methenolone and methenolone-enanthate

Anabolic androgenic steroids (AAS) are used illicitly at high doses by bodybuilders. The misuse of these drugs is associated with serious adverse effects to the liver, including cellular adenomas and adenocarcinomas. We report two very different cases of adult male bodybuilders who developed hepatocellular adenomas following AAS abuse. The first patient was asymptomatic but had two large liver lesions which were detected by ultrasound studies after routine medical examination. The second patient was admitted to our hospital with acute renal failure and ultrasound (US) studies showed mild hepatomegaly with several very close hyperecogenic nodules in liver, concordant with adenomas at first diagnosis. In both cases the patients have evolved favourably and the tumours have shown a tendency to regress after the withdrawal of AAS. The cases presented here are rare but may well be suggestive of the natural course of AAS induced hepatocellular adenomas. In conclusion, sportsmen taking AAS should be considered as a group at risk of developing hepatic sex hormone related tumours. Consequently, they should be carefully and periodically monitored with US studies. In any case, despite the size of the tumours detected in these two cases, the possibility of spontaneous tumour regression must also be taken in account.

Topics: Adenoma, Liver Cell; Administration, Oral; Adult; Anabolic Agents; Biopsy, Fine-Needle; Humans; Liver Neoplasms; Magnetic Resonance Imaging; Male; Methenolone; Nandrolone; Nandrolone Decanoate; Oxymetholone; Stanozolol; Substance Abuse, Intravenous; Substance-Related Disorders; Testosterone; Testosterone Propionate; Ultrasonography; Weight Lifting

Two fungal cultures Aspergillus niger and Cunninghamella blakesleeana were used for the biotransformation of methenolone enanthate (1). Biotransformation with A. niger led to the synthesis of three new (2-4), and three known (5-7) metabolites, while fermentation with C. blakesleeana yielded metabolite 6. Substrate 1 and the resulting metabolites were evaluated for their immunomodulatory activities. Substrate 1 was found to be inactive, while metabolites 2 and 3 showed a potent inhibition of ROS generation by whole blood (IC50=8.60 and 7.05μg/mL), as well as from isolated polymorphonuclear leukocytes (PMNs) (IC50=14.0 and 4.70μg/mL), respectively. Moreover, compound 3 (34.21%) moderately inhibited the production of TNF-α, whereas 2 (88.63%) showed a potent inhibition of TNF-α produced by the THP-1 cells. These activities indicated immunomodulatory potential of compounds 2 and 3. All products were found to be non-toxic to 3T3 mouse fibroblast cells.

Topics: Adult; Aspergillus niger; Biotransformation; Cells, Cultured; Cunninghamella; Fermentation; Humans; Immunologic Factors; Methenolone; Molecular Structure; Neutrophils; Reactive Oxygen Species; Tumor Necrosis Factor-alpha; Young Adult

Topics: Anabolic Agents; Androgens; Humans; Hypertensive Encephalopathy; Magnetic Resonance Imaging; Male; Methandrostenolone; Methenolone; Young Adult

The aim of this study was the investigation of effects of the metenolone enanthate (ME) that is used among athletes as doping and muscle amplifier, on hearts of male and female rats that are in puberty using morphometrical methods. A total of 36 rats which were divided into three separate groups (Experiment, ME; vehicle, PO; control, C) each consisting of 6 male and 6 female rats were used. 0.5 mg/kg metenolone enanthate was applied intraperitoneally into experiment subjects 5 times a week over a period of 4 weeks. At the end of experiment, rats were euthanized and their hearts were cut at the level of musculus papillaris after the fixation in formalin. Hearts were taken out and embedded in paraffin wax. Photos were taken at cut surfaces, and thickness, diameters and surface area levels were measured. Left ventriculus mass (LVM) and left ventriculus mass index (LVMI) were calculated. In the study LVM (p<0.005) and LVMI (p<0.05) were found to be significantly higher in the ME group in females whereas left ventricular lumen diameter (LVLD) were found to be significantly lower (p<0.05). Thus left ventricular hypertrophy development was observed. LVM and LVMI were found to be similar in ME and C groups among male rats and the highest level of these data were found in the group. LVM and LVMI were higher among females (p<0.006). In conclusion, it has been shown that the adverse effects of ME on heart were developing starting from puberty and resulting with the enlargement of the heart and left ventricular hypertrophy and especially among females this condition was more evident. It has also been discussed that the continuous use of drugs may further enhance this condition.

Topics: Aging; Anabolic Agents; Animals; Body Weight; Female; Heart; Hypertrophy, Left Ventricular; Male; Methenolone; Organ Size; Rats; Rats, Sprague-Dawley; Sex Characteristics

Anabolic-androgenic steroids are widely misused in human sports and are also used as growth promoters in livestock. Athletes who consume meat containing such hormone residues may risk failing a sports drug test. Prompted by an athlete's defense case, we questioned whether the consumption of small livestock given doses of anabolic steroid, orally or intramuscularly, could generate positive results in samples tested by our analytical procedures. We analyzed urine from eight men who consumed chickens that had been either fed with methenolone acetate (1 mg/day) from day 0 to 21 or injected with methenolone heptanoate depot (1 mg/intramuscular injection) on days 0, 7, and 14 and slaughtered on day 22. No methenolone or characteristic major metabolite was detected in samples from subjects who ate meat from the orally dosed chickens. However, 50% of the samples collected 24 h after consumption of the intramuscularly dosed chickens were confirmed positive. Hence, eating meat containing small amounts of injected hormone may constitute a serious liability to the athlete.

Topics: Administration, Oral; Adult; Anabolic Agents; Animals; Chickens; Delayed-Action Preparations; Doping in Sports; False Positive Reactions; Humans; Injections, Intramuscular; Male; Meat; Methenolone; Middle Aged

Lateral radiographs of the thoracic and lumbar spine were taken periodically in 49 patients with osteoporosis. Thirty patients were postmenopausal, and 19 nonmenopausal with osteoporosis due to steroids, male hypogonadism, alcoholism, thyrotoxicosis or unknown cause. Patients were studied before, during and after treatment with high calcium alone, or with combined calcium and sex steroids. Calcium was given as effervescent calcium lactate gluconate, and sex hormones as oestradiol valerate, testosterone oenanthate, or methenolone oenanthate. A total of 964 films covering 409 patient-years were available for measurement. On each vertebra, deformity due to loss of anterior height was measured and assigned to one of four grades. For the time interval between each consecutive pair of films, a patient's vertebral fracture rate score was calculated and expressed per thousand patient-years. In comparison with the corresponding pretreatment fracture rate score, both the postmenopausal and the nonmenopausal groups who had not received sex hormones previously, failed to show significant changes (p = 0.144; p = 0.017) on high calcium alone during mean periods of 4.3 and 2.8 years respectively. If the first 2 years on high calcium were excluded for the postmenopausal group, they still failed to show a reduction in fracture rate score (observed for a mean period of 5.0 years; p = 0.04). When treated with combined calcium and sex hormones, both postmenopausal and nonmenopausal groups showed a lower fracture rate score of 20 and 207 respectively when compared with the pretreatment levels of 1500 and 1697 (in mean treatment periods of 3.2 and 4.4 years; p less than 0.001 in each case). When given high-dose calcium alone, but after treatment with sex hormones as well, the postmenopausal group showed no change in fracture rate score from pretreatment (in a mean of 3.1 years; p = 0.069); however the nonmenopausal group still showed a significant reduction in fracture rate score from 1697 to 42 over a mean period of 2.3 years (p = 0.001). The postmenopausal group, after stopping all treatment, showed a higher fracture rate score of 1286 (in a mean of 2.6 years) than did those on combined calcium and sex hormones, in whom the fracture rate score was 20 (in a mean of 3.2 years; p = 0.008). A subgroup of 11 patients with osteoporosis of both the menopausal and nonmenopausal types, had data both before (in a mean of 5.5 years) and during (for a mean of 2.5 years) treatment with c

Topics: Adult; Calcium; Drug Therapy, Combination; Estradiol; Estrogens, Conjugated (USP); Female; Gonadal Steroid Hormones; Humans; Male; Methenolone; Middle Aged; Osteoporosis; Osteoporosis, Postmenopausal; Spinal Fractures; Testosterone; Time Factors

A randomized blind prospective study was carried out to determine if an anabolic androgenic steroid with a high anabolic/androgenic ratio, Group A, (1/0.05) methenolone enanthate (me), compared to an anabolic/androgenic agent with a low anabolic/androgenic ratio, Group B, (1.0/1.0) testosterone propionate (tp), compared to a control, Group C, cottonseed oil (co), affected midhumeral osteotomy healing in 100 two-month-old female Wistar rats. The rats received 4 mg/kg me, 4 mg/kg te, and equal volumes of co weekly. The rats were sacrificed at 2, 4, and 6 weeks. The entire humerus with the healing osteotomy was carefully dissected until all soft tissue attachments were stripped. The healing callus was then subjected to (1) biochemical analysis (hexosamine, hydroxyproline, and calcium), (2) biomechanical testing (progressive distraction of the callus at 1 mm/min on an electrohydraulic materials test system, model 1331, Instron Corp, Canton, MA, and (3) histology. Results of the biochemical testing demonstrated that the percentage of calcium in the healing callus at 2 weeks in group B (tp) was 7.3 +/- 1.0, and this value was greater than that in group C (co), 4.8 +/- 1.6 (p greater than .01), and greater than that in group A (me), 5.6 +/- 0.6 (p greater than .01). At 4 weeks, the percentage of calcium in the callus in group B (tp) was 6.8 +/- 1.9, in group A (me) 7.3 +/- 3.7, and these values were both greater than that in group C (co), 3.9 +/- 2.2 (p greater than .02 and .01, respectively). At 6 weeks the percentage of calcium in the callus in group B (tp) was 11.7 +/- 3.9 and in group A (me) 12.7 +/- 3.9, and again these values were both greater than that in group C (co), 6.7 +/- 2.6 (p greater than .02 and .01, respectively). The remainder of the biochemical analysis, hexosamine and hydroxyproline content, did not show a statistical difference in groups A, B, and C at 2, 4, and 6 weeks. The biomechanical studies and histology also failed to show statistical differences between the three groups at 2, 4, and 6 weeks. The conclusion of this study is that an agent with a low androgenic activity does not increase calcium callus concentrations early in the course of fracture healing compared to an agent with higher androgenic activity. As healing progresses, both agents increase the concentration of calcium in osteotomy healing. The clinical significance of this study is that agents with low androgenic activities favorably influence osteotomy healing and may be c

Topics: Animals; Bony Callus; Calcium; Disease Models, Animal; Double-Blind Method; Drug Evaluation, Preclinical; Female; Fractures, Bone; Hexosamines; Humerus; Hydroxyproline; Methenolone; Osteotomy; Prospective Studies; Random Allocation; Rats; Rats, Inbred Strains; Stress, Mechanical; Testosterone; Wound Healing

Topics: Animals; Castration; Kidney; Male; Methenolone; Microscopy, Electron; Rats; Rats, Inbred Strains; Testis

Of 27 patients with hypoplastic anemia treated between 1971 and 1974 with male hormone and protein-assimilating hormone, 3 developed superior sagittal sinus thrombosis (SSST). The clinical symptoms and signs and angiographic findings of SST were characteristic enough to allow an early diagnosis. Signs related to SST were seizures, hemiplegia, facial palsy, stupor, and coma, with the most important prodrome and consistent subjective complaint being headache. Following discontinuation of the hormone therapy, neurological signs and symptoms related to SSST gradually subsided. In all cases, the hematological picture improved with discontinuation of the hormone therapies. It appears that administration of male hormone can be associated with the development of SSST. If neurological symptoms and signs of SSST appear, administration of the hormones should be discontinued.

Topics: Adult; Anemia, Aplastic; Cranial Sinuses; Female; Fluoxymesterone; Humans; Intracranial Embolism and Thrombosis; Male; Methenolone; Middle Aged; Oxymetholone; Testosterone; Thrombophlebitis

The medical records of 66 women treated with metenolone for metastasized breast carcinomas were analysed. In 26 patients a remission developed with a mean duration of 8.2 (3-29) months. Patients whose treatment started in the first year after the menopause as well as patients with a beneficial effect of a therapeutic ovariectomy in the past were more often improved by metenolone than average. Metenolone had a better effect against osseous metastases than against visceral metastases. In most cases the treatment was well tolerated. In four patients, however, the treatment had to be interrupted because of cholestasis, pulmonary embolism and hypercalcaemia.

Topics: Adult; Aged; Anabolic Agents; Breast Neoplasms; Castration; Female; Humans; Mastectomy; Menopause; Methenolone; Middle Aged

For the development of an aplastic anaemia a large number of causes is taken into consideration. In our own clinical material of 26 patients in 15 patients none of the up to now known noxae could be established. Recently in the clarification of the picture of the disease important pathophysiological realizations were got. In these cases disturbances of the stem cell compartments, effects through the matrix of the haematopoietic cells and immunological processes have been recognized as significant. --Own investigations concerning the therapy with the anabolic metenolonenanthat (Primobolan-S) yielded approximately the same large number of therapeutic failures and patients with a good result of the treatment or a partial remission in 15 idiopathic and 11 toxically conditioned anaemias. In the partial remissions in most cases a thrombocytopenia continued existing. A therapy lasting at least two months is necessary in order to estimate the result of the therapy. At the present time cannot yet be predicted on which conditions the use of anabolics will be successful.

Topics: Anemia, Aplastic; Autoantibodies; Bone Marrow Cells; Cell Differentiation; Hematopoiesis; Hematopoietic Stem Cells; Humans; Methenolone

Topics: Adolescent; Anabolic Agents; Biomedical Research; Body Weight; Child; Drug Therapy; Humans; Infant; Infant, Newborn; Infant, Premature; Infant, Premature, Diseases; Methenolone; Steroids; Testosterone Congeners; Thinness

Topics: Anabolic Agents; Burns; Drug Therapy; Humans; Methenolone; Steroids; Testosterone Congeners

Topics: Anabolic Agents; Dementia; Depressive Disorder, Major; Drug Therapy; Geriatrics; Methenolone; Psychotic Disorders; Steroids; Testosterone Congeners

Topics: Androgens; Hormone Replacement Therapy; Humans; Methenolone; Postoperative Care; Postoperative Period

Topics: Acetates; Androgens; Animals; Body Weight; Enzymes; Growth; Heptanoates; Methenolone; Testosterone