The bioequivalence of a single intravenous administration of the anesthetic alfaxalone in cyclodextrin versus alfaxalone in cyclodextrin plus preservatives in cats

Pasloske, Kirby; Ranasinghe, M. G.; Sauer, Susanne K.; Hare, Jonathan

doi:10.1111/jvp.12485

Cited by 7 publications

(5 citation statements)

References 6 publications

(7 reference statements)

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“…In this study, blood pharmacokinetic parameters were calculated using the non-compartmental analysis model 200 (intravenous or extravascular dosing, linear/log trapezoidal method) in the WinNonlin™ software (version 8.1; Certara USA) and WinNonlin 8.1 was used for bioequivalence analysis. Analysis of variance (ANOVA) was used to calculate a 90% CI for the ratio of the two treatments ( 24 , 25 ).…”

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics and bioequivalence of two cyclosporine oral solution formulations in cats

et al. 2022

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The pharmacokinetic profiles and bioequivalence of two cyclosporine oral solutions were investigated in cats. Twenty-four cats were randomly allocated to two equally sized treatment groups in a randomized four-cycle, and dual-sequence cross-over design. Test and reference articles were orally administered in a single dose of 7 mg/kg Bodyweight. Serial blood samples were collected, and blood cyclosporine concentration was determined by ultra-performance liquid chromatography-mass spectrometry (UPLC-MS/MS). No significant differences were present in the major pharmacokinetic parameters (Cmax, AUC0−last,) between the two formulations. The blood profiles of cyclosporine following the administration of both formulations were similar. The findings of the study suggested that the two articles were bioequivalent for cyclosporine oral solution.

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Section: Methodsmentioning

confidence: 99%

Pharmacokinetics and bioequivalence of two cyclosporine oral solution formulations in cats

et al. 2022

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“…The anesthetic properties of alfaxalone have been known since 1971, but due to adverse reactions it was withdrawn from the market, after which it returned in 2001 in a new formulation. In the new presentation, it was complexed with HP-β-CD aiming to increase solubility and bioavailability [ 85 , 86 , 87 , 88 ].…”

Section: Other Inclusion Complexes Used In Veterinary Therapymentioning

confidence: 99%

Short Review on the Biological Activity of Cyclodextrin-Drug Inclusion Complexes Applicable in Veterinary Therapy

et al. 2023

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Cyclodextrins (CDs) are a family of carrier molecules used to improve the pharmacokinetic parameters of therapeutic molecules. These cyclic oligosaccharides have medical and pharmaceutical applications by being able to form inclusion complexes with molecules that are poorly soluble in water. The benefits of these complexes are directed towards improving the chemical and biological properties—i.e., solubility, bioavailability, stability, non-toxicity and shelf life of drug molecules. Since the 1960s, the first inclusion complexes used in therapeutics were those with α-, β- and γ-CD, which proved their usefulness, but had certain degrees of particularly renal toxicity. Currently, to correct these deficiencies, β-CD derivatives are most frequently used, such as sulfobutylether-β-CD, hydroxypropyl-β-CD, etc. Therefore, it is of interest to bring to the attention of those interested the diversity of current and potential future clinical applications of inclusion complexes in veterinary medicine and to present the contribution of these inclusion complexes in improving drug efficacy. The most important biological activities of β-CD complexed molecules in the veterinary field are summarized in this short review.

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“…Alfaxalone is a synthetic neuroactive steroid which interacts with the yaminobutyric acid (GABA) receptors of the central nervous system, producing anesthesia and muscle relaxation [6]. When comparing their effects, propofol is associated with decreases in heart rate and mean arterial pressure, and also promote respiratory depression [7]; alfaxalone does not accumulate in tissues after repeated doses due to its rapid metabolism and clearance [7], and also has been reported that cardiovascular and respiratory parameters remained remarkably stable during general anesthesia [8].…”

Section: Introductionmentioning

confidence: 99%

Comparison of Propofol and Alfaxalone as Anesthesic Drugs in Bitches Undergoing Ovariohysterectomies (Health Bitches and with Pyometra) and Cesarean Sections

Rodríguez-Trujillo,

Batista-Arteaga,

Iusupova

et al. 2024

Preprint

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This study compared the efficacy of alfaxalone and propofol to induce anesthesia in bitches undergoing an ovariohysterectomy or cesarean sections. 34 healthy and pyometra-affected females were induced with IV propofol administration, 35 healthy and pyometra-affected bitches were induced with the IV administration of alfaxalone. For the cesarean sections, females were induced with propofol (n=14) or alfaxalone (n=14). Maternal physiological parameters (heart rate, blood pressure, temperature) were recorded throughout surgeries; the viability and a modified Apgar score was recorded in the neonates at 5, 60 and 120 minutes after delivery. The use of propofol and alfaxalone did not show relevant differences over parameters assessed, when ovariohysterectomy was performed in healthy bitches or females with pyometra, as well as when cesarean sections were compared; only, a transient tachycardia appeared after alfaxalone administration. However, a higher percentage of bitches needed extra-doses of propofol. Neonatal mortality was similar between both groups, but when alfaxalone was used a higher neonatal viability was observed. Propofol and alfaxalone showed similar efficacy to perform the ovariohysterectomy in all bitches. Both protocols were optimal for cesarean sections, but alfaxalone was associated with a higher neonatal viability and a higher neonatal survival rate.

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The bioequivalence of a single intravenous administration of the anesthetic alfaxalone in cyclodextrin versus alfaxalone in cyclodextrin plus preservatives in cats

Cited by 7 publications

References 6 publications

Pharmacokinetics and bioequivalence of two cyclosporine oral solution formulations in cats

Pharmacokinetics and bioequivalence of two cyclosporine oral solution formulations in cats

Short Review on the Biological Activity of Cyclodextrin-Drug Inclusion Complexes Applicable in Veterinary Therapy

Comparison of Propofol and Alfaxalone as Anesthesic Drugs in Bitches Undergoing Ovariohysterectomies (Health Bitches and with Pyometra) and Cesarean Sections

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