Comparative Experimental Pharmacokinetics of Benzimidazole Derivatives

Сергеева, С. А.; Gulyaeva, I. L.

doi:10.1007/s10517-009-0382-9

Cited by 4 publications

(3 citation statements)

References 4 publications

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“…To avoid overuse of medications for combined treatment of patients with CCT, it is necessary to synthesize new preparations with specific pharmacological activity. Antihypoxant bemithyl (2-ethylthio-benzimidazole hydrobromide) possesses nootropic and mild psychostimulant activity and fully conforms these requirements [4,8,9]. Here we studied the cerebroprotective effect of individual and combined treatment with the antihypoxant bemithyl and antidepressant pyrazidol in animals with CCT characterized by different resistance to hypoxia.…”

Section: Antihypoxants Antidepressants and Brain Injurymentioning

confidence: 99%

Hypoxia and antihypoxants, focus on brain injury

Shabanov

Zarubina

2019

Rev Clin Pharm Drug Ther

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Experiments on rats showed that the individual resistance of the body to acute hypoxia is of decisive importance in the early recovery period after mechanical craniocerebral trauma. Antihypoxant ethomersol administration (25 mg/kg, 3 days, intraperitoneally) following trauma decreased behavioral impairments in rats with different levels of resistance to acute hypoxia, restored the structure of individual behavior, and prevented metabolic disturbances in the brain. Monotherapy of consequences of craniocerebral trauma with antidepressant pyrazidol (1 mg/kg) produced an anxiolytic effect in animals highly resistant to hypoxia and activating effect on low resistant animals. Treatment with bemithyl, an antihypoxant of benzimidazole structure, in a dose of 25 mg/kg produced a cerebroprotective effect and normalized individual behavioral characteristics, parameters of energy metabolism, and state of the antioxidant system in the brain of highly and low resistant rats. The effect of bemithyl was most pronounced in highly resistant animals. During combined treatment, pyrazidol and bemithyl had an additive effect in animals of both groups. They normalized behavioral reactions and prevented the development of metabolic disturbances in the brain.

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Section: Antihypoxants Antidepressants and Brain Injurymentioning

confidence: 99%

Hypoxia and antihypoxants, focus on brain injury

Shabanov

Zarubina

2019

Rev Clin Pharm Drug Ther

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“…The effect of ritonavir on albendazole 2 and mebendazole 218 has been documented . Pharmacokinetics of bemithyl 219 was compared with etomerzole in organs and tissues after single and course treatment (Fig. ).…”

Section: Pharmacokinetics/pharmacodynamics Of Benzimdazolementioning

confidence: 99%

Functionalized Benzimidazole Scaffolds: Privileged Heterocycle for Drug Design in Therapeutic Medicine

Ajani

Aderohunmu

Ikpo

et al. 2016

Archiv der Pharmazie

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Benzimidazole derivatives are crucial structural scaffolds found in diverse libraries of biologically active compounds which are therapeutically useful agents in drug discovery and medicinal research. They are structural isosteres of naturally occurring nucleotides, which allows them to interact with the biopolymers of living systems. Hence, there is a need to couple the latest information with the earlier documentations to understand the current status of the benzimidazole nucleus in medicinal chemistry research. This present work unveils the benzimidazole core as a multifunctional nucleus that serves as a resourceful tool of information for synthetic modifications of old existing candidates in order to tackle drug resistance bottlenecks in therapeutic medicine. This manuscript deals with the recent advances in the synthesis of benzimidazole derivatives, the widespread biological activities as well as pharmacokinetic reports. These present them as a toolbox for fighting infectious diseases and also make them excellent candidates for future drug design.

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“…These data are necessary for appropriate use of drugs: individual adjustment of the optimal therapeutic dose, treatment regimen, and permissible combination of drugs, detection of active metabolites, and prevention of adverse reactions. In this regard, experimental pharmacokinetic studies are an essential stage of preclinical trials of new drugs [1][2][3][4][5][6]9].…”

mentioning

confidence: 99%

Study of the Absolute Bioavailability of Citrocard, a New GABA Derivative

et al. 2013

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The main pharmacokinetic parameters attest to short elimination half-life and mean retention time of a single citrocard molecule. The average rate of plasma concentration decrease of the compound determined small area under the pharmacokinetic curve. Steady-state distribution volume was low and only slightly surpassed the volume of extracellular body fluids in rat, which indicated moderate capacity of citrocard to distribution and accumulation in the tissues, which is seen from low systemic clearance (Cl) despite the quick elimination of the compound. Absolute bioavailability was 64%.

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Comparative Experimental Pharmacokinetics of Benzimidazole Derivatives

Cited by 4 publications

References 4 publications

Hypoxia and antihypoxants, focus on brain injury

Hypoxia and antihypoxants, focus on brain injury

Functionalized Benzimidazole Scaffolds: Privileged Heterocycle for Drug Design in Therapeutic Medicine

Study of the Absolute Bioavailability of Citrocard, a New GABA Derivative

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