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At least 685 records · Page 38Linked to original sources
PubMed2003

Effects of dimethindene maleate nasal spray on the quality of life in seasonal allergic rhinitis.

OBJECTIVE: To determine if the H1-receptor antagonist dimethindene maleate (DMM), topically applied, is able to improve the quality of life (QoL) in patients with seasonal allergic rhinitis better than placebo. METHODS: The study was a multi-centre, randomised, placebo-controlled, double-blinded phase III trial including 157 patients. Two parallel groups received either DMM nasal spray or placebo for 2 weeks. Patients answered 5 QoL questionnaires (Rhinoconjunctivitis QoL Questionnaire (LQ-AR), Munich Life Dimension List (MLDL), Profile of Mood States (POMS), 2 Visual Analogue Scales (VAS-QoL, VAS-GES)) on days 1, 4, 8, and 15. RESULTS: QoL improved significantly in all scales and groups. Statistically significant differences between groups were achieved in the sub-scales LQ-AR Eye Symptoms and Daily Activities, MLDL Total, POMS Depression and Energy, VAS-QoL and VAS-General Health. All differences favoured the DMM group and were present initially but disappeared in visit 4, except MLDL Total and POMS Energy. Almost all other scores had a better tendency of DMM. CONCLUSION: A significant improvement of QoL was found in both groups. Only weak differences between groups (in favour of DMM) were found. There are several reasons explaining this outcome, mainly the rainy weather during the study period (mean weather index 10-20% less sunny than in previous seasons).

Administration, Intranasal↗
PubMed1992

Dose-proportional plasma levels of the analgesic flupirtine maleate in man. Application of a new HPLC assay.

Single oral doses of the non-opioid, centrally-acting analgesic flupirtine maleate (Katadolon, CAS 75507-68-5) were administered to healthy volunteers and the 2 h plasma levels determined with a new specific HPLC assay. 50, 100, 200, and 300 mg were ingested as the commercial capsules in a double-blind randomized cross-over design with time intervals of at least 6 d. Dose-proportionality was observed for the median 2 h plasma levels which is in agreement with dose-proportionality previously described for multiple-dose studies.

Aminopyridines↗
PubMed2004

[Prescription and safety of dimethindene maleate micropellet capsules in Hungary].

INTRODUCTION: Dimethindene maleate, the active substance of the extended-release Fenistil 24 capsule, is a first-generation histamine receptor antagonist, which is marketed in 10 European countries. In Hungary approximately 200,000 boxes are sold yearly from this product, which is mainly used for treatment of symptoms associated with allergic diseases (urticaria, itch, hay fever) The aim of the present study was to gather information with the help of medical doctors about the indications, efficacy and primarily the safety of use, observed side effects and frequency of adverse events associated with this product. METHOD: During the study 4574 questionnaires were evaluated out of the 5578 filled by 249 doctors. Responses were included into the evaluation only if the address and type of polyclinic of the doctor filling the questionnaire, indication of the use of the product could be precisely identified and the patient returned for control visit at least once. RESULTS: Based on the study results in Hungary in most cases the product is prescribed according to the indications and dosing schedule given in the SPC. In this study participating doctors found the drug to be effective in 95% of cases. Unexpected, new adverse events were not observed during the study. Approximately 22% of patients reported adverse events, tiredness and sleepiness being the most frequent ones. Occurrence of sedative adverse events was more frequent among those who were prone to tiredness (51 vs. 17%). The adverse events most frequently were reported 10-12 hours after intake. The average length of treatment was 4 weeks or less. The medicine is taken usually at night, before going to sleep. CONCLUSIONS: In Hungary in most cases the product is prescribed according to the indications and dosing schedule given in the current approved Summary of Product Characteristics.

Adolescent↗
PubMedDate not supplied

[Effect of enalapril maleate and lozartan on the size of experimental myocardial infarction, hemoglobin affinity to oxygen and various parameters of lipid peroxidation].

The intravenous injections of enalapril maleate (0.1 and 0.5 mg/kg) and losartan (0.5 and 2.5 mg/kg) produced a 22-32% decrease in the size of myocardial infarction in rats with coronary ligation. This was accompanied by inhibition of the lipid peroxidation as revealed by the MDA test and Fe2+ induced chemiluminescence. Both drugs also increased the oxygen affinity of hemoglobin in the P50 test in vitro. Enalapril did not significantly alter the MDA level and superoxide dismutase (SOD) activity in the whole human blood. In contrast, losartan reliably inhibited SOD activity.

Angiotensin II↗
PubMed2004

[Postpartum cerebral angiopathy--a case report the vasculopathy associated with co-administration of two vasoconstrictives, methylergometrine maleate and sumatriptan].

A 25-year-old woman (gravida 1, para 0) who had no history indicating the toxemia of pregnancy developed hypertension and severe throbbing headache after the delivery of her first child by the cesarean section. Generalized tonic-clonic seizure ensued 5 days after the delivery, after which she did not fully regain her consciousness. Her head T2-weighted and FLAIR MRIs showed areas of multiple high intensities in the basal ganglia and cerebral white matter. Her cerebral MRA revealed the segmental stenosis and irregular wall of the major vessels, in particular of the right MCA trunk. Three weeks later, these abnormalities in the neuroimages disappeared and she was free of any symptoms. The history disclosed that obstetricians had used methylergometrine maleate for uterine contraction after delivery and then sumatriptan for her throbbing headache. We speculate that these vasoconstrictive agents might have induced the postpartum cerebral angiopathy. Postpartum cerebral angiopathy may be distinct from reversible posterior leukoencephalopathy in that the abnormalities are not restricted to the posterior lobes and that the vascular changes are apparent on neuroimagings. However, this entity might have a common underlying physiology, which is the abnormally elevated blood pressure that occurs in the setting of early postpartum period. Caution should be exercised when vasoconstrictives are to be used in postpartum period.

Adult↗
PubMedDate not supplied

Kinetics of degradation of enalapril maleate in dosage forms.

The effect of humidity and temperature on the stability of enalapril maleate (ENA) in tablets have been studied. Tablets with ENA were stored in final packs (blisters) and without final packs in the atmosphere of increased humidity (76.4 % RH) and in the temperature range from 313 K to 333 K (forced degradation test). Degradation of ENA in tablets stored in final packs and without final packs followed the first order reaction model. During this study, the product of hydrolysis of the ester group and intramolecular cyclization have been observed. Thermodynamic parameters (activation energies, enthalpy and entropy) for the decomposition of ENA in tablets were calculated.

Angiotensin-Converting Enzyme Inhibitors↗
PubMed1992

[Colonic radiography by double-contrast enema in the elderly patient with the use of trimebutine maleate].

About 15% of hospitalizations of patients over 65 are due to disorders of the colon which means that accurate analysis of history and clinical and instrumental investigation are mandatory. Our attention has been focused on x-ray examination using a double-contrast enema which, together with endoscopy, permits to diagnose colonic disorders with significant reliability. Our aim was to adapt the method to the special needs of the patient over 65 by employing the active substance trimebutine maleate (M.T.) as a "contact" pressure-lowering agent. Thirty-five subjects aged 65-75 with pathologies implying a risk for the use of parasympatholytic agents were examined. None of these patients showed side effects. It can therefore be said that the use of M.T. as a hypotonic agent in double-contrast enemas is an indisputable diagnostic aid.

Aged↗
PubMedDate not supplied

Determination of phenylephrine hydrochloride, chlorpheniramine maleate, and methscopolamine nitrate in tablets or capsules by liquid chromatography with two UV absorbance detectors in series.

A procedure is presented for the simultaneous determination of phenylephrine HCI (PE), chlorpheniramine maleate (CM), and methscopolamine nitrate in commercial tablets or capsules by liquid chromatography (LC) with 2 UV absorbance detectors in series. Reference and sample solutions are prepared in methanol. LC separations are performed on a 7.5 cm Novapak silica column. The mobile phase is prepared by mixing 930 mL methanol with 70 mL of a 0.5% aqueous solution of 1-pentanesulfonic acid, sodium salt. The injection volume is 20 microL; the flow rate is approximately 1 mL/min. Retention times are approximately 1.5 min for PE, 3 min for CM, and 6 min for methscopolamine nitrate. One detector determines the first 2 compounds at 265 nm, but the third compound does not produce a detectable peak. The other detector set at 210 nm generates peaks for all 3 compounds, but only methscopolamine is within the recorder range; the other 2 compounds are exceedingly off scale. If it is not feasible or desirable to arrange 2 UV absorbance detectors in series, separate determinations can be made, one for the first 2 compounds and the other for the third component of the mixture. Two commercial samples of tablets and 2 commercial samples of capsules were analyzed by the proposed method. Recovery studies were also conducted with amounts of the 3 compounds ranging from 80 to 120% of the quantities present in the sample solutions.

Capsules↗
PubMed2006

Formulation and evaluation of mucoadhesive dosage form containing rosiglitazone maleate.

Extending the residence time of a dosage form at a particular site and controlling the release of drug from the dosage form are useful especially for achieving controlled plasma level of the drug as well as improving bioavailability. The objective of this study was to extend the GI residence time of the dosage form and control the release of rosiglitazone using mucoadhesive tablet to achieve controlled plasma level of the drug which is especially useful after 8 to 12 weeks of monotherapy using conventional dosage forms when dose is doubled and plasma level also doubles. Direct compression method using simplex lattice design, followed by optimization of the evaluation parameters was employed to get final optimized formulation. The optimized formulation showed a mucoadhesive strength >40 gm-f, and a mucoadhesion time >12 hours with release profile closer to the target release profile and followed Non-Fickian diffusion mediated release of rosiglitazone maleate.

Adhesives↗
PubMed1991

Pharmacological properties of 5-[(6,7,8-trimethoxy-4-quinazolinyl) amino]-1-pentanyl nitrate maleate in cardiovascular system.

Effects of 5-[6,7,8-trimethoxy-4-quinazolinyl)amino]-1-pentanyl nitrate maleate (KT-1, CAS 47487-05-8), whose chemical structure has both a prazosin and a nitrate moiety, on cardiovascular system were investigated in in vivo and in vitro experiments. KT-1 i.v. decreased aortic pressure, renal blood flow, left ventricular enddiastolic pressure and resistances of total peripheral, vertebral, coronary and renal vasculatures and increased aortic blood flow, vertebral blood flow, coronary blood flow, peak positive left ventricular dP/dt and heart rate in anesthetized open-chest dogs. These cardiovascular effects of KT-1 were similar to those of glyceryl trinitrate (nitroglycerin, GTN). Nitrate-deleted KT-1 from its chemical structure (denitro KT-1) equimolar to KT-1 produced no marked changes in these cardiovascular parameters, but 3 or 10 times large doses of denitro KT-1 showed relatively long persisting vasodilator effects. In isolated dog coronary artery preparations contracted with KCl, the order of relaxant potency was GTN greater than KT-1 greater than denitro KT-1. In isolated dog mesenteric artery preparations, phenylephrine produced concentration-dependent contractions which were significantly inhibited by prazosin and KT-1 but not by denitro KT-1. In anesthetized open-chest dogs, phenylephrine produced pressor responses which were significantly inhibited by KT-1 but not by GTN or denitro KT-1. In isolated rat thoracic aorta strips, in contrast to GTN, KT-1 hardly developed a tachyphylaxis. Thus, KT-1 showed cardiovascular effects similar to those of both nitrates and a1-adrenoceptor blocking agents with no development of a tachyphylaxis.

Animals↗
PubMed1991

Cost of switching hypertensive patients from enalapril maleate to lisinopril.

The costs and potential savings associated with switching patients in a hypertension clinic from enalapril maleate to lisinopril were analyzed. Patients taking enalapril were randomized to receive lisinopril or to continue taking enalapril. For the 47 patients randomized, data were collected for 25 patients switched to an equal milligram dosage of lisinopril and for 21 patients who continued to receive a constant dosage of enalapril. To maintain blood pressure control, it was necessary to double the dosage of lisinopril in five patients (20%) and have it in one patient (4%), while the enalapril dosage was doubled in two patients (9.5%). The total direct cost of switching patients to lisinopril was $66.33 per patient. The annual drug cost savings per patient for switching to lisinopril would be $52.08, $46.80, and $120.24 for therapy with one 5-, 10-, and 20-mg tablet per day, respectively. A patient would have to receive 15, 17, or 7 months of therapy with 5-, 10-, or 20-mg tablets of lisinopril, respectively, before a net cost savings would be realized. In the evaluation of a less expensive therapeutic alternative, the total cost of switching must be considered.

Antihypertensive Agents↗
PubMed1991

[Intracoronary administration of ergonovine maleate for detecting vasospastic angina; one dose method].

Coronary spasm is an important etiologic mechanism in the pathogenesis of myocardial ischemia. Provocative test of coronary spasm during coronary arteriography is clinically useful. The ergonovine test has gained widespread use, and we have examined the efficacy and safety of intracoronary ergonovine application with a fixed dose of 16 micrograms. We studied 119 patients undergoing coronary arteriography. Coronary spasm was induced in 34 cases by intracoronary administration of 16 micrograms of ergonovine maleate. Coronary spasm was readily resolved by intracoronary administration of isosorbide dinitrate. None of the cases negative to the intracoronary ergonovine applications could be induced by additional systemic administration of 0.4 mg of ergonovine. Side effects of ergonovine such as elevation of blood pressure, headache and chest symptoms were infrequent in the intracoronary ergonovine test. We conclude that our method of intracoronary ergonovine application is sensitive and safe for the diagnosis of coronary spasm.

Aorta↗
PubMed1991

Perhexiline maleate-induced hepatitis.

We report on a case of perhexiline maleate-induced hepatitis secondary to a long-term administration of recommended daily dosages of 300 mg. The patient had a spectacular weight loss of 29 kg. He developed hepatitis, which subsided after drug withdrawal. Our electron-microscopic findings with the typical inclusion bodies and impaired hydroxylation capacity point to an underlying metabolic disorder as the pathogenetic mechanism.

Angina Pectoris↗
PubMed1990

Physico-chemical properties and stability of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H- dibenz[2,3:6,7]oxepino[4,5-c]pyrrolidine maleate.

The physico-chemical properties of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H- dibenz[2,3:6,7]oxepino[4,5-c]pyrrolidine maleate (Org 5222), a new potential antipsychotic compound, were studied by interpretation of its spectra (UV,IR,NMR,mass), X-ray analysis, thermal properties, solubilities and partition coefficient. Analytical methods such as GLC and TLC were developed for use in stability tests. Crystalline Org 5222 was shown to be stable with respect to heat. Only excessive exposure to light was shown to induce degradation of crystalline Org 5222. In solutions of pH 1, 4 and 7 only slight degradation was observed at high temperature or after exposure to light.

Antipsychotic Agents↗
PubMed1990

Biotransformation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1-H-dibenz[2,3:6,7]oxepin o [4,5-c]pyrrolidine maleate in rats.

The metabolism of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1 H-dibenz[2,3:6,7]oxepinol [4,5-c]pyrrolidine maleate (Org 5222) labelled with [3H] or [14C] was investigated in Wistar rats. Metabolites were identified by mass spectrometry, 13C- and 1H-NMR analysis, IR spectroscopy and, wherever possible, by comparison with authentic reference compounds. The metabolites found in plasma, bile, faeces and urine revealed the processes of metabolism in which Org 5222 underwent oxidation to yield an N-oxide existing in two diastereoisomeric forms, or N-demethylation to yield a demethyl metabolite. A novel metabolite was found in bile, viz. a carbamate glucuronide, formed from an intermediate carbamic acid, derived from the addition of CO2 to the demethyl metabolite.

Animals↗
PubMed1990

Behavioural pharmacology of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro- 1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrolidine maleate, a compound interacting with dopaminergic and serotonergic receptors.

trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H- dibenz[2,3:6,7]oxepinol[4,5-c]pyrrolidine maleate (Org 5222) is a new compound with effects on animal behaviour indicating strong antipsychotic potential based on antagonism of dopaminergic and serotonergic effects. The compound inhibits apomorphine-induced climbing behaviour, mouse locomotor activity, rat activity in an open field, shuttle box behaviour in rats, pergolide induced circling in 6-hydroxydopamine(6-OHDA) lesioned rats, serotonin agonist-induced forepaw treading, head shakes and penile erections. The compound is less effective in inducing catalepsy, and antagonising SKF-38393 (tetrahydro- 1-phenyl-1H-3-benzazepine-7,8-diol HCl)-induced circling in 6-OHDA-lesioned rats and it does not induce perioral movements in rats. Based on these data and the neurochemical profile of the compound it was decided that this compound merits clinical investigation in a programme aiming for an effective antipsychotic agent with reduced risks of extrapyramidal side-effects.

Animals↗
PubMed1990

Neurochemical studies with the potential antipsychotic compound trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H- dibenz[2,3:6,7]oxepino[4,5-c]pyrrolidine maleate.

trans-5-Chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz [2,3:6,7]oxepino[4,5-c]pyrrolidine maleate (Org 5222) has dopamine D2 antagonistic and negligible anticholinergic properties of the classical neuroleptic haloperidol. In addition it combines the strong antiserotonergic and antihistaminergic properties of chlorpromazine and clozapine with the potent dopamine D-1 antagonistic properties of Sch 23390 (R-(+)-delta-chloro-2,3,4,5-tetrahydro-3-methyl-5- phenyl-1H-3-benazepin-7-ol(Z)-2-buteneoate). This in conjunction to its behavioural properties, warrants clinical testing in psychotic patients.

8-Hydroxy-2-(di-n-propylamino)tetralin↗