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Class of compounds
Antiprogestogens , or antiprogestins , also known as progesterone antagonists or progesterone blockers , are a class of
drugs which prevent
progestogens like
progesterone from mediating their
biological effects in the body. These drugs competitively inhibit progestin at progesterone receptors. They act by
blocking the
progesterone receptor (PR)and/or
inhibiting or
suppressing progestogen
production . Antiprogestogens are one of three types of
sex hormone antagonists , the others being
antiestrogens and
antiandrogens .
[1]
Antiprogestogens are used as
abortifacients and
emergency contraceptives and in the treatment of
uterine fibroids . They are also being studied in the treatment of
breast cancer . Examples of antiprogestogens include the
progesterone receptor weak
partial agonist
mifepristone , the
selective progesterone receptor modulator (SPRM)
ulipristal acetate , and the
silent antagonist
aglepristone .
[2]
[3] For
medical abortion , mifepristone is combined with a
prostaglandin (e.g.,
gemeprost ). Ulipristal is used as a form of emergency contraception.
[4]
Several hundred antiprogestogens have been developed, but only three,
mifepristone ,
lilopristone , and
onapristone , have been given to humans, and of these, only mifepristone has been approved and introduced for clinical use.
[5]
Progestins, including progesterone are important for the body to prepare the uterus for implantation of fertilized egg during the luteal phase of the menstrual cycle and, if fertilization, implantation, and other events necessary for pregnancy occur, increased progestin (i.e. progesterone) levels are heavily involved in maintaining the pregnancy. Blocking the effects of progestins, such as progesterone, is associated with anti-gestational events.
[6]
See also
References
^ Judi Lindsley Nath (2006).
Using Medical Terminology: A Practical Approach . Lippincott Williams & Wilkins. pp. 977–.
ISBN
978-0-7817-4868-1 .
^ Spitz, IM. (Oct 2006). "Progesterone receptor antagonists". Curr Opin Investig Drugs . 7 (10): 882–90.
PMID
17086932 .
^ Tang, OS.; Ho, PC. (Dec 2006). "Clinical applications of mifepristone". Gynecol Endocrinol . 22 (12): 655–9.
doi :
10.1080/09513590601005946 .
PMID
17162706 .
S2CID
23295715 .
^ Le, Tao; Bhushan, Vikas; Qiu, Connie; Chalise, Anup; Kaparaliotis, Panagiotis (2023). First Aid . McGraw Hill.
^ Thomas H. Bourne; George Condous (17 October 2006).
Handbook of Early Pregnancy Care . CRC Press. pp. 41–.
ISBN
978-0-203-01621-3 .
^ Le, Tao; Bhushan, Vikas; Qiu, Connie; Chalise, Anup; Kaparaliotis, Panagiotis (2023). First Aid . McGraw Hill.
External links
This article incorporates
public domain material from
Dictionary of Cancer Terms .
U.S. National Cancer Institute .
PR Tooltip Progesterone receptor
Agonists
Testosterone derivatives: Progestins:
6,6-Difluoronorethisterone
6,6-Difluoronorethisterone acetate
17α-Allyl-19-nortestosterone
Allylestrenol
Altrenogest
Chloroethynylnorgestrel
Cingestol
Danazol
Desogestrel
Dienogest
Ethinylandrostenediol
Ethisterone
Ethynerone
Etonogestrel
Etynodiol
Etynodiol diacetate
Gestodene
Gestrinone
Levonorgestrel
Levonorgestrel esters (e.g.,
levonorgestrel butanoate )
Lynestrenol
Lynestrenol phenylpropionate
Metynodiol
Metynodiol diacetate
Norelgestromin
Norethisterone (norethindrone)
Norethisterone esters (e.g.,
norethisterone acetate ,
norethisterone enanthate )
Noretynodrel
Norgesterone
Norgestimate
Norgestrel
Norgestrienone
Norvinisterone
Oxendolone
Quingestanol
Quingestanol acetate
Tibolone
Tigestol
Tosagestin ; Anabolic–androgenic steroids:
11β-Methyl-19-nortestosterone
11β-Methyl-19-nortestosterone dodecylcarbonate
19-Nor-5-androstenediol
19-Nor-5-androstenedione
19-Nordehydroepiandrosterone
Bolandiol
Bolandiol dipropionate
Bolandione
Dimethisterone
Dienedione
Dienolone
Dimethandrolone
Dimethandrolone buciclate
Dimethandrolone dodecylcarbonate
Dimethandrolone undecanoate
Dimethyldienolone
Dimethyltrienolone
Ethyldienolone
Ethylestrenol (ethylnandrol)
Methyldienolone
Metribolone (R-1881)
Methoxydienone (methoxygonadiene)
Mibolerone
Nandrolone
Nandrolone esters (e.g.,
nandrolone decanoate ,
nandrolone phenylpropionate )
Norethandrolone
Normethandrone (methylestrenolone, normethandrolone, normethisterone)
RU-2309
Tetrahydrogestrinone
Trenbolone (trienolone)
Trenbolone esters (e.g.,
trenbolone acetate ,
trenbolone enanthate )
Trendione
Trestolone
Trestolone acetate
Mixed (
SPRMs Tooltip Selective progesterone receptor modulators ) Antagonists
mPR Tooltip Membrane progesterone receptor (
PAQR Tooltip Progestin and adipoQ receptor )