Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Purpose of this study was to evaluate the activity of dihydroergocristine (DHEC, CAS 17479-19-5) at three different dosages, when administered to aged patients with senile dementia of Alzheimer type. Eighty patients, 48 males and 32 females, aged 55-80 years, affected with senile organic brain syndrome, were admitted to the trial. Clinical evaluation was made by SCAG (Sandoz Clinical Assessment Geriatric Scale). Inclusion criteria considered patients presenting at the basal evaluation a total SCAG score between 60 and 90, with stressed impairment of cognitive function. All the patients were divided in four groups and treated with DHEC 1.5, 3, 6 mg/d or placebo for three months. The evaluation of the total SCAG score demonstrated a significant activity of the drug compared vs placebo, and a dose-related effect. Also for the single clusters it was demonstrated a significant (p < 0.05) dose/effect relation, except for the "affective" one; on the contrary "cognitive functioning" cluster displayed the best benefit. The drug was very well tolerated, as only some cases of dyspepsia, mild gastralgia and nausea were reported in some patients.
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PMID:[Dihydroergocristine in the treatment of organic brain psychosyndrome. Dose-finding study against placebo]. 149 61

Aim of the study was to assess the activity of dihydroergocristine (DHEC, CAS 17479-19-5) in aged patients with impaired cognitive function. Twenty-five university hospital centres and 250 physicians participated in the study. 2,600 patients (1,104 males and 1,496 females, age range 50-80 years) were admitted to the study. Each patient was administered 6 mg/d DHEC for 120 days. Clinical evaluation was made through the SCAG Rating Scale registered at basal time, after 60 and 120 days. Responsivity to treatment was considered high when the final score was reduced by 30% and none if less than 10%. Analysis of results demonstrated that at the end of the study responsivity was high in 73% of cases, moderate in 20.4% and absent in 6.5%. Tolerability was very good as side effects were reported only in 3.16% of patients. Most frequent side effects were: nausea (1.23%), gastralgia (1.11%), headache (0.29%), hypotension (0.12%), vertigo (0.12%) and rash (0.08%). Drop-outs for gastralgia were reported only in 0.53% of the patients.
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PMID:[Epidemiologic study on the effectiveness and safety of dihydroergocristine in impaired memory and behavioral functions in aged humans]. 149 66

One hour after suicidal ingestion of about 20 mL of a 38% solution of bromofosmethyl, CAS: 2104-96-3 (bromophos), a 52 year-old female was admitted to the hospital with extreme miosis, hypersalivation, hyperperistalsis and muscular fibrillation. Gastric lavage was performed and activated charcoal administered. Cholinergic symptoms were antagonized by repeated doses of 0.5 mg atropine. Because of the high dose of bromophos, hemoperfusion was performed with amberlite XAD4. The bromophos clearance during hemoperfusion was 95 mL/min (flow 200 mL/min). The patient received two doses of 500 mg obidoxime for recurrent muscular fibrillation. The further clinical course was uneventful. On day 4, the patient was transferred to a psychiatric ward because of persistent suicidality. In contrast to poisoning by most organophosphates, red blood cell acetyl cholinesterase was only minimally depressed but the plasma butyryl cholinesterase was initially decreased and normalized within a few days. The records of 25 patients reported to our Poison Control Center with ingestion of more than 1 g bromophos were also evaluated. The most frequent symptoms were miosis, hyperperistalsis, hypersalivation, agitation, nausea/vomiting and convulsions. Nine of the patients had no symptoms. Bromophos is relatively less toxic than its phosphate derivative, parathion.
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PMID:Acute poisoning with bromofosmethyl (bromophos). 205 7

The objective of this study was two-fold: 1. to determine the pharmacokinetic parameters and the bioavailability of two 20 mg isosorbide-5-mononitrate (CAS 16051-77-7, IS-5-MN) preparations (treatments A and B) after single oral administration and 2. to evaluate the absolute bioavailability of IS-5-MN, which was possible by the administration of a third IS-5-MN preparation (treatment C) by the intravenous route (1 mg/ml, dose 20 mg). The three preparations were examined in 24 healthy volunteers according to a randomized 3-way cross-over design, blood samples were withdrawn up to 24 h following the administration of IS-5-MN and plasma concentrations of IS-5-MN were quantified by a gas chromatography method. The two oral preparations led to peak concentration values of about 360 ng/ml of IS-5-MN in the mean 0.90 h (treatment A) and 0.97 h (treatment B) after drug administration. The corresponding values for the infusion were 339.6 ng/ml and 2.59 h in the mean. For the areas under the curve (AUC(0-infinity)) mean values of 2733 (treatment A). 2724 (treatment B) and 2877 h x ng/ml (treatment C) were found. The absolute bioavailability of both oral treatments revealed values of 95.00% and 94.74% for treatments A and B, respectively. The statistical comparison (ANOVA, confidence intervals) of the pharmacokinetic parameters showed bioequivalence between both oral preparations and equivalence in the amount of drug absorption between both oral formulations and the i.v.-infusion. The observed undesired side effects (e.g. headache or nausea) are well known to occur after IS-5-MN administration.
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PMID:Evaluation of the pharmacokinetics and absolute bioavailability of three isosorbide-5-mononitrate preparations in healthy volunteers. 771 Apr 35

The trial randomly assigned 652 patients with non-ulcer dyspepsia (NUD), defined as chronic or recurrent complaints of acid-related (heartburn, acid regurgitation, epigastric pain) and non-acid related (fullness/vomiting, nausea) symptoms and with no evidence of organic disease, to treatment for 4 weeks with 150 mg of ranitidine (Zantic, CAS 66357-59-3) twice a day, or placebo, according to a double-blind design. The presence and duration of all dyspeptic symptoms were recorded by interviews at the beginning and after 2 and 4 weeks of treatment as well as by diaries. The complete disappearance of all dyspeptic symptoms after 4 weeks in the placebo group was 36%; ranitidine treatment resulted in a significant improvement after 4 weeks (p < 0.05). The effect of ranitidine was slightly more pronounced in acid-related than in non-acid-related symptoms. We conclude that suppression of gastric acid secretion is of clinical value in NUD patients, especially in those suffering from epigastric pain, acid regurgitation and heartburn.
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PMID:Ranitidine in the treatment of non-ulcer dyspepsia. A placebo-controlled study in the Federal Republic of Germany. 781 86

The activity of pidotimod ((R)-3-[(S)-(5-oxo-2-pyrrolidinyl) carbonyl]-thiazolidine-4-carboxylic acid, PGT/1A, CAS 121808-62-6) was studied vs. placebo in a double-blind, randomized, multicentre trial, involving 60 pediatric patients with recurrent urinary tract infections. Recovery from acute events was quicker with pidotimod than with placebo (9.6 vs. 12.3 days). In treated patients antibiotic therapy was shorter (6.9 vs. 8.3 days) and main symptomatic parameters (body temperature, vesical tenesmus, stranguria, pollakiuria, total number of symptoms, total symptomatic intensity, rate of asymptomatic patients, haematuria, leukocyturia, positive urinary culture) receded quickly. In patients receiving the drug as well as in patients treated with placebo changes in laboratory parameters were observed, indicating recovery from the acute infectious disease. A significant trend to normalization of the immune response, expressed by chemotaxis and index of leukocyte phagocytosis, was found only in patients treated with pidotimod. After the acute episode a significant decrease of risk of relapses (69%) was observed in these patients. If a relapse occurs, the response of treated patients is quicker (duration of fever, total time of relapses) than for control patients. These findings allow to correlate the individual immune response activation to the resistance to recurrent infections and also to a better response to therapy if the disease occurs and becomes clinically relevant. No side effects were observed. Mild reactions (4 nausea/vomiting, 1 erythema) occurred only in 5 patients (2 pidotimod, 3 placebo) but were attributed to concomitant antibiotic therapy. No alterations of main laboratory parameters were found. These findings confirm the tolerability of the drug also in long-term treatment.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Therapeutic efficacy and safety of pidotimod in the treatment of urinary tract infections in children. 785 49

Twenty-three of 34 workers who had worked in the injection molding operation making polyurethane foam parts at an automobile parts manufacturing plant developed respiratory symptoms and/or systemic symptoms over a 2-month period following the full production use of a new diisocyanate paint that contained 1,3-bis(isocyanatomethyl)cyclohexane pre-polymer (BIC)(CAS #75138-76-0, 38661-72-2). At 3 months, all subjects underwent an interview, physical examination, pre- and post-shift pulmonary function tests, and either methacholine challenge test or bronchodilator challenge at an occupational health clinic. The most frequently cited symptoms were dyspnea (65%), cough (61%), chest tightness (57%), chills (57%), wheezing (30%), and myalgias, arthralgias, and nausea (26%). Thirteen subjects had either a positive methacholine challenge test or a positive response to bronchodilator challenge, making the overall prevalence of airway hyperresponsiveness 38%. The overall prevalence of hypersensitivity pneumonitis-like reactions among line operators in the injection molding process was 27%. This disease outbreak suggests that 1,3-bis(isocyanatomethyl)cyclohexane pre-polymer may cause asthma and hypersensitivity pneumonitis-like reactions. The use of BIC was discontinued 6 months after the first workers developed symptoms.
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PMID:Hypersensitivity pneumonitis-like reaction and occupational asthma associated with 1,3-bis(isocyanatomethyl) cyclohexane pre-polymer. 883 82

A pilot study in 14 patients with mild asthma was performed to study the anti-inflammatory efficacy of theophylline (CAS 58-55-9). At the start, during and at the end of a 3 months' treatment with oral sustained release theophylline and during 1 week thereafter, the influence on airway hyperreactivity and ECP (eosinophil cationic protein) serum levels was investigated. Airway responsiveness was expressed as the cumulative provocative dose of methacholine necessary to decrease FEV1 by 20% (PD20-FEV1). Data of 8 patients were suitable for evaluation. At a mean predose serum concentration of 6.5 mg/l, theophylline increased the mean PD20-FEV1 for methacholine from 151 micrograms (at start) to 332 micrograms (at the end of medication), and reduced the mean ECP serum concentration from 34.6 to 24.5 micrograms/l. Up to 1 week after theophylline treatment, the improvement of airway hyperreactivity compared to the baseline was maintained, whereas ECP-serum levels tended to increase. Thus, theophylline markedly attenuated airway hyperreactivity in patients with bronchial asthma at "subtherapeutic" serum theophylline concentrations as well as ECP serum concentrations, suggesting the anti-inflammatory efficacy of theophylline. These observations may have therapeutic implications in the treatment of patients with mild asthma. A slight improvement of lung function and dyspnoea, and a reduction of additional beta 2-bronchodilator use was also observed. Two patients only complained of slight nausea, tremor and restlessness.
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PMID:[The anti-inflammatory action of an oral sustained-release theophylline preparation. Results of a clinical pilot study with low dosages]. 967 55

The present study was conducted to describe and compare the in vivo performance (systemic exposure), clinical and laboratory safety of a fixed combinational product of inhaled reproterol (CAS 54063-54-6) plus disodium cromoglycate (DSCG; CAS 15826-37-6) using a novel freon (CFC)-free metered dose inhaler (MDI), which uses 1,1,1,2,3,3,3-heptafluoropropane (HFA-227; CAS 431-89-0) as propellant and polyoxyethylene glyceryl trioleate (Tagat TO; CAS 68958-64-5) as surfactant relative to the conventional freon-driven MDI Allergospasmin in healthy male and female volunteers. Twenty-four young male and female healthy subjects were randomly allocated in gender-balanced fashion to 4 parallel treatment groups with single and repeated dosing of either reproterol + DSCG by HFA- or CFC-MDI (each time N = 8) or placebo by HFA- or CFC-MDI (each time N = 4) using matched placebo devices thus allowing a double-blind (with regard to placebo) approach. Treatments consisted of a single morning dose of 2 actuations followed 4 days later by a 1 week treatment course of 2 actuations four times daily. Subjects were investigated extensively in terms of blood pressure, pulse rate, electrocardiography, spirometry, respiratory rate, body temperature, laboratory safety (haematology, clinical chemistry, urinalysis) and clinical well-being. There were no treatment, compound or device related effects for any of the tolerability and safety end points. The treatments were well tolerated. In particular, there was no irritative cough or any sign of broncho-irritation on application. Adverse events were reported in a total of 9 subjects: 3/8, 4/8, 0/4 and 2/4 subjects treated with reproterol + DSCG by HFA-MDI, reproterol + DSCG by CFC-MDI, placebo by HFA-MDI and placebo by CFC-MDI, respectively. Of these, 6 events in 6 subjects receiving the active treatments were considered probably or definitely related to the test drug administration (i.e. adverse drug reactions): after reproterol + DSCG one subject in each treatment group (HFA-MDI and CFC-MDI) complained of an unpleasant bitter taste immediately after application; one further subject in each group complained of headache. Under treatment with reproterol + DSCG by CFC-MDI one male subject complained of mild transient nausea with onset on day 5. Under treatment with reproterol + DSCG by HFA-MDI one female subject complained of mild dizziness and mildly disturbed (blurred) vision with onset on day 1. All adverse events occurred only transitory and required no treatment. Systemic exposure, evaluated by the plasma concentrations of DSCG at 1 h after application, was slightly higher with the HFA-MDI compared to the CFC-MDI. It is concluded that the safety, tolerability and in vivo performance of the newly developed freon-free MDI is at least as well tolerable as the already marketed freon-driven conventional formulation.
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PMID:Tolerability and in vivo performance of a novel freon-free metered dose inhaler for a fixed combinational product of reproterol and disodium cromoglycate. 968 24

An oral solution available as ethanol-free droplets of the fixed drug combination tilidine-HCl 50 mg/naloxone-HCl 4 mg (CAS 27107-79-5 and CAS 465-65-6, respectively; Tilidin-ratiopharm plus Tropfen) was investigated in 12 healthy volunteers together with an ethanol-containing reference preparation for comparable bioavailability. The study was conducted in an open, randomized, two-way cross-over design applying single doses of 20 droplets (equivalent to 50 mg tilidine-HCl/4 mg naloxone-HCl) of either formulation in the fasting state. The drug plasma profiles were monitored for a period of 48 h by means of LC-MS/MS for tilidine and its active metabolite nortilidine, whereas GC-MS was employed in order to determine naloxone and its phase I metabolite, 6-beta-naloxole. Maximum concentrations (Cmax) achieved were 22.28 ng/ml (tilidine) and 92.78 ng/ml (nortilidine) for the test preparation. Corresponding values for the reference preparation were 24.95 ng/ml (tilidine) and 100.73 ng/ml (nortilidine). The extent of drug absorption (AUC0-infinity) amounted to 38.83 ng h/ml and 467.63 ng h/ml for the prodrug tilidine and the metabolite nortilidine of the test preparation and corresponded well to 43.81 ng h/ml and 493.85 ng h/ml of the reference. Regarding the rate of drug absorption, essentially identical tmax and Rabs values for both tilidine and nortilidine of either preparation in addition pointed to well comparable liquid formulations and equipotent analgesia may be inferred from opioid pharmakokinetic profiles. Pharmacokinetics of the opioid antagonist naloxone and 6-beta-naloxole were also determined and resulted in well coinciding profiles for both preparations. Thus despite the fact that only minimum oral naloxone bioavailabilities were observed, plasma level monitoring of naloxone and 6-beta-naloxole allowed for demonstration of systemic exposure of opioid antagonistic compounds throughout a period of 2-3 h after oral drug administration. Due to the limited number of subjects involved, the primary aim of the study did not consist in demonstration of drug bioequivalence. Rather a comparable bioavailability between preparations was assumed if AUC and Cmax point estimators of 90% confidence intervals would be contained within a 0.80-1.20 range. The study outcome revealed that all four investigated analytes met this requirement, whilst nortilidine pharmacokinetic parameters even fulfilled commonly accepted bioequivalence criteria, i.e. inclusion of 90% confidence intervals of AUC- and Cmax-ratios within acceptance limits of 80% and 125%. Increased data variation observed with bioavailability parameters of tilidine, naloxone and 6-beta-naloxole prevented their bioequivalence demonstration based on only 12 study participants. In conclusion, single doses of two different tilidine/naloxone 50 mg/4 mg liquid formulations revealed well comparable bioavailability for all 4 analytes investigated. Both treatments were fairly well tolerated. Most frequently reported adverse events were dizziness, headache and nausea, which all recovered without sequelae and necessity of concomitant treatment.
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PMID:Bioavailability investigation of a new tilidine/naloxone liquid formulation compared to a reference formulation. 1044 8


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