2014
DOI: 10.1007/s00228-013-1634-1
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Abstract: Using EFV as an example of a drug with a narrow therapeutic index and a high inter-patient variability in plasma concentrations corresponding to a standard dose of the drug, this review demonstrates how genotyping of the primary metabolising enzyme can be useful for appropriate dosage adjustments in individuals. However, other variables such as drug interactions and auto-induction may necessitate plasma concentration measurements as well, prior to personalising the dose.

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Cited by 39 publications
(49 citation statements)
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“…Given that studies have shown that genetic variations, particularly of the enzyme CYP2B6, in patients affect the plasma levels of efavirenz 9,35 , studies need to be conducted in a broader range of countries to determine region-specific guidelines for efavirenz dosing. These polymorphisms have been shown to be more common in patients of African descent and such patients should be monitored more closely as they are more likely to experience higher plasma levels of efavirenz and be susceptible to neuropsychiatric side effects 35 .…”
Section: Discussionmentioning
confidence: 99%
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“…Given that studies have shown that genetic variations, particularly of the enzyme CYP2B6, in patients affect the plasma levels of efavirenz 9,35 , studies need to be conducted in a broader range of countries to determine region-specific guidelines for efavirenz dosing. These polymorphisms have been shown to be more common in patients of African descent and such patients should be monitored more closely as they are more likely to experience higher plasma levels of efavirenz and be susceptible to neuropsychiatric side effects 35 .…”
Section: Discussionmentioning
confidence: 99%
“…The standard dose of efavirenz is 600mg daily generally taken at bedtime 9 . Only four studies explicitly stated the dose of efavirenz being received by the patients.…”
Section: Patient Populationsmentioning
confidence: 99%
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“…Gender differences in CYP2B6 are controversial. Although a few studies have reported gender differences in CYP2B6 protein or activity (Lamba et al, 2003;Al Koudsi and Tyndale, 2010;Naidoo et al, 2014), a number of other studies have not observed this phenomenon (Hesse et al, 2004;Parkinson et al, 2004;Hofmann et al, 2008;Croom et al, 2009). Exposure to inducers potentially could account for a portion of the large variability observed in this study; however, only two individuals had known exposure to drugs capable of inducing CYP2B6 (both 7 year olds) and five individuals had a history of chronic alcohol use (five adults), which has been shown to cause CYP2B6 induction (Hesse et al, 2004;Ferguson et al, 2013).…”
Section: Discussionmentioning
confidence: 99%
“…Further complicating the predictive ability of phenotype from genotype is that for some CYP2B6 variants the relative catalytic activity appears to be dependent on the substrate examined (Helsby et al, 2010;Tingle, 2011, 2012). For example, individuals with a CYP2B6*6 allele demonstrate decreased efavirenz 8-hydroxylation and clearance in vivo (Naidoo et al, 2014) but increased cyclophosphamide 4-hydroxylation and clearance (relative to CYP2B6*1 homozygotes) (Xie et al, 2006). Hence, to accurately estimate CYP2B6 biotransformation capacity for a particular medication in an individual, an understanding of the influence of CYP2B6 genetic variation on the clearance of the drug will be required, and it may even be necessary to empirically determine drug clearance for some compounds, given the wide range of CYP2B6 interindividual variability.…”
Section: Discussionmentioning
confidence: 99%