Chemical: Drug
octreotide

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Overview

Generic Names
  • Octreotida [Spanish]
  • Octreotide acetate
  • Octreotidum [Latin]
  • Octrotide
Trade Names
  • Atrigel
  • Longastatin
  • Sandostatin
  • Sandostatin LAR
  • Sandostatin LAR (Novartis)
Brand Mixture Names

PharmGKB Accession Id

PA450678

Type(s):

Drug

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.

Source: Drug Bank

Indication

For treatment of acromegaly and reduction of side effects from cancer chemotherapy

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Octreotide 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.

Source: Drug Bank

Pharmacology

Octreotide 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.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Route of Elimination

About 32% of the dose is excreted unchanged into the urine.

Source: Drug Bank

Volume of Distribution

Source: Drug Bank

Chemical Properties

Chemical Formula

C49H66N10O10S2

Source: Drug Bank

Isomeric SMILES

C[C@H]([C@@H]1C(=O)N[C@@H](CSSC[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)NC(=O)[C@H](CC5=CC=CC=C5)N)C(=O)N[C@@H](CO)[C@H](C)O)O

Source: Drug Bank

Canonical SMILES

Not Available

Source: Drug Bank

Average Molecular Weight

1019.2390

Source: Drug Bank

SMILES

C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)CC2=CC=CC=C2)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@H](CC2=CNC3=C2C=CC=C3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)O)C(=O)N1

Source: Drug Bank

InChI String

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

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Drug Targets

Gene Description
SSTR1 (source: Drug Bank )
SSTR2 (source: Drug Bank )
SSTR5 (source: Drug Bank )
TACR2 (source: Drug Bank )

Drug Interactions

Interaction Description
cyclosporine - octreotide Octreotide decreases the effect of cyclosporine (source: Drug Bank )
cyclosporine - octreotide Octreotide decreases the effect of cyclosporine (source: Drug Bank )
quinupristin - octreotide This combination presents an increased risk of toxicity (source: Drug Bank )
thiothixene - octreotide May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank )
thiothixene - octreotide May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank )
toremifene - octreotide Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank )
trimipramine - octreotide Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank )
voriconazole - octreotide Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank )
vorinostat - octreotide Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank )
ziprasidone - octreotide Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. (source: Drug Bank )
zuclopenthixol - octreotide Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank )

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0078-0180-01
DrugBank:
DB00104
KEGG Compound:
C07306
KEGG Drug:
D00442
PubChem Compound:
383414
PubChem Substance:
7847508
IUPHAR Ligand:
2055
Drugs Product Database (DPD):
2248639
BindingDB:
50175592
Therapeutic Targets Database:
DAP000397
FDA Drug Label at DailyMed:
4e2c9856-1836-49f0-9472-4dbeeb408f39

Clinical Trials

These are trials that mention octreotide and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.