Pharmacokinetics, metabolism and serum concentrations of progestins used in contraception

Many different forms of hormonal contraception are used by millions of women worldwide. These contraceptives differ in the dose and type of synthetic progestogenic compound (progestin) used, as well as the route of administration and whether or not they contain estrogenic compounds. There is an incr...

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Bibliographic Details
Published in:Pharmacology & therapeutics (Oxford) Vol. 222; p. 107789
Main Authors: Bick, Alexis J., Louw-du Toit, Renate, Skosana, Salndave B., Africander, Donita, Hapgood, Janet P.
Format: Journal Article
Language:English
Published: England Elsevier Inc 01.06.2021
Subjects:
Contraception
Contraception - adverse effects
Contraception - methods
Contraceptive Agents - blood
Contraceptive Agents - metabolism
Contraceptive Agents - pharmacokinetics
Female
Humans
Metabolism
Pharmacokinetics
Progestin
Progestins - blood
Progestins - metabolism
Progestins - pharmacokinetics
Serum concentration
IVR
LNG
CBG
DRSP
E2
SC
MA
COC
E2C
DSG
NET-A
BMI
SR
EE
IM
P4
MS
E2V
Contraception
p.i
RIA
Metabolism
Serum concentration
NoMAc
GES
NET-EN
Progestin
CPA
NGM
ETG
HC
Pharmacokinetics
DNG
NET
SHBG
NES
NGMN
MPA
ISSN:0163-7258, 1879-016X, 1879-016X
Online Access:Get full text
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Summary:Many different forms of hormonal contraception are used by millions of women worldwide. These contraceptives differ in the dose and type of synthetic progestogenic compound (progestin) used, as well as the route of administration and whether or not they contain estrogenic compounds. There is an increasing awareness that different forms of contraception and different progestins have different side-effect profiles, in particular their cardiovascular effects, effects on reproductive cancers and susceptibility to infectious diseases. There is a need to develop new methods to suit different needs and with minimal risks, especially in under-resourced areas. This requires a better understanding of the pharmacokinetics, metabolism, serum and tissue concentrations of progestins used in contraception as well as the biological activities of progestins and their metabolites via steroid receptors. Here we review the current knowledge on these topics and identify the research gaps. We show that there is a paucity of research on most of these topics for most progestins. We find that major impediments to clear conclusions on these topics include a lack of standardized methodologies, comparisons between non-parallel clinical studies and variability of data on serum concentrations between and within studies. The latter is most likely due, at least in part, to differences in intrinsic characteristics of participants. The review highlights the importance of insight on these topics in order to provide the best contraceptive options to women with minimal risks. [Display omitted]
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ISSN:0163-7258
1879-016X
1879-016X
DOI:10.1016/j.pharmthera.2020.107789