Disclaimer

Before I get started I should be very explicit about one issue. When I am talking about using drugs creatively, I would never recommend acting on any of these ideas without being under the supervision of a health professional who can administer tests and interpret the results. While androgens are generally quite safe, especially if one follows a few simple rules, our physiologies are all different. What works for one person will not necessarily work for another. I strongly advise anyone who is taking hormones to seek out a qualified and sympathetic physician. Please note: The fact that someone has an M.D. does not automatically make them qualified to supervise you in these endeavours. As I have recommended in previous articles, if you can find a Life Extension physician, do so, and don’t let her (or him) go. They are some of the most progressive and open-minded medical professionals practicing today, and they are often quite open (as they should be) to patients making requests.

I write these articles to help inform trans people about options available to them that they might never have known about. I do not and will not dispense medical advice. I want to give you the ability to converse intelliegntly with your doctor, and to help you understand what is going on in your body. Hopefully I can do that.

Meet the Meat

A friend of mine, a trans guy, has almost doubled his dosage of testosterone over the last couple of months. He is on testosterone cypionate, an long-acting oil-based testosterone ester that is injected intramuscularly. Its half-life is approximately eight days. He was injecting 1mL every two weeks, but has since increased his dosage to 1.75mL every two weeks and is doing his injections weekly. He reported a dramatic increase in androgenic effects (hair growth, etc.) with no appreciable negative emotional effects and no increase in liver values. His blood pressure has gone up slightly, but he is still at a perfectly normal 120/80. He sees his physician regularly and has regular tests. Basically, he’s taking more, getting better results, and seeing no negative side effects.

Sounds pretty cool, huh?

It is!

Speaking broadly, androgens are drugs whose effects become more pronounced with increased dosages. To put it another way, if you take more, you will get hairier faster. Therapeutic dosages of testosterone, especially for hormone replacement in FTM guys, are quite low: along the lines of what the average non-trans guy would have in his body. This sounds great, and certainly you can be comfortable with these dosages. However, there is absolutely no clinical evidence demonstrating that supraphysiological dosages, up to a certain level, are at all harmful. If they won’t hurt you, and they will help you, why not consider increasing them?

There is a fair bit of evidence demonstrating that significantly supraphysiological doses of testosterone can be quite safe, especially when taken for short periods of time (6 weeks to 6 months). Therapeutic dosages up to 600mg/week are not unheard of in clinical tests or experimental studies. For many drug using male bodybuilders, 600mg/week is a perfectly normal dose for the purposes of muscle size and strength gains. Contrast that with the average replacement dosage for FTM guys: 100mg/week. Wow. Big difference.

Before you go nuts and start injecting six times the testosterone, do think about the fact that your physiology is different from most guys. The effects of androgens on FTM guys are still being investigated. Extrapolating from the experiences of female bodybuilders and orchidectomized male bodybuilders I would guess that guys with an XX chromosomal makeup shouldn’t be any more concerned about side effects it than guys with XY chromosomes. The “negative side effects” usually mentioned include unwanted hair growth and deepening of the voice. I’ve yet to meet a transman on hormones who didn’t want those things, so it seems to me that we’ve made them positive effects by just looking at them through trans eyes.

Want to know another secret? Increased androgen levels have been conclusively shown to upregulate (increase) the synthesis of androgen receptors. That is, the more testosterone you have in your system, the more efficient your body becomes in using it.

One option that FTMs should be aware of is the concept of cycling. Cycling is the process of changing drug dosage and administration patterns to maximize positive effects while minimizing negative effects.

All androgens are not created equal. There are several different synthetic androgens available as drugs. They have different potencies and different effects. There is no reason to limit yourself to testosterone.

So why aren’t more guys increasing their dosages or changing their dosage patterns? Part of this is probably due to the fact that their physicians don’t know about these options, or are unfamiliar with any research on the subject. Hopefully this article will arm you with some information you need to be able to discuss this intelligently with your physician. If s/he makes fun of you or resents your questioning their supposed omnipotence, find another physician, and make sure to get one who will listen to you. But don’t feel like you have to argue with your physician, either: you should find someone who is comfortable having a discussion with you in which you are an active participant and not just a recipient of knowledge. Once you stumble across a physician like this, be nice to them. Bring them chocolates or NBA tickets or something, because they’re rare.

Side Effects

I think it’s important to talk again about possible negative side effects of drugs. The three most important health-related potential side effects of testosterone use are: elevated liver values, elevated blood lipid levels, and high blood pressure. I have discussed these side effects before, but I’m going to review them along with specific options for minimizing or avoiding them entirely.

Elevated liver values: Conventional wisdom states that androgen supplementation can cause liver damage. This is true, but only for 17-alpha alkylated androgens that are administered orally. There is no evidence supporting the assertion that the standard intramuscular formulations can cause liver damage. In fact, there are studies demonstrating the exact opposite. It is something that should be monitored with regular laboratory tests regardless of the androgen used, but if you have otherwise normal liver function and wish to pretty much eliminate the risk of liver damage, stay with injectable drugs. It might be easier to take pills but it is not good for your liver.

Elevated blood lipid levels: These are sometimes incorrectly referred to as “cholesterol levels.” There is a reasonable amount of evidence that androgen supplementation decreases HDL (“good cholesterol”) levels. Have your physician monitor this, or switch to another androgen that might not have this effect: nandrolone is one possible option.

High blood pressure, a.k.a. hypertension: Hypertension is another common side effect of androgen supplementation. Have your blood pressure checked regularly. If it reaches an unhealthy level, ask your doctor to decrease your dosage or perhaps switch you to another androgen. There is some anecdotal evidence that less androgenic androgens like methenolone and oxandrolone might be better options for those prone to hypertension.

In addition, FTM guys should consider the possibility of losing their hair. Dihydrotestosterone (DHT) and dihydronandrolone (DHN) are androgens which are metabolically created from testosterone and nandrolone respectively by the 5a -reductase (5aR) enzymes. DHT has an extremely high affinity for androgen receptors. High concentrations of 5aR are found in hair follicles, which is why DHT is considered to be the primary culprit for hair loss. (Curiously, DHN is actually a less androgenic version of nandrolone.) Anyway, the negative effects of DHT can be limited by an agent that inhibits the action of 5aR enzymes, or by switching to an androgen that has no dihydro (or a less aggressive dihydro) metabolite: trenbolone, nandrolone and oxandrolone, for example. Consult your physician for more information on these.

Finally, consider that some androgens can be converted to estrogens. The friend that I mentioned at the beginning of this article is seeing one negative side effect from doubling his dosage: elevated estrogen levels. This is usually (but not always) a result of the metabolic conversion of testosterone to estrogens by the aromatase enzyme. There are a couple of ways of preventing this activity. One is to block the action of aromatase using drugs such as Armidex or Cytadren. Another is to take a drug that deactivates or destroys the enzyme itself. An alternative and arguably superior anti-estrogenic treatment would be a drug that blocks the activity of estrogens at the estrogen receptors: drugs such as Clomid and Tamoxifen, which are commonly used in the treatment of breast cancer. There are also several drugs that have no metabolic pathway to estrogens, such as oxandrolone, trenbolone, methenolone and stanozolol. Finally, and maybe somewhat peculiarly, androgens themselves have been shown to have anti-estrogenic effects. This is confusing but true.

To some degree the less bodyfat you have, the less likely it is that androgens will convert to estrogens. This is because the aromatase enzyme is present in high concentrations in fat cells. Staying lean is a good idea for FTMs.

It is not unreasonable (nor unhealthy) to take an androgen at the same time as a 5aR inhibitor and an anti-estrogenic drug. I think that more physicians should consider this, especially if they are supervising hormone regimens that utilize supraphysiological doses of hormones.

What Are Your Options?

Unfortunately many androgens are not available in the US or Canada, but I recognize that many Trans-Health readers do not live in the US or Canada and therefore I am going to list a few more choices. It is possible that, even if a drug is not manufactured or distributed in your country, it can be purchased under governmental guidelines from overseas pharmacies with a prescription. Understanding the laws of your country are beyond the scope of this article. I recommend consulting an attorney, your country’s Customs department or ministry, or your physician. DO NOT BUY TESTOSTERONE FROM THE BLACK MARKET, ESPECIALLY FROM BODYBUILDERS. They will probably rip you off, and there’s absolutely no telling what you will get, if it will contain what it says, or even if it is sanitary or sterile. Counterfeit androgens are a huge and profitable business for many unscrupulous assholes. What they give you might be dangerous. Don’t let yourself get screwed by them. Please. I’m not kidding.

Below I describe four androgens and a few other drugs that might be of interest to FTM guys. Remember that 250mg of one testosterone ester is not the same as 250mg of another testosterone ester, nor is it the same as 250mg of another androgen. I won’t make specific dosage recommendations: that’s up to your physician.

TESTOSTERONE: Testosterone is the FTM’s androgen of choice for a variety of reasons. It has excellent androgenic and anabolic properties, and is the substance that is produced naturally within your body. It does have a 5aR metabolite and an aromatase metabolite, so one should consider adding an anti-estrogenic agent if one is supplementing with supraphysiological doses of the drug. If you are prone to hair loss and/or male pattern baldness, you should also consider a 5aR inhibitor. Physicians specializing in hair loss can usually help you find an appropriate one. There are several different testosterone drugs, including testosterone cypionate (Depo-testosterone), testosterone enanthate (Testoviron/Delatestryl), testosterone propionate and testosterone decanoate. Testosterone cypionate and testosterone enanthate are the most common testosterone esters used by FTMs. One possibility that FTMs should consider is a drug called Sustanon 250, which is an injectable drug containing 250mg of four different testosterone esters. It might not be available in your country. Organon is reputable manufacturer of Sustanon 250, but there’s a whole bunch of fake Sustanon out there. Buy it from a REPUTABLE pharmacy. Omnadren 250 is a drug similar to Sustanon 250, but with one different ester that reduces the overall half life by a few days. Omnadren is also faked quite frequently.

NANDROLONE: At first glance nandrolone might seem to be a weird substance. It resembles both an androgen and an estrogen, but it has reasonably high anabolic effects. It is known to be a progestin, which might cause some undesirable effects in an FTM guy. Nevertheless, it is a reasonable choice, especially for guys who are concerned about hair loss or specifically about gaining muscle size. By far the most common nandrolone drug is the injectable Deca Durabolin, or nandrolone decanoate. This is without a doubt the most commonly counterfeited androgen, so definitely don’t buy it off of the street.

TRENBOLONE: I think this androgen fucking rocks. It seems to cause the fewest negative side effects and the maximum positive effects. Pound for pound it seems to be almost three times as effective as testosterone. It has no metabolic pathway to estrogens, and seems to have reasonably little negative effect on hair loss. Unfortunately it is very hard to get in most countries. One possibility is the drug Parabolan (trenbolone cyclohexylmethylcarbonate), an oil-based injectable. There are some agricultural drugs containing trenbolone, but…well, they’re not made for human use. Same drug, possibly fewer quality controls during the manufacturing process. And if you buy this on the black market (assuming that what you buy even contains trenbolone, and that’s quite an assumption to make) you’re probably buying something that some schmoe whipped up in his basement after extracting trenbolone acetate from cattle implants. Most of these schmoes know and care very little about making the drug safe. But Good Gravy, if you can find trenbolone then you should definitely ask your doctor for a prescription.

METHENOLONE: This is a weaker androgen, but a reasonable choice for FTM guys because it does not metabolize to an estrogen. It might increase the rate of hair loss, but seems to be less aggressive in this regard than testosterone. Primobolan Depot (methenolone enanthate) is the most common injectable preparation of methenolone. Primobolan is expensive.

OTHER ANDROGENS: There are quite a few oral androgens that I’m just not going to mention. Suffice to say that you should stay away from them if you can find injectables. If you are seeing a physician, just have him prescribe an injectable and show you how to inject it (or have him inject it for you).

CLOMIPHENE: Clomiphene seems to be a very effective anti-estrogenic compound. It is not an androgen. It is most commonly used in the treatment of breast cancer. It is an oral drug, but as it is not an oral androgen it does not have hepatotoxic effects. The most common drug preparation of clomiphene is called Clomid (clomiphene citrate). It is widely available around the world.

AMINOGLUTETHIMIDE: This is a drug that inhibits the action of aromatase, the enzyme that converts androgens to estrogens. At higher dosages, through another mechanism, it can inhibit the production of cortisol. This might sound good (cortisol is catabolic) but you need normal cortisol levels to be healthy. If you’re going to take aminoglutethimide, don’t take a lot of it, and have your cortisol levels checked regularly. The brand name for it is Cytadren. There are better anti-estrogenic choices such as tamoxifen and clomiphene, so really, don’t bother with it.

ANASTROZOLE: This compound works like aminoglutethimide in that it blocks the aromatization of androgens to estrogens, but it does not seem to have the same effects on cortisol. Its brand name is Arimidex. It is expensive but effective. I still think tamoxifen and clomiphene are better choices for anti-estrogens.

TAMOXIFEN: Tamoxifen is quite similar to clomphene. Most readily available under the brand name Nolvadex, and like clomiphene it blocks estrogen receptors in some tissues and activates them in others. (However, this activation in reality blocks the estrogenic effects anyway, so no worries.)

To summarize, keep all of this in mind the next time you talk to your physician:

S/he can probably double, triple or even quadruple your dosage of testosterone with great results and few negative effects, especially for periods of a few weeks or months.

There are drugs available that reduce estrogenic effects. You should consider them, especially if you are using testosterone.

There are other androgens available besides testosterone.

You should have your lipid, testosterone, estrogen and liver levels, as well as your blood pressure, checked regularly.

Enjoy! And if you try something like this, let me know what you experience. I would be particularly interested in your dosage patterns, drug choices, laboratory results and reports of the physical, mental and emotional changes you experience, because there is a real lack of good information out there for FTMs. I would love to put something together and issue a study, even if it’s an informal anecdotal study. And if you find a good physician who is willing to listen to and work with you, send me their name and contact information!! I am collecting a list of well informed and progressive doctors all over the world, and will publish that list in an upcoming issue of Trans-Health.

Glossary

Alkyl – An organic radical of the formula CnH(2n+1) that forms a single bond.

Anabolic – An effect that increases growth. For FTM purposes this usually refers to muscle growth, and should more specifically be described as “muscle anabolism.”

Androgenic – A “masculinizing” effect such as increased body hair growth.

17-alpha alkylated – A steroid that has an alkyl group attached at the 17alpha position.

Acute – A state or condition that comes on rapidly and disappears within a short amount of time.

Atherosclerosis – A cardiological arteriosclerotic condition resulting from fatty deposits on the walls of arteries. This can cause elevated blood pressure and dramatically increase the risk of heart disease.

Chronic – A state or condition that continues over an extended period of time.

Ester – In chemistry, an organic compound in which an oxygen is bonded to carbon atom(s). In practical terms relevant to our discussion of androgens, esters of drugs are more soluble in oil (important for many injectable drugs) and longer-acting because it appears that the body must remove the ester chain before the compound can act at androgen receptors.

Half-life – For our purposes, the amount of time it takes for a substance to be metabolically reduced to one half of its original concentration.

LDL – Low density lipoprotein, a.k.a. “bad cholesterol.” High LDL levels increase the risk of atherosclerosis.

HDL – High density lipoprotein, a.k.a. “good cholesterol.” High HDL levels seem to decrease the risk of heart disease. There is some evidence that high HDL levels can aid in treatment of athersclerosis.

Hepatotoxicity – Toxic to the liver

Hypertension – Chronically high blood pressure.

Intramuscular – A delivery mechanism in which a drug is intended to be injected directly into muscles.

Metabolic – An action that takes place inside the body.

Oral – A delivery mechanism that involves taking a drug by mouth.

Prodrug – A pharmacological term applied to drugs that require some kind of metabolic action to be converted to a form that can be used by the body.

Supraphysiological – Dosages that are greater than what the “normal, healthy” body will produce.

References and Interesting Research

1. Pope HG Jr, Kouri EM, Hudson JI. “Effects of supraphysiologic doses of testosterone on mood and aggression in normal men: a randomized controlled trial.” Arch Gen Psychiatry 2000 Feb;57(2):133-40; discussion 155-6.

2. Yates WR, Perry PJ, MacIndoe J, Holman T, Ellingrod V. “Psychosexual effects of three doses of testosterone cycling in normal men.” Biol Psychiatry 1999 Feb 1;45(3):254-60.

3. Hajjar RR, Kaiser FE, Morley JE. “Outcomes of long-term testosterone replacement in older hypogonadal males: a retrospective analysis.” J Clin Endocrinol Metab 1997 Nov;82(11):3793-6.

4. Sih R, Morley JE, Kaiser FE, Perry HM 3rd, Patrick P, Ross C. “Testosterone replacement in older hypogonadal men: a 12-month randomized controlled trial.” J Clin Endocrinol Metab 1997 Jun;82(6):1661-7.

5. Kouri EM, Pope HG Jr, Oliva PS. “Changes in lipoprotein-lipid levels in normal men following administration of increasing doses of testosterone cypionate.” Clin J Sport Med 1996 Jul;6(3):152-7.

6. Welder AA, Robertson JW, Melchert RB. “Toxic effects of anabolic-androgenic steroids in primary rat hepatic cell cultures.” J Pharmacol Toxicol Methods. 1995 Aug;33(4):187-95.

7. Rejeski WJ, Gregg E, Kaplan JR, Manuck SB. “Anabolic-androgenic steroids: effects on social behavior and baseline heart rate.” Health Psychol. 1990;9(6):774-91.

8. Grino PB, Isidro-Gutierrez RF, Griffin JE, Wilson JD. “Androgen resistance associated with a qualitative abnormality of the androgen receptor and responsive to high dose androgen therapy.” J Clin Endocrinol Metab. 1989 Mar;68(3):578-84.

9. Crist DM, Peake GT, Stackpole PJ. “Lipemic and lipoproteinemic effects of natural and synthetic androgens in humans.” Clin Exp Pharmacol Physiol. 1986 Jul;13(7):513-8.

10. Meyer WJ 3rd, Webb A, Stuart CA, Finkelstein JW, Lawrance B, Walker PA. “Physical and hormonal evaluation of transsexual patients: a longitudinal study.” Arch Sex Behav. 1986 Apr;15(2):121-38.

11. Forbes GB. “The effect of anabolic steroids on lean body mass: the dose response curve.” Metabolism. 1985 Jun;34(6):571-3.