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PubMed1991

Effect time-course of the inhibition of histamine induced skin reactions by orally applied dimethindene maleate.

We have investigated the time-course of the flare inhibiting activity of dimethindene maleate in man and compared the resulting effect-kinetic data with those from pharmacokinetic investigations. The study was carried out in a double-blind, placebo-controlled cross-over design with randomly assigned healthy volunteers. Dimethindene maleate (4 mg) was orally applied, followed by intracutaneous histamine provocations (-1, 2, 5, 14, 17, 20, 23, 26, 29 h). The two cross-over periods were separated by a wash-out phase of 17 h. Flare areas were documented 5, 10, 20 and 30 min after provocation with histamine. A strong inhibition of the development of flares was observed. With regard to the time-course of the inhibiting effect, its maximum was observed at a provocation time of 5 h. The mean residence time of the inhibiting effect was calculated to be ca. 13 h. This is different from the mean residence time of ca. 8 h obtained from blood level data. Blood- and effect-levels are not linearly related under oral treatment conditions.

Adult↗
PubMedDate not supplied

Fluvoxamine maleate: metabolism in man.

The metabolic fate of fluvoxamine maleate in man was investigated. The metabolites were isolated from the pooled urines of healthy volunteers who had ingested either 5 mg radioactive, or 100 mg non-radioactive fluvoxamine maleate as a single dose. The main isolation methods were solvent extraction, column and thin-layer chromatography. Eleven metabolites were isolated; eight of these were carboxylic acids. Identification of nine metabolites was accomplished by mass spectrometry supported by information from the UV spectra and the ionogenic properties. The main route of metabolic degradation of fluvoxamine begins with oxidative elimination of the methoxyl group, another route with removal of the primary amino group. In view of the nature of the degradation pattern none of the metabolites is likely to possess psychotropic activity. For the two primary metabolites this has, in effect, been demonstrated.

Biotransformation↗
PubMed1996

Bioequivalence study of two enalapril maleate tablet formulations in healthy male volunteers. Pharmacokinetic versus pharmacodynamic approach.

OBJECTIVE: Two different conventional release enalapril maleate tablet formulations were evaluated for their relative bioavailability (Eupressin tablets 10 mg, Biosintética as the test formulation vs Renitec tablets 10 mg Merck Sharp & Dhome, as the reference formulation). A single 20 mg oral dose of each preparation was administered to 18 healthy male adult volunteers and their bioequivalence was assessed by comparing the serum enalaprilat and total enalapril (enalaprilat plus enalapril maleate) concentration-time curves. Angiotensin converting enzyme (ACE) activity was also quantified in each serum sample. RESULTS: The pharmacokinetic parameters obtained for each formation were the area under the time-concentration curve from 0 to 24 h (AUC[0-24]), maximum concentration Cmax and the time at which it occurred (tmax). When serum enalaprilat concentration-time curves were employed to assess bioequivalence, the formulations were bioequivalent in the extent but not in the rate of absorption. However, no difference in either the extent or the rate of absorption were observed when serum total enalapril vs time curves were analysed. ACE activity-time curves were similar for both formulations and showed that ACE was 90% inhibited for 3-5 h after enalapril administration, and till approximately 50% after 24 h. At that time, circulating enalaprilat and total enalapril levels were less than the tenth of Cmax. CONCLUSION: The results show that complete bioequivalence of the two formulations can be concluded from serum total enalapril concentration data, and that serum ACE activity is not a suitable pharmacodynamic variable for assessing bioequivalence.

Adult↗
PubMed1999

Identification of connexins in human oral mucosa and therapeutic effect of irsogladine maleate on aphthous stomatitis.

We identified connexins 26 and 32 in human oral mucosa. The presence of the connexins indicates the presence of gap junctions in this tissue. However, immunofluorescence study found no significant differences in the expression of the connexins between patients with aphthons stomatitis and controls. Irsogladine maleate, which reinforces gap junctional intercellular communication in vitro, was effective for the treatment of transient and relapsing aphthous stomatitis, as well as symptomatic and drug-induced aphthous stomatitis. It was also useful for prevention of episodes of relapsing aphthous stomatitis, with daily administration preverting recurrence of stomatitis for more than 4 years one patient. These findings suggest that irsogladine maleate accelerates the wound healing process in oral mucosa by reinforcing gap junctional intercellular communication among oral mucosal cells; and that it is useful for the treatment and prevention of aphthous stomatitis.

Adult↗
PubMed1977

Provocation of coronary spasm with ergonovine maleate. New test with results in 57 patients undergoing coronary arteriography.

Ergonovine maleate (Ergotrate) was given to 57 patients undergoing coronary arteriography for investigation of angina occurring at rest or without provocation when routine study showed normal arteries or insufficient occlusive disease to explain their symptoms. This provocative test induced coronary arterial spasm in 13 patients, 10 of whom had definite Prinzmetal's angina. The spasm was easily reversed with sublingually administered nitroglycerin. The spasm was occlusive or nearly occlusive in nine patients, and there was associated reproduction of the chest pain and S-T elevation similar to the spontaneous episodes. One patient with Prinzmetal's angina had S-T depression rather than elevation in association with the chest pain. The other three patients without Prinzmetal's angina had focal narrowing without coronary occlusion, reproduction of the chest pain or electrocardiographic changes. Of the 44 patients who did not demonstrate coronary spasm in response to ergonovine, 29 had normal coronary arteries and 15 had various degrees of atherosclerotic occlusive disease. We conclude that cautious administration of ergonovine maleate during coronary arteriography can be safely used to elicit coronary spasm in some patients who have insufficient fixed occlusive disease to explain their symptoms.

Adult↗
PubMed1984

Effect of indomethacin on the ocular hypotensive action of timolol maleate.

A randomized, double-masked, cross-over study of nine healthy normal subjects was conducted to determine whether indomethacin affected the ocular hypotensive action of timolol maleate. A significant decrease in intraocular pressure occurred with timolol maleate 0.5% eyedrops (used twice a day) alone. Indomethacin (25 mg three times a day, given orally) administered concurrently had no effect on timolol's hypotensive action. No subjective or objective side effects occurred and there were no significant changes in blood pressure, pulse rate, or respiratory rate with either treatment.

Double-Blind Method↗
PubMed1982

Total serum angiotensin converting enzyme activity in rats and dogs after enalapril maleate (MK-421).

A centrifugal gel filtration separation of serum angiotensin converting enzyme (ACE) from a potent stable inhibitor is described. This, together with a 20 hr assay incubation of very dilute enzyme, permitted the assessment of the effects of enalapril maleate treatment on total serum ACE in rats and dogs. Total serum ACE increased in both species after 1 or 2 weeks at 10 mg/kg/day. Serum ACE in rats was more than doubled; whereas the increase was modest in dogs (48 +/- 9% minimum). The effect of the drug on serum ACE combined with inherent variability of ACE precluded use of serum ACE activity as an accurate measure of inhibitor concentration in animals receiving enalapril maleate.

Angiotensin-Converting Enzyme Inhibitors↗
PubMed1991

Phase I study of DABIS maleate given once every 3 weeks.

DABIS maleate is an alkylating quaternary nitrogen. In a phase I study DABIS maleate was administered as a single intravenous infusion once every 3 weeks. 32 patients with solid tumours were studied, at least 3 per dose level (50-1400 mg/m2). Dose-limiting toxicity was severe paresthaesias in the face, around the mouth and in the tongue. Cerebellar ataxia developed at 750 mg/m2 or higher. Haematological toxicity was minimal. Nausea and vomiting were mild to moderate. No other non-haematological side-effects were noted. The recommended dose for phase II studies at once every 3 weeks is 750 mg/m2 intravenously as a 15 min infusion.

Adenocarcinoma↗
PubMed1984

Chronic toxicity tests of pyrilamine maleate and methapyrilene hydrochloride in F344 rats.

Methapyrilene hydrochloride was administered at levels of 125 or 250 ppm in the diet to groups of male and female F344 rats. The closely analogous antihistaminic drug pyrilamine, as the maleate, was given at 2000 ppm in the diet or at 2 g/litre drinking-water to groups of male and female F344 rats. Almost all of the rats given the higher dose of methapyrilene had either carcinomas or neoplastic nodules of the liver, whereas at 125 ppm 40% of the rats had neoplastic nodules in the liver. Among the 20 male and 20 female rats treated with pyrilamine maleate mixed into the diet, two males and two females had hepatocellular carcinomas and, in addition, five males and eight females had neoplastic nodules in the liver. The incidence of liver neoplasms in the rats given pyrilamine in the drinking-water did not differ from that in the untreated controls, of which five males and three females had neoplastic nodules in the liver.

Aminopyridines↗
PubMed1995

Simultaneous determination of enalapril maleate and hydrochlorothiazide by first-derivative ultraviolet spectrophotometry and high-performance liquid chromatography.

Two methods are described for the simultaneous determination of enalapril maleate and hydrochlorothiazide in combined pharmaceutical tablets. The first method depends on first-derivative ultraviolet spectrophotometry, with zero-crossing and peak-to-base measurement methods. The first-derivative amplitudes at 224 and 260 nm were selected for the assay of enalapril maleate and hydrochlorothiazide, respectively. The second method is based on high-performance liquid chromatography on a reversed-phase column using a mobile phase of acetonitrile-water (20:80, v/v) (pH 3.8) with programmable detection at 215 and 275 nm. Both methods showed good linearity, precision and reproducibility. The proposed methods were successfully applied to the determination of these drugs in laboratory-prepared mixtures and in commercial tablets.

Angiotensin-Converting Enzyme Inhibitors↗
PubMed2006

Pharmacokinetic and bioequivalence evaluation of two formulations of 100 mg trimebutine maleate (Recutin and Polybutin) in healthy male volunteers using the LC-MS/MS method.

BACKGROUND: Trimebutine maleate is a prokinetic agent that acts directly on the smooth muscle of the GI tract. A bioequivalence (BE) study of 2 oral formulations of 100 mg trimebutine maleate (TMB) was carried out in 24 healthy male Korean volunteers according to a crossover-randomized design. METHODS: Subjects were given a single dose of 2 100 mg tablets of each formulation. The test and reference formulations were Recutin (Hutax Co., South Korea) and Polybutin (Samil Co., South Korea), respectively. Each set of tablets was administered with 240 ml of water to subjects after 10 h overnight fasting on 2 treatment days separated by a 1 week washout period. After dosing, serial blood samples were collected for a period of 36 h. Plasma was analyzed for the main metabolite of TMB, N-monodesmethyl trimebutine (nor-TMB), by a validated LC with MS/MS detection capacity for nor-TMB in the range 5-1500 ng/ml, with a lower limit of quantification (LLOQ) of 5 ng/ml. Several pharmacokinetic (PK) parameters (including AUC(t), AUC(infinity), C(max), T(max), T(1/2), and K(e)) were determined from the plasma concentrations of nor-TMB of both formulations. AUC(t), AUC(infinity), and C(max) were tested for BE after log-transformation of the data. RESULTS: No significant difference was found based on ANOVA; 90% confidence intervals (98.98%112.03% for AUC(t); 98.60%-113.20% for AUC(infinity); 90.85%-107.87% for C(max)) for the test and reference were found within KFDA acceptance range of 80-125%. CONCLUSIONS: Based on these statistical inferences, it was concluded that Recutin is bioequivalent to Polybutin and can be used interchangeably in a clinical setting.

Adult↗
PubMed2005

Tumor-necrosis-factor-related apoptosis-inducing-ligand (TRAIL)-mediated death of neurons in living human brain tissue is inhibited by flupirtine-maleate.

Neuronal damage mediated by the TRAIL-system might be involved in the pathogenesis of neuroinflammatory diseases of the central nervous system. Here we used an investigator-independent approach to quantify TRAIL-mediated death of total CNS cells and neurons in a living human brain slice culture system, a model which is much closer to the in vivo situation than dissociated cell culture. We observed dose-dependent TRAIL-mediated death of both total human CNS cells and neurons, which was prevented by flupirtine-maleate, a centrally acting analgesic drug with proposed neuroprotective properties. Our data suggest flupirtine-maleate as an orally available neuroprotective approach in the course of neuroinflammation.

Aminopyridines↗
PubMed2005

Pharmacokinetic study of trimebutine maleate in rabbit blood using in vivo microdialysis coupled to capillary electrophoresis.

In vivo microdialysis was used together with capillary electrophoresis (CE) to monitor the concentration of trimebutine maleate (TM) in rabbit blood. Dialysis probe was perfused at 3 microl/min resulting in relative recovery of 26.6+/-3.1% (n=3). After a one step sample preparation the samples were injected directly into the capillary. TM was detected on-column using UV detector at 214 nm. Separation of TM from other components in the dialysate was achieved within 15 min. Evaluation was based on the relative collected peak height (TM/IS). The response for TM in the blood dialysate was linear over the range of 0.5-100 microg/ml. The detection limit of TM in the blood dialysate was 0.1 microg/ml (S/N=3). This method has been successfully applied to the pharmacokinetic study of trimebutine maleate in rabbit blood following oral administration of 200 mg/kg. It provides a fast and simple technique for the pharmacokinetic study of TM in vivo.

Administration, Oral↗
PubMed2006

Robustness testing of a chiral NACE method for R-timolol determination in S-timolol maleate and uncertainty assessment from quantitative data.

A robustness test of a capillary electrophoresis method for the chiral separation of timolol in nonaqueous acidified media was performed. A two-level Plackett-Burman design was applied in which one qualitative and six quantitative factors were examined. Resolution, migration times and relative migration times to pyridoxine (selected as internal standard) were examined as qualitative responses to evaluate electrophoretic performance. A quantitative response, the content of R-timolol in S-timolol maleate sample, was also considered. Even though some significant factor effects were observed on the qualitative responses, it was still possible to quantify the R-timolol in the S-timolol maleate samples properly. The quantitative response was not significantly affected by the selected factors, demonstrating the robustness of the procedure. However, the use of different HDMS-beta-CD batches seemed to affect both types of responses necessitating to introduce a warning in the procedure. Since the experiments of the Plackett-Burman design can be assimilated to laboratories in an interlaboratory study, uncertainty can be evaluated using the robustness test data. The robustness test was set-up in such a way that the required variances could be estimated.

Adrenergic beta-Antagonists↗
PubMed2003

Timolol 0.5%/dorzolamide 2% fixed combination vs timolol maleate 0.5% and unoprostone 0.15% given twice daily to patients with primary open-angle glaucoma or ocular hypertension.

OBJECTIVE: To compare the efficacy and safety of timolol 0.5%/dorzolamide 2% fixed combination vs timolol maleate 0.5% and unoprostone 0.15% given twice daily. DESIGN: Prospective multicenter, randomized, double-masked, crossover comparison study. METHODS: Primary open-angle glaucoma or ocular hypertension patients were randomly assigned to one of the treatment groups for a 6-week treatment period and then crossed over to the opposite treatment. Diurnal curve testing was performed at 8:00 AM, 10:00 AM, 4:00 PM, 6:00 PM, and 8:00 PM at baseline and the end of each treatment period. The run-in medicine was timolol twice daily for 28 days. RESULTS: Thirty-two patients completed this trial. The baseline trough pressure was 24.3 +/- 3.0 mm Hg, and the diurnal curve was 23.4 +/- 3.2 mm Hg. For the fixed combination the treatment trough pressure was 20.8 +/- 4.1 mm Hg and the diurnal curve was 19.6 +/- 3.6 mm Hg, whereas timolol and unoprostone concomitant therapy showed a treatment trough pressure of 20.1 +/- 4.5 mm Hg and a diurnal pressure of 19.8 +/- 4.1 mm Hg. There was no significant difference between treatment groups at any time point, for the diurnal curve, or in the extended reduction from baseline. There was no difference between treatment groups regarding ocular and systemic unsolicited or solicited adverse events. Burning, stinging, and conjunctival hyperemia were the adverse events most noted. There were no serious adverse events during this trial. CONCLUSIONS: This study suggests that both timolol/dorzolamide 2% fixed combination and concomitant timolol maleate 0.5% and unoprostone 0.15% therapy provide similar efficacy and safety throughout the daytime diurnal curve.

Antihypertensive Agents↗
PubMed1984

Trace analysis of the antihistamines methapyrilene hydrochloride, pyrilamine maleate and triprolidine hydrochloride monohydrate in animal feed, human urine and wastewater by high-performance liquid chromatography and gas chromatography with nitrogen-phosphorus detection.

Toxicological evaluation of the antihistamines methapyrilene hydrochloride, pyrilamine maleate, and triprolidine hydrochloride monohydrate using methapyrilene hydrochloride as the positive indicator was investigated as part of a structure-activity relationship study in rats and mice. Prerequisites for the toxicological tests were the development of analytical procedures to certify the dose, homogeneity and stability of the drugs in animal feed and to monitor human urine for possible exposure and to ensure removal of the test agents from wastewater prior to its discharge into the environment. A high-performance liquid chromatographic (HPLC) system was developed using a fluorescence detector for the determination of methapyrilene hydrochloride and pyrilamine maleate in feed at levels as low as 100 ng/g and in human urine as low as 1 ng/g. An HPLC-UV procedure was developed for the determination of triprolidine hydrochloride monohydrate in feed at levels as low as 10 micrograms/g. Data concerning p-values, extraction efficiencies from feed and stability experiments in feed are presented for these antihistamines. A gas chromatographic procedure using a nitrogen-phosphorus detector was also developed for determining the three antihistamines in admixture in wastewater at levels as low as 10 ng/g.

Animal Feed↗
PubMed2003

Tegaserod maleate in the treatment of irritable bowel syndrome: a clinical review.

BACKGROUND: Approved in July 2002, tegaserod maleate is a partial 5-hydroxytryptamine 4-receptor agonist used to improve symptoms of constipation-predominant irritable bowel syndrome (IBS). The physiologic actions of tegaserod relate to its ability to stimulate gastric and intestinal motility. OBJECTIVE: This article reviews available data on the pharmacokinetic and pharmacodynamic properties and clinical efficacy of tegaserod. METHODS: Searches of MEDLINE and PubMed from 1966 to the present were conducted using the search terms tegaserod, tegaserod maleate, irritable bowel syndrome, and Rome criteria. Abstracts presented at national meetings between 1997 and 2002 were reviewed and included if perceived to be reliable and relevant. RESULTS: In clinical trials, tegaserod was associated with significantly better scores on the subject's global assessment of relief compared with placebo (P < 0.05). The absolute efficacy of tegaserod compared with placebo varied between trials and averaged 10% to 12%. Tegaserod had a good safety profile; diarrhea was the only adverse effect that occurred more often in tegaserod recipients than in placebo recipients. No electrocardiographic changes were observed at therapeutic concentrations of tegaserod. Long-term (1-year) treatment with tegaserod appeared to be well tolerated. The recommended dosage for patients aged >18 years with constipation-predominant IBS is 6 mg PO BID before meals for 4 to 6 weeks, with an additional 4 to 6 weeks of treatment if initial therapy is partially effective. CONCLUSIONS: The addition of tegaserod to the arsenal of moderately effective medication currently used in the treatment of IBS may be helpful in patients with constipation-predominant IBS. Continuous postmarketing surveillance and reporting of adverse reactions are essential to further characterize the safety profile of this new agent.

Clinical Trials as Topic↗
PubMed1994

A comparison of timolol maleate and levobunolol. Length of use per 5-ml bottle.

PURPOSE: The authors analyzed the actual length of use of commercially available 5-ml bottles of 0.5% timolol maleate (Timoptic) and 0.5% levobunolol (Betagan) among patients who routinely use topical beta-blockers (1 drop twice daily in both eyes) for glaucoma treatment. METHODS: Patients were randomized to receive two 5-ml bottles of either timolol or levobunolol in a double-blind fashion. The patients used the drops independently and the bottles in sequence. The dates were recorded when each of the two 5-ml bottles were used. Sixty patients were enrolled, 15 were excluded from the study, and the data from the remaining 45 were analyzed. RESULTS: There was a 21% greater length of use per 5-ml bottle among patients who were randomized to 0.5% timolol maleate (36.6 +/- 10.4 days) compared with 0.5% levobunolol (28.9 +/- 8.1 days) (P = 0.009). The length of use of the first bottle versus the second bottle was compared and was found not to be significantly different in either group. There was no statistical difference in intraocular pressure control among patients before and after the study. CONCLUSION: There is a markedly greater length of use of the 5-ml bottle of timolol compared with the 5-ml bottle of levobunolol. The difference is believed to be due to the configuration of the levobunolol's bottle tip and the vehicle used to deliver the drug. The data may be extrapolated to a substantial patient savings and should be considered in prescription recommendations.

Aged↗