Pharmacokinetics of carvedilol after intravenous and oral administration in conscious healthy dogs

Arsenault, Wendy G.; Boothe, Dawn M.; Gordon, Sonya G.; Miller, Matthew W.; Chalkley, Jeffrey R.; Petrikovics, Ilona

doi:10.2460/ajvr.2005.66.2172

Cited by 20 publications

(14 citation statements)

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“…Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential (von Mollendorff et al, 1987;Morgan, 1994;Hokama et al, 1999;Arsenault et al, 2005). This renders the drug unsuitable for traditional methods of bioavailability enhancement like micronization, solid dispersions using hydrophilic carriers and block-copolymers, complexation with water-soluble carrier(s), etc.…”

Section: Original Articlementioning

confidence: 99%

Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential

Khurana²,

et al. 2011

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Section: Original Articlementioning

confidence: 99%

Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential

Khurana²,

et al. 2011

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“…The maximum concentration for vasodilators commonly prescribed for cardiac disorders, such as enalapril [7], carvedilol [1] and furosemide [4] occur within 1 to 1.5 hr after oral administration. Therefore, these drugs may induce excessive decline in BP when they are taken with food and may cause similar symptoms as postprandial hypotension in humans.…”

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confidence: 99%

Effect of Diet on the Cardiovascular System in Healthy Beagles

Nakagawa

Miyagawa

Takemura

et al. 2010

The Journal of Veterinary Medical Science

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ABSTRACT. In management of canine cardiac disorders, cardiac drugs are commonly administered with food, although the cardiovascular effects of feeding and frequency of feeding are unknown. This study investigated the cardiovascular effect of feeding and frequency of feeding using a telemetry monitoring system in unanesthetized and unrestrained dogs. Systolic and diastolic blood pressure, heart rate and double product were steeply elevated during the five minutes immediately before feeding. They showed a sharp fall within 60 min after feeding time, especially the systolic and diastolic blood pressure, which showed lower values than from before feeding time. There were no significant differences in the means of preprandial elevation, postprandial fall or 24-hr averages in the once-and twice-daily feeding periods.KEY WORDS: blood pressure, canine, cardiovascular effect, feeding, telemetry system. J. Vet. Med. Sci. 72(5): 615-619, 2010 Cardiovascular disorders are common in elderly dogs, one-third of which have been shown to suffer from valvular heart disease [2]. Vasodilators such as angiotensin-converting enzyme inhibitors, beta-blockers and diuretics are commonly prescribed in this situation [2], and these drugs are usually administered with food for the sake of convenience. Some studies [5,12,13] that have used telemetry systems to track systolic blood pressure (SBP) and diastolic blood pressure (DBP) in dogs have suggested that feeding regimens affect canine variations of blood pressure (BP) and heart rate (HR). Household dogs are generally fed once or twice a day, depending on the lifestyle of the owner, and the precise cardiovascular effects of various times of feeding are not known. The purpose of this study was to examine the influence of feeding and times of feeding on the variation of BP, HR and double product (DP), a parameter of oxygen consumption, in healthy Beagles.Animals: Three healthy female Beagles (mean age of 7.3  4.6 years; mean weight of 9.1  0.3 kg) were used in this study. Based on the results of a physical examination, complete blood count and serum chemistry, the dogs were confirmed to be healthy. They were acclimated for 10 weeks under experimental conditions at the Laboratory of Veterinary Internal Medicine, School of Veterinary Medicine, Nippon Veterinary and Life Science University.Feeding time: Food (Hill's Science Diet Canine Maintenance) was given at 15:00 in the once-daily feeding group and at 9:00 and 17:00 in the twice-daily feeding group. Water was given ad libitum.Experimental environment: The dogs were housed in individual stainless steel cages measuring 710 (W)  1,095 (D)  795 (H) mm. The cages were placed under environment conditions similar to those for household animals; human entry to the room was unlimited from 7:00-24:00, and neither the room temperature nor the lighting cycle was controlled.Procedures: This experiment was carried out in a crossover design. Placement of a BP telemetry system (Data Science International, New Brighton, MN, U.S.A.) and collection o...

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“…This in vivo data supported our initial plan to evaluate the effect of a single concentration of propranolol or carvedilol prior to a single dose of radiation; but it is important to note that clinically, chronic drug administration or altered route of administration (IV vs oral) and fractionated radiation may alter tumour response. For example, carvedilol exhibits poor oral bioavailability in dogs but its intravenous administration can result in a peak plasma concentration of 476 μg/L (1.17 μM) with a range up to 1900 μg/L (4.66 μM) with longer half‐life, suggesting that higher concentrations may be clinically achievable with intravenous carvedilol …”

Section: Discussionmentioning

confidence: 99%

The adrenergic receptor antagonists propranolol and carvedilol decrease bone sarcoma cell viability and sustained carvedilol reduces clonogenic survival and increases radiosensitivity in canine osteosarcoma cells

Duckett

Phung

Linh-Trung

et al. 2019

Vet Comparative Oncology

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Adrenergic receptor (AR) expression has been demonstrated at several sites of primary and metastatic tumour growth and may influence proliferation, survival, metastasis and angiogenesis. AR antagonists like propranolol and carvedilol inhibit proliferation, induce apoptosis and synergize with chemotherapy agents in some cancers. Radiation resistance is mediated in many cells by upregulation of pro‐survival pathways, which may be influenced by ARs. Studies evaluating AR antagonists combined with radiation are limited. The purpose of this study was to determine the effect of propranolol and carvedilol on viability and radiosensitivity in sarcoma cell lines. The hypothesis was that propranolol and carvedilol would increase radiosensitivity in four primary bone sarcoma cell lines. Single agent propranolol or carvedilol inhibited cell viability in all cell lines in a concentration‐dependent manner. The mean inhibitory concentrations (IC50) for carvedilol were approximately 4‐fold lower than propranolol and may be clinically relevant in vivo. Immunoblot analysis confirmed AR expression in both human and canine sarcoma cell lines; however, there was no correlation between baseline AR protein expression and radiosensitivity. Short duration treatment with carvedilol and propranolol did not significantly affect clonogenic survival. Prolonged exposure to propranolol and carvedilol significantly decreased the surviving fraction of canine osteosarcoma cells after 3Gy radiation. Based on our results and possible in vivo activity in dogs, further studies investigating the effects of carvedilol on sarcoma are warranted.

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Pharmacokinetics of carvedilol after intravenous and oral administration in conscious healthy dogs

Abstract: Although results suggested a 3-hour dosing interval on the basis of MRT, pharmacodynamic studies investigating the duration of beta-adrenoreceptor blockade provide a more accurate basis for determining the dosing interval of carvedilol.

Cited by 20 publications

References 10 publications

Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential

Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential

Effect of Diet on the Cardiovascular System in Healthy Beagles

The adrenergic receptor antagonists propranolol and carvedilol decrease bone sarcoma cell viability and sustained carvedilol reduces clonogenic survival and increases radiosensitivity in canine osteosarcoma cells

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