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Nifedipine Pharmacokinetics Are Influenced by CYP3A5 Genotype When Used as a Preterm Labor Tocolytic

Nifedipine Pharmacokinetics Are Influenced by CYP3A5 Genotype When Used as a Preterm Labor Tocolytic

David M Haas, Sara K Quinney, Jayanti M Clay, Jamie L Renbarger, Mary F Hebert, Shannon Clark, Jason G Umans, Steve N Caritis, Obstetric-Fetal Pharmacology Research Units Network

Am J Perinatol. 2013 Apr;30(4):275-81.

PMID: 22875663

Abstract:

Objective:
To characterize the pharmacokinetics and pharmacogenetics of nifedipine in pregnancy.
Study design:
Pregnant women receiving oral nifedipine underwent steady-state pharmacokinetic testing over one dosing interval. DNA was obtained and genotyped for cytochrome P450 (CYP) 3A5 and CYP3A4*1B. Nifedipine and oxidized nifedipine concentrations were measured in plasma, and pharmacokinetic parameters were compared between those women who expressed a CYP3A5*1 allele and those who expressed only variant CYP3A5 alleles (*3,*6, or *7).
Results:
Fourteen women had complete data to analyze. Four women (29%) expressed variant CYP3A5; three of these women were also CYP3A4*1B allele carriers. The mean half-life of nifedipine was 1.68 ± 1.56 hours. The area under the curve from 0 to 6 hours for the women receiving nifedipine every 6 hours was 207 ± 138 µg·h /L. Oral clearance was different between high expressers and low expressers (232.0 ± 37.8 µg/mL versus 85.6 ± 45.0 µg/mL, respectively; p = 0.007).
Conclusion:
CYP3A5 genotype influences the oral clearance of nifedipine in pregnant women.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP67035227-B	Oxidized Nifedipine		67035-22-7	Price

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