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. 2021 Dec 3:12:12-19.
doi: 10.1016/j.ibneur.2021.11.002. eCollection 2022 Jun.

Studies on some neuropharmacological properties of Nevirapine in mice

Peter Uchogu Ahmadu  1 , Ejigah Victor  2 , Fidelis Solomon Ameh  1
Affiliations

Studies on some neuropharmacological properties of Nevirapine in mice

Peter Uchogu Ahmadu et al. IBRO Neurosci Rep. .

Abstract

Nevirapine (NVP) is non-nucleoside reverse transcriptase inhibitor and an anti-retroviral drug (ARV) with the highest BBB penetrating ability. Its specific pharmacologic effects on central nervous system (CNS) are not well known. The objective of the study was to investigate some CNS effects of Nevirapine. Oral acute toxicity test (Lorke, 1983) was used to estimate the LD50. Exploratory or sedative effects were tested using open field test(OFT), Hole-board test (HBT), diazepam-induced sleeping time test, and ketamine-induced sleeping time test. Five groups of mice were used (5 mice /group). The negative control group received vehicle (distilled water) (10 mL /kg) while groups II, III, and IV received NVP- 15.625 mg/kg, 31.25 mg/kg, 62.5 mg/kg body weight respectively while group V received 0.25 mg/kg of diazepam intraperitoneal. Groups I to IV were treated orally. The oral LD50 was determined to be 2154. 07 mg/kg. NVP, in a dose dependent fashion, increased the number of line-crossing in the OFT. Also, NVP in a dose-dependent fashion, significantly reduced the duration of diazepam-induced sleeping time as well as delayed onset. NVP significantly potentiated ketamine-induced sleeping time duration. Nevirapine possess excitatory effects possibly through antagonism of GABA receptors. Nevirapine causes wakefulness (shortening of sleep) possibly via antagonism of GABAergic neurotransmission.

Keywords: Blood brain barrier; Excitatory (stimulatory) effects; Mice; Neuro-pharmacological properties; Nevirapine.

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Figures

Fig. 1
Fig. 1
Effect of NVP on number of line crossings in open field test in mice; n = 5, One-way ANOVA followed by Dunnet's post hoc test; *p < 0.05, * *p < 0.01 when compared against control; Dzp=Diazepam, NVP = Nevirapine.
Fig. 2
Fig. 2
Effect of NVP on number of head deeps in hole-board test in mice; n = 5, One-way ANOVA followed by Dunnet'sposthoctest * *p < 0.01 when compared against control; Dzp = Diazepam, NVP = Nevirapine.
Fig. 3
Fig. 3
A. Effect of NVP on onset of sleep in both Diazepam(25 mg/kg) and Ketamine (100 mg/kg) induced sleeping time in mice. B. Effect of NVP on duration of sleep in both Diazepam (25 mg/kg) and Ketamine (100 mg/kg) induced sleeping time in mice. n = 5, One-way ANOVA followed by Dunnet'sposthoctest *p < 0.05, **p < 0.01, ***p < 0.001 when compared against control.
Fig. 4
Fig. 4
Shows the diagrammatic representation of blood brain barrier penetration by Nevirapine and its interaction with ketamine to potentiate the duration of ketamine-induced sleeping time at the post synaptic membrane. Also, Nevirapine interaction with diazepam at the post synaptic membrane to cause a decrease in the duration of Diazepam-induced sleeping time.
See this image and copyright information in PMC

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