Peringatan Keamanan

Patients experiencing an overdose may present with hypotension, bradycardia, cardiac insufficiency, cardiogenic shock, and cardiac arrest.L7889,L7892 Patients should remain in a supine position and may be given atropine for bradycardia and glucagon followed by sympathomimetics to support cardiovascular function.L7889,L7892

Carvedilol

DB01136

small molecule approved investigational

Deskripsi

Carvedilol is a racemic mixture where the S(-) enantiomer is both a beta and alpha-1 adrenoceptor blocker, and the R(+) enantiomer is an alpha-1 adrenoceptor blocker.L7889,L7892 It is currently used to treat heart failure, left ventricular dysfunction, and hypertension.L7889,L7892 The dual action of carvedilol is advantageous in combination therapies as moderate doses of 2 drugs have a decreased incidence of adverse effects compared to high dose monotherapy in the treatment of moderate hypertension.A182306

Carvedilol was granted FDA approval on 14 September 1995.L7889

Struktur Molekul 2D

Berat 406.4742
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of carvedilol is between 7-10 hours, though significantly shorter half lives have also been reported.[A182306,L7889,L7892]
Volume Distribusi Carvedilol has a volume of distribution of 1.5-2L/kg[A182306] or 115L.[L7892]
Klirens (Clearance) The plasma clearance of carvedilol has been reported as 0.52L/kg[A182306] or 500-700mL/min.[L7889,L7892]

Absorpsi

Carvedilol has a bioavailability of 25-35%.A182306,L7889,L7892 Carvedilol has a Tmax of 1 to 2 hours.A182306 Taking carvedilol with a meal increases Tmax without increasing AUC.A182306 Carvedilol doses of 50mg lead to a Cmax of 122-262µg/L and an AUC of 717-1600µg/L\*h.A182306 Carvedilol doses of 25mg lead to a Cmax of 24-151µg/L and an AUC of 272-947µg/L\*h.A182306 Carvedilol doses of 12.5mg lead to a Cmax of 58-69µg/L and an AUC of 208-225µg/L\*h.A182306

Metabolisme

Carvedilol can be hydroxlated at the 1 position by CYP2D6, CYP1A2, or CYP1A1 to form 1-hydroxypheylcarvedilol; at the 4 position by CYP2D6, CYP2E1, CYP2C9, or CYP3A4 to form 4'-hydroxyphenylcarvedilol; at the 5 position by CYP2D6, CYP2C9, or CYP3A4 to form 5'-hydroxyphenylcarvedilol; and at the 8 position by CYP1A2, CYP3A4, and CYP1A1 to form 8-hydroxycarbazolylcarvedilol.A39000 Carvedilol can also be demethylated by CYP2C9, CYP2D6, CYP1A2, or CYP2E1 to form O-desmethylcarvedilol.A39000 Carvedilol and its metabolites may undergo further sulfate conjugation or glucuronidation before elimination.A39000 Carvedilol can be O-glucuronidated by UGT1A1, UGT2B4, and UGT2B7 to form carvedilol glucuronide.A182303

Rute Eliminasi

16% of carvedilol is excreted in the urine with <2% excreted as unmetabolized drug.A182306 Carvedilol is primarily excreted in the bile and feces.L7889,L7892

Farmakogenomik

1 Varian
ADRB1 (rs1801253)

Patients with this genotype in ADRB1 have an increased likelihood of responding to carvedilol for the treatment of increased blood pressure.

Interaksi Makanan

1 Data
  • 1. Take with food. Food slows the absorption and reduces the incidence of adverse effects.

Interaksi Obat

1739 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Carvedilol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Carvedilol is combined with Levodopa.
Risperidone Carvedilol may increase the hypotensive activities of Risperidone.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Carvedilol.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Carvedilol.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Carvedilol.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Carvedilol.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Carvedilol.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Carvedilol.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Carvedilol.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Carvedilol.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Carvedilol.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Carvedilol.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Carvedilol.
Silodosin The excretion of Silodosin can be decreased when combined with Carvedilol.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Carvedilol.
Ceritinib Carvedilol may increase the bradycardic activities of Ceritinib.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Carvedilol.
Deferasirox The serum concentration of Carvedilol can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Carvedilol can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Carvedilol can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Carvedilol can be decreased when it is combined with Teriflunomide.
Amifostine Carvedilol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Carvedilol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Carvedilol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Carvedilol.
Obinutuzumab Carvedilol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Carvedilol.
Rituximab Carvedilol may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Carvedilol.
Doxapram Doxapram may decrease the antihypertensive activities of Carvedilol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Carvedilol.
Naratriptan Naratriptan may decrease the antihypertensive activities of Carvedilol.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Carvedilol.
Dopamine Dopamine may decrease the antihypertensive activities of Carvedilol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Carvedilol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Carvedilol.
Amineptine Amineptine may decrease the antihypertensive activities of Carvedilol.
Naluzotan Naluzotan may decrease the antihypertensive activities of Carvedilol.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Carvedilol.
Cinitapride Cinitapride may decrease the antihypertensive activities of Carvedilol.
Tyramine Tyramine may decrease the antihypertensive activities of Carvedilol.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Carvedilol.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Carvedilol.
Butriptyline Butriptyline may decrease the antihypertensive activities of Carvedilol.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Carvedilol.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Carvedilol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Carvedilol.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Carvedilol.
Piclozotan Piclozotan may decrease the antihypertensive activities of Carvedilol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Carvedilol.
Tramazoline Tramazoline may decrease the antihypertensive activities of Carvedilol.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Carvedilol.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Carvedilol.
Quinupramine Quinupramine may decrease the antihypertensive activities of Carvedilol.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Carvedilol.
Fenozolone Fenozolone may decrease the antihypertensive activities of Carvedilol.
Melitracen Melitracen may decrease the antihypertensive activities of Carvedilol.
Lofepramine Lofepramine may decrease the antihypertensive activities of Carvedilol.
Xenon Xenon may decrease the antihypertensive activities of Carvedilol.
Iprindole Iprindole may decrease the antihypertensive activities of Carvedilol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Carvedilol.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Carvedilol.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Carvedilol.
Mefenorex Mefenorex may decrease the antihypertensive activities of Carvedilol.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Carvedilol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Carvedilol.
Solriamfetol Solriamfetol may decrease the antihypertensive activities of Carvedilol.
Remifentanil Remifentanil may decrease the antihypertensive activities of Carvedilol.
Desflurane Desflurane may decrease the antihypertensive activities of Carvedilol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Carvedilol.
Buspirone Buspirone may decrease the antihypertensive activities of Carvedilol.
Sufentanil Sufentanil may decrease the antihypertensive activities of Carvedilol.
Alfentanil Alfentanil may decrease the antihypertensive activities of Carvedilol.
Fentanyl Fentanyl may decrease the antihypertensive activities of Carvedilol.
Almotriptan Almotriptan may decrease the antihypertensive activities of Carvedilol.
Finasteride Finasteride may decrease the antihypertensive activities of Carvedilol.
Yohimbine Yohimbine may decrease the antihypertensive activities of Carvedilol.
Solifenacin Solifenacin may decrease the antihypertensive activities of Carvedilol.
Flibanserin Flibanserin may decrease the antihypertensive activities of Carvedilol.
Cariprazine Cariprazine may decrease the antihypertensive activities of Carvedilol.
Vortioxetine Vortioxetine may decrease the antihypertensive activities of Carvedilol.
Tianeptine Tianeptine may decrease the antihypertensive activities of Carvedilol.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Carvedilol.
Protriptyline Protriptyline may decrease the antihypertensive activities of Carvedilol.
Opipramol Opipramol may decrease the antihypertensive activities of Carvedilol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Carvedilol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Carvedilol.
Amiodarone The therapeutic efficacy of Carvedilol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Carvedilol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Carvedilol.
Disopyramide Disopyramide may increase the bradycardic activities of Carvedilol.
Dronedarone Dronedarone may increase the bradycardic activities of Carvedilol.
Fingolimod Carvedilol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Carvedilol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Carvedilol.
Methacholine Carvedilol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Carvedilol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Carvedilol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Carvedilol.

Target Protein

Beta-1 adrenergic receptor ADRB1
Alpha-1A adrenergic receptor ADRA1A
Alpha-1 adrenergic receptors ADRA1A
NADH dehydrogenase [ubiquinone] 1 subunit C2 NDUFC2
Beta-2 adrenergic receptor ADRB2
Vascular endothelial growth factor A, long form VEGFA
Natriuretic peptides B NPPB
Gap junction alpha-1 protein GJA1
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2
Vascular cell adhesion protein 1 VCAM1
Alpha-1D adrenergic receptor ADRA1D
Alpha-1B adrenergic receptor ADRA1B
Alpha-2C adrenergic receptor ADRA2C
Alpha-2B adrenergic receptor ADRA2B
Alpha-2A adrenergic receptor ADRA2A
E-selectin SELE
Hypoxia-inducible factor 1-alpha HIF1A
Inward rectifier potassium channel 4 KCNJ4
Inward rectifier potassium channel 2 KCNJ2

Referensi & Sumber

Synthesis reference: Ilan Kor, "Crystalline solids of carvedilol and processes for their preparation." U.S. Patent US20030166702, issued September 04, 2003.
Artikel (PubMed)
  • PMID: 9824960
    Vanderhoff BT, Ruppel HM, Amsterdam PB: Carvedilol: the new role of beta blockers in congestive heart failure. Am Fam Physician. 1998 Nov 1;58(7):1627-34, 1641-2.
  • PMID: 9280405
    Oldham HG, Clarke SE: In vitro identification of the human cytochrome P450 enzymes involved in the metabolism of R(+)- and S(-)-carvedilol. Drug Metab Dispos. 1997 Aug;25(8):970-7.
  • PMID: 22293344
    Takekuma Y, Yagisawa K, Sugawara M: Mutual inhibition between carvedilol enantiomers during racemate glucuronidation mediated by human liver and intestinal microsomes. Biol Pharm Bull. 2012;35(2):151-63. doi: 10.1248/bpb.35.151.
  • PMID: 7914479
    Morgan T: Clinical pharmacokinetics and pharmacodynamics of carvedilol. Clin Pharmacokinet. 1994 May;26(5):335-46. doi: 10.2165/00003088-199426050-00002.

Contoh Produk & Brand

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International Brands
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