Peringatan Keamanan

There is limited information regarding cases of octreotide overdose aside from case reports of an overdose with injectable octreotide. The dose ranged from 2.4 mg/day to 6 mg/day administered by continuous infusion or subcutaneous administration of 1.5 mg three times daily. Effects of an overdose with octreotide may include hypotension, brain hypoxia, arrhythmia, cardiac arrest, lactic acidosis, pancreatitis, hepatomegaly, diarrhea, flushing, lethargy, and weakness.L14528

Octreotide

DB00104

biotech approved investigational

Deskripsi

Acromegaly is a disorder caused by excess growth hormone (GH), increasing the growth of body tissues and causing metabolic dysfunction.L14501 In most cases, it results from an anterior pituitary growth hormone-releasing tumor. Typically, the feet, hands, and face grow abnormally large; organomegaly and insulin resistance may also occur. Acromegaly is a life-threatening disease requiring life-long management.L14501

Octreotide is a long-acting drug with pharmacologic activities that mimic those of the natural hormone, somatostatin, which inhibits the secretion of growth hormone.L14513 Additionally, it is used for the treatment of acromegaly and symptoms arising from various tumors, including carcinoid tumors and vasoactive intestinal tumors (VIPomas).L14513 In the past, octreotide has been administered solely by injection. On June 26, 2020, the first approved delayed-release oral somatostatin analog, Mycapssa, received FDA approval for the long term maintenance treatment of acromegaly. This drug was developed by Chiasma Inc.L14495,L14507,L14528

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) After a subcutaneous dose, the plasma half-life is estimated to be 0.2 hours. The average elimination half-lives for subcutaneous and oral administration ranged from 2.3 - 2.7 hours and did not differ significantly.[L14528] One pharmacokinetic study revealed a plasma half-life ranging from 72-113 minutes.[A214721]
Volume Distribusi In a pharmacokinetic study, the volume of distribution was 13.6 L in healthy volunteers.[L14528] One pharmacokinetic study revealed a volume of distribution ranging from 18.1-30.4L after intravenous administration in healthy volunteers.[A214721]
Klirens (Clearance) The total body clearance of octreotide is 7-10 L/h.[L14528] One pharmacokinetic study revealed a total body clearance of 11.4 L/h.[A214721]

Absorpsi

After a subcutaneous dose, octreotide is absorbed completely upon administration.A214721,L14513 After the administration of an oral delayed-release capsule, peak concentrations were found to be 33% lower than after subcutaneous administration.L14528 The Cmax was attained at 1.67–2.5 hours after oral administration versus 30 minutes for the subcutaneous route. At 20 mg twice a day in patients with acromegaly, peak concentration was 2.5 mg/nL versus 5.30 ng/mL at 40 mg twice a day.L14528 AUC increases in proportion with the dose, regardless of the route.A214721,L14528

Metabolisme

Octreotide has been reported to be heavily metabolized in the liver.A214721

Rute Eliminasi

About 32% of an oral octreotide dose is excreted into the urine L14528 and 30-40% is excreted by the liver into the feces.A214721. About 11% of the unchanged parent drug is found in the urine, and 2% of the unchanged parent drug can be recovered in the feces.A214721

Interaksi Makanan

2 Data
  • 1. Take on an empty stomach. The oral capsules should be taken on an empty stomach. Food reduces oral octreotide absorption by 90%.
  • 2. Take with or without food. Octreotide injections may be taken with or without food.

Interaksi Obat

782 Data
Ceritinib Octreotide may increase the bradycardic activities of Ceritinib.
Pegvisomant The risk or severity of increased transaminases can be increased when Octreotide is combined with Pegvisomant.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Octreotide.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Octreotide.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Octreotide.
Colchicine The metabolism of Colchicine can be decreased when combined with Octreotide.
Fentanyl The serum concentration of the active metabolites of Octreotide can be increased when Octreotide is used in combination with Fentanyl.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Octreotide.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Octreotide.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Octreotide.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Octreotide.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Octreotide.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Octreotide.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Octreotide.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Octreotide.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Octreotide.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Octreotide.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Octreotide.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Octreotide.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Octreotide.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Octreotide.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Octreotide.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Octreotide.
Leuprolide The risk or severity of QTc prolongation can be increased when Octreotide is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Goserelin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Moxifloxacin.
Sulpiride The risk or severity of QTc prolongation can be increased when Octreotide is combined with Sulpiride.
Promazine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Prochlorperazine.
Droperidol The risk or severity of QTc prolongation can be increased when Octreotide is combined with Droperidol.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Octreotide.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Ciprofloxacin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Octreotide is combined with Fluorouracil.
Perflutren The risk or severity of QTc prolongation can be increased when Octreotide is combined with Perflutren.
Atropine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Atropine.
Efavirenz The risk or severity of QTc prolongation can be increased when Octreotide is combined with Efavirenz.
Adenosine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Adenosine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Octreotide is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Octreotide is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Octreotide is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Cinoxacin.
Granisetron The risk or severity of QTc prolongation can be increased when Octreotide is combined with Granisetron.
Ondansetron The risk or severity of QTc prolongation can be increased when Octreotide is combined with Ondansetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Octreotide is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Desloratadine.
Telithromycin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Telithromycin.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Octreotide is combined with Dimenhydrinate.
Papaverine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Papaverine.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Chlorpheniramine.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Ofloxacin.
Flecainide The risk or severity of QTc prolongation can be increased when Octreotide is combined with Flecainide.
Probucol The risk or severity of QTc prolongation can be increased when Octreotide is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Terlipressin.
Lofexidine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Lofexidine.
Azimilide The risk or severity of QTc prolongation can be increased when Octreotide is combined with Azimilide.
Pracinostat The risk or severity of QTc prolongation can be increased when Octreotide is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Octreotide is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Octreotide is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Telavancin.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Nemonoxacin.
Antazoline The risk or severity of QTc prolongation can be increased when Octreotide is combined with Antazoline.
Bedaquiline The risk or severity of QTc prolongation can be increased when Octreotide is combined with Bedaquiline.
Butriptyline The risk or severity of QTc prolongation can be increased when Octreotide is combined with Butriptyline.
Lenvatinib The risk or severity of QTc prolongation can be increased when Octreotide is combined with Lenvatinib.
Melperone The risk or severity of QTc prolongation can be increased when Octreotide is combined with Melperone.
Dexchlorpheniramine maleate The risk or severity of QTc prolongation can be increased when Octreotide is combined with Dexchlorpheniramine maleate.
Amifampridine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Amifampridine.
Mocetinostat The risk or severity of QTc prolongation can be increased when Octreotide is combined with Mocetinostat.
Entinostat The risk or severity of QTc prolongation can be increased when Octreotide is combined with Entinostat.
Gilteritinib The metabolism of Gilteritinib can be decreased when combined with Octreotide.
CUDC-101 The risk or severity of QTc prolongation can be increased when Octreotide is combined with CUDC-101.
Simendan The risk or severity of QTc prolongation can be increased when Octreotide is combined with Simendan.
Ricolinostat The risk or severity of QTc prolongation can be increased when Octreotide is combined with Ricolinostat.
Mizolastine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Mizolastine.
Abexinostat The risk or severity of QTc prolongation can be increased when Octreotide is combined with Abexinostat.
Oxatomide The risk or severity of QTc prolongation can be increased when Octreotide is combined with Oxatomide.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Sitafloxacin.
Sultopride The risk or severity of QTc prolongation can be increased when Octreotide is combined with Sultopride.
Nizofenone The risk or severity of QTc prolongation can be increased when Octreotide is combined with Nizofenone.
Bunaftine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Bunaftine.
Lorcainide The risk or severity of QTc prolongation can be increased when Octreotide is combined with Lorcainide.
Dexchlorpheniramine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Dexchlorpheniramine.
Azithromycin The metabolism of Azithromycin can be decreased when combined with Octreotide.
Chlorpromazine The metabolism of Chlorpromazine can be decreased when combined with Octreotide.
Erythromycin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Erythromycin.
Ranolazine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Ranolazine.
Amitriptyline The risk or severity of QTc prolongation can be increased when Octreotide is combined with Amitriptyline.
Methadone The risk or severity of QTc prolongation can be increased when Octreotide is combined with Methadone.
Imipramine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Imipramine.
Chloroquine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Chloroquine.
Primaquine The risk or severity of QTc prolongation can be increased when Octreotide is combined with Primaquine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Octreotide is combined with Levofloxacin.

Target Protein

Somatostatin receptor type 2 SSTR2
Somatostatin receptor

Referensi & Sumber

Synthesis reference: Nishith Chaturvedi, "Novel process for production of the somatostatin analog, octreotide." U.S. Patent US20040225108, issued November 11, 2004.
Artikel (PubMed)
  • PMID: 28091879
    Biermasz NR: New medical therapies on the horizon: oral octreotide. Pituitary. 2017 Feb;20(1):149-153. doi: 10.1007/s11102-016-0785-3.
  • PMID: 2689136
    Battershill PE, Clissold SP: Octreotide. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in conditions associated with excessive peptide secretion. Drugs. 1989 Nov;38(5):658-702. doi: 10.2165/00003495-198938050-00002.
  • PMID: 1976930
    Prelevic GM, Wurzburger MI, Balint-Peric L, Nesic JS: Inhibitory effect of sandostatin on secretion of luteinising hormone and ovarian steroids in polycystic ovary syndrome. Lancet. 1990 Oct 13;336(8720):900-3. doi: 10.1016/0140-6736(90)92270-r.
  • PMID: 12874677
    Clarke DL, McKune A, Thomson SR: Octreotide lowers gastric mucosal blood flow in normal and portal hypertensive stomachs. Surg Endosc. 2003 Oct;17(10):1570-2. doi: 10.1007/s00464-002-9274-z. Epub 2003 Jul 21.

Contoh Produk & Brand

Produk: 133 • International brands: 1
Produk
  • BYNFEZIA Pen
    Injection • 2.5 mg/1mL • Subcutaneous • US • Approved
  • Mycapssa
    Capsule, delayed release • 20 mg/1 • Oral • US • Approved
  • Mycapssa
    Capsule, delayed release • 20 mg/1 • Oral • US • Approved
  • Mycapssa
    Capsule, delayed release • 20 mg • Oral • EU • Approved
  • Ocphyl
    Solution • 100 mcg / mL • Intravenous; Subcutaneous • Canada • Approved
  • Ocphyl
    Solution • 500 mcg / mL • Intravenous; Subcutaneous • Canada • Approved
  • Ocphyl
    Solution • 50 mcg / mL • Intravenous; Subcutaneous • Canada • Approved
  • Octreotide
    Injection, solution • 200 ug/1mL • Intravenous; Subcutaneous • US • Generic • Approved
Menampilkan 8 dari 133 produk.
International Brands
  • Sandostatin LAR — Novartis Pharmaceuticals

Sekuens Gen/Protein (FASTA)

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