资料单张
MIRELLE
SCHEDULING STATUS:
S3
PROPRIETARY NAME
(and dosage form):
MIRELLE
Tablets
COMPOSITION
The 28-day pack (Every-Day pack) contains 24 hormonal tablets each with
gestodene
(17alpha-ethinyl-13-ethyl-17beta-
hydroxy-4,15-gonadiene-3-one) 0,06 mg and
ethinylestradiol
(17alpha-ethinyl-estra-1,3,5(10)-triene-3,17beta-diol)
0,015 mg, plus 4 inactive tablets.
PHARMACOLOGICAL CLASSIFICATION
A. 18.8 Ovulation controlling agents.
PHARMACOLOGICAL ACTION
Pharmacodynamics
Mirelle is a low-dose monophasic ovulation controlling agent with estrogenic and progestogenic peripheral effects.
The mode of action of gestodene in combination with ethinylestradiol includes:
* the inhibition of ovulation by suppression of the mid-cycle surge of luteinising hormone;
* the suppression of endometrial development thus rendering the endometrium unreceptive to implantation; and
* the thickening of cervical mucus so as to constitute a barrier to sperm.
Pharmacokinetics
• Gestodene
Absorption
Orally administered gestodene is rapidly and completely absorbed. Peak serum concentrations of 4 ng/ml is reached at
about 1 hour after single ingestion. Bioavailability is approximately 99%.
Distribution
Gestodene is bound to serum albumin and to sex hormone binding globulin (SHBG). Only 1 to 2% of the total serum
drug concentration is present as free steroid, 50 to 70% is specifically bound to SHBG. The ethinylestradiol-induced
increase in SHBG influences the proportion of gestodene bound to the serum proteins, causing an increase of the SHBG-
bound fraction and a decrease of the albumin-bound fraction. The apparent volume of distribution of gestodene is 0,7 to
1,4 L/kg.
Metabolism
Gestodene is completely metabolised by the known pathways of steroid metabolism. The metabolic clearance rate from
the serum is 0,8 to 1,0 ml
阅读完整的文件
资料单张 