Testosterone (ester mixture) (Testosterone mixture of esters)
Before you begin to talk about the properties of all testosterone esters, you must warn the reader about the dangers of using steroid drugs, since the use and distribution of steroid drugs can lead to criminal liability
Ether is a compound of carbon and hydrogen (CH-type, for example, CH3OCH3 - Dimethyl ether), which is attached via a hydrogen bond to the molecular structure of a substance that reacts with ether, in our case, ether with hormonal anabolics, to assign it the necessary chemical qualities (slow dissolution of the drug in the blood). Many of the hormonal anabolics are almost instantly destroyed in the human body. From this it follows that injections of the male-free hormone testosterone must be administered every day, due to this treatment with such drugs can be difficult.
To facilitate the use of special drugs that inhibit the reaction of testosterone with blood and containing hormonal steroids with the addition of an ether formula and an oil mixture. Esters have the properties of lipophilicity (they interact well and react with oil) and hydrophobicity (do not dissolve in water), that is, in water the reaction of dissolution of the molecular structure (hormonal steroid (testosterone) and essential oil) will occur slowly. With intramuscular injections, the same delayed dissolution in the muscle and the gradual excretion of the anabolic in the blood occurs. The duration of absorption of the steroid preparation depends on the half-life of the ether combined with it. The elimination half-life is the period of time during which the amount of essential substance in the human body after a single injection is halved (1 2 of the drug administered is removed from the blood).
There are a large number of short (in structure) esters that differ with each other only in the half-life (period). More complex esters with an elongated structure mix up much faster with various oils, due to their increased lipophilic ability, while they have a short period of entry into the blood and an increased half-life (period). Such an ether acts in time for approximately slightly less than two half-lives. From this it follows that the larger the structure of the ether and its chains, the longer the administered drug lasts. Ethers affect only the duration of the action of the hormonal drug in the blood; esters in combination with anabolic agents do not give more benefits.
The length of the esters is of great importance, the longer the carbon chain of the ester, the greater the molecular weight of the substance in solution with an anabolic steroid. The mass of ether in the solution is about 15-30%. For example, if you take the main doses of anabolic drugs, then 0.25 grams of testosterone enanthate will approximately 0.18 grams of steroid and approximately 0.07 grams of ether (Enanthate occupies 28% of the total weight of the solution). You can also calculate the amount of other ethers and the main substance.
- Acetate (13%)
- Propionate (17%)
- Enanthate (28%)
- Cypionate (30%)
- Phenylpropionate (33%)
- Decanoate and Undecanoate (36%)
Testosterone ester formation:
The half-life of a testosterone molecule is approximately a few minutes. The formation of an ester occurs under conditions when an acid residue is attached to the site of the H atom in the testosterone structure (for example, let it be enanthic). The result is an anabolic drug called Testosterone Enanthate.
|Title||The value of the Wyszkowski Index ®|
|Omnadren ® 250||0.075|
|Testenat for injection 10%||0.0008|
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What it is?
As a result of a chemical reaction of a carboxylic acid molecule with an alcohol molecule, ether is formed with the release of water. The testosterone ester is a carboxylic acid residue attached to the alcohol group of the steroid molecules.
It gives the steroid a specific pharmacological property: organized storage of substances with the goal of subsequent slow release into the blood.
The vast majority of steroids rapidly decay in the body. To better control this process, depot preparations were created, which are an oil-based steroid + ether tandem.
This combination significantly slows the release of the steroid. This is due to the fact that the ether is poorly soluble in water and, getting in the oily state in the aquatic environment, it begins to pass very slowly with the steroid into the body.
Slow release of the substance is a significant plus from a medical point of view. Many hormones (including free testosterone) break down in the body in a few hours. To maintain them at a certain level, it would be necessary to give injections very often, but adding ether to the hormone can reduce the number of injections to 1 time per week (month).
The half-life of testosterone ester is the time period during which its content in the blood is halved. It does not mean the absolute end of the period of the drug in the body. This indicator is used to calculate the course of admission.
The half-life is based on the number of carbon atoms in the chain. By attaching various esters to the base of testosterone, we essentially attach a certain number of carbon atoms. It is a non-polar compound, with weak electronegativity.
Its outer shell has 4 electrons that interact poorly with other electrons. When more atoms are added, the non-polarity of the compound increases and, based on this, its ability to dissolve in water (in blood) is greatly reduced.
In simple terms, the more carbon atoms, the less polarity and worse the solubility in a liquid medium, but better in a "non-polar" butter.
It will be appropriate to say that The half-life depends on the length of the chain of carbon atoms, which is different for all ethers. The longest at Undecanoate. Its number of carbon atoms is eleven. And, for example, propionate has only three such atoms, which makes it a relatively instant testosterone ester, i.e. it can be called short.
The half-life is from 19 to 21 days. It has the highest duration of exposure to the body. Up to 14 weeks on an oil basis and up to 2 weeks on an aqueous basis. High conversion to dehydrotestosterone, which can lead to the development of unpleasant consequences.
Testosterone undecanoate is recommended as part of the hormone replacement course in men with a lack of male hormones that occurs in connection with old age or in connection with pathologies of the genital glands. Can not be used for carcinoma of the breast or prostate.
Introduced by the French company Catalent France Beineim called Andriol. It has the form of capsules, in the amount of 60 pcs, with a concentration of 40 mg. Also available in the form of 250 mg Nebido injections by Bayer.
Medications should only be prescribed by a doctor. All names are for informational purposes only.
The half-life is from 15 to 16 days. Pretty common broadcast. It has the ability to retain water in the body. The peculiarity of its use is that, due to the danger of conversion to estrogens, it is used in conjunction with arotamase blockers.
Used by doctors in testosterone replacement therapy, eg:
- for violations in the reproductive system,
- prostatic hypertrophy,
- during the period of male menopause.
It is produced in the form of ampoules with an oil solution under the same name by the Genesis company (Poland) with a concentration of 200 mg.
Varieties of ethers:
Below are the most popular esters used with esters:
- Acetate - Acetic acid ester, has the shortest half-life (about 24 hours). In combination with acetate, Primobolan, Trenbolone, Anotrophin, Stenbolone, Trenbol, Finaject are usually used.
- Propionate - It is one of the most common esters, due to the frequent use by athletes of a steroid drug called Testosterone Propionate. Also often used with this ether are Methandriol, Masteron (Drostanolone), Mastabol, Masterid, Mastizol, Masteril, Metolon, Drolban, Masterin, Permastril, Androlan, Virormon, Testenon, Testoviron, Testenat, Methandriol, Agovirin, Androlan, Nombreolt, Androfon Pri, , Testopin and many others. The half-life ranges from 24 to 48 hours.
- Phenylpropionate - Ether is essentially an improved propionate formula. Nandrolone, Omnadren, Sustanon are more often synthesized and combined with this ether (phenylpropionate). It produces Anabolin, Dubol, Durabolin, Superanabolin, Phenobolin, Equibolin, Activin, Androlon, Nandrobolin, Turinabol, Nerobolin, Ferbolico, Durandron from this ether. The half-life of this essential oil is already 48-72 hours.
- Isocapronate - Used in Omnadren, Sustanon and Estandron.
- Enanthate - It is also very famous and is used with methenol, trenbolone and other anabolics. The elimination half-life is approximately equal to a week or a little less.
- Hexahydrobenzyl carbonate (Hexahydrobenzyl carbonate) - The ether has a structure of eight carbon atoms, the half-life is approximately equal to a week, similar in its characteristics to Enanthate. It is used with Trenbolone or Parabolan.
- Cypionate - It is also very similar in properties to Enanthate. These two ethers freely replace each other. The elimination half-life is about a week.
- Decanoate - used with Nandrolone and Sustanon. One of the longest running ethers, the half-life is already more than a week (about 9 days). To maintain a steady concentration of anabolic steroid in the blood, intramuscular injection is performed approximately once every week during the entire course.
- Laurat - The longest running broadcast, which is used in sports. The half-life is already 10 days, some sources claim a 12-day work of the ether in the human body. It is used with Nandrolone, in Laurabolin.
The half-life is from 10 to 14 days. Very common among athletes. It is used in medicine to treat impotence, male infertility, which is a consequence of problems with spermatogenesis and with an insufficient level of androgens.
It is believed that it does not have a detrimental effect on the liver, but if there are pathologies in it, it is not recommended to use it. Also, it can not be used:
- with sick kidneys,
- with nephrosis,
- oncological diseases of the prostate gland,
- prostatic hypertrophy,
- atherosclerosis, etc.
Now it is not released on its own. It is part of Sustanon 250 from ORGANON, which is in the form of oil-based ampoules. It contains a mixture of esters including decanoate in a total concentration of 250 mg.
The half-life is from 5 to 7 days. Also very fond of professional athletes. The period of its action may stretch for 14 - 21 days. This is an ester of testosterone, a sex hormone that produces testicles. The development of the genital organs and the manifestation of the secondary sexual characteristics of a man directly depend on this hormone.
therefore enanthate is actively used:
- with underdevelopment of the genitals,
- insufficient testosterone,
- endocrine impotence,
- osteoporosis, developed due to androgen deficiency.
- with carcinoma
- liver diseases
- heart problems
- hypertrophy of the prostate gland.
Balkan Pharmaceuticals produces this ester as a 250 mg oil solution in ampoules.
The half-life of 3 to 4 days. According to the observations of patients, it has a less edematous effect than other drugs. Also, the percentage of those who are faced with "estrogen" effects after taking it is also much smaller. But no scientific evidence has yet been confirmed.
Indications for use:
- hypogonadism of any type,
- menopause syndrome
It is forbidden to accept if there is:
- prostate cancer
- liver disease
- prostatic hypertrophy,
- renal or liver failure.
Manufactured by Pharmacom Labs under the name PharmaTest-PH in the form of oil ampoules.
The half-life is from 2 to 3 days. Not very convenient to use, because requires frequent injections. According to many people, it has a fat burning effect and low conversion to estradiol.
This drug is effective in many diseases:
- fatigue and nervous tension.
The drug is presented in the form of injections under the name Farmak of Ukrainian production and Dalhimpharm of Russian production.
Half-life 1 day. One of the fastest broadcasts. Also requires constant injection. It is mainly used in combination with other ethers as part of certain drugs.
- with an age-related lack of male hormones,
- with pathologies of the genital glands,
- androgen deficiency, etc.
The list of contraindications is standard for such drugs.
The most popular in the form of a mixture of five testosterone esters in the Androbol-300 injection drug from Lyka Labs (India).
For many men, medications based on testosterone esters were just a salvation. Now you, owning full-fledged information, can weigh the pros and cons. But so that you do not decide be sure to consult your doctor.
The drug is a mixture of natural testosterone esters. Testosterone is produced by the male sex glands and is the main endogenous hormone that is necessary for the normal development and growth of the male genital organs, secondary and tertiary sexual characteristics in men. In adult men, testosterone is necessary for the functioning of the testicles and its appendage, seminal vesicles and prostate gland, maintenance of libido, erectile function, and well-being. The use of the drug leads to an increase in plasma concentrations of testosterone, estradiol, dihydrotestosterone, androstenedione, as well as to a decrease in the content of sex hormone binding globulin.Follicle-stimulating and luteinizing hormone levels are restored to normal levels. The symptoms of testosterone deficiency are reduced. Muscle mass and bone mineral density increase, and in obese patients body weight decreases. Sexual function is normalized, including libido, erectile function. The plasma content of high density lipoproteins decreases, the hematocrit and hemoglobin concentration increase, while the activity of liver enzymes and prostate-specific antigen does not clinically significantly change. The drug can increase the size of the prostate gland, while no changes in its work are noted. In men with hypogonadism and concomitant diabetes mellitus, the use of the drug reduces serum glucose or / and improves insulin sensitivity. In boys with delayed puberty and growth, the use of the drug stimulates the development of secondary sexual characteristics, accelerates growth. Therapy of transgender women with the drug promotes masculinization.
The drug consists of testosterone esters, which have different absorption and elimination rates, thereby ensuring a continuous, uniform effect of the drug for 4 weeks after a single injection. Testosterone propionate acts immediately after administration, the duration of action is up to a day. Testosterone phenylpropionate and testosterone isocaproate have a similar action in duration, which begins in a day and lasts up to 14 days. Testosterone decanoate begins to act when the effects of testosterone phenylpropionate and isocaproate cease. A single dose of the drug increases total serum testosterone, the maximum concentration is approximately 70 nmol / L and develops approximately 1 to 2 days after administration. The drug binds to approximately 98% with a specific fraction of globulins, which binds testosterone and estradiol. The half-life of testosterone is 10 to 100 minutes. Metabolized in the liver to 17 ketosteroids, which after conjugation with sulfuric or glucuronic acid are excreted by the kidneys (about 90%). With feces, 6% of the accepted dose is excreted in an unbound form.
Types of Ethers
Consider the most used esters of testosterone and its derivatives in bodybuilding.
Acetate. It has the shortest half-life of approximately 1 day. With this ether, the most commonly used steroids are trenbolone and primobolan. In addition, testosterone acetate is included in the five-ester mixture of testosterone esters, the gaining popularity of Lyka Labs.
Propionate One of the most famous esters, due to the widespread use by bodybuilders of testosterone propionate. In addition, of the most common uses of propionate are drostanolone propionate (masteron) and methandriol dipropionate. Has a half-life in the range of one to two days.
Phenylpropionate. Based on this ester, nandrolone phenylpropionate is best known. Testosterone phenylpropionate is also available. It is also used in testosterone mixtures, such as Sustanon, Omnadren, etc. The half-life of 2 to 3 days.
Isocaproate (isohexanoate). It is part of Sustanon and Omnadren along with other testosterone esters. The half-life is 4 to 5 days
Enanthate. One of the most commonly used esters. Used with testosterone, trenbolone, methenolone and other drugs. Has a half-life of 5-7 days.
Hexahydrobenzyl carbonate or cyclohexyl methyl carbonate (synonyms: hexahydrobencyclocarbonate, English: cyclohexylmethylcarbonate, hexahydrobencylcarbonic or hexahydrobenzyl carbonate). The chain has 8 carbon atoms, although an erroneous indication of 7 atoms is often found, the half-life of various sources is about 6-8 days, similar in properties to the enanthate. It occurs in trenbolone (parabolan). Names differ due to the use of different items.
Cypionate. Almost interchangeable with enanthate. The most common in the United States, although it is found quite often in the form of testosterone cypionate and nandrolone. Half-life up to 7 days.
Decanoate. I immediately recall the nandrolone decanoate, although it is also a part of Sustanon, as the ether with the longest duration in it. According to various sources, the half-life is 7–9 days. To maintain a constant level in the blood, injections are done on average once a week. Previously produced as a separate drug under the brand name Neotest 250 (Loeffler), but is no longer manufactured.
Undecylenate or undecylenate. Has a half-life of 9 to 11 days. Of the most famous uses, boldenone undecylenate.
Laurat. The half-life of 10 to 12 days. The most long-running ether used in bodybuilding. Of the applications - nandrolone laurate.
There are still a lot of ethers, but they are practically not used in bodybuilding or are used quite rarely, therefore they were not included in this article.
The mechanism of action of all these esters on the body is well understood and, in addition to the time of steroid absorption into the bloodstream, does not affect any other characteristics of the action of this steroid.
Due to the overlapping meaning of pharmacological terms, disagreements often arise over the half-life of various esters. There are two different concepts:
- Half-life or half-life (T1 / 2) - the time required to halve the concentration of the drug in the blood depends on the rate constant of elimination (T1 / 2 = 0.693 / Kel) and absorption, as a limiting factor. This indicator is important for calculations related to the construction of the course and post-cycle therapy.
- The half-absorption period (T1 / 2, a) - the time required for absorption of half the dose of the drug from the injection site into the blood is proportional to the absorption rate constant (T1 / 2, a = 0.693 / Ka). The pharmacokinetics of essential drugs proceeds according to the “flip-flop” type, therefore, the semi-absorption indicator also characterizes the time required to destroy half of the administered dose of the drug, and therefore confusion arises.
Simply put, the half-life reflects the concentration of the drug in the blood, and the half-absorption indicates the remaining amount of this drug in the body. Example: after injection of nandrolone decanoate 100 mg, the concentration of the drug will drop by half in 7 days, in another 7 days in four, etc., while 50% of the drug will be destroyed only after 14-15 days. Formally, the effect of the drug ends after 4 half-lives, when about 5% concentration remains.
Most often in the network there are charts of semi-absorption of esters, which must be divided by 2 in order to obtain a half-life that characterizes the concentration of anabolic in the blood. The following are half-lives for anabolic drugs in the blood, taken from various scientific sources:
- Format 0.5 days
- Acetate 1 day
- Propionate 1-2 days
- Phenylpropionate 2 days
- Butyrate 2-3 days
- Valerat 3 days
- Hexanoate 3-4 days
- Caproat 4-5 days
- Isocaproate 4-5 days
- Heptanoate 5-6 days
- Enanthate 5-6 days
- Hexahydrobenzyl carbonate (cyclohexyl methyl carbonate) 6-7 days
- Octanoate 6-7 days
- Cypionate 6-7 days
- Nonanoate 7 days
- Decanoate 7-8 days
- Undecanoate 8 days
- Undecylenate 8-9 days
- Laurat 10 days
Injection into the deltoid muscle instead of the buttocks slows down excretion. The type of solvent oil also plays a significant role. Chaudry and James studies have shown that as the carbon chain lengthens, anabolic activity increases and androgenic activity decreases.
Method of use of testosterone (mixture of esters) and doses
The drug is administered intramuscularly, deep into the gluteal muscle. Doses are set individually depending on the indications and response of the patient.
The drug can not be administered intravenously. Using the drug as a dope can cause serious adverse reactions. Androgenic treatment for patients with delayed puberty should be prescribed with caution, the condition of the skeletal system should be monitored every six months. In older men, the risk of developing hypertrophy or prostate cancer increases, before and after therapy, it is necessary to control the level of prostate-specific antigen and examine the prostate gland. The appearance of jaundice, hepatitis, changes in functional liver indices, edema is a reason for stopping therapy, it is necessary to monitor the functional state of the liver. When using high doses of testosterone, it is necessary to control the hematocrit and the hemoglobin content in the blood. The use of testosterone in breast cancer can cause hypercalcemia, which is associated with the stimulation of osteolysis. This process can increase bone metastasis. With an increase in hypercalcemia, it is necessary to cancel the drug. In women with therapy with androgenic drugs, it is necessary to carefully monitor the calcium content in plasma and urine.
Use the drug with caution in drivers of vehicles and people whose professions are associated with increased concentration of attention and the speed of psychomotor reactions.
Side effects of testosterone (mixture of esters)
Endocrine and reproductive system: men - gynecomastia, oligospermia, priapism, impaired spermatogenesis, libido disorders, women - inhibition of gonadotropin secretion, menstruation and amenorrhea, masculinization, with prolonged use: libido disorders, excessive hair growth on the face and body, coarsening of the voice, atrophy of the mammary glands.
Skin: male pattern baldness, hirsutism, acne.
Digestive system: nausea, impaired liver function, cholestatic jaundice, tumor neoplasms of the liver, hepatic purpura.
Blood and laboratory indicators: polycythemia, retention of chlorine, sodium, water, calcium, potassium, inorganic phosphates, bleeding in patients taking anticoagulant drugs, inhibition of the activity of plasma coagulation factors II, V, VII, X, increased cholesterol concentration in blood plasma.
Nervous system: headaches, paresthesia, fear.
Other: soreness and inflammation at the injection site, in boys - premature closure of the pineal glands, premature puberty.
The interaction of testosterone (a mixture of esters) with other substances
In patients with diabetes, androgenic drugs can reduce the need for insulin and glucose. Patients who take anticoagulant drugs need constant monitoring of blood coagulation when used together with androgenic drugs. When using testosterone with glucocorticosteroids or adrenocorticotropic hormone, the risk of developing peripheral edema increases, especially in people with pathology of the heart or liver. Inducers of microsomal liver enzymes (barbiturates, rifampicin, carbamazepine, phenylbutazone, salicylates, primidone, phenytoin) can reduce the effect of testosterone.