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PubMed1995

Nandrolone decanoate: pharmacological properties and therapeutic use in osteoporosis.

The therapeutic profile on bone of nandrolone decanoate is that of inhibitor of bone resorption with temporary increase in bone formation, followed by an absence of suppression of bone formation, indicating uncoupling of bone resorption and formation. This results is an increase in bone mineral content at the proximal and distal radius, and in some patients at the lumbar spine. Furthermore, nandrolone decanoate increases calcium balance and muscle mass, diminishes vertebral pain and increases the mobility of the spine. Virilization occurred in around 50% of the patients (mainly hoarseness and/or hirsutism), and 9% of the patients dropped out because of this reason. A dose of 50 mg every 3 to 4 weeks is indicated in the treatment of osteoporosis in women, especially when they have low muscle mass, associated debilitating disease, and in patients with corticosteroid induced osteoporosis. It should only be prescribed after the age of 65 to 75 years to minimize the occurrence of clinical adverse effects and to increase its tolerability, which is higher in this group. Although some effects are reported on fracture rate, insufficient prospective data are available.

Aged↗
PubMed1987

Effects of nandrolone decanoate on forearm mineral density and calcium metabolism in osteoporotic postmenopausal women.

Although anabolic steroids have been used for many years to treat osteoporosis there is little available evidence about their efficacy or mode of action. These agents have recently been shown to produce an increase in total body calcium and bone density and it has been suggested that they stimulate bone formation. In this study 27 osteoporotic postmenopausal women were given 50 mg of nandrolone decanoate intramuscularly, every 2 or 3 weeks for 3 months, and the changes in forearm mineral density, fasting plasma, and urinary calcium, urinary hydroxyproline, and radiocalcium absorption were measured. Associated with a rise in forearm mineral density was a significant fall in fasting urinary calcium, but no significant change in fasting urinary hydroxyproline. The plasma calcium and phosphate fell significantly and there was a significant rise in the renal tubular reabsorption of calcium and a fall in the renal tubular reabsorption of phosphate. In a subset of 22 patients there was a significant rise in radiocalcium absorption. The results are consistent with the concept that nandrolone exerts a significant positive effect on bone formation and that this results in a fall in the fasting plasma calcium level, and consequently calcium excretion.

Absorption↗
PubMed1986

Effects of nandrolone decanoate or testosterone decanoate on murine lupus: further evidence for a dissociation of autoimmunosuppressive and endocrine effects.

Nandrolone decanoate injections (20, 40 or 80 mg/kg/3 weeks) in female or castrated male New Zealand black/white mice, starting at various ages (4, 9, 17 or 26 weeks) prolong survival, reduce proteinuria and affect the weights of various endocrine and non-endocrine organs. Nandrolone decanoate is at least equally potent as testosterone decanoate with respect to its beneficial effects on lupus-associated symptoms; in contrast, its effects on some other androgen-sensitive endocrine parameters are significantly less. These observations show that the autoimmunosuppressive effects of steroids are not quantitatively correlated to endocrine properties.

Animals↗
PubMed1991

The prevention of corticosteroid-induced osteoporosis with nandrolone decanoate.

The effects of nandrolone decanoate (ND; 50 mg IM every three weeks) on calcium metabolism and forearm bone density were studied in a randomized trial in 35 women receiving long-term therapy with corticosteroids (CST) for rheumatic disease. The 17 patients who served as controls were on CST therapy for less years and their bone density was higher. Thus a second control group, pair-matched with the active treatment group for age, duration of CST therapy and bone density, was selected retrospectively. At the end of the 18 months' treatment course with ND, forearm bone density was increased by 5.1% (P less than 0.01) but fell by 11.3% (P less than 0.01) and 6.7% respectively in the first and second control group. The patients on ND differed significantly from both control groups in the changes at 6, 12 and 18 months (P less than 0.01). Urinary excretion of hydroxyproline fell significantly in patients receiving ND, whereas the biochemical indices of bone formation did not change (alkaline phosphatase) or increased (osteocalcin; P less than 0.01). In conclusion, nandrolone decanoate therapy may be used in the prevention of CST-induced osteoporosis. It also seems to exert mild inhibition of bone resorption without affecting or even stimulating bone formation.

Absorptiometry, Photon↗
PubMed2005

The impact of chronic nandrolone decanoate administration on the NK1 receptor density in rat brain as determined by autoradiography.

Adult male Sprague-Dawley rats were treated with the anabolic androgenic steroid nandrolone decanoate (15 mg/kg day) or oil vehicle (sterile arachidis oleum) during 14 days. The effect on the densities of the neurokinin NK1 receptor in brain was examined with autoradiography. An overall tendency of attenuation of NK1 receptor density was observed after completed treatment with nandrolone decanoate. The density of the NK1 receptor was found to be significantly lower compared to control animals in the nucleus accumbens core (37% density reduction), in dentate gyrus (26%), in basolateral amygdaloid nucleus (23%), in ventromedial hypothalamic nucleus (36%), in dorsomedial hypothalamic nucleus (43%) and finally in the periaqueductal gray (PAG) (24%). In the cortex region, no structures exhibited any significant reduction of NK1 receptor density. This result provides additional support to the hypothesis that substance P and the NK1 receptor may be involved as important components that participate in mediating physiological responses including the adverse behaviors often associated with chronically administrated anabolic androgenic steroids in human.

Animals↗
PubMed2003

Chronic administration with nandrolone decanoate induces alterations in the gene-transcript content of dopamine D(1)- and D(2)-receptors in the rat brain.

Some adolescent and young males are engaged in misuse of anabolic-androgenic steroids (AASs) in connection with multiple drug use, in order to become intoxicated and brave, apart from currently known motives connected to sports performance and physical appearance. Recent studies suggest that alterations in neurobiological circuits implicated in the regulation of reward-related learning, aggression and motoric behavior underlie the behavioral changes associated with AAS misuse. We have previously shown that AASs induce alterations in dopamine receptor densities. The aim of the present study was to investigate if these effects could be attributed to altered mRNA content for tyrosine hydroxylase, L-amino acid decarboxylase, dopamine D(1)- and dopamine D(2)-receptor as measured by in situ hybridisation. Male Sprague-Dawley rats were subjected to 2 weeks of treatment with daily intramuscular injections of the AAS nandrolone decanoate at three different doses (1, 5 and 15 mg/kg/day). Results of the in situ hybridization showed that the mRNA content of the dopamine D(1)-receptor subtype was significantly reduced at all doses in the caudate putamen and at the highest doses in the nucleus accumbens shell. The mRNA expression of the dopamine D(2)-receptor was significantly increased at the two lowest doses in the caudate putamen and the nucleus accumbens shell. In conclusion, nandrolone has been shown to affect the expression of gene transcripts of dopaminergic receptors possibly implicated in underlying mechanisms of reward-related behavioral changes among AAS misusers.

Anabolic Agents↗
PubMed1997

The effects of 17 alpha-methyltestosterone, methandrostenolone, and nandrolone decanoate on the rat estrous cycle.

In a series of four separate experiments, the effects of anabolic-androgenic steroid (AAS) compounds on the estrous cycle of adult Long-Evans rats were examined. Sexual receptivity, vaginal cytology, and body weight were monitored throughout a 2-week baseline, AAS treatment, and recovery periods. In Experiments 1-3, subjects were administered 17 alpha-methyltestosterone, methandrostenolone, or nandrolone decanoate at doses selected to mimic the human abuse levels of each compound. In these studies, the highest doses of 17 alpha-methyltestosterone (7.5 mg/kg) and nandrolone decanoate (5.6 mg/kg) disrupted behavioral and vaginal cyclicity, whereas the highest dose of methandrostenolone (3.75 mg/kg) appeared to have slightly less robust effects. To compare effects on estrous cyclicity across AAS compounds, subjects in Experiment 4 received a single high dose (7.5 mg/kg) of each compound for 2 weeks. At this dose, all AAS compounds interfered with vaginal cyclicity, although effects on behavioral cyclicity and uterine weight were not uniform. Across all 4 experiments, AAS effects on body weight were minimal. The short-term administration of AAS compounds at levels commonly used by humans disrupts female neuroendocrine function in a dose-dependent manner.

Anabolic Agents↗
PubMed1996

Comparison of the effects of 17 alpha-methyltestosterone, methandrostenolone, and nandrolone decanoate on the sexual behavior of castrated male rats.

In a series of 3 experiments, adult male Long-Evans rats were castrated and treated with 1 of 3 different anabolic-androgenic steroid (AAS) compounds (17 alpha-methyltestosterone, methandrostenolone, or nandrolone decanoate) for 6 weeks. In each experiment, subjects received daily injections of a high, medium, or low dose of AAS or the oil vehicle. The AAS effects on body weight in gonadectomized male rats were modest, and no effects on locomotor activity were observed. The AAS compounds administered at doses comparable with human abuse levels were not equipotent in maintaining male sexual behavior patterns (nandrolone decanoate > methandrostenolone > 17 alpha-methyltestosterone). In addition, the behavioral actions of AAS compounds did not parallel stimulation of sexual accessory glands. The authors reported that this study is the first to quantify the dose-response characteristics of individual AAS compounds with regard to these behavioral and endocrine measures.

Anabolic Agents↗
PubMed2001

The anabolic-androgenic steroid nandrolone decanoate affects the density of dopamine receptors in the male rat brain.

In recent years a male group of anabolic-androgenic steroid misusers has been identified to share socio-demographic and personality related background factors with misusers of psychotropic substances, as well as being involved in habits of multiple drug use. The present study aimed to assess whether anabolic-androgenic steroids (AAS) would affect the density of the dopamine receptors in areas implicated in reward and behaviour in the male rat brain. The effects of 2 weeks of treatment with i.m. injections of nandrolone decanoate (15 mg/kg/day) on the expression of the D(1)-like and D(2)-like receptors were evaluated by autoradiography. Specific binding of D(1)-like receptors was significantly down regulated in the caudate putamen, the nucleus accumbens core and shell. D(2)-like receptor densities were down regulated in the nucleus accumbens shell, but up regulated in the caudate putamen, the nucleus accumbens core and the ventral tegmental area. These results are compatible with nandrolone induced neuroadaptive alterations in dopamine circuits associated with motor functions and behavioural paradigms known to be affected following AAS misuse.

Anabolic Agents↗
PubMed2003

Nandrolone decanoate enhances hypothalamic biogenic amines in rats.

PURPOSE: To identify possible mechanisms for an anabolic-androgenic steroid induced increase in aggressive behavior and work capacity, the levels of some biogenic amines considered to be closely related to a systemic hyper-adrenergic state were measured in selected regions of the brain. METHODS: Wistar male rats were divided randomly into five groups: nontreated (control), oil-vehicle-treated (vehicle) or one of three (therapeutic dose and 10- or 100-fold higher dose) anabolic-androgenic steroid-treated (steroid-1, -2, -3) groups. Rats in the steroid and vehicle groups were given a single dose of nandrolone decanoate or oil vehicle, respectively, one week before tissue sampling. The levels of norepinephrine (NE) and its metabolite, 4-hydroxy-3-methoxyphenylglycol (MHPG), serotonin (5-HT) and its metabolite, 5-hydroxy-indole-3-acetic acid (5-HIAA) were measured in the cerebral cortex, hypothalamus and cerebellum by high-performance liquid chromatography. Immunostaining for c-fos was performed as a confirmation of increased neural activity. RESULTS: The levels of NE and MHPG were increased by approximately 2- and approximately 7-fold in the hypothalamus of the steroid-2 compared with the control and vehicle groups. The levels of 5-HT and 5-HIAA were approximately 40 and approximately 50% higher in the steroid-2 compared with the control and vehicle groups. A significantly higher number of c-fos expressing neurons were observed in the periventricular region of the steroid-2 than the control and vehicle groups, indicating enhanced neuronal activity after nandrolone decanoate treatment. CONCLUSIONS: The present results, combined with previously reported findings of physical performance enhancement after anabolic-androgenic steroid treatment, are consistent with the interpretation that elevated levels of adrenergic and serotonergic amines in the hypothalamus could contribute to aggressive behaviors as well as improved physical performance.

Anabolic Agents↗
PubMed1997

Effects of nandrolone decanoate on respiratory and peripheral muscles in male and female rats.

Thirty male and 18 female adult rats received weekly an intramuscular injection of either saline (control; C), 1.5 mg/kg (low-dose; LD) nandrolone decanoate or 7.5 mg/kg (high-dose; HD) nandrolone decanoate during 5 wk. Compared with respective C, growth rate was stunted in male HD rats from 2 wk of treatment on, whereas it was enhanced in female LD and HD rats after 1 wk. Mass of all muscles studied varied proportionally to body weight, except for the gastrocnemius (males: 0.49 +/- 0.04 vs. C: 0.52 +/- 0.03%, not significant; females: 0.17 +/- 0.01 vs. C: 0.15 +/- 0.01%, P < 0.05). In vitro contractile and fatigue properties of the diaphragm remained unchanged, except for a decrease in twitch kinetics (time to peak tension: C, 21 +/- 2; LD, 19 +/- 1; HD, 19 +/- 2 ms, P < 0.05; half-relaxation time: C, 26 +/- 5, LD, 25 +/- 5, HD, 23 +/- 3 ms, P < 0.01). Histochemistry of the diaphragm and the gastrocnemius revealed a significant increase in type IIx/b dimensions. In the gastrocnemius, type I fiber dimensions also increased. A pair-fed study, including another 24 female rats, showed that the changes in oral food intake only partly accounted for the observed anabolic effects.

Anabolic Agents↗
PubMed2000

Nandrolone decanoate does not enhance training effects but increases IGF-I mRNA in rat diaphragm.

To examine whether concomitant anabolic steroid treatment combined with training might enhance previously observed training effects (A. Bisschop, G. Gayan-Ramirez, H. Rollier, R. Gosselink, R. Dom, V. de Bock, and M. Decramer. Am. J. Respir. Crit. Care Med. 155: 1583-1589, 1997) and whether insulin-like growth factor I (IGF-I) was involved in these changes, male and female rats were submitted to inspiratory muscle training (IMT) for 8 wk (30 min/day, 5 times/wk) and were compared with untrained controls. During the last 5 wk of training, trained rats were divided to receive weekly either low-dose (LD; 1.5 mg/kg) or high-dose (HD; 7.5 mg/kg) nandrolone decanoate or saline for the IMT and control rats. In both sexes, diaphragm muscle mass and contractile properties were unchanged with treatment. In males, HD resulted in decreased diaphragm type I cross-sectional area (-15%; P < 0.05, HD vs. IMT), whereas no changes were observed in females. Finally, an increase in IGF-I mRNA levels was present in HD male (+73%; P < 0.05, HD vs. IMT) and female treated rats [LD (+58%) and HD (+96%) vs. IMT; P < 0.001]. We conclude that administration of nandrolone decanoate did not enhance the previously observed training effects in rat diaphragm, although it increased the IGF-I mRNA expression levels.

Anabolic Agents↗
PubMed2004

Nandrolone decanoate and load increase remodeling and strength in human supraspinatus bioartificial tendons.

BACKGROUND: To date, no studies document the effect of anabolic steroids on rotator cuff tendons. STUDY DESIGN: Controlled laboratory study. HYPOTHESIS: Anabolic steroids enhance remodeling and improve the biomechanical properties of bioartificially engineered human supraspinatus tendons. METHODS: Bioartificial tendons were treated with either nandrolone decanoate (nonload, steroid, n = 18), loading (load, nonsteroid, n = 18), or both (load, steroid, n = 18). A control group received no treatment (nonload, nonsteroid [NLNS], n = 18). Bioartificial tendons' remodeling was assessed by daily scanning, cytoskeletal organization by staining, matrix metalloproteinase-3 levels by ELISA assay, and biomechanical properties by load-to-failure testing. RESULTS: The load, steroid group showed the greatest remodeling and the best organized actin cytoskeleton. Matrix metallo-proteinase-3 levels in the load, steroid group were greater than those of the nonload, nonsteroid group (P <.05). Ultimate stress and ultimate strain in the load, steroid group were greater than those of the nonload, nonsteroid and nonload, steroid groups (P <.05). The strain energy density in the load, steroid group was greater when compared to other groups (P <.05). CONCLUSIONS: Nandrolone decanoate and load acted synergistically to increase matrix remodeling and biomechanical properties of bioartificial tendons. CLINICAL RELEVANCE: Data suggest anabolic steroids may enhance production of bioartificial tendons and rotator cuff tendon healing in vitro. More research is necessary before such clinical use is recommended.

Adult↗
PubMed2002

Post-effects of nandrolone decanoate treatment on contractile responses of rat skeletal muscles.

The post-effects of nandrolone decanoate treatment (15 mg.kg(-1).week(-1)) were studied on contractile responses of isolated small bundles of intact slow-(soleus) and fast-(extensor digitorum longus, edl) twitch fibers in rat. Five weeks of treatment induced, in edl, an increase in the amplitude of twitch (55%) and K(+) contracture (32%) without significant change in the time constant of relaxation and caffeine contracture. In soleus, an increase in the amplitude of twitch (35%) and caffeine contracture (0.2 mM: 218%, 0.5 mM: 88%, 5 mM: 28%, and 10 mM: 25%) was observed without change in K(+) contracture characteristics. In addition to these effects, 10 weeks of drug treatment increased the amplitude of soleus K(+) contracture (29%) and edl caffeine contracture (0.2 mM: 247%, 0.5 mM: 170%, 5 mM: 29%, and 10 mM: 45%), and reduced the 50% recovery time for K(+) contracture (EC(50)) (soleus: 37%, edl: 12%). After 5-week treatment followed by 5-week arrest, as compared to the control group, no change in the amplitude of twitch, K(+) or caffeine contractures was found in edl. In soleus, although no significant difference was observed in the amplitude of twitch, the amplitude of K(+) (35%) and caffeine contractures (0.2 mM: 227%, 0.5 mM: 128%) remained greater than the control group. Moreover, the EC(50) values were prolonged (46%) in soleus, whereas no significant difference was observed in edl. The present work suggests that nandrolone decanoate treatment induced differential post-effects on contractile responses developed in slow- and fast-twitch skeletal muscles by acting differently on the different steps of the excitation-contraction coupling mechanism.

Anabolic Agents↗
PubMed2003

Nandrolone decanoate reduces changes induced by hindlimb suspension in voltage-dependent tension of rat soleus muscle.

The effect of 8 weeks of nandrolone decanoate treatment (15 mg kg(-1)/week, 5 weeks under normal conditions followed by 3 weeks of unloading) was tested for the voltage-dependence of activation and steady-state inactivation of contraction in isolated small bundles (2-4 cells) of intact slow-twitch skeletal muscle in rats. Twenty-four male rats were divided into three groups (8 rats/group, weight matched) for 8 weeks: (1) control, (2) unloaded, and (3) unloaded-treated. Compared with age-matched control values (unloaded vs. control), suspension induced a shift in the isometric tension characteristics toward fast-twitch types in the soleus muscle. In contrast, nandrolone decanoate treatment of suspended animals reduced unweighting-induced atrophy in the muscle and maintained: (1) the relative amplitude of twitch tension to the maximal Ca(2+) activated in saponin-treated fibers (control: 3.6 +/- 0.4%, unloaded: 6.9 +/- 1.1% and unloaded-treated: 4.6 +/- 0.2%), (2) the time to peak tension (control: 130 +/- 18 ms, unloaded: 85 +/- 12 ms and unloaded-treated: 110 +/- 11 ms), (3) the time constant of relaxation (control: 320 +/- 12 ms, unloaded: 120 +/- 13 ms and unloaded-treated: 349 +/- 20 ms), (4) the relative amplitude of K(+) contracture tension to the maximal Ca(2+) activated in saponin-treated fibers (control: 82.9 +/- 3.1%, unloaded: 65.1 +/- 2.8%, and unloaded-treated: 91.7 +/- 1.9%), (5) the potential at 50% of the activation curve (control: -40.4 +/- 1.2 mV, unloaded: -35.5 +/- 1.6 mV, and unloaded-treated: -48.4 +/- 1.2 mV), and (6) the potential at 50% of the inactivation curve (control: 42.2 +/- 1.9 mV, unloaded: -34.5 +/- 1.1 mV, and unloaded-treated: -37.9 +/- 1.1 mV). This study clearly shows that treatment with anabolic-androgenic steroids can prevent atrophy and functional changes induced by 3 weeks of unweighting in rat skeletal muscles.

Animals↗
PubMed1989

Effects of nandrolone decanoate and antiresorptive therapy on vertebral density in osteoporotic postmenopausal women.

Conventional antiresorptive therapy for osteoporosis can delay bone loss, but secondary inhibition of bone formation appears to prevent an increase in bone density. Recently, anabolic steroid therapy has been shown to increase total body calcium and forearm density in osteoporotic patients, perhaps by causing an increase in bone formation. It is not known if these agents affect vertebral density. We have measured vertebral mineral density in 71 postmenopausal osteoporotic women before and after treatment with either the anabolic steroid nandrolone decanoate or antiresorptive therapy. After a mean treatment period of 14 months, there was a mean increase of 20% in vertebral mineral density in the former group, and no significant change in the latter group. The difference in the time-weighted mean rates of change between the two groups was significant. The results suggest that nandrolone decanoate therapy increases bone formation.

Aged↗
PubMed1986

Therapeutic effects of nandrolone decanoate, tibolone, lynestrenol and ethylestrenol on Sjögren's syndrome-like disorder in NZB/W mice.

Growth of mononuclear cell infiltration in submandibular glands is significantly inhibited by Org OD14 (tibolone), lynestrenol and ethylestrenol given orally to New Zealand Black/White (NZB/W) mice from 26 weeks of age onwards. In addition, the extent of already established mononuclear cell infiltrations is significantly inhibited and reduced by nandrolone decanoate injected from 43 weeks of age onwards. Tibolone and nandrolone decanoate are the most potent of the four drugs. The therapeutic effect of these four steroids on the Sjögren's syndrome-like disorder in NZB/W mice is not related to their endocrine activities.

Animals↗
PubMed2000

Consequence of boar edible tissue consumption on urinary profiles of nandrolone metabolites. I. Mass spectrometric detection and quantification of 19-norandrosterone and 19-noretiocholanolone in human urine.

For the first time in the field of steroid residues in humans, demonstration of 19-norandrosterone (19-NA: 3alpha-hydroxy-5alpha-estran-17-one) and 19-noretiocholanolone (19-NE: 3alpha-hydroxy-5beta-estran-17-one) excretion in urine subsequent to boar consumption is reported. Three male volunteers agreed to consume 310 g of tissues from the edible parts (meat, liver, heart and kidney) of a boar. The three individuals delivered urine samples before and during 24 h after meal intake. After deconjugation of phase II metabolites, purification and specific derivatisation of target metabolites, the urinary extracts were analysed by mass spectrometry. Identification was carried out using measurements obtained by gas chromatography/high resolution mass spectrometry (GC/HRMS) (R = 7000) and liquid chromatography/tandem mass spectrometry (LC/MS/MS) (positive electrospray ionisation (ESI+)). Quantification was realised using a quadrupole mass filter. 19-NA and 19-NE concentrations in urine reached 3.1 to 7.5 microg/L nearby 10 hours after boar tissue consumption. Levels returned to endogenous values 24 hours after. These two steroids are usually exploited to confirm the exogenous administration of 19-nortestosterone (19-NT: 17beta-hydroxyestr-4-en-3-one), especially in the antidoping field. We have thus proved that eating tissues of non-castrated male pork (in which 17beta-nandrolone is present) might induce some false accusations of the abuse of nandrolone in antidoping.

Adult↗