Pharmacokinetic Drug Interaction between Carvedilol and Ticlopidine in Rats

Choi, Dong‐Hyun

doi:10.4062/biomolther.2010.18.3.343

Cited by 5 publications

(4 citation statements)

References 25 publications

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“…of carvedilol in the presence of glipizide was significantly increased by 36.8%. These results were consistent with report by Choi and Choi (2010), in which ticlopidine significantly increased the AUC and C max of carvedilol, a substrate for CYP2C9.…”

Section: Discussionsupporting

confidence: 93%

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Effects of Glipizide on the Pharmacokinetics of Carvedilol after Oral and Intravenous Administration in Rats

Lee¹,

Choi

2011

Biomolecules and Therapeutics

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Abstractscavenges free radicals of oxygen (Feuerstein et al., 1997). It is used to treat systemic arterial hypertension (Cournot et al., 1992;Lund-Johansen et al., 1992) and congestive heart failure (DasGupta et al., 1991) and is purported to improve exercise capacity (Cleland et al., 1996;Hampton, 1996) and longevity in humans .Carvedilol is well absorbed from the gastrointestinal tract, but is subject to considerable fi rst-pass metabolism in the intestinal and/or liver (McTavish et al., 1993;Morgan, 1994). Carvedilol is more than 98% bound to plasma proteins. Carvedilol is metabolized by both oxidation and conjugation pathways in the liver into some metabolites (Neugebauer et al., 1987;Neugebauer and Neubert, 1991). The oxidation pathways are mainly catalyzed by CYP2C9 enzymes in human (McTavish et al., 1993;Morgan, 1994;Oldham and Clarke, 1997), and then CYP2D6 is responsible for the formation of 4'-hydroxy carvedilol and 5'-hydroxy carvedilol, and both metabolites are excreted into urine (Neugebauer and Neubert, 1991). Since carvedilol is a substrate of both CYP2C9 en-

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Section: Discussionsupporting

confidence: 93%

“…These results were consistent with report by Choi and Choi (2010), in which ticlopidine did not signifi cantly change the pharmacokinetic parameters of intravenous administration of carvedilol.…”

Section: Discussionsupporting

confidence: 93%

Effects of Glipizide on the Pharmacokinetics of Carvedilol after Oral and Intravenous Administration in Rats

Lee¹,

Choi

2011

Biomolecules and Therapeutics

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“…These results were consistent with the results of previous reports indicating other CYP450 inhibitors, including ketoconazole [20], cilostazol [21], glipizide [22], and ticlopidine [23], which increased the plasma levels of carvedilol in rats to a similar extent as that of bupropion.…”

Section: Discussionsupporting

confidence: 82%

The Pharmacokinetic Interaction Study between Carvedilol and Bupropion in Rats

Abrudan

Gheldiu²,

Neag³

et al. 2017

Pharmacology

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Background/Aims: The effects of multiple-dose bupropion on the pharmacokinetics of single-dose carvedilol were investigated in order to evaluate this possible drug-drug interaction. Methods: A preclinical study was conducted among white male Wistar rats. Each rat was cannulated on the femoral vein prior to being connected to BASi Culex ABC®. During the reference period, each rat received an intravenous and an oral dose of 3.57 mg/kg body weight (b.w.) carvedilol, at 2 days distance. After 5 days of pretreatment with 21.42 mg/kg b.w. bupropion (by oral route, twice a day - given in order to reach the steady state), during the sixth day, 3.57 mg/kg b.w. carvedilol and 21.42 mg/kg b.w. bupropion were orally co-administrated (test period). After each administration of carvedilol, several samples of 200 µL blood were collected. The pharmacokinetic parameters of carvedilol were analyzed by the noncompartmental method. Results: The 5 days pretreatment with bupropion increased the exposure to carvedilol in rats by 180%, considering the modifications observed in the area under the curve of carvedilol. Carvedilol was shown to have higher plasma concentrations, delay in maximum concentration, and a prolonged half-life, after being pretreated with bupropion. Conclusion: The administration of multiple-dose bupropion influences the pharmacokinetics of carvedilol (single oral dose) in rats.

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“…As the effect of the drugs is similar under equivalent concentrations, it could be inferred that the pharmacokinetics accounts for different antioxidative effects. The reported blood half-life for Car ranges from 7 to 10 h 44,45 and that for Ato is 14 h. 46 The shorter blood circulation time of Car leads to lower bioavailability and less therapeutic effect. Although Res reported an even shorter half-life of only 8−14 min, 47 it still showed strong antioxidant efficacy.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

Real-Time Visualization of the Antioxidative Potency of Drugs for the Prevention of Myocardium Ischemia-Reperfusion Injury by a NIR Fluorescent Nanoprobe

et al. 2022

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The burst of the reactive oxygen species (ROS) is the culprit of myocardial ischemia-reperfusion injury. As direct ROS scavengers, antioxidants are clinically documented drugs for the prevention of reperfusion injury. However, some drugs give disappointing therapeutic performance despite their good in vitro effects. Therefore, in vivo assessments are necessary to screen the antioxidants before clinical trials. However, traditional methods such as histological study require invasive and complicated preprocessing of the biological samples, which may fail to reflect the actual level of the unstable ROS with a very short lifetime. Peroxynitrite (ONOO − ) is a characteristic endogenous ROS produced during reperfusion. Here, we modified the ONOO − -responsive near-infrared fluorescent probe on a myocardium-targeting silica cross-linked micelle to prepare a nanoprobe for the real-time monitoring of ONOO − during coronary reperfusion. A ROS-stable cyanine dye was co-labeled as an internal reference to achieve ratiometric sensing. The nanoprobe can passively target the infarcted myocardium and monitor the generation of ONOO − during reperfusion in real-time. The antioxidants, carvedilol, atorvastatin, and resveratrol, were used as model drugs to demonstrate the capability of the nanoprobe to evaluate the antioxidative potency in situ. The drugs were either loaded and delivered by the nanoprobe to compare their in vivo efficacy under similar concentrations or administered intraperitoneally as a free drug to take their pharmacokinetics into account. The imaging results revealed that pharmacokinetics might be the determinant factor that influences the efficacy of the antioxidants.

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Pharmacokinetic Drug Interaction between Carvedilol and Ticlopidine in Rats

Cited by 5 publications

References 25 publications

Effects of Glipizide on the Pharmacokinetics of Carvedilol after Oral and Intravenous Administration in Rats

Effects of Glipizide on the Pharmacokinetics of Carvedilol after Oral and Intravenous Administration in Rats

The Pharmacokinetic Interaction Study between Carvedilol and Bupropion in Rats

Real-Time Visualization of the Antioxidative Potency of Drugs for the Prevention of Myocardium Ischemia-Reperfusion Injury by a NIR Fluorescent Nanoprobe

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