Advancement of OCP formulations: Pill taking regulations.Onward
modification of COC after 1970: Further modification of each components of
contraceptive steroids and Pill taking patterns and Schedules: Modifications A) As because of oestrogens dose :- Because orally administered estrogen
is Thrombophilic and increases the risk
of both arterial and venous thrombosis
in a dose dependent manner an
effort was made of reduce the dose of EE
an OCP formulations . In the United States the estrogen dose was initially lowered from 150 ug
of mestranol to 50 mcg and then EE was
lowered to 20 µg. Mestranol is
more potent then EE per unit weight
and 50 ug of mestranol is
roughly equivalent to 35 mcg of EE . The
true low dose formulations are
those with are less than 35 mcg . A formulation with 15 ug EE is now marketed in
Europe and India as Minesse.
Modification
B:-The dose of progestin was also reduced and newer
more potent progestins than norethynodrel were developed
. Most modern OCPs contain
progestins derived from morethindrone or norgestrel .These progestins
chemically resemble testosterone but have
a low degree of androgenic activity.
The antiprogestogene mifepristone was
derived by manipulation of the norethinedrone molecule and Tibolone is a derivative of norethynodrl
.
Modification 3 :
In 2002 a new oral contraceptive
Yasmin was introduced containing drospirenone a progestin
structurally related to
spironolactone. This progestin exhibits
progestogenic anti
mineralocorticoid and anti androgenic
activities . A transdermal
method received regulatory approval for use in the United States in 2001.
Modification 4:- The transdermal contraceptive system was designed to release a constant
rate of 150 ug of norelgestronomin and 20 ug of EE into the systemic circulation each day .
Modification 5:- Marketing of the contraceptive
vaginal ring (Nuvaring) that
daily releases 120 ug of etonogestrel the biologically active metabolite of desogestrel and 150 ug of EE began in 2002.
Modification 6: Gestodene containg Pills:
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