- 10-20-2004, 12:35 PM
Basic Summary: Raloxifene is a second generation SERM that has been shown to reverse pre-existing gyno as well as show all benefits of first generation SERMs.
**Taken from Superior Muscle**
Selective estrogen receptor modulators (SERMs) are a relatively new family of drugs designed to act as estrogens on some, but not all, tissues.2 Tamoxifen is a first-generation SERM. Raloxifene, a second-generation SERM, has been extensively studied on postmenopausal women, and is indicated for the treatment of postmenopausal osteoporosis.3 It is an alternative to estrogen replacement therapy in women with a history of breast cancer.4, 5 Its anti-proliferative effect on mammary tissue is such that prolonged use reduces the risk of breast cancer among osteoporotic women.6
In a recent placebo-controlled short-term trial, the drug was administered to 34 healthy males (mean age, 48 years) at the dose of 60 mg/day for one month; no subject developed gynocomastia. Besides, serum testosterone increased 20%, and serum estradiol decreased slightly.7
We decided to evaluate the effect of raloxifene in a series of patients with gynocomastia. Twelve patients aged 18-84 years were treated. Breast enlargement was unilateral in 5 cases; its duration ranged from a few weeks (7 cases) to several years (5 cases). Four patients were hypogonadal by clinical criteria, and had low serum testosterone. In two patients there was a possible drug effect (prasterone in one, ranitidine in the other). The size of breast tissue ranged between 1.5 and 6.0 cm. All patients had normal testes by palpation, and normal serum levels of estradiol, LH, FSH, prolactin, and alpha-hCG. Liver function tests and serum creatinine also were normal. The dose of raloxifene was 60 mg every other day in 4 elderly patients (age 70 years or more), and 60 mg daily in the remaining; the medication was given for 2-12 months. Hypogonadal patients received, in addition, i.m. injections of testosterone enanthate, 100 mg twice a month.
Raloxifene was well tolerated; only one young patient reported a slight decrease in sexual potency. No subject complained of hot flushes; there were no episodes of thrombophlebitis during follow-up. The analgesic effect of treatment was fast (2-4 weeks) and sustained among 9 patients with pain and tenderness. The size of the gynocomastia was evaluated monthly by means of a caliper (all patients), and ultrasonography (7 patients). All patients responded: there was an average reduction in size of 61% (range: 34-100%); in 2 patients gynocomastia disappeared. Six of 8 eugonadal patients (75%) had a reduction in the size of breast tissue of at least 50% (average, 73%). Among hypogonadal patients (all of them followed with ultrasonography) gynocomastia disappeared in one, and size reduction in the remaining subjects ranged between 46 and 67% (this is particularly noteworthy, since testosterone replacement not infrequently causes or aggravates gynocomastia due to local aromatization to estrogens by mammary tissue). Maximal effect was observed during the first 2 months of treatment.
This open, observational study suggests that raloxifene may be a safe, well tolerated and effective therapeutic alternative for drug-induced or idiopathic gynocomastia in men of all ages.
Zulema Man, MD.
TIEMPO, Buenos Aires, Argentina
Ariel S??nchez, MD, PhD;
Hugo Carretto, MD;
Ricardo Parma, MD.
Centro de Endocrinolog??a, Rosario, Argentina
1. Khan HN, Blamey RW. Endocrine treatment of physiological gynaecomastia. Br Med J 2003;327:301-2.
2. Compston JE. Selective oestrogen receptor modulators: potential therapeutic implications. Clin Endocrinol 1998;48:389-91.
3. Agnusdei D, Iori N. Raloxifene: results from the MORE study. J Musculoskel Neuron Interact 2000;1:127-32.
4. Cummings SR, Eckert S, Krueger KA, Grady D, Powles TJ, Cauley JA, Norton L, Nickelsen T, Bjarnasson NH, Morrow M, Lippman ME, Black D, Glusman JE, Costa A, Jordan VC. The effect of raloxifene on risk of breast cancer in postmenopausal women. J Am Med Ass 1999;281:2189-97.
5. Mincey BA, Morahan TJ, Perez EA. Prevention and treatment of osteoporosis in women with breast cancer. Mayo Clin Proc 2000;75:821-9.
6. Cauley JA, Norton L, Lippman ME, Eckert S, Krueger KA, Purdie DW, Farrerons J, Karasik A, Mellstrom D, Ng KW, Stepan JJ, Powles TJ, Morrow M, Costa A, Silfen SL, Walls EL, Schmitt H, Muchmore DM, Jordan VC. Continued breast cancer risk reduction in postmenopausal women treated with raloxifene: 4-year results from the MORE trial. Breast Cancer Res Treatment 2001;65:125-34.
7. Uebelhart B, Bonjour JP, Draper MW, Pavo I, Basson R, Rizzoli R. Effects of selective estrogen receptor modulator raloxifene on the pituitary gonadal axis in healthy males (Abstract). J Bone Miner Res 2000;15(Suppl 1):S453.
- 10-20-2004, 02:57 PM
If only raloxifen was as easy to get as tamox is...I used tamox at 30mg/day for 2 months to try and rid myself of pubescent gyno. I got mostly unilateral results, with the right breast shrinking more than the left. Regardless, I got results in both sides. Unfortunately in the few weeks after I got some slight rebound effect (extra puffy nipples, itchy/sensitive as well).
I would love to give raloxifen a 2 month shot, although I might give nolva another shot at a higher dose (after a good amount of time off to let my lipid levels and such return to normal).
10-20-2004, 03:39 PM
Try letrozole for gyno it completley starves the tissue for estrogen. Ive heard of more reverse gyno cases with letro then with nolva.
Im trying it myself to evaluate.
10-20-2004, 04:18 PM
I never have heard this.Originally Posted by BryanM
Major problem with raloxifene is the availability.
10-20-2004, 05:33 PM
Both work the same way by starving the tissue for estrogen but letro blocks up to 98% of all estrogen im not sure of nolva but I know that nolva in itself is a weak estrogen so the tissue is still getting estro to it.
The only problem is letro leaves the entire body without estrogen and messes with lipid profiles. But ill take screwed lipids for a month to get rid of gyno.
Ill make a thread if the letro reverses my gyno
10-20-2004, 07:22 PM
I dont know why letro would work with this. Maybe for newly formed gyno, or for gyno symptoms while on cycle if you catch them early enough, but I highly doubt for full blown fibrous tissue would letro work. It is an AI, and stops estrogen conversion in the entire body, while nolva binds to estrogen receptors in the mammary tissue (breast tissue) to prevent estrogen from binding and effecting the tissue.
I could be wrong on this, but I have only seen studies done for the treatment of pubescent gyno with nolva/ralox
10-20-2004, 08:03 PM
10-20-2004, 08:54 PM
Bryan and Engima.. I hate to be an ******* but read the damn board rules.. consider this a warning..
10-20-2004, 09:24 PM
10-20-2004, 11:31 PM
The ral might be great for PCT like tor is (Another new gen SERM) but it would take 120-240mg/d. The low potency is justified by lower liver and nerve toxicity.
10-20-2004, 11:36 PM
I saw that study a while back and picked up a 3 month supply of raloxifene. Used it for a couple weeks and then had a blood test done to see if it was the real deal (it was-- my cholesterol profile was much better than usual). I stopped taking it though and haven't gotten around to using it since.
10-21-2004, 12:20 AM
Matt not to be an ******* but I have read the board rules, numerous times. I have also been "warned" here previously; I am not source posting, and I am over 18. As per the rules, I can post here, as long as I am not source posting (when I was warned I pointed this out and was then allowed to post still).
Unless the rules have changed, I don't see how I am in violation.
10-21-2004, 12:37 AM
10-21-2004, 12:45 AM
Matt, you should probably move this post to the OCT form where it fits in a little better anyway. It doesn't belong in the steroid forum cause its about an Rx SERM drug. Then they could still talk there, right?
10-21-2004, 12:47 AM
10-21-2004, 02:46 PM
My bad its because of the age I will wait i turn 21 soon so ill wait till then to repost.
Or I agree and suggest that we move this to the OTC forum.
But I always thought nolva works by locally blocking estro at the site of breast tissue.
Letro just stops mostly all estrogen from even forming so there is no estrogen to even attach to the receptors. Same princible but letro is very strong.
There is a rebound so you taper your doseage of letro towards the end.
05-27-2005, 04:42 PM
To the Administrator- What rules have Enigma and Brian broken? I don't see any thing that they could have done wrong but I could be wrong though.
05-27-2005, 04:57 PM
Asap - at the time the posts were made this thread was located in the Anabolics section. You must be at least 21 to post in there.Originally Posted by asap nutrition
05-29-2005, 04:39 PM
06-18-2005, 01:22 PM
09-12-2005, 04:36 PM
Try aromasin it is an ai that is a suicide inhibitor, that means it stays attached to the aromatase enzyme until it leaves the body so there is no rebound affect
09-14-2005, 11:11 PM
If Letro removes 98% of your estrogen, isnt long term use (well long enough to remove gyno) going to temporarilly cause your lipids to go bad? Or is it the lesser of 2 evils?
Also, whats this talk about AI's causing a rebound? It doesnt seem possible. Now not tapering a SERM down, I can see rebound.
09-15-2005, 05:57 AM
2.5mg/day letro removes 98% estro. It's those high doses that can promote rebound too. 0.1-0.2mg/day only kills about 60% of estro. That's the secret, use low doses! Steroidal AI's don't rebound, only the enzyme inhibitors and SERMs.Originally Posted by Ghosting
09-15-2005, 07:06 AM
09-15-2005, 08:10 AM
not sure I'm taking your meaning here, Dr.D - you mean that steroidal AIs are qualitatively defferent from non-steroidal AIs?Originally Posted by DR.D
also - what's your sense of the best time to take letro? AM? PM?
09-16-2005, 10:17 PM
Hey Wiz! Steroidal AIs act as suicide substrates that deactivate aromatase. They don't suppress or induce enzymes so there is no rebound when you stop using them. In fact, if you take them long enough there have been reports of protracted anti-e activity long after the compound is discontinued. Letro, on the other hand, prevents estro formation. Enzymes can rebound hard if big doses of letro are taken for a few months straight. This is well documented in women using 2.5mg daily. It is unnecessary because optimal estrogen suppression occurs at 0.25mg daily. I recommend 0.1mg daily or 0.25mg EOD for an average cycle of aromatizable androgens.Originally Posted by BodyWizard
Letro has a long half-life, so just take it at the same time every day. First thing in the morning would be fine, but it probably doesn't matter too much when.
09-16-2005, 11:06 PM
Hey G, sorry I didn't answer the whole question! Yes, letro hurts lipids, but I still love the stuff and think it has it's place. Especially on high test cycles, but Aromasin and Rebound, 2 steroidal AIs, show possible evidence of improving lipids (or at least lowering LDL), maybe due to the 17b-OH metabolites. If letro is used anyway, use the lowest dose required so that estrogen is just attenuated and not completely destroyed.Originally Posted by Ghosting
09-16-2005, 11:19 PM
1 question, what do you know about ATD causing a rebound? I dont fully understand (from what I know of AI's), how a rebound would be possible.?.? In my mind you would have a reduction of the aromatase enzyme, so Im lost when people say taper AI's. Give us the Dr.D final word on this.Originally Posted by DR.D
09-16-2005, 11:34 PM
ATD will not cause a rebound (ironic that it's named Rebound ) because it's a steroidal AI like Teslac and Aromasin. The aromatase inhibition that they cause can be noncompetetive and irreversible, that's why they don't rebound. When people say to taper AIs they probably mean Anastrazol and Letrozole, they are enzyme inhibitors and suppress enzymes that are needed to make estrogen. The body tries to rebalance that by inducing the production of more enzymes proportional to the degree of inhibition and time that they were used. If you use an enzyme inhibitor like letro, just keep the dose low, use it for the shortest amount of time possible and taper at the end if you choose to use higher doses. It's pretty much that simple.Originally Posted by Ghosting
09-16-2005, 11:40 PM
Ooooh...cool, I could just PCT at 3 caps a day for a while, then drop to 2 maybe and call it quits? no need to taper?
Always full of good info