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PubMed1977

Pharmacology of cis(Z)-clopenthixol decanoate, a depot neuroleptic.

The duration and intensity of the neuroleptic effect of cis(Z)-clopenthixol decanoate in Viscoleo have been compared with those of cis(Z)-clopenthixol, 2 HCl in aqueous solution in a number of animal experimental models. Cis(Z)-clopenthixol, 2 HCl had a strong, but short-lasting neuroleptic effect (apomorphine antagonistic effect in dogs, inhibition of conditioned avoidance response in rats) which was accompanied by marked sedation. In contrast, cis(Z)-clopenthixol decanoate in oil had an effect which was slower in onset, but of much longer duration and only the highest doses caused a slight sedation. In rats catalepsy could be induced in some animals by high doses of cis(Z)-clopenthixol decanoate whereas cis(Z)-clopenthixol, 2 HCl at all the doses tested caused catalepsy in all animals. In mice only high doses of cis(Z)-clopenthixol decanoate in oil caused reduction of spontaneous motor activity and potentiation of barbiturate anaesthesia. The results are discussed with special reference to the clinical use of the depot preparation.

Administration, Oral↗
PubMed1984

A 5-year follow-up study of chronic schizophrenics treated with clopenthixol decanoate.

Twenty-three chronic schizophrenic patients were followed-up over periods up to 5 years (1978-1983) while receiving treatment with depot injections of clopenthixol decanoate in doses ranging from 100 to 600 mg every 2 to 4 weeks. The highest single dose given was 1600 mg. Improvement in psychotic symptoms occurred progressively over the 5 years, with reduction in mean overall symptom score for schizophrenia from 7.43 to 0.88. Mean side-effects scores decreased over the same period from 2.0 to 0.5. After 5 years, 10 patients were still maintained on clopenthixol decanoate. Although during the first 2 months there was little improvement in 'negative' or 'loss' symptoms, improvement was similar in 'positive' and 'negative' symptoms after 5 years. Clopenthixol decanoate appeared to have a better calming effect than that encountered with flupenthixol decanoate. At higher doses, it caused drowsiness and subdued hostility and aggression.

Adult↗
PubMed1993

[Intraindividual comparison of haloperidol decanoate and oxyprothepine in maintenance therapy in schizophrenic psychoses].

In an open intraindividual comparison of haloperidol and oxyprothepine decanoates there was a tendency in favour of haloperidol decanoate. At the end of 9 months' maintenance treatment there were no statistically significant differences in the global BPRS score, CGI and individual BPRS items with exception of paranoidity. No differences in the occurrence of rehospitalizations and ambulatory relapses were found. As for side effects with haloperidol decanoate a higher occurrence of akathisia and a lower mean weigh increase (2 kg v. 4 kg) were observed and twice more pts had no side effects in comparison with oxyprothepine decanoate, but also these differences were not statistically significant. Taking into consideration the differences found (even if not statistically significant) and the individual reactivity, it seems to us advantageous to have a broader choice of depot neuroleptics.

Adult↗
PubMedDate not supplied

Lack of a strong influence of neuroleptic decanoates on dopaminergic and GABAergic functions.

Data concerning the incidence of extrapyramidal symptoms and the development of the supersensitivity to dopamine after administration of depot neuroleptics are controversial. The aim of the study was to examine the influence of depot neuroleptics on the sensitivity of dopamine receptors and GABA nigral receptors. Haloperidol decanoate (30 or 60 mg/kg im) and fluphenazine decanoate (12.5 or 25 mg/kg im) were injected twice at a 15 day interval. These treatments induced weak but very long-lasting catalepsy (60-105 days depending on the neuroleptic and its dose). The only significant enhancement of the apomorphine (0.25 mg/kg sc) stereotypy was observed 135 days after the lower dose of haloperidol and 230 days after the lower dose of fluphenazine. Haloperidol decanoate (30 mg/kg) did not influence the number of contralateral rotations induced by muscimol (10 or 25 ng/0.5 microliter) injected into the substantia nigra pars reticulata 35, 55 and 135 days after the first injection. Present results indicate that the dopaminergic supersensitivity after administration of depot neuroleptics is weak and appears very late, and that haloperidol decanoate does not induce nigral supersensitivity to GABA. It is suggested that the depot neuroleptics might induce less extrapyramidal symptoms in the clinic than the daily neuroleptic treatment.

Animals↗
PubMed1996

[Rhabdomyolysis and acute renal failure caused by haloperidol-decanoate (neuroleptic malignant syndrome)].

A case of rhabomyolysis with attendant severe acute renal failure, arisen in a 59-year-old male treated with haloperidol-decanoate, is presented. The patient has been affected by paranoia schizophrenia since childhood, and he was treated with electroshock and successively with neuroleptics p.o. Four years before our observation, a therapy with haloperidol decanoate (50 mg i.m. monthly) was started. After some time, catatonic like episodes appeared, which got more and more frequent, until they appeared weekly. In occasion of the last of them, he was admitted to our hospital. At the objective examination he presented psychomotory arrest, perspiration, mytacism, severe muscle rigidity, moderate oedems to lower limbs. Laboratory findings showed a pattern consistent with rabdomyolysis and severe renal failure. After that haloperidol decanoate was stopped and rehydration and intensive diuretic therapy was started, the clinical and laboratory pattern went normal, persisting however a light creatinine increase. Probably the rhabdomyolysis was induced by the haloperidol decanoate, and renal failure by secondary severe hyvolemia. This case comes into the so-called neuroleptic malignant syndrome which can rarely arise in patients treated with antipsycotic agents and which causes high mortality, particularly when there are rhabdomyolysis and acute renal failure.

Acute Kidney Injury↗
PubMed1988

Rectal absorption enhancement of rate-controlled delivered ampicillin sodium by sodium decanoate in conscious rats.

Because of the relatively poor intestinal absorption of ampicillin sodium, efforts have been made to enhance ampicillin absorption by co-administration of absorption promoters. In the present study the enhancing effect of sodium decanoate on rate and extent of rectal ampicillin absorption in rats has been evaluated after rate-controlled and site-controlled delivery of aqueous solutions. Rectal absorption without enhancer was extremely low (8 +/- 7%), and the addition of 0.032 M sodium decanoate gave comparable values. However, administration in 0.16 M decanoate considerably increased ampicillin bioavailability, to 79 +/- 30%, whereas the absorption rate was not significantly affected.

Administration, Rectal↗
PubMed1975

Stimulatory effect of glucose upon triglyceride synthesis from acetate, decanoate, and palmitate by mammary gland slices from lactating mice.

Slices prepared from the mammary glands of lactating mice incorporate only small amounts of (1--14C) acetate, (1--14C) decanoate, or (1--14C) palmitate into lipids. However, when glucose is added to the incubation medium, fatty acid incorporation is stimulated-13-fold from acetate, 17-fold from decanoate, and 2-fold from palmitate. Over 90% of the -14C activity in the lipid fraction is in triglycerides. Analysis of fatty acids in the triglycerides showed that almost all of the decanoate and the palmate were incorporated as intact molecules, while acetate yielded acids of varying chain lengths. The glucose stimulation of triglyceride synthesis is not solely due to its effect upon chain elongation but also could involve glyceride-glycerol availability, as well as other unknown factors. However, from measurements of the amounts of glycerol 3-phosphate in the tissue incubated in the presence of palmitate, it would appear that glyceride-glycerol availability is not rate limiting in triglyceride synthesis.

Acetates↗
PubMed2006

Hexyl decanoate, the first trail pheromone compound identified in a stingless bee, Trigona recursa.

Foragers of many species of stingless bees guide their nestmates to food sources by means of scent trails deposited on solid substrates between the food and the nest. The corresponding trail pheromones are generally believed to be produced in the mandibular glands, although definitive experimental proof has never been provided. We tested the trail following behavior of recruits of Trigona recursa in field experiments with artificial scent trails branching off from natural scent trails of this stingless bee. First-time recruits (newcomers) did not follow these trails when they were laid with pure solvent or mandibular gland extract. However, they did follow trails made with labial gland extract. Chemical analyses of labial gland secretions revealed that hexyl decanoate was the dominant component (72.4 +/- 1.9% of all volatiles). Newcomers were significantly attracted to artificial trails made with synthetic hexyl decanoate, demonstrating its key function in eliciting scent-following behavior. According to our experiments with T. recursa, the trail pheromone is produced in the labial glands and not in the mandibular glands. Hexyl decanoate is the first component of a trail pheromone identified and proved to be behaviorally active in stingless bees.

Animal Communication↗
PubMed2004

Positional distribution of decanoic acid: effect on chylomicron and VLDL TAG structures and postprandial lipemia.

Although medium-chain FA (MCFA) are mainly absorbed via the portal venous system, they are also incorporated into chylomicron TAG; therefore, the positional distribution of MCFA in TAG is likely to affect their metabolic fate. We studied chylomicron and VLDL TAG structures, as well as the magnitude of postprandial lipemia, after two oral fat loads containing decanoic acid (10:0) predominantly at the sn-1(3),2 (MML) or at the sn-1,3 positions (MLM) of TAG in a randomized, double-blind, crossover clinical trial with 10 healthy, normal-weight volunteers. An MS-MS method was used to analyze TAG regioisomers. The position of decanoic acid in chylomicron TAG reflected its position in the TAG ingested, and TAG with none, one, two, or three decanoic acid residues were detected after ingestion of both fats. More (P < 0.05) 30:0 and 38:1 TAG (acyl carbons:double bonds) and fewer 46:5, 54:5, and 54:4 TAG were found in chylomicrons after ingestion of MML than after MLM. The VLDL TAG composition did not differ between the fat loads but did change (P < 0.05) 2 to 6 h after ingestion of both fats. No statistical differences were seen between the fat loads in areas under the plasma, chylomicron, or VLDL TAG response curves or in FFA concentrations. Thus, the positional distribution of MCFA in TAG affects their metabolic fate, but the magnitude of postprandial lipemia does not seem to be dependent on the positional distribution of MCFA in the ingested fat.

Adult↗
PubMed1985

Effects of nandrolone decanoate in NZB/W mice treated concomitantly with maintenance doses of dexamethasone sodium phosphate.

Treatment of female or castrated male NZB/W mice with nandrolone decanoate (80 mg/kg s.c.), once every three weeks, delays the onset of murine lupus and associated symptoms, even when treatment was started at the 17th week of age. Continuous low dose glucocorticoid therapy did not affect the therapeutic effects of the nandrolone decanoate injections. These results indicate that SLE patients receiving maintenance low dose glucocorticoid therapy may also benefit from treatment with nandrolone-decanoate.

Animals↗
PubMed2005

Histological assessment of ovaries and uterus of rats subjected to nandrolone decanoate treatment.

This study aimed to analyze the effects of nandrolone decanoate on the ovaries and uterus of adult females rats. This drug was administered intraperitoneally, at one, two and three doses of 3 mg nandrolone decanoate/kg of body weight, respectively, in the first, second and third week of treatment. The females of the control group received a physiological solution. The rats treated with nandrolone decanoate showed estral acyclicity and there was destruction of follicular units and an absence of corpus luteum in the ovaries. In the uterus, the drug promoted morphological alterations, characterized by vacuolated epithelium and endometrial stroma fibrosis. Ovary, uterus and pituitary weights were not affected by the steroid treatment. Nandrolone decanoate affects the sexual cycle and promotes histological alterations in the ovaries and uterus of adult female rats.

Anabolic Agents↗
PubMed2005

Phase behavior and rheological properties of enzymatically synthesized trehalose decanoate aqueous solutions.

Surface tension properties of an enzymatically synthesized equimolar mixture of trehalose mono- and didecanoate in aqueous solutions have been determined. At 20 degrees C a critical micellar concentration (CMC) of 50 micromol/l and a minimal surface tension of 28 mN/m have been obtained. Above the CMC, it has been shown that up to a concentration of 42 wt%, and in a 20-60 degrees C temperature range the sugar ester aqueous solutions do not form any crystalline structure, nor present any phase transition, and the trehalose decanoate molecules form an isotropic worm-like micellar phase. The rheological properties indicate however a more complicated picture in the same concentration and temperature ranges. In steady shear, the viscosity of the trehalose decanoate solutions do not exhibit any shear rate dependence from 1 to 100 s(-1) for concentrations up to 42 wt%. Below 0.8 wt%, the viscosity remains constant and close to that of water; then, between 0.8 and 23 wt%, the viscosity shows a quadratic increase with surfactant concentration. For higher concentrations, up to 42 wt%, no further significant increase in viscosity is observed. In oscillatory shear experiments, the solutions exhibit viscoelastic properties. The observed rheological behavior as a function of concentration and temperature may be due to a progressive evolution of the trehalose decanoate molecular associations: as the concentration increases, the system evolves towards an entangled and/or partially branched or cross-linked micellar network, and eventually a multiconnected network of cross-linked micelles.

Cross-Linking Reagents↗
PubMed2005

Administration of the anabolic androgenic steroid nandrolone decanoate affects substance P endopeptidase-like activity in the rat brain.

The effect of the anabolic androgenic steroid, nandrolone decanoate, on substance P endopeptidase-like activity was examined in adult male Sprague-Dawley rats. Nandrolone decanoate (15 mg/kg day) or oil vehicle (sterile arachidis oleum) were administered by intramuscular injections during 14 days. Substance P endopeptidase, a predominantly cytosolic enzyme, generates the bioactive N-terminal fragment substance P(1-7) from the enzyme substrate substance P. Nandrolone decanoate significantly reduced the substance P endopeptidase-like activity compared to control animals in hypothalamus (43% reduction), caudate putamen (44%), substantia nigra (32%) and the ventral tegmental area (27%). It was previously reported that both hypothalamus and caudate putamen contained significantly higher levels of substance P after nandrolone administration. The higher concentration of substance P in these regions could to an extent be attributed to the reduction in substance P endopeptidase-like activity. This result elucidates the important role of peptidase activity in the regulation of the substance P transmitter system. The present study provides additional support for the hypothesis that alterations in the substance P system in certain brain areas may contribute to some of the personality changes reported in connection with AAS abuse.

Amygdala↗
PubMed1996

Effects of the anabolic steroid nandrolone decanoate on plasma lipids and coronary arteries of female cynomolgus macaques.

In this study, we examined the effect of nandrolone decanoate, and anabolic steroid (AS), on plasma lipid concentrations and coronary arteries of female cynomolgus monkeys fed a moderately atherogenic diet. There were four treatment groups: (1) intact, sham-ovariectomized (n = 12); (2) ovariectomized (OVX) + placebo for 2 years (n = 15); (3) OVX + nandrolone decanoate for 2 years (n = 14); and (4) OVX + nandrolone decanoate beginning 1 year after ovariectomy (n = 11). Serial blood samples were analyzed for total plasma cholesterol (TPC), high-density lipoprotein cholesterol (HDL-C), very-low-density lipoprotein (VLDL-C) plus low-density lipoprotein (LDL-C) cholesterol, and estradiol. All animals were necropsied after 2 years, and the coronary arteries were evaluated. There was no difference in plasma lipid concentrations between groups (P > .05) at any time. Coronary artery atherosclerosis extent (plaque size) was significantly greater in the group administered nandrolone for 2 years compared with the intact sham-operated group (P < .05), but not with the OVX + placebo group. The groups administered nandrolone had significantly larger arteries than the other two groups. Lumen area was significantly larger in the group given nandrolone for 1 year compared with all other groups (P < .05). All artery effects remained after controlling the statistical analysis for body weight. Longer-term treatment with nandrolone resulted in increased plaque size, and therefore, the possible benefit of increased lumen area was compromised. The data also suggest that nandrolone was converted to estradiol, and this conversion also may play a role in the arterial and lipid effects observed.

Anabolic Agents↗
PubMed1997

The androgenic anabolic steroid nandrolone decanoate prevents osteopenia and inhibits bone turnover in ovariectomized cynomolgus monkeys.

We examined the effects of nandrolone decanoate (25 mg im every 3 weeks) on bone mass, serum biomarkers, and bone histomorphometric endpoints in 52 female cynomolgus macaques randomized into four treatment groups: (1) sham-ovariectomized (sham); (2) ovariectomized + placebo for 2 years (ovx); (3) ovx + nandrolone decanoate for 2 years (Nan); and (4) ovx + nandrolone decanoate beginning 1 year after ovx (dNan). Serum alkaline phosphatase (ALP), osteocalcin, and tartrate-resistant acid phosphatase (TRAP) were assayed every 3 months, and X-ray densitometry of the lumbar spine was done every 6 months. Fluorochrome-labeled iliac biopsies collected at baseline and 1 year, and lumbar vertebrae and midshaft femur collected at 2 years, were evaluated histomorphometrically. Body weight increased over 50% with administration of nandrolone. After 2 years, ovx animals had lower spinal BMC and BMD than all other groups. Ovx animals also had higher bone turnover rates than all other groups, as indicated by higher levels of the serum and urine biomarkers, and by at least twofold higher label-based bone formation rates in the femur diaphysis and in both cancellous and cortical bone of the ilium and vertebral bodies. Nandrolone-treated animals had similar serum estradiol levels as the sham animals, presumably due to conversion of endogenous or exogenous androgens. The effects of nandrolone on bone in this experiment are consistent with estradiol action and may be attributable to the increased serum estradiol. Despite >50% higher body weight, nandrolone-treated, ovariectomized animals did not have higher bone mass than sham animals.

Absorptiometry, Photon↗
PubMed1996

Safety and efficacy of nandrolone decanoate for treatment of wasting in patients with HIV infection.

OBJECTIVE: To evaluate the safety and efficacy of the anabolic steroid, nandrolone decanoate (Deca Durabolin) in patients with HIV wasting who are resistant to nutritional intervention. DESIGN: A 16-week open trial with subjects who had lost 5-15% of their usual body weight. SETTING: HIV/AIDS specialist ambulatory care services, both public and private, in sydney, Australia. PARTICIPANTS: Two hundred and twenty men entered the pre-therapy phase, and of these, 24 failed to gain weight and were enrolled. Seventeen subjects (81%) completed the 16-week trial. INTERVENTIONS: Pre-therapy nutritional assessment and education was conducted by the clinical dietitian. Those who failed to gain weight (10.9%) were treated with nandrolone decanoate (100 mg/ml) by deep intramuscular injection every 2 weeks for 16 weeks. MAIN OUTCOME MEASURES: Changes in weight and body composition (lean body mass, total body water and nitrogen index) were measured by anthropometry, bioelectrical impedance, and in vivo neutron activation. Changes in quality of life were assessed by the 30-item Medical Outcomes Study short form questionnaire. Changes in biochemistry, haematology and immunology were also measured. RESULTS: There were significant increases in weight (mean, 0.14 kg per week; P < 0.05) and lean body mass (mean, 3 kg by anthropometry; P < 0.005). The change in lean body mass was of similar magnitude across all measurement modalities. Quality of life parameters, especially functionality, increased significantly during the trial. No subject experienced toxicity. CONCLUSION: Nandrolone decanoate has beneficial effects on weight, lean body mass and quality of life in selected patients who have mild to moderate HIV wasting.

Acquired Immunodeficiency Syndrome↗
PubMed1998

Nandrolone decanoate for men with osteoporosis.

To compare the efficacy and safety of nandrolone decanoate and calcium (NDC) with those of calcium alone (CAL) in men with idiopathic osteoporosis, a 12-month, randomized, prospective, controlled study, was performed in an outpatient clinic. Twenty-one men with idiopathic osteoporosis (as determined by radiological and dual energy x-ray absorptiometry findings) were randomly allocated to either 50 mg nandrolone decanoate intramuscularly (im) weekly and 1,000 mg oral calcium carbonate daily (NDC group) or to 1,000 mg oral calcium carbonate daily (CAL group). Bone densitometry (total body, left femur, and lumbar spine), serum, and urine biochemical parameters were measured at 3-month intervals. In the NDC group, bone mineral density initially increased, reached a plateau, and then decreased to near baseline levels at 12 months. Increases in lean muscle mass mirrored these changes. Free and total testosterone significantly decreased. Hemoglobin increased in all patients in this group. Patients in the CAL group exhibited no significant change in either total body or bone mineral density or biochemical parameters. Thus, nandrolone decanoate, 50 mg im weekly, transiently increases the bone mass of men with idiopathic osteoporosis in this preliminary study. Careful monitoring is necessary.

Absorptiometry, Photon↗
PubMed2005

Chronic administration of nandrolone decanoate does not increase the plasma homocysteine level of male rats.

Androgenic-anabolic steroids are used widely by many athletes in order to increase muscle mass and strength. Since plasma total homocysteine, an independent risk factor of vascular diseases, is higher in men than in women, it has been proposed that androgenic hormones could increase the plasma total homocysteine level and it might play some role in sudden death when used at supraphysiological doses. To study the association between the use of androgenic-anabolic steroids and plasma homocysteine level, nandrolone decanoate was administered in 3 and 10 mg/kg doses to male rats by intramuscular weekly injections. Control animals received the solvent of nandrolone decanoate. After 14 weeks, plasma total homocysteine level was measured. In order to make sure about the adequacy of doses and bioavailability of drug, testes parameters were also considered. While all testes parameters were suppressed significantly, no association between androgenic-anabolic steroids use and total homocysteine level was found. It is concluded that chronic administration of nandrolone decanoate does not have any significant effect on plasma total homocysteine of male rats. Thus, factors other than plasma total homocysteine level may contribute to increased cardiovascular events after chronic abuse of androgenic-anabolic steroids.

Anabolic Agents↗