Wednesday, 22 April 2020

Advancement of OCP formulations: Pill taking regulations.


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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