descriptionCostUnit
Sandostatin lar 30 mg kit3860.62USD kit
Sandostatin lar 20 mg kit2578.19USD kit
Sandostatin lar 10 mg kit1967.81USD kit
Sandostatin 1 mg/ml vial234.49USD ml
Sandostatin 0.5 mg/ml ampul111.48USD ml
Octreotide 1000 mcg/ml vial67.2USD ml
Sandostatin 0.2 mg/ml vial47.66USD ml
Octreotide acet 500 mcg/ml vial24.48USD ml
Sandostatin 0.1 mg/ml ampul23.11USD ml
Octreotide acet 100 mcg/ml vial15.36USD ml
Octreotide acet 200 mcg/ml vial14.4USD ml
Sandostatin 0.05 mg/ml ampul11.92USD ml
Octreotide acet 50 mcg/ml vial3.6USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1328402 No1994-04-122011-04-12Canada
US5538739 No1993-07-232013-07-23Us
US5753618 Yes1995-11-192015-11-19Us
US5922338 Yes1997-01-132017-01-13Us
US5922682 Yes1997-01-132017-01-13Us
Properties
StateLiquid
Experimental Properties
PropertyValueSource
logP1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0122 mg/mLALOGPS
logP0.42ALOGPS
logP-1.4ChemAxon
logS-4.9ALOGPS
pKa (Strongest Acidic)11.4ChemAxon
pKa (Strongest Basic)10.17ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count12ChemAxon
Hydrogen Donor Count13ChemAxon
Polar Surface Area332.22 Å2ChemAxon
Rotatable Bond Count17ChemAxon
Refractivity269.77 m3·mol-1ChemAxon
Polarizability107.65 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Nishith Chaturvedi, “Novel process for production of the somatostatin analog, octreotide.” U.S. Patent US20040225108, issued November 11, 2004.

US20040225108
General References
  1. Uhl W, Anghelacopoulos SE, Friess H, Buchler MW: The role of octreotide and somatostatin in acute and chronic pancreatitis. Digestion. 1999;60 Suppl 2:23-31. [PubMed:10207228 ]
External Links
ATC CodesH01CB02
AHFS Codes
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (69.7 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololOctreotide may increase the bradycardic activities of Acebutolol.
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Octreotide.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Octreotide.
AlogliptinAlogliptin may increase the hypoglycemic activities of Octreotide.
AmiodaroneOctreotide may increase the bradycardic activities of Amiodarone.
AnagrelideOctreotide may increase the QTc-prolonging activities of Anagrelide.
Arsenic trioxideOctreotide may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherOctreotide may increase the QTc-prolonging activities of Artemether.
AsenapineOctreotide may increase the QTc-prolonging activities of Asenapine.
AtenololOctreotide may increase the bradycardic activities of Atenolol.
AzithromycinOctreotide may increase the QTc-prolonging activities of Azithromycin.
BedaquilineOctreotide may increase the QTc-prolonging activities of Bedaquiline.
BendroflumethiazideOctreotide may increase the bradycardic activities of Bendroflumethiazide.
BeractantOctreotide may increase the bradycardic activities of Beractant.
BetaxololOctreotide may increase the bradycardic activities of Betaxolol.
BisoprololOctreotide may increase the bradycardic activities of Bisoprolol.
BretyliumBretylium may increase the bradycardic activities of Octreotide.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Octreotide.
CalfactantOctreotide may increase the bradycardic activities of Calfactant.
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Octreotide.
CarteololOctreotide may increase the bradycardic activities of Carteolol.
CarvedilolOctreotide may increase the bradycardic activities of Carvedilol.
CeritinibOctreotide may increase the bradycardic activities of Ceritinib.
ChloroquineOctreotide may increase the QTc-prolonging activities of Chloroquine.
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Octreotide.
ChlorpromazineOctreotide may increase the QTc-prolonging activities of Chlorpromazine.
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Octreotide.
CiprofloxacinOctreotide may increase the QTc-prolonging activities of Ciprofloxacin.
CisaprideOctreotide may increase the QTc-prolonging activities of Cisapride.
CitalopramOctreotide may increase the QTc-prolonging activities of Citalopram.
ClarithromycinOctreotide may increase the QTc-prolonging activities of Clarithromycin.
ClonidineOctreotide may increase the bradycardic activities of Clonidine.
ClozapineOctreotide may increase the QTc-prolonging activities of Clozapine.
CodeineThe metabolism of Codeine can be decreased when combined with Octreotide.
CrizotinibOctreotide may increase the bradycardic activities of Crizotinib.
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Octreotide.
DexmedetomidineOctreotide may increase the bradycardic activities of Dexmedetomidine.
DigoxinOctreotide may increase the bradycardic activities of Digoxin.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Octreotide.
DiltiazemOctreotide may increase the bradycardic activities of Diltiazem.
DisopyramideOctreotide may increase the QTc-prolonging activities of Disopyramide.
DofetilideOctreotide may increase the QTc-prolonging activities of Dofetilide.
DolasetronOctreotide may increase the QTc-prolonging activities of Dolasetron.
DomperidoneOctreotide may increase the QTc-prolonging activities of Domperidone.
DonepezilOctreotide may increase the bradycardic activities of Donepezil.
DronedaroneOctreotide may increase the bradycardic activities of Dronedarone.
DroperidolOctreotide may increase the QTc-prolonging activities of Droperidol.
EliglustatOctreotide may increase the QTc-prolonging activities of Eliglustat.
ErythromycinOctreotide may increase the QTc-prolonging activities of Erythromycin.
EscitalopramOctreotide may increase the QTc-prolonging activities of Escitalopram.
EsmololEsmolol may increase the bradycardic activities of Octreotide.
FingolimodOctreotide may increase the bradycardic activities of Fingolimod.
FlecainideOctreotide may increase the QTc-prolonging activities of Flecainide.
FluoxetineOctreotide may increase the QTc-prolonging activities of Fluoxetine.
FlupentixolOctreotide may increase the QTc-prolonging activities of Flupentixol.
Gadobenic acidOctreotide may increase the QTc-prolonging activities of Gadobenate Dimeglumine.
GalantamineOctreotide may increase the bradycardic activities of Galantamine.
GemifloxacinOctreotide may increase the QTc-prolonging activities of Gemifloxacin.
GliclazideGliclazide may increase the hypoglycemic activities of Octreotide.
GlimepirideGlimepiride may increase the hypoglycemic activities of Octreotide.
GliquidoneGliquidone may increase the hypoglycemic activities of Octreotide.
GlyburideGlyburide may increase the hypoglycemic activities of Octreotide.
GoserelinOctreotide may increase the QTc-prolonging activities of Goserelin.
GranisetronOctreotide may increase the QTc-prolonging activities of Granisetron.
GuanfacineOctreotide may increase the bradycardic activities of Guanfacine.
HaloperidolOctreotide may increase the QTc-prolonging activities of Haloperidol.
IbutilideOctreotide may increase the QTc-prolonging activities of Ibutilide.
IloperidoneOctreotide may increase the QTc-prolonging activities of Iloperidone.
Insulin AspartInsulin Aspart may increase the hypoglycemic activities of Octreotide.
Insulin DetemirInsulin Detemir may increase the hypoglycemic activities of Octreotide.
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Octreotide.
Insulin GlulisineInsulin Glulisine may increase the hypoglycemic activities of Octreotide.
Insulin HumanInsulin Regular may increase the hypoglycemic activities of Octreotide.
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Octreotide.
IvabradineOctreotide may increase the bradycardic activities of Ivabradine.
LabetalolOctreotide may increase the bradycardic activities of Labetalol.
LacosamideOctreotide may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LanreotideOctreotide may increase the bradycardic activities of Lanreotide.
LenvatinibOctreotide may increase the QTc-prolonging activities of Lenvatinib.
LeuprolideOctreotide may increase the QTc-prolonging activities of Leuprolide.
LevobunololOctreotide may increase the bradycardic activities of Levobunolol.
LevofloxacinOctreotide may increase the QTc-prolonging activities of Levofloxacin.
LinagliptinLinagliptin may increase the hypoglycemic activities of Octreotide.
LopinavirOctreotide may increase the QTc-prolonging activities of Lopinavir.
LucinactantOctreotide may increase the bradycardic activities of Lucinactant.
LumefantrineOctreotide may increase the QTc-prolonging activities of Lumefantrine.
MetforminMetformin may increase the hypoglycemic activities of Octreotide.
MethadoneOctreotide may increase the QTc-prolonging activities of Methadone.
MethyldopaOctreotide may increase the bradycardic activities of Methyldopa.
MetipranololOctreotide may increase the bradycardic activities of Metipranolol.
MetoprololOctreotide may increase the bradycardic activities of Metoprolol.
MifepristoneMifepristone may increase the QTc-prolonging activities of Octreotide.
MoxifloxacinOctreotide may increase the QTc-prolonging activities of Moxifloxacin.
NadololOctreotide may increase the bradycardic activities of Nadolol.
NebivololOctreotide may increase the bradycardic activities of Nebivolol.
NilotinibOctreotide may increase the QTc-prolonging activities of Nilotinib.
OfloxacinOctreotide may increase the QTc-prolonging activities of Ofloxacin.
OndansetronOctreotide may increase the QTc-prolonging activities of Ondansetron.
OsimertinibOctreotide may increase the QTc-prolonging activities of Osimertinib.
OxandroloneOxandrolone may increase the hypoglycemic activities of Octreotide.
PaliperidoneOctreotide may increase the QTc-prolonging activities of Paliperidone.
PanobinostatOctreotide may increase the QTc-prolonging activities of Panobinostat.
ParoxetineParoxetine may increase the hypoglycemic activities of Octreotide.
PasireotideOctreotide may increase the bradycardic activities of Pasireotide.
PazopanibOctreotide may increase the QTc-prolonging activities of Pazopanib.
PegvisomantThe risk or severity of adverse effects can be increased when Octreotide is combined with Pegvisomant.
PenbutololOctreotide may increase the bradycardic activities of Penbutolol.
PentamidineOctreotide may increase the QTc-prolonging activities of Pentamidine.
PerflutrenOctreotide may increase the QTc-prolonging activities of Perflutren.
PhenelzinePhenelzine may increase the hypoglycemic activities of Octreotide.
PimozideOctreotide may increase the QTc-prolonging activities of Pimozide.
PindololOctreotide may increase the bradycardic activities of Pindolol.
Poractant alfaOctreotide may increase the bradycardic activities of Poractant alfa.
PrimaquineOctreotide may increase the QTc-prolonging activities of Primaquine.
ProcainamideOctreotide may increase the QTc-prolonging activities of Procainamide.
PromazineOctreotide may increase the QTc-prolonging activities of Promazine.
PropafenoneOctreotide may increase the bradycardic activities of Propafenone.
PropranololOctreotide may increase the bradycardic activities of Propranolol.
QuetiapineOctreotide may increase the QTc-prolonging activities of Quetiapine.
QuinidineOctreotide may increase the QTc-prolonging activities of Quinidine.
QuinineOctreotide may increase the QTc-prolonging activities of Quinine.
RepaglinideRepaglinide may increase the hypoglycemic activities of Octreotide.
RitonavirOctreotide may increase the QTc-prolonging activities of Ritonavir.
RivastigmineOctreotide may increase the bradycardic activities of Rivastigmine.
RuxolitinibRuxolitinib may increase the bradycardic activities of Octreotide.
SaquinavirOctreotide may increase the QTc-prolonging activities of Saquinavir.
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Octreotide.
SotalolOctreotide may increase the bradycardic activities of Sotalol.
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Octreotide.
SufentanilOctreotide may increase the bradycardic activities of Sufentanil.
SulfisoxazoleOctreotide may increase the QTc-prolonging activities of Sulfisoxazole.
TelavancinOctreotide may increase the QTc-prolonging activities of Telavancin.
TelithromycinOctreotide may increase the QTc-prolonging activities of Telithromycin.
TestosteroneTestosterone may increase the hypoglycemic activities of Octreotide.
TetrabenazineOctreotide may increase the QTc-prolonging activities of Tetrabenazine.
ThioridazineOctreotide may increase the QTc-prolonging activities of Thioridazine.
TimololOctreotide may increase the bradycardic activities of Timolol.
TizanidineOctreotide may increase the bradycardic activities of Tizanidine.
TofacitinibTofacitinib may increase the bradycardic activities of Octreotide.
TolbutamideTolbutamide may increase the hypoglycemic activities of Octreotide.
ToremifeneOctreotide may increase the QTc-prolonging activities of Toremifene.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Octreotide.
VandetanibOctreotide may increase the QTc-prolonging activities of Vandetanib.
VemurafenibOctreotide may increase the QTc-prolonging activities of Vemurafenib.
VerapamilOctreotide may increase the bradycardic activities of Verapamil.
VildagliptinVildagliptin may increase the hypoglycemic activities of Octreotide.
ZiprasidoneOctreotide may increase the QTc-prolonging activities of Ziprasidone.
ZuclopenthixolOctreotide may increase the QTc-prolonging activities of Zuclopenthixol.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Somatostatin receptor activity
Specific Function:
Receptor for somatostatin with higher affinity for somatostatin-14 than -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins.
Gene Name:
SSTR1
Uniprot ID:
P30872
Molecular Weight:
42685.77 Da
References
  1. Wang ZZ, Qu W, Wang F, Li Y, Wang SK, Wang JQ: [Expression of somatostatin receptor reporter gene and its correlation with targeted imaging in vivo for detection of pancreas carcinoma]. Zhonghua Zhong Liu Za Zhi. 2005 Nov;27(11):663-6. [PubMed:16438887 ]
  2. Matrone C, Pivonello R, Colao A, Cappabianca P, Cavallo LM, Del Basso De Caro ML, Taylor JE, Culler MD, Lombardi G, Di Renzo GF, Annunziato L: Expression and function of somatostatin receptor subtype 1 in human growth hormone secreting pituitary tumors deriving from patients partially responsive or resistant to long-term treatment with somatostatin analogs. Neuroendocrinology. 2004 Mar;79(3):142-8. Epub 2004 Apr 16. [PubMed:15103227 ]
  3. Jaquet P, Gunz G, Saveanu A, Barlier A, Dufour H, Taylor J, Dong J, Kim S, Moreau JP, Culler MD: BIM-23A760, a chimeric molecule directed towards somatostatin and dopamine receptors, vs universal somatostatin receptors ligands in GH-secreting pituitary adenomas partial responders to octreotide. J Endocrinol Invest. 2005;28(11 Suppl International):21-7. [PubMed:16625841 ]
  4. Schmid HA, Silva AP: Short- and long-term effects of octreotide and SOM230 on GH, IGF-I, ACTH, corticosterone and ghrelin in rats. J Endocrinol Invest. 2005;28(11 Suppl International):28-35. [PubMed:16625842 ]
  5. Ruan W, Fahlbusch F, Clemmons DR, Monaco ME, Walden PD, Silva AP, Schmid HA, Kleinberg DL: SOM230 inhibits insulin-like growth factor-I action in mammary gland development by pituitary independent mechanism: mediated through somatostatin subtype receptor 3? Mol Endocrinol. 2006 Feb;20(2):426-36. Epub 2005 Oct 13. [PubMed:16223973 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Somatostatin receptor activity
Specific Function:
Receptor for somatostatin 28 and to a lesser extent for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Increases cell growth inhibition activity of SSTR2 following heterodimerization.
Gene Name:
SSTR5
Uniprot ID:
P35346
Molecular Weight:
39201.925 Da
References
  1. Bronstein MD: Acromegaly: molecular expression of somatostatin receptor subtypes and treatment outcome. Front Horm Res. 2006;35:129-34. [PubMed:16809928 ]
  2. Xie Y, Tang CW, Wang CH: [Effect of HBV X gene transfection on octreotide-inhibited growth of hepatocellular carcinoma cell line HepG2]. Ai Zheng. 2005 Aug;24(8):965-9. [PubMed:16086874 ]
  3. Wang ZZ, Qu W, Wang F, Li Y, Wang SK, Wang JQ: [Expression of somatostatin receptor reporter gene and its correlation with targeted imaging in vivo for detection of pancreas carcinoma]. Zhonghua Zhong Liu Za Zhi. 2005 Nov;27(11):663-6. [PubMed:16438887 ]
  4. Jaquet P, Gunz G, Saveanu A, Barlier A, Dufour H, Taylor J, Dong J, Kim S, Moreau JP, Culler MD: BIM-23A760, a chimeric molecule directed towards somatostatin and dopamine receptors, vs universal somatostatin receptors ligands in GH-secreting pituitary adenomas partial responders to octreotide. J Endocrinol Invest. 2005;28(11 Suppl International):21-7. [PubMed:16625841 ]
  5. Schmid HA, Silva AP: Short- and long-term effects of octreotide and SOM230 on GH, IGF-I, ACTH, corticosterone and ghrelin in rats. J Endocrinol Invest. 2005;28(11 Suppl International):28-35. [PubMed:16625842 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
binder
General Function:
Somatostatin receptor activity
Specific Function:
Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and PLC via pertussis toxin insensitive as well as sensitive G proteins. Inhibits calcium entry by suppressing voltage-dependent calcium channels. Acts as the functionally dominant somatostatin receptor i...
Gene Name:
SSTR2
Uniprot ID:
P30874
Molecular Weight:
41332.37 Da
References
  1. Yim CB, Boerman OC, de Visser M, de Jong M, Dechesne AC, Rijkers DT, Liskamp RM: Versatile conjugation of octreotide to dendrimers by cycloaddition ("click") chemistry to yield high-affinity multivalent cyclic Peptide dendrimers. Bioconjug Chem. 2009 Jul;20(7):1323-31. doi: 10.1021/bc900052n. [PubMed:19537708 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Peroxidase activity
Specific Function:
Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production of hypohalous acids, primarily hypochlorous acid in physiologic situations, and other toxic intermediates that greatly enhance PMN microbicidal activity.
Gene Name:
MPO
Uniprot ID:
P05164
Molecular Weight:
83867.71 Da
References
  1. Alatas E, Alatas O, Colak O: Octreotide inhibits myeloperoxidase activity in rat uterus. Acta Obstet Gynecol Scand. 2000 Jul;79(7):524-7. [PubMed:10929949 ]
  2. Alatas E, Gunal O, Alatas O, Colak O: Octreotide prevents postoperative adhesion formation by suppressing peritoneal myeloperoxidase activity. Hepatogastroenterology. 2000 Jul-Aug;47(34):1034-6. [PubMed:11020872 ]
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Drug created on June 13, 2005 07:24 / Updated on July 01, 2016 03:05