Entry Type
Name
Value
Parent Entry
Toxicology Data Field
Increases risk of breast cancer and coronary heart disease in hormone replacement therapy (HRT) users by disturbing normal signaling of natural androgens which play a protective role against breast cancer. Negative effects on bone density due to glucocorticoid activity. Possible weight gain, increased blood pressure, and cardiovascular complications due to no or very weak antimineralocorticoid activity. As an injectable contraceptive, associated with increased HIV acquisition.
Nervousness, abdominal distress, headache, metrorrhagia, amenorrhoea, libido decreased, dizziness, weight increased, asthenia, injection site reaction.
Medroxyprogesterone Acetate (API)
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 but no agonist activity. "Weak," "partial" or "moderate" antagonist.
Nomegestrol Acetate (API)
Pharmacology Data Field
Antagonist (40% of CPA, the most potent anti-androgenic progestin)
Dienogest (API)
Pharmacology Data Field
Weak or no agonist and antagonist activity
Dienogest (API)
Pharmacology Data Field
Low to no activity
Dienogest (API)
Pharmacology Data Field
No activity
Dienogest (API)
Pharmacology Data Field
Antagonist
Drospirenone (API)
Pharmacology Data Field
Antagonist (antimineralocorticoid or aldosterone antagonist). Agonist reports vary: "weak" (Africander) to "strong" (Bartsch).
Drospirenone (API)
Pharmacology Data Field
Antagonist
Levonorgestrel (API)
Pharmacology Data Field
Conflicting reports: not active (Ruan, Lello), weakly effective (Nath), active (Bartsch), binds to GR (Jordan), low affinity (Africander)
Levonorgestrel (API)
Pharmacology Data Field
Agonist with high relative binding affinity. Conflicting reports on antagonism: Ruan and Lello indicate not active, while Africander says some anti-mineralocorticoid activity in rat models.
Levonorgestrel (API)
Toxicology Data Field
Generally very well tolerated, positive safety profile
Nomegestrol Acetate (API)
Pharmacology Data Field
Reported as agonist with high relative binding affinity and no antagonist activity, but Stanczyk notes that data consistent with low androgenic potential and strong antagonist effects demonstrated in vitro.
Gestodene (API)
Pharmacology Data Field
Antagonist
Gestodene (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)
Physical & Chemical Properties Data Field
Test value
Levonorgestrel (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
Progesterone (API)
Pharmacology Data Field
Antagonist
Progesterone (API)
Pharmacology Data Field
"weak partial agonist" (Africander, Hapgood), activates GR "minimally" (Turgeon), "active" (Ruan, Lello)
Progesterone (API)
Pharmacology Data Field
"weak partial agonist" (Africander), active agonist (Bartsch). Antagonist.
Progesterone (API)