Afloqualone (AFQ) is a GABAergic drug (affecting the neurotransmitter GABA) and is used as muscle relaxant. Researchers have created a model i.e. Population Pharmacokinetic in order to obtain safe and appropriate usage of this drug1.
Afloqualone (AFQ) is a quinazoline family GABA affecting drug and is somewhat similar to that of methaqualone developed in 19762. It has muscle relaxing and soothing effects due to its physiological response to GABAA receptors3. This drug lack hypnosis like effects. It has different effects on sleep-wakefulness cycle than those of both the hypnotics and the other muscle relaxants used4. Its behavior pharmacological properties are different from other anti-axiety, hypnosis inducing drugs and stimulants5.
Oral application of this drug may cause some side effects in some individuals. Systemic exposure of afloqualone in healthy human was observed with high inter-individual variability (IIV). Therefore a study was conducted to develop a population pharmacokinetic model of AFQ and search possible reason of high inter-individual variability (IIV) in the clinical study and further demonstrate its impact on exposure on AFQ through simulation
In order to assess the exposure of AFQ and confirm the high difference between subjects, non-compartmental analysis was assessed. A Population Pharmacokinetic model of AFQ was developed using healthy human Afloqualone Pharmacokinetic data and simulation study was performed with final PK model.
Two groups were made, high exposure group (HEG) and normal exposure group (NEG). In a group with high exposure high HIV levels were found. Through simulations, it was proved that big difference of AFQ exposure between subjects could be observed in some individual and dose of AFQ needs to be reduced for such subjects in HEG.
This study effectively developed the population pharmacokinetics model of AFQ and elucidated the large dissimilarity of AFQ contact in some subjects and suggested a suitable dose of AFQ could have likelihood of genetic polymorphism.
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18 August, 2019