Peringatan Keamanan

Data is not available.

Somatostatin

DB09099

small molecule approved investigational

Deskripsi

Somatostatin, also known as growth hormone-inhibiting hormone, is a naturally-occurring peptide hormone of 14 or 28 amino acid residues T28 that regulates the endocrine system. It is secreted by the D cells of the islets to inhibit the release of insulin and glucagon, and is also generated in the hypothalamus, where it inhibits the release of growth hormone and thyroid-stimulating hormones from the anterior pituitary T28. Somatostatin is initially secreted as a 116 amino acid precursor, preprosomatostatin, which undergoes endoproteolytic cleavage to prosomastatin. Prosomastatin is further process into two active forms, somatostatin-14 (SST-14) and somatostatin-28 (SST-28), an extended SST-14 sequence to the N-terminus A20384. The actions of somatostatin are mediated via signalling pathways of G protein-coupled somatostatin receptors.

Antineoplastic effects and potential uses of somatostatin on various tumours, including pituitary adenomas, GEP-NETs, paragangliomas, carcinoids, breast cancers, malignant lymphoma and small-cell lung cancers, have been extensively investigated A20384. Somatostatin has been used in the clinical setting for the diagnosis of acromegaly and gastrointestinal tract tumours. Its analogues have been developed to achieve more favourable kinetics for efficiency use in the management of acute conditions, such as esophageal varices. DB00104 is a long-acting analogue of somatostatin that inhibits the release of a number of hormones, and is clinically used to relieve symptoms of uncommon gastroenteropancreatic endocrine tumours, as well as treat acromegaly T28.

Struktur Molekul 2D

Berat 1637.9
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of endogenous somatostatin is 1-3 minutes due to rapid degradation by peptidase enzymes present in the plasma and tissues [A20384].
Volume Distribusi This pharmacokinetic data is irrelevant.
Klirens (Clearance) Following intravenous administration of 3H-labeld endogenous somatostatin, the total body clearance was approximately 50 mL/min [A32596]. In man, the value was calculated to be as high as 3000 mL/minutes, which is greatly exceeds the hepatic blood flow. This suggests that rapid enzymatic breakdown in the circulation and other tissues serves as a critical route of elimination [A32596].

Absorpsi

This pharmacokinetic data is irrelevant.

Metabolisme

Somatostatin is rapidly degraded by peptidase enzymes present in cells and plasma A20384.

Rute Eliminasi

As a polypeptide chain, somatostatin is primarily eliminated via metabolism by peptidase enzymes A20384.

Interaksi Obat

210 Data
Lomitapide The metabolism of Lomitapide can be decreased when combined with Somatostatin.
Bromocriptine The serum concentration of Bromocriptine can be increased when it is combined with Somatostatin.
Pegvisomant The risk or severity of increased transaminases can be increased when Somatostatin is combined with Pegvisomant.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Somatostatin.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Somatostatin.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Somatostatin.
Colchicine The metabolism of Colchicine can be decreased when combined with Somatostatin.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Somatostatin.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Somatostatin.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Somatostatin.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Somatostatin.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Somatostatin.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Somatostatin.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Somatostatin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Somatostatin.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Somatostatin.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Somatostatin.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Somatostatin.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Somatostatin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Somatostatin.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Somatostatin.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Somatostatin.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Somatostatin.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Somatostatin.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Somatostatin.
Butalbital The risk or severity of adverse effects can be increased when Somatostatin is combined with Butalbital.
Pentobarbital The risk or severity of adverse effects can be increased when Somatostatin is combined with Pentobarbital.
Secobarbital The risk or severity of adverse effects can be increased when Somatostatin is combined with Secobarbital.
Methohexital The risk or severity of adverse effects can be increased when Somatostatin is combined with Methohexital.
Thiopental The risk or severity of adverse effects can be increased when Somatostatin is combined with Thiopental.
Primidone The risk or severity of adverse effects can be increased when Somatostatin is combined with Primidone.
Methylphenobarbital The risk or severity of adverse effects can be increased when Somatostatin is combined with Methylphenobarbital.
Thiamylal The risk or severity of adverse effects can be increased when Somatostatin is combined with Thiamylal.
Phenobarbital The risk or severity of adverse effects can be increased when Somatostatin is combined with Phenobarbital.
Amobarbital The risk or severity of adverse effects can be increased when Somatostatin is combined with Amobarbital.
Hexobarbital The risk or severity of adverse effects can be increased when Somatostatin is combined with Hexobarbital.
Barbital The risk or severity of adverse effects can be increased when Somatostatin is combined with Barbital.
Barbexaclone The risk or severity of adverse effects can be increased when Somatostatin is combined with Barbexaclone.
Butabarbital The risk or severity of adverse effects can be increased when Somatostatin is combined with Butabarbital.
Cyclosporine The bioavailability of Cyclosporine can be decreased when combined with Somatostatin.
Dotatate gallium Ga-68 Somatostatin may decrease effectiveness of Dotatate gallium Ga-68 as a diagnostic agent.
Lutetium Lu 177 dotatate The therapeutic efficacy of Lutetium Lu 177 dotatate can be decreased when used in combination with Somatostatin.
Aripiprazole The metabolism of Aripiprazole can be decreased when combined with Somatostatin.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be decreased when combined with Somatostatin.
Ziprasidone The metabolism of Ziprasidone can be decreased when combined with Somatostatin.
Cephalexin The metabolism of Cephalexin can be decreased when combined with Somatostatin.
Norethisterone The metabolism of Norethisterone can be decreased when combined with Somatostatin.
Rosuvastatin The metabolism of Rosuvastatin can be decreased when combined with Somatostatin.
Drospirenone The metabolism of Drospirenone can be decreased when combined with Somatostatin.
Allylestrenol The metabolism of Allylestrenol can be decreased when combined with Somatostatin.
Zuclopenthixol The metabolism of Zuclopenthixol can be decreased when combined with Somatostatin.
Roflumilast The serum concentration of Roflumilast can be increased when it is combined with Somatostatin.
Lacosamide The metabolism of Lacosamide can be decreased when combined with Somatostatin.
Tasimelteon The metabolism of Tasimelteon can be decreased when combined with Somatostatin.
Dihydroergocornine The metabolism of Dihydroergocornine can be decreased when combined with Somatostatin.
9-aminocamptothecin The metabolism of 9-aminocamptothecin can be decreased when combined with Somatostatin.
Methylprednisone The metabolism of Methylprednisone can be decreased when combined with Somatostatin.
Dihydroergocristine The metabolism of Dihydroergocristine can be decreased when combined with Somatostatin.
Dihydroergocryptine The metabolism of Dihydroergocryptine can be decreased when combined with Somatostatin.
Medical Cannabis The metabolism of Medical Cannabis can be decreased when combined with Somatostatin.
Elexacaftor The metabolism of Elexacaftor can be decreased when combined with Somatostatin.
Azithromycin The metabolism of Azithromycin can be decreased when combined with Somatostatin.
Chlorpromazine The metabolism of Chlorpromazine can be decreased when combined with Somatostatin.
Albendazole The metabolism of Albendazole can be decreased when combined with Somatostatin.
Doxazosin The metabolism of Doxazosin can be decreased when combined with Somatostatin.
Fenofibrate The metabolism of Fenofibrate can be decreased when combined with Somatostatin.
Atazanavir The metabolism of Atazanavir can be decreased when combined with Somatostatin.
Fosaprepitant The metabolism of Fosaprepitant can be decreased when combined with Somatostatin.
Linagliptin The metabolism of Linagliptin can be decreased when combined with Somatostatin.
Vorapaxar The metabolism of Vorapaxar can be decreased when combined with Somatostatin.
Suvorexant The metabolism of Suvorexant can be decreased when combined with Somatostatin.
Netupitant The metabolism of Netupitant can be decreased when combined with Somatostatin.
Lefamulin The metabolism of Lefamulin can be decreased when combined with Somatostatin.
Nintedanib The metabolism of Nintedanib can be decreased when combined with Somatostatin.
Tenofovir alafenamide The metabolism of Tenofovir alafenamide can be decreased when combined with Somatostatin.
Duvelisib The metabolism of Duvelisib can be decreased when combined with Somatostatin.
Gilteritinib The metabolism of Gilteritinib can be decreased when combined with Somatostatin.
Tazemetostat The metabolism of Tazemetostat can be decreased when combined with Somatostatin.
Methysergide The metabolism of Methysergide can be decreased when combined with Somatostatin.
Meperidine The metabolism of Meperidine can be decreased when combined with Somatostatin.
Ebastine The metabolism of Ebastine can be decreased when combined with Somatostatin.
Terfenadine The metabolism of Terfenadine can be decreased when combined with Somatostatin.
Cisapride The metabolism of Cisapride can be decreased when combined with Somatostatin.
Isavuconazole The metabolism of Isavuconazole can be decreased when combined with Somatostatin.
Pretomanid The metabolism of Pretomanid can be decreased when combined with Somatostatin.
Pimavanserin The metabolism of Pimavanserin can be decreased when combined with Somatostatin.
Estetrol The metabolism of Estetrol can be decreased when combined with Somatostatin.
Infigratinib The metabolism of Infigratinib can be decreased when combined with Somatostatin.
Sirolimus The metabolism of Sirolimus can be decreased when combined with Somatostatin.
Quinidine The metabolism of Quinidine can be decreased when combined with Somatostatin.
Pimozide The metabolism of Pimozide can be decreased when combined with Somatostatin.
Amiodarone The metabolism of Amiodarone can be decreased when combined with Somatostatin.
Paclitaxel The metabolism of Paclitaxel can be decreased when combined with Somatostatin.
Dasatinib The metabolism of Dasatinib can be decreased when combined with Somatostatin.
Everolimus The metabolism of Everolimus can be decreased when combined with Somatostatin.
Dronedarone The metabolism of Dronedarone can be decreased when combined with Somatostatin.
Temsirolimus The metabolism of Temsirolimus can be decreased when combined with Somatostatin.
Carbamazepine The metabolism of Carbamazepine can be decreased when combined with Somatostatin.
Digitoxin The metabolism of Digitoxin can be decreased when combined with Somatostatin.
Dofetilide The metabolism of Dofetilide can be decreased when combined with Somatostatin.

Target Protein

Mu-type opioid receptor OPRM1
Delta-type opioid receptor OPRD1
Somatostatin receptor type 1 SSTR1
Somatostatin receptor type 2 SSTR2
Somatostatin receptor type 3 SSTR3
Somatostatin receptor type 4 SSTR4
Somatostatin receptor type 5 SSTR5

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25956467
    Rai U, Thrimawithana TR, Valery C, Young SA: Therapeutic uses of somatostatin and its analogues: Current view and potential applications. Pharmacol Ther. 2015 Aug;152:98-110. doi: 10.1016/j.pharmthera.2015.05.007. Epub 2015 May 5.
  • PMID: 1385068
    Hanisch E, Doertenbach J, Usadel KH: Somatostatin in acute bleeding oesophageal varices. Pharmacology and rationale for use. Drugs. 1992;44 Suppl 2:24-35; discussion 70-2.
  • PMID: 10433861
    Patel YC: Somatostatin and its receptor family. Front Neuroendocrinol. 1999 Jul;20(3):157-98.
  • PMID: 12431842
    Lamberts SW, de Herder WW, Hofland LJ: Somatostatin analogs in the diagnosis and treatment of cancer. Trends Endocrinol Metab. 2002 Dec;13(10):451-7.
  • PMID: 1355590
    Marbach P, Briner U, Lemaire M, Schweitzer A, Terasaki T: From somatostatin to sandostatin: pharmacodynamics and pharmacokinetics. Metabolism. 1992 Sep;41(9 Suppl 2):7-10.
  • PMID: 11207395
    Carlton SM, Du J, Davidson E, Zhou S, Coggeshall RE: Somatostatin receptors on peripheral primary afferent terminals: inhibition of sensitized nociceptors. Pain. 2001 Feb 15;90(3):233-44.
  • PMID: 1356016
    Reubi JC, Laissue J, Krenning E, Lamberts SW: Somatostatin receptors in human cancer: incidence, characteristics, functional correlates and clinical implications. J Steroid Biochem Mol Biol. 1992 Sep;43(1-3):27-35.
  • PMID: 12639942
    Florio T, Morini M, Villa V, Arena S, Corsaro A, Thellung S, Culler MD, Pfeffer U, Noonan DM, Schettini G, Albini A: Somatostatin inhibits tumor angiogenesis and growth via somatostatin receptor-3-mediated regulation of endothelial nitric oxide synthase and mitogen-activated protein kinase activities. Endocrinology. 2003 Apr;144(4):1574-84. doi: 10.1210/en.2002-220949.
Textbook
  • ISBN: 978-0-7020-3471-8
    29, 30, 32, 33, 41, . (2012). In Rang and Dale's Pharmacology (7th ed., pp. 362, 372, 377, 394-395, 412, 522). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Stilamin - Pws IV 3mg/amp
    Powder, for solution • 3 mg / amp • Intravenous • Canada • Approved
  • Stilamin - Pws Liq IV
    Liquid; Powder, for solution • - • Intravenous • Canada • Approved

Sekuens Gen/Protein (FASTA)

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