Abstract
Varenicline is a medication used for smoking treatment that acts as a partial agonist for nicotinic cholinergic receptors α4β2 and α3β4 and as a total agonist of receptor α7 in the central nervous system. Pharmacokinetic is important information for medications that acts in the central nervous system. This kind of assay is commonly done by expensive and complex analytical techniques. Therefore, the aim of this study was to evaluate the possibility of using the open field test as a pharmacokinetic model for varenicline in male rats exposed to a single dose of varenicline. Male rats received a single dose orally (gavage) of three different concentrations of varenicline: 0.03 (therapeutic dose for humans), 0.1 and 0.3 mg/kg or water (control group). The open field observations were recorded 30 min, 1, 2, 4, 6, 24, 48, 72 h and 7 days after the administration of varenicline or water. The results showed alterations in locomotion and rearing frequencies, as well as in immobility time observed in open field, which is consistent with this drug’s plasma peak. Consequently, this behavioral test apparently can be considerate as a model for pharmacokinetic evaluation of varenicline.
Highlights
IntroductionPharmacokinetic is important information for medications that acts in the central nervous system (HENCHOZ et al, 2009)
Varenicline is a medication used for smoking treatment (FAESSEL et al, 2010) that acts as a partial agonist for nicotinic cholinergic receptors α4β2 and α3β4 and as a total agonist of receptor α7 (CRUNELLE et al, 2009), promoting the same effects as nicotine, but at a lower intensity, without the effects of withdrawal, and prevents exogenous nicotine from binding to the receptors, blocking the reinforcing effects of its continuous use (ROLLEMA et al, 2010; IIDA et al, 2012)
Researchers have indicated the possible use of varenicline for the treatment of drug abuse, such as alcohol (ERWIN; SLATON, 2014), cocaine (MELLO et al, 2014), amphetamines (VERRICO et al, 2014) and opioids (HOOTEN et al, 2015), due to its modulation in nicotinic cholinergic receptors, which results in different effects in dopaminergic activity and other neurotransmitters systems (MELLO et al, 2014)
Summary
Pharmacokinetic is important information for medications that acts in the central nervous system (HENCHOZ et al, 2009). This kind of assay is commonly done by expensive and complex analytical techniques. The aim of this study was to evaluate the possibility of using the open field test as a pharmacokinetic model for varenicline in male rats exposed to a single dose of this drug. Considering its wide application, this test can be used to evaluate the plasma decay of drugs that act directly on the general activity, through reducing behavioral parameters
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