Blood pressure medication
Carvedilol is a beta-blocker medication, that may be prescribed for the treatment of high blood pressure (hypertension) and chronic heart failure with reduced ejection fraction (also known as HFrEF or systolic heart failure).
[1]
[2] Beta-blockers as a collective medication class are not recommended as routine first-line treatment of high blood pressure for all patients, due to evidence demonstrating less effective cardiovascular protection and a less favourable safety profile when compared to other classes of blood pressure-lowering medications.
[1]
[3]
[4]
Common
side effects include
dizziness ,
tiredness ,
joint pain ,
low blood pressure ,
nausea , and
shortness of breath .
[5] Severe side effects may include
bronchospasm .
[5] Safety during
pregnancy or
breastfeeding is unclear.
[6] Use is not recommended in those with
liver problems .
[7] Carvedilol is a
nonselective beta blocker and
alpha-1 blocker .
[5] How it improves outcomes is not entirely clear but may involve
dilation of blood vessels .
[5]
Carvedilol was patented in 1978 and approved for medical use in the United States in 1995.
[5]
[8] It is on the
World Health Organization's List of Essential Medicines .
[9] It is available as a
generic medication .
[5] In 2021, it was the 26th most commonly prescribed medication in the United States, with more than 21 million prescriptions.
[10]
[11]
Medical uses
Carvedilol is indicated in the management of
congestive heart failure (CHF), commonly as an adjunct to angiotensin-converting-enzyme inhibitor (
ACE inhibitors ) and
diuretics . It has been clinically shown to reduce mortality and hospitalizations in people with CHF.
[12] The mechanism of carvedilol in heart failure is due to its inhibition of receptors in the adrenergic nervous system, which releases
noradrenaline to the body, including the heart.
[13] Noradrenaline is a hormone that causes the heart to beat faster and work harder.
[13] Blocking its binding to adrenergic receptors in the heart causes vasodilation, decreases heart rate and blood pressure, and improves myocardial contractility,
[14] which ultimately decreases the heart's workload.
[13]
Carvedilol reduces the risk of death, hospitalisations, and recurring heart attacks in patients with moderate to severe heart failure (with an ejection fraction <40%) following a heart attack
[15]
[16]
[17] Carvedilol has also been proven to reduce death and hospitalization in patients with severe heart failure.
[18]
Carvedilol is not considered a first-line treatment for hypertension; however, research has demonstrated that it exhibits an antihypertensive effect when compared to a placebo or other antihypertensive medications.
[19]
[20]
Carvedilol has shown efficacy in preventing bleeding from oesophageal varices in patients with mild to moderate cirrhosis and may have benefit in avoiding successive bleeds.
[21]
[22]
Available forms
Carvedilol is available in the following forms:
Contraindications
Carvedilol should not be used in patients with bronchial asthma or bronchospastic conditions due to increased risk of bronchoconstriction.
[25]
[26] It should not be used in people with second- or third-degree
atrioventricular block ,
sick sinus syndrome , severe
bradycardia (unless a permanent
pacemaker is in place), or a
decompensated heart condition . People with severe hepatic impairment should use carvedilol with caution.
[27]
[28]
[29]
Side effects
The most common
side effects (>10% incidence) of carvedilol include:
[23]
Carvedilol is not recommended for people with uncontrolled bronchospastic disease (e.g. current asthma symptoms) as it can block receptors that assist in opening the airways.
[23]
Carvedilol may mask symptoms of
low blood sugar ,
[23] resulting in
hypoglycemia unawareness . This is termed
beta blocker induced hypoglycemia unawareness .
Drug Interactions
The risk of bradycardia is increased if used with amiodarone, digoxin, diltiazem, ivabradine, or verapamil.
[30] Also, combination of carvedilol with non-dihydropyridine calcium channel blockers, including diltiazem and verapamil, enhances it cardiodepressant effects.
[30]
Pharmacology
Pharmacodynamics
Carvedilol
Site
Ki (nM)
Action
5-HT1A
3.4
Antagonist
5-HT2
207
Antagonist
D2
213
Antagonist
α1
3.4
Antagonist
α2
2,168
Antagonist
β1
0.24–0.43
Antagonist
β2
0.19–0.25
Antagonist
M
2
?
Antagonist
[31]
Carvedilol is both a
non-selective
β-adrenergic receptor antagonist (
β1 ,
β2 ) and an
α-adrenergic receptor antagonist (
α1 ). The S(–)
enantiomer accounts for the beta-blocking activity whereas the S(–) and R(+) enantiomers have alpha-blocking activity.
[23] The
affinity (Ki ) of carvedilol for the β-adrenergic receptors is 0.32 nM for the human β1 -adrenergic receptor and 0.13 to 0.40 nM for the β2 -adrenergic receptor.
[32]
Using rat proteins, carvedilol has shown affinity for a variety of targets including the β1 -adrenergic receptor (Ki = 0.24–0.43 nM), β2 -adrenergic receptor (Ki = 0.19–0.25 nM), α1 -adrenergic receptor (Ki = 3.4 nM),
α2 -adrenergic receptor (Ki = 2,168 nM),
5-HT1A receptor (Ki = 3.4 nM),
5-HT2 receptor (Ki = 207 nM),
H1 receptor (Ki = 3,034 nM),
D2 receptor (Ki = 213 nM),
μ-opioid receptor (Ki = 2,700 nM),
veratridine site of
voltage-gated sodium channels (IC50 = 1,260 nM),
serotonin transporter (Ki = 528 nM),
norepinephrine transporter (Ki = 2,406 nM), and
dopamine transporter (Ki = 627 nM).
[33] It is an antagonist of the human
5-HT2A receptors with moderate affinity (Ki = 547 nM), although it is unclear if this is significant for its pharmacological actions given its much stronger activity at adrenergic receptors.
[34]
Carvedilol reversibly binds to β-adrenergic receptors on cardiac
myocytes . Inhibition of these receptors prevents a response to the
sympathetic nervous system , leading to decreased
heart rate and
contractility . This action is beneficial in
heart failure patients where the
sympathetic nervous system is activated as a compensatory mechanism.
[35] Carvedilol blockade of α1 -adrenergic receptors causes
vasodilation of
blood vessels . This inhibition leads to decreased
peripheral
vascular resistance and an
antihypertensive effect. There is no reflex
tachycardia response due to carvedilol blockade of β1 -adrenergic receptors on the
heart .
[36]
Pharmacokinetics
Carvedilol is about 25% to 35%
bioavailable following
oral administration due to extensive
first-pass metabolism .
Absorption is slowed when administered with food, however, it does not show a significant difference in bioavailability. Taking carvedilol with food decreases the risk of
orthostatic hypotension .
[23]
The majority of carvedilol is
bound to plasma proteins (98%), mainly to
albumin . Carvedilol is a
basic ,
hydrophobic compound with a
steady-state
volume of distribution of 115 L. Plasma
clearance ranges from 500 to 700 mL/min.
[23] Carvedilol is
lipophilic and easily crosses the
blood–brain barrier in animals, and hence is not thought to be
peripherally selective .
[37]
[38]
The compound is
metabolized by
liver
enzymes ,
CYP2D6 and
CYP2C9 via
aromatic ring
oxidation and
glucuronidation , then further
conjugated by glucuronidation and
sulfation . The three
active metabolites exhibit only one-tenth of the vasodilating effect of the
parent compound . However, the 4'-hydroxyphenyl
metabolite is about 13-fold more potent in β-blockade than the parent.
[23]
The mean
elimination half-life of carvedilol following oral administration ranges from 7 to 10 hours. The pharmaceutical product is a mix of two
enantiomorphs , R (+)-carvedilol and S (–)-carvedilol, with differing metabolic properties. R(+)-Carvedilol undergoes preferential selection for metabolism, which results in a fractional half-life of about 5 to 9 hours, compared with 7 to 11 hours for the S(-)-carvedilol fraction.
[23]
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Further reading
External links
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Carvedilol .
β , non-selective
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Tryptamines (e.g.,
5-BT ,
5-CT ,
5-Et-DMT ,
5-MT ,
5-(nonyloxy)tryptamine ,
DMT )
5-HT1E
5-HT1F
5-HT2
5-HT2A
Agonists: 25H/NB series (e.g.,
25I-NBF ,
25I-NBMD ,
25I-NBOH ,
25I-NBOMe ,
25B-NBOMe ,
25C-NBOMe ,
25TFM-NBOMe ,
2CBCB-NBOMe ,
25CN-NBOH ,
2CBFly-NBOMe )
2Cs (e.g.,
2C-B ,
2C-E ,
2C-I ,
2C-T-2 ,
2C-T-7 ,
2C-T-21 )
2C-B-FLY
2CB-Ind
5-Methoxytryptamines (
5-MeO-DET ,
5-MeO-DiPT ,
5-MeO-DMT ,
5-MeO-DPT ,
5-MT )
α-Alkyltryptamines (e.g.,
5-Cl-αMT ,
5-Fl-αMT ,
5-MeO-αET ,
5-MeO-αMT ,
α-Me-5-HT ,
αET ,
αMT )
AL-34662
AL-37350A
Bromo-DragonFLY
Dimemebfe
DMBMPP
DOx (e.g.,
DOB ,
DOC ,
DOI ,
DOM )
Efavirenz
Ergolines (e.g.,
1P-LSD ,
ALD-52 ,
bromocriptine ,
cabergoline ,
ergine (LSA) ,
ergometrine (ergonovine) ,
ergotamine ,
lisuride ,
LA-SS-Az ,
LSB ,
LSD ,
LSD-Pip ,
LSH ,
LSP ,
methylergometrine (methylergonovine) ,
pergolide )
Flumexadol
IHCH-7113
Jimscaline
Lorcaserin
MDxx (e.g.,
MDA (tenamfetamine) ,
MDMA (midomafetamine) ,
MDOH ,
MMDA )
O-4310
Oxaflozane
PHA-57378
PNU-22394
PNU-181731
RH-34
SCHEMBL5334361
Phenethylamines (e.g.,
lophophine ,
mescaline )
Piperazines (e.g.,
BZP ,
quipazine ,
TFMPP )
Serotonin (5-HT)
TCB-2
TFMFly
Tryptamines (e.g.,
5-BT ,
5-CT ,
bufotenin ,
DET ,
DiPT ,
DMT ,
DPT ,
psilocin ,
psilocybin ,
tryptamine )
Antagonists:
5-I-R91150
5-MeO-NBpBrT
AC-90179
Adatanserin
Altanserin
Antihistamines (e.g.,
cyproheptadine ,
hydroxyzine ,
ketotifen ,
perlapine )
AMDA
Atypical antipsychotics (e.g.,
amperozide ,
aripiprazole ,
asenapine ,
blonanserin ,
brexpiprazole ,
carpipramine ,
clocapramine ,
clorotepine ,
clozapine ,
fluperlapine ,
gevotroline ,
iloperidone ,
lurasidone ,
melperone ,
mosapramine ,
ocaperidone ,
olanzapine ,
paliperidone ,
quetiapine ,
risperidone ,
sertindole ,
zicronapine ,
ziprasidone ,
zotepine )
Chlorprothixene
Cinanserin
CSP-2503
Deramciclane
Dotarizine
Eplivanserin
Ergolines (e.g.,
amesergide ,
LY-53857 ,
LY-215,840 ,
mesulergine ,
metergoline ,
methysergide ,
sergolexole )
Fananserin
Flibanserin
Glemanserin
Irindalone
Ketanserin
KML-010
Landipirdine
LY-393558
mCPP
Medifoxamine
Metitepine (methiothepin)
MIN-117 (WF-516)
Naftidrofuryl
Nantenine
Nelotanserin
Opiranserin (VVZ-149)
Pelanserin
Phenoxybenzamine
Pimavanserin
Pirenperone
Pizotifen
Pruvanserin
Rauwolscine
Ritanserin
Roluperidone
S-14671
Sarpogrelate
Serotonin antagonists and reuptake inhibitors (e.g.,
etoperidone ,
hydroxynefazodone ,
lubazodone ,
mepiprazole ,
nefazodone ,
triazoledione ,
trazodone )
SR-46349B
TGBA01AD
Teniloxazine
Temanogrel
Tetracyclic antidepressants (e.g.,
amoxapine ,
aptazapine ,
esmirtazapine ,
maprotiline ,
mianserin ,
mirtazapine )
Tricyclic antidepressants (e.g.,
amitriptyline )
Typical antipsychotics (e.g.,
chlorpromazine ,
fluphenazine ,
haloperidol ,
loxapine ,
perphenazine ,
pimozide ,
pipamperone ,
prochlorperazine ,
setoperone ,
spiperone ,
spiramide ,
thioridazine ,
thiothixene ,
trifluoperazine )
Volinanserin
Xylamidine
Yohimbine
5-HT2B
Agonists:
4-Methylaminorex
Aminorex
Amphetamines (e.g.,
chlorphentermine ,
cloforex ,
dexfenfluramine ,
fenfluramine ,
levofenfluramine ,
norfenfluramine )
BW-723C86
DOx (e.g.,
DOB ,
DOC ,
DOI ,
DOM )
Ergolines (e.g.,
cabergoline ,
dihydroergocryptine ,
dihydroergotamine ,
ergotamine ,
methylergometrine (methylergonovine) ,
methysergide ,
pergolide )
Lorcaserin
MDxx (e.g.,
MDA (tenamfetamine) ,
MDMA (midomafetamine) ,
MDOH ,
MMDA )
Piperazines (e.g.,
TFMPP )
PNU-22394
Ro60-0175
Serotonin (5-HT)
Tryptamines (e.g.,
5-BT ,
5-CT ,
5-MT ,
α-Me-5-HT ,
bufotenin ,
DET ,
DiPT ,
DMT ,
DPT ,
psilocin ,
psilocybin ,
tryptamine )
Antagonists:
Agomelatine
Atypical antipsychotics (e.g.,
amisulpride ,
aripiprazole ,
asenapine ,
brexpiprazole ,
cariprazine ,
clozapine ,
N-desalkylquetiapine (norquetiapine) ,
N-desmethylclozapine (norclozapine) ,
olanzapine ,
pipamperone ,
quetiapine ,
risperidone ,
ziprasidone )
Cyproheptadine
EGIS-7625
Ergolines (e.g.,
amesergide ,
bromocriptine ,
lisuride ,
LY-53857 ,
LY-272015 ,
mesulergine )
Ketanserin
LY-393558
mCPP
Metadoxine
Metitepine (methiothepin)
Pirenperone
Pizotifen
Propranolol
PRX-08066
Rauwolscine
Ritanserin
RS-127445
Sarpogrelate
SB-200646
SB-204741
SB-206553
SB-215505
SB-221284
SB-228357
SDZ SER-082
Tegaserod
Tetracyclic antidepressants (e.g.,
amoxapine ,
mianserin ,
mirtazapine )
Trazodone
Typical antipsychotics (e.g.,
chlorpromazine )
TIK-301
Yohimbine
5-HT2C
Agonists:
2Cs (e.g.,
2C-B ,
2C-E ,
2C-I ,
2C-T-2 ,
2C-T-7 ,
2C-T-21 )
5-Methoxytryptamines (
5-MeO-DET ,
5-MeO-DiPT ,
5-MeO-DMT ,
5-MeO-DPT ,
5-MT )
α-Alkyltryptamines (e.g.,
5-Cl-αMT ,
5-Fl-αMT ,
5-MeO-αET ,
5-MeO-αMT ,
α-Me-5-HT ,
αET ,
αMT )
A-372159
AL-38022A
Alstonine
CP-809101
Dimemebfe
DOx (e.g.,
DOB ,
DOC ,
DOI ,
DOM )
Ergolines (e.g.,
ALD-52 ,
cabergoline ,
dihydroergotamine ,
ergine (LSA) ,
ergotamine ,
lisuride ,
LA-SS-Az ,
LSB ,
LSD ,
LSD-Pip ,
LSH ,
LSP ,
pergolide )
Flumexadol
Lorcaserin
MDxx (e.g.,
MDA (tenamfetamine) ,
MDMA (midomafetamine) ,
MDOH ,
MMDA )
MK-212
ORG-12962
ORG-37684
Oxaflozane
PHA-57378
Phenethylamines (e.g.,
lophophine ,
mescaline )
Piperazines (e.g.,
aripiprazole ,
BZP ,
mCPP ,
quipazine ,
TFMPP )
PNU-22394
PNU-181731
Ro60-0175
Ro60-0213
Serotonin (5-HT)
Tryptamines (e.g.,
5-BT ,
5-CT ,
bufotenin ,
DET ,
DiPT ,
DMT ,
DPT ,
psilocin ,
psilocybin ,
tryptamine )
Vabicaserin
WAY-629
WAY-161503
YM-348
Antagonists:
Adatanserin
Agomelatine
Atypical antipsychotics (e.g.,
asenapine ,
clorotepine ,
clozapine ,
fluperlapine ,
iloperidone ,
melperone ,
olanzapine ,
paliperidone ,
quetiapine ,
risperidone ,
sertindole ,
ziprasidone ,
zotepine )
Captodiame
CEPC
Cinanserin
Cyproheptadine
Deramciclane
Desmetramadol
Dotarizine
Eltoprazine
Ergolines (e.g.,
amesergide ,
bromocriptine ,
LY-53857 ,
LY-215,840 ,
mesulergine ,
metergoline ,
methysergide ,
sergolexole )
Etoperidone
Fluoxetine
FR-260010
Irindalone
Ketanserin
Ketotifen
Latrepirdine (dimebolin)
Medifoxamine
Metitepine (methiothepin)
Nefazodone
Pirenperone
Pizotifen
Propranolol
Ritanserin
RS-102221
S-14671
SB-200646
SB-206553
SB-221284
SB-228357
SB-242084
SB-243213
SDZ SER-082
Tedatioxetine
Tetracyclic antidepressants (e.g.,
amoxapine ,
aptazapine ,
esmirtazapine ,
maprotiline ,
mianserin ,
mirtazapine )
TIK-301
Tramadol
Trazodone
Tricyclic antidepressants (e.g.,
amitriptyline ,
nortriptyline )
Typical antipsychotics (e.g.,
chlorpromazine ,
loxapine ,
pimozide ,
pipamperone ,
thioridazine )
Xylamidine
5-HT3 –
7
5-HT3
Agonists:
Alcohols (e.g.,
butanol ,
ethanol (alcohol) ,
trichloroethanol )
m-CPBG
Phenylbiguanide
Piperazines (e.g.,
BZP ,
mCPP ,
quipazine )
RS-56812
Serotonin (5-HT)
SR-57227
SR-57227A
Tryptamines (e.g.,
2-Me-5-HT ,
5-CT ,
bufotenidine (5-HTQ) )
Volatiles/gases (e.g.,
halothane ,
isoflurane ,
toluene ,
trichloroethane )
YM-31636
Antagonists:
Alosetron
Anpirtoline
Arazasetron
AS-8112
Atypical antipsychotics (e.g.,
clozapine ,
olanzapine ,
quetiapine )
Azasetron
Batanopride
Bemesetron (MDL-72222)
Bupropion
Cilansetron
CSP-2503
Dazopride
Dolasetron
Galanolactone
Granisetron
Hydroxybupropion
Lerisetron
Memantine
Ondansetron
Palonosetron
Ramosetron
Renzapride
Ricasetron
Tedatioxetine
Tetracyclic antidepressants (e.g.,
amoxapine ,
mianserin ,
mirtazapine )
Thujone
Tropanserin
Tropisetron
Typical antipsychotics (e.g.,
loxapine )
Volatiles/gases (e.g.,
nitrous oxide ,
sevoflurane ,
xenon )
Vortioxetine
Zacopride
Zatosetron
5-HT4
5-HT5A
5-HT6
Agonists:
Ergolines (e.g.,
dihydroergocryptine ,
dihydroergotamine ,
ergotamine ,
lisuride ,
LSD ,
mesulergine ,
metergoline ,
methysergide )
Hypidone
Serotonin (5-HT)
Tryptamines (e.g.,
2-Me-5-HT ,
5-BT ,
5-CT ,
5-MT ,
Bufotenin ,
E-6801 ,
E-6837 ,
EMD-386088 ,
EMDT ,
LY-586713 ,
N-Me-5-HT ,
ST-1936 ,
tryptamine )
WAY-181187
WAY-208466
Antagonists:
ABT-354
Atypical antipsychotics (e.g.,
aripiprazole ,
asenapine ,
clorotepine ,
clozapine ,
fluperlapine ,
iloperidone ,
olanzapine ,
tiospirone )
AVN-101
AVN-211
AVN-322
AVN-397
BGC20-760
BVT-5182
BVT-74316
Cerlapirdine
EGIS-12,233
GW-742457
Idalopirdine
Ketanserin
Landipirdine
Latrepirdine (dimebolin)
Masupirdine
Metitepine (methiothepin)
MS-245
PRX-07034
Ritanserin
Ro 04-6790
Ro 63-0563
SB-258585
SB-271046
SB-357134
SB-399885
SB-742457
Tetracyclic antidepressants (e.g.,
amoxapine ,
mianserin )
Tricyclic antidepressants (e.g.,
amitriptyline ,
clomipramine ,
doxepin ,
nortriptyline )
Typical antipsychotics (e.g.,
chlorpromazine ,
loxapine )
5-HT7
Antagonists:
Atypical antipsychotics (e.g.,
amisulpride ,
aripiprazole ,
asenapine ,
brexpiprazole ,
clorotepine ,
clozapine ,
fluperlapine ,
olanzapine ,
risperidone ,
sertindole ,
tiospirone ,
ziprasidone ,
zotepine )
Butaclamol
DR-4485
EGIS-12,233
Ergolines (e.g.,
2-Br-LSD (BOL-148) ,
amesergide ,
bromocriptine ,
cabergoline ,
dihydroergotamine ,
ergotamine ,
LY-53857 ,
LY-215,840 ,
mesulergine ,
metergoline ,
methysergide ,
sergolexole )
JNJ-18038683
Ketanserin
LY-215,840
Metitepine (methiothepin)
Ritanserin
SB-258719
SB-258741
SB-269970
SB-656104
SB-656104A
SB-691673
SLV-313
SLV-314
Spiperone
SSR-181507
Tetracyclic antidepressants (e.g.,
amoxapine ,
maprotiline ,
mianserin ,
mirtazapine )
Tricyclic antidepressants (e.g.,
amitriptyline ,
clomipramine ,
imipramine )
Typical antipsychotics (e.g.,
acetophenazine ,
chlorpromazine ,
chlorprothixene ,
fluphenazine ,
loxapine ,
pimozide )
Vortioxetine
CAR Tooltip Constitutive androstane receptor
PXR Tooltip Pregnane X receptor
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