What Is Oxymetholone?

Oxymetholone is a white crystalline powder and is odorless. Melting point is 173-176 ° C (178-180 ° C). [] D + 38 ° (chloroform), insoluble in water, easily soluble in chloroform, soluble in dioxane and vegetable oil, slightly soluble in ethanol and ether. This product can be obtained by acetylation, reduction, ring-opening, oxidation, hydrolysis, elimination, oximation, rearrangement, hydrolysis, addition, oxidation, hydrolysis, condensation and other steps of sapogenin or sisal saponin. Clinically, it can promote protein synthesis and inhibit protein alienation, and can reduce blood cholesterol, reduce calcium and phosphorus excretion, reduce bone marrow suppression, and promote development.

Chinese name: Oxymetholone
Foreign name: oxymetholone

CAS number: 434-07-1
Molecular formula: C21H32O3

Introduction to oxymetholone compounds

Oxymetholone Basic Information

Chinese name: hydroxymethene dragon

Chinese alias: Tofatinib citrate; 17-hydroxy-2-hydroxymethylene-17-methyl-5-androst (alkane) -3-one; 2-hydroxymethylene-17-methyl -5-androstane (17) -17-ol-3-one; 17-Hydroxy-2- (hydroxymethylene) -17-methyl-5-androstan-3-one;

English name: oxymetholone

English alias: Roboral; Adroidin; Stanozolol impurity B; Androstan-3-one, 17-hydroxy-2- (hydroxymethylene) -17-methyl-; Becorel; Adroyd; Oxymetholone; Anadroyd; Anadrol; Raboral;

CAS number: 434-07-1

MDL number: MFCD00133083

EINECS number: 207-098-6

RTECS number: BV8060000

PubChem number: 24979930

Molecular formula: C ₂₁ H ₃₂ O ₃

Structural formula:

Molecular weight: 332.47700

Exact mass: 332.23500

PSA: 57.53000

LogP: 4.40100

Physicochemical properties of hydroxymetholone

Appearance and properties: white crystalline powder

Density: 1.169g / cm ³

Melting point: 172-180 ° C

Boiling point: 465.9ºC at 760mmHg

Flash point: 249.7ºC

Refractive index: 38 ° (C = 1, CHCl3)

Stability: Stability May be light sensitive. Combustible. Incompatible with strong oxidizing agents.

Storage conditions: 2-8ºC

Vapor pressure: 1.23E-10mmHg at 25 ° C

Oxymetholone Safety Information

Symbol: GHS08

Signal Word: Warning

Hazard statement: H351; H361

Cautionary Statement: P281

Customs code: 2937290023

WGK Germany: 3

Danger category code: R40

Safety instructions: S53-S22-S26-S36 / 37/39

RTECS number: BV8060000

Dangerous goods mark: T ^[1]

Oxymetholone molecular structure data

1. Molar refractive index: 95.89

2. Molar volume (m / mol): 284.2

3. Isometric Zhang Rong (90.2K): 757.0

4. Surface tension (dyne / cm): 50.3

5. Polarizability (10cm): 38.01

Oxymetholone synthesis method

This product can be obtained by acetylation, reduction, ring-opening, oxidation, hydrolysis, elimination, oximation, rearrangement, hydrolysis, addition, oxidation, hydrolysis, condensation and other steps of sapogenin or sisal saponin.

Oxymetholone uses

Stanozolol intermediate. It is an anabolic hormone drug, which can promote protein synthesis and inhibit protein heterogeneity, and can reduce blood cholesterol, reduce calcium and phosphorus excretion and reduce bone marrow suppression, promote development, and promote tissue regeneration and granulation. Prevents and counteracts adrenal insufficiency caused by long-term use of adrenal corticosteroids. ^[2]

Description of hydroxymetholone compounds

Oxymetholone pharmacological action

Oxymetholone can promote protein synthesis and inhibit protein heterogeneity, and can reduce blood cholesterol, reduce calcium and phosphorus excretion and reduce bone marrow suppression, promote development, and promote tissue regeneration and granulation formation. Its protein assimilation is four times that of methyltestosterone, androgen activity is 0.39 times that of the latter, and the differentiation index is about 10.5. It has antagonistic effect on protein adrenalization caused by excessive adrenal corticosteroids, and has preventive and antagonistic effects on adrenal cortical dysfunction caused by long-term use of adrenal corticosteroids.

Oxymetholone indications

It is used for osteoporosis, chronic wasting diseases, frail old age, severe illness and postoperative frailty, dysplasia in children, aplastic anemia, leukopenia, hyperlipidemia, etc.

Contraindications to oxymetholone

Patients with liver and kidney dysfunction, prostate cancer and pregnant women are prohibited.

Oxymetholone dosage

Take orally, 5-10 mg daily, divided into 1 to 3 times. The dosage for children is 1.25 to 5 mg per day. For osteoporosis, 2.5mg each time, 3 times a day, can also reach 20mg per day. For aplastic anemia, 1 to 5 mg / kg per day.

Oxymetholone adverse reactions

Occasionally nausea, edema, liver dysfunction and jaundice. Young women occasionally have delayed menstruation, which can be recovered by stopping the drug.

Precautions for oxymetholone

1. Do not use medicine for more than 30 days for children and 90 days for adults. Reuse after stopping.

2. For aplastic anemia, the medication time can be longer. ^[3]

Oxymetholone Expert Reviews

Oxymetholone assimilation is 4 times as much as testosterone, androgen activity is 0.39 times as much as the latter, and the differentiation index is about 10.5. ^[3]

Other studies of oxymetholone

Oxymetholone improves memory

Previous studies have found that oxymetholone treatment can prevent coronary heart disease, treat osteoporosis, and reduce the risk of colon cancer. Hydroxymethylene

Central nervous system Dragon has a positive effect on some psychological functions, and can modify the connection of the central nervous system. Even elderly people aged 70 to 80 have this potential re-recovery ability, which may also reduce the incidence of dementia.

In this study, magnetic resonance imaging (MR1) was used to measure brain activity. In 46 women, oxymetholone increased the activity of memory-related brain regions and stimulated the brain to form what young people see. Type of neural connection. Although there is no quantitative evidence for memory improvement, the authors believe that the increased activity of oxymetholone in the relevant brain area implies an improvement in memory function, suggesting that oxymetholone can change the neural circuit of memory in mature individuals.

Some experts believe that the results of this study are meaningful, but oxymetholone replacement therapy also increases the risk of endometrial cancer and breast cancer. Therefore, it cannot be regarded as a panacea. It seems that further research is needed on its good effects and potential side effects.

Oxymetholone is good for men

Oxymetholone can stimulate male parasexual organs to develop and mature, maintain normal sexual desire, promote sperm development and maturity, promote protein synthesis and

Sex organ The growth of skeletal muscles develops muscles; inhibits the increase in body fat, stimulates the production of red blood cells and the growth of long bones; and promotes the formation of secondary sexual characteristics.

For example, if the man is 11 to 12 years old, the larynx knot begins to increase and becomes more pronounced. At the same time, the vocal cords become thicker and thicker, so that the pronunciation is deep and bright. At the age of 12 to 13 years, pubic hairs appear and gradually become thinner and thicker, thinner and thicker. Underarm hair appears at the age of 16 years, breasts swell, and nipples become darker; beards begin to grow from 16 to 17 years of age, skin becomes rough, subcutaneous fat layer becomes thin, and sebaceous glands secrete vigorously to cause acne (also known as acne); body hair becomes coarse Short thick black chest body hair is also longer, and the hairstyle shows a certain two corners in the forehead recessed into the hairline. Endocrine System

All these phenomena are due to the action of oxymetholone. If oxymetholone is insufficiently secreted, it will not only affect the growth and development of the human body, reduce sexual function, but also have female characteristics that do not have male "male wind". Scientists believe that although endocrine is produced by various endocrine glands, it is also dominated by the nerve center of the brain. People's mental emotions can stimulate the parasympathetic nerve and endocrine system, and strengthen the secretion of the endocrine system through feedback.

Endocrine System Promote blood circulation, strengthen breathing rhythm, increase body temperature, accelerate the body's metabolism and hormone formation, so that young men are handsome and healthy, skin is smooth and elastic, eyes are bright and spirited, the spirit is radiant, and has the beauty of male masculinity. Middle-aged and elderly people have a small number of oxymetholone, sexual function also gradually subsided, the metabolic function of each system is also becoming lower and lower. Therefore, oxymetholone is very important to maintain the youth vitality of men and keep youth alive.

Oxymetholone athletes disabled

Because oxymetholone is a hormonal drug, it is a stimulant in a sense, so for athletes. This medicine is prohibited. The banned drugs used by athletes announced by the State General Administration of Sport are clearly marked with oxymetholone.

Oxymetholone disabled for athletes

Test procedure for athletes: For the endogenous production of an anabolic androgenic steroid listed in the Doping Catalog, the concentration of the banned substance or its metabolite or its marker in the athlete's sample and (or ) In cases where the relevant ratio is out of the normal range of the population and cannot be considered as a normal endogenous generation, this sample is considered to contain this banned substance and the laboratory will report a positive test result. If the athlete can prove that the concentration of the banned substance or its metabolite or its marker in the sample and / or the related ratio abnormality is caused by pathological or physiological reasons, the sample should not be considered to contain the banned substance.

In any case and concentration, if the laboratory can prove that the banned substance is an exogenous source through a reliable analysis method (such as isotope ratio mass spectrometry), the athlete's sample is considered to contain a banned substance and the laboratory will report a positive test result. No further investigation is required in this case

For example, the value of a substance in the test results does not deviate too much from the normal range of the population, and the external source of the substance cannot be confirmed by any reliable analysis method (such as isotope ratio mass spectrometry), but there are some hints such as the reference A comparison of steroid metabolism profiles reveals that a banned substance may be used; or when the laboratory has reported that the testosterone-to-testosterone ratio (T / E) is greater than 4, and the substance cannot be confirmed by any reliable analytical method (such as isotope ratio mass spectrometry) For exogenous sources, the relevant anti-doping organization must investigate this by reviewing the results of previous inspections or further inspections.

For samples that require further investigation, test results should be reported as uncertain rather than positive. If the laboratory reports an extraneous source of the banned substance using additional reliable detection methods (such as isotope ratio mass spectrometry), no further investigation is necessary and the sample is considered to contain the banned substance. Without a reliable analytical method (such as isotope ratio mass spectrometry) and the results of at least three previous inspections do not exist, the relevant anti-doping organization must perform at least three unannounced inspections on the athlete within three months to be tracked Examine the data distribution. The results of this sample requiring follow-up inspection should be reported as uncertain. If the data distribution of these follow-up checks proves that the athlete's test result is abnormal outside the normal physiological range, the result will be reported as a positive result.

Test strip

However, there are very few cases where low concentrations (ng / ml) of endogenous bodidone (botanone) can always be detected in urine samples. If the laboratory reports very low concentrations of bodidone and if any reliable analytical method (such as isotope ratio mass spectrometry) cannot determine that the substance has an exogenous source, further investigation can be performed by follow-up inspection.

If the laboratory reports a positive 19-nordrosterone, the banned substance is an exogenous source. In this case, no further investigation is required. If the athlete does not cooperate with the follow-up inspection, the athlete's sample will be deemed to contain prohibited substances.

The doping list can be divided into specific substances that are particularly likely to cause unintentional violations of anti-doping rules or are unlikely to be successfully abused as stimulants due to their widespread presence in pharmaceutical products. "Violations involving these substances can be punished lightly, but athletes must be able to demonstrate that the use of these specific substances is not intended to improve athletic performance.

Oxymetholone treatment effect

Osteoporosis is a common metabolic bone disease. It is more common in menopausal women. The incidence of osteoporosis in men is only 1/6 of that in women. Under general external force, fractures can occur in those with osteoporosis. Osteoporosis in postmenopausal women is related to endogenous estrogen, a decrease in estrogen,

Granulocytes The inhibitory effect on osteoclasts is weakened, osteoclasts are relatively strengthened, osteoclasts and osteogenesis are clearly imbalanced, bone absorption is increased, bone formation is reduced, and bone mass is gradually lost. In order to improve and improve the quality of life of menopausal women, alternative therapies have received increasing attention in recent years. This article summarizes the progress of drug treatment for correct selection and application. There are two types of hormone replacement therapy, namely the method of simple estrogen administration and the method of combined administration of estrogen and progestin. Depending on the combination of estrogen and progesterone, it can be divided into two types: periodic medication and continuous medication. The former refers to progestin added periodically for 10-14 days on the basis of estrogen medication, and there will be withdrawal bleeding after withdrawal. The latter is a continuous use of low-dose estrogen and progesterone, which has a low vaginal bleeding rate and is currently widely used.

Bone cells

Although hormone replacement therapy is widely used and its effect is accurate, long-term application may cause uterine bleeding, and improper use will also increase the incidence of breast cancer. Therefore, people are always looking for a safe and effective drug that is complementary to estrogen. As early as the 1970s, some people began to use oxymetholone to treat osteoporosis. In the 1980s, it has been systematically used in clinical practice, and it has gradually become an important class of drugs for the prevention and treatment of osteoporosis. The mechanism of oxymetholone treatment of osteoporosis is mainly on osteoclasts. It can specifically aggregate on the surface of osteoclasts, destroy its cell membrane, so that it no longer has the activity of absorbing bone, thereby inhibiting bone resorption. Decreases bone turnover and inhibits the formation of new osteoclasts by altering the properties of the bone matrix that activates the osteoclasts. There are more than ten species of oxymetholone that have been used clinically. Oxymetholone treatment of osteoporosis is a new and highly effective inhibitor of bone resorption, which can inhibit the activity of osteoclasts and reduce bone resorption without directly inhibiting the activity of osteoblasts. The process of bone formation is not affected. Inhibition, which can effectively inhibit bone loss associated with endogenous estrogen reduction, is an alternative treatment for postmenopausal osteoporosis. According to reports, 32 patients with postmenopausal osteoporosis were treated with oxymetholone. After half a year of treatment, the ulnar and radial bone density of all age groups increased significantly, and the total effective rate for the treatment of bone pain increased.

Oxymetholone treatment principle

The white blood cells in the blood are the body's patrol to prevent the invasion of bacteria. When foreign bodies such as bacteria invade, white blood cells enter the invaded site, enclosing, engulfing, and destroying the bacteria. Therefore, white blood cells are known as "white guards" of the human body. It can be seen that the reduction of the number of white blood cells will weaken the human body's antibacterial ability and be susceptible to infection. However, leukopenia does not necessarily require treatment, depending on the degree of reduction; the second depends on the cause of the decrease.

Cell membrane

The normal number of white blood cells is (4 to 10) × 109 / liter, which is 4,000 to 10,000 per cubic millimeter, and the average is 7,000. If it is between 4000 and 7000, it is normal and low, and no treatment is needed; if it is less than 4000, it can be diagnosed as leukocytopenia. Even so, treatment may not necessarily be needed, for example, it is only slightly reduced or transiently reduced, and it does not continue to decline during the review, and there are no symptoms or discomforts, so there is no need for tension and no treatment. Of course, the following cases of white blood cells need attention, and under the guidance of a doctor, take interventions.

A severe reduction in white blood cell count requires urgent treatment. White blood cells are composed of granulocytes, lymphocytes, and monocytes. Generally speaking, the most common and most important thing is the reduction of granulocytes. If the reduction is too obvious, the bacteria may spread rapidly when the body is completely or basically resistant, and even enter the blood to cause sepsis, which is a serious threat to life. .

leukocyte

Caused leukopenia should be treated for the cause. There are three common causes of leukopenia: one is medicine, such as taking antipyretic analgesics, sulfa drugs, etc. At this time, if leukopenia is too obvious, you should stop taking or change medicines; the second is viral infection, such as epidemic Colds, viral infections, etc. At this time, you should actively perform antiviral treatment on the one hand, and take drugs that increase white blood cells, as appropriate. Third, you have immune system diseases such as rheumatoid arthritis, etc. In the same intervention, choose drugs that can increase white blood cells.

Red blood cells and / or thrombocytopenia require further diagnosis and treatment. When leukopenia occurs, if there are abnormal changes in the other two cells in the blood, red blood cells and platelets, the problem is more complicated. The first step is to further check, and the most common is a bone marrow test to rule out the presence of other blood diseases, and then decide treatment plan.

Oxymetholone reference

Chinese Medical Pharmacopoeia

The Golden Doctor