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    Chemistry

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    Also known as: 72956-09-3, Coreg, Dilatrend, Eucardic, Kredex, Carvedilolum [latin]
    Molecular Formula
    C24H26N2O4
    Molecular Weight
    406.5  g/mol
    InChI Key
    OGHNVEJMJSYVRP-UHFFFAOYSA-N
    FDA UNII
    0K47UL67F2
    Carvedilol
    A carbazole and propanol derivative that acts as a non-cardioselective beta blocker and vasodilator. It has blocking activity for ALPHA 1 ADRENERGIC RECEPTORS and, at higher doses, may function as a blocker of CALCIUM CHANNELS; it also has antioxidant properties. Carvedilol is used in the treatment of HYPERTENSION; ANGINA PECTORIS; and HEART FAILURE. It can also reduce the risk of death following MYOCARDIAL INFARCTION.
    Carvedilol is an alpha-Adrenergic Blocker and beta-Adrenergic Blocker. The mechanism of action of carvedilol is as an Adrenergic alpha-Antagonist and Adrenergic beta1-Antagonist and Adrenergic beta2-Antagonist.
    1 2D Structure

    Carvedilol

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
    2.1.2 InChI
    InChI=1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3
    2.1.3 InChI Key
    OGHNVEJMJSYVRP-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O
    2.2 Other Identifiers
    2.2.1 UNII
    0K47UL67F2
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. 14c-labeled Carvedilol

    2. Bm 14190

    3. Bm-14190

    4. Bm14190

    5. Carvedilol Hydrochloride

    6. Carvedilol, (+)

    7. Carvedilol, (+)-isomer

    8. Carvedilol, (+-)-isomer

    9. Carvedilol, (-)

    10. Carvedilol, (-)-isomer

    11. Carvedilol, (r)-isomer

    12. Carvedilol, (s)-isomer

    13. Carvedilol, 14c Labeled

    14. Carvedilol, 14c-labeled

    15. Coreg

    16. Coropres

    17. Dilatrend

    18. Eucardic

    19. Kredex

    20. Querto

    2.3.2 Depositor-Supplied Synonyms

    1. 72956-09-3

    2. Coreg

    3. Dilatrend

    4. Eucardic

    5. Kredex

    6. Carvedilolum [latin]

    7. Carvedilolum

    8. Querto

    9. Bm 14190

    10. 1-(9h-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol

    11. Bm-14190

    12. Dimitone

    13. Artist

    14. Skf 105517

    15. 1-(9h-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol

    16. 1-((9h-carbazol-4-yl)oxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)propan-2-ol

    17. Coronis

    18. Korvasan

    19. Talliton

    20. Dq 2466

    21. Dq-2466

    22. C07ag02

    23. (+-)-1-(carbazol-4-yloxy)-3-((2-(o-methoxyphenoxy)ethyl)amino)-2-propanol

    24. Chembl723

    25. Nsc-758694

    26. Sk&f-105517

    27. Bm 14.190

    28. Bm-14-190

    29. Bm-14.190

    30. Chebi:3441

    31. 0k47ul67f2

    32. [3-(9h-carbazol-4-yloxy)-2-hydroxypropyl][2-(2-methoxyphenoxy)ethyl]amine

    33. 1-(9h-carbazol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol

    34. Skf-105517

    35. (r)-bm 14190

    36. (s)-bm 14190

    37. Coropress

    38. Dibloc

    39. R-(+)-carvedilol

    40. S-(-)-carvedilol

    41. 1-(9h-carbazol-4-yloxy)-3-[(2-{[2-(methyloxy)phenyl]oxy}ethyl)amino]propan-2-ol

    42. Smr000449280

    43. Artist (tn)

    44. Coreg (tn)

    45. Hsdb 7044

    46. Sr-01000759289

    47. Unii-0k47ul67f2

    48. Mfcd00869663

    49. 1-(9h-carbazol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol

    50. Carvedilol D5

    51. Eg-p042

    52. Mfcd00864692

    53. Carvedilol - Bio-x

    54. Bm14190

    55. Carvedilol [usan:usp:inn:ban:jan]

    56. Spectrum_001665

    57. Carvedilol [mi]

    58. Carvedilol [inn]

    59. Carvedilol [jan]

    60. Spectrum2_001673

    61. Spectrum3_001182

    62. Spectrum4_000636

    63. Spectrum5_001436

    64. Carvedilol [hsdb]

    65. Carvedilol [usan]

    66. Carvedilol [vandf]

    67. Carvedilol [mart.]

    68. Carvedilol [usp-rs]

    69. Carvedilol [who-dd]

    70. Schembl22293

    71. Gtpl551

    72. Kbiogr_001252

    73. Kbioss_002145

    74. Mls000758299

    75. Mls000759508

    76. Mls001424092

    77. Mls006011886

    78. Spbio_001885

    79. Carvedilol (jp17/usp/inn)

    80. Carvedilol [orange Book]

    81. Dtxsid8022747

    82. Schembl10082334

    83. Schembl13287211

    84. Bdbm25759

    85. Kbio2_002145

    86. Kbio2_004713

    87. Kbio2_007281

    88. Kbio3_002323

    89. Carvedilol [ep Monograph]

    90. (r)-1-[(4-carbazolyl)oxy]-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol

    91. Carvedilol [usp Monograph]

    92. Hms2051n03

    93. Hms2089b09

    94. Hms2093e12

    95. Hms3261e15

    96. Hms3269n11

    97. Hms3393n03

    98. Hms3413b14

    99. Hms3655o14

    100. Hms3677b14

    101. Hms3715d15

    102. Hms3750i15

    103. Hms3884e12

    104. Pharmakon1600-01504257

    105. Carvedilol 1.0 Mg/ml In Methanol

    106. ((c)i)-carvedilol-d4(ethyl-d4)

    107. Amy40801

    108. Bcp23386

    109. Ex-a5746

    110. Hy-b0006

    111. Tox21_500347

    112. Bbl029064

    113. Mfcd00869664

    114. Nsc758694

    115. S1831

    116. Stk621453

    117. Akos005554967

    118. Carvedilol, >=98% (hplc), Solid

    119. Ac-1641

    120. Bcp9000493

    121. Ccg-100917

    122. Ccg-207952

    123. Cs-1194

    124. Db01136

    125. Ks-1037

    126. Lp00347

    127. Nc00167

    128. Nsc 758694

    129. Sb17441

    130. Sdccgsbi-0206771.p002

    131. 2-propanol, 1-(9h-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)-, (+-)-

    132. Ncgc00167832-01

    133. Ncgc00167832-02

    134. Ncgc00167832-03

    135. Ncgc00167832-04

    136. Ncgc00167832-19

    137. Ncgc00261032-01

    138. Bc164291

    139. Sy129821

    140. Sy283162

    141. Bcp0726000253

    142. Sbi-0206771.p001

    143. Db-055704

    144. Db-057556

    145. Db-057557

    146. Ft-0603055

    147. Ft-0603057

    148. Ft-0652640

    149. Ft-0664397

    150. Sw197547-3

    151. C06875

    152. D00255

    153. F19969

    154. Ab00639903-07

    155. Ab00639903-09

    156. Ab00639903_10

    157. Ab00639903_11

    158. Ab00639903_12

    159. 956c093

    160. L001243

    161. Q412534

    162. Q-200801

    163. Sr-01000759289-5

    164. Sr-01000759289-6

    165. Sr-01000759289-9

    166. Brd-a10977446-001-04-8

    167. Brd-a10977446-001-05-5

    168. Brd-a10977446-045-01-1

    169. Z2786051695

    170. Carvedilol, European Pharmacopoeia (ep) Reference Standard

    171. Ethyl 2-(9-(pyridin-4-ylmethyl)-9h-fluoren-9-yl)acetate

    172. Carvedilol, United States Pharmacopeia (usp) Reference Standard

    173. 1-(9h-carbazol-4-yloxy)-3-[2-(2-methoxy-phenoxy)-ethylamino]-propan-2-ol

    174. Carvedilol, Pharmaceutical Secondary Standard; Certified Reference Material

    175. (+/-)-1-carbazol-4-yloxy)-3-((2-(o-methoxyphenoxy)ethyl)amino)-2-propanol

    176. 1-(carbazol-4-yloxy)-3-((2-(o-methoxy-phenoxy)ethyl)amino)-2-propanol

    177. Carvedilol For System Suitability, European Pharmacopoeia (ep) Reference Standard

    178. 107741-96-8

    179. 2-propanol, 1-(9h-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)-, (+/-)-

    2.4 Create Date
    2005-03-25
    3 Chemical and Physical Properties
    Molecular Weight 406.5 g/mol
    Molecular Formula C24H26N2O4
    XLogP34.2
    Hydrogen Bond Donor Count3
    Hydrogen Bond Acceptor Count5
    Rotatable Bond Count10
    Exact Mass406.18925731 g/mol
    Monoisotopic Mass406.18925731 g/mol
    Topological Polar Surface Area75.7 Ų
    Heavy Atom Count30
    Formal Charge0
    Complexity508
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count1
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 6  
    Drug NameCarvedilol
    PubMed HealthCarvedilol (By mouth)
    Drug ClassesAntianginal, Antihypertensive, Cardiovascular Agent
    Drug LabelCarvedilol is a nonselective -adrenergic blocking agent with 1-blocking activity. It is ()-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol. Carvedilol is a racemic mixture with the following structure:Carvedilol tablets, US...
    Active IngredientCarvedilol
    Dosage FormTablet
    RouteOral
    Strength6.25mg; 25mg; 3.125mg; 12.5mg
    Market StatusPrescription
    CompanyRanbaxy; Glenmark Generics; Teva; Apotex; Aurobindo Pharma; Sun Pharm Inds; Beximco Usa; Pliva Hrvatska Doo; Taro; Lupin; Zydus Pharms Usa; Dr Reddys Labs; Sandoz; Cipla; Mylan; Hikma

    2 of 6  
    Drug NameCoreg
    PubMed HealthCarvedilol (By mouth)
    Drug ClassesAntianginal, Antihypertensive, Cardiovascular Agent
    Drug LabelCarvedilol is a nonselective -adrenergic blocking agent with 1-blocking activity. It is ()-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol. Carvedilol is a racemic mixture with the following structure:COREG is a white, oval...
    Active IngredientCarvedilol
    Dosage FormTablet
    RouteOral
    Strength6.25mg; 25mg; 3.125mg; 12.5mg
    Market StatusPrescription
    CompanySmithkline Beecham

    3 of 6  
    Drug NameCoreg cr
    PubMed HealthCarvedilol (By mouth)
    Drug ClassesAntianginal, Antihypertensive, Cardiovascular Agent
    Active IngredientCarvedilol phosphate
    Dosage FormCapsule, extended release
    RouteOral
    Strength10mg; 80mg; 40mg; 20mg
    Market StatusPrescription
    CompanySb Pharmco

    4 of 6  
    Drug NameCarvedilol
    PubMed HealthCarvedilol (By mouth)
    Drug ClassesAntianginal, Antihypertensive, Cardiovascular Agent
    Drug LabelCarvedilol is a nonselective -adrenergic blocking agent with 1-blocking activity. It is ()-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol. Carvedilol is a racemic mixture with the following structure:Carvedilol tablets, US...
    Active IngredientCarvedilol
    Dosage FormTablet
    RouteOral
    Strength6.25mg; 25mg; 3.125mg; 12.5mg
    Market StatusPrescription
    CompanyRanbaxy; Glenmark Generics; Teva; Apotex; Aurobindo Pharma; Sun Pharm Inds; Beximco Usa; Pliva Hrvatska Doo; Taro; Lupin; Zydus Pharms Usa; Dr Reddys Labs; Sandoz; Cipla; Mylan; Hikma

    5 of 6  
    Drug NameCoreg
    PubMed HealthCarvedilol (By mouth)
    Drug ClassesAntianginal, Antihypertensive, Cardiovascular Agent
    Drug LabelCarvedilol is a nonselective -adrenergic blocking agent with 1-blocking activity. It is ()-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol. Carvedilol is a racemic mixture with the following structure:COREG is a white, oval...
    Active IngredientCarvedilol
    Dosage FormTablet
    RouteOral
    Strength6.25mg; 25mg; 3.125mg; 12.5mg
    Market StatusPrescription
    CompanySmithkline Beecham

    6 of 6  
    Drug NameCoreg cr
    PubMed HealthCarvedilol (By mouth)
    Drug ClassesAntianginal, Antihypertensive, Cardiovascular Agent
    Active IngredientCarvedilol phosphate
    Dosage FormCapsule, extended release
    RouteOral
    Strength10mg; 80mg; 40mg; 20mg
    Market StatusPrescription
    CompanySb Pharmco

    4.2 Therapeutic Uses

    Adrenergic alpha-1 Receptor Antagonists; Adrenergic beta-Antagonists; Antihypertensive Agents; Vasodilator Agents

    National Library of Medicine's Medical Subject Headings online file (MeSH, 2009)

    Carvedilol is indicated for the treatment of mild-to-severe chronic heart failure of ischemic or cardiomyopathic origin, usually in addition to diuretics, ACE inhibitors, and digitalis, to increase survival and, also, to reduce the risk of hospitalization. /Included in US product label/

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    Carvedilol is indicated to reduce cardiovascular mortality in clinically stable patients who have survived the acute phase of a myocardial infarction and have a left ventricular ejection fraction of greater than 40 percent (with or without symptomatic heart failure). /Included in US product label/

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    Carvedilol is indicated for the management of essential hypertension. It can be used alone or in combination with other antihypertensive agents, especially thiazide-type diuretics. /Included in US product label/

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    For more Therapeutic Uses (Complete) data for CARVEDILOL (10 total), please visit the HSDB record page.

    4.3 Drug Warning

    Carvedilol is contraindicated in the following conditions: Bronchial asthma or related bronchospastic conditions. Deaths from status asthmaticus have been reported following single doses of carvedilol; second- or third-degree AV block; sick sinus syndrome; severe bradycardia (unless a permanent pacemaker is in place); Patients with cardiogenic shock or who have decompensated heart failure requiring the use of intravenous inotropic therapy. Such patients should first be weaned from intravenous therapy before initiating carvedilol; patients with severe hepatic impairment; patients with a history of a serious hypersensitivity reaction (eg, Stevens-Johnson syndrome, anaphylactic reaction, angioedema) to any component of this medication or other medications containing carvedilol.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    Patients with coronary artery disease, who are being treated with carvedilol, should be advised against abrupt discontinuation of therapy. Severe exacerbation of angina and the occurrence of myocardial infarction and ventricular arrhythmias have been reported in angina patients following the abrupt discontinuation of therapy with beta-blockers. The last 2 complications may occur with or without preceding exacerbation of the angina pectoris. As with other beta-blockers, when discontinuation of carvedilol is planned, the patients should be carefully observed and advised to limit physical activity to a minimum. Carvedilol should be discontinued over 1 to 2 weeks whenever possible. If the angina worsens or acute coronary insufficiency develops, it is recommended that carvedilol be promptly reinstituted, at least temporarily. Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue therapy with carvedilol abruptly even in patients treated only for hypertension or heart failure.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    Worsening heart failure or fluid retention may occur during up-titration of carvedilol. If such symptoms occur, diuretics should be increased and the carvedilol dose should not be advanced until clinical stability resumes. Occasionally it is necessary to lower the carvedilol dose or temporarily discontinue it. Such episodes do not preclude subsequent successful titration of, or a favorable response to, carvedilol. In a placebo-controlled trial of patients with severe heart failure, worsening heart failure during the first 3 months was reported to a similar degree with carvedilol and with placebo. When treatment was maintained beyond 3 months, worsening heart failure was reported less frequently in patients treated with carvedilol than with placebo. Worsening heart failure observed during long-term therapy is more likely to be related to the patients' underlying disease than to treatment with carvedilol.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    Rarely, use of carvedilol in patients with heart failure has resulted in deterioration of renal function. Patients at risk appear to be those with low blood pressure (systolic blood pressure greater than 100 mm Hg), ischemic heart disease and diffuse vascular disease, and/or underlying renal insufficiency. Renal function has returned to baseline when carvedilol was stopped. In patients with these risk factors it is recommended that renal function be monitored during up-titration of carvedilol and the drug discontinued or dosage reduced if worsening of renal function occurs.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    For more Drug Warnings (Complete) data for CARVEDILOL (24 total), please visit the HSDB record page.

    4.4 Drug Indication

    Carvedilol is indicated to treat mild to severe heart failure, left ventricular dysfunction after myocardial infarction with ventricular ejection fraction 40%, or hypertension.

    FDA Label

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Carvedilol reduces tachycardia through beta adrenergic antagonism and lowers blood pressure through alpha-1 adrenergic antagonism. It has a long duration of action as it is generally taken once daily and has a broad therapeutic index as patients generally take 10-80mg daily. Patients taking carvedilol should not abruptly stop taking this medication as this may exacerbate coronary artery disease.

    5.2 MeSH Pharmacological Classification

    Calcium Channel Blockers

    A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (See all compounds classified as Calcium Channel Blockers.)

    Antioxidants

    Naturally occurring or synthetic substances that inhibit or retard oxidation reactions. They counteract the damaging effects of oxidation in animal tissues. (See all compounds classified as Antioxidants.)

    Adrenergic alpha-1 Receptor Antagonists

    Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS. (See all compounds classified as Adrenergic alpha-1 Receptor Antagonists.)

    Adrenergic beta-Antagonists

    Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety. (See all compounds classified as Adrenergic beta-Antagonists.)

    Antihypertensive Agents

    Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)

    Vasodilator Agents

    Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    CARVEDILOL
    5.3.2 FDA UNII
    0K47UL67F2
    5.3.3 Pharmacological Classes
    Adrenergic beta1-Antagonists [MoA]; Adrenergic beta2-Antagonists [MoA]; alpha-Adrenergic Blocker [EPC]; beta-Adrenergic Blocker [EPC]; Adrenergic alpha-Antagonists [MoA]
    5.4 ATC Code

    C07AG02

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    C - Cardiovascular system

    C07 - Beta blocking agents

    C07A - Beta blocking agents

    C07AG - Alpha and beta blocking agents

    C07AG02 - Carvedilol

    5.5 Absorption, Distribution and Excretion

    Absorption

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

    Route of Elimination

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

    Volume of Distribution

    Carvedilol has a volume of distribution of 1.5-2L/kg or 115L.

    Clearance

    The plasma clearance of carvedilol has been reported as 0.52L/kg or 500-700mL/min.

    Carvedilol is rapidly and extensively absorbed following oral administration, with absolute bioavailability of approximately 25 percent to 35 percent due to a significant degree of first-pass metabolism.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011 https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    Food decreases the rate of the drug's absorption (ie, increases time to peak plasma concentration), but not the extent (ie, no effect on bioavailability) of absorption. Administration with food may decrease the risk of orthostatic hypotension.

    American Society of Health-System Pharmacists 2011; Drug Information 2011. Bethesda, MD. 2011, p. 1888

    Following oral administration of radiolabelled carvedilol to healthy volunteers, carvedilol accounted for only about 7 percent of the total radioactivity in plasma as measured by area under the curve (AUC). Less than 2 percent of the dose was excreted unchanged in the urine. ... The metabolites of carvedilol are excreted primarily via the bile into the feces.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011 https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    Carvedilol is more than 98 percent bound to plasma proteins, primarily with albumin. The plasma-protein binding is independent of concentration over the therapeutic range.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011 https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    For more Absorption, Distribution and Excretion (Complete) data for CARVEDILOL (13 total), please visit the HSDB record page.

    5.6 Metabolism/Metabolites

    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. Carvedilol can also be demethylated by CYP2C9, CYP2D6, CYP1A2, or CYP2E1 to form O-desmethylcarvedilol. Carvedilol and its metabolites may undergo further sulfate conjugation or glucuronidation before elimination. Carvedilol can be O-glucuronidated by UGT1A1, UGT2B4, and UGT2B7 to form carvedilol glucuronide.

    Carvedilol is metabolized primarily by aromatic ring oxidation and glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011 https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    Carvedilol is extensively metabolized; phenol ring demethylation and hydroxylation produce 3 metabolites with beta-adrenergic blocking activity and (weak) vasodilating activity. Plasma concentrations of active metabolites are about 10% those of carvedilol. The 4'-hydroxyphenyl metabolite is 13 times more potent than carvedilol in beta-adrenergic blocking activity.

    American Society of Health-System Pharmacists 2011; Drug Information 2011. Bethesda, MD. 2011, p. 1888

    Compared to carvedilol, the 3 active metabolites exhibit weak vasodilating activity. Plasma concentrations of the active metabolites are about one-tenth of those observed for carvedilol and have pharmacokinetics similar to the parent.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011 https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    Carvedilol undergoes stereoselective first-pass metabolism with plasma levels of R(+)-carvedilol approximately 2 to 3 times higher than S(-)-carvedilol following oral administration in healthy subjects.

    US Natl Inst Health; DailyMed. Current Medication Information for CARVEDILOL (carvedilol) tablet (May 2011). Available from, as of September 19, 2011 https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0b802a9c-332f-4ea8-bb34-75c677264654

    For more Metabolism/Metabolites (Complete) data for CARVEDILOL (7 total), please visit the HSDB record page.

    Carvedilol has known human metabolites that include (2S,3S,4S,5R)-6-[1-(9H-Carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid.

    S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560

    5.7 Biological Half-Life

    The half life of carvedilol is between 7-10 hours, though significantly shorter half lives have also been reported.

    The half-life of carvedilol is 7-10 hours; 5-9 hours for R(+)-carvedilol, and 7-11 hours for S(-)-carvedilol.

    American Society of Health-System Pharmacists 2011; Drug Information 2011. Bethesda, MD. 2011, p. 1888

    The pharmacokinetics and absolute bioavailability of carvedilol have been studied in 20 male healthy volunteers in a randomised 4-period, cross-over trial. Carvedilol 12.5 mg was given i.v., 50 mg was administered p.o. as a suspension and 25 and 50 mg were given in a capsule formulation. For the 50 mg capsule Cmax was 66 micrograms.l-1, tmax 1.2 h, t1/2 6.4 h. The t1/2 after i.v. administration was 2.4 h, CL 589 ml/min and VZ 132 l. The absolute bioavailability was 24% (50 mg capsule). The kinetics after the 25 and 50 mg capsules were consistent with dose linearity.

    PMID:3428345 von Mollendorff E, et al; Eur J Clin Pharmacol 33(5): 511-513 (1987)

    5.8 Mechanism of Action

    Carvedilol inhibits exercise induce tachycardia through its inhibition of beta adrenoceptors. Carvedilol's action on alpha-1 adrenergic receptors relaxes smooth muscle in vasculature, leading to reduced peripheral vascular resistance and an overall reduction in blood pressure. At higher doses, calcium channel blocking and antioxidant activity can also be seen. The antioxidant activity of carvedilol prevents oxidation of low density lipoprotein and its uptake into coronary circulation.

    Carvedilol is a nonselective beta-adrenergic blocking agent with selective alpha1-adrenergic blocking activity. The principal physiologic action of carvedilol is to competitively block adrenergic stimulation of beta-receptors within the myocardium (beta1-receptors) and within bronchial and vascular smooth muscle (beta2-receptors), and to a lesser extent alpha1-receptors within vascular smooth muscle. The beta1-antagonist activity of carvedilol is similar to that of propranolol and greater than that of labetalol, and the duration of carvedilol's effect is longer than those of labetalol and propranolol.

    American Society of Health-System Pharmacists 2011; Drug Information 2011. Bethesda, MD. 2011, p. 1888

    Studies in animals indicate that the drug may exert an antioxidant effect on the myocardium and an antiproliferative effect on intimal tissue. The commercially available drug is a racemic mixture of the 2 enantiomers, (R)[+] and (S)[-], and both enantiomers have equal alpha1-adrenergic blocking activity; however, only the S(-)-enantiomer of carvedilol has beta-adrenergic blocking activity. Carvedilol does not exhibit intrinsic sympathomimetic (beta1-agonist) activity and possesses only weak membrane-stabilizing (local anesthetic) activity.

    American Society of Health-System Pharmacists 2011; Drug Information 2011. Bethesda, MD. 2011, p. 1888

    Vasodilation resulting in reduced total peripheral resistance mediated through carvedilol's alpha1-adrenergic blockade and reduced sympathetic tone appear to play a major role in the drug's hypotensive effect. Carvedilol causes reductions in cardiac output, exercise-induced tachycardia, isoproterenol-induced tachycardia, and reflex orthostatic tachycardia. Clinically important beta-adrenergic blocking activity of carvedilol usually is evident within 1 hour of oral administration, and the drug's hypotensive effect is similar to that of metoprolol. Carvedilol's alpha1-adrenergic blocking effects, which contribute to the drug's hypotensive effects, generally are evident within 30 minutes of oral administration and include reductions in phenylephrine-induced pressor effects, vasodilation, and decreased peripheral vascular resistance. The dose-dependent hypotensive effect of carvedilol results in blood pressure (systolic and diastolic) reductions of 5-46% with little, if any, reflex tachycardia. This hypotensive effect occurs approximately 30 minutes after oral administration and has a maximum effect 1.5-7 hours after oral administration.

    American Society of Health-System Pharmacists 2011; Drug Information 2011. Bethesda, MD. 2011, p. 1888

    The precise mechanism of the beneficial effects of carvedilol in the treatment of congestive heart failure has not been fully elucidated. beta1-Adrenergic blockade and vasodilation generally are associated with reflex tachycardia and peripheral vasoconstriction in therapeutic agents in which one of these pharmacologic effects predominates, but the combined effects of carvedilol appear to attenuate these two major untoward responses by balancing the potential adverse effects associated with adrenergic blockade and vasodilation. The drug's vasodilatory action appears to enable the patient to tolerate the negative inotropic effect of carvedilol during the initiation and titration of therapy in the treatment of compensated heart failure.

    American Society of Health-System Pharmacists 2011; Drug Information 2011. Bethesda, MD. 2011, p. 1888

    For more Mechanism of Action (Complete) data for CARVEDILOL (18 total), please visit the HSDB record page.

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    DOSAGE - TABLET;ORAL - 12.5MG

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    ABOUT THIS PAGE

    Looking for 72956-09-3 / Carvedilol API manufacturers, exporters & distributors?

    Carvedilol manufacturers, exporters & distributors 1

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    PharmaCompass offers a list of Carvedilol API manufacturers, exporters & distributors, which can be sorted by GMP, USDMF, JDMF, KDMF, CEP (COS), WC, Price,and more, enabling you to easily find the right Carvedilol manufacturer or Carvedilol supplier for your needs.

    Send us enquiries for free, and we will assist you in establishing a direct connection with your preferred Carvedilol manufacturer or Carvedilol supplier.

    PharmaCompass also assists you with knowing the Carvedilol API Price utilized in the formulation of products. Carvedilol API Price is not always fixed or binding as the Carvedilol Price is obtained through a variety of data sources. The Carvedilol Price can also vary due to multiple factors, including market conditions, regulatory modifications, or negotiated pricing deals.

    API | Excipient name

    Carvedilol

    Synonyms

    72956-09-3, Coreg, Dilatrend, Eucardic, Kredex, Carvedilolum [latin]

    Cas Number

    72956-09-3

    Unique Ingredient Identifier (UNII)

    0K47UL67F2

    About Carvedilol

    A carbazole and propanol derivative that acts as a non-cardioselective beta blocker and vasodilator. It has blocking activity for ALPHA 1 ADRENERGIC RECEPTORS and, at higher doses, may function as a blocker of CALCIUM CHANNELS; it also has antioxidant properties. Carvedilol is used in the treatment of HYPERTENSION; ANGINA PECTORIS; and HEART FAILURE. It can also reduce the risk of death following MYOCARDIAL INFARCTION.

    Carvedilol Manufacturers

    A Carvedilol manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Carvedilol, including repackagers and relabelers. The FDA regulates Carvedilol manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Carvedilol API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

    click here to find a list of Carvedilol manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.

    Carvedilol Suppliers

    A Carvedilol supplier is an individual or a company that provides Carvedilol active pharmaceutical ingredient (API) or Carvedilol finished formulations upon request. The Carvedilol suppliers may include Carvedilol API manufacturers, exporters, distributors and traders.

    click here to find a list of Carvedilol suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

    Carvedilol USDMF

    A Carvedilol DMF (Drug Master File) is a document detailing the whole manufacturing process of Carvedilol active pharmaceutical ingredient (API) in detail. Different forms of Carvedilol DMFs exist exist since differing nations have different regulations, such as Carvedilol USDMF, ASMF (EDMF), JDMF, CDMF, etc.

    A Carvedilol DMF submitted to regulatory agencies in the US is known as a USDMF. Carvedilol USDMF includes data on Carvedilol's chemical properties, information on the facilities and procedures used, and details about packaging and storage. The Carvedilol USDMF is kept confidential to protect the manufacturer’s intellectual property.

    click here to find a list of Carvedilol suppliers with USDMF on PharmaCompass.

    Carvedilol JDMF

    The Pharmaceuticals and Medical Devices Agency (PMDA) established the Japan Drug Master File (JDMF), also known as the Master File (MF), to permit Japanese and foreign manufacturers of drug substances, intermediates, excipients, raw materials, and packaging materials (‘Products’) to voluntarily register confidential information about the production and management of their products in Japan.

    The Carvedilol Drug Master File in Japan (Carvedilol JDMF) empowers Carvedilol API manufacturers to present comprehensive information (e.g., production methods, data, etc.) to the review authority, i.e., PMDA (Pharmaceuticals & Medical Devices Agency).

    PMDA reviews the Carvedilol JDMF during the approval evaluation for pharmaceutical products. At the time of Carvedilol JDMF registration, PMDA checks if the format is accurate, if the necessary items have been included (application), and if data has been attached.

    click here to find a list of Carvedilol suppliers with JDMF on PharmaCompass.

    Carvedilol KDMF

    In Korea, the Ministry of Food and Drug Safety (MFDS) is in charge of regulating pharmaceutical products and services.

    Pharmaceutical companies submit a Carvedilol Drug Master File in Korea (Carvedilol KDMF) to the MFDS, which includes comprehensive information about the production, processing, facilities, materials, packaging, and testing of Carvedilol. The MFDS reviews the Carvedilol KDMF as part of the drug registration process and uses the information provided in the Carvedilol KDMF to evaluate the safety and efficacy of the drug.

    After submitting a Carvedilol KDMF to the MFDS, the registered manufacturer can provide importers or distributors with the registration number without revealing confidential information to Korean business partners. Applicants seeking to register their Carvedilol API can apply through the Korea Drug Master File (KDMF).

    click here to find a list of Carvedilol suppliers with KDMF on PharmaCompass.

    Carvedilol CEP

    A Carvedilol CEP of the European Pharmacopoeia monograph is often referred to as a Carvedilol Certificate of Suitability (COS). The purpose of a Carvedilol CEP is to show that the European Pharmacopoeia monograph adequately controls the purity of Carvedilol EP produced by a given manufacturer. Suppliers of raw materials can prove the suitability of Carvedilol to their clients by showing that a Carvedilol CEP has been issued for it. The manufacturer submits a Carvedilol CEP (COS) as part of the market authorization procedure, and it takes on the role of a Carvedilol CEP holder for the record. Additionally, the data presented in the Carvedilol CEP (COS) is managed confidentially and offers a centralized system acknowledged by numerous nations, exactly like the Carvedilol DMF.

    A Carvedilol CEP (COS) is recognised by all 36 nations that make up the European Pharmacopoeia Convention. Carvedilol CEPs may be accepted in nations that are not members of the Ph. Eur. at the discretion of the authorities there.

    click here to find a list of Carvedilol suppliers with CEP (COS) on PharmaCompass.

    Carvedilol WC

    A Carvedilol written confirmation (Carvedilol WC) is an official document issued by a regulatory agency to a Carvedilol manufacturer, verifying that the manufacturing facility of a Carvedilol active pharmaceutical ingredient (API) adheres to the Good Manufacturing Practices (GMP) regulations of the importing country. When exporting Carvedilol APIs or Carvedilol finished pharmaceutical products to another nation, regulatory agencies frequently require a Carvedilol WC (written confirmation) as part of the regulatory process.

    click here to find a list of Carvedilol suppliers with Written Confirmation (WC) on PharmaCompass.

    Carvedilol NDC

    National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Carvedilol as an active pharmaceutical ingredient (API).

    Finished drug products

    The FDA updates the NDC directory daily. The NDC numbers for Carvedilol API and other APIs are published in this directory by the FDA.

    Unfinished drugs

    The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.

    Pharmaceutical companies that manufacture Carvedilol as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.

    Compounded drug products

    The NDC directory also contains data on finished compounded human drug products that contain Carvedilol and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Carvedilol NDC to their finished compounded human drug products, they may choose to do so.

    click here to find a list of Carvedilol suppliers with NDC on PharmaCompass.

    Carvedilol GMP

    Carvedilol Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

    GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

    PharmaCompass offers a list of Carvedilol GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Carvedilol GMP manufacturer or Carvedilol GMP API supplier for your needs.

    Carvedilol CoA

    A Carvedilol CoA (Certificate of Analysis) is a formal document that attests to Carvedilol's compliance with Carvedilol specifications and serves as a tool for batch-level quality control.

    Carvedilol CoA mostly includes findings from lab analyses of a specific batch. For each Carvedilol CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

    Carvedilol may be tested according to a variety of international standards, such as European Pharmacopoeia (Carvedilol EP), Carvedilol JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Carvedilol USP).

    Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
    For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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