Zuhra Pavlova, WHC, endocrinologist Moscow State University Hospital, scientific director of the Clinic system medicine, https://t.me/doctorpavlova
Testosteronzamestitelnaya therapy (TZT) designed to replace lost function gonads (testes) to develop hormone testosterone. Testosterone is produced even in small amounts by the adrenal glands, but the lion's share of it in the testicles.
If someone does not know, testosterone is produced from cholesterol.
What forms of testosterone preparations are available? Immediately recall that all the drugs a doctor prescribes, and self-medication in this area will make you disabled.
They can be divided into five groups:
1. Transdermal - patches and gels;
2. Oral (the ones that we ingest in the form of capsules or tablets);
3. Injectable forms;
4. Buccal ( "buccal" - applique drug on the oral mucosa);
5. Subcutaneous implants.
Each form of drugs, there are advantages and disadvantages. And describes the advantages and disadvantages of drugs for the hundredth time, probably does not make sense. All of this is already in the Internet.
What interesting things you can add to the information available. In my opinion that supraphysiological (ie much larger than the natural) testosterone is bad. Normal physiological testosterone values are numbers from 14 to 17.5 (rate from 12.1 to 33). Always remember that we are all individual and that one rule for another critical figure.
Besides testosterone, we take into account the level of SHBG, to convert free testosterone fraction, that is exactly the one that affects the target organs. SHBG can mislead you, for example in terms of insulin resistance. But, it can also clarify the picture to whether the free fraction of testosterone is sufficient, with a relative reduction of its overall fraction. It is important to assess and those hormones that are derived from testosterone - it estradiol and dihydrotestosterone. Many doctors do not consider it necessary to do so, many associated standards and security system that does not pay the costs of these tests. And a coherent picture does not add up.
1. Patches and gels
The transdermal route of administration of testosterone - noninvasive (diffusion through the skin), painless. testosterone concentration rises during the first hour during the day and constantly maintained at a normal level. Administration of the drug does not require nurses or travel to medical centers.
This kind TZT safest because therapy can cancel it if will develop side effects or adverse events. In other words, it is the short-range products.
Furthermore, the concentration of testosterone usually reaches values supraphysiological if certainly adhere to recommended doses. Well, another not unimportant factor - is the absence of first pass through the liver.
There are also disadvantages of this form of administration - is on the skin irritation, the probability of getting into testosterone the body of those who are close contacts with the patient, and, of course, constant, daily application of the drug on skin.
If these forms are used girls, the risk of the appearance of cellulite in this area is very high.
It was about the gel. But there is more, and patches. They are two types:
a) scrotal (scrotal) - they only adhered to the skin of the scrotum;
b) cutaneous (neskrotalnye) - they are used in other parts of the body (back, shoulders, hips, abdomen), except for the face, genitals, neck, hands and feet.
Why is the idea of using scrotal patches. From the knowledge of the physiology, we know that different areas of the body have a greater or lesser number of particular receptors and enzyme activity is also higher or lower depending on the body part. So in the skin of the scrotum activity of 5-alpha reductase significantly higher than, for example, in thoracic skin glands. Producers relied on the fact that the enzyme will increase the conversion of testosterone to dihydrotestosterone (DHT), and its androgenic ratio significantly higher than that of testosterone and efficacy of treatment will be substantially expressed. But, at the same time increase the side effects of DHT, lowering of the effects of testosterone. In addition, technically wearing the patch on the skin is not convenient, it is not fixed in one place and by the way, you need to constantly shave the skin of the scrotum, which sooner or later leads to damage to the epidermis.
Neskrotalny patch (androderm) less prone to conversion to DHT or estradiol. Depending on the starting level of the patient or his designate patch 1 or 2 day (2.5 or 5 mg). Pasting it is necessary on those skin areas that are not in contact with bone (e.g., over the tibia) or on those areas that are exposed crush (during sleep, for example), since it is fraught with burns (a substance which helps to better penetrate the active metabolite in the body through the skin).
2. Oral forms - there are three types of
a) testosterone undecanoate. It has a small dose of testosterone, a high price and is good with moderate androgen deficiency. This drug does not pass the primary metabolization by the liver, because it is absorbed by the small intestine into the lymph, thereby reducing the burden on the liver and increasing bioavailability to the organism. He has another invaluable effect, it reduces the level of SHBG, thereby increasing the bioavailability of testosterone.
b) 17 Alpha-alkylated androgens. The most prominent representative is methyltestosterone. The main advantage of these drugs is their affordability and ease of use - this pill. But they are hepatotoxic and hepatocarcinogs.
c) analogs of dihydrotestosterone. For example, Mesterolone - in my opinion, the use of this group of drugs is limited to a very narrow range of needs. Previously, he was recommended in patients with hypogonadism and obesity, high activity to the flavor and risk of hyperestrogenia. But even this patient is not shown, although it really is not metabolized into estrogen, but it does not possess all the list of the effects of testosterone.
Bodybuilders love it for its ability to "dry" muscle mass, making it more relief. At high concentrations of dihydrotestosterone promotes benign prostatic hyperplasia and Of course skin manifestations, such as hair loss on the head - androgenic alopecia, the greasiness of the skin and acne disease.
3. Injection.
Drugs are divided into three groups according to the duration of action:
- short-acting (testosterone propionate and acetate) half-period of about two days and nights, respectively;
- average duration (cypionate - 1 injection once a week, cypionate depot -1 every 3-4 weeks, once a enanthema -1 - 2-3 weeks, a mixture of testosterone esters - 1 every 2 weeks)
- long-acting (testosterone undecanoate and butsiklat) - from 10-12 to 12-16 weeks, respectively.
Technically very comfortable injection rarely do, which is a plus long-acting preparations. But simultaneously we must pay a large sum to arrive at the injection to the medical institution, as such injections do yourself without the required knowledge can not (oily solution, but still large volume caught in a vessel threatens embolism and pulmonary vessels death). And of course there is soreness at the injection site.
There is one drawback - if necessary, discontinue therapy is not possible to wait for the termination of the drug in the body.
Short-acting drugs and with an average duration of action are "bad farmokokinetiku". What does that mean - after injection to supraphysiological concentration increases and then falls below the reference. It turns a palisade, which adversely affects the hypothalamic-pituitary-testicular arc, which in turn negatively affects the circadian inherent in the body.
By the way, a long-acting drugs stockade is not as strong, but they can not be used in patients at high risk of cardiovascular disease or very overweight - obesity, the more pronounced, the more flavor the surface and the risk of hyperestrogenia. And here and cardiovascular risk is increased, and cancer.
With the positive drug group in the mixture of testosterone esters (sustanon, omnadren) is that the different esters have different pharmacokinetics -with varying speed are absorbed and excreted, so interact and have a joint effect over a longer time than cypionate or propionate.
4. Buccal ( "cheek")
This group of drugs testosterone, are rather expensive, but it also has its own niche.
Tablets are used up to 3 times a day. The dose of 30 mg. Metabolism also eliminates the initial passage through the liver, which of course is a plus.
If necessary, short-TZT and skin reactions, this option is an alternative. There are downsides, besides cost - the likelihood of testosterone partner by kissing, irritation of the mouth and changes in taste.
5. subcutaneous implants
Less and less popular. Effect is for six months, unless they are "pushed" out earlier. Installation is performed under local anesthesia, as a rule in nadpupochnoy region into the subdermal layer. The gradual release of drugs creates a uniform concentration (about any circadian we are not talking, but also constantly changing concentrations from 0 to supraphysiological doses also no). If necessary, stop therapy simply removed the implant and the wound treated.
In other words, each group of drugs has its own niche, its indications and contraindications, advantages and disadvantages. Therefore, the appointment should be done only an experienced doctor, and the patient can not be broken recommendations.
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