Trisoralen — trioxsalen

Trioxsalen is a melanizing agent of the psoralen family. The normal pigmentation of the skin is due to melanin, a chemical produced in melanocytes located in the base layers of the epidermis (skin). Melanin is formed by an enzyme reaction, which involves the conversion of tyrosine to DOPA via the enzyme tyrosinase. Radiant energy in the form of ultraviolet light is needed to complete this process. The exact mechanism that trioxsalen uses to exert its action on melanin is not clear. Some investigators feel that this drug has a direct impact on the epidermis, or more specifically the melanocytes. Others feel its action is an inflammatory one, and that the process of increased melanogenesis is only a secondary effect. Regardless of the exact mechanism, trioxsalen is widely regarded as an effective mediator of skin pigmentation.

Trioxsalen is used medically to treat conditions associated with pigmentation dysfunction. The most known of these disorders is vitiligo, a condition that involves a marked loss of skin pigmentation (often in a very blotchy and uneven appearance). Treatment usually involves several consecutive months of regular trioxsalen use combined with UV light exposure. This is undertaken in an effort to slowly and safely rebuild the skin's appearance. In many instances periodic treatment (maintenance) will be required indefinitely to control the disease. Trioxsalen has also been used to increase a patient's tolerance to sunlight, which is accomplished by the increased retention of melanin in the skin. At one time this drug was regularly prescribed to fair skinned people to reduce the likelihood of sunburn, however, due to the potential for adverse reactions the drug is no longer widely used for this purpose.

Competitive bodybuilders often regard trioxsalen as an extremely useful finishing tool when readying for a stage appearance. It is no secret that a dark tan is considered important to the bodybuilding physique. Muscle features seem to be markedly improved with tanning, resulting in a more "ripped" and impressive look on stage. Many bodybuilders, especially fair skinned individuals, have trouble developing a very dark skin base. Although the use of various skin dyes (sun-less tanning products) may be popular, a tanning agent like trioxsalen is also a very common choice. While both may be valid methods for completing a competition physique, many individuals regard the process of using trioxsalen, which produces actual pigmentation changes in the skin, as being more desirable.

Brand name Trisoralen, Tripsor, Puvadin, Trioxsalen

Trisoralen History

Trioxsalen was developed after methoxsalen, and first became an established a medicine in the U.S. during the 1960s. It has been most notably associated with ICN Pharmaceuticals, who sold the drug under the Trisoralen brand name for many years (the company has since changed its name to Valeant Pharmaceuticals). Trisoralen was FDA approved for the repigmentation of idiopathic vitiligo, for increasing tolerance to sunlight, and for enhancing pigmentation. In some instances the drug would be prescribed to fair skin people before sun exposure (such as a tropical vacation or summer beach excursions). This was done in an effort to increase sun tolerance and the likelihood of tanning instead of burning. Later studies demonstrated the potential for psoralens to increase skin cancer risk and cataracts, however, eventually eliminating the use of Trisoralen for this purpose. Prescriptions for this drug have since been largely focused on the treatment of vitiligo.

While trioxsalen remained for sale in many nations over the years, it was never able to supplant methoxsalen in the pharmaceutical market. To the contrary, trioxsalen came to be regardless as a secondary medication to the much more readily prescribed methoxsalen capsules. By 2000, Valeant Pharmaceuticals began discontinuing its Trisoralen products in almost all of its remaining markets worldwide. U.S. brand Trisoralen tablets were included in the discontinuations, and have been unavailable for many years now.Trioxsalen tablets are still sold today, but only in a select few markets. This drug has for all intents and purposes been disregarded by Western medicine.

How is Trisoralen Supplied

Trioxsalen is most commonly supplied in tablets of 5 mg.

Structural Characteristics of Trisoralen

Trioxsalen is a photoactive substance belonging to a class of compounds known as psoralens. It has the chemical designation 2,5,9-trimethyl-7H-furo [3,2-g] [1] benzopyran-7-one.

Trisoralen Warnings (Heightened sensitivity to light)

Psoralen drugs do not protect the skin from sun damage. These drugs increase the skin's sensitivity to sunlight, and can increase the likelihood of skin damage, skin aging, and skin cancer. Medical professionals do not prescribe psoralens for cosmetic purposes (tanning) due to these potential risks.

Trisoralen Warnings (Ocular damage)

Psoralen drugs can increase susceptibility to ocular damage and cataracts. Goggles with complete UVA blocking properties must be worn at all times during light exposure therapy, and for 24 hours following exposure. The medical use of psoralens drugs does not appear to increase the rate of cataract formation when proper eye protection is used.

Trisoralen Side Effects

The most common adverse reactions to trioxsalen therapy include nausea, itching, and reddening of the skin (erythema). Other adverse reactions include nausea, nervousness, insomnia, depression, edema, dizziness, headache, malaise, pigmentation irregularities, cyst, blister, rash, herpes simplex, prickly heat, inflammation of the hair follicles, gastrointestinal disturbances, skin touch sensitivity, leg cramps, low blood pressure, and exacerbated psoriasis.

Trisoralen Administration

When used medically to increase tolerance to sunlight, a dose of 10 mg is usually given 2 to 4 hours priorto UV light exposure. Treatment may be given once daily, but continued for no longer than 14 consecutive days. This medication is normally taken with food or milk.

When used (off-label) for cosmetic ("tanning") purposes, a dosage of 10 mg per application is typically used. As with medical use, UV light exposure is scheduled approximately 2 to 4 hours after administration. The amount of time spent exposed to UV light is also increased slowly, starting with very brief intervals as the user becomes accustomed to the drug. In an effort to minimize the potential for unwanted side effects, most users will limit the intake of trioxsalen to no more than two weeks of regular use. Cautious individuals usually opt to wait 48 hours between applications.

Trisoralen Availability

Trixosalen is produced for sale in select markets including Finland (Tripsor), Greece (Trisoralen), and Malaysia (Puvadin). This medication is not readily available, nor a popular target for drug counterfeit operations.

Newbies Research Guide reference

This is a prescription drug which bodybuilders often use to enhance tanning. A deep dark tan is a precious commodity to a bodybuilder. It will make muscles look bigger and harder while giving the illusion of less body fat. Trisoralen is used for the treatment of vitiligo, which is a condition where skin pigmentation fades. This is usually what the drug is prescribed for, but doctors do prescribe it to especially pale patients who might be headed for a tropical vacation. The drug increases tolerance to solar exposure and enhances pigmentation. Trisoralen seems to act on melanin, which is what is responsible for a person’s natural skin pigmentation. The drug works only if it is taken prior to sun exposure. Recommended use of the drug for accelerating tanning is outlined. The drug should not be taken for more than 14 days at a total dosage of 28 tablets. This means two tablets, 10 mg, taken two to four hours before measured periods of exposure to sun or ultraviolet radiation everyday for 14 days in a row. Trisoralen dosage should not be increased nor taken for longer than 14 days. At least 4 weeks should be taken between dosages. It does not prevent burning, it just promotes tanning. No toxicity has been reported. Nearly all bodybuilders that have used Trisoralen felt it worked to some degree. Fair skinned users seemed to get the most out of the drug. It is rarely seen on the market anymore, but many
doctors will prescribe it.

References

Wlliam Llewellyn (2017) - Anabolics
Newbies Research Guide

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