Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
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Query: CAS:80-08-0 (
DSS
)
2,544
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
A group of South Indian subjects was studied for their capacities to acetylate sulfamethazine (SMZ) and dapsone (
DDS
) and to clear
DDS
from the circulation. An apparent trimodal distribution of acetylator phenotypes was found in 49 subjects (51% slow, 12% intermediate, and 37% rapid acetylators) from measurements of the percentage acetylation of SMZ in 6-hour plasma samples after administration of 10 mg SMZ/kg. The intermediate phenotype was not discernible from either the percentage acetylation of SMZ in urine (collected concurrently with the plasma after SMZ) or that of
DDS
in plasma after the ingestion of 50 mg
DDS
by the same subjects. The latter two measurements yielded a bimodal distribution of 59% slow and 41% rapid acetylators, nearly identical to earlier reported distributions of isoniazid inactivator phenotypes in larger numbers of South Indian tuberculosis patients. In the current group, acetylation of
DDS
and SMZ was positively correlated. The half-time of disappearance (T 1/2) of
DDS
, an expression of the rate of clearance from the plasma, ranged from 13 to 40 hours. No correlation was found between the subject's capacity to acetylate
DDS
and the T 1/2 value for
DDS
. These results were generally consistent with earlier observations made during similar studies of American and Filipino subjects.
...
PMID:Polymorphic acetylation of the antibacterials, sulfamethazine and dapsone, in South Indian subjects. 115 99
Dapsone
(4,4'-diaminodiphenylsulfone [
DDS
]) was administered intravenously to anesthetized dogs; urine was collected, heparinized venous blood was obtained, and bile was collected from some of the dogs. A constant infusion of inulin was maintained, and isosmotic or hypoosmotic fluids were administered. Dogs were studied under conditions of standardized, increased or decreased urine flow, and before and after plasmapheresis. Plasma, urine, and bile samples were analyzed for
DDS
and
DDS
conjugates; the degree of binding of
DDS
by plasma proteins was also determined. The renal clearances of inulin and
DDS
were calculated. No monoacetyldapsone (MADDS) was detected in the plasma, and only negligible quantities were found in the urine. Small quantities of
DDS
and
DDS
conjugates were detected in the bile in 4 h following the dose. Between 10 and 30% of the administered drug could be identified as
DDS
plus
DDS
conjugates in the urine in 8 h after the dose. Renal clearance of unbound
DDS
was proportional to the urine flow rate, and the clearance ratio of
DDS
to inulin approached the same maximal value as that for urea. Although the rate of urinary excretion of
DDS
conjugates was the same in the dog as in man, the rates of excretion of
DDS
and of
DDS
plus
DDS
conjugates were greater in the dog than in man, suggesting that the acetylation of
DDS
to MADDS by man but not by the dog and the greater degree of plasma protein binding of
DDS
and MADDS by man account for the longer half-time of disappearance of
DDS
in man compared to that in the dog.
...
PMID:Renal and biliary disposition of dapsone in the dog. 115 23
The proportion of accumulated metaphases, as well as the frequency of aneuploidies and structural chromosome aberrations were investigated in
DDS
-treated and untreated (controls) leukocyte cultures from two samples of healthy adult Caucasoid individuals. In one sample, the sulfone-treated cultures differed from the controls in that they contained 0.4 mug of
DDS
per ml of tissue culture medium plus phytohemagglutinin. In the other sample, these cultures differed from the controls in that they contained a tenfold higher concentration of
DDS
. The two concentrations of
DDS
used have not significantly affected the rate of metaphases, while 0.4 mug/ml
DDS
did not increase the frequency of chromosome aberrations. The same was not true for the cultures treated with 4 mug/ml
DDS
in which the proportion of aneuploides and achromatic gaps increased significantly.
...
PMID:In vitro effect of dapsone on human chromosomes. 117 30
Female Buffalo and Lewis rats receiving 1.0 mg
DDS
/kg ip exhibited higher plasma levels of
DDS
and its monoacetylated metabolite, MADDS, than did male rats of each strain receiving the same dose. The fraction of the total measured drug in plasma as MADDS at 8 hr in female rats of both strains ranged from 43 to 62% compared with a range of 28-31% in male rats. Plasma half times of disappearance (T1/2) of
DDS
ranged from 5.0 to 6.8 hr and were not different among sexes and strains. Deacetylation of MADDS to
DDS
occurred when equimolar doses of MADDS were administered. An approach to a steady state of acetylation-deacetylation was indicated by comparing the percentage MADDS of the total drug in plasma in the respective sexes and strains receiving both drugs. T1/2 values of MADDS were significantly lower than values for
DDS
in Lewis rats. They were not different in Buffalo rats. Protein binding studies in plasma from rats receiving 5.0 mg
DDS
or 5.8 mg MADDS/kg showed 67-72% binding of
DDS
and 91% binding of MADDS. These in vivo observations were confirmed by in vitro binding studies. Comparison of these results with those of earlier studies in mice and man indicates that the rat is a better model of man than is the mouse for studies on the disposition of
DDS
.
...
PMID:Disposition of dapsone and monoacetyldapsone in rats. 120 66
In vitro anti-leprosy activities of various antimicrobials were measured by using the BACTEC 460 TB System. The Growth Index reducing activities of test drugs were strong in clofazimine, KRM-1648, rifabutin, clarithromycin and rifampicin; intermediate in sparfloxacin, minocycline and ofloxacin; and weak in ciprofloxacin, fleroxacin and
DDS
. Amikacin, pipemidic acid, enoxacin and norfloxacin had no such in vitro activities. There is a close correlation between in vitro and in vivo anti-M. leprae activities of a given agent, therefore indicating usefulness of the BACTEC 460 TB System in evaluation of in vitro anti-M. leprae activity of a given agent.
...
PMID:Evaluation of BACTEC 460 TB system for measurement of in vitro anti-Mycobacterium leprae activity of various antimicrobials. 130 82
We developed a porous hydroxyapatite ceramic (HAP) incorporating adriamycin (ADM), that is, ADM-HAP as a new delivery system (
DDS
) to release ADM gradually. We also researched the possibility of hyperthermic chemotherapy using ADM-HAP by in vitro and in vivo experiments. As for in vitro experiments, we implanted HAPs into uniform Agar-Phantom, and observed thermal distribution generated by Thermotron-RF 8 using thermography. Then we found the hot spot that the edge temperature of HAPs always at the range of 0.5-0.7 degrees C than in the other regions. On the other hand, slow constant release (1%) of ADM from ADM-HAP in PBS was recognized for 24 hrs up to 30 days. When the incubating temperature was shifted up to 42.5 degrees C or 44 degrees C from 37 degrees C, the quantity released over 24 hrs increased about 1.1-fold or 1.3-1.4-fold of the cases at 37 degrees C, respectively. In the in vivo experiment, we inoculated Sarcoma 180 cells in the leg of ddY-mice, and measured the tumor growing times by the treatment of hyperthermia+ADM (whole body), hyperthermia+ADM (tumor region) or hyperthermia+ADM-HAP (tumor region). Then we found that the effect of hyperthermia with ADM-HAP inhibited synergistically the tumor growth as compared with hyperthermia with ADM. Consequently, we succeeded in tumor growth inhibition by increasing the temperature and by limiting ADM release to only a target region using hyperthermia with ADM-HAP.
...
PMID:[Fundamental study on hyperthermic chemotherapy using adriamycin-loaded hydroxyapatite]. 132 24
This paper describes the leprosy control programme in 7 districts of the South Sulawesi Province in Indonesia. This province is reported to have the highest prevalence of leprosy in the country. The programme started in 1986 with re-registration of all patients on the cumulative registers. Strict criteria for admission of patients to MDT were initially applied. In 1990 it appeared that these criteria had been too strict, thus necessitating a second re-registration of patients still on
DDS
monotherapy. More flexible criteria for admission to MDT led to an increase in MDT coverage from 45% to 78% within 6 months. By April 1991, 5 years after the start of the programme, the registered prevalence had decreased from 4.4 per 1000 in 1986 to 1.6 per 1000; the coverage with MDT had increased from 6% in 1986 to 78%, and the case detection rate remained stable around 4 per 10,000 after an initial increase at the start of the programme.
...
PMID:Leprosy control in 7 districts of south Sulawesi, Indonesia, 1986-91. 140 19
To understand how albumin on the surface inhibits surface-induced platelet activation, we adsorbed albumin on dimethyldichlorosilane-coated glass (DDS-glass) and modified the adsorbed albumin by three different methods. The adsorbed albumin was crosslinked with glutaraldehyde, dried and rehydrated, or digested with trypsin. Surface albumin concentration did not change by crosslinking; however, it decreased by about 15% by a simple dry-and-rehydration process. Trypsin digestion reduced the surface albumin concentration by 50%. Platelets were found to adhere and activate on albumin coated
DDS
-glass, if the adsorbed albumin was modified. The extent of platelet activation was quantified with two numeric parameters, the spread area and circularity. Fibrinogen adsorption to the dried or digested albumin layer resulted in enhancement of platelet activation, while adsorption of more albumin inhibited platelet activation. The results suggest that albumin can inhibit platelet activation as long as it covers the surface completely and remains flexible on the surface. This study indicates that steric repulsion is one of the mechanisms of surface passivation by albumin.
...
PMID:Study on the prevention of surface-induced platelet activation by albumin coating. 141 69
Ninety paucibacillary leprosy patients having indeterminate (I), tuberculoid (TT) and borderline tuberculoid (BT) type of leprosy with bacterial index (BI) of less than two on the Ridley scale were treated with rifampicin (RFM) 600 mg once a month, dapsone (
DDS
) 100 mg daily and prothionamide (PTH) 250 mg daily. Treatment was stopped at the end of six months. The patients tolerated the drugs fairly well and in only two patients the drugs had to be stopped (in one due to jaundice and in the other due to gastric intolerance). About 6% of patients had early reactions which subsided with additional steroid therapy. The inactivity rate was 60% at six months and this improved to 96% at 12 months. No cases of late reactions and relapses were encountered in the limited follow-up period of six months; and a longer follow-up is necessary for ascertaining the relapse rates. The preliminary results however suggest that the addition of prothionamide to the standard WHO paucibacillary regimen is well-tolerated with increased inactivity rate and fewer instances of late reactions.
...
PMID:Treatment of paucibacillary leprosy with a regimen containing rifampicin, dapsone and prothionamide. 143 19
Simple methods of determining the water-soluble vitamins B1, B2, B6 and B12 in milk by HPLC are described. Compared to existing procedures, the following improvements can be realized. The oxidation of vitamin B1 to thiochrome is stopped by the addition of sodium sulphite. This step significantly increases repeatability. Thiochrome is then extracted with butan-1-ol, which results in fewer co-extracts and greater selectivity. After the hydrolysis of the 5-phosphates of the vitamin B6 (pyridoxine, pyridoxal and pyridoxamine), these three vitamers are determined by isocratic HPLC as
DDS
-ion-pairs and with fluorimetric detection. As only microbiological methods have so far been used for the determination of minute quantities of vitamin B12 in milk, a new HPLC procedure is proposed with a detection limit of 0.2 micrograms vitamin B12/L milk.
...
PMID:[Determination of water-soluble vitamins B1, B2, B6 and B12 in milk using HPLC]. 144 59
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