lecture 14.pptx
- 1. Lecture Doping And Its Types Testosterone Esters
- 2. Testosterone esters Much of the testosterone that is prescribed for the purposes of hormone therapy is in the form of testosterone "esters." An ester is simply a name for a chemical compound that is formed from reaction between a carboxylic acid and an alcohol. A simple chemical diagram of this reaction is shown below in Figure A.
- 3. Figure B shows the chemical structure of free testosterone (chemical formula C19H28O2) as well as two different esters of testosterone (testosterone cypionate and testosterone enanthate).
- 4. • There are a number of different esters of testosterone, including the commonly prescribed injectables of testosterone enanthate and testosterone cypionate, as well others such as acetate, propionate, phenylpropionate, isocaproate, caproate, decanoate, and undecanoate. • Each of these different esters is a molecular chain composed of carbon, hydrogen, and oxygen atoms. • The main difference between the different esters is how many carbon and hydrogen atoms make up the chain. • For example, the propionate ester is composed of 3 carbons, 6 hydrogens, and 2 oxygens, whereas the cypionate ester is composed of 8 carbons, 14 hydrogens, and 2 oxygens. • Esterification of testosterone is done in order to improve the solubility of testosterone in oil, which in turn slows the release of the testosterone from the site where it enters the body. Testosterone esters
- 5. • Testosterone, in its free, non-esterified form, has poor solubility in either oil or water-- though it can be suspended in water. Non-esterified testosterone is available in an aqueous injectable form with the drug name "Aquaviron. • " However, this form of testosterone stays active in the body for a very short period of time (only a matter of hours). Because of this, it must be injected on a daily basis in order to maintain a continuous level of testosterone in the blood. Therefore it is rarely used for testosterone replacement therapy as an injectable. • Once you have added an ester group to testosterone, it becomes even less soluble in water and more soluble in oil. Additionally, as a general rule, the more carbon atoms there are in an ester, the more soluble the ester is in oil. For example, testosterone propionate (with 3 carbon atoms in the ester group) is less soluble in oil than testosterone cypionate (with 8 carbon atoms in the ester group). • So generally, the more carbons the ester group has, the more soluble in oil it becomes, and the less soluble in water. The term for this ratio between oil and water solubility is called the "partition coefficient"-- the higher the solubility in oil, the higher the partition coefficient. Testosterone esters
- 6. • Testosterone cypionate has a high partition coefficient. When injected into the body, the drug remains in its esterified form in a deposit in the muscle tissue, depending on the type of injection. • From there, it will slowly enter the circulation as it is picked up in small quantities by the blood. Once the esterified testosterone is brought into the blood stream, "esterase enzymes" cleave off the ester chain in a process known as "hydrolization," thus leaving the testosterone in its free form to perform its various actions and effects. • When people speak of whether a particular testosterone ester is "fast acting" or "slow acting," they are usually referring to the partition coefficient/solubility in oil. • As described above, esters with more carbon atoms will generally be more soluble in oil-- they are often referred to as "slow-acting" esters (they stay active in the system longer). • Esters that are less soluble in oil are often referred to as "fast-acting" forms of testosterone, referring to the fact that they are more quickly available and used up in the blood stream. Testosterone esters
- 7. Testosterone Enanthate • Testosterone enanthate has Chemical formula C26H40O3 • Testosterone enanthate, also known as testosterone heptanoate, is an anabolic and androgenic steroid (AAS) drug used to treat low testosterone levels. • Anabolic drugs work by building muscles, while androgenic refers to the enhancement of male sex characteristics. • Used in medical procedures since the 1950s, testosterone enanthate is marketed under numerous brand names, including Androfil, Andropository, Cernos, Delatestryl, Depandro, Durathate, Everone, Sustrone, Testanon, Testanova, Testrin, Testostroval, Testoviron, and Testro.
- 8. • Use of testosterone enanthate has been shown to significantly increase strength within 6-12 weeks of administration • It is a slow-acting ester with a release time between 7-9 days. • . Testosterone enanthate is typically injected anywhere between once every week to once every three weeks. • Testosterone enanthate is available by prescription only and is classified as a prohibited substance by the World Anti-Doping Agency Testosterone Enanthate
- 9. Common Side Effects As a substance designed to alter hormone levels, testosterone enanthate has both its clear benefits and risks. According to the FDA, the most common side effects associated with testosterone enanthate use include: • Injection site pain and swelling • Headaches • Dizziness • Mood changes, including aggression • Depression or anxiety • Increased or decreased libido • Generalized tingling sensations • Oily skin and acne • Thinning hair • Weight gain
- 10. Adverse Reactions Less common but potentially more serious are side effects associated with the long-term use or overuse of testosterone enanthate. Some are related to the androgenic effects of the drug; others can affect the heart and liver by elevating the cholesterol and liver enzyme levels. • Male-pattern hair loss • Male-pattern hair growth in women • Male breast enlargement • Deepening voice in women • Menstrual irregularities • Difficulty urinating or frequent urination at night in men • Severe psychiatric symptoms, including major depression, paranoia, or psychosis
- 11. Testosterone Propionate INTRODUCTION Testosterone propionate was discovered in 1936 and was introduced for medical use in 1937 This type of testosterone is a slow-releasing anabolic steroid with a short half- life of 4-5. It is used in short Testosterone Propionate cycles in the range of 8 – 10 weeks, sometimes in as little as even 6 weeks. This is due to the shorter time required for optimal blood plasma levels to be achieved because of the faster release. It will result in the fastest peak plasma levels of Testosterone. The high level will be followed by a crash in T levels if you do not inject twice or thrice a week to maintain stable levels. This testosterone ester can peak in the blood within hours of being administered and metabolized over three days. C22H32O3
- 12. • Propionate requires frequent injections compared to other types of testosterone such as cypionate or enanthate. • Injections should be administered every two to three days. • Competition bodybuilders like to use Testosterone Propionate along with Stanozolol and Trenbolone, as well as Growth Hormone, which ensures optimal muscle protection even during the toughest diets and heaviest exercise phases. However, this combination should only be used by ambitious athletes. • For amateur bodybuilders who have no competitive ambitions, the sole use of Testosterone Propionate is usually completely sufficient and low side effects.
- 13. Testosterone Cypionate C27H40O3 Introduction 1. Testosterone Cypionate was first created in the mid-1950s, and was released on the prescription drug market under the brand name Depo-Testosterone 2. Testosterone Cypionate is most likely the second most popular esterified variant (the first being Testosterone Enanthate). 3. It is an injectable form of Testosterone with a slow rate of release and a longer half-life. 4. However, the release rates and half-life of both Testosterone Cypionate and Testosterone Enanthate are very much identical and the two compounds are easily interchangeable (for example, an individual can easily run a 10 week cycle of Testosterone and switch between Testosterone Enanthate and Testosterone Cypionate seamlessly).
- 14. 5. Testosterone Cypionate possesses a half-life of approximately 8- 10 days while Testosterone Enanthate possesses a half-life of approximately 7-9 days – hardly much difference. 6. the most common difference that we know about the difference between testosterone enanthate and testosterone cypionate is that the latter lasts longer. 7. In addition to the difference in the effect of the two, testosterone enanthate and cypionate has a difference in their chemical structure as well. The Testosterone enanthate has 7- carbons whereas Testosterone cypionate has 8-carbons. 8. Testosterone cypionate comes only in the form of an injectable solution given into your muscle. You can give this medication to yourself at home after your doctor shows you how.
- 15. When it needs to take Testosterone cypionate is used to treat symptoms of hypogonadism in males. In this condition, males don't produce enough of the sex hormone testosterone. Testosterone cypionate works to treat hypogonadism in males by replacing the testosterone your body is unable to make.
- 16. Testosterone Phenylpropionate Testosterone phenylpropionate, Chemical formula C28H36O3, otherwise called testosterone hydrocinnamate, is an engineered anabolic-androgenic steroid which was once in the past promoted in Romania. Testosterone phenylpropionate is a slow-acting ester, with a release time of 1-3 weeks. Testosterone phenylpropionate was first released into the market in 1955 by Sicomed Pharmaceutical house but was selling under the name brand Testolent. Testosterone phenylpropionate is a drug that should be administered through injection. After the injection, the drug remains active for about five days when then you can take another dose. The drug can be used independently or administered with other testosterone esters for testosterone treatments in a patient with affirmed testosterone insufficiency.
- 17. Additionally, by taking testosterone phenylpropionate, bodybuilders report increment of craving, forcefulness, and quality. Testosterone Phenylpropionate Half life Testosterone phenylpropionate is an injectable drug with a half-life of 3 to 4 days. You will be required to take your dose once in 4 days. A professional health practitioner should administer the injection.
- 18. Testosterone decanoate Testosterone decanoate is an androgen and anabolic steroid and a testosterone ester. It is a component of Sustanon, along with testosterone propionate, testosterone phenylpropionate, and testosterone isocaproate. The medication has not been marketed as a single-drug preparation. Testosterone decanoate has been investigated as a potential long-acting injectable male contraceptive. It has a longer duration of action than testosterone enanthate, but its duration is not as prolonged as that of testosterone undecanoate. The molecular formula of Testosterone decanoate is C29H46O3. It is the fourth compound of Sustanon 250 has the longest half-life and is thus the most powerful one. Its half-life extends for more than two weeks. It may also have an active life of a month thus you may need to inject it after a month. But, this only happens in the case of hormone replacement therapy.
- 19. Testosterone caproate Testosterone caproate (TCa), also known as testosterone hexanoate, is an androgen and anabolic steroid and a testosterone ester that is no longer marketed. The molecular formula of Testosterone caproate is C25H38O3. Testosterone isocaproate Testosterone isocaproate, sold under the brand names Sustanon 100, Sustanon 250, and Omnadren 250, is an androgen and anabolic steroid medication and a testosterone ester which has been used as a component of mixed testosterone ester preparations. Also known as isohexane,4-methylvaleric acid, and isocaproic acid. The half- life if this compound is 7-9 days. If it is used as a single testosterone supplement, then you need to inject it after every week.
- 20. Stanozolol In 1962, Stanozolol was brought to market in the US by Winthrop under the tradename "Winstrol" is a synthetic anabolic steroid derived from dihydrotestosterone. t was developed by Winthrop Laboratories (Sterling Drug) in 1962, and has been approved by the FDA for human use. Unlike most injectable anabolic steroids, stanozolol is not esterified and is sold as an aqueous suspension, or in oral tablet form. The drug has a high oral bioavailability, Stanozolol has been used in both animal and human patients for a number of conditions. In humans, it has been demonstrated to be successful in treating anaemia and hereditary angioedema. Veterinarians may prescribe the drug to improve muscle growth, red blood cell production, increase bone density and stimulate the appetite of debilitated or weakened animals
- 21. Stanozolol is one of the anabolic steroids commonly used as performance-enhancing drugs and is banned from use in sports competition under the auspices of the International Association of Athletics Federations (IAAF) and many other sporting bodies. Additionally, stanozolol has been used in US horse racing. Stanozolol is subject to non-medically supervised off-label use by some athletes for its anabolic properties frequently presenting with concomitant reduction of body fat. Commonly used by athletes and bodybuilders alike to lose fat while retaining lean body mass. It is usually used in a "cutting or leaning out" cycle, to help preserve lean body mass while metabolizing adipose, although it has not been proven conclusively that it has any special fat- burning properties. It is presented most commonly as a 50 mg/mL injection. However, recently 75 mg/ml 100 mg/mL versions have become available Stanozolol is metabolized in the liver, ultimately becoming glucuronide and sulfate conjugates. Its biological half-life is reported to be 9 hours when taken by mouth and 24 hours when given by intramuscular injection in the form of an aqueous suspension.
- 22. Clenbuterol Clenbuterol is a compound that belongs to a class of drugs called beta 2- agonists. Drugs in this category can cause dilation of the bronchial muscles. Beta2-agonists are often used to treat asthma. In addition to being used to treat asthma, clenbuterol has become popular as a weight loss supplement. That’s because of its effect on muscle growth and fat reduction. Clenbuterol isn’t a steroid, but it has some properties similar to those of anabolic steroids, such as promoting an increase in muscle mass. Due to these properties, clenbuterol has been used in livestock to increase the amount of lean muscle.
- 23. Clenbuterol has been observed to both increase muscle mass and reduce body fat. Additionally, it remains in the body with an active effect for up to about six days after consumption (detectable traces can remain longer). Because of these properties, it’s often used as a weight loss supplement or to enhance athletic performance. Clenbuterol has a half-life of up to 39 hours. People taking clenbuterol for weight loss or performance enhancement often use anabolic steroids or growth hormones as well.
- 24. Clenbuterol usage The FDA hasn’t approved clenbuterol for use in humans. A liquid form of the drug is approved by the FDA for treatment of airway obstruction in horses. Outside of the United States, clenbuterol is available by prescription only for the treatment of asthma.
- 25. Clenbuterol side effects Clenbuterol can have negative side effects when overused or misused. These can include: increased heart rate rapid breathing heart palpitations (A heart palpitation is the sensation that your heart has skipped a beat or added an extra beat.) chest pain tremor anxiety electrolyte imbalance