|
|
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result sql = Comparison of the pharmacokinetic properties of bisoprolol and carvedilol in healthy dogs.
Comparison of the pharmacokinetic properties of bisoprolol and carvedilol in healthy dogs.char = <;code = 60
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char = s;code = 115
char = s;code = 115
char = e;code = 101
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char = <;code = 60
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char = r;code = 114
char = /;code = 47
char = >;code = 62
char = <;code = 60
char = b;code = 98
char = >;code = 62
char = R;code = 82
char = E;code = 69
char = S;code = 83
char = U;code = 85
char = L;code = 76
char = T;code = 84
char = S;code = 83
char = ;code = 32
char = :;code = 58
char = ;code = 32
char = <;code = 60
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char = b;code = 98
char = >;code = 62
char = A;code = 65
char = f;code = 102
char = t;code = 116
char = e;code = 101
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char = a;code = 97
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char = a;code = 97
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char = m;code = 109
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char = a;code = 97
char = t;code = 116
char = i;code = 105
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char = b;code = 98
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char = p;code = 112
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char = o;code = 111
char = l;code = 108
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char = t;code = 116
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char = g;code = 103
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char = t;code = 116
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char = c;code = 99
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char = a;code = 97
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char = u;code = 117
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char = o;code = 111
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char = a;code = 97
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char = e;code = 101
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char = t;code = 116
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char = e;code = 101
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char = c;code = 99
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char = a;code = 97
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char = c;code = 99
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char = e;code = 101
char = x;code = 120
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char = a;code = 97
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char = e;code = 101
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char = t;code = 116
char = o;code = 111
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char = i;code = 105
char = n;code = 110
char = f;code = 102
char = i;code = 105
char = n;code = 110
char = i;code = 105
char = t;code = 116
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char = A;code = 65
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char = C;code = 67
char = i;code = 105
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char = 2;code = 50
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char = L;code = 76
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char = c;code = 99
char = o;code = 111
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char = f;code = 102
char = i;code = 105
char = c;code = 99
char = i;code = 105
char = e;code = 101
char = n;code = 110
char = t;code = 116
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char = o;code = 111
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char = v;code = 118
char = a;code = 97
char = r;code = 114
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char = a;code = 97
char = t;code = 116
char = i;code = 105
char = o;code = 111
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char = [;code = 91
char = C;code = 67
char = V;code = 86
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char = ,;code = 44
char = ;code = 32
char = 1;code = 49
char = 5;code = 53
char = %;code = 37
char = );code = 41
char = .;code = 46
char = ;code = 32
char = A;code = 65
char = f;code = 102
char = t;code = 116
char = e;code = 101
char = r;code = 114
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char = I;code = 73
char = V;code = 86
char = ;code = 32
char = a;code = 97
char = d;code = 100
char = m;code = 109
char = i;code = 105
char = n;code = 110
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char = s;code = 115
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char = r;code = 114
char = a;code = 97
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char = i;code = 105
char = o;code = 111
char = n;code = 110
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char = o;code = 111
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char = ;code = 32
char = b;code = 98
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char = s;code = 115
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char = o;code = 111
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char = ,;code = 44
char = ;code = 32
char = t;code = 116
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char = e;code = 101
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char = s;code = 115
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char = m;code = 109
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char = a;code = 97
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char = 0;code = 48
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char = m;code = 109
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char = c;code = 99
char = r;code = 114
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char = L;code = 76
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char = V;code = 86
char = ,;code = 44
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char = 1;code = 49
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char = %;code = 37
char = );code = 41
char = .;code = 46
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char = O;code = 79
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char = a;code = 97
char = l;code = 108
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char = b;code = 98
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char = a;code = 97
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char = a;code = 97
char = b;code = 98
char = i;code = 105
char = l;code = 108
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char = t;code = 116
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char = o;code = 111
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char = a;code = 97
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char = A;code = 65
char = U;code = 85
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char = 7;code = 55
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char = C;code = 67
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char = ,;code = 44
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char = 8;code = 56
char = 1;code = 49
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char = );code = 41
char = .;code = 46
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char = A;code = 65
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char = t;code = 116
char = e;code = 101
char = r;code = 114
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char = ;code = 32
char = a;code = 97
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char = m;code = 109
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char = (;code = 40
char = C;code = 67
char = V;code = 86
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char = ;code = 32
char = 2;code = 50
char = 3;code = 51
char = %;code = 37
char = );code = 41
char = .;code = 46
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char = O;code = 79
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char = a;code = 97
char = l;code = 108
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char = b;code = 98
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char = a;code = 97
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char = a;code = 97
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char = 1;code = 49
char = 4;code = 52
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char = .;code = 46
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char = T;code = 84
char = o;code = 111
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char = a;code = 97
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char = <;code = 60
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char = C;code = 67
char = O;code = 79
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char = C;code = 67
char = L;code = 76
char = U;code = 85
char = S;code = 83
char = I;code = 73
char = O;code = 79
char = N;code = 78
char = S;code = 83
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char = A;code = 65
char = N;code = 78
char = D;code = 68
char = ;code = 32
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char = I;code = 73
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char = A;code = 65
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char = R;code = 82
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char = L;code = 76
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char = V;code = 86
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char = N;code = 78
char = C;code = 67
char = E;code = 69
char = ;code = 32
char = :;code = 58
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char = s;code = 115
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char = f;code = 102
char = i;code = 105
char = r;code = 114
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char = t;code = 116
char = -;code = 45
char = p;code = 112
char = a;code = 97
char = s;code = 115
char = s;code = 115
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char = e;code = 101
char = f;code = 102
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result sql = OBJECTIVE : To compare the pharmacokinetic properties and bioavailability following oral and IV administration of bisoprolol, a second-generation beta1-adrenoceptor-selective blocking agent, with those of carvedilol, a third-generation beta1/beta2 and alpha1-adrenoceptor blocking agent, in dogs.
ANIMALS : 12 healthy adult Beagles.
PROCEDURES : A prospective, parallel group study was performed. The dogs were allocated to 1 of 2 groups (6 dogs/group) and were administered orally a 1 mg/kg dose of either bisoprolol or carvedilol. Following a 1-week washout period, each cohort received a 1 mg/kg dose of the same drug IV. Blood samples were collected before and after drug administration, and serum concentrations, pharmacokinetic variables, and bioavailability for each agent were assessed.
RESULTS : After oral administration of bisoprolol, the geometric mean value of the area under the concentration-time curve extrapolated to infinity (AUCinf) was 2,195 microg/L (coefficient of variation [CV], 15%). After IV administration of bisoprolol, the dose-normalized geometric mean AUCinf was 2,402 microg/L (CV, 19%). Oral bioavailability of bisoprolol was 91.4%. After oral administration of carvedilol, the geometric mean AUCinf was 70 microg/L (CV, 81%). After IV administration of carvedilol, the geometric mean AUCinf was 491 microg/L (CV, 23%). Oral bioavailability of carvedilol was 14.3%. Total body clearance was low (0.42 L/h/kg) for bisoprolol and high (2.0 L/h/kg) for carvedilol.
CONCLUSIONS AND CLINICAL RELEVANCE : After oral administration, carvedilol underwent extensive first-pass metabolism and had limited bioavailability; bisoprolol had less first-pass effect and higher bioavailability. Collectively, these differences suggested that, in dogs, bisoprolol has less interindividual pharmacokinetic variability, compared with carvedilol.
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result sql = Comparison of the pharmacokinetic properties of bisoprolol and carvedilol in healthy dogs.
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char = d;code = 100
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char = I;code = 73
char = V;code = 86
char = .;code = 46
char = ;code = 32
char = B;code = 66
char = l;code = 108
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char = a;code = 97
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char = l;code = 108
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char = a;code = 97
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char = s;code = 115
char = e;code = 101
char = s;code = 115
char = s;code = 115
char = e;code = 101
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char = <;code = 60
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char = R;code = 82
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char = S;code = 83
char = U;code = 85
char = L;code = 76
char = T;code = 84
char = S;code = 83
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char = :;code = 58
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result sql = OBJECTIVE : To compare the pharmacokinetic properties and bioavailability following oral and IV administration of bisoprolol, a second-generation beta1-adrenoceptor-selective blocking agent, with those of carvedilol, a third-generation beta1/beta2 and alpha1-adrenoceptor blocking agent, in dogs.
ANIMALS : 12 healthy adult Beagles.
PROCEDURES : A prospective, parallel group study was performed. The dogs were allocated to 1 of 2 groups (6 dogs/group) and were administered orally a 1 mg/kg dose of either bisoprolol or carvedilol. Following a 1-week washout period, each cohort received a 1 mg/kg dose of the same drug IV. Blood samples were collected before and after drug administration, and serum concentrations, pharmacokinetic variables, and bioavailability for each agent were assessed.
RESULTS : After oral administration of bisoprolol, the geometric mean value of the area under the concentration-time curve extrapolated to infinity (AUCinf) was 2,195 microg/L (coefficient of variation [CV], 15%). After IV administration of bisoprolol, the dose-normalized geometric mean AUCinf was 2,402 microg/L (CV, 19%). Oral bioavailability of bisoprolol was 91.4%. After oral administration of carvedilol, the geometric mean AUCinf was 70 microg/L (CV, 81%). After IV administration of carvedilol, the geometric mean AUCinf was 491 microg/L (CV, 23%). Oral bioavailability of carvedilol was 14.3%. Total body clearance was low (0.42 L/h/kg) for bisoprolol and high (2.0 L/h/kg) for carvedilol.
CONCLUSIONS AND CLINICAL RELEVANCE : After oral administration, carvedilol underwent extensive first-pass metabolism and had limited bioavailability; bisoprolol had less first-pass effect and higher bioavailability. Collectively, these differences suggested that, in dogs, bisoprolol has less interindividual pharmacokinetic variability, compared with carvedilol.
Publication: Am. J. Vet. Res. 2008 Dec ;69(12)::1659-63. :doi: 10.2460/ajvr.69.12.1659.
Publication Date: 2008 Dec
Study Author(s): Beddies, Gerald;Fox, Philip R;Papich, Mark D;Kanikanti, Venkata-Rangaro;Krebber, Ralph;Keene, Bruce W;
Institution: Research & Development-Clinical Research & Development, Animal Health Division, Bayer HealthCare AG, 51368 Leverkusen, Germany.
Shortcut link to this study:
Publication Date: 2008 Dec
Study Author(s): Beddies, Gerald;Fox, Philip R;Papich, Mark D;Kanikanti, Venkata-Rangaro;Krebber, Ralph;Keene, Bruce W;
Institution: Research & Development-Clinical Research & Development, Animal Health Division, Bayer HealthCare AG, 51368 Leverkusen, Germany.
Shortcut link to this study:
OBJECTIVE : To compare the pharmacokinetic properties and bioavailability following oral and IV administration of bisoprolol, a second-generation beta1-adrenoceptor-selective blocking agent, with those of carvedilol, a third-generation beta1/beta2 and alpha1-adrenoceptor blocking agent, in dogs.
ANIMALS : 12 healthy adult Beagles.
PROCEDURES : A prospective, parallel group study was performed. The dogs were allocated to 1 of 2 groups (6 dogs/group) and were administered orally a 1 mg/kg dose of either bisoprolol or carvedilol. Following a 1-week washout period, each cohort received a 1 mg/kg dose of the same drug IV. Blood samples were collected before and after drug administration, and serum concentrations, pharmacokinetic variables, and bioavailability for each agent were assessed.
RESULTS : After oral administration of bisoprolol, the geometric mean value of the area under the concentration-time curve extrapolated to infinity (AUCinf) was 2,195 microg/L (coefficient of variation [CV], 15%). After IV administration of bisoprolol, the dose-normalized geometric mean AUCinf was 2,402 microg/L (CV, 19%). Oral bioavailability of bisoprolol was 91.4%. After oral administration of carvedilol, the geometric mean AUCinf was 70 microg/L (CV, 81%). After IV administration of carvedilol, the geometric mean AUCinf was 491 microg/L (CV, 23%). Oral bioavailability of carvedilol was 14.3%. Total body clearance was low (0.42 L/h/kg) for bisoprolol and high (2.0 L/h/kg) for carvedilol.
CONCLUSIONS AND CLINICAL RELEVANCE : After oral administration, carvedilol underwent extensive first-pass metabolism and had limited bioavailability; bisoprolol had less first-pass effect and higher bioavailability. Collectively, these differences suggested that, in dogs, bisoprolol has less interindividual pharmacokinetic variability, compared with carvedilol.
ANIMALS : 12 healthy adult Beagles.
PROCEDURES : A prospective, parallel group study was performed. The dogs were allocated to 1 of 2 groups (6 dogs/group) and were administered orally a 1 mg/kg dose of either bisoprolol or carvedilol. Following a 1-week washout period, each cohort received a 1 mg/kg dose of the same drug IV. Blood samples were collected before and after drug administration, and serum concentrations, pharmacokinetic variables, and bioavailability for each agent were assessed.
RESULTS : After oral administration of bisoprolol, the geometric mean value of the area under the concentration-time curve extrapolated to infinity (AUCinf) was 2,195 microg/L (coefficient of variation [CV], 15%). After IV administration of bisoprolol, the dose-normalized geometric mean AUCinf was 2,402 microg/L (CV, 19%). Oral bioavailability of bisoprolol was 91.4%. After oral administration of carvedilol, the geometric mean AUCinf was 70 microg/L (CV, 81%). After IV administration of carvedilol, the geometric mean AUCinf was 491 microg/L (CV, 23%). Oral bioavailability of carvedilol was 14.3%. Total body clearance was low (0.42 L/h/kg) for bisoprolol and high (2.0 L/h/kg) for carvedilol.
CONCLUSIONS AND CLINICAL RELEVANCE : After oral administration, carvedilol underwent extensive first-pass metabolism and had limited bioavailability; bisoprolol had less first-pass effect and higher bioavailability. Collectively, these differences suggested that, in dogs, bisoprolol has less interindividual pharmacokinetic variability, compared with carvedilol.
PMID: 19046015
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