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At least 235 records · Page 13Linked to original sources
PubMed1999

The effect of hemodialysis on cycloserine, ethionamide, para-aminosalicylate, and clofazimine.

STUDY OBJECTIVES: Determine hemodialysis clearances of the second-line antitubercular drugs cycloserine (CS), ethionamide (ETA), para-aminosalicylate (PAS), and clofazimine (CFZ). DESIGN: Open-label, pharmacokinetic study SETTING: Outpatient long-term hemodialysis unit PARTICIPANTS: Eight long-term hemodialysis patients Interventions: Single oral doses of CS, 500 mg, ETA, 500 mg, PAS, 4,000 mg, and CFZ, 200 mg, were given 2 h (4 h for PAS) prior to hemodialysis (median blood flow rate, 400 mL/min; median dialysate flow rate, 600 mL/min; median hemodialysis time, 3.5 h). MEASUREMENTS AND RESULTS: Arterial and venous serum samples were collected at the beginning and end of hemodialysis, and hourly during hemodialysis. Dialysate fluid was collected for the duration of hemodialysis. All samples were assayed for drug concentrations using validated high-performance liquid chromatography (for ETA and PAS), capillary electrophoresis (for CS), and colorimetry (for CFZ). Dialysate samples were analyzed for acetyl-PAS. Median recoveries of drug in dialysate were 56% (CS), 2.1% (ETA), 6.3% (PAS parent compound), and 0% (CFZ) of the doses administered. Acetyl-PAS was dialyzed to a greater extent than its parent compound. Median hemodialysis clearances calculated by dividing the amount recovered in dialysate by the serum area under the curve during dialysis were 189 (CS), 58 (ETA), 206 (PAS), and 0 (CFZ) mL/min. CONCLUSIONS: ETA, CFZ, and PAS were not significantly dialyzed. CS is significantly removed by hemodialysis and should be dosed after hemodialysis.

Adolescent↗
PubMed1990

Enumeration and confirmation of Clostridium tyrobutyricum in silages using neutral red, D-cycloserine, and lactate dehydrogenase activity.

Spores of clostridia in big bale silages, manure, and dairy products were enumerated and distinguished from other spore formers by using Reinforced Clostridium Agar containing .005% neutral red. Spores of Clostridium tyrobutyricum predominated, but spores of Clostridium butyricum, Clostridium sporogenes, Clostridium bifermentans, Clostridium putrificum, and Clostridium sphenoides occurred to a lesser extent. In samples with high bacterial spore counts, growth of Bacillus spp., but not C. tyrobutyricum, was retarded by the addition of 200 ppm D-cycloserine. Clostridia isolated from silages and milk products were identified and tested on lactate dehydrogenase activity. Of 275 investigated strains, only strains identified as C. tyrobutyricum tested positively. Only 65% of the tested strains of C. tyrobutyricum grew in the confirmatory substrate containing minerals, lactic acid, and acetic acid. Tyrobutyricum Broth was not selective for C. tyrobutyricum, since C. butyricum and C. sporogenes also grew in this medium.

Animal Feed↗
PubMedDate not supplied

Cytotoxicity of L-cycloserine against human neuroblastoma and medulloblastoma cells is associated with the suppression of ganglioside expression.

BACKGROUND: Human neuroblastoma and medulloblastoma express abnormal ganglioside patterns especially GD2 and GM2 which are important for tumour growth. We tested the effects of L-cycloserine (L-CS), a potent inhibitor of synthesis of glycosphingolipids, on the growth, viability and expression of GD2 and GM2 in neuroblastoma and medulloblastoma cells. MATERIALS AND METHODS: The cytotoxic effects of L-CS were tested using the MTT dye reduction assay on four neuroblastoma (IMR-32, SK-N-SH, UKF-NB-2 and UKF-NB-3), two medulloblastoma (D283 and D341) and normal human fibroblasts and epithelial cell lines. In some experiments cytotoxicity of L-CS was tested in the presence of exogenous GD2 and GM2. The expression of GD2 and GM2 was analysed by flow cytometry. The antitumoral effects of L-CS in vivo were assessed on established xenografts of UKF-NB-3 or D283 cells in athymic (nude) mice using systemic administration of the drug (150 mg/kg intraperitoneally, once per day on 20 consecutive days). RESULTS: In vitro experiments revealed that L-CS was toxic for tumour cells at concentrations ranging from 0.5 to 20 micrograms/ml without any significant effects on normal fibroblasts and epithelial cells. L-CS treatment of UKF-NB-3 and D283 cells significantly inhibited expression of GD2 and GM2. The addition of exogenous GD2 and GM2 to culture medium partially prevented cytotoxic effects of L-CS on tumour cells. In vivo treatment resulted in complete tumour regression of UKF-NB-3 xenografts whereas growth of D283 xenografts was reduced by 60%. CONCLUSIONS: L-CS is a selective antitumoral agent for neuroblastoma and medulloblastoma cells with the ability to reduce expression of tumour associated gangliosides. In vivo experiments suggest that L-CS may be effective drug for treatment of neuroblastoma and medulloblastoma.

Animals↗
PubMed2002

Facilitation of conditioned fear extinction by systemic administration or intra-amygdala infusions of D-cycloserine as assessed with fear-potentiated startle in rats.

NMDA receptor antagonists block conditioned fear extinction when injected systemically and also when infused directly into the amygdala. Here we evaluate the ability of D-cycloserine (DCS), a partial agonist at the strychnine-insensitive glycine-recognition site on the NMDA receptor complex, to facilitate conditioned fear extinction after systemic administration or intra-amygdala infusions. Rats received 10 pairings of a 3.7 sec light and a 0.4 mA footshock (fear conditioning). Fear-potentiated startle (increased startle in the presence vs the absence of the light) was subsequently measured before and after 30, 60, or 90 presentations of the light without shock (extinction training). Thirty non-reinforced light presentations produced modest extinction, and 60 or 90 presentations produced nearly complete extinction (experiment 1). DCS injections (3.25, 15, or 30 mg/kg) before 30 non-reinforced light exposures dose-dependently enhanced extinction (experiment 2) but did not influence fear-potentiated startle in rats that did not receive extinction training (experiment 3). These effects were blocked by HA-966, an antagonist at the glycine-recognition site (experiment 4). Neither DCS nor HA-966 altered fear-potentiated startle when injected before testing (experiment 5). The effect of systemic administration was mimicked by intra-amygdala DCS (10 microg/side) infusions (experiment 6). These results indicate that treatments that promote NMDA receptor activity after either systemic or intra-amygdala administration promote the extinction of conditioned fear.

Acoustic Stimulation↗
PubMedDate not supplied

Rapid detection of Clostridium perfringens: comparison of lactose sulfite broth with tryptose-sulfite-cycloserine agar.

The lactose sulfite (LS) medium recommended for the detection and identification of Clostridium perfringens in foods was compared with a reference method using tryptose-sulfite-cycloserine (TSC) agar for the enumeration of this organism in a variety of foods and food ingredients. C. perfringens was detected and enumerated in 17 of the 54 samples examined with LS broth, but its presence could be confirmed in only 9 of the samples with TSC agar. In only 2 instances, C. perfringens was detected on TSC agar but not in LS broth. A positive response (FeS + and gas +) in LS broth incubated at 46 degrees C always corresponded to the presence of C. perfringens; whereas the black colonies formed on TSC agar incubated at 37 degrees C were frequently found to be Clostridium species other than C. perfringens. Thus, because of its highly selective nature, LS broth was superior to TSC agar for enumerating and confirming the small numbers of C. perfringens that were present in a majority of the samples. This was especially true when other clostridia were also present. Besides its greater selectivity and sensitivity, LS broth had the additional advantages of requiring less work and giving confirmed results within 24-48 h compared with 3 days for the TSC agar method.

Agar↗
PubMed1982

Enhancement of GABAergic inhibition: a mechanism of action of benzodiazepines, phenobarbital, valproate and L-cycloserine in the cat spinal cord.

Unanaesthetized spinal cats were used to assess the effects of several central depressant drugs on GABA-mediated presynaptic inhibition. Benzodiazepines enhance GABAergic inhibition by interaction with specific receptors in the spinal cord. Phenobarbital facilitates GABAergic inhibition by a mechanism unrelated to that of benzodiazepines, perhaps by an effect on the Cl- ionophore within the GABA-benzodiazepine-barbiturate receptor complex. A similar mechanism or the inhibition of GABA re-uptake might be responsible for the facilitating effect of valproate on GABA transmission. By selectively inhibiting GABA transaminase, L-cycloserine presumably increases the amount of GABA available for release.

Animals↗
PubMed1995

[Ofloxacin-cycloserine-protionamide-INH combination against treatment refractory lung tuberculosis].

Multiresistant tuberculoses are on the increase. The conversion rates in "additional" therapy are only modest. 17 multiresistant patients and 6 treatment-refractory tuberculoses were treated by us with ofloxacin-cycloserin-protionamide-INH. 16 of these patients were HIV positive. 21 patients converted after 3 months of treatment by the latest. 3 patients died of HIV syndrome. There was otherwise no difference between HIV positive and HIV negative patients. As a rule, the combination was well tolerated. In multiresistant tuberculosis, it is mandatory to administer at least 3 drugs to which there is no resistance.

AIDS-Related Opportunistic Infections↗
PubMed1997

D-cycloserine blocks the effects of ethanol and HA-966 in rats tested in the elevated plus-maze.

Previous studies from our laboratory have shown gender-related behavior in rats tested in the elevated plus-maze under the influence of ethanol and other drugs. The present study investigated the effects of pretreatment with the NMDA-receptor partial agonist at the glycine site D-cycloserine (DCS; doses 3 to 9 mg/kg for females; 3 to 12 mg/kg for males, intraperitoneally) on the effects of ethanol (1.2 g/kg, i.p.; 14% w/v) and (+/-)-3-amino-1-hydroxy-2-pyrrolidone (HA-966; 2 or 4 mg/kg, i.p.), an antagonist at the glycine site of the NMDA receptor complex in rats submitted to the elevated plus-maze test. The results showed that DCS, at doses that did not affect the behavior of control animals, significantly (p < 0.05) prevented the increase in the percentage of open-arm entries and the time spent in the open arms of elevated plus-maze test induced by ethanol, exhibiting a U-shaped dose-response curve. Similarly, DCS blocked the anxiolytic effects of HA-966 in animals of both gender. Data confirm our previous results, suggesting that the NMDA-receptor system contributes significantly to the anxiolytic effect of ethanol. Furthermore, the similarity between the blockade by DCS of anxiolysis induced either by ethanol or by HA-966 strengthens the suggestion that ethanol acts on the glycine site of the NMDA receptor complex.

Animals↗
PubMed1998

[D-cycloserine is active in the adult mouse and inactive in the aged mouse, in the forced swim test].

The glycinergic site agonist of the NMDA receptors, D-cycloserine (DCS), exhibit an anti-immobility effect in the forced swim (FS) test, on adult mice. This effect, predicting antidepressive properties, is of the same order as those of imipramine (IMI). In constrast, DCS and IMI did not exhibited any significant anti-immobility effect on aged mice (12 months). IMI being active, in the depression of aged persons, it seems that the FS test has not any predictive value concerning the action of antidepressant drugs on aged persons. On the other hand Gabalid, a mixed (A, B) GABAergic agonist, AE37, a partial muscarinic agonist and N-linoleyl glycine, a mixed (A, B) glycinergic agonists, are active, in the FS test, on adult as well on aged mice. Mixed (A, B) glycinergic agonist, Gabalid or AE37 and, generally, partial muscarinic agonists, are active on the passive avoidance test (step-down) on mice, which predict nootropic effects. These results, considered in relation with recent data on the impact of FS or functional inhibition (GABAergic, glycinergic A, antimuscarinic) of glutamatergic neurons on the glycinergic modulation of the NMDA receptors, could suggest that the FS test on aged mice could possess a predictive value for nootropic rather than for antidepressant drugs.

Aging↗
PubMed1998

Double-blind, placebo-controlled, crossover trial of D-cycloserine adjuvant therapy for treatment-resistant schizophrenia.

Dysfunction of N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission may be relevant to the pathogenesis of negative symptoms in schizophrenia. The tuberculostatic compound D-cycloserine (DCS) acts as a partial agonist at the strychnine-insensitive glycine regulatory site on the NMDA receptor complex. Dose-finding trials suggest that DCS doses of 50-100 mg/d may be beneficial in the treatment of negative symptoms in schizophrenia. Nine treatment-resistant chronic schizophrenic patients participated in a double-blind, placebo-controlled, adjuvant treatment trial with 50 mg/d DCS. Between treatment-groups differences in symptom changes were not significant. However, a significant (p<0.05) reduction in negative symptoms was registered during treatment with DCS but not placebo. Greater reductions were registered in patients with lower baseline serum glycine levels (p<0.008). No side effects were registered. These preliminary findings indicate a potential role of DCS in the treatment of negative symptoms in schizophrenia. However, the degree of symptom reduction may be modest, at least among treatment-resistant inpatients.

Journal Article↗
PubMed1970

Inhibition of the Synthesis of Wax D Peptidoglycolipid of Mycobacterium tuberculosis by d-Cycloserine.

The antibiotic d-cycloserine inhibits the synthesis of the wax D peptidoglycolipid in cells of the H37Ra strain of Mycobacterium tuberculosis. This inhibition occurs at a lower concentration of the drug than that required for the inhibition of growth. The inhibition is completely reversed by d-alanine. An arabino-galactan-galactosamine-(diaminopimelic acid)-mycolate accumulates in H37Ra cells exposed to the antibiotic. The chemical and functional group analyses of this lipid suggests it to be a possible precursor to the synthesis of wax D.

Journal Article↗
PubMed1962

REVERSAL OF d-CYCLOSERINE INHIBITION OF BACTERIAL GROWTH BY ALANINE.

Zygmunt, Walter A. (Mead Johnson & Co., Evansville, Ind.). Reversal of d-cycloserine inhibition of bacterial growth by alanine. J. Bacteriol. 84:154-156. 1962.-Reversal of the antibacterial activity of d-4-amino-3-isoxazolidone by alanine in bacterial cultures actively growing on chemically defined media was compared in cultures requiring exogenous alanine and those capable of its synthesis. dl-Alanine was the most effective reversal agent in Pediococcus cerevisiae, an alanine-requiring organism, and d-alanine was effective in Escherichia coli and Staphylococcus aureus, organisms synthesizing alanine. With all three cultures, l-alanine was the least effective reversal agent.

Journal Article↗