Peringatan Keamanan

Although no data on overdosage in humans are available, conivaptan has been administered as a 20 mg loading dose on Day 1 followed by continuous infusion of 80 mg/day for 4 days in hyponatremia patients and up to 120 mg/day for 2 days in CHF patients. No new toxicities were identified at these higher doses, but adverse events related to the pharmacologic activity of conivaptan, e.g. hypotension and thirst, occurred more frequently at these higher doses.

Conivaptan

DB00872

small molecule approved investigational

Deskripsi

Conivaptan is a non-peptide inhibitor of antidiuretic hormone (vasopressin). It was approved in 2004 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH). Conivaptan inhibits both isotypes of the vasopressin receptor (V1a and V2).

Struktur Molekul 2D

Berat 498.5744
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 5 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

CYP3A4 is the sole cytochrome P450 isozyme responsible for the metabolism of conivaptan. Four metabolites have been identified. The pharmacological activity of the metabolites at V1a and V2 receptors ranged from approximately 3-50% and 50-100% that of conivaptan, respectively.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

1603 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Conivaptan is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Conivaptan is combined with Levodopa.
Risperidone Conivaptan may increase the hypotensive activities of Risperidone.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Conivaptan.
Armodafinil The metabolism of Conivaptan can be increased when combined with Armodafinil.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Conivaptan.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Conivaptan.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Conivaptan.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Conivaptan.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Conivaptan.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Conivaptan.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Conivaptan.
Silodosin The excretion of Silodosin can be decreased when combined with Conivaptan.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Conivaptan.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Conivaptan.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Conivaptan.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Conivaptan.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Conivaptan.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Conivaptan.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Conivaptan.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Conivaptan.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Conivaptan.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Conivaptan.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Conivaptan.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Conivaptan.
Metreleptin The metabolism of Conivaptan can be increased when combined with Metreleptin.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Conivaptan.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Conivaptan.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Conivaptan.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Conivaptan.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Conivaptan.
Crizotinib The metabolism of Conivaptan can be decreased when combined with Crizotinib.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Conivaptan.
Nicorandil Nicorandil may increase the hypotensive activities of Conivaptan.
Vincristine The excretion of Vincristine can be decreased when combined with Conivaptan.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Conivaptan.
Linezolid Linezolid may increase the orthostatic hypotensive activities of Conivaptan.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Conivaptan.
Procaine Procaine may increase the orthostatic hypotensive activities of Conivaptan.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Conivaptan.
Procarbazine Procarbazine may increase the orthostatic hypotensive activities of Conivaptan.
Moclobemide Moclobemide may increase the orthostatic hypotensive activities of Conivaptan.
Isocarboxazid Isocarboxazid may increase the orthostatic hypotensive activities of Conivaptan.
Rasagiline Rasagiline may increase the orthostatic hypotensive activities of Conivaptan.
Pargyline Pargyline may increase the orthostatic hypotensive activities of Conivaptan.
Clorgiline Clorgiline may increase the orthostatic hypotensive activities of Conivaptan.
Iproniazid Iproniazid may increase the orthostatic hypotensive activities of Conivaptan.
Nialamide Nialamide may increase the orthostatic hypotensive activities of Conivaptan.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Conivaptan.
Hydracarbazine Hydracarbazine may increase the orthostatic hypotensive activities of Conivaptan.
Pirlindole Pirlindole may increase the orthostatic hypotensive activities of Conivaptan.
Toloxatone Toloxatone may increase the orthostatic hypotensive activities of Conivaptan.
Benmoxin Benmoxin may increase the orthostatic hypotensive activities of Conivaptan.
Mebanazine Mebanazine may increase the orthostatic hypotensive activities of Conivaptan.
Octamoxin Octamoxin may increase the orthostatic hypotensive activities of Conivaptan.
Pheniprazine Pheniprazine may increase the orthostatic hypotensive activities of Conivaptan.
Phenoxypropazine Phenoxypropazine may increase the orthostatic hypotensive activities of Conivaptan.
Pivhydrazine Pivhydrazine may increase the orthostatic hypotensive activities of Conivaptan.
Safrazine Safrazine may increase the orthostatic hypotensive activities of Conivaptan.
Caroxazone Caroxazone may increase the orthostatic hypotensive activities of Conivaptan.
Harmaline Harmaline may increase the orthostatic hypotensive activities of Conivaptan.
Brofaromine Brofaromine may increase the orthostatic hypotensive activities of Conivaptan.
Tranylcypromine Tranylcypromine may increase the orthostatic hypotensive activities of Conivaptan.
Hexobarbital Hexobarbital may increase the hypotensive activities of Conivaptan.
Methohexital Methohexital may increase the hypotensive activities of Conivaptan.
Thiopental Thiopental may increase the hypotensive activities of Conivaptan.
Streptokinase The risk or severity of adverse effects can be increased when Streptokinase is combined with Conivaptan.
Methyclothiazide The risk or severity of adverse effects can be increased when Methyclothiazide is combined with Conivaptan.
Ropinirole The risk or severity of adverse effects can be increased when Ropinirole is combined with Conivaptan.
Triamterene The risk or severity of adverse effects can be increased when Triamterene is combined with Conivaptan.
Spironolactone The risk or severity of adverse effects can be increased when Spironolactone is combined with Conivaptan.
Nabilone The metabolism of Nabilone can be decreased when combined with Conivaptan.
Sotalol The risk or severity of adverse effects can be increased when Sotalol is combined with Conivaptan.
Amiloride The risk or severity of adverse effects can be increased when Amiloride is combined with Conivaptan.
Thioridazine The risk or severity of adverse effects can be increased when Thioridazine is combined with Conivaptan.
Tizanidine The risk or severity of adverse effects can be increased when Tizanidine is combined with Conivaptan.
Apomorphine The risk or severity of adverse effects can be increased when Apomorphine is combined with Conivaptan.
Isoflurane The risk or severity of adverse effects can be increased when Isoflurane is combined with Conivaptan.
Etacrynic acid The risk or severity of adverse effects can be increased when Conivaptan is combined with Etacrynic acid.
Levosimendan The risk or severity of adverse effects can be increased when Conivaptan is combined with Levosimendan.
Thalidomide The metabolism of Thalidomide can be decreased when combined with Conivaptan.
Iloprost The risk or severity of adverse effects can be increased when Conivaptan is combined with Iloprost.
Papaverine The risk or severity of adverse effects can be increased when Conivaptan is combined with Papaverine.
Amifostine The risk or severity of adverse effects can be increased when Conivaptan is combined with Amifostine.
Diclofenamide The risk or severity of adverse effects can be increased when Conivaptan is combined with Diclofenamide.
Desflurane The risk or severity of adverse effects can be increased when Conivaptan is combined with Desflurane.
Carbetocin The risk or severity of adverse effects can be increased when Conivaptan is combined with Carbetocin.
Amyl Nitrite The risk or severity of adverse effects can be increased when Conivaptan is combined with Amyl Nitrite.
Nesiritide The risk or severity of adverse effects can be increased when Conivaptan is combined with Nesiritide.
Azilsartan medoxomil The risk or severity of adverse effects can be increased when Conivaptan is combined with Azilsartan medoxomil.
Obinutuzumab The risk or severity of adverse effects can be increased when Conivaptan is combined with Obinutuzumab.
Isoxsuprine The risk or severity of adverse effects can be increased when Conivaptan is combined with Isoxsuprine.
Dinutuximab The risk or severity of adverse effects can be increased when Conivaptan is combined with Dinutuximab.
Nitrous acid The risk or severity of adverse effects can be increased when Conivaptan is combined with Nitrous acid.
Fimasartan The risk or severity of adverse effects can be increased when Conivaptan is combined with Fimasartan.
Pipamperone The risk or severity of adverse effects can be increased when Conivaptan is combined with Pipamperone.
Valsartan The risk or severity of adverse effects can be increased when Valsartan is combined with Conivaptan.
Ramipril The risk or severity of adverse effects can be increased when Ramipril is combined with Conivaptan.
Esmolol The risk or severity of adverse effects can be increased when Esmolol is combined with Conivaptan.
Betaxolol The risk or severity of adverse effects can be increased when Betaxolol is combined with Conivaptan.

Target Protein

Vasopressin V1a receptor AVPR1A
Vasopressin V2 receptor AVPR2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17919259
    Ali F, Raufi MA, Washington B, Ghali JK: Conivaptan: a dual vasopressin receptor v1a/v2 antagonist corrected. Cardiovasc Drug Rev. 2007 Fall;25(3):261-79.
  • PMID: 19695403
    Mao ZL, Stalker D, Keirns J: Pharmacokinetics of conivaptan hydrochloride, a vasopressin V(1A)/V(2)-receptor antagonist, in patients with euvolemic or hypervolemic hyponatremia and with or without congestive heart failure from a prospective, 4-day open-label study. Clin Ther. 2009 Jul;31(7):1542-50. doi: 10.1016/j.clinthera.2009.07.011.
  • PMID: 20054444
    Ghali JK, Farah JO, Daifallah S, Zabalawi HA, Zmily HD: Conivaptan and its role in the treatment of hyponatremia. Drug Des Devel Ther. 2009 Dec 29;3:253-68.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Vaprisol
    Solution • 20 mg/100mL • Intravenous • US • Approved
  • Vaprisol
    Liquid • 5 mg/1mL • Intravenous • US • Approved
  • Vaprisol Dextrose In Plastic Container
    Injection, solution • 20 mg/100mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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