Levothyroxine Sodium History
Levothyroxine sodium was the first synthetic thyroid medication to be sold in the U.S., and was first introduced to market in 1955 by Flint Laboratories as Synthroid. The drug has a long history of therapeutic use in the U.S. and internationally, and for decades has been the most widely prescribed medication for the treatment of hypothyroid. The Synthroid brand has historically been the most successful, with figures estimating that it retained 85% of total levothyroxine sales and $600 million in annual revenues (1990 estimates). In the bodybuilding and athletic communities, however, the faster acting and more powerful drug Cytomel (liothyronine sodium) is most popular. Since Synthroid is weaker and slower acting, athletes need to take the drug for a longer duration to achieve similar results.
The Synthroid brand itself has a long and at times controversial history. For many years after its inception by Flint Laboratories, Synthroid enjoyed a virtual monopoly on the levothyroxine sodium market. Generic medications finally began taking a large share of levothyroxine sodium sales going in to the 1980s. In response, Flint Laboratories funded a study at the University of California in 1986 which attempted to demonstrate that Synthroid had a higher therapeutic value than its generic counterparts. The study was completed in 1990, and, in fact, proved that the generic drugs had equal efficacy to Synthroid. Flint exercised a clause in its contract requiring company approval before the university could publish its study. A legal battle over its publication ensued.Even after Flint Laboratories was sold to Boots, and thereafter Boots sold to Knoll, publication of the study was vigorously opposed. It was eventually ordered into publication in 1997. A class action lawsuit followed, alleging that misconduct over the publication and marketing claims forced consumers to pay 2 to 3 times more for a brand name drug than an equivalent generic counterpart. Knoll eventually settled for $135 million.
How is Levothyroxine Sodium Supplied
Levothyroxine sodium is most commonly supplied in oral tablets of 25 mcg,50 mcg,75 mcg, 100 mch, 125 mcg, 150 mcg, 200 mcg, and 300 mcg.
Structural Characteristics of Levothyroxine Sodium
Levothyroxine sodium is a synthetic form of T4 thyroid hormone. It has the chemical designation L-3,3',5,5'- tetraiodothyronine sodium salt.
Levothyroxine Sodium Warnings
FDA requires that the following black box warning accompany prescription liothyronine sodium products sold in the U.S. “Thyroid hormones, including levothyroxine sodium, either alone or with other therapeutic agents, should not be used for the treatment of obesity or for weight loss. In euthyroid patients, doses within the range of daily hormonal requirements are ineffective for weight reduction. Larger doses may produce serious or even life threatening manifestations of toxicity, particularly when given in association with sympathomimetic amines such as those used for their anorectic effects.”
Levothyroxine Sodium Side Effects
Side effects are generally associated with overdosage, and may include headache, irritability, nervousness, sweating, irregular heartbeat, increased bowel motility, or menstrual irregularities. Overdosage may also induce shock, and may aggravate or trigger angina or congestive heart failure. Chronic overexposure to levothyroxine sodium will produce symptoms normally associated with hyperthyroidism, or the overproduction of natural thyroid hormones in the body. The occurrence of over-exposurelinked side effects is normally cause to immediately reduce or discontinue therapy with levothyroxine sodium. Acute massive overdose may be life threatening.
Levothyroxine Sodium Administration
When used to treat mild to moderate hypothyroidism, the average replacement dose of levothyroxine sodium is approximately 1.7 mcg/kg/day. This equates to 100-125 mcg/day per day for a 154lb adult. The full therapeutic dose may be given from the onset of therapy in otherwise healthy adult patients. Note that due to the long half-life of levothyroxine, the peak therapeutic effect at a given dose may not be achieved for 4 to 6 weeks.
When used (off-label) to accelerate fat loss by bodybuilders and athletes, the typical protocol involves slow buildup of the dosage so that the body has ample time to adjust to the changing thyroid hormone levels. An individual will generally start with a low dosage of 25- 50 mcg, and will slowly increase the amount 25-50 mcg each day or two. The final dosage will usually be in the range of 100-150 mcg, and will rarely exceed 250 mcg. It is important to remember that thyroid drugs are strong medications with significant side effect potential. Cautious individuals will be sure not to use excessive amounts of levothyroxine sodium, nor continue treatment for longer than eight weeks. It is also generally advised to also reduce the Synthroid dosage gradually at the conclusion of each cycle. This is usually accomplished by dropping the dosage by 25 mcg every second or third day. The focus here, again, is to help avoid any sudden change in hormone levels that might otherwise trigger side effects. Note that due to the slow acting nature of levothyroxine sodium, it may take several weeks or longer for the active drug to be fully eliminated from the body.
Levothyroxine Sodium Availability
Although levothyroxine sodium is a widely manufactured drug, it is not as common on the black market as the stronger thyroid drug Cytomel. Large scale counterfeiting does not appear to be a problem.
Synthroid is a man-made synthetically manufactured version of T-4/L-thyroxine. The average person produces about 76 MCG/d of T-4/L-thyroxine which is then converted by the liver into the more active T-3/L-triiodothyronine. This is true of the oral T-4/L-thyroxine medications as well. The average conversion rate of T-4 to T-3 is about 30-33%/ MCG. Since the conversion of T-4 to T-3 is dependent upon adequate levels of since and selenium, athletes commonly increase daily intake of these minerals during synthetic T-4/L-thyroxine use.
As is the case with all thyroid hormone drug use, most athletes were noted as wiser to begin at a lower dosage of 100 MCG/d and slowly progress to their chosen dosage. Daily dosages of T-4/L-thyroxine that exceed 400 MCG will not increase metabolic rate beyond what is realized at 400 + MCG/d.
Dosages that were increased too rapidly or that were too high commonly resulted in diarrhea, excessive sweating, rapid heart beat, nausea, vomiting, insomnia and trembling.
T-4 drugs suppress endogenous thyroid hormone production significantly. After discontinuance, most athletes experienced a metabolic lag period of 3-15 days before thyroid function rebound occurred. Interesting fact is that most monitored athletes experienced a 120-130 % increase in endogenous thyroid hormones at that point. And some maintain that level permanently.
*See guggulsterones for other possibilities.
Wlliam Llewellyn (2011) - Anabolics
L. Rea (2002) - Chemical Muscle Enhancement Bodybuilders Desk Reference