Peringatan Keamanan

There is no information available regarding the drug's LD50. While there is limited clinical experience with terlipressin overdose, manifestations are expected to be similar to the adverse reactions experienced with therapeutic doses. In case of an overdosage, initiate close monitoring of vital signs, electrolytes, and potential ischemic events and initiate appropriate symptomatic treatment.L43217

Terlipressin

DB02638

biotech approved investigational

Deskripsi

Terlipressin is a synthetic analogue of vasopressin, which is an endogenous neurohormone that acts as a vasoconstrictor.A2601 It is a prodrug of lypressin, or lysine vasopressin. Compared to endogenous vasopressin, terlipressin has a longer half life and increased selectivity for the V1 receptor.L43217 As a potent vasopressor, terlipressin has been investigated in various shock states and conditions with diminished vasomotor tone.A2601, A2602, A2603, A2604, A2605 It was also studied in hepatorenal syndrome (HRS) and variceal bleeding.A252672 The drug was first approved by the FDA in September 2022.L43217

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) The terminal half-life of terlipressin was 0.9 hours and 3.0 hours for lysine-vasopressin.[L43217]
Volume Distribusi The volume of distribution of terlipressin was 6.3 L and 1370 L for lysine-vasopressin.[L43217]
Klirens (Clearance) The clearance of terlipressin was 27.4 L/hr and 318 L/hr for lysine-vasopressin. Clearance of terlipressin in HRS-1 patients increased with body weight, while body weight had no effect on the clearance of lysine-vasopressin.[L43217]

Absorpsi

Following a 1 mg IV injection of terlipressin acetate in patients with HRS-1, the median Cmax, AUC24h and Cave of terlipressin at steady-state were 70.5 ng/mL, 123 ng × hr/mL and 14.2 ng/mL, respectively. The median Cmax, AUC24h and Cave of lypressin were 1.2 ng/mL, 11.2 ng × hr/mL and 0.5 ng/mL, respectively. Terlipressin and lypressin exhibit linear pharmacokinetics in healthy subjects. Plasma concentrations of terlipressin demonstrate proportional increases with the dose administered.L43217

Metabolisme

The N-terminal glycyl residues of terlipressin is cleaved by various tissue peptidases to release its pharmacologically active metabolite, lypressin or lysine-vasopressin. Once formed, lypressin is undergoes various peptidase-mediated metabolic pathways in body tissues. Terlipressin is not metabolized in the blood or plasma. Due to the ubiquitous nature of peptidases in body tissues, it is unlikely that the metabolism of terlipressin will be affected by disease state or other drugs.L43217

Rute Eliminasi

Less than 1% of terlipressin and <0.1% of lysine-vasopressin is excreted in urine in healthy subjects.L43217

Interaksi Obat

377 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Terlipressin.
Dofetilide The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Dofetilide.
Citalopram The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Citalopram.
Anagrelide The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Valproic acid.
Terfenadine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Terfenadine.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Grepafloxacin.
Quinine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Quinine.
Sotalol The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Sotalol.
Erlotinib The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Erlotinib.
Toremifene The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Toremifene.
Cisapride The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Cisapride.
Imatinib The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Imatinib.
Astemizole The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Astemizole.
Thioridazine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Thioridazine.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Trovafloxacin.
Mifepristone The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Mifepristone.
Cocaine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Cocaine.
Quinidine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Quinidine.
Procainamide The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Procainamide.
Pimozide The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Pimozide.
Amiodarone The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Amiodarone.
Arsenic trioxide The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Arsenic trioxide.
Escitalopram The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Escitalopram.
Domperidone The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Domperidone.
Sparfloxacin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Sparfloxacin.
Halofantrine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Halofantrine.
Bepridil The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Bepridil.
Paliperidone The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Paliperidone.
Lithium cation The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Lithium cation.
Temafloxacin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Temafloxacin.
Zuclopenthixol The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Zuclopenthixol.
Tetrabenazine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Tetrabenazine.
Dronedarone The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Dronedarone.
Nilotinib The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Nilotinib.
Iloperidone The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Iloperidone.
Vandetanib The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Vandetanib.
Romidepsin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Romidepsin.
Asenapine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Asenapine.
Artemether The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Lumefantrine.
Vemurafenib The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Vemurafenib.
Eliglustat The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Eliglustat.
Ribociclib The risk or severity of QTc prolongation can be increased when Ribociclib is combined with Terlipressin.
Glasdegib The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Glasdegib.
Deutetrabenazine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Deutetrabenazine.
Macimorelin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Macimorelin.
Terodiline The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Terodiline.
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Terlipressin.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Terlipressin.
Erythromycin The risk or severity of QTc prolongation can be increased when Erythromycin is combined with Terlipressin.
Azithromycin The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Terlipressin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Terlipressin.
Ranolazine The risk or severity of QTc prolongation can be increased when Ranolazine is combined with Terlipressin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Terlipressin.
Amitriptyline The risk or severity of QTc prolongation can be increased when Amitriptyline is combined with Terlipressin.
Methadone The risk or severity of QTc prolongation can be increased when Methadone is combined with Terlipressin.
Diltiazem The risk or severity of QTc prolongation can be increased when Diltiazem is combined with Terlipressin.
Clozapine The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Clozapine.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Terlipressin.
Nimodipine The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Terlipressin.
Promazine The risk or severity of QTc prolongation can be increased when Promazine is combined with Terlipressin.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Prochlorperazine is combined with Terlipressin.
Droperidol The risk or severity of QTc prolongation can be increased when Droperidol is combined with Terlipressin.
Imipramine The risk or severity of QTc prolongation can be increased when Imipramine is combined with Terlipressin.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Chlorpromazine is combined with Terlipressin.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Terlipressin.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Ciprofloxacin is combined with Terlipressin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Terlipressin.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Terlipressin.
Cinnarizine The risk or severity of QTc prolongation can be increased when Cinnarizine is combined with Terlipressin.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Terlipressin.
Chloroquine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Terlipressin.
Efavirenz The risk or severity of QTc prolongation can be increased when Efavirenz is combined with Terlipressin.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Terlipressin.
Pentamidine The risk or severity of QTc prolongation can be increased when Pentamidine is combined with Terlipressin.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Terlipressin.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Carbinoxamine is combined with Terlipressin.
Dolasetron The risk or severity of QTc prolongation can be increased when Dolasetron is combined with Terlipressin.
Roxithromycin The risk or severity of QTc prolongation can be increased when Roxithromycin is combined with Terlipressin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Nalidixic acid is combined with Terlipressin.
Cinoxacin The risk or severity of QTc prolongation can be increased when Cinoxacin is combined with Terlipressin.
Loperamide The risk or severity of QTc prolongation can be increased when Loperamide is combined with Terlipressin.
Granisetron The risk or severity of QTc prolongation can be increased when Granisetron is combined with Terlipressin.
Ondansetron The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Terlipressin.
Levosimendan The risk or severity of QTc prolongation can be increased when Levosimendan is combined with Terlipressin.
Mesoridazine The risk or severity of QTc prolongation can be increased when Mesoridazine is combined with Terlipressin.
Desloratadine The risk or severity of QTc prolongation can be increased when Desloratadine is combined with Terlipressin.
Telithromycin The risk or severity of QTc prolongation can be increased when Telithromycin is combined with Terlipressin.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Lomefloxacin is combined with Terlipressin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Terlipressin.
Primaquine The risk or severity of QTc prolongation can be increased when Primaquine is combined with Terlipressin.
Papaverine The risk or severity of QTc prolongation can be increased when Papaverine is combined with Terlipressin.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Chlorpheniramine is combined with Terlipressin.
Nifedipine The risk or severity of QTc prolongation can be increased when Nifedipine is combined with Terlipressin.
Levofloxacin The risk or severity of QTc prolongation can be increased when Levofloxacin is combined with Terlipressin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Gemifloxacin is combined with Terlipressin.

Target Protein

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

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17148649
    Pesaturo AB, Jennings HR, Voils SA: Terlipressin: vasopressin analog and novel drug for septic shock. Ann Pharmacother. 2006 Dec;40(12):2170-7. Epub 2006 Dec 5.
  • PMID: 17125115
    Klein M, Weksler N, Borer A, Koyfman L, Kesslin J, Gurman GM: Terlipressin facilitates transport of septic patients treated with norepinephrine. Isr Med Assoc J. 2006 Oct;8(10):691-3.
  • PMID: 16015526
    Leone M, Charvet A, Delmas A, Albanese J, Martin C, Boyle WA: Terlipressin: a new therapeutic for calcium-channel blockers overdose. J Crit Care. 2005 Mar;20(1):114-5.
  • PMID: 15803052
    Matok I, Vard A, Efrati O, Rubinshtein M, Vishne T, Leibovitch L, Adam M, Barzilay Z, Paret G: Terlipressin as rescue therapy for intractable hypotension due to septic shock in children. Shock. 2005 Apr;23(4):305-10.
  • PMID: 15488059
    Kam PC, Williams S, Yoong FF: Vasopressin and terlipressin: pharmacology and its clinical relevance. Anaesthesia. 2004 Oct;59(10):993-1001.
  • PMID: 33065772
    Kulkarni AV, Arab JP, Premkumar M, Benitez C, Tirumalige Ravikumar S, Kumar P, Sharma M, Reddy DN, Simonetto DA, Rao PN: Terlipressin has stood the test of time: Clinical overview in 2020 and future perspectives. Liver Int. 2020 Dec;40(12):2888-2905. doi: 10.1111/liv.14703.
  • PMID: 30252325
    Cuzzo B, Padala SA, Lappin SL: Physiology, Vasopressin .

Contoh Produk & Brand

Produk: 1 • International brands: 3
Produk
  • Terlivaz
    Injection, powder, lyophilized, for solution • 0.85 mg/5mL • Intravenous • US • Approved
International Brands
  • Glypressin — Ferring Pharmaceuticals
  • Lucassin
  • Teripress — New Medicon Pharma

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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