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PubMed1986

Comparison of calcium, calcitriol, ovarian hormones and nandrolone in the treatment of osteoporosis.

Most therapy for osteoporosis has been aimed at decreasing bone resorption and is capable of preventing further bone loss. Recently, anabolic steroids have been claimed to cause increased bone mass in osteoporosis, but the mechanism for this effect is not understood. In this study calcium, and calcium with calcitriol, caused a slowing of forearm bone mineral loss. Calcium and ovarian hormones, with or without calcitriol, caused a small non-significant rise in forearm mineral density, and nandrolone decanoate 50 mg intramuscularly, every 2 or 3 weeks caused a significant rise in forearm mineral density (+15.9 +/- 2.4 mg/ml/yr and +13.7 +/- 3.4 mg/ml/yr, respectively). The 3-weekly regime caused few side effects and is considered the optimal dose. The striking rise in bone density in patients in whom bone resorption was controlled before therapy, suggests that anabolic steroids can increase the bone formation rate.

Aged↗
PubMed2002

Dopaminergic effects after chronic treatment with nandrolone visualized in rat brain by positron emission tomography.

Anabolic-androgenic steroids (AAS) have recently been shown to induce neurochemical alterations in areas of the male rat CNS related to behavioural changes that have been observed among AAS misusers. In the present study, positron emission tomography (PET) is suggested as a suitable in vivo method in order to visualize the density of the dopamine transporter ([11C]-FE-beta-CIT) as well as the dopamine D1-like ([11C]-(+)-SCH23390) and the D2-like receptors ([11C]-raclopride) in the male rat brain. Chronic treatment with the AAS nandrolone decanoate (15 mg/kg/day for 14 days) caused an up-regulation of the binding potential of the dopamine transporter in the striatum.

Anabolic Agents↗
PubMed2003

The anabolic-androgenic steroid nandrolone induces alterations in the density of serotonergic 5HT1B and 5HT2 receptors in the male rat brain.

Anabolic-androgenic steroids (AAS) are partly misused by males in order to become brave and intoxicated and these agents are highly associated with psychosis, disinhibition, aggression and acts of violence. Since such behavioral states have been related to an imbalanced serotonergic system and the involvement of the serotonergic 5HT(1B) and the 5HT(2) receptors, it was important to discern the impact of AAS on these receptors. The objective of our study was to investigate the effects of 2 weeks of treatment with the AAS nandrolone decanoate at three different doses (1, 5, 15 mg/kg/day) on the total specific binding of the radioligands [(125)I]-(+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) (5HT(2) receptors) by autoradiography. All doses caused a significant down-regulation of the 5HT(1B) receptor density in the hippocampal CA(1) and in the medial globus pallidus and a significant up-regulation of the 5HT(2) receptor density in the nucleus accumbens shell. Alterations in receptor density were also observed in the lateral globus pallidus, ventromedial hypothalamus, the amygdala and in the intermediate layers of various cortex regions. In conclusion, serotonergic 5HT(1B) or 5HT(2) receptors are likely to play important roles in mediating observed emotional states and behavioral changes among AAS abusers.

Anabolic Agents↗
PubMed2000

The effect on opioid peptides in the rat brain, after chronic treatment with the anabolic androgenic steroid, nandrolone decanoate.

In recent years, an increase in abuse of anabolic androgenic steroids (AAS) has been seen among individuals not directly connected to sports. Clinical evidence suggests that abuse of these steroids may result in profound changes in personality, expressed by depressive symptoms, irritability and increased aggression. It is still unknown whether these alterations are related to changes in any particular transmitter system or whether they are persistent or reversible. In this study we focused on AAS effect on the endogenous dynorphin and enkephalin system in the brain. Male rats were given intramuscular injections of the AAS nandrolone decanoate (15 mg/kg), once daily for 2 weeks. The levels of the opioid peptide immunoreactivities (ir) were assessed by radioimmunoassay in two groups immediately after the treatment and in two other groups after additional 3 weeks without any drug treatment (recovery period). The result indicates that chronic AAS treatment increased the activity in the dynorphin B- and Met-enkephalin-Arg(6)Phe(7)-ir in the hypothalamus, striatum and periaqueductal gray (PAG) compared to controls. In addition, the steroid induced an imbalance between the dynorphin and the enkephalin opioid system in the nucleus accumbens, hypothalamus and PAG. This imbalance remained after the recovery period. Since increased peptide activity was found in brain regions regulating emotions, dependence, defensive reactions and aggression, it was suggested that the actual endogenous opioid systems are involved in previously reported AAS-induced changes in these behaviours.

Anabolic Agents↗
PubMedDate not supplied

Enzyme-assisted synthesis and structure characterization of glucuronide conjugates of methyltestosterone (17 alpha-methylandrost-4-en-17 beta-ol-3-one) and nandrolone (estr-4-en-17 beta-ol-3-one) metabolites.

A new and useful method based on enzyme-assisted synthesis was developed for producing 3 alpha-O-beta-D-glucuronide conjugates from synthetic phase I metabolites of methyltestosterone and nandrolone. The formed glucuronide conjugates of 17 alpha-methyl-5 alpha-androstane-3 alpha,17 beta-diol (I), 17 alpha-methyl-5 beta-androstane-3 alpha,17 beta-diol (II), 5 alpha-estran-3 alpha-ol-17-one (III), and 5 beta-estran-3 alpha-ol-17-one (IV) are urinary metabolites, indicating the human misuse of the above-mentioned anabolic androgenic steroids (AAS). The common lack of reference material precludes the use and validation of these biomarkers in human doping control. Liver microsomes from Aroclor 1254-induced rats were used as a highly active source of mammalian UDP-glucuronosyltransferases (UGT, EC 2.4.1.17). After purification by protein precipitation, liquid-liquid extraction (dichloromethane), C-18 solid-phase extraction, and lyophilization, the steroid glucuronide structures were characterized by (1)H and (13)C NMR spectroscopy and tandem mass spectrometry. The enzymatic method was highly stereoselective, producing a single major conjugate from the parent steroids I-IV. The stereochemically pure steroid glucuronide conjugates were recovered in milligram amounts (1.0-2.8 mg, yield 12-29%), which is sufficient for veterinary and human doping control analyses; for pharmaco-, toxico-, and enzyme kinetic studies in the pharmaceutical industry; for clinical laboratories; and for forensic medicine. A new sensitive LC-MS method was developed for controlling the product purity in syntheses, as well as for enzyme kinetic characterization of AAS-metabolizing UGT activities in rat liver toward the aglycones I-IV. In this study, the UGT enzymes responsible for the formation of 3 alpha-O-linked glucuronides from the substrates I, II, III, and IV exhibited the specific enzyme activity values: 25, 124, 48, and 212 nmol/mg microsomal protein in a 2-h incubation, respectively.

Animals↗
PubMed1999

The use of an anabolic steroid (nandrolone decanoate) to improve nutritional status after esophageal resection for carcinoma.

Anabolic steroids increase appetite and muscle mass. This randomized, double-blind trial investigates any nutritional benefits of anabolic steroid in patients after surgery for esophageal cancer. Forty patients were recruited: 19 patients had five injections of 50 mg nandrolone decanoate and 21 patients received placebo over 3 months, starting 1 month after surgery. Measurements of body weight, mid-arm muscle circumference (MAMC) and appetite were taken over a 6-month period. Nutrition was optimized by dietary advice and by esophageal dilatation if required. Percent ideal weight, percent ideal MAMC and appetite score did not show significant differences between steroid and placebo groups, but there was a trend to an increase over 6 months for percent ideal MAMC in the test group. With this protocol, we have experienced minimal side-effects. However, we have not demonstrated any therapeutic benefit with low-dose steroid. An increased dose schedule over a longer period might produce a significant response.

Aged↗
PubMed2005

The effect of nandrolone decanoate on bone mineral density, muscle mass, and hemoglobin levels in elderly women with osteoporosis: a double-blind, randomized, placebo-controlled clinical trial.

METHODS: In a randomized, double-blind, placebo-controlled clinical trial, we evaluated the effect of a 2-year treatment with nandrolone decanoate (ND) on bone mineral density (BMD) of lumbar spine, femoral neck, and trochanter and on vertebral fracture rate, muscle mass, and hemoglobin levels. Sixty-five osteoporotic women older than 70 years were studied. Thirty-two patients received injections of 50 mg ND, and 33 received placebos every 3 weeks. All patients received 500 mg calcium tablets daily. RESULTS: Compared to baseline, ND increased the BMD of the lumbar spine (3.4% +/- 6.0 and 3.7% +/- 7.4; p < .05) and femoral neck (4.1% +/- 7.3 and 4.7% +/- 8.0; p < .05) after 1 and 2 years, respectively. The BMD of trochanter increased significantly only after the first year (4.8% +/- 9.3, p < .05). Compared to the placebo group, the ND group presented with significantly increased BMD of the trochanter and neck. ND significantly reduced incidence of new vertebral fractures (21% vs 43% in the placebo group; p < .05). ND showed a significant statistical increase in lean body mass after the first (6.2% +/- 5.8; p < .01) and second years (11.9% +/- 29.2; p < .01). In addition, a 2-year treatment with ND significantly increased hemoglobin levels compared to baseline (14.3%; p < .01) and placebo (p < .01). CONCLUSIONS: ND increased BMD, hemoglobin levels, and muscle mass, and reduced the vertebral fracture rate of elderly osteoporotic women.

Absorptiometry, Photon↗
PubMedDate not supplied

Endogenous nandrolone metabolites in human urine. Two-year monitoring of male professional soccer players.

19-Norandrosterone (19-NA) and 19-noretiocholanolone (19-NE) are the two main indicators used to prove the illegal use of nandrolone by humans. Recent studies showed that 19-NA and 19-NE can be endogenously produced in some individuals. The mediated cases observed over the last three years generated some questions about the appropriateness of the official International Olympic Committee cutoff level, which is 2 ng/mL of 19-NA in male urine samples. In the present study, professional soccer players belonging to the French First League were studied over a period of 19 months. In total, 385 urine samples were taken immediately before and after soccer competitions and were coupled with 200 blood samples for testosterone and LH determination. Results of the study showed that the mean values for 19-NA and 19-NE were 0.097 ng/mL and 0.033 ng/mL, respectively. For 19-NA, 70% of the samples proved to be below 0.1 ng/mL, whereas less than 20% were found to be between 0.1 and 0.2 ng/mL, and 7% were between 0.2 and 0.3 ng/mL. Only four urine samples were above 1.0 ng/mL; the maximal value was 1.79 ng/mL. For 19-NE, only one sample was above 1.0 ng/mL; the value was 1.42 ng/mL. Concentrations of these compounds after games were generally significantly higher than those before games.

Adult↗
PubMed1989

Lichenoid drug eruptions due to nandrolone furylpropionate (Demelon).

A case of lichenoid drug eruption due to nandrolone furylpropionate (Demelon) is reported. A 71-year-old man with aplastic anemia developed widespread erythema and reticulation with violaceous papules and pigmentation after receiving intramuscular injections of Demelon weekly for 2 months. The eruption gradually resolved after drug withdrawal, leaving reticular pigmentation. A biopsy specimen of the skin lesion showed lichenoid-type reactions including hydropic or colloid degeneration of the basal cells, sometimes with satellite necrosis, and a band-like subepidermal lymphocytic infiltrate. Most of the mononuclear cells stained strongly for helper/inducer T lymphocytes (Leu 3a).

Aged↗
PubMed1975

The percutaneous penetration of nandrolone decanoate.

A study has been carried out on the penetration of nandrolone decanoate through human cadaver skin in vitro using radioactive tracer material. The radiochemical purity of the material desorbed from the dermal skin surface is very much less than that of the material absorbed into the epidermal surface. These observations are a consequence of the low level of overall penetration of the skin by the steroid. There is also a possibility that a small percentage of the steroid is being metabolized by micro-organisms present in the skin samples.

Aged↗
PubMed1982

Effects of nandrolone phenylpropionate in the horse: (1) resting animal.

The effects of 7 weekly injections of the anabolic steroid nandrolone phenylpropionate (400 mg) were investigated in 4 healthy, mature geldings. Measurement of body weight, nitrogen retention and plasma urea failed to demonstrate a consistent anabolic effects. Examination of biopsies from the semitendinosus and biceps femoris muscles showed no alteration in water content or glycogen concentration with treatment. Similarly no changes were found in the activities of 6 muscle enzymes. However, a significant increase in the proportion of fast twitch low oxidative fibres of the biceps femoris was observed. The effects of the treatment on a wide range of plasma biochemical constituents were investigated. The occurrence of some components of stallion behaviour in the geldings was taken to reflect a residual androgenic activity in the compound.

Anabolic Agents↗
PubMed2005

Double-blind, placebo-controlled study of the efficacy of nandrolone laurate in the treatment of dobermanns with subclinical hepatitis.

Twenty-one three-year-old dobermanns with subclinical hepatitis were treated with nandrolone laurate or a placebo in a double-blind trial. The dogs were scored clinically before and after four months of treatment and they were evaluated by clinical biochemistry and liver biopsies. After the treatment no significant differences were observed between the two groups in any of the clinical biochemistry values; eight of the 21 dogs had no histological evidence of hepatitis and five other dogs had improved, but there was no significant difference between the responses of the two groups.

Androgens↗
PubMed2002

Role of IGF-I and IGF-binding proteins within diaphragm muscle in modulating the effects of nandrolone.

Recent studies suggest that the anabolic effects of testosterone in muscle may be mediated, in part, by the insulin-like growth factor (IGF) system. The aim of this study was to examine the effects of nandrolone (NAN) on both IGF-I and IGF-binding proteins (IGFBPs) in the diaphragm muscle of 1-yr-old female rats. NAN (6.6 mg. kg(-1) x day(-1)) was infused continuously for 17 days using a subcutaneous Silastic implant, whereas controls (CTL) received blank capsules. Muscle fibers were classified immunohistochemically, and fiber cross-sectional areas (CSA) were determined quantitatively. IGF-I levels in both serum and muscle were determined by RIA. Immunoreactivity to an IGF-I antibody was used to localize IGF-I expression within individual muscle fibers. Muscle IGFBPs were determined by SDS-PAGE and Western ligand blotting and measured by scanning densitometry. Body weight was higher in the NAN group compared with CTL (9.4 +/- 4.5% vs. -0.6 +/- 3.1%). There were no changes in the fiber composition of the diaphragm. NAN increased the CSA of type IIa (20%) and type IIx/b (30%) diaphragm fibers. Levels of IGF-I in the diaphragm muscle were significantly higher (50%) in NAN-treated animals. Immunohistochemistry revealed increased localization of IGF-I within type IIx/b diaphragm fibers. In addition, NAN increased IGFBP-3 within the diaphragm (69%), whereas IGFBP-4 decreased (40%). We conclude that NAN-induced diaphragm muscle fiber hypertrophy is mediated, in part, by influences of the IGF system within the muscle, such that coordinated changes in IGFBPs reflect a direction of change that has been associated with an anabolic response in other test systems.

Anabolic Agents↗
PubMed1999

Alterations in diaphragm contractility after nandrolone administration: an analysis of potential mechanisms.

The aim of this study was to evaluate the potential mechanisms underlying the improved contractility of the diaphragm (Dia) in adult intact male hamsters after nandrolone (Nan) administration, given subcutaneously over 4 wk via a controlled-release capsule (initial dose: 4.5 mg. kg-1. day-1; with weight gain, final dose: 2.7 mg. kg-1. day-1). Control (Ctl) animals received blank capsules. Isometric contractile properties of the Dia were determined in vitro after 4 wk. The maximum velocity of unloaded shortening (Vo) was determined in vitro by means of the slack test. Dia fibers were classified histochemically on the basis of myofibrillar ATPase staining and fiber cross-sectional area (CSA), and the relative interstitial space was quantitated. Ca2+-activated myosin ATPase activity was determined by quantitative histochemistry in individual diaphragm fibers. Myosin heavy chain (MHC) isoforms were identified electrophoretically, and their proportions were determined by using scanning densitometry. Peak twitch and tetanic forces, as well as Vo, were significantly greater in Nan animals compared with Ctl. The proportion of type IIa Dia fibers was significantly increased in Nan animals. Nan increased the CSA of all fiber types (26-47%), whereas the relative interstitial space decreased. The relative contribution of fiber types to total costal Dia area was preserved between the groups. Proportions of MHC isoforms were similar between the groups. There was a tendency for increased expression of MHC2B with Nan. Ca2+-activated myosin ATPase activity was increased 35-39% in all fiber types in Nan animals. We conclude that, after Nan administration, the increase in Dia specific force results from the relatively greater Dia CSA occupied by hypertrophied muscle fibers, whereas the increased ATPase activity promotes a higher rate of cross-bridge turnover and thus increased Vo. We speculate that Nan in supraphysiological doses have the potential to offset or ameliorate conditions associated with enhanced proteolysis and disordered protein turnover.

Anabolic Agents↗
PubMed2003

Overload-induced androgen receptor expression in the aged rat hindlimb receiving nandrolone decanoate.

This study's purpose was to examine whether functional overload with nandrolone decanoate (ND) administration increased muscle mass and steroid receptor concentration in aged rat soleus (Sol) and plantaris (Plan) muscle. ND (6 mg/kg body wt) was administered once a week for 4 wk, whereas control rats received sesame seed oil injections. Functional overload of the hindlimb Sol and Plan was induced by synergistic gastrocnemius muscle ablation at the beginning of the fourth week. Adult (5 mo of age) and aged rats (25 mo of age) were randomly assigned to four groups: control, overload, control-ND, and overload-ND. Seven days of functional overload increased adult Sol muscle mass 27%, whereas the aged Sol muscle mass did not change. The aged overloaded Sol muscle receiving ND significantly increased muscle weight by 35% and total muscle protein by 24%. Aged Plan muscle did not increase muscle weight with overload or ND treatment. Androgen receptor protein was induced by ND treatment and functional Ov, and combining the two treatments induced Sol androgen receptor protein concentration above either alone. Sol glucocorticoid receptor protein concentration increased in overload groups of both ages. ND administration can increase aged Sol muscle mass and protein content after 7 days of functional overload, and the cooperative induction of androgen receptor may be important for this response.

Anabolic Agents↗
PubMed1991

Dose-dependent effects of an anabolic steroid, nandrolone phenylpropionate (Durabolin), on body composition and muscle protein metabolism in female rats.

The effects of three doses (1, 4 and 10 mg/kg body weight) of an anabolic steroid, nandrolone phenylpropionate (NPP), on body weight and composition, and muscle protein metabolism were investigated in female rats. Daily injections of 1 mg/kg of NPP for 10 days caused a significant increase in weight gain which was associated with an increase in body protein (9%) without affecting body fat. At higher doses this effect on body weight was attenuated, resulting in no change in body weight at 10 mg/kg. However body protein content was still increased (9%) whereas body fat content was significantly reduced (32%). NPP did not affect metabolizable energy intake at any dose tested. Body energy gain and gross energetic efficiency were both significantly reduced in animals treated with a dose of 10 mg/kg. The mass and protein content of gastrocnemius muscle were significantly increased in animals injected with NPP at all doses. Muscle protein synthesis measured in vivo was also significantly stimulated at 1 and 4 mg/kg but was not affected at 10 mg/kg. These data confirm an anabolic action of NPP and suggest highly dose-dependent effects on other parameters such as body weight, fat deposition and muscle protein synthesis.

Anabolic Agents↗
PubMed1978

[Androgen therapy of incurable breast neoplasms. Controlled clinical study: nandrolone-testololactone-drostanolone].

In 91 patients with advanced breast cancer testololactone, drostanolone, and nandrolone were compared in a controlled clinical trial. Remissions were registered after 4 weeks and after another 12 week period; during this second interval the patients received an additional treatment with cyclophosphamide. There was no difference in the effectivity between the three drugs. Remission rate was in average after 4 weeks 24% and after 16 weeks 46%.

Androstanols↗