Testosterone Replacement Therapy (TRT) – Part 2 – IronMag Bodybuilding & Fitness Blog

Testosterone Varieties and Supply & Supply Strategies

Overview
In testosterone remedy , testosterone (typically referred to as “T” for brief) might be administered into the physique in various methods. The commonest methodology is intramuscular (IM) injection with a syringe. Different supply strategies embrace transdermal utility by gel, cream, or patch utilized to the pores and skin; orally by swallowing tablets (this methodology is rare because it has been proven to have adverse results on the liver); sublingually/buccally by dissolving a pill beneath the tongue or towards the gums; or by a pellet inserted beneath the pores and skin. The T-delivery methodology used will depend upon the kind of treatment accessible within the nation of therapy, the well being dangers/advantages for the affected person of the supply methodology in query, private desire, and price.

Testosterone is just not saved by the physique for future use, so in an effort to preserve wholesome ranges, it have to be administered in timed intervals, and in acceptable dosages. Injectable and subcutaneous T pellets stay energetic within the physique the longest. Injectable T is often administered between as soon as per week to as soon as each three weeks, and subcutaneous T pellets are changed each 3-4 months. Transdermal T (patch, gel, or cream) is often utilized to the pores and skin in smaller every day doses; oral and sublingual/buccal T are additionally usually taken every day.

“Regular” testosterone Ranges
A person’s testosterone ranges are normally confirmed by a blood take a look at referred to as a “serum whole testosterone take a look at .” Testosterone exists in your bloodstream in two varieties– “sure” testosterone and “free” testosterone . The vast majority of sure testosterone within the physique is chemically sure to a protein referred to as “intercourse hormone binding globulin” (SHBG). The remaining sure testosterone within the system is generally sure to albumin, one other protein . Free testosterone is taken into account the “energetic” type of testosterone , as it’s not chemically hooked up to any proteins; thus, it’s available to bind to androgen receptor websites on cells.

A serum whole testosterone take a look at measures the full of those two types of T. What are thought of regular take a look at ranges of mixed sure and free testosterone in male our bodies can vary anyplace from 300-1100 ng/dl (nanograms per deciliter). Ranges will range with age and particular person components.

It’s helpful to additionally measure the extent of free testosterone within the system, as this can be extra indicative of how hormone remedy is progressing. Ranges of free testosterone can vary between 0.3%-5% of the full testosterone depend, with about 2% thought of an optimum stage. Ask your physician to examine for each whole and free ranges of testosterone in your system.

A observe of warning about tremendously rising your T dosage
Through the first months of T remedy, many males really feel impatient ready for modifications to occur. Some could contemplate doubling or tripling their dose, pondering that the extra they put in, the quicker the modifications will come. Nevertheless, dramatically rising your dose might need the impact of slowing your modifications. It is because extra testosterone in your physique might be transformed into estrogen by an enzyme referred to as “aromatase.” This conversion is a part of the physique’s pure suggestions system– if there may be an abundance of testosterone within the physique, it’s transformed (“aromatized”) to estrogen in an effort to preserve a “regular” hormonal stability. Subsequently, taking very massive doses of testosterone won’t be an excellent concept. Be affected person; if you’re not seeing ends in an inexpensive time period, and/or your T ranges are low, talk about modifying your dosage along with your physician.

Testosterone esters: what they’re and the way they work
A lot of the testosterone that’s prescribed for the needs of hormone remedy is within the type of testosterone “esters.” An ester is solely a reputation for a chemical compound that’s fashioned from response between a carboxylic acid and an alcohol. A easy chemical diagram of this response is proven under in Determine A. Determine B reveals the chemical construction of free testosterone (chemical method C19H28O2) in addition to two totally different esters of testosterone (testosterone cypionate and testosterone enanthate ).

There are a variety of various esters of testosterone , together with the generally prescribed injectables of testosterone enanthate and testosterone cypionate , as properly different esters reminiscent of acetate, propionate , phenylpropionate, isocaproate, caproate, decanoate, and undecanoate. Every of those totally different esters is a molecular chain composed of carbon, hydrogen and oxygen atoms. The principle distinction between the totally different esters is what number of carbon and hydrogen atoms make up the chain. For instance, the propionate ester consists of three carbons, 6 hydrogens, and a pair of oxygens, whereas the cypionate ester consists of 8 carbons, 14 hydrogens, and a pair of oxygens.

Esterification of testosterone is completed in an effort to enhance the solubility of testosterone in oil, which in flip slows the discharge of the testosterone from the location at which it enters the physique.

Testosterone, in its free, non-esterified kind, has poor solubility in both oil or water– although it may be suspended in water. Non-esterified testosterone is out there in an aqueous injectable kind with the drug identify “Aquaviron.” Nevertheless, this type of testosterone stays energetic within the physique for less than a really quick time period (solely a matter of hours, which is defined additional under). Due to this, it have to be injected every day in an effort to preserve a steady stage of testosterone within the blood. Subsequently it’s not often used for testosterone alternative remedy as an injectable.

After getting added an ester group to testosterone , it turns into even much less soluble in water and extra soluble in oil. Moreover, as a basic rule, the extra carbon atoms there are in an ester, the extra soluble the ester is in oil. For instance, testosterone propionate (with 3 carbon atoms within the ester group) is much less soluble in oil than testosterone cypionate (with 8 carbon atoms within the ester group). Keep in mind, that is basic, simplified rule for our functions herein; the solubility of a molecule will depend on structural components which might be past the scope of this part.

So, usually, the extra carbons the ester group has, the extra soluble in oil it turns into, and the much less soluble in water. The time period for this ratio between oil and water solubility known as the “partition coefficient”– the upper the solubility in oil, the upper the partition coefficient.

The partition coefficient of the ester in query is necessary as a result of is results how lengthy the drug itself stays within the system. If the testosterone transfers too rapidly from the oil to the blood, the result’s a sudden spike in testosterone which then quickly drops as soon as the dose has been used up. Within the instance of free testosterone injected into the muscle from a water suspension (as in Aquiviron, talked about above), the testosterone is basically instantly accessible to the bloodstream on account of its low partition coefficient, and thus there may be a direct spike of testosterone which is used up rapidly within the physique.

Testosterone cypionate, however, has a excessive partition coefficient. When injected into the muscle, the drug stays in its esterified kind in a deposit within the muscle tissue. From there, it would slowly enter the circulation as it’s picked up in small portions by the blood. As soon as the esterified testosterone is introduced into the blood stream, “esterase enzymes” cleave off the ester chain in a course of often called “hydrolization,” thus leaving the testosterone in its free kind to carry out its varied actions and results.

When individuals converse of whether or not a selected testosterone ester is “quick performing” or “gradual performing,” they’re normally referring to the partition coefficient/solubility in oil. As described above, esters with extra carbon atoms will usually be extra soluble in oil– they’re also known as “slow-acting” esters (they keep energetic within the system longer). Esters which might be much less soluble in oil are also known as “fast-acting” types of testosterone , referring to the truth that they’re extra rapidly accessible and used up within the blood stream.

For males who’re utilizing injectable testosterone, slow-acting esters are typically most popular, as fewer injections are wanted over time to maintain the blood ranges of T moderately fixed. Testosterone enanthate (7 carbons) and testosterone cypionate (8 carbons) each take about 8-10 days to be totally launched within the system, and so they’re usually injected as soon as each 7-14 days. Testosterone propionate (3 carbons) takes about 3-4 days to be totally launched within the system, and have to be injected in smaller doses at the least weekly if not twice weekly. For that reason it’s not typically prescribed for males in transition.

Testosterone Supply Strategies
Injectable testosterone – The dosage quantity and timing for injectable testosterone will rely largely upon which ester is getting used, in addition to the person’s personal response to the hormone. Usually, dosages will range between 50 mg and 300 mg per injection , relying on the ester and the dosing routine. A mean injectable dose is about 200-250 mg each two weeks, although many trans males inject 100 mg each week or each 10 days, or different variations relying on their very own our bodies’ wants and sensitivities. Once more, the precise dosage required will range from individual to individual, and well being and well-being needs to be fastidiously monitored whereas figuring out a person’s superb dose.

Some docs suggest reducing the dosage of injectables to 100-150 mg each two weeks for these trans males whose ovaries are inactive, or who’ve had their ovaries eliminated. Once more, this may range from individual to individual.

There are a variety of several types of injectable testosterone ; these accessible could differ relying on the nation during which you reside. The drug names for a similar ester of testosterone may differ relying on the corporate who produces it. This isn’t an exhaustive record, although it does cowl the principle injectable types of T that are utilized by trans males for testosterone remedy .

Lastly, testosterone esters are usually suspended in both cottonseed oil or sesame seed oil. Some individuals discover that they could have an allergic response to one of many oils, or they could discover that their zits will increase or decreases relying on the kind of oil they use. Sure brand-name testosterone esters are mass produced utilizing one oil or the opposite (as famous under), however by utilizing a compounding pharmacy, you may have any testosterone ester suspended in your selection of oil (with a correct prescription).

Injectable esters generally used for testosterone remedy:

Testosterone enanthate: Chemical method C26H40O3
Testosterone enanthate is among the most important types of testosterone prescribed to males in the US. It’s a slow-acting ester with a launch time between 8-10 days. The name-brand of T-enanthate accessible in the US known as “Delatestryl,” which is suspended in sesame oil. Testosterone enanthate is often injected anyplace between as soon as each week to as soon as each three weeks. Generic testosterone enanthate can be obtained by a compounding pharmacy; such pharmacies can combine the enanthate in both sesame or cotton seed oil.

Testosterone cypionate: Chemical method C27H40O3
Testosterone cypionate is the opposite most important injectable type of testosterone prescribed tomen in the US. It’s a slow-acting ester with a launch time between 8-10 days, just like that of enanthate . The name-brand of T-cypionate accessible in the US known as “Depo-Testosterone ,” which is suspended in cottonseed oil. Testosterone cypionate is often injected anyplace between as soon as each week to as soon as each three weeks. Generic testosterone cypionate can be obtained by a compounding pharmacy; such pharmacies can combine the cypionate in both sesame or cotton seed oil.

Sustanon 100 or 250
“Sustanon ” is the model identify for 2 formulation of injectable testosterone that comprise a mix of esters. “Sustanon 100” comprises three testosterone esters: testosterone propionate (C22H32O3), testosterone phenylpropionate (C28H36O3), and testosterone isocaproate (C25H3803). “Sustanon 250” comprises 4 testosterone esters: testosterone propionate (C22H32O3), testosterone phenylpropionate (C28H36O3), testosterone isocaproate (C25H3803), and testosterone decanoate (C29H4603). Each formulation characteristic each fast-acting and slow-acting esters, and might be injected anyplace from as soon as each week to as soon as each 4 weeks. Sustanon is prescribed outdoors of the US.

Different injectable esters of testosterone:

Testosterone propionate: Chemical method C22H32O3
Testosterone propionate is a fast-acting ester with a launch time of 3-4 days. To maintain blood ranges from fluctuating tremendously, propionate is normally injected between one to a few instances per week. It is for that reason that it’s not normally prescribed hormone remedy . Some customers additionally report that propionate is a extra painful injection , with swelling and noticeable ache across the injection website. Model names of testosterone propionate embrace “Testovis” and “Virormone.”

Testosterone phenylpropionate: Chemical method C28H36O3
Testosterone phenylpropionate is a slow-acting ester, with a launch time of 1-3 weeks. A preferred identify model for T-phenylpropionate is “Testolent .” Testosterone phenylpropionate can also be one of many elements of Sustanon and Omnadren .

Omnadren
“Omnadren ” is the model identify for a mix of 4 testosterone esters: testosterone propionate (C22H32O3), testosterone phenylpropionate (C28H36O3), testosterone isocaproate (C25H3803), and testosterone decanoate (C29H4603). Previously, Omnadren consisted of a mix of various esters, however now could be primarily the identical method as Sustanon , talked about above. It options each fast-acting and slow-acting esters, and might be injected anyplace from as soon as each week to as soon as each 4 weeks. It’s typically prescribed in components of Europe.

Aqueous testosterone suspension
In the US, injectable aqueous (non-esterified) testosterone is out there, however it is rather short-acting (it’s utterly launched within the system inside a matter of hours). Subsequently, it’s not usually used for males in transition, as it could require fixed re-injection to take care of common blood ranges. The model identify for aqueous testosterone suspension is “Aquaviron.”

Transdermal testosterone
The time period “transdermal” refers to topical testosterone supply by the pores and skin, by means of a patch, gel, or cream.
Transdermal testosterone is normally utilized to the pores and skin every day in small doses in an effort to maintain a gradual stage of testosterone within the system always. This strategy avoids the “peaks and valleys” in T-levels typically related to injectable testosterone . With injectables, T ranges can attain a low-point just a few days earlier than the following shot is due, which may trigger irritability, scorching flashes, and low vitality in some customers. Day by day transdermal utility can assist alleviate such issues. Certainly, some males who frequently use injectable testosterone typically complement with a gel or patch throughout the previous few days of their dosing cycle to take care of their T ranges.

Transdermal utility can also be engaging to these people who are usually not snug with needles and injections .

Nevertheless, there are some disadvantages to transdermal supply. Some types of every day transdermal testosterone utility, significantly the patch, are considerably costlier than injectable testosterone . Testosterone patches typically trigger pores and skin irritation and/or allergic reactions to customers. They’ll fall off with extreme sweating, and so they have to be totally protected with plastic when swimming. Testosterone cream and gel might be transferred by direct pores and skin contact with a companion; particular care have to be taken with feminine companions who want to keep away from potential virilization.

Testosterone patches
There are at the moment two brand-name testosterone patches accessible in the US: “Androderm” and “Testoderm.” (Be aware that there are two types of Testoderm accessible: a scrotal patch and a non-scrotal patch. The non-scrotal patch, “Testoderm TTS,” is described herein). Generic testosterone patches are usually not but accessible. Each Androderm and Testoderm TTS are very fast-acting as soon as they’ve permeated the pores and skin. The testosterone within the patches is suspended in an alcohol-based gel.

With a view to ship the testosterone effectively into the physique, chemical enhancers are added to the patch to extend permeability of the pores and skin. It’s these enhancers which might be typically the reason for pores and skin irritation in lots of customers. Some people discover Testoderm TTS to be much less irritating to the pores and skin than Androderm, however this may range from individual to individual.

Androderm
Androderm patches are available two doses: 2.5 mg/patch and 5.0 mg/patch. The precise quantity of testosterone within the 2.5 mg patch is 12.2 mg, and the precise quantity within the 5.0 mg patch is 24.3 mg. The reason being that a lot of the testosterone within the patch is not going to handle to get into the system. So, for instance, the purpose of the two.5 mg patch is to get about 2.5 mg efficiently into the bloodstream per day. Subsequently, it’s potential to soak up barely extra or barely lower than the two.5 mg of the patch’s superb dosage (the identical reasoning, in fact, applies to the 5.0 mg patch as properly).

Androderm patches are normally utilized on the again, stomach, thighs, or higher arms. As a result of the energetic space of the patch is roofed, the wearer doesn’t have to fret about pores and skin contact with a companion. Dosages will range between 2.5 mg – 10 mg every day, by making use of a single patch or mixture of patches. As with every type of testosterone , dosage needs to be decided by your general well being, your testosterone ranges as checked by your physician, and your progress in masculinization.

Testoderm TTS
There are two sorts of Testoderm patches: one is meant for scrotal utility, and one for utility on different areas of the physique. Testoderm TTS refers back to the non-scrotal model of the patch– that is the patch that needs to be utilized by males.

Testoderm TTS patches are available two doses: 4.0 mg/patch and 6.0 mg/patch. As with Androderm, the precise quantity of testosterone in these patches is bigger than the listed dose. The reason being the identical as defined above within the Androderm part.

Testoderm TTS patches are normally utilized on the again, stomach, thighs, or higher arms. As a result of the energetic space of the patch is roofed, the wearer doesn’t have to fret about pores and skin contact with a companion. Dosages will range between 4.0 mg – 10 mg every day, by making use of a single patch or mixture of patches. As with every type of testosterone , dosage needs to be decided by your general well being, your testosterone ranges as checked by your physician.

Testosterone gel and cream
There are at the moment two brand-name variations of testosterone gel accessible in the US: Androgel and Testim. There aren’t any brand-name testosterone lotions right now. Each cream and gel formulations of testosterone might be made by compounding pharmacies. (For extra details about compounding pharmacies, click on right here.) Gel formulations of testosterone are usually alcohol-based, whereas lotions are usually safflower oil-based. The testosterone in lotions and gels is often very fast-acting as soon as absorbed by the pores and skin. Thus, it have to be utilized a few times every day to take care of T ranges.

Lotions and gels are utilized straight onto the pores and skin. Care have to be taken to keep away from skin-to-skin contact with a companion on the location of utility. Switch of the testosterone from the location might be prevented by protecting the realm coated.

Androgel
Androgel is a transparent, alcohol-based gel that comprises 1% non-esterified testosterone . It is vitally fast-acting as soon as it has been absorbed by the pores and skin, and so have to be utilized 1-2 instances every day to take care of T ranges. It’s accessible in both unit-dose packets or multiple-dose pumps. The unit dose packets comprise both 25 mg or 50 mg of testosterone . Roughly 10% of the utilized testosterone from the packets is absorbed into the system, leading to an efficient dose of two.5 mg or 5.0 mg, respectively.

Androgel needs to be utilized to wash, dry pores and skin and shouldn’t be utilized to the genital space. Software websites needs to be allowed to dry for a couple of minutes previous to dressing. Fingers needs to be washed completely with cleaning soap and water after utility.

With a view to stop switch to a different particular person, clothes needs to be worn to cowl the applying websites. If direct skin-to-skin contact with one other particular person is anticipated, the applying websites needs to be washed completely with cleaning soap and water. Customers ought to wait at the least 2 hours after making use of earlier than showering or swimming; for optimum absorption, it might be finest to attend 5-6 hours.

Testim
Testim, like Androgel , is a transparent, alcohol-based gel that comprises 1% non-esterified testosterone . It is vitally fast-acting as soon as it has been absorbed by the pores and skin, and so have to be utilized 1-2 instances every day to take care of T ranges. It’s accessible in 5.0g unit-dose tubes. A 5.0g unit dose tube comprises 50 mg of testosterone . Roughly 10% of the utilized testosterone from the tube is absorbed into the system, leading to an efficient dose of 5.0 mg.

Testim needs to be utilized to wash, dry pores and skin– ideally to the shoulders and/or higher arms. It shouldn’t be utilized to the genitals or to the stomach. Software websites needs to be allowed to dry for a couple of minutes previous to dressing. Fingers needs to be washed completely with cleaning soap and water after utility.

With a view to stop switch to a different particular person, clothes needs to be worn to cowl the applying websites. If direct skin-to-skin contact with one other particular person is anticipated, the applying websites needs to be washed completely with cleaning soap and water. Customers ought to wait at the least 2 hours after making use of earlier than showering or swimming; for optimum absorption, it might be finest to attend 5-6 hours.

Compounded lotions and gels
Compounded lotions and gels might be combined by compounding pharmacies, and are related in dosing, utility, and precautions to what’s described above for Androgel and Testim.

There are two benefits of utilizing compounding pharmacies for testosterone gel or cream. The primary is value: till a generic model of the gel is out there, compounded gel will normally be the cheaper different. The second is customization: your physician can write a prescription of various focus for gels or lotions.

Oral testosterone
Methyltestosterone (C-17 alpha methylated testosterone )
Methyltestosterone is among the earliest accessible oral testosterones. Its chemical construction is the hormone testosterone with an added methyl group on the c-17 alpha place of the molecule. The usage of oral c-17 alpha methylated testosterone for masculinization is out of date on account of its toxicity to the liver. As such, methyltestosterone is just not really useful for FTM hormone remedy . Model names embrace “Metesto,” “Methitest,” “Testred,” “Oreton Methyl,” and “Android.”

Testosterone undecanoate
Testosterone undecanoate is just not a c-17 alpha alkylated hormone . Subsequently, it’s thought of a safer oral type of testosterone . It’s designed to be absorbed by the small gut into the lymphatic system, posing much less burden on the liver. Model names for testosterone undecanoate embrace “Andriol ,” “Androxon,” “Understor,” “Restandol,” and “Restinsol.” It isn’t accessible in the US.