Peringatan Keamanan

No systemic toxicities were found in rat and dog studies at dosages equivalent to 10 times normal human exposure L2469. It is thought that the risk of toxicity is low due to the short duration of action and short half life of atosiban A32685.

Atosiban

DB09059

small molecule approved investigational

Deskripsi

Atosiban is an inhibitor of the hormones oxytocin and vasopressin. It is used intravenously to halt premature labor. Although initial studies suggested it could be used as a nasal spray and hence would not require hospital admission, it is not used in that form. Atobisan was developed by the Swedish company Ferring Pharmaceuticals. It was first reported in the literature in 1985. Atosiban is licensed in proprietary and generic forms for the delay of imminent pre-term birth in pregnant adult women.

Struktur Molekul 2D

Berat 994.19
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Atosiban does not conform to either 1-compartment or 2-compartment kinetics. It has been determined to have an initial half life (t?) of 0.21 h and a terminal half life (t?) of 1.7 h [L2469].
Volume Distribusi Atosiban has a mean volume of distribution of 41.8 L. Atosiban crosses the placenta and, at a dose of 300 ?g/min, was found to have a 0.12 maternal/fetal concentration ratio [L2469].
Klirens (Clearance) Atosiban has a mean clearance rate of 41.8 L/h [L2469].

Absorpsi

In women receiving 300 ?g/min by infusion for 6-12 h, average steady state concentrations of 442 ng/mL were reached within 1 h L2469. Steady state concentrations increase proportionally to dosage.

Metabolisme

There are two metabolites of atosiban created through the cleavage of the peptide bond between ornithine and proline which is thought to be facilitated by prior cleavage of the disulfide bridge L2469,A32690. The larger fragment remains active as an antagonist of oxytocin receptors but is 10 times less potent than the parent molecule. At a dosage of 300 ?g/min the ratio of parent molecule to the main metabolite was observed to be 1.4 at the second hour and 2.8 at the end of infusion L2469.

Rute Eliminasi

Small amounts of atosiban are found in the urine with 50 times the amount appearing as the large fragment metabolite (des-(Orn?, Gly?-NH2)-Mpa¹, D-Tyr(Et)², Thr?-oxytocin L2469. The amount of drug excreted in the feces is not known.

Interaksi Obat

35 Data
Isoetharine The risk or severity of adverse effects can be increased when Isoetharine is combined with Atosiban.
Norepinephrine The risk or severity of adverse effects can be increased when Norepinephrine is combined with Atosiban.
Phenylpropanolamine The risk or severity of adverse effects can be increased when Phenylpropanolamine is combined with Atosiban.
Epinephrine The risk or severity of adverse effects can be increased when Epinephrine is combined with Atosiban.
Orciprenaline The risk or severity of adverse effects can be increased when Orciprenaline is combined with Atosiban.
Dobutamine The risk or severity of adverse effects can be increased when Dobutamine is combined with Atosiban.
Ritodrine The risk or severity of adverse effects can be increased when Ritodrine is combined with Atosiban.
Terbutaline The risk or severity of adverse effects can be increased when Terbutaline is combined with Atosiban.
Bitolterol The risk or severity of adverse effects can be increased when Bitolterol is combined with Atosiban.
Salmeterol The risk or severity of adverse effects can be increased when Salmeterol is combined with Atosiban.
Formoterol The risk or severity of adverse effects can be increased when Formoterol is combined with Atosiban.
Albuterol The risk or severity of adverse effects can be increased when Salbutamol is combined with Atosiban.
Isoprenaline The risk or severity of adverse effects can be increased when Isoprenaline is combined with Atosiban.
Arbutamine The risk or severity of adverse effects can be increased when Arbutamine is combined with Atosiban.
Arformoterol The risk or severity of adverse effects can be increased when Arformoterol is combined with Atosiban.
Fenoterol The risk or severity of adverse effects can be increased when Fenoterol is combined with Atosiban.
Pirbuterol The risk or severity of adverse effects can be increased when Pirbuterol is combined with Atosiban.
Ephedra sinica root The risk or severity of adverse effects can be increased when Ephedra sinica root is combined with Atosiban.
Procaterol The risk or severity of adverse effects can be increased when Procaterol is combined with Atosiban.
Clenbuterol The risk or severity of adverse effects can be increased when Clenbuterol is combined with Atosiban.
Bambuterol The risk or severity of adverse effects can be increased when Bambuterol is combined with Atosiban.
Celiprolol The risk or severity of adverse effects can be increased when Celiprolol is combined with Atosiban.
Indacaterol The risk or severity of adverse effects can be increased when Indacaterol is combined with Atosiban.
Droxidopa The risk or severity of adverse effects can be increased when Droxidopa is combined with Atosiban.
Protokylol The risk or severity of adverse effects can be increased when Protokylol is combined with Atosiban.
Hexoprenaline The risk or severity of adverse effects can be increased when Hexoprenaline is combined with Atosiban.
Olodaterol The risk or severity of adverse effects can be increased when Olodaterol is combined with Atosiban.
Vilanterol The risk or severity of adverse effects can be increased when Vilanterol is combined with Atosiban.
Doxofylline The risk or severity of adverse effects can be increased when Doxofylline is combined with Atosiban.
Racepinephrine The risk or severity of adverse effects can be increased when Racepinephrine is combined with Atosiban.
Etafedrine The risk or severity of adverse effects can be increased when Etafedrine is combined with Atosiban.
PF-00610355 The risk or severity of adverse effects can be increased when PF-00610355 is combined with Atosiban.
Abediterol The risk or severity of adverse effects can be increased when Abediterol is combined with Atosiban.
Batefenterol The risk or severity of adverse effects can be increased when Batefenterol is combined with Atosiban.
Levosalbutamol The risk or severity of adverse effects can be increased when Levosalbutamol is combined with Atosiban.

Target Protein

Oxytocin receptor OXTR
Vasopressin V1a receptor AVPR1A
Vasopressin V1b receptor AVPR1B
Vasopressin V2 receptor AVPR2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12763125
    Lamont RF: The development and introduction of anti-oxytocic tocolytics. BJOG. 2003 Apr;110 Suppl 20:108-12.
  • PMID: 8952002
    Fjellestad-Paulsen A, Lundin S: Metabolism of vasopressin, oxytocin and their analogues Mpa1, D-Arg8-vasopressin (dDAVP) and Mpa1, D-Tyr(Et)2, Thr4, Orn8-oxytocin (antocin) in human kidney and liver homogenates. Regul Pept. 1996 Nov 14;67(1):27-32.
  • PMID: 15705593
    Reversi A, Rimoldi V, Marrocco T, Cassoni P, Bussolati G, Parenti M, Chini B: The oxytocin receptor antagonist atosiban inhibits cell growth via a "biased agonist" mechanism. J Biol Chem. 2005 Apr 22;280(16):16311-8. doi: 10.1074/jbc.M409945200. Epub 2005 Feb 10.
  • PMID: 26586210
    Kim SH, MacIntyre DA, Hanyaloglu AC, Blanks AM, Thornton S, Bennett PR, Terzidou V: The oxytocin receptor antagonist, Atosiban, activates pro-inflammatory pathways in human amnion via G(alphai) signalling. Mol Cell Endocrinol. 2016 Jan 15;420:11-23. doi: 10.1016/j.mce.2015.11.012. Epub 2015 Nov 14.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Atosiban Sun
    Injection, solution • 6.75 mg/0.9ml • Intravenous • EU • Approved
  • Atosiban Sun
    Injection, solution, concentrate • 37.5 mg/5ml • Intravenous • EU • Approved
  • Tractocile
    Injection, solution • 6.75 mg/0.9ml • Intravenous • EU • Approved
  • Tractocile
    Injection, solution, concentrate • 37.5 mg/5ml • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

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