Testosterone Esters and Injection Protocol's...What you and your Doctor need to know.

[steroid.com 1]

The following extracts explains the PK/PD of testosterone esters and describes the marked fluctuations with injection and transdermal administration. It strongly supports the weekly injections administration schedule, NOT biweekly or longer. If you have a Doctor who has you on any injection protocol longer then days you must have him/her read this study. Also note the LH/FSH suppression all studies noted.

Testosterone enanthate and testosterone cypionate are long-acting testosterone esters suspended in oil to prolong absorption. Peak levels occur about 24-72 hours after intramuscular injection and are followed by a slow decline during the subsequent 1 to 2 weeks. http://www.testosteroneupdate.org/mi...highlights.pdf

Nakazawa R, Baba K, Nakano M, et al. Hormone profiles after intramuscular injection of testosterone enanthate in patients with hypogonadism. Endocr J 2006;53(3):305-10. http://www.jstage.jst.go.jp/article/.../53/3/305/_pdf

To examine hormone levels after androgen replacement therapy (ART) in Japanese male patients with hypogonadism, nine Japanese male patients with hypogonadism (serum total testosterone (tT) or free testosterone (fT) levels of < or = 2.7 ng/mL or < or = 10 pg/mL, respectively; average age, 59 years) were enrolled. They were treated with 125 mg of testosterone enanthate by single intramuscular injection. Blood samples were collected on the morning of the day of treatment, pre-ART, as well as on days 1 to 7 and day 14 after administration.

Serum levels of tT, fT, estradiol (E2), follicle-stimulating hormone (FSH), luteinizing hormone (LH), and sex hormone-binding globulin (SHBG) were determined. On day 1 after administration, the mean serum levels of tT and fT were 7.62 ng/mL and 23.22 pg/mL, respectively. Serum levels of tT and fT on day 14 after administration were lower than their pre-ART values. One patient exhibited abnormally high serum tT and fT levels of 19.6 ng/mL and 44.4 pg/mL, respectively. Serum levels of LH and FSH began to decrease gradually on day 5 after administration. Serum levels of SHBG did not change throughout the observation period. Serum levels of E2 increased 1.7 times on day 1 after administration but returned to its pre-ART value by day 14 after administration.

The dose of testosterone enanthate for male patients with hypogonadism requiring ART should be determined carefully because some patients exhibited high serum levels of androgen beyond the physiological range and gonadotropin was suppressed in all treated patients (GD: Noted here at HPTA suppression and why HCG is needed to keep the testes functioning).

Weinbauer GF, Partsch C-J, Zitzmann M, Schlatt S, Nieschlag E. Pharmacokinetics and Degree of Aromatization Rather Than Total Dose of Different Preparations Determine the Effects of Testosterone : A Nonhuman Primate Study in Macaca fascicularis. J Androl 2003;24(5):765-74. http://www.andrologyjournal.org/cgi/.../full/24/5/765

Currently available testosterone (T) preparations differ substantially in their pharmacokinetic profile that might influence their androgenic properties in terms of suppression of the gonadal axis, effects on anabolic parameters, lipid metabolism, and erythropoiesis. The present work was undertaken to determine the physiological effects of three T preparations with different serum kinetics. Twenty adult male cynomolgus monkeys (Macaca fascicularis) were randomly assigned to receive treatment for 28 weeks with either T enanthate (TE) every 4 weeks, T buciclate (TB) every 7 weeks, or T undecanoate (TU) every 10 weeks orremaining untreated (controls). Each injection delivered 20 mg pure T per kilogram body weight. Pharmacokinetic profiles demonstrated higher peak levels of T for TE-treated animals; serum half-lives were longer for TU or TB. Estradiol levels (area under the curve) were significantly higher in TB vs TU or TE. All T regimens suppressed serum luteinizing hormone bioactivity and testicular volumes declined (all P < .001 vs controls). Sperm counts were markedly lowered in all animals but least in TE (P < .01 vs TB or TU). During recovery phase, return to normal for all three parameters occurred significantly earlier in TE-treated animals, followed by those given TU,compared with TB (all P < .001 between groups). Body weight increased significantly during T exposure. This effect was stronger and more sustained in TB vs TU or TE (both P < .001). Serum creatinine and hemoglobin increased with highsignificance in all T-treated animals (all P < .001 vs controls). The lowering impact of T on serum lipids was markedly stronger in the longer-acting T preparations in comparison with TE, as were effects on purine metabolism (all P < .001). The pattern of exposure and degree of aromatization rather than overall exposure to T determine its effects in the preclinical primate model. Both fluctuations of androgen concentrations and the conversion rate to estradiol influence gonadal suppression as well as metabolism. These results have to be considered in men receiving treatment for hypogonadism or regimens for hormonal contraception.

Dobs AS, Meikle AW, Arver S, Sanders SW, Caramelli KE, Mazer NA. Pharmacokinetics, Efficacy, and Safety of a Permeation-Enhanced Testosterone Transdermal System in Comparison with Bi-Weekly Injections of Testosterone Enanthate for the Treatment of Hypogonadal Men. J Clin Endocrinol Metab 1999;84(10):3469-78. http://jcem.endojournals.org/content/84/10/3469.full

The pharmacokinetics, efficacy, and safety of the Androderm testosterone (T) transdermal system (TTD) and intramuscular T enanthate injections (IM) for the treatment of male hypogonadism were compared in a 24-week multicenter, randomized, parallel-group study. Sixty-six adult hypogonadal men (22–65 years of age) were withdrawn from prior IM treatment for 4–6 weeks and then randomly assigned to treatment with TTD (two 2.5-mg systems applied nightly) or IM (200 mg injected every 2 weeks); there were 33 patients per group. Twenty-six patients in the TTD group and 32 in the IM group completed the study.

TTD treatment produced circadian variations in the levels of total T, bioavailable T, dihydrotestosterone, and estradiol within the normal physiological ranges. IM treatment produced supraphysiological levels of T, bioavailable T, and estradiol (but not dihydrotestosterone) for several days after each injection. Mean morning sex hormone levels were within the normal range in greater proportions of TTD patients (range, 77–100%) than IM patients (range, 19–84%). Both treatments normalized LH levels in approximately 50% of patients with primary hypogonadism; however, LH levels were suppressed to the subnormal range in 31% of IM patients vs. 0% of TTD patients. Both treatments maintained sexual function (assessed by questionnaire and Rigiscan) and mood (Beck Depression Inventory) at the prior treatment levels.

Prostate-specific antigen levels, prostate volumes, and lipid and serum chemistry parameters were comparable in both treatment groups. Transient skin irritation from the patches was reported by 60% of the TTD patients, but caused only three patients (9%) to discontinue treatment. IM treatment produced local reactions in 33% of patients and was associated with significantly more abnormal hematocrit elevations (43.8% of patients) compared with TTD treatment (15.4% of patients). Gynecomastia resolved more frequently during TTD treatment (4 of 10 patients) than with IM treatment (1 of 9 patients).

Although both treatments seem to be efficacious for replacing T in hypogonadal men, the more physiological sex hormone levels and profiles associated with TTD may offer possible advantages over IM in minimizing excessive stimulation of erythropoiesis, preventing/ameliorating gynecomastia, and not over-suppressing gonadotropins.

[*Admin*]

Great information thanks!!!

[austinite]

Awesome GD.

Folks, this is also a sticky in case you're ever looking for it.

[steroid.com 1]

Not just to educate members and visitors (and visitors should become members!) but for men to use to educate their Doc's on correct injection protocols and drug half life.

The sticky is locked down so if you want to comment and keep this thread alive post in here as you can't in the sticky!

gd

[EverettCD]

Great information as usual. Thank you for posting!!!

[VTX1800]

GD TO THE RESCUE!!!! Great info brother, thanks for posting.

[rockmon]

Thanks GD, very useful information.

[jackkerouc]

What's your definition of biweekly?
Merriam-Websters defines biweekly as:
1. Occurring twice a week
2. Occurring every two weeks

[steroid.com 1]

What's your definition of biweekly?
Merriam-Websters defines biweekly as:
1. Occurring twice a week
2. Occurring every two weeks

1. Occurring twice a week. Better would have been "twice weekly" I like that because even Pharmacy's get it wrong and think it's number 2.

[phaedo]

1. Occurring twice a week. Better would have been "twice weekly" I like that because even Pharmacy's get it wrong and think it's number 2.

^ very true! I've had several pharmacies call my doctor to "confirm" the twice weekly perscription, since the silly medical standard is 200
mg injection once every other week! Good thread, btw.

[Sunwind]

What do I need to say to my endocrinoligst to get myself on more frequent injections? I have a broken pituitary and take an injection once every 3 months. Obviously this goes against the whole thread saying you should be having it WEEKLY. So why is a specialist giving it me every 3 months? is it less expensive? I read the thread, but all the numbers and information there is way over my head - i'm not a doctor, but I need some solid literature or writing to take with me to my next appointment.

[JuicDinNY]

I LOVEEEEEEEEE THIS THREAD!!!!!! I am NEW on here and very well informed on TRT and HRT in general and the "doctors and specialists" here on Long Island are CLUELESS to what the F they are doing when it comes to dosing!!!! I have LITERALLY been to about 7-10 "Hormone Docs" or "endos" and they ALL would not give more then 1cc/200mg EVERY 2 weeks!
My latest doc I had to leave due to this! Before writing you the "take home" rx, he does in office injections with FREQUENT blood labs to monitor how your entire body is reacting especially as it adjusts to the new exogenous hormone. Completely Understandable!!! What is NOT UNDERSTOOD by myself or ANYONE else i ask is the fact that during this 8 week "Trial" in office to assess my levels and how they rise and fall in order to find MY correct dosing since my LH and FSH are COMPLETELY non existent, literally, or shut off due to alot of bs and ignorant stuff in the past, it can be a little tricky to find the right dose which is fine.
The thing I have an issue with is the fact that this "doctor" saw on the labs that i spike after the injection to around 800-1100 approx and then by day 6 or 7 or 8 I severely, not gradually, plummet back down to double digit totals! Anyone on here who knows anything at all and has been there and done that knows how TERRIBLE you feel for lack of better terms.
With my Labs in front of both of us and his little fake assistant(keep in mind this happened at multiple doctors so has been going on for well over a year now) and SEES as an intelligent, well educated DOCTOR, the patterns of my levels and how the Roller Coaster ride of hormones inside me is not good at all at the 2 week dose. Long story short, I finally told him how I felt about him and his wonderful practice and was released from his practice for good LOL
The GOOD news is I finally found a good TRT doc who deals with a lot of UFC fighters which I find pretty cool and has worked with a lot of former and current big name pro ifbb bodybuilders so I knew he had a better grasp on the REAL DEAL and what goes on with this stuff. Not to mention hes like 260lbs and chizzled like an Under Armour Manican!!! lol I FINALLY am on a WEEKLY dose and already feel so much better and more steady and consistent with energy levels, libido and just mental clarity.
THANK YOU VERY MUCH for the POST!!!! Love seeing things like this and I hope one day we can get something like this seen PUBLICLY by as many people as a JUSTIN BIEBER video on Youtube or Gangham Style that got ONE BILLION+ hits on YouTube and is useless. If this is seen by SO many people and goes NATIONALLY or INTERNATIONALLY even, issues like this might get back to the doctors and make them open their know it all ignorant minds and start doing the right thing for their patients!!!!
Thanks again man SICKKKK post! Keep em coming! Lets start an AWARENESS CAMPAIGN I am serious I will help run it! For the publics knowledge to maybe change on the misconceptions due to abuse and horror stories of overdosing and also to get to the doctors minds and see that maybe the thousands of patients telling them they feel like crap really aren't lying after all. LOVE IT!

[keep fightin]

great post GD! have a doc friend who couldnt do shots and am shooting him this work right now , perfect timing!

[Novice489]

Both treatments normalized LH levels in approximately 50% of patients with primary hypogonadism; however, LH levels were suppressed to the subnormal range in 31% of IM patients vs. 0% of TTD patients

TTD treatment did not suppress LH to subnormal values? I thought all exogenous T would eventually shut down HPTA. Can someone shed some light.

[Dale38]

I was just diagnosed with low t.. My doctor is having me inject 100mg of test every 2 weeks. And then a blood drow in 6 weeks. Now is this dosing just a starting phase? I am having a difficult time understanding every 2 weeks

[Lifted1]

I was just diagnosed with low t.. My doctor is having me inject 100mg of test every 2 weeks. And then a blood drow in 6 weeks. Now is this dosing just a starting phase? I am having a difficult time understanding every 2 weeks

for the best responses you should start a thread, but thats not going to do anything except make you feel like shit. you need to be injecting atleast 100mg per week, preferably split into 50mg shots every 3.5 days. if you like your testicles the way they are, your gonna need hcg too. gL