A pharmacodynamic and pharmacokinetic study of the Chinese No. 1 pill.
A pharmacodynamic and pharmacokinetic study of the Chinese No. 1 pill, a combined oral contraceptive containing 35 micrograms ethynyloestradiol (EE) and 600 micrograms norethisterone (NET), was performed in 29 women over a period of six months. Blood samples for analysis were taken during a pretreatment cycle, the first and 6th treatment cycles and post-treatment. Minor changes in carbohydrate metabolism occurred and these were particularly noticeable when the incremental areas under the serum concentration-time curves for both glucose and insulin in response to a glucose tolerance test were calculated. No changes occurred in the serum glycosylated haemoglobin levels. The serum concentrations of all the lipids measured (total cholesterol, triglycerides, LDL-C, HDL-C and apolipoproteins AI, AII and B) were significantly increased on treatment as were levels of Factor X, SHBG and caeruloplasmin whereas antithrombin III decreased. In 38 of the 40 treatment cycles, ovulation was suppressed. In one cycle serum oestradiol and progesterone levels showed a typical ovulatory pattern and in another there was evidence of follicular activity without ovulation. Serum EE concentrations showed a similar pattern in both treatment cycles showing that co-administration of NET did not affect EE metabolism. Serum NET levels were higher in the 6th than in the first treatment cycles. On comparing pharmacodynamic and pharmacokinetic parameters, the only statistically significant correlations were between the percentage change in triglycerides and SHBG and serum NET, but not EE concentrations, and between apolipoproteins AI and serum EE.
Chen
J K
JK
Institute of Planned Parenthood Research, Shanghai, China.
Song
S
S
Yang
P J
PJ
He
M L
ML
Fan
S B
SB
Li
L M
LM
Gui
Y L
YL
Fotherby
K
K
D000328:Adult; D000990:Antithrombin III / Q000737:chemistry; D001053:Apolipoproteins / Q000097:blood; D002570:Ceruloplasmin / Q000737:chemistry; D002784:Cholesterol / Q000097:blood; D003277:Contraceptives, Oral, Combined / Q000493:pharmacokinetics*; D004958:Estradiol / Q000097:blood; D004997:Ethinyl Estradiol / Q000493:pharmacokinetics*; D005170:Factor X / Q000737:chemistry; D005260:Female; D005947:Glucose / Q000378:metabolism; D006801:Humans; D007328:Insulin / Q000097:blood; D009640:Norethindrone / Q000493:pharmacokinetics*; D011374:Progesterone / Q000097:blood; D012738:Sex Hormone-Binding Globulin / Q000737:chemistry
D001053:Apolipoproteins; D003277:Contraceptives, Oral, Combined; D007328:Insulin; D012738:Sex Hormone-Binding Globulin; D004997:Ethinyl Estradiol; D011374:Progesterone; D004958:Estradiol; D000990:Antithrombin III; D005170:Factor X; D002784:Cholesterol; D002570:Ceruloplasmin; D005947:Glucose; D009640:Norethindrone