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This is a comparison of progestogens, or agonists of the progesterone receptor (PR), as medications. Progestogens include both progesterone and progestins (synthetic progestogens).


Video Comparison of progestogens



Pharmacology

Comparison of structural classes

The different structural classes of progestins have different pharmacological profiles. 19-Norprogesterone and retroprogesterone derivatives tend to be pure progestogens. 17?-Hydroxyprogesterone derivatives tend to have antiandrogen and glucocorticoid properties. Notable exceptions include hydroxyprogesterone caproate, which is a pure progestogen, and medroxyprogesterone acetate, which has weak androgenic actions. 17?-Ethynyltestosterone and 19-nortestosterone derivatives tend to possess weak androgenic actions. Gestodene is a 19-nortestosterone derivative with antimineralocorticoid properties. 17?-Spirolactones tend to have antimineralocorticoid and antiandrogen actions. Progesterone itself has potent antimineralocorticoid properties and very weak glucocorticoid actions.

Comparison of individual progestogens

Activity profiles

The following pharmacodynamic data on various progestogens has been reported by Schindler et al. (2003), Kuhl (2005), and Schindler (2015):

Binding profiles

The following relative binding affinity data on various progestogens has been reported by Kuhl (2005) and Schindler (2015):

The following relative binding affinity on progestogen metabolites and prodrugs has been reported by Kuhl (2005):

Oral progestogenic potency

The following oral potencies of various progestogens for antigonadotropic effect (ovulation inhibition) and producing endometrial transformation in women, as well as dosages used in commercial contraceptive preparations and estimated comparable dosages, have been reported by Schindler et al. (2003), Kuhl (2011), and Fritz & Speroff (2012):

The following has been reported by Lauritzen (1990):


Maps Comparison of progestogens



Pharmacokinetics

The following pharmacokinetic data on various progestogens has been reported by Stanczyk (2002), Kuhl (2009), and Schindler (2015):


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Chemistry

Structural classification

Progestogens used clinically (and/or in veterinary medicine) can be broadly categorized by chemical structure as follows:


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History, society, and culture

Comparison of introductions

The following is a table of clinically used progestogens by decade of introduction, adapted, with additions and corrections, from Schneider & Naftolin (2004):

First-generation oral contraceptives

The following is a table of first-generation oral contraceptives by year of introduction, adapted from Gelijns (1991), Blum (2013), Marks (2001), and Tone & Watkins (2007):


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See also

  • Comparison of estrogens
  • List of steroidal progestogens
  • Progestogen ester

When to use vaginal progesteron suppository


References


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