Pharmacokinetics of Selegiline in a Rabbit Model

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Background:Selegiline is used to treat Parkinsonian patients. Other indications of its use have recently been discovered.Objective:Scouting special and beneficial side effects of selegiline treatment.Method:Two-year old male Wistar rats were daily treated with 0.25 mg/kg of selegiline s.c. (subcutaneous injection). The rats were sacrificed following a four-weeks’ treatment.Results:Mass of testes, number of sperms, progressive motility of sperms, and their viability definitely increased.Conclusion:Selegiline can successfully be used to stop/counterbalance certain symptoms of aging.

Section: Introductionsupporting

confidence: 87%

Effects on Sperms’ Quality of Selegiline in Aged Rats

Kalász

Thuróczy

Karvaly

et al. 2017

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“…administration to avoid the first-pass effect of the drug. This method has been used and reported in our preliminary publications [ 9 , 24 , 25 , 27 ]. However, to monitor the pharmacokinetics related to the use of selegiline in humans, oral administration should be applied.…”

Section: Discussionmentioning

confidence: 99%

“…Our recent publications definitely suggested incorporation of selegiline in the brain and testes following i.p. administration [ 24 , 25 ]. Similarly, deuterated fluoroselegiline showed incorporation and served for PET studies of monoamino oxidase B in the cynomolgus monkey brain [ 26 ].…”

Section: Introductionmentioning

confidence: 99%

Monitoring the Level of 14C-Labelled Selegiline Following Oral Administration

Kalász

Tekes

Faigl

et al. 2017

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Background:Selegiline [(-)-deprenyl] is widely used for the treatment of Parkinson’s disease in humans.Objective:Time-dependence of tissue distribution of selegiline following per os administration to rats.Method:Oral administration of radiolabeled selegiline to rats resulted in a pattern of tissue distribution similar to that following intraperitoneal injection. Analyses were done using both reversed-phase HPLC and also by counting radioactivity in various body compartments of rats.Results:As a consequence of oral administration of 30 mg/kg of selegiline, its level in the stomach was extremely high (179.57 µg/g tissue through 54.67 µg/g at 15 min to 120 min), that is one magnitude higher than that in the serum level. High selegiline concentrations were also detected in the lacrimal glands (7.45 µg/g), kidneys (6.87 µg/g), livers (6.01 µg/g) and lungs (3.47 µg/g) after 30 minutes of application, which were higher than after intraperitoneal injections.Conclusion:The relatively high tissue levels remained for 120 min monitoring. Selegiline levels in the brain (1.69 µg/g) and in the testes (1.88 µg/g) were also considerably higher than following intraperitoneal administration during the entire period of observation (15 to 120 min).

Investigation of the Experimental Pharmacokinetics of the Bis-Chlorinated Bis-pyridinium Mono-aldoxime Cholinesterase Reactivator K-868 in Rats

Kalász¹,

Tekes²,

Bátor³

et al. 2021

Background: The widespread use of organophosphorus compounds in agriculture and their existence in some military arsenals present continuous threats. Quaternary bis-pyridinium aldoximes are potent, highly polar cholinesterase reactivators and the most intensively studied candidate antidotes against poisoning with organophosphorus compounds. Objective: The in vivo experimental pharmacokinetic properties of K-868, a novel bis-chlorinated, bis-pyridinium mono-aldoxime are detailed and put in context with regard to similar compounds described earlier. Methods: Rats received 30 µmol K-868 i.m. and were sacrificed at various time points following treatment. Blood, cerebrospinal fluid and tear were collected, while the brains, eyes, kidneys, livers, lungs and testes were removed, dissected and homogenized. K-868 concentrations were determined using high performance liquid chromatography with ultraviolet absorption detection. Results: K-868 was detected in the eyes, kidneys, lungs and tear within 5 minutes in maximal serum concentrations attained 15 minutes following administration. Elimination was slow for K-868 which remained detectable at 120 minutes in the blood and the kidneys, and at 60 minutes in the eyes, lungs and tear following its administration. Nevertheless, its distribution was overall poor with areas under the 120-minute concentration curves (AUC120) showing close similarity in the blood and the kidneys, while reaching just approximately 5% of serum AUC120 in the eyes and lungs. Conclusion: K-868 is a potent candidate antidote against organophosphate poisoining with a prolonged presence in the circulation.