Peringatan Keamanan

Toxicity information regarding milrinone is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as hypotension and adverse cardiac events such as ventricular arrhythmias. Symptomatic and supportive measures are recommended.L31483

Milrinone

DB00235

small molecule approved

Deskripsi

Heart failure is a multifactorial condition that affects roughly 1-2% of the adult population. Often the result of long-term myocardial ischemia, cardiomyopathy, or other cardiac insults, heart failure results from an inability of the heart to perfuse peripheral tissues with sufficient oxygen and metabolites, resulting in complex systemic pathologies. Heart failure is underpinned by numerous physiological changes, including alteration in ?-adrenergic signalling and cyclic adenosine monophosphate (cAMP) production, which affects the heart's contractile function and cardiac output.A228323 Milrinone is a second-generation bipyridine phosphodiesterase (PDE) inhibitor created through chemical modification of amrinone.A228333 As a PDE-III inhibitor, milrinone results in increased cAMP levels and improves cardiac function and peripheral vasodilation in acute decongested heart failure.A228338, A11759, A228323, A228333, A228348, L31483

Milrinone was originally synthesized at the Sterling Winthrop Research Institute in the 1980s.A228333 It was approved by the FDA on December 31, 1987, and was marketed under the trademark PRIMACOR® by Sanofi-Aventis US before being discontinued.L31483

Struktur Molekul 2D

Berat 211.2194
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Milrinone administered intravenously to congestive heart failure patients had a mean terminal elimination half-life of 2.3 hours (injections between 12.5-125 ?g/kg) and 2.4 hours (infusions between 0.2-0.7 ?g/kg/min.[L31483]
Volume Distribusi Milrinone administered intravenously to congestive heart failure patients had a volume of distribution of 0.38 L/kg (injections between 12.5-125 ?g/kg) and 0.45 L/kg (infusions between 0.2-0.7 ?g/kg/min.[L31483]
Klirens (Clearance) Milrinone administered intravenously to congestive heart failure patients had a clearance of 0.13 L/kg/hr (injections between 12.5-125 ?g/kg) and 0.14 L/kg/hr (infusions between 0.2-0.7 ?g/kg/min.[L31483]

Absorpsi

When administered as an IV bolus dose of 10-100 ?g/kg, milrinone induces hemodynamic effects within 60 seconds reaching a peak effect by 2-5 minutes.A228333 The plasma AUC is significantly dose-dependent.L31483

Metabolisme

Animal studies suggest that two oxidative pathways are involved in milrinone metabolism, albeit only involving a small proportion of the administered dose. The major metabolite is the O-glucuronide metabolite.A228333, L31483

Rute Eliminasi

Milrinone is primarily excreted in the urine, with 60% of a dose recovered after two hours and 90% within eight hours. Approximately 83% of milrinone recovered in urine is unchanged while 12% is present as the main O-glucuronide metabolite.A228333, A228358, L31483

Interaksi Obat

731 Data
Anagrelide The risk or severity of congestive heart failure, bleeding, hypotension, and Tachycardia can be increased when Milrinone is combined with Anagrelide.
Cilostazol The risk or severity of congestive heart failure, bleeding, hypotension, and Tachycardia can be increased when Milrinone is combined with Cilostazol.
Amrinone The risk or severity of congestive heart failure, bleeding, hypotension, and Tachycardia can be increased when Milrinone is combined with Amrinone.
Enoximone The risk or severity of congestive heart failure, bleeding, hypotension, and Tachycardia can be increased when Milrinone is combined with Enoximone.
Riociguat Milrinone may increase the hypotensive activities of Riociguat.
Patent Blue The therapeutic efficacy of Milrinone can be decreased when used in combination with Patent Blue.
Cyclosporine Cyclosporine may decrease the excretion rate of Milrinone which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Milrinone which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Milrinone which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Milrinone which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Milrinone which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Milrinone which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Milrinone which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Milrinone which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Milrinone which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Milrinone which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Milrinone which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Milrinone which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Milrinone which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Milrinone which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Milrinone which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Milrinone which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Milrinone which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Milrinone which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Milrinone which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Milrinone which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Milrinone which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Milrinone which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Milrinone which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Milrinone which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Milrinone which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Milrinone which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Milrinone which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Milrinone which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Milrinone which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Milrinone which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Milrinone which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Milrinone which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Milrinone which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Milrinone which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Milrinone which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Milrinone which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Milrinone which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Milrinone which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Milrinone which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Milrinone which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Milrinone which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Milrinone which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Milrinone which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Milrinone which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Milrinone which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Milrinone which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Milrinone which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Milrinone which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Milrinone which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Milrinone which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Milrinone which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Milrinone which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Milrinone which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Milrinone which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Milrinone which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Milrinone which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Milrinone which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Milrinone which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Milrinone which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Milrinone which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Milrinone which could result in a higher serum level.

Target Protein

cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A PDE3A

Referensi & Sumber

Synthesis reference: Baldev Singh, "Preparation of 1,2-dihydro-6-(lower alkyl)-2-oxo-5-(pyridinyl)nicotinonitriles." U.S. Patent US4413127A, issued November 1, 1983.
Artikel (PubMed)
  • PMID: 26756631
    Tanai E, Frantz S: Pathophysiology of Heart Failure. Compr Physiol. 2015 Dec 15;6(1):187-214. doi: 10.1002/cphy.c140055.
  • PMID: 8659556
    Shipley JB, Tolman D, Hastillo A, Hess ML: Milrinone: basic and clinical pharmacology and acute and chronic management. Am J Med Sci. 1996 Jun;311(6):286-91. doi: 10.1097/00000441-199606000-00011.
  • PMID: 6177950
    Kariya T, Wille LJ, Dage RC: Biochemical studies on the mechanism of cardiotonic activity of MDL 17,043. J Cardiovasc Pharmacol. 1982 May-Jun;4(3):509-14. doi: 10.1097/00005344-198205000-00024.
  • PMID: 2680495
    Colucci WS: Myocardial and vascular actions of milrinone. Eur Heart J. 1989 Aug;10 Suppl C:32-8. doi: 10.1093/eurheartj/10.suppl_c.32.
  • PMID: 30543176
    Kislitsina ON, Rich JD, Wilcox JE, Pham DT, Churyla A, Vorovich EB, Ghafourian K, Yancy CW: Shock - Classification and Pathophysiological Principles of Therapeutics. Curr Cardiol Rev. 2019;15(2):102-113. doi: 10.2174/1573403X15666181212125024.
  • PMID: 29045285
    Chong LYZ, Satya K, Kim B, Berkowitz R: Milrinone Dosing and a Culture of Caution in Clinical Practice. Cardiol Rev. 2018 Jan/Feb;26(1):35-42. doi: 10.1097/CRD.0000000000000165.
  • PMID: 12181427
    Zhang W, Ke H, Colman RW: Identification of interaction sites of cyclic nucleotide phosphodiesterase type 3A with milrinone and cilostazol using molecular modeling and site-directed mutagenesis. Mol Pharmacol. 2002 Sep;62(3):514-20.

Contoh Produk & Brand

Produk: 73 • International brands: 3
Produk
  • Apo-milrinone Injectable
    Solution • 1.0 mg / mL • Intravenous • Canada • Generic • Approved
  • Milrinone Injection
    Solution • 1 mg / mL • Intravenous • Canada • Approved
  • Milrinone Lactate
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Milrinone Lactate
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Milrinone Lactate
    Injection, solution • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Milrinone Lactate
    Injection, solution • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Milrinone Lactate
    Injection, solution • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Milrinone lactate
    Injection, solution • 1 mg/1mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 73 produk.
International Brands
  • Corotrop
  • Corotrope
  • Milrila

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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