Phenotyping of CYP3A by Oral Midazolam in Healthy Mazandarani Volunteers (Iran)

BACKGROUND AND OBJECTIVE: CYP3A is responsible for hepatic microsomal metabolism of more than 50% of drugs which are its specific substrate. Metabolic activity of this enzyme depends on several factors. Since it has not been done a systematic study of the enzyme activity in Iranian population, this...

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Autores principales:	MR Shiran, S , Gharooee Ahangar, SH Rostamkolaee, AA Sefidgar, M Baradaran, M Hashemi, M Baleghi, AA Moghadamnia
Formato:	article
Lenguaje:	EN FA
Publicado:	Babol University of Medical Sciences 2011
Materias:	phenotype of cyp3a midazolam clearance hepatic metabolism Medicine R Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/5555eaa65f3c492897092a62fa8cdf5b
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spelling	oai:doaj.org-article:5555eaa65f3c492897092a62fa8cdf5b2021-11-10T08:56:42ZPhenotyping of CYP3A by Oral Midazolam in Healthy Mazandarani Volunteers (Iran)1561-41072251-7170https://doaj.org/article/5555eaa65f3c492897092a62fa8cdf5b2011-07-01T00:00:00Zhttp://jbums.org/article-1-3838-en.htmlhttps://doaj.org/toc/1561-4107https://doaj.org/toc/2251-7170BACKGROUND AND OBJECTIVE: CYP3A is responsible for hepatic microsomal metabolism of more than 50% of drugs which are its specific substrate. Metabolic activity of this enzyme depends on several factors. Since it has not been done a systematic study of the enzyme activity in Iranian population, this study was conducted to investigate the enzyme activity in a small sample of Mazandarani population (from north of Iran) using midazolam (MDZ) blood levels as an important probe.METHODS: This study was done on 100 Mazandarani healthy volunteers. After recoding individual information (age, sex and weight), subjects were given 100 ml syrup containing 10 mg midazolam. Blood samples were taken after 0.5, 2 and 6 hr after drug administration and plasma concentrations of midazolam were measured using HPLC method. Oral clearance of midazolam (CL/F) as criteria of the enzyme activity was assessed using P-Pharm software.FINDINGS: The mean (SD) of age was 24.5 ± 6.9 years. Eighteen persons were female. All the subjects experienced some degrees of sedation. The mean (SD) of clearance of MDZ was 77.22 ± 20.98 l/h and clearance of MDZ in female (83.79 ± 15.19 l/h) was higher than male (75.68 ± 21.85l/h) (p<0.001). Total volume of distribution (Vd) and elimination half life were 312.65 ± 50.44 and 2.96 ± 0.68, respectively.CONCLUSION: According to the results, a normal phenotype of CYP3A activity was observed in the Iranian participants in this study. The clearance of oral MDZ and/or CYP3A activity is higher in female subjects than in males.MR ShiranS , Gharooee AhangarSH RostamkolaeeAA SefidgarM BaradaranM HashemiM BaleghiAA MoghadamniaBabol University of Medical Sciencesarticlephenotype of cyp3amidazolamclearancehepatic metabolismMedicineRMedicine (General)R5-920ENFAMajallah-i Dānishgāh-i ̒Ulūm-i Pizishkī-i Bābul, Vol 13, Iss 4, Pp 19-25 (2011)
institution	DOAJ
collection	DOAJ
language	EN FA
topic	phenotype of cyp3a midazolam clearance hepatic metabolism Medicine R Medicine (General) R5-920
spellingShingle	phenotype of cyp3a midazolam clearance hepatic metabolism Medicine R Medicine (General) R5-920 MR Shiran S , Gharooee Ahangar SH Rostamkolaee AA Sefidgar M Baradaran M Hashemi M Baleghi AA Moghadamnia Phenotyping of CYP3A by Oral Midazolam in Healthy Mazandarani Volunteers (Iran)
description	BACKGROUND AND OBJECTIVE: CYP3A is responsible for hepatic microsomal metabolism of more than 50% of drugs which are its specific substrate. Metabolic activity of this enzyme depends on several factors. Since it has not been done a systematic study of the enzyme activity in Iranian population, this study was conducted to investigate the enzyme activity in a small sample of Mazandarani population (from north of Iran) using midazolam (MDZ) blood levels as an important probe.METHODS: This study was done on 100 Mazandarani healthy volunteers. After recoding individual information (age, sex and weight), subjects were given 100 ml syrup containing 10 mg midazolam. Blood samples were taken after 0.5, 2 and 6 hr after drug administration and plasma concentrations of midazolam were measured using HPLC method. Oral clearance of midazolam (CL/F) as criteria of the enzyme activity was assessed using P-Pharm software.FINDINGS: The mean (SD) of age was 24.5 ± 6.9 years. Eighteen persons were female. All the subjects experienced some degrees of sedation. The mean (SD) of clearance of MDZ was 77.22 ± 20.98 l/h and clearance of MDZ in female (83.79 ± 15.19 l/h) was higher than male (75.68 ± 21.85l/h) (p<0.001). Total volume of distribution (Vd) and elimination half life were 312.65 ± 50.44 and 2.96 ± 0.68, respectively.CONCLUSION: According to the results, a normal phenotype of CYP3A activity was observed in the Iranian participants in this study. The clearance of oral MDZ and/or CYP3A activity is higher in female subjects than in males.
format	article
author	MR Shiran S , Gharooee Ahangar SH Rostamkolaee AA Sefidgar M Baradaran M Hashemi M Baleghi AA Moghadamnia
author_facet	MR Shiran S , Gharooee Ahangar SH Rostamkolaee AA Sefidgar M Baradaran M Hashemi M Baleghi AA Moghadamnia
author_sort	MR Shiran
title	Phenotyping of CYP3A by Oral Midazolam in Healthy Mazandarani Volunteers (Iran)
title_short	Phenotyping of CYP3A by Oral Midazolam in Healthy Mazandarani Volunteers (Iran)
title_full	Phenotyping of CYP3A by Oral Midazolam in Healthy Mazandarani Volunteers (Iran)
title_fullStr	Phenotyping of CYP3A by Oral Midazolam in Healthy Mazandarani Volunteers (Iran)
title_full_unstemmed	Phenotyping of CYP3A by Oral Midazolam in Healthy Mazandarani Volunteers (Iran)
title_sort	phenotyping of cyp3a by oral midazolam in healthy mazandarani volunteers (iran)
publisher	Babol University of Medical Sciences
publishDate	2011
url	https://doaj.org/article/5555eaa65f3c492897092a62fa8cdf5b
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Phenotyping of CYP3A by Oral Midazolam in Healthy Mazandarani Volunteers (Iran)

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