The total amount of testosterone per ml is mg. Skip to content. Sustanon '' Testosterone propionate, phenylpropionate, isocaproate and decanoate Consumer Medicine Information What is in this leaflet This leaflet answers some common questions about Sustanon.
It does not take the place to talking to your doctor or pharmacist. If you have any concerns about using this medicine, ask your doctor or pharmacist.
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Advertisement Advertisement. Advertisement cookies are used to provide visitors with relevant ads and marketing campaigns. These cookies track visitors across websites and collect information to provide customized ads. Others Others. From the point of view of the testosterone esters in Sustanon , the most important carbon atom is in position Carbon number 17 on the testosterone molecule is where the secret sauce is added.
The shortest chain being testosterone propionate and the longest is testosterone decanoate. Because there are 10 carbon deca atoms in the chain. Sustanon is designed to provide an initial rapid increase in testosterone levels followed by a more extended release profile.
This is based on the different release characteristics of the testosterone esters. The rationale behind the use of testosterone esters is to prolong the therapeutic window following administration, which will lead to fewer injections compared to unesterified steroid injections. In these preparations, testosterone is esterified at the hydroxy position see above diagram.
This modification of the molecule decreases the polarity less water-loving making it more lipophilic fat-loving , thus making the molecule more soluble in the injection oil. This has the effect of slowing down the absorption of testosterone from the area of injection. Once in the bloodstream, the ester is removed hydrolysed — see below to release the free or active testosterone into the circulation, thereby creating a long-acting effect. The testosterone esters in Sustanon each have different pharmacokinetic profiles and elimination release half-lives.
Thus, each testosterone ester will diffuse into the blood in a sequence of increasing lipophilicity. This will, in effect, cause a steady-state of normalised testosterone levels.
Sustanon was designed to provide a more physiologic like testosterone level compared when the testosterone esters are used individually. So, when the testosterone propionate has been eliminated then the testosterone phenylpropionate would kick in, and so on. Sequential diffusion of the esters from the area of injection would in theory facilitate steady-state levels of testosterone.
Studies have shown that these preparations are actually more likely to cause a higher initial supraphysiological above normal peak in testosterone levels. That means that there is significant overlap between the esters. This will be discussed in further details below when we will analyse the pharmacokinetic release studies on Sustanon This is a drug which is only activated once the body performs an enzymatic action on it. In the case of Sustanon and other testosterone esters, it is a process called hydrolysis carried out by blood esterase enzymes.
Hydrolysing esters involves splitting them into carboxylic acids or their salts and alcohols by the action of water, dilute acid or dilute alkali. Once the testosterone esters in Sustanon have been hydrolysed, the testosterone is released and can then enter the general circulation. From the circulation, it can travel around the body to act on the androgen receptor AR inside cells. The unesterified testosterone, therefore, is the active substance for testosterone substitution therapy of male hypogonadism.
The term pharmacokinetics refers to how the body acts on the drug in terms of administration, distribution, metabolism and excretion.
This is summarised by the acronym ADME. So, while pharmacokinetics describes how the body processes the drug, pharmacodynamics refers to the action the drug does to the body. Plasma testosterone levels return to the lower limit of the normal range in males in approximately 21 days. After hydrolysis of the testosterone esters, the testosterone enters circulation in the plasma, or blood, where it hitches a ride on carrier proteins such as albumin and SHBG. Testosterone is metabolised to dihydrotestosterone via 5 alpha-reductase and oestradiol via the aromatase enzyme, which is found in adipose or fat tissue.
Excretion mainly takes place via the urine as conjugates of etiocholanolone and androsterone. These compounds then undergo the chemical processes of glucuronidation or sulfation which basically makes molecules more polar and hence easier to excrete in the urine. The data from the pharmacokinetic profiles suggest that Sustanon will provide a physiological level of testosterone for up to 21 days. This is in fact confirmed by numerous studies that found that Sustanon provided a rapid peak in testosterone levels Hours after injection and maintained physiological concentrations for approximately 21 days.
Esterification of the testosterone molecule at position 17, e. Comparisons of the absorption kinetics of different testosterone esters clearly show that the half-lives of the absorption of the esters increase when the esterified fatty acids have a longer chain. So, the longer the side chain at position 17, the longer the duration of action of the testosterone ester. This is exploited in Sustanon with each ester having a progressively longer chain. So, in theory when the shorter ester chains are being eliminated the intermediate esters are in the process of being absorbed.
Studies were able to show that after intramuscular administration, the testosterone ester is slowly absorbed into the general circulation and then rapidly converted to the active unesterified metabolite. The observation that the time at the injection site is the major factor determining the residence time of the drug in the body agrees with pharmacokinetic studies which demonstrated that the testosterone ester is absorbed unchanged from the injection depot in the muscle into the general circulation according to first-order kinetics, that is the rate of elimination of the drug is proportional to its concentration, with a long half-life time taken for the drug to reduce to half of its original concentration of h.
The ester is then rapidly hydrolysed in plasma, as could be shown by in vitro rat studies van der Vies [8] and in vivo human studies [9]. Although the rate of hydrolysis again depends to some degree on the structure of the acid chain, this process in comparison to the release from the injection deposit is far more rapid van der Vies So, the main determining factor affecting the activity of testosterone esters is the absorption of the testosterone ester from the site of administration into the plasma.
This is because in comparison the process of hydrolysis of the esters is rapid. Further proof of the rapid hydrolysis of the testosterone esters to the unesterified testosterone has been confirmed by studies which injected both testosterone and testosterone enanthate intravenously.
If there was a delay in the hydrolysis of testosterone enanthate then this would be reflected in a different pharmacokinetic profile. However, after intravenous injection of testosterone enanthate or testosterone, these compounds have similar pharmacokinetics.
Despite the rapid hydrolysis of the testosterone esters in the serum it is still possible to measure the concentration of the esters themselves. However, this requires a greater degree of sophistication and this method is used when testing for performance-enhancing drugs in sport. When testosterone ester preparations are applied, either orally or as a depot injection, the ester diffuses slowly into the bloodstream.
Although the cleavage process, by esterase enzymes, starts immediately, a detectable portion of the pro-drug, the testosterone ester itself, is still detectable in the blood. A clinical study was designed to investigate the detection window of injected testosterone esters as a mixed substance preparation Sustanon and as a single substance preparation in serum and plasma.
The study comprised of six participants who were either administered a single intramuscular injection of either mg testosterone undecanoate Nebido or a Sustanon It was found that all testosterone esters could be subsequently detected in the samples. The results of this study found that the depot effect of the testosterone ester preparation increases in proportion to the length of the ester side chain.
This is because the half-life of the absorption increases with longer chains. This is because once the testosterone esters have managed to diffuse into the plasma from the depot the hydrolysis occurs at a rapid rate. The following graphs illustrate the findings.
As expected, the shortest chained ester, testosterone propionate showed the most rapid elimination and shortest half-life. However, the ester could still be detected for at least 4 days in serum and plasma of all study participants receiving the drug.
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