Not all progestins are the same: implications for usage.
Recent clinical evidence showing unexpected side-effects of progestins used in contraception and hormone replacement therapy has highlighted the importance of choice of synthetic progestin. The molecular mechanisms of action of the relatively nonspecific and most widely used synthetic progestins, medroxyprogesterone acetate and norethisterone, are discussed in the context of this recent clinical evidence. Future directions involving a more mechanism-based approach for improved therapeutics, with greater specificity and fewer side-effects, are discussed.
Hapgood
Janet P
JP
Department of Biochemistry, University of Stellenbosch, Private Bag X1, Matieland 7602, South Africa. JHap@sun.ac.za
Koubovec
Dominique
D
Louw
Ann
A
Africander
Donita
D
D003280:Contraceptives, Oral, Synthetic / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008525:Medroxyprogesterone / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology; D009640:Norethindrone / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D045167:Progesterone Congeners / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D003280:Contraceptives, Oral, Synthetic; D045167:Progesterone Congeners; D008525:Medroxyprogesterone; C024319:norethindrone enanthate; D009640:Norethindrone