Third Generation Birth Control Pills

 

Ever since the early 1960’s when birth control pills (BCP’s) were first introduced, they have gone through evolutionary changes in chemical makeup and dosages. 

 

 

Researchers Blamed Estrogens Early On for Blood Clots

 

The very earliest BCP’s (birth control pills) were a combination of relatively high doses of a chemically altered estrogen, called ethinyl estradiol and a progestin, usually norethindrone.  It wasn’t long before multiple side effects were beginning to be noticed, including blood clots, strokes, high blood pressure, significant mood changes and depression.

 

Early investigators attributed the side effects to the estrogen portion of the Pill and began reducing the dosage levels.  Early estrogen doses were approximately 20 times the equivalent synthetic hormone that are now used in hormone replacement therapy (HRT)  and ten times what’s currently found in  BCP’s.

 

 

New Theory on Blood Clots – Caused by Progestins

 

However, the side effects didn’t significantly improve, which called into question whether the estrogen-like component was the culprit or not.  The theory then switched to the progestin part of the formulation, in particular that being the leading cause for the rise in blood clots.

 

This demonstrates how confused researchers become over a multi-year review of prescription medications and their resulting side effects.  To this day, researches still hazard educated guesses on many aspects of drug research and effects. Some of those guesses pan out. Others fall by the wayside.

 

 

Second Generation Pills Synthesized

 

 A second generation Pill was introduced primarily emphasizing a new class of progestins.  This new progestin was most commonly in the form of a chemical called levonorgestrel. 

 

 

Second Generation Pills Too Similar to Anabolic Steroids

 

The side effects continued.  Drug manufacturers encountered complaints from women about the masculinizing effects of the early progestin components and became quite creative in new progestin compounds. The first and second generation BCP’s had effects similar to the male hormone testosterone.  

 

Testosterone falls into the class of anabolic steroids.  So, just like athletes doping up in the gym, women were shaving facial hair and beards, becoming more aggressive and frantically trying to hide their acne.

 

Chemical laboratories were working overtime. Artificially creating designer progestins trying to imitate the action of the natural hormone, progesterone, but trying to get away from the testosterone-like effects of the earlier progestins.

 

 

Third Generation Birth Control Pills Created in the Laboratory

 

Drug companies then came out with the “third generation” progestins for the Pill.  These chemicals became the darlings of the industry with names like desogestrel (DSG), gestodine, and norgestimate acetate (NORGac).  Many drug companies manufactured a number of brands using these third generation compounds.  These were supposed to be the panacea for oral contraception in women.

 

Early studies following the introduction of third generation progestins showed a problematic increase in the risk of blood clots, called venous thrombo-embolism.   Blood clots typically include a clot in the leg veins frequently extending up into the pelvis.  Oftentimes, these clots become dislodged - with the clot actually ending up in the lungs for a potentially fatal event.  Many young women under the age of 40 have died as a result of these lethal clots.

 

 

Third Generation Pills Doubled the Risk of Blood Clots

 

However, blood clots didn’t begin with these third generation pills.  They were already a significant problem with the earlier versions as well.  What shocked the industry was the research actually showing a DOUBLING of the incidence of blood clots with the newer Pills.  Going back as far as 1995, these studies led the FDA to issue a warning about blood clots when using these drugs. 

 

Subsequent studies confirmed this dramatic rise in blood clot risk.  A study in the journal, Contraception, published in June of 2006, did single out one of the third generation progestins, norgestimate, as having a blood clot incidence merely equal to the previous Pill versions.  But that study confirmed again the doubling of the blood clot risk with desogestrel (DSG) and gestodine.

 

This study conflicts with a French investigation done in 1999 which implicated all three of the third generation progestins, including norgestimate.  This clinical trial also showed the blood clot risk was found to be 2 to 5 times higher than the already unacceptable blood clot risk of earlier BCP’s.

 

 

Fourth Generation Progestins are Already Here

 

Recently, drug companies have developed a fourth generation of progestins.  These have tongue-twisting names like drospirenone, dienogest, nesterone, nomegestrol, and trimegestone.  One of them, drospirenone was synthetically derived from a common diuretic called spironolactone and even exhibits different side effects than the others.

 

These fourth generation progestins were published in the journal, Human Reproduction Updates.  The authors of that article discuss the “very early stage of development” and that “striking differences exist regarding the side effects among the progestins.”   They conclude by calling for large clinical trials for these drugs.

 

 

Fourth Generation Pills - Time Will Tell

 

If the experience with these newer generation progestins bears any similarities with the previous versions, time will ultimately reveal their side effect profile as well.  The drug industry and the FDA should not be surprised by any tragic or disastrous effects.