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1.
Akathisia usually consists of two components, subjective restlessness and typical movements such as shuffling of the legs, pacing, shifting weight from one leg to the other, and rocking movements of the trunk. The ability to measure akathisia reliably is essential for the assessment of treatments for akathisia and for the evaluation of drug-induced side effects in general. To date, investigators have generally used self-constructed assessment scales without reporting data about reliability or validity. The Hillside Akathisia Scale (HAS) has two subjective and three objective items for which anchored rating points are provided. Reliability was 0.89 for the HAS total score. Reliability for rating subjective symptoms ranged from 0.86 to 0.92, and the objective scores ranged from 0.51 to 0.89. The correlation between HAS and a global assessment of akathisia (modified CGI) was 0.87. These values compare favorably with the original report on the scale indicating that the Hillside Akathisia Scale can validly quantify akathisia with a satisfactory degree of interrater reliability.  相似文献   

2.
BackgroundThis study aimed to develop and validate a shortened version of the Drinking Refusal Self-Efficacy Questionnaire-Revised Adolescent version (DRSEQ-RA) using a large sample of adolescents.MethodsSecondary school students (N = 2609, M = 14.52 years, SD = 0.94) completed the DRSEQ-RA (consisting of subscales: Social Pressure; Opportunistic; Emotional Relief) and the Alcohol Use Disorders Identification Test (AUDIT). These data were analysed using non-parametric item response theory (NIRT) including Mokken scalability coefficients, and confirmatory factor analysis.ResultsSocial Pressure subscale items were better able to distinguish between adolescents with lower or higher levels of drinking refusal self-efficacy, while the Opportunistic and Emotional Relief subscale items were able to distinguish adolescents with low drinking-refusal self-efficacy. The DRSEQ-RA was reduced from 19-items to a 9-item scale and retained the original three-factor structure. The reduced scale was named the Drinking Refusal Self-Efficacy Questionnaire-Shortened Revised Adolescent version (DRSEQ-SRA). The DRSEQ-RA and the DRSEQ-SRA have almost identical psychometric properties. They both demonstrated good fit to the data, each explained 18% of the variance in alcohol consumption, Adj. R2 = 0.18, p < .001 respectively. The DRSEQ-RA and the DRSEQ-SRA also have excellent scale and subscale internal reliability (αs = 0.92–0.99).ConclusionsThe DRSEQ-SRA is a short, 9-item, measure of adolescent drinking-refusal self-efficacy which demonstrates both reliability and validity. A significant advantage is brevity. The DRSEQ-SRA may be a valuable tool for identifying risk of adolescent drinking and prevention/treatment planning in settings where survey administration time is critical.  相似文献   

3.
There is a growing body of evidence that the renin-angiotensin system (RAS) plays a pivotal role in the pathogenesis of cardiovascular diseases. Indeed, large clinical trials have demonstrated a substantial benefit of the blockade of this system for cardiovascular-organ protection. Although several types of angiotensin II type 1 (AT1) receptor blockers (ARBs) are commercially available for the treatment of patients with hypertension, comparisons of the binding affinity to AT1 receptor among them remain to be elucidated. In this study, we examined the dissociation rate of several ARBs from AT1 receptor in vitro. Angiotensin II time-dependently dissociated telmisartan, olmesartan, candesartan, valsartan, losartan and an active metabolite of losartan, EXP3174, from membrane components containing human AT1 receptor The dissociation rate constant of each ARB was 0.003248, 0.004171, 0.005203, 0.009946, 0.01027 and 0.008561 min(-1), with corresponding half-lives of 213, 166, 133, 70, 67 and 81 min, respectively. These results demonstrate that telmisartan has the strongest binding affinity to AT1 receptor among various ARBs examined herein. The rank order of affinity was telmisartan > olmesartan > candesartan > EXP3174 > or = valsartan > or = losartan. The present findings suggest that telmisartan (Micardis) may have long-lasting blood pressure-lowering effects and superior cardioprotective properties in patients with hypertension due to its strongest AT1 receptor antagonistic ability.  相似文献   

4.
We measured cortical dopamine transporter (DAT) in Cloninger type 1 and 2 alcoholics by using [125I]PE2I as a radioligand in human postmortem whole hemispheric autoradiography, and evaluated the putative correlations of DAT between cortical areas and nucleus accumbens. There was a low, but distinct cortical binding in the cryosections. The mean binding was generally higher in both groups of alcoholics compared to controls, and the results reached statistical significance with a large effect size (1.25) in the temporal cortex of type 2 alcoholics. This is surprising, because several studies have reported lower DAT densities in the striatum among alcoholics compared to controls. Moreover, the density of DAT had a statistically significant positive correlation between temporal cortex and nucleus accumbens in controls, whereas among type 2 alcoholics the correlation was statistically significantly negative, which may suggest some pathology relating to the antisocial behaviour of these alcoholics.  相似文献   

5.
吕邵华 《河北医药》2007,29(1):40-42
目的 研究高血压、2型糖尿病对以血清可溶性E-选择素为标志的内皮激活的影响,并探寻高血压合并糖尿病是否会对其产生额外的效应.方法 通过酶联免疫吸附法测定41例单纯高血压、42例单纯糖尿病、37例高血压合并糖尿病患者以及45例健康个体的血清可溶性E-选择素水平.结果 与健康对照组[(28.32±5.46)ng/ml]相比,单纯高血压、单纯糖尿病、高血压合并糖尿病组的血清可溶性E-选择素水平[分别为:(67.34±9.49)ng/ml,P<0.05;(76.36±11.44)ng/ml,P<0.01;(75.09±10.05)ng/ml,P<0.01)显著增高.3组之间血清可溶性E-选择素水平差异并无显著性(P>0.05).非糖尿病个体其血清可溶性E-选择素与收缩压(r=0.418,P=0.015)独立相关.糖尿病患者血清可溶性E-选择素与糖化血红蛋白(HbA1C)(r=0.459,P=0.020)及体重指数(r=0.21,P=0.028)呈正相关.结论 高血压和2型糖尿病均可诱导内皮激活,但二者合并并未对其产生叠加作用.  相似文献   

6.
BACKGROUND: Immunization against poliomyelitis is recommended for international travelers to developing countries. However, the level of antibodies varies even in previously unvaccinated persons, due to wild-type or vaccine-type infections in the eldest travelers. METHODS: In 1999, we conducted a seroprevalence study in the Lombardy region (northern Italy), using sera collected in 1994 from a population aged 50 to 59 years. The study subjects were consecutive, randomly selected travelers enrolled in an anti-hepatitis A virus antibody study. Neutralizing antibodies were titrated on Vero cells in microtiter plates. Each serum dilution (1:8 to 1:256) was challenged against 100 tissue culture infective doses of the three Sabin strains. Titers> 1:8 were considered to be protective. RESULTS: We studied 98 travelers, 59 male and 39 female, of mean age 54 years. Seventy-three (74.4%) reported previous travel abroad, but none had been vaccinated against polio. Dietary habits included consumption of seafood in 74.4% and raw vegetables from their own garden in 52.1%. The seroprevalences for neutralizing antibodies against poliovirus type 1, type 2 and type 3 were 86.7%, 89.9%, and 86.7%, respectively. All travelers presented protective antibody titers against at least one of the three viral types. Protective antibody titers were unrelated to travel history or dietary habit. CONCLUSIONS: A high proportion of the previously unvaccinated adults in our sample presented protective immunity to polioviruses. This observation may have implications for cost-effectiveness analysis of generalized polio vaccination in adult Italian travelers.  相似文献   

7.
Derosa G 《Drugs》2010,70(15):1945-1961
Diabetes mellitus is a debilitating disease that is estimated to affect 366 million people by the year 2030. Type 2 diabetes mellitus (T2DM) is characterized by a progressive decline in pancreatic β-cell function and increased insulin resistance, and accounts for approximately 90% of people with diabetes. Oral antihyperglycaemic agents are extensively used in the treatment of T2DM. Thiazolidinediones are insulin sensitizers developed specifically for T2DM, which act via activation of peroxisome proliferator-activated receptors (PPARs). Pioglitazone is a thiazolidinedione that displays high affinity for PPARγ(1) and PPARγ(2), which are predominately expressed in adipose tissue. This review examines the published literature comparing the efficacy and tolerability of pioglitazone with other oral antihyperglycaemic agents in the treatment of patients with T2DM. Glycosylated haemoglobin, fasting glucose, insulin parameters and β-cell function are all improved with pioglitazone treatment, with efficacy similar to third-generation sulfonylureas, metformin and dipeptidyl peptidase-4 inhibitors. Pioglitazone reduces vascular risk and inflammatory markers, and improves carotid intima media thickness independent of its glycaemic effect. When compared with rosiglitazone, pioglitazone is associated with a reduction in the risk of hospitalization for acute myocardial infarction. Blood pressure is reduced and lipid profiles are favourably improved with pioglitazone; however, an increased risk for the development/exacerbation of heart failure, which is related to the increased incidence of oedema due to fluid retention, and fractures remain a concern. A low incidence of hypoglycaemia is observed with pioglitazone, especially compared with sulfonylureas. In conclusion, pioglitazone is an effective oral antihyperglycaemic agent with additional cardiovascular and lipid benefits that allows for the successful management of patients with T2DM.  相似文献   

8.
PurposeThe study aimed to translate and validate the Arabic version of General Medication Adherence Scale (GMAS) in Saudi patients with chronic diseases.MethodsA multi-center cross sectional study was conducted for a month in out-patient wards of hospitals in Khobar, Dammam, Makkah, and Madinah, Saudi Arabia. Patients were randomly selected from a registered patient pools at hospitals and the item-subject ratio was kept at 1:20. The tool was assessed for factorial, construct, convergent, known group and predictive validities as well as, reliability and internal consistency of scale were also evaluated. Sensitivity, specificity, and accuracy were also evaluated. Data were analyzed using SPSS v24 and MedCalc v19.2. The study was approved by concerned ethics committees (IRB-129-25/6/1439) and (IRB-2019-05-002).ResultsA total of 282 responses were received. The values for normed fit index (NFI), comparative fit index (CFI), Tucker Lewis index (TLI) and incremental fit index (IFI) were 0.960, 0.979, 0.954 and 0.980. All values were >0.95. The value for root mean square error of approximation (RMSEA) was 0.059, i.e., <0.06. Hence, factorial validity was established. The average factor loading of the scale was 0.725, i.e., >0.7, that established convergent validity. Known group validity was established by obtaining significant p-value <0.05, for the associations based on hypotheses. Cronbach’s α was 0.865, i.e., >0.7. Predictive validity was established by evaluating odds ratios (OR) of demographic factors with adherence score using logistic regression. Sensitivity was 78.16%, specificity was 76.85% and, accuracy of the tool was 77.66%, i.e., >70%.ConclusionThe Arabic version of GMAS achieved all required statistical parameters and was validated in Saudi patients with chronic diseases.  相似文献   

9.
目的研究转录因子7类似物2(TCF7L,2)基因多态性与2型糖尿病患者口服瑞格列奈及罗格列酮疗效之间的相关性。方法选取新诊断的2型糖尿病患者209例,随机分为2组,分别接受瑞格列奈(104例)或罗格列酮(105例)单药治疗48 wk。检测治疗前后人体基本参数及糖、脂代谢相关指标,以及TCF7L2基因rs7903146变异。并分析不同基因型患者这2种药物的疗效有无差异。结果 209例患者中完成48 wk随访168例,已知基因型189例,其中CC、CT、TT基因型频率分别为92.6%(175例),6.9%(13例),0.5%(1例)。治疗48 wk后,瑞格列奈组CT+TT基因型患者糖化血红蛋白改善程度优于CC型患者(P<0.05)。罗格列酮组CC基因型患者的空腹胰岛素水平和胰岛素抵抗指数高于CT+TT基因型患者,差异有显著意义(P<0.05),其余指标各基因型间均无显著差异(P>0.05)。结论 TCF7L2基因rs7903146变异与瑞格列奈治疗2型糖尿病的疗效相关,T等位基因型携带者对瑞格列奈的反应优于CC基因型携带者。未发现这一位点变异与罗格列酮的疗效相关。  相似文献   

10.
The experimental drugs butanserin (R 53393), ritanserin (R 55667), R 56413, flufylline (Sgd 195/78) and fluprofylline (Sgd 144/80) were evaluated with respect to their antagonism at postjunctional alpha 1- and alpha 2-adrenoceptors and 5-HT2-receptors in pithed rats. Moreover, affinity for [3H]mianserin, [3H]prazosin and [3H]yohimbine binding sites was assessed using rat brain preparations. In all experiments ketanserin was taken as a reference compound. It is concluded that of the compounds investigated butanserin is the most potent and selective alpha 1-adrenoceptor antagonist, whereas ritanserin was found to be a potent and selective 5-HT2-antagonist. Of the other compounds, fluprofylline was a very selective though not very potent alpha 1-adrenoceptor antagonist. The other compounds were less active and less selective in this respect.  相似文献   

11.
The efficiency of (E)-5-(2-bromovinyl)- and 5-vinyl-1-beta-D-arabinofuranosyluracil (BrVaraU, VaraU) as inhibitors of three herpes simplex virus type 1 (HSV-1) strains was assessed in comparison to (E)-5-(2-bromovinyl)-2'-deoxyuridine (BrVUdR), 9-(2-hydroxyethoxymethyl)guanine (ACV), and trisodium phosphonoformate (Na3PFA) using a plaque assay in human embryonic lung fibroblast (HELF) cell cultures. The following order of decreasing activity was found: BrVaraU greater than VaraU greater than BrVU-dR greater than ACV much greater than Na3PFA. In HELF cell cultures, the selectivity indexes of VaraU and BrVaraU were 10 times higher than those of BrVUdR and ACV. Protection of mice from encephalitis and death due to intracerebral (i.c.) infection with a clinical HSV-1 isolate was nearly complete if mice were treated intraperitoneally (i.p.) with two daily doses of VaraU and BrVaraU (100 or 200 mg/kg per day) over a period of 5 or 10 days. The efficacy was similar to ACV, but, using a treatment schedule of three daily i.p. doses over 10 days, with equimolar amounts of the nucleoside analogs, VaraU and BrVaraU (140 and 180 mg/kg per day) were superior to ACV (130 mg/kg per day) (P less than 0.05).  相似文献   

12.
13.
[1-14C]-Naphthol and [8-14C]2-naphthol (25 mg/kg) injected into cats were excreted in the urine almost entirely as sulphate conjugates. Only about 1–2% of the dose appeared as naphthylglucuronides. 1-Naphthol gave entirely 1-naphthylsulphate whereas 2-naphthol gave 2-naphthylsulphate and an unidentified hydroxynaphthylsulphate in the ratio of 4 : 1.

When [8-14C]2-naphthol was injected into pigs (dose 25 mg/kg) it was excreted mainly as 2-naphthylglucuronide with a small amount of 2-naphthyl sulphate (ratio about 15 : 1), but when [1-14C]1-naphthol was injected, 1-naphthylglucuronide and 1-naphthylsulphate were excreted in the ratio of 2 : 1. The pig, therefore, formed substantial amounts of 1-naphthylsulphate but not of 2-naphthylsulphate.

The cat excreted injected [14C]morphine mainly as morphine 3-sulphate and [14C]phenacetin as 4-acetamidophenylsulphate, but injected [3H]phenolphthalein was excreted as the glucuronide and sulphate in the ratio of 3 : 2. The cat, therefore, formed substantial amounts of phenolphthalein glucuronide, but not of morphine 3-glucuronide or 4-acetamidophenylglucuronide.

The pig excreted [14C]phenacetin mainly as 4-acetamidophenylglucuronide, with small amounts of the corresponding sulphate. About half of injected 4-hydroxy[14C]amphetamine was excreted unchanged by the pig, the rest being conjugated mainly with glucuronic acid.

The cat tends to excrete phenols mainly as sulphates and the pig mainly as glucuronides, but certain phenols, such as phenolphthalein, form substantial amounts of glucuronides in cats and certain others, such as 1-naphthol, form substantial amounts of sulphates in pigs.  相似文献   

14.

Rationale

Acute exposure to (±) 3, 4-methylenedioxymethamphetamine (MDMA) produces hyperlocomotion that is preferentially expressed in the periphery of closed chambers. Following repeated administration, however, a sensitized hyperlocomotor response is preferentially expressed in the center of an activity box, so that the response resembles the more generalized activity that is produced by d-amphetamine (AMPH).

Objectives

The present study was designed to determine whether common neuroadaptations underlie the acute and sensitized responses to MDMA and AMPH.

Methods

Rats were pretreated with five daily injections of MDMA (10.0?mg/kg), AMPH (2.0?mg/kg), or saline. Following a 2-day drug-free period, dose–response curves for hyperactivity produced by MDMA (2.5–10.0?mg/kg), AMPH (0.5–2.0?mg/kg), SKF-81297 (1.0–2.0?mg/kg), or quinpirole (0.25–1.0?mg/kg) were obtained.

Results

Effects of MDMA and AMPH were increased by pretreatment with both drugs. The sensitized response following MDMA exposure was preferentially expressed in the center compartment, but, following AMPH pretreatment, the sensitized response was observed in both compartments. Cross-sensitization was unidirectional; AMPH pretreatment failed to sensitize to the effects of MDMA, but MDMA pretreatment sensitized to the effects of AMPH. MDMA and AMPH pretreatment produced marginal increases in the effects of SKF-81297. The response to quinpirole was, however, greater following MDMA, but not AMPH, pretreatment.

Conclusions

These data suggest that repeated MDMA exposure produces sensitization via a unique neurochemical effect.  相似文献   

15.
Introduction: Canagliflozin, a sodium-glucose co-transporter-2 (SGLT2) inhibitor, improves various cardiometabolic parameters. Although canagliflozin was originally discovered in Japan, no comprehensive summary of its effects in Japanese patients has been reported. As differences exist in the pathologic features of diabetes between Japanese and non-Japanese populations, it is important to consolidate Japanese data for canagliflozin.

Areas covered: The authors summarize Japanese clinical trial and post-marketing surveillance data for canagliflozin, and make comparisons with non-Japanese data. They also consider the therapeutic potential of canagliflozin in Japanese patients by presenting results from the CANagliflozin cardioVascular Assessment Study (CANVAS) Program.

Expert opinion: In Japanese patients, canagliflozin 100 mg, administered as monotherapy or combination therapy, improved blood glucose, body weight, and blood pressure, and was well tolerated; the efficacy and safety profiles were comparable to previous clinical studies in other countries. In the CANVAS Program, canagliflozin reduced major cardiovascular events, and although Japan was not included in this program, canagliflozin may have cardiovascular benefits in Japanese patients, in whom control of multiple risk factors is important for preventing diabetic complications. Patients with high cardiovascular risk often have multiple comorbidities, so it is important to consider the risk–benefit balance of using SGLT2 inhibitors in individual patients.  相似文献   


16.
The 5-substituted 1-beta-D-arabinofuranosyl (araU) analogues, (E)-5-(2-bromovinyl)-araU (BrVaraU) and 5-vinyl-araU (VaraU), which can be considered as structural analogues of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BrVUdR), are potent and selective inhibitors of herpes simplex virus type 1 (HSV-1) replication in vitro. BrVaraU and VaraU have been compared with BrVUdR for their therapeutic effect on acute HSV-1 keratitis in rabbits. Both araU derivatives applied as 0.1% eyedrops suppressed the development of keratitis as monitored by the reduced number of herpes efflorescences. The healing effect of BrVaraU and VaraU was less pronounced than that of 0.1% BrVUdR eyedrops, the difference between BrVUdR and VaraU being statistically significant at the 10th day of treatment. As a further indication of the healing effect the number of cornea with opacities seen after cessation of drug treatment were 3.3, 7.4, 27.6 and 46.9% for the BrVUdR-BrVaraU-, VaraU- and placebo-treated eyes, respectively.  相似文献   

17.
18.
Effects of 1-(2-ethoxyethyl)-2(4-methyl-1-homopiperazinyl)benzimidazole difumarate (KB-2413) on the circulation and the other systems were compared with those of ketotifen and chlorpheniramine. 1. Among the effects on the circulation and the respiratory system, KB-2413 as well as ketotifen and chlorpheniramine transiently inhibited respiration at 3 mg/kg i.v. and slightly decreased blood pressure in dogs. KB-2413 slightly decreased heart rate in dogs, but ketotifen slightly increased it. 2. KB-2413 at 100 mg/kg p.o. slightly decreased the volume of gastric juice in rats and dose-dependently increased biliary secretion in rats in the dose range of 10-100 mg/kg i.d. On the other hand, ketotifen and chlorpheniramine decreased biliary secretion. 3. KB-2413 inhibited the spontaneous movements of various isolated smooth muscles at a high concentration of 10(-4) g/ml. 4. The autonomic system in cats and the motor nervous system in rats were not influenced by KB-2413 at 3 mg/kg i.v. 5. The blood clotting system, blood sugar level, urine volume and urinary electrolytes in rats were not affected by KB-2413 in the dose range of 10-100 mg/kg p.o. 6. KB-2413 inhibited carrageenin-induced rat paw edema at 100 mg/kg p.o. In conclusion, KB-2413 showed a less potent effect on the circulation and the other systems than ketotifen and chlorpheniramine, and no results suggested serious side effects of KB-2413.  相似文献   

19.
Human breast milk is rich in 2-palmitoyl 1,3 unsaturated triacyglycerols and during the neonatal period, when milk is the sole source of nutrients, their role could be particularly important. Betapol is a novel triacylglycerol mix resembling human breast milk in its high palmitic acid content and positional distribution. The total fat absorption from Betapol has been shown to be higher than fat from conventional infant milk formulas and closer to human breast milk in infants. However, the relative fate of purified palmitic acid esterified to glycerol in the 1-, 3- and 2-positions in neonatal and young animals has not previously been established. Therefore, the fate of orally administered 1-[1-14C]palmitoyl, 2,3 dioleoyl glycerol ([14C]POO) and 1,3 dioleoyl,2-[1-14C]palmitoyl glycerol (O[14C]PO) was investigated in suckling and weanling rats using liquid scintillation counting of tissues and expired air and whole-body autoradiography. The results obtained indicate that orally administered [14C]POO and O[14C]PO are extensively absorbed from the gut, probably either as palmitic acid or as a palmitoyl glyceride in both suckling and weanling rats. Radioactivity initially concentrated in brown fat with apparent migration to the white fat of weanling rats by 96 h. Levels of 14C were low in blood, brain and other tissues. Excretion of 14C was mainly by expiration of CO(2) (approximately 72% in 96 h), indicating beta-oxidation as a major route of metabolism. Urine and faeces accounted for only approximately 6% of the excreted radioactivity. The design and size of the experiment did not allow tests of statistical significance between the absorption and excretion of OPO and POO to be conducted. However, the absorption, distribution, beta-oxidation and excretion appeared to be similar.  相似文献   

20.
钮丽萍 《安徽医药》2014,(12):2279-2282
目的:探讨研究2型糖尿病肾病患者肾功能、糖化血红蛋白、尿微量白蛋白与血脂代谢的关系。方法120例诊断患者依尿微量白蛋白排泄率分为正常白蛋白尿( NAU)组、微量白蛋白尿( MAU)组和临床蛋白尿( CAU)组,依糖化血红蛋白水平分为A、B、C三组,另外选30例体检健康者作为对照组( NC)。检测各种生化指标:空腹血糖( FBG)、胆固醇( TCH)、甘油三酯(TG)、血清素氮(BUN)、血清肌酐(Cr)、高密度脂蛋白(HDL-C)、低密度脂蛋白(LDL-C)、糖化血红蛋白(HbA1C)、尿微量白蛋白(mAlb)。结果 T2DM组和NC组相比,FBG、TG、TC、LDL-C、HbA1C水平高于NC组(P<0.01),HDL-C低于对照组(P<0.05);CAU组、MAU组的FBG、TG、TC、LDL-C、HbA1C指标要明显的高于NAU组(P<0.05);CAU的FBG、TG、TC、LDL-C、HbA1C明显大于MAU组(P<0.01),CAU 组的HDL要低于MAU 组和NUA组(P<0.05),2型糖尿病肾病患者在FPG、HbA1C、TCH、TG、UAE和NC组相比较差异有统计学意义(P<0.05),BUN、Cr与NC组相对比,其差异无统计学意义(P>0.05)。 T2DM患者各组之间FPG、HbA1C相互比较,差异有统计学意义(P<0.05);而各组间的TCH、TG、BUN、Cr相互比较无统计学意义( P>0.05)。结论2型糖尿病肾病患者的尿微量白蛋白增高程度与糖化血红蛋白的增高有关,而尿微量白蛋白是糖尿病早期肾脏损害的灵敏指标,联合检测 HbA1 C、mAlb以及各项血脂水平对糖尿病肾病的早期预防诊断及治疗有重要意义。  相似文献   

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