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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Vydáno v:Pharmacology & therapeutics (Oxford) Ročník 222; s. 107789
Hlavní autoři: Bick, Alexis J., Louw-du Toit, Renate, Skosana, Salndave B., Africander, Donita, Hapgood, Janet P.
Médium: Journal Article
Jazyk:angličtina
Vydáno: England Elsevier Inc 01.06.2021
Témata:
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
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Abstract 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]
AbstractList 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.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.
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.
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]
ArticleNumber 107789
Author Bick, Alexis J.
Hapgood, Janet P.
Africander, Donita
Louw-du Toit, Renate
Skosana, Salndave B.
AuthorAffiliation 2 Department of Biochemistry, Stellenbosch University, Stellenbosch 7602, South Africa
3 Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town, South Africa
1 Department of Molecular and Cell Biology, University of Cape Town, Private Bag X3, Rondebosch, 7700, South Africa
AuthorAffiliation_xml – name: 2 Department of Biochemistry, Stellenbosch University, Stellenbosch 7602, South Africa
– name: 3 Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town, South Africa
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  fullname: Bick, Alexis J.
  organization: Department of Molecular and Cell Biology, University of Cape Town, Private Bag X3, Rondebosch 7700, South Africa
– sequence: 2
  givenname: Renate
  surname: Louw-du Toit
  fullname: Louw-du Toit, Renate
  organization: Department of Biochemistry, Stellenbosch University, Stellenbosch 7602, South Africa
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  givenname: Salndave B.
  surname: Skosana
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  surname: Africander
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  surname: Hapgood
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  email: janet.hapgood@uct.ac.za
  organization: Department of Molecular and Cell Biology, University of Cape Town, Private Bag X3, Rondebosch 7700, South Africa
BackLink https://www.ncbi.nlm.nih.gov/pubmed/33316287$$D View this record in MEDLINE/PubMed
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ISSN 0163-7258
1879-016X
IngestDate Tue Sep 30 15:45:33 EDT 2025
Sat Sep 27 16:50:28 EDT 2025
Mon Jul 21 06:00:24 EDT 2025
Sat Nov 29 07:25:01 EST 2025
Tue Nov 18 20:24:56 EST 2025
Fri Feb 23 02:45:09 EST 2024
IsDoiOpenAccess false
IsOpenAccess true
IsPeerReviewed true
IsScholarly true
Keywords 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
Language English
License Copyright © 2020. Published by Elsevier Inc.
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OpenAccessLink https://www.ncbi.nlm.nih.gov/pmc/articles/8122039
PMID 33316287
PQID 2470283816
PQPubID 23479
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ParticipantIDs pubmedcentral_primary_oai_pubmedcentral_nih_gov_8122039
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crossref_primary_10_1016_j_pharmthera_2020_107789
crossref_citationtrail_10_1016_j_pharmthera_2020_107789
elsevier_sciencedirect_doi_10_1016_j_pharmthera_2020_107789
PublicationCentury 2000
PublicationDate 2021-06-01
PublicationDateYYYYMMDD 2021-06-01
PublicationDate_xml – month: 06
  year: 2021
  text: 2021-06-01
  day: 01
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PublicationPlace England
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PublicationTitle Pharmacology & therapeutics (Oxford)
PublicationTitleAlternate Pharmacol Ther
PublicationYear 2021
Publisher Elsevier Inc
Publisher_xml – name: Elsevier Inc
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Snippet Many different forms of hormonal contraception are used by millions of women worldwide. These contraceptives differ in the dose and type of synthetic...
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SubjectTerms 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
Title Pharmacokinetics, metabolism and serum concentrations of progestins used in contraception
URI https://dx.doi.org/10.1016/j.pharmthera.2020.107789
https://www.ncbi.nlm.nih.gov/pubmed/33316287
https://www.proquest.com/docview/2470283816
https://pubmed.ncbi.nlm.nih.gov/PMC8122039
Volume 222
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