Testosterone (Testosteronum)
Absorption of testosterone from mucous membranes and skin is high and depends on the dosage form.
It is used in the form of testosterone undecanoate (orally, intramuscularly) and active testosterone (cutaneously). About 98% of circulating testosterone is bound to SHB and albumin. Only the free fraction of testosterone is considered biologically active. Biotransformation to inactive metabolites occurs in the liver. After administration of labeled testosterone, about 90% of the radioactivity is determined in the urine in the form of glucuronide and sulfate acid conjugates. Products detected in urine include androsterone and etiocholanolone. 6% of the active substance after passing through the enterohepatic circulation is found in feces.
Testosterone, formed from testosterone undecanoate as a result of cleavage of the ester bond, is metabolized and excreted from the body in the same ways as endogenous testosterone. Undecanoic acid is metabolized by β-oxidation in the same way as other aliphatic carboxylic acids.
Features of pharmacokinetics for various routes of administration
After ingestion
a significant portion of testosterone (in the form of undecanoate ester) is absorbed in the small intestine and enters the lymphatic system, thereby partially bypassing the primary passage through the liver. From the lymphatic system, testosterone undecanoate enters the plasma. In plasma and tissues, as a result of hydrolysis, natural male sex hormones testosterone and dihydrotestosterone are released.
A single dose of 80-160 mg of testosterone undecanoate leads to a clinically significant increase in the total plasma concentration of testosterone, the maximum concentration is approximately 40 nmol/l and is achieved 4-5 hours after administration. The increased concentration of testosterone persists for at least 8 hours. The half-life is from 10 to 100 minutes.
After intramuscular injection
testosterone undecanoate is gradually released from the depot form (oil solution) and is almost completely broken down by serum esterases into testosterone and undecanoic acid. The very next day there is an increase in serum testosterone concentration.
According to two studies, in men with hypogonadism, after a single intramuscular injection of 1000 mg testosterone undecanoate, mean maximum testosterone concentrations of 45 and 24 nmol/L were determined after 7 and 14 days, respectively. Postmaximal testosterone levels decline with a half-life of approximately 53 days.
After repeated intramuscular injections of 1000 mg testosterone undecanoate into hypogonadal men with an interval of 10 weeks between injections, steady-state concentrations were achieved between the 3rd and 5th injections. The mean values of the maximum and minimum testosterone concentrations at steady state were about 42 and 17 nmol/L, respectively. Postmaximal serum testosterone levels decreased with a half-life of approximately 90 days, consistent with the rate at which the drug is released from storage.
For cutaneous application
the degree of testosterone absorption ranges from 9 to 14% of the applied dose. After absorption through the skin, testosterone enters the systemic circulation in relatively constant concentrations over a 24-hour cycle. Daily fluctuations in testosterone concentrations have the same amplitude as circadian changes in endogenous testosterone levels. External use of testosterone allows you to avoid distribution peaks in the blood that occur with the injection method of its administration. In contrast to oral androgen therapy, topical testosterone does not increase hepatic steroid concentrations above physiological norms.
The use of 50 mg of testosterone externally causes an average increase in its plasma concentration by approximately 2.5 ng/ml (8.7 nmol/l). After discontinuation of treatment, testosterone concentrations begin to decrease approximately 24 hours after the last use. The concentration returns to the original level approximately 72-96 hours after the last dose. The main active metabolites of testosterone when applied cutaneously are dihydrotestosterone and estradiol.
Pros of admission
- Muscles are growing.
- The fat layer becomes smaller.
- The desired “cubes” appear.
- The level of strength indicators increases.
- Sexual desire and activity increases.
- Cholesterol decreases.
- Minimal risk of heart disease.
The action of the component is not very long-lasting and this is its main disadvantage when compared with other steroids. The second, no less important drawback is the rather high price. Injections are usually given at daily intervals. This hormone can be used in two periods: for weight growth and for “drying”.
Since each body reacts differently, such a pronounced short-term effect of testosterone can be a plus. After all, not every organism can react normally to a foreign component. An allergic reaction may occur, which, however, can pass just as quickly.
An undoubted advantage (of course, with the correct and competent dosage of the drug) is the almost complete absence of edema. Taking this medicine will not cause an immediate increase in muscle growth by several kilograms; its effect will be as delicate, high-quality and “dry” as possible. The most positive effect can be felt almost immediately after the first injection. Therefore, for these reasons, bodybuilders use another component: enanthate. And the component described in the article is used when it is necessary to “dry” the body of excess fat. It is suitable for absolutely all athletes, from inexperienced to higher level.
How to use
It is better to take this anabolic in courses and in combination with other medications: this will increase their chemical activity. The optimal dosage for beginners is fifty milligrams, taken every other day, while for more experienced athletes the usual daily dose is more than one hundred milligrams.
A very important point is taking medications that block the appearance of female sex hormones: antiestrogens. The most common is Proviron. If you do not take them, gynecomastia (excessive development of the mammary glands, like in a woman), and swelling may develop. Antiestrogens should be taken from the second week after starting to take the anabolic steroid. As soon as the course of taking the drug is completed, restorative therapy is carried out. At this time, another drug is taken - tamoxifen.
To maintain the gained weight and prevent the formation of a repeated fat layer in the abdominal area, it is advisable to take cortisol (stress hormone) blockers. And of course, an individual sports nutrition regimen that excludes everything harmful.
Combination and effect when taken with other drugs
If you use this anabolic to significantly “dry” your body, then it goes well with the following drugs:
- Stanozolol (anabolic, steroid and doping banned in sports).
- Trenbolone acetate (the most effective anabolic steroid for increasing strength and muscle growth).
- Masteron (strongest androgen)
- Primobolan (a milder anabolic, suitable for beginners).
How to take anabolic steroids for beginners:
- First - fifty milligrams of the main component according to the instructions.
- Thirty milligrams of Stanozolol. But you should start with ten milligrams and gradually increase to the desired dosage.
- After six weeks, anabolic steroids are discontinued and rehabilitation therapy is carried out.
The main advantage of taking a course of drugs is the positive effect of simultaneous use than if they were taken separately. Moreover, the side effects are very minimal. Among experienced athletes, there are also those who inject medication directly into the desired muscles, although the effectiveness of such a technique has not yet been proven. Any anabolic drugs appear only after absorption into the bloodstream. The effect of their influence directly on the muscular system is not observed, otherwise complete asymmetry of growth would be observed (if synthol is used).
Common side effects
The most common complaint is pain in the place where the injection was made. Increased level of aggression. The main “side effects” of Propionate are their conversion into female sex hormones and DHT. This causes the following unpleasant consequences:
- Gynecomastia (enlarged mammary glands).
- Severe acne.
- Loss of hair on the head.
- Strong hair growth on other parts of the body.
- Prostate enlargement.
- The appearance of secondary sexual characteristics (if the steroid is used by female bodybuilders).
The peculiarity of the medication is that it blocks the production of testosterone, the most important component of the male body. Recovery occurs within a couple of months after you stop taking the drug. If the course is long, then it is necessary to administer additional medications: gonadotropin 50 IU (from the second week. The frequency of the course is daily, one-time). The risk to the liver and kidneys is minimal. Women should not take it.
Cross-drug interactions
Rifampicin, barbiturate, Phenylbutazone, Carbamazepine and Phenytoin reduce the therapeutic effect.
If the patient suffers from hypogynadism, then specialists should prescribe additional estrogens and thyroid stimulants.
Vitamins, anabolic steroids, phosphorus and calcium are enhanced under the influence of the drug.
Elimination of cyclosporine is slowed by testosterone.
Androgens require a reduction in the dosage of hypoglycemic agents.
Testosterone can affect the metabolism of certain medications. Oral anticoagulants sometimes require a dose reduction.
Due to cross-reaction with corticosteroid or adrenocorticotropic hormones, edema may occur.
Alcohol and barbiturates reduce the activity of the described drug.
Warnings
Each medical product has its own contraindications. This steroid is no exception. Firstly, it is strictly contraindicated for children. Secondly, treatment is possible only on medical advice. This information is presented for informational purposes only and is intended to reduce the risk of side effects and related complications.
In preparing this article, materials and articles from open Internet sources were used, as well as excerpts from textbooks by Russian and foreign authors.
Notes[edit | edit code]
- Korenchevsky V, Dennison M, Eldridge M (1937). "The prolonged treatment of castrated and ovariectomized rats with testosterone propionate." Biochem. J. 31(3):475–85. doi:10.1042/bj0310475. PMC 1266958 Freely accessible. PMID 16746360.
- Eberhard Nieschlag; Hermann M. Behre; Susan Nieschlag (26 July 2012). Testosterone: Action, Deficiency, Substitution. Cambridge University Press. pp. 9.315–. ISBN 978-1-107-01290-5.
- William Llewellyn (2011). Anabolics. Molecular Nutrition LLC. pp. 357–361,413,426,607. ISBN 978-0-9828280-1-4.
- Pushkar D. Yu., Segal A. S. Modern possibilities for correcting age-related androgen deficiency in men // Effective pharmacotherapy. – 2010. – No. 32. – pp. 16-21.
- Eberhard Nieschlag; Hermann M. Behre; Susan Nieschlag (13 January 2010). Andrology: Male Reproductive Health and Dysfunction. Springer Science & Business Media. pp. 441–446. ISBN 978-3-540-78355-8.
- Behre HM, Abshagen K, Oettel M, Hübler D, Nieschlag E (1999). "Intramuscular injection of testosterone undecanoate for the treatment of male hypogonadism: phase I studies." Eur. J. Endocrinol. 140(5):414–9. doi:10.1530/eje.0.1400414. PMID 10229906.
- Bayramov A. A., Kuznetsova N. N. Androgen-dependent influence of the m-anticholinergic metamizil on the bioelectrical activity of the brain // Psychopharmacology and biological narcology. – 2006. – T. 6. – No. 1-2.
- https://www.fitnessuncovered.co.uk/performance-drugs/profiles/testosterone-propionate
- J Clin Endocrinol Metab. 1997 Feb;82(2):407-13.
- Am J Physiol Endocrinol Metab. 2002 Mar;282(3):E601-7.
- Curr Opin Clin Nutr Metab Care. 2004 May;7(3):271-7.
- Heart. 2004 Aug;90(8):871-6.
- https://iron-set.com/farmakologiya/propik
- Pope, H. G., Kouri, E. M., & Hudson, J. I. (2000). Effects of supraphysiologic doses of testosterone on mood and aggression in normal men: A randomized controlled trial. Archives of General Psychiatry, 57, 133-140
Indications for use
The drug is intended for both men and women.
Testosterone injections for the stronger sex are prescribed when there is a delay in sexual development, disruptions in the functioning of the reproductive system, menopause, as well as vascular and nerve diseases. The drug is prescribed when prostate hypertrophy, acromegaly, eunuchoidism, impotence (developed due to endocrine disruptions), syndrome after surgical castration and a small amount of sperm are detected.
Testosterone injections for women are needed to treat nerve and vascular disorders caused by menopause, as well as to relieve ovarian and breast cancer. Additionally, the main active component stops bleeding from the uterus in older women, and also eliminates mastopathy, accompanied by tension in the mammary glands during PMS, uterine fibroids and the proliferation of endometrial cells.
Reviews
If they note a good effect on the body, people most often note the following:
- Muscle mass increases significantly.
- No swelling.
- Growth of “dry” mass.
- Increasing levels of stamina and sexual desire.
- Painless injections.
- Increased incentive to train.
- Affordable price.
Naturally, it is noted that this anabolic works best in combination. For example, when combining Propionate with Winstrol in tablets, swelling is eliminated: the medication removes it. When combined with Turinabol, the level of endurance increases.
The most popular and effective brands are Testosterone Propionate from Farmak (Ukraine), Testopin (India), and Propionate from Iran.
