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A non-invasive method is described for estimating dopamine beta-hydroxylase (DBH) activity in sympathetic neurons. Our assay is based on the measurement of the in vivo rate of tritiated water (THO) release from dopamine specifically labeled in the beta-position ([beta-3H]DA). In validation of this method, we have establsihed in human subjects that 1) THO release from [beta-3H]DA correlates with [beta-3H]norepinephrine metabolite excretion, and 2) partial inhibition of DBH with disulfiram (5.5 mg/kg for 4 days) causes parallel decreases in these two indices of dopamine beta-hydroxylation. Since there is a strong correlation (r = 0.89; P < 0.05) between the effect of disulfiram on THO release and the effect of the drug on [3H]-norepinephrine metabolite excretion, our data indicate that the rate at which THO is liberated from [beta-3H]DA into the total body water can be used as an in vivo index of DBH activity.
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Neither oral tariquidar nor oral disulfiram increased brain uptake of (11)C-dLop. Injecting (11)C-dLop during tariquidar infusion, when plasma tariquidar concentrations reach their peak, resulted in a brain uptake of the radioligand approximately 5-fold greater than baseline. Brain uptake was similar with 2 and 4 mg of intravenous tariquidar per kilogram; however, the lower dose was better tolerated. Injecting (11)C-dLop after tariquidar infusion also increased brain uptake, though higher doses (up to 6 mg/kg) were required. Brain uptake of (11)C-dLop increased fairly linearly with increasing plasma tariquidar concentrations, but we are uncertain whether maximal uptake was achieved.
Preparations of sheep liver cytoplasmic aldehyde dehydrogenase obtained by published methods were found by analytical isoelectric focusing in the pH range 5--8 to contain 5--10% by weight of the mitochondrial aldehyde dehydrogenase. Under the conditions used the pI of the cytoplasmic enzyme is 6.2 and that of the mitochondrial enzyme 6.6. The mitochondrial enzyme can be removed from the preparation by selective precipitation of the cytoplasmic enzyme with (NH4)2SO4. Kinetic experiments and inhibition experiments with disulfiram show that the properties of the two sheep liver enzymes are so different that the presence of 10% mitochondrial enzyme in preparations of the cytoplasmic enzyme can introduce serious errors into results. Our results suggest that the presence of 10 microM-disulfiram in assays may completely inactivate the pure cytoplasmic enzyme. This result is in contrast with a previous report [kitson (1978) Biochem. U. 175, 83--90].
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This study supports the position that the experience of an acetaldehyde reaction is not necessary for disulfiram's action and does not lead to a better treatment outcome. Hence, there is no evidence for the necessity of a test drink before the initiation of a supervised disulfiram therapy.
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The emergence of large, computerized pharmacoepidemiologic databases has enabled us to study drug utilization with the individual user as the statistical unit. A recurrent problem in such analyses, however, is the overwhelming volume and complexity of data. We here describe a graphical approach that effectively conveys some essential utilization parameters for a drug. The waiting time distribution for a group of drug users is a charting of their first prescription presentations within a specified time window. For a drug used for chronic treatment, most current users will be captured at the beginning of the window. After a few months, the graph will be dominated by new, incident users. As examples, we present waiting time distributions for insulin, ulcer drugs, systemic corticosteroids, antidepressants, and disulfiram. Appropriately analyzed and interpreted, the waiting time distributions can provide information about the period prevalence, point prevalence, incidence, duration of use, seasonality, and rate of prescription renewal or relapse for specific drugs. Each of these parameters has a visual correlate. The waiting time distributions may be an informative supplement to conventional drug utilization statistics, and possibly also a useful screening tool for unusual prescribing patterns.
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A total of 595 patients (48.4%) were diagnosed with depression (DSM-IV criteria). The prevalence of SUD (excluding nicotine dependence) in this group was 18.1%. The group with SUD had a significantly larger proportion of males, young adults, patients seen in public general hospitals, and non-managed care public plans. No significant group differences were found for primary payer, locus of care, length of treatment, type of current or past treatment, and prescription of medications. Only 2.2% of SUD patients were prescribed with an anti-SUD medication (i.e., disulfiram and naltrexone).
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A rapid and simple HPLC-ED method is described to identify and measure catecholamines (CTs) and their major metabolites in immune cells. Using this method, intracellular CTs were quantified in human peripheral blood mononuclear cells (PBMCs), T and B lymphocytes, monocytes and granulocytes. Immune cell subsets were separated by density gradient centrifugation and immunomagnetic cell sorting. CTs were also found in the human hematopoietic cell lines NALM-6 (pre-B) and (in smaller amounts) in Jurkat (T lymphoblastoid) and U937 (promonocytic). In cultured PBMCs, intracellular CTs were reduced by both the tyrosine hydroxylase inhibitor alpha-methyl-p-tyrosine and the chromaffin granule depletant reserpine. In NALM-6 cells, both alpha-methyl-p-tyrosine and the dopamine-beta-hydroxylase inhibitor disulfiram reduced intracellular CTs, supporting the presence of active synthetic pathways in these cells. Since sympathoadrenergic mechanisms play a key role in the interactions between the immune system and the nervous system, these findings may be relevant for a better understanding of the neuro-immune network.
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The effects of carbon disulfide (CS2), diethyldithiocarbamate (DTC) and disulfiram (DS) on hepatic drug metabolism were studied in a noncirculating and hemoglobin-free rat liver perfusion system using p-nitroanisole (p-NA) as a substrate. Infusion of 1 mumol of CS2 into a normal rat liver instantaneously lowered the free p-nitrophenol (p-NP) concentration in the effluent perfusate; however, the effects on the levels of its glucuronide and sulfate conjugates were much less marked. The suppression of p-NP production by CS2 was also observed in livers isolated from phenobarbital (PB)- and 3-methylcholanthrene (3-MC)-treated rats; to a greater extent, in the normal and 3-MC groups. Partial recovery was observed in the normal and PB-treated groups, but it was slow and slight in the 3-MC-treated group. Infusion of DTC, up to 20 mumol, did not lower free p-NP levels, but a slight transient increase was noted, especially in the 3-MC-group. Using 50 mumol of DTC, a slight suppression resulted. DS, up to 20 mumol, did not decrease p-NP production, but rather gradually increased it, especially in the 3-MC-treated groups. Without the p-NP infusion, about 60-70% of the infused DS (10 mumol) was recovered in the effluent perfusate as DTC plus its glucuronide conjugate, the formation of the latter being greatly enhanced by the inducer treatments and markedly suppressed during the p-NP infusion. In this paper, these results are discussed with regards to the mechanisms of drug metabolism inhibition by DS administration.
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To examine the roles of oxygen free radicals in the inhibition of tumor cell proliferation, we have used disulfiram (DS), a metal-chelator, to inactivate superoxide dismutase and ascorbic acid (AsA) to inhibit catalase. Simultaneous addition of DS and AsA to Meth A tumor cells or Ehrlich ascites tumor cells induced marked inhibition of the cell proliferation assessed by [3H]thymidine uptake and trypan blue dye exclusion method. Similar augmented inhibition of Meth A tumor cell proliferation was observed when the cells were pretreated with DS and AsA. However, the addition of catalase (2000 u/ml) nullified the augmentation of anti-proliferative effect which can be induced in the combined use of DS and AsA. These results suggest that the steady-state increase of intracellular oxygen free radicals within tumor cells could be induced in the combined use of DS and AsA.
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Quinazoline oxide--an intermediate in chlordiazepoxide synthesis--is the most potent contact allergen in the pharmaceutical industry. Penicillins proved to be potent allergens. Conditions of the technological process favor development of hypersensitivity to tetracyclines. No single case of allergy to erythromycin was noted. In case of employees hypersensitive to disulfiram and aminophylline cross reactions with compounds of similar structure were observed. The authors discuss also some problems concerning contact allergy in all persons occupationally dealing with various medicines.
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To examine the factors influencing the pattern and extent of anti-craving medication adherence and drinking outcomes in alcohol-dependent patients.
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The present study examines the metabolism of 3,4-dimethoxy-2-phenylethylamine in vitro and in freshly prepared and cryopreserved guinea pig liver slices and the relative contribution of different aldehyde-oxidizing enzymes was estimated by pharmacological means.
Two cases of disulfiram peripheral neuropathy are discussed. The first case is that of a 25-year-old Caucasian woman who was exposed to disulfiram therapy for a total of 8 months and developed pain and stiffness that prevented her from walking. The second case is that of a 46-year-old Caucasian woman who developed sudden-onset numbness in her lower extremities with progression to pain. Her symptoms improved over the course of 2 months after cessation of disulfiram therapy. In both cases, symptoms improved after cessation of disulfiram therapy.
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A 39-year-old woman developed a severe sensorimotor polyneuritis after simultaneous ingestion of ethanol and disulfiram in high doses. The disorder was similar to other cases of disulfiram neuropathy, but was acute and more severe. Disulfiram can cause a fulminant polyneuropathy that is not always benign and reversible.
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The treatment of cocaine dependence is difficult as no approved pharmacotherapy is available as yet. However, in preclinical and clinical trials, a variety of compounds were tested for suitability as inhibitors of craving for and relapse into the use of cocaine, among these antidepressants, antiepileptics, dopamine agonists, disulfiram, and naltrexone. Nalmefene, a structural derivative of naltrexone, shares with its parent compound approval (granted by the European Medical Agency in 2013) as a medication for the treatment of alcohol addiction in the European Union. It differs from naltrexone by a higher affinity for the δ opioid-receptors and a partial agonistic affinity to the κ opioid-receptors. It should be noted that patients addicted to cocaine show a considerable increase in κ receptors in the nucleus accumbens. This report describes the case of an abstinent cocaine-addicted patient regularly afflicted with cravings for cocaine. The patient took as-needed nalmefene for 5 months whenever she developed a craving for cocaine. For most of these interventions, the patient reported an abatement of craving and could avoid relapsing into cocaine consumption. This effect may be accounted for by nalmefene acting, other than naltrexone, as a partial agonist of the κ opioid-receptors. Therefore, nalmefene might be a promising new option in the pharmacological repertoire for the treatment of cocaine addiction.
Disulfiram is widely used for aversive treatment of alcoholism. Neuropathy is one of the most severe side effects of disulfiram therapy. We report the case of a young man who developed a neuropathy following disulfiram administration, with a virtually complete recovery within 2 months.
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The thresholds for pentylenetetrazol and lidocaine-induced clonic convulsions were significantly influenced by manipulation of brain biogenic amines. Pretreatment with inhibitors of monoamine synthesis, alpha-methyl-p-tyrosine and p-chlorophenylalanine, caused significant decreases in brain monoamine contents and pentylenetetrazol seizure threshold, while the threshold for lidocaine-induced convulsions was significantly increased by either treatment. Moreover, the inhibitor of dopamine-beta-hydroxylase, disulfiram, caused significant decrease in brain noradrenaline (NA) and significant increase in brain dopamine (DA) contents. The threshold for pentylenetetrazol-induced convulsions was decreased by treatment with disulfiram, while that of lidocaine was increased by the same treatment. Furthermore, treatment with L-dihydroxyphenylalanine (L-DOPA) caused significant increase in brain DA contents, while 5-hydroxytryptophan (5-HTP) treatment caused significant increase in brain 5-hydroxytryptamine (5-HT) contents, but the thresholds for lidocaine and pentylenetetrazol-induced convulsions were not influenced by either treatment. These results may suggest that the brain monoaminergic systems, different from their ability to inhibit control of pentylenetetrazol seizures, act to potentiate lidocaine-induced convulsions.
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The behavioral therapies evaluated did not significantly differ in effectiveness for African Americans and whites, suggesting that they are broadly applicable across these ethnic groups. Findings also suggest possible strategies for improving retention of African Americans in treatment. Such strategies might include offering treatment with a medication component and better addressing participants' treatment expectations.
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Abstinence behaviour after disulfiram implantation has been investigated in 21 chronic alcoholics. The blood levels of disulfiram and its metabolites, carbon disulfide (CS2) and reduced disulfiram (diethyldithiocarbamate) were determined and the blood levels of patients with implants were compared with those of patients receiving disulfiram orally. The blood levels in the implanted patients were significantly lower than those of the group taking disulfiram orally. No metabolites were detectable after 3 months, despite the sensitive method employed. Nevertheless, 14 of the 21 chronic alcoholics remained abstinent for 6 months after implantation. This result is probably due in the main to psychotherapeutic guidance.
In a double-blind crossover study, 8 patients with classical migraine received disulfiram (400 mg/day) for 6 days, alternating with matched placebo tablets at 2 weekly intervals. Intravenous dopamine and tyramine pressor tests were performed on the 3rd and 6th days of each phase, respectively. 50-75% of patients experienced migraine attacks within 24 h of a test. There was no difference in the incidence of attacks between dopamine and tyramine injections. The number of migraine-free days was more during the placebo week than during disulfiram treatment (p less than 0.05). The post-tyramine migraine index correlated directly with the amount of tyramine administered during the dose-response test (r = 0.66), but no such relationship was found with dopamine. In a further study, post-tyramine migraine was observed in only 1 of 5 patients treated with propranolol (80 mg/day) for 4 weeks. Neither disulfiram nor propranolol influenced the tyramine pressor sensitivity. It is concluded that increased adrenergic activity is responsible for more frequent attacks during disulfiram medication. A similar mechanism probably is responsible for post-dopamine/tyramine migraine in susceptible subjects. It is unlikely that tyramine plays any specific role, except via its effect on the adrenergic system, in the pathogenesis of migraine attacks. However, the tyramine challenge test can be useful in the evaluation of a putative antimigranous activity of a new drug.
The literature search strategy included: electronic searches of Cochrane Library holdings, EMBASE, MEDLINE, PsycLIT, Biological Abstracts and LILACS; scans of reference lists of relevant articles, personal communications, conference abstracts, unpublished trials from the pharmaceutical industry and book chapters on the treatment of cocaine dependence. Randomized controlled trials (RCTs) focusing on the use of antidepressants (ADs), carbamazepine (CBZ), dopamine agonists (DAs) and other drugs used in the treatment of cocaine dependence were included. The reviewers extracted data independently, and relative risks (RR) with 95% confidence interval (CI) were estimated. Qualitative assessments were carried out using a Cochrane validated checklist. Where possible, analysis was carried out according to 'intention-to-treat' principles.
Pharmacological relapse prevention in alcoholism is a rather new clinical field with few drugs being available. Acamprosate, acting predominantly via glutamatergic pathways, and the opioid receptor antagonist naltrexone, were both shown to be efficient in improving rates for continuous abstinence, and not relapsing to heavy drinking in a number of clinical trials and meta-analyses. There are conflicting data on both drugs, especially for acamprosate, according to some recent US studies. However, overall, the evidence is good. Both drugs are approved in most European countries and the US. Efficacy data for disulfiram are mixed; it is a second-line medication compared with other drugs, and is probably most effective when used in a supervised setting. Recently, anticonvulsants including carbamazepine and topiramate have been discussed as possible anti-craving drugs, but there is still limited evidence for their efficacy. Although there is a significant comorbidity for alcoholism with affective disorder, anxiety and schizophrenia, relatively few controlled clinical trials have been performed in this area. Tricyclics have been found to be more effective than serotonin reuptake inhibitors in improving depressive symptoms in these patients.
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Compared with aminoglycosides, chloramphenicol, sulfonamides, tetracyclines, and even penicillins, the cephalosporins represent a remarkably safe class of antibiotics. Among the cephalosporins, the extended spectrum, third generation agents developed generally produce few side effects and appear to be less allergenic than the penicillins. Nephrotoxicity has not been a problem at recommended doses. Some third generation agents can cause hypoprothrombinemia if not administered with vitamin K, and disulfiram-like reactions occur with some agents because of the presence of a thiomethyl tetruzole moiety affixed to the cephem nucleus. There is a greater incidence of diarrhea associated with the agents excreted through a primarily biliary route, and this may contribute to the selection of drug resistant bacteria. Some agents are less active against staphylococci and their use may result in an increased incidence of superinfection or overgrowth of enterococci. If attention is given to the potential for adverse effects, many of these problems can be avoided and the third generation cephalosporins can be used safely in hospitals, nursing homes, and home care settings.
To compare efficacy of atrovent alone and in combination with erespal in patients with chronic bronchitis (CB) and chronic obstructive pulmonary disease (COPD).
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Adverse reactions to various antibacterial drugs were compared in a review of the following: multiple-dose studies of cefotaxime (n = 3,463), cefazolin (n = 554), the combination gentamicin-clindamycin (n = 163), and cefoxitin (n = 18); prophylactic studies of cefotaxime (n = 300) and cefazolin (n = 149); and single-dose studies of cefotaxime (n = 314) and penicillin G procaine (n - 265). The demographic and background characteristics of the groups were similar. Results of extensive pretreatment and posttreatment laboratory tests, measures of vital signs, and physical examinations revealed no clinically important intergroup differences. In the multiple-dose studies, side effects were reported in 9.8% of the cefotaxime, 3.8% of the cefazolin, 17.2% of the gentamicin-clindamycin, and 16.7% of the cefoxitin patients. The most frequent side effects were reactions at the injection site, of the skin and appendages, and of the digestive and urogenital systems, the only significant difference being fewer injection-site reactions in the cefazolin group than in the other three groups. In the prophylactic studies one cefotaxime patient reported rash and pruritus. In the single-dose studies, side effects were reported in 1.6% of the cefotaxime and 4.2% of the penicillin patients. Side effects sufficiently severe to warrant drug discontinuation were reported in 2.1% of the cefotaxime, 0.7% of the cefazolin, 1.8% of the gentamicin-clindamycin, and in none of the cefoxitin patients. Posttreatment prolongation of prothrombin time was found in one cefotaxime patient, whose pretreatment value was also abnormal, and in two gentamicin-clindamycin patients. No patient deaths were attributed to any of the drugs.
Randomised controlled trials (RCTs) on the efficacy of antipsychotics for the treatment of schizophrenic patients with comorbid SUD are reviewed and analysed on the basis of a systematic literature search (PubMed) ranging from 1985 to 2015. On the same basis, findings from RCTs on the efficacy of psychotropic and other medications used for primary SUD are summarised, and the main issues liable to influence treatment choice are discussed, including pharmacodynamic as well as pharmacokinetic interactions, adherence, medical comorbidity and the impact on brain structure.
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Proteinuria, hematuria and leukocyturia in chronic alcoholics were mostly pronounced in abstinence, particularly in those with a long-term alcoholism. In proportion to alcohol d s-intoxication treatment, their urinalyses normalized. Being hospitalized in a sober state the patients had insignificantly elevated or practically normal urinalyses. Disulfiramum tests performed both in abstinence or sobriety demonstrated pronounced abnormalities in urinalyses. In the course of disulfuramum treatment in the absence of alcohol tests urinalyses normalized completely. Urinalysis follow-up demonstrated the appearance of renal failure due to hemodynamic disorders that ran the pattern of renal sensitization due to the effect of acetaldehyde production in alcohol tests.
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Disulfiram administration markedly inhibited chlorzoxazone 6-hydroxylation by more than 95%, but did not affect metabolism of debrisoquine or mephenytoin. Caffeine N3-demethylation was decreased by 34% (P < 0.05). Monoacetyldapsone concentrations were markedly elevated by disulfiram administration resulting in a nearly 16-fold increase in the dapsone acetylation index, calculated as the plasma concentration ratio of monoacetyldapsone to dapsone. CYP-mediated dapsone N-hydroxylation was not significantly altered.