Short-term buserelin administration induces apoptosis and morphological changes in adult rat testes

Khadivi, Behnaz; Peirouvi, Tahmineh; JavanmardI, Masumeh Zirak; Rasmi, Yousef

doi:10.1590/s0102-865020170206

Cited by 3 publications

(3 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…However, there are some attempts which can slow-down absorption from delivery site or slow-down enzymatic degradation and elimination to improve the bioavailability, such as sodium glycodeoxycholate, Zn 2+ suspension within the buserelin solution, and cyclodextrin derivatives [ 13 , 14 , 17 ]. Meanwhile some reports hold the view that buserelin administration induces loss of erectile potency, hot flush [ 9 ], uterine bleeding [ 6 ], apoptosis in spermatozoa lineage and inhibits immune system function [ 28 , 29 ], further investigations are required to assess its side effects in practical applications.…”

Section: Discussionmentioning

confidence: 99%

The pharmacokinetics of buserelin after intramuscular administration in pigs and cows

Kong

Liu

et al. 2022

BMC Vet Res

View full text Add to dashboard Cite

Background Buserelin is a luteinizing hormone releasing hormone (LHRH) agonist used for the treatment of hormone-dependent diseases in males and females. However, the pharmacokinetics of buserelin in pigs and cows are not fully understood. This study was designed to develop a sensitive method to determine the concentration of buserelin in blood plasma and to investigate the pharmacokinetic parameters after intramuscular (i.m.) administration in pigs and cows. Results A sensitive and rapid stability method based on ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) was developed. The pharmacokinetic parameters of buserelin after i.m. administration were studied in five pigs and five cows at a single dose of 1 mg per pig and 3 mg per cow. The plasma kinetics were analyzed by WinNonlin 8.1.0 software using a non-compartmental model. The mean concentration area under the curve (AUC0-t) was 25.02 ± 6.93 h × ng/mL for pigs and 5.63 ± 1.86 h × ng/mL for cows. The maximum plasma concentration (Cmax) and time to reach the maximum concentration (tmax) were 10.99 ± 2.04 ng/mL and 0.57 ± 0.18 h for pigs and 2.68 ± 0.36 ng/mL and 1.05 ± 0.27 h for cows, respectively. The apparent volume of distribution (Vz) in pigs and cows was 80.49 ± 43.88 L and 839.88 ± 174.77 L, respectively. The elimination half-time (t1/2), and clearance (CL) were 1.29 ± 0.40 h and 41.15 ± 11.18 L/h for pigs and 1.13 ± 0.3 h and 545.04 ± 166.40 L/h for cows, respectively. No adverse effects were observed in any of the animals. Conclusion This study extends previous studies describing the pharmacokinetics of buserelin following i.m. administration in pigs and cows. Further studies investigating other factors were needed to establish therapeutic protocol in pigs and cows and to extrapolate these parameters to others economic animals.

show abstract

Section: Discussionmentioning

confidence: 99%

The pharmacokinetics of buserelin after intramuscular administration in pigs and cows

Kong

Liu

et al. 2022

BMC Vet Res

View full text Add to dashboard Cite

show abstract

“…However, there are some attempts which can slow-down absorption from delivery site or slow-down enzymatic degradation and elimination to improve the bioavailability, such as sodium glycodeoxycholate, Zn 2+ suspension within the buserelin solution, and cyclodextrin derivatives [13,14,16]. Meanwhile some reports hold the view that buserelin administration induces loss of erectile potency, hot ush [9], uterine bleeding[6], apoptosis in spermatozoa lineage and inhibits immune system function [27,28], further investigations are required to assess its side effects in practical applications.…”

Section: Discussionmentioning

confidence: 99%

The Pharmacokinetics of Buserelin after Intramuscular Administration in Pigs and Cows

Gao¹,

Liu²,

Yang³

et al. 2021

Preprint

View full text Add to dashboard Cite

Background: Buserelin is a LHRH agonist used for the treatment of hormone-dependent diseases in males and females. However, the pharmacokinetics of buserelin in pigs and cows are not clearly understood. This study was designed to develop a sensitive method to determine the concentration of buserelin and to investigate the pharmacokinetic parameters after intramuscular (i.m.) administration in pigs and cows. Results: A sensitive and rapid stability method based on ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) was developed. The pharmacokinetic parameters of buserelin after i.m. administration were studies in five pigs and five cows at a single dose of 1 mg per pig and 3 mg per cow. The plasma kinetics were analyzed by WinNonlin 8.1.0 software using a non-compartmental model. The mean concentration area under the curve (AUC0-t) was 25.02 ± 6.93 h·ng/mL for pigs and 5.63 ±1.86 h·ng/mL for cows. The maximum plasma concentration (Cmax) and time to reach the maximum concentration (tmax) were 10.99 ± 2.04 ng/mL and 0.57 ± 0.18 h for pigs and 2.68 ± 0.36 ng/mL and 1.05 ±0.27 h for cows, respectively. The apparent volume of distribution (Vz) in pigs and cows was 80.49 ± 43.88 L and 839.88 ± 174.77 L, respectively. The elimination half-time (t1/2λz), and clearance (CL) were 1.29 ± 0.40 h and 41.15 ± 11.18 L/h for pigs and 1.13 ± 0.3 h and 545.04 ± 166.40 L/h for cows, respectively. No adverse effects were observed in any of the animals. Conclusion: This study extends previous studies describing the pharmacokinetics of buserelin following i.m. administration in pigs and cows. Further studies investigating other factors were needed to establish therapeutic protocol in pigs and cows and to extrapolate these parameters to others economic animals.

show abstract

“…Nevertheless, while buserelin is already used in the clinic, many side effects have been reported in various cell and animal models, likely due to internalization and downregulation of type I mammalian GnRH-R [ 65 ]. It may induce severe gut dysmotility and enteric neurodegeneration in rat [ 66 ], apoptotic cell death and decreased diameter and epithelium thickness of seminiferous tubules in the adult rat testes [ 67 ]. In human, after a 6- to 9-month period of treatment by buserelin, side effects were observed [ 68 ].…”

Section: Discussionmentioning

confidence: 99%

Buserelin alleviates chloride transport defect in human cystic fibrosis nasal epithelial cells

et al. 2017

View full text Add to dashboard Cite

Cystic fibrosis (CF) is the most common autosomal recessive disease in Caucasians caused by mutations in the gene encoding the Cystic Fibrosis Transmembrane conductance Regulator (CFTR) chloride (Cl-) channel regulated by protein kinases, phosphatases, divalent cations and by protein-protein interactions. Among protein-protein interactions, we previously showed that Annexin A5 (AnxA5) binds to CFTR and is involved in the channel localization within membranes and in its Cl- channel function. The deletion of phenylalanine at position 508 (F508del) is the most common mutation in CF which leads to an altered protein (F508del-CFTR) folding with a nascent protein retained within the ER and is quickly degraded. We previously showed that AnxA5 binds to F508del-CFTR and that its increased expression due to a Gonadoliberin (GnRH) augments Cl- efflux in cells expressing F508del-CFTR. The aim of the present work was to use the GnRH analog buserelin which is already used in medicine. Human nasal epithelial cells from controls and CF patients (F508del/F508del) were treated with buserelin and we show here that the treatment alleviates Cl- channel defects in CF cells. Using proteomics we highlighted some proteins explaining this result. Finally, we propose that buserelin is a potential new pharmaceutical compound that can be used in CF and that bronchus can be targeted since we show here that they express GnRH-R.

show abstract

Short-term buserelin administration induces apoptosis and morphological changes in adult rat testes

Cited by 3 publications

References 22 publications

The pharmacokinetics of buserelin after intramuscular administration in pigs and cows

The pharmacokinetics of buserelin after intramuscular administration in pigs and cows

The Pharmacokinetics of Buserelin after Intramuscular Administration in Pigs and Cows

Buserelin alleviates chloride transport defect in human cystic fibrosis nasal epithelial cells

Contact Info

Product

Resources

About