Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Decanoates”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 343 records · Page 19Linked to original sources
PubMed1996

Haloperidol and reduced haloperidol plasma concentrations after a loading dose regimen with haloperidol decanoate.

1. Haloperidol and reduced haloperidol plasma levels were measured in schizophrenic patients who received both oral (10 mg, N=16 and 20 mg, N=4) and depot haloperidol treatment 2. Patients were of Asian ethnicity and were safely and effectively converted from oral to depot therapy using a loading dose regimen using a 100 mg weekly injection interval for 4 weeks, biweekly for one month and then monthly. 3. Significant correlations were found for plasma haloperidol and reduced haloperidol levels and reduced haloperidol/haloperidol ratios between oral and depot therapy in these non-smoking patients. 4. A loading dose regimen is needed due to the long elimination half-life of decanoate of 26 days otherwise steady-state condition will not occur until 34 months of therapy. 5. Patients were maintained on monthly depot treatment for 40 weeks after the loading dose regimen and only one patient relapsed during treatment despite dosage increases. 6. The formation of reduced haloperidol remained consistent for oral and depot haloperidol treatment.

Adult↗
PubMed1995

Effects of chronic naloxone administration on vacuous chewing movements and catalepsy in rats treated with long-term haloperidol decanoate.

Most antipsychotic medications produce motoric side effects, including parkinsonism and tardive dyskinesia (TD). Correlates of these behaviors in rats (catalepsy and vacuous chewing movements, respectively) were used as a model to assess the usefulness of chronic naloxone administration in symptom reduction. Previous studies have suggested that increased neurotransmission in the endogenous opioid system modulates neuroleptic-induced motoric side effects. Rats were treated with haloperidol decanoate or vehicle for 27 weeks, and withdrawn for 30 weeks. Subsequently, naloxone (0.5 to 2.0 mg/kg SC twice daily) was given for 5 weeks. Long-term haloperidol treatment produced a syndrome of vacuous chewing movements (VCMs) that persisted during the drug withdrawal period. Catalepsy developed rapidly and also persisted. Naloxone treatment had little effect on VCMs but increased catalepsy scores in both haloperidol and vehicle treated groups. Naloxone reduced rearing and grooming in haloperidol rats while increasing these measures in vehicle treated rats. The results indicate that neuroleptic-induced motoric side effects are not reversed by naloxone in rats. Furthermore, they suggest that increased opioid neurotransmission may not underlie the expression of VCMs. This does not rule out the possibility that endogenous opioid system may be involved in the development of VCMs. To the extent that this animal model is valid, naloxone may not be effective in treating TD and neuroleptic-induced parkinsonism in humans.

Animals↗
PubMedDate not supplied

Fluphenazine decanoate dose and severity of depression in patients with post-psychotic depression.

The authors examined the fluphenazine decanoate dose and the fluphenazine plasma levels in comparison with measures of severity of depression in schizophrenic and schizoaffective patients. All patients were selected for study on the basis of having stable, syndromally defined, antiparkinsonian non-responsive syndromes of post-psychotic depression. No meaningful relationships were found. The implications of this observation with regard to the notion that depressive symptomatology in such patients is neuroleptic-induced is discussed.

Adult↗
PubMed1992

The determination of the steady-state pharmacokinetic profile of fluphenazine decanoate by gas chromatography/mass spectrometry detection.

This study uses the highly sensitive method of gas chromatography/mass spectrometry to compare the basic steady-state pharmacokinetic parameters of two fluphenazine decanoate formulations. Sixteen stable outpatients participated in a two-way crossover design study of the bioavailability of a new formulation of FPZ Dec, i.e., 10 mg/ml, to the standard 25 mg/ml formulation. When compared to a 1 ml injection of the standard formulation (25 mg/ml) over a two-week, steady-state period, we found bioequivalence as evidenced by similar mean areas under the curve (hrs x ng/ml). We did find that the injection volume of the same dose (2.5 ml of a 10 mg/ml formulation) results in a statistically significantly higher maximum serum level of parent fluphenazine. A tendency toward faster time to peak level was observed with the 10 mg/ml formulation but the difference was not statistically significant. Both of these differences are considered too small to be clinically significant. In a subgroup of 10 patients, pre-injection serum fluphenazine levels correlated significantly (Pearson r = 0.78, p < 0.05) with serum prolactin levels.

Adult↗
PubMed1993

Prolonged haloperidol and reduced haloperidol plasma concentrations after decanoate withdrawal.

Haloperidol and reduced haloperidol plasma concentrations were measured in twelve schizophrenic patients upon cessation of haloperidol decanoate (HLD) treatment. Each patient received HLD 100 mg every 4 weeks for five injections. After the fifth injection, HLD was discontinued. Haloperidol and reduced haloperidol plasma concentrations were obtained prior to cessation and at weeks 1, 3, 4, 5, 7, 9, 11, and 13 post-injection. Haloperidol and reduced haloperidol plasma concentrations were assayed by HPLC. Both haloperidol and reduced haloperidol plasma concentrations were detectable 13 weeks post HLD discontinuation. Maximal haloperidol plasma concentrations were observed at one week post cessation and gradually declined. The mean elimination half-life for haloperidol was 27.4 +/- 8.6 days (range 19.0-47.0 days). Reduced haloperidol plasma concentrations declined very slowly. Our results show that both haloperidol and reduced haloperidol plasma concentrations can remain for extended time periods after HLD is discontinued.

Adult↗
PubMed1998

Expression of Fos protein in the limbic regions of the rat following haloperidol decanoate.

To identify sites of antipsychotic drug action, the effects of acute and chronic haloperidol treatment on Fos protein expression in rat brain regions were examined by immunohistochemical methods. Male Wistar rats were injected with haloperidol decanoate (40 mg/kg, i.m. ) or vehicle. Fourteen days after injection, each rat was given an acute subcutaneous injection of haloperidol (0.25 mg/kg) or vehicle, and was transcardially perfused 2 h after the second injection. A single dose of haloperidol to chronic vehicle-treated rats produced significant increases in Fos-positive neurons in 18 of 21 brain regions examined including the several cortical areas, caudate-putamen, nucleus accumbens, lateral septum, thalamic nuclei, amygdala, hippocampus CA1, mesencephalic dopaminergic nuclei, and periaqueductal grey. The rats treated with acute vehicle after chronic haloperidol showed persistent Fos increases in confined brain regions comprising the lateral and central amygdala, lateral septum, and entorhinal cortex. Additional haloperidol injection to the chronic haloperidol-treated rats induced significant increases in Fos immunoreactivity in more widespread limbic-thalamo-cortical areas, whereas no significant increase was seen in the dorsolateral caudate-putamen. The persisting effects of haloperidol in the limbic and related structures, especially the amygdala, lateral septum, and entorhinal area may be of significance to the efficacy of long-term haloperidol treatment.

Analysis of Variance↗
PubMed2002

Investigation of a novel preparation of testosterone decanoate in men: pharmacokinetics and spermatogenic suppression with etonogestrel implants.

We have investigated the pharmacokinetics and effects on the male reproductive axis of a novel preparation of testosterone decanoate (TD) with a progestogen implant. Twenty healthy Chinese men were administered TD (400 mg intramuscular 4 weekly) with two subcutaneous (SC) etonogestrel implants. Trough testosterone concentrations rose with repeated administration. Peak concentrations 1 week after the fourth injection were 31 +/- 2 nmol/liter. Both LH and FSH were rapidly suppressed and continued to fall during treatment. Spermatogenesis was also suppressed, to <or=1 x 10(6)/mL in all men with 16 (80%) azoospermic at 12 weeks. Treatment was associated with an increase in weight, and also increases in hemoglobin concentration (9%) and hematocrit (15%). No subjects withdrew from the study, although the study was terminated after subjects had completed 12 to 18 weeks as some men were found to have elevated liver enzyme tests. These data demonstrate that the pharmacokinetics of TD are improved compared to previous injectable testosterone preparations, although peak testosterone concentrations rise briefly into the supraphysiological range. The speed and degree of spermatogenic suppression suggest that this combination has promise as an effective male contraceptive.

Adult↗
PubMed2003

Phase behavior in the system water-butylammonium decanoate-decane.

The phase diagram at 298.2 and 281.2 K for the ternary system water-butylammonium decanoate-decane has been determined. An isotropic solution phase extending from the water corner to the decane corner was obtained without any macroscopic phase separation. A large two-phase region extending from the water-decane axis was also observed. In addition to these phases, an anisotropic and optically birefrigent liquid crystalline phase is formed below 290.3 K. Sound velocity, conductivity, and viscosity measurements were used successfully for studies of microstructural transitions in the isotropic solution phase. From these measurements, it was concluded that a transition from normal micelles to reverse micelles takes place while passing through a bicontinuous region.

Journal Article↗
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↗
PubMed1978

A comparative controlled trial of pimozide and fluphenazine decanoate in the continuation therapy of schizophrenia.

Evidence from a controlled, comparative trial indicates that oral pimozide is clinically at least as effective as depot injections of fluphenazine decanoate in the continuation therapy of a group of schizophrenic patients discharged from hospital. The administration of pimozide was associated with fewer unwanted effects. The implications of the findings are discussed.

Adult↗
PubMed1997

Studies on the mechanism of absorption of depot neuroleptics: fluphenazine decanoate in sesame oil.

PURPOSE: The purpose of the present study was to investigate the pharmacokinetic characteristics of fluphenazine (FLU) and its decanoate (FLU-D) after intravenous and intramuscular administration to dogs. METHODS: A group of four beagle dogs was used in all intravenous and intramuscular experiments, with washout periods of no less than three months between doses. RESULTS: After intravenous FLU-D, the pharmacokinetics of the prodrug (mean +/- SD) were as follows: Clearance (CL) 42.9 +/- 6.3 L/h; terminal half-life (t1/2) 3.5 +/- 0.8 h; volume of distribution (Vd) 216 +/- 61 L. The fractional availability of FLU was 1.0 +/- 0.2. After intravenous FLU, the volume of distribution of FLU (51 +/- 17.8 L) was some 4 fold less than that of the prodrug. Simulations (Stella II) suggested that the rate limiting step was slow formation of FLU from the prodrug in the tissue compartment. After intramuscular FLU-D in sesame oil, the apparent t1/2 of FLU was 9.7 +/- 2.0 days whereas after intramuscular FLU base in sesame oil, the apparent t1/2 was only 7.7 +/- 3.4 h showing that the absorption of FLU itself from the intramuscular site and proximal lymph nodes is relatively rapid. CONCLUSIONS: The rate limiting step after intramuscular FLU-D appeared to be the slow partitioning of the prodrug out of the sesame oil at the injection site and in proximal lymph nodes.

Absorption↗
PubMed1977

A controlled trial of nondrolone decanoate in the treatment of uremic anemia.

Thirty-seven male dialysis patients, from three university hospital centers known to have adequate iron B12, and folate stores, were entered into a controlled trial to study the effects of nandrolone decanoate (200 mg i.m. weekly) on their anemia. An initial six-month stabilization period was followed by a randomized 12-month study, with crossover between treatment and control groups occurring at six months. Patients received parenteral iron therapy plus oral folate throughout the trial. All serious illnesses or major blood losses excluded the patients from analysis. The 24 patients with remnant kidneys showed an increase in hemoglobin and hematocrit of 24% by the end of six months of treatment (P less than 0.005), with a corresponding decrement during the six months of control, but the five anephric patients showed no statistically significant change compared to those patients whose kidneys were in place during the study. Complications of treatment were minimal, with injection site hematoma the only significant local effect and a rise in triglyceride the only significant systemic disturbance. Despite the improvement in anemia, the disadvantages, including the high cost of treatment, the apparent plateauing of benefits by five months, the minimal subjective improvement in life style, the risk of i.m. injection, plus the long term effects of increased lipids, should limit this therapy to patients with remnant kidneys who have severe symptomatic anemia or frequent transfusion requirements.

Adult↗
PubMed2002

The anabolic androgenic steroid, nandrolone decanoate, increases the density of Fos-like immunoreactive neurons in limbic regions of guinea-pig brain.

The increased abuse of anabolic androgenic steroids is a major concern because of physiological and psychological side-effects. In some individuals they induce dramatic behavioural changes such as increased aggression, anxiety and depression. The mechanisms behind these behavioural changes are still poorly understood. In order to obtain information on the brain regions affected by anabolic androgenic steroids, the distribution of neurons containing c-Fos, the protein product of the immediate early gene c-fos, and Fos-related antigens was studied following chronic treatment of guinea-pigs with a high dose of nandrolone decanoate (15 mg/kg i.m. daily for 14 days). The behaviour of the guinea-pigs was monitored for 1 h each day. Animals treated with nandrolone exhibited a significantly greater incidence of biting behaviour during the 14 day treatment period than vehicle-treated animals. A significantly greater density of c-Fos and Fos-related antigen-positive neurons was found in the central nucleus of the amygdala, and of Fos-related antigen-positive neurons in the frontal cortex, the shell of the nucleus accumbens and the supraoptic nucleus in nandrolone-treated animals than in vehicle controls. Therefore, nandrolone induced Fos in brain regions involved in stress, behavioural responses and reward. The increased Fos expression in these limbic brain regions is of particular interest in relation to the behavioural changes reported in humans who abuse anabolic androgenic steroids and the abuse potential of these drugs.

Aggression↗
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↗
PubMed1978

[Studies on the long acting neuroleptic agent flupenthixol decanoate--a review (author's transl)].

The development of long acting neuroleptic agents is considered as important progress in the treatment of schizophrenic psychoses. An outline of pharmacological and clinical results with flupenthixol decanoate is given. Special attention is paid to pharmacokinetics, the methods for determining plasma concentration, to the profile of action and duration of action, to other dosage as well as to safety. Importance is also placed on the possible use for prophylaxis of affective psychoses.

Delayed-Action Preparations↗
PubMed1994

Zuclopenthixol decanoate in maintenance treatment of schizophrenic outpatients. Minimum effective dose and corresponding serum levels.

23 schizophrenic outpatients in maintenance treatment with zuclopenthixol decanoate were included in a study aimed at finding the minimum effective dose and corresponding serum concentration of zuclopenthixol. Every three months the dose was gradually reduced until prodromal symptoms appeared, indicative of an incipient relapse. A slightly higher dose was then promptly reinstituted (the minimum effective dose). At each dose level, two blood samples were drawn to determine the serum concentration. This dose reduction principles proved feasible. Only one patient had a clear-cut relapse. The condition of the remaining patients was acceptably maintained by a dose increase. The minimum effective dose of zuclopenthixol was 200 mg/2 weeks (range 60-400), with a serum concentration of 22 nmol/l (7.1-69.7). There was a significant correlation between the administered dose and the corresponding serum level of the drug (r = 0.66, P < 0.01). A trend towards a positive correlation was found between the serum level at the minimum effective dose and the BPRS score (r = 0.42, P < 0.1). No correlation was found between the serum level and the side-effects or length of neuroleptic treatment. It is concluded that routine serum drug monitoring is hardly indicated in the long-term depot-neuroleptic treatment of schizophrenic patients. A strategy aiming at continually seeking the lowest effective dose on the basis of clinical parameters appears more appropriate, especially in case of depot-neuroleptic treatment.

Adult↗
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↗