Entry Type
Name
Value
Parent Entry
Pharmacology Data Field
Reported as weakly effective to effective agonist.
Medroxyprogesterone Acetate (API)
Pharmacology Data Field
Agonist
Levonorgestrel (API)
Pharmacology Data Field
No activity
Nestorone (API)
Pharmacology Data Field
Binds to GR but does not show activity in in vivo assays
Nestorone (API)
Pharmacology Data Field
No activity
Medroxyprogesterone Acetate (API)
Pharmacology Data Field
No activity
Medroxyprogesterone Acetate (API)
Pharmacology Data Field
Near 100%
Medroxyprogesterone Acetate (API)
Pharmacology Data Field
88% bound to serum albumin, no binding to SHBG or CBG
Medroxyprogesterone Acetate (API)
Pharmacology Data Field
- Oral: Around 45%
- Vaginal Ring: 55%
Ethinyl Estradiol (API)
Pharmacology Data Field
97% bound. Mainly to serum albumin. No binding to SHBG, but induces SHBG synthesis.
Ethinyl Estradiol (API)
Pharmacology Data Field
Binds but no agonist activity. "Weak," "partial" or "moderate" antagonist.
Nomegestrol Acetate (API)
Pharmacology Data Field
No activity
Nomegestrol Acetate (API)
Pharmacology Data Field
No activity
Nomegestrol Acetate (API)
Pharmacology Data Field
Antagonist (40% of CPA, the most potent anti-androgenic progestin)
Dienogest (API)
Pharmacology Data Field
Partial antagonist (about 30% activity of cyproterone acetate)
Drospirenone (API)
Pharmacology Data Field
Antagonist
Drospirenone (API)
Pharmacology Data Field
No activity
Drospirenone (API)
Pharmacology Data Field
Antagonist (antimineralocorticoid or aldosterone antagonist). Agonist reports vary: "weak" (Africander) to "strong" (Bartsch).
Drospirenone (API)
Pharmacology Data Field
CYP3A4. No hepatic first pass effects after oral intake.
Medroxyprogesterone Acetate (API)
Pharmacology Data Field
Reports vary: "weak" (Kuhl), "active" (Bartsch), "not active" (Ruan, Lello)
Etonogestrel (API)
Pharmacology Data Field
76-85%
Drospirenone (API)
Pharmacology Data Field
Reported as "weak" (Africander, Kuhl) and "active" (Ruan, Lello) agonist
Gestodene (API)
Pharmacology Data Field
Binds. Activity reports vary slightly: reported as an antagonist (Ruan, Lello, Kuhl), while Africander reports that some antagonist activity is seen in rat models and Stanczyk claims it to be relatively weak compared to progesterone.
Gestodene (API)
Pharmacology Data Field
Agonist
Norethindrone (API)
Pharmacology Data Field
Agonist and antagonist
Norethindrone (API)
Pharmacology Data Field
No activity
Norethindrone (API)
Pharmacology Data Field
No activity
Norethindrone (API)
Pharmacology Data Field
> 95%, 61% to albumin, 36% to SHBG
Norethindrone (API)
Pharmacology Data Field
- Inhibits CYP2C9,
CYP2C19, CYP3A4, CYP2B6
- After formation of very reactive intermediate by oxidation of C17 ethinyl, can irreversibly inhibit cytochrome P450 enzymes (e.g. CYP2C8, CYP3A4). Thus it exerts strong effects on hepatic metabolism.
- Nuclear receptor subfamily 1 group I member 2: agonist
- Bile salt export pump: inhibitor, inducer
- Sodium/bile acid cotransporter: inducer
- Canalicular multispecific organic anion transporter 1:
inducer
- Multidrug resistance protein 1: substrate
- Uridine diphosphate glucuronosyltransferase
(UGT): inducer
Ethinyl Estradiol (API)
Pharmacology Data Field
Antagonist
Chlormadinone Acetate (API)
Pharmacology Data Field
Antagonist
Progesterone (API)
Pharmacology Data Field
"weak partial agonist" (Africander), active agonist (Bartsch). Antagonist.
Progesterone (API)