DEPO LEUPROLIDE OR LEUPROLIDE ACETATE AS A CHEMICAL CASTRATE FOR MALE TO FEMALE TRANSSEXUALS - Edited by Jennifer Wells from material submitted through GenderLine.
NOTICE: This is not a medical report. Its information is presented by non medical personnel. Any drug program should be discussed with your physician or endocronologist!
Many of us, both TV and TS have often wondered whether we would take "a magic pill" that turns you into a woman, if such a thing existed. While estrogens and other female hormones may do most of the job, Depo leuprolide may help complete the job. This drug produces total chemical castration in males, and one dose lasts for a month. It does cost $360 a dose though.
OVERVIEW OF STUDIES:
In studies underway in efforts to develop a male birth control pill research have focused on gonadotropin-releasing hormone (GnRH) agonists and antagonists to inhibit reproductive hormonal function. GnRh, according to L.M. Globe "is one of the hormones involved in the complex hypothalmic-pituitary-gonadal axis which regulates the release of testosterone. Tests, in male rats (Heber, Swerdloff, et al) have indicated GnRH analogs are long lasting agonists in man and laboratory animals, resulting "in suppression of testosterone secretion and diminished sperm counts". GnRH agonists "result in suppressed LH (leutinizing Hormone) FSH (folicle stimulating hormone) and testoster one levels." Leucolide acetate, per W.C. Dodson is "a long lasting GnRH agonist."
The studies however did indicate an early peaking of LH before taper ing off, according to Trachtengerg, this peak of LH can be controled with a drug called Ketoconazole. It was his conlusion that ketoconazole inhibited the surge of testosterone induced by the ad ministration of a potent luteinizing releasing hormone agonist causing testosterone levels to decline to unmeasureable levels. According to H.F. English, Leuprolide alone lowered basal testosterone levels alone to 0.20 +/- 0.02 ng/ml and that " combining ketoconazole with leuprolide achieves greater suppression of testosterone" to levels of 0.11 +/- 0.01.
In long term tests on men with advanced prostrate cancer, which is treated with leuprolide, L. M. Globe concluded that " a daily administration of 1mg leuprolide acetate subcutaneoulsy produces durable, and complete suppression of gonadotropins and testosterone for prolonged periods."
These tests indicate that Leuprolide Acetate either in combination with other drugs or alone can significantly reduce levels of testosterone to castrate levels, further according to Ichikawa, they can cause a decrease in the weight of the sex organ dependant on the dose administered. However, "No treatment with leuprolide surpassed the effect caused by castration." USES:
In females it is used in fertility clinics to treat fibroids of the uterus. The main use is treatment of men for prostatic cancer. Although it is unknown at this time if it has been used in pre- operative TS's, estrogens are not contraindicated and it's use may make sense. Cost would be a big factor in its use though.(1)
LEUPROLIDE ACETATE (Depo leuprolide) basically shuts down steroido genesis in the testicle or ovary. According to referrence books (including the PDR) ... Leuprolide acetate ... is an LH - RH agonist. What that means basically is that it inhibits the secretion of gonado tropins by the body, when it is given continuously and in theraputic doses (1mg/day administered in a subcutaneous inj. or 7.5mg/month adminstered in "depot form" in an intramuscular injection) It causes the inhibition of the production of LH (leutinizing hormone) and FSH (follicle stimulating hormone) which influence the production, by the body, of the gonadal steroids.
This means is that it does result in a decrease in production of testosterone to castrate levels (after an initial increase...which occurs over about 1 week - after initial administration). At this time there are no known major side effects, or contraindications, and no evidence of mutagenicity has been uncovered in animal studies.(2)
You may want to inform your endocrinologist/gynocologist of this drug as a possible compliment to your hormonal program. Drug use of any kind should be left up to your doctor.
1. Natalie (tv)
2. Cynthia K.
1) Swerdloff RS, Heber D, et al - Effect of GnRH superactive analogs on testicular function in man and experimental animals.
2) Heber D, Dodson R, et al - Counteractive effects of agonistic and antagonistic GnRH analogs on spermatogenesis: sites of action.
3) Rajfer J, Heber D, et al - Effects of chronic D-Leu6, des-GLY10- gonadotropin releasing hormone ethylamide on male sex tissues.
4) Trachtenberg J. - The effects of ketoconazole on testosterone production and normal and malignant androgen dependant tissues of the adult rat.
5) Swerdloff RS, Handelsman DJ, et al - Hormonal effects of GnRH agonist in the human male: an approach to male contraception using combined androgen and GnRH agonist treatment.
6) English HF, Santner SJ, et al - Inhibition of testosterone production with ketoconazole alone and in combination with GnRH analogue in the rat.
7) Hickey D, Todd B et al - Pre treatment testosterone levels: significance in androgen deprivation therapy.
8) Globe LM, Smith JA Jr - Long term supression of leuteinizing hormone, folicle stimulating hormone, and testosterone by daily administration of leuprolide.
9) Rittmaster RS, Thompson DL - Effect of leuprolide and dexamethasone on hair growth and hormone levels in hirsute women.
10) Ichikawa T, Akimoto S, et al - Effect of leuprolide on growth of rat prostatic tumor (R3327) and weight of male accessory sex organs.