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At least 235 records · Page 13Linked to original sources
PubMed2005

Brimonidine 0.2% vs unoprostone 0.15% both added to timolol maleate 0.5% given twice daily to patients with primary open-angle glaucoma or ocular hypertension.

PURPOSE: To compare the efficacy and safety of brimonidine 0.2% vs unoprostone 0.15%, both added to timolol maleate 0.5% each given twice daily. METHODS: In this prospective, multi-centred, double-masked, crossover comparison, patients were randomized to one treatment group for a 6-week treatment period, and then crossed over to the opposite treatment. Measurements were performed at 0800, 1000, 1600, 1800, and 2000 h at baseline and at the end of each treatment period. RESULTS: In all, 33 patients entered this trial and 29 completed. The baseline trough intraocular pressure (IOP) was 23.3+/-2.4 and the diurnal curve IOP was 22.0+/-1.3 mmHg. For the brimonidine and timolol maleate treatment group, the trough IOP was 21.6+/-3.3 and the diurnal curve IOP was 19.8+/-2.1 mmHg, while the timolol and unoprostone treatment showed a trough IOP of 20.9+/-3.8 and a diurnal curve IOP of 19.3+/-2.4 mmHg. There was no significant difference between treatment groups at any time point for the diurnal curve, or in the reduction from baseline (P>0.05). Both treatments failed to statistically reduce the IOP from baseline at 1800 h. There was no difference between treatment groups regarding ocular and systemic unsolicited adverse events, but patients admitted to more dryness (P=0.02) and burning upon instillation (P<0.0001) with unoprostone by survey. CONCLUSION: Brimonidine 0.2% or unoprostone 0.15% added to timolol maleate 0.5% provide similar efficacy and safety throughout the daytime diurnal curve.

Antihypertensive Agents↗
PubMed1998

Stability of alprazolam, chloroquine phosphate, cisapride, enalapril maleate, and hydralazine hydrochloride in extemporaneously compounded oral liquids.

The stability of five drugs commonly prescribed for use in oral liquid dosage forms but not commercially available as such was studied. Alprazolam 1 mg/mL, chloroquine phosphate 15 mg/mL, cisapride 1 mg/mL, enalapril maleate 1 mg/mL, and hydralazine hydrochloride 4 mg/mL were each prepared in a 1:1 mixture of Ora-Sweet and Ora-Plus (Paddock Laboratories), a 1:1 mixture of Ora-Sweet SF and Ora-Plus, and cherry syrup and placed in 120-mL amber clear polyethylene terephthalate bottles. Three bottles of each liquid were stored at 5 degrees C and three at 25 degrees C, all in the dark. Samples were taken initially and at various times up to 60 days for analysis by high-performance liquid chromatography and assessment of appearance and odor; pH was measured. A mean of at least 91% of the initial drug concentration was retained for 60 days in the alprazolam, chloroquine phosphate, cisapride, and enalapril maleate liquids. The hydralazine hydrochloride liquids retained more than 90% of the initial concentration for only one day at 5 degrees C when prepared with Ora-Sweet-Ora-Plus and two days when prepared with Ora-Sweet SF-Ora-Plus and for less than a day in these preparations at 25 degrees C and in cherry syrup at 5 and 25 degrees C. No substantial changes in the appearance, odor, or pH of any liquid were observed. Alprazolam 1 mg/mL, chloroquine phosphate 15 mg/mL, cisapride 1 mg/mL, and enalapril maleate 1 mg/mL were stable in three extemporaneously compounded oral liquids for 60 days at 5 and 25 degrees C; hydralazine hydrochloride 4 mg/mL was stable at 5 degrees C for one day in Ora-Sweet-Ora Plus and for two days in Ora-Sweet SF-Ora-Plus.

Alprazolam↗
PubMed1992

Antitumor activity of 1,4-bis (2'-chloroethyl)-1,4-diazabicyclo-[2.2.1] heptane dimaleate (Dabis Maleate) in M5076 and its subline resistant to cyclophosphamide M5/CTX.

We investigated the antitumoral activity of Dabis Maleate given on different dosage schedules and as continuous infusion in a murine reticular cell sarcoma M5076 (M5) and in a subline made resistant to cyclophosphamide and other nitrogen mustards (M5/CTX). The therapeutic index of Dabis Maleate was clearly better when the drug was given as a continuous 72-h infusion. Dabis Maleate appeared non-cross-resistant to cyclophosphamide and this property renders it interesting for further clinical development.

Animals↗
PubMed2000

Comparison of the effects of 0.5% timolol maleate, 2% carteolol hydrochloride, and 0.3% metipranolol on intraocular pressure and perimetry findings and evaluation of their ocular and systemic effects.

PURPOSE: To compare the effects of 0.5% timolol maleate, 2% carteolol, and 0.3% metipranolol on intraocular pressure (IOP) in 45 patients with primary open-angle glaucoma (POAG) and ocular hypertension. A secondary goal of this study was to evaluate the ocular and systemic side effects of these medications. METHODS: Measurements of IOP were taken at baseline (pretreatment) and 2, 6, and 12 hours after instillation on treatment days 15, 30, 60, and 90. Mean sensitivity (MS) and mean defect (MD) values of perimetry before and after treatment and the effects of the three beta blockers on serum lipid profiles were determined. Ocular and systemic side effects were recorded. RESULTS: The most prominent IOP lowering effect was noted with metipranolol at 2 and 6 hours on day 15, and with timolol maleate at 12 hours on day 15 and at all hours of the subsequent days on which measurements were taken. Timolol maleate produced a significant decrease in IOP at 12 hours on day 15 compared with carteolol. There was not a statistically significant difference between the MS and MD values on perimetry before and after treatment for any treatment. There was a statistically significant decrease in levels of total cholesterol and high-density lipoprotein (HDL) cholesterol and a significant increase in triglyceride levels; these changes were observed for all treatments. CONCLUSION: The effects of the three medications were not statistically different from each other in terms of IOP reduction and visual field changes. Careful monitoring of blood lipid levels is necessary with long-term treatment with beta blockers, because these agents reduced serum levels of HDL and total cholesterol while increasing triglycerides. Such changes in lipid levels could lead to increased incidence of complications, particularly in patients with atherosclerosis or coronary heart disease.

Adrenergic beta-Antagonists↗
PubMed2003

Bis(2-aminopyridinium) maleate.

Two cyclic eight-membered hydrogen-bonded rings exist in the title compound, 2C(5)H(7)N(2)(+) x C(4)H(2)O(4)(2-), involving the 2-aminopyridinium and maleate ions. The dihedral angle between the two pyridinium rings hydrogen bonded to the maleate ion is 74.80 (4) degrees. The maleate anion lies on a twofold axis and is linked to the pyridinium cations by intermolecular N-H.O hydrogen bonds. The heterocycle is fully protonated, which enables amino-imino tautomerization.

Journal Article↗
PubMed1982

Enalapril maleate and a lysine analogue (MK-521): disposition in man.

1 The disposition of two angiotensin converting-enzyme inhibitor drugs was studied in normal volunteers. One drug was enalapril maleate (MK-421), which requires in vivo esterolysis to yield active inhibitor (MK-422). The other was a lysine analogue of MK-422 (MK-521), which requires no bioactivation. 2 Absorption of enalapril maleate (10 mg, p.o.) was rapid, with peak serum concentrations of enalapril observed 0.5-1.5 h after administration. Based upon urinary recovery of total drug (enalapril plus MK-422), absorption was at least 61%. Bioactivation appeared to be largely post-absorptive. From the ratio of MK-422 to total drug in urine, the minimum extent of bioactivation was estimated at 0.7. 3 A similar dose of MK-521 was absorbed more slowly, reaching peak serum concentrations 6-8 h following drug administration. Minimum absorption, based upon urinary recovery, was 29%. 4 Serum concentration v time profiles for both drugs were polyphasic and exhibited prolonged terminal phases. 5 Recovery in urine and faeces of administered enalapril maleate (intact and as MK-422) was 94%. Recovery of MK-521 was 97%. These results indicate lack of significant metabolism of these agents, apart from the bioactivation of enalapril.

Angiotensin-Converting Enzyme Inhibitors↗
PubMed1987

The effect of topical dimethindene maleate on weal reactions.

The topical effect of the histamine H1-receptor antagonist dimethindene maleate on the wealing response to intradermal histamine, compound 48/80 and house dust mite antigen was studied in 16 subjects using a double-blind procedure. The mean reduction in weal area +/- s.e. mean was 44% +/- 13%, 43% +/- 13% and 31% +/- 13% for histamine, 48/80 and antigen respectively. We conclude that dimethindene maleate is a moderately potent H1-receptor antagonist, and that the inhibition of the 48/80 and house dust mite induced weals is accounted for by the antihistaminic effect of dimethindene maleate.

Adult↗
PubMed1990

Effect-kinetic characterization of dimethindene maleate following oral administration (Fenistil, Tropfen).

Dimethindene maleate is a well known H1-receptor antagonist with strong affinity to the H1-receptor. In order to evaluate the time course of its activity, dimethindene maleate was investigated in a histamine provocation model in man. Eight healthy male volunteers were treated either with 4 mg dimethindene maleate using a commercially available solution (Fenistile, Tropfen) or an identically appearing placebo solution (po) following a double-blind, crossover study design. Intracutaneous histamine injections were administered at -1, 2, 5, 14, 17, 20, 23, 26 and 29 h following drug administration. Areas of flares and weals were measured 5, 10, 20, and 30 min following histamine provocation. A strong inhibition of the development of flares and weals was observed to be more pronounced in flares than in weals. Baseline adjusted areas under the curve differ statistically significantly following verum and placebo treatment conditions (P = 0.0028). According to the time schedule of the study maximal effects were observed at time point 5 h. The mean residence times of the inhibitory effects were calculated to be congruent to 13 h compared to the mean residence times of dimethindene blood levels of approximately 8 h indicating a non-linear relationship between blood level and effect.

Administration, Oral↗
PubMed1988

Effects of a beta-blocking agent, timolol maleate, on saliva in healthy volunteers.

The effects of timolol maleate on the secretion and composition of human saliva were studied in vivo. Eight healthy volunteers received orally 10 mg timolol maleate. Stimulated parotid saliva samples, resting whole saliva samples, and blood samples were collected immediately before and four times after the drug intake at intervals of 1 h. The levels of total protein, lysozyme, IgA, IgG and IgM, salivary peroxidase, myeloperoxidase, lactoferrin, amylase, thiocyanate (SCN-), and hypothiocyanite (OSCN-) were analyzed from saliva samples. Drug levels were measured both from parotid saliva and blood samples. Results were compared to the analyses of the samples collected in a similar way but without administration of any drugs. Decreased levels of total protein, lactoferrin, amylase, and salivary peroxidase were observed in parotid saliva after a single oral dose of timolol maleate. No such decrease was found in lysozyme, myeloperoxidase, SCN-, OSCN-, or immunoglobulins. Salivary flow rate was not significantly changed after drug intake. The results suggest that the beta-blocking drug may cause qualitative changes in the composition of saliva by inhibiting the synthesis and/or release of acinar proteins.

Amylases↗
PubMed1979

Timolol maleate in treatment of open angle glaucoma.

The effect of Timolol maleate on the intraocular pressure in open angle glaucoma has been examined in 37 patients, of these simple glaucoma in 26 (48 eyes), capsular glaucoma in 9 (14 eyes) and chronic secondary glaucoma in 2 patients (2 eyes). These cases constituded a group which was relatively difficult to manage. The average pressure reduction caused by Timolol maleate alone was about 23%. In 18 patients the intraocular pressure was adequately controlled on Timolol as the only drug and in 10 on additional drug therapy. Five patients failed on drug treatment, and the remaining four failed on one eye while the fellow eye was well regulated. Tonography indicates that the effect is caused by a reduction of the aqueous humour production. Side effects of locally applied Timolol maleate have not been observed. This drug may be the drug of choice in many instances.

Adult↗
PubMedDate not supplied

Comparison of efficacy and tolerability between two gel-forming timolol maleate ophthalmic solutions in patients with glaucoma or ocular hypertension.

PURPOSE: To compare two gel-forming timolol maleate ophthalmic solutions, Timoptol XE and Lizmon TG, in regard to efficacy and tolerability in patients with glaucoma or ocular hypertension by means of a patient-masked prospective randomized crossover study. SUBJECTS AND METHODS: A total of 37 patients with glaucoma or ocular hypertension under treatment with antiglaucoma ophthalmic solutions including 0.5% twice-daily timolol maleate participated in this study. Only timolol maleate was withdrawn and either Timoptol XE or Lizmon TG was randomly allocated. After instillation for 1 month, the other ophthalmic solution was subsequently instilled for another month. Routine ophthalmic examination including slit-lamp examination and intraocular pressure (IOP) monitoring was conducted before instillation of gel-forming ophthalmic solutions and just after completing the instillation of each ophthalmic solution. Patient questionnaire surveys were also performed just after completing the instillation of each ophthalmic solution. RESULTS: Mean IOP, just before the withdrawal of timolol ophthalmic solution, was 16.4 +/- 2.9 mm Hg. At the end of Timoptol XE or Lizmon TG instillation, mean IOPs were 16.3 +/- 2.5 or 16.3 +/- 3.0 mm Hg, respectively. The results of the questionnaire survey showed no significant difference between Timoptol XE and Lizmon TG in regard to all survey items. Twenty-nine patients (78.4%) preferred to use gel-forming timolol solutions rather than twice-daily timolol ophthalmic solution. The presence of concurrently used ophthalmic solutions did not effect the incidences of subjective symptoms. The incidences of objective adverse effects were not significantly different between two gel-forming timolol ophthalmic solutions. CONCLUSION: Both gel-forming timolol ophthalmic solutions could be good choices for glaucoma treatment.

Adult↗
PubMed2005

Airway closure after antigen challenge in cynomolgus monkeys: effect of the histamine H1 receptor antagonist, chlorpheniramine maleate.

BACKGROUND: Airway closure is frequently observed in human asthma. However, limited information exists on the factors that cause this condition. In this study, an allergic cynomolgus monkey model was used to characterize the condition of airway closure and assess the contribution of histamine H1 receptors to this response. METHODS: Oscillatory lung mechanics, arterial blood gases during ventilation on 100% O2 and functional residual capacity (FRC) assessed by helium dilution were measured before and then 10 min and 24 h after Ascaris aerosol challenge in 12 male Ascaris-sensitive cynomolgus monkeys. The monkeys were pretreated with intravenous saline or chlorpheniramine maleate (0.3 mg/kg) in a randomized crossover design. RESULTS: Ascaris challenge produced a large increase in airway resistance, an increase in lung tissue damping (G) that measures ventilation inhomogeneity in the lung, a reduction in arterial oxygen tension (PaO2) during ventilation on 100% O2 and a reduction in FRC. These effects were seen 10 min after the Ascaris challenge, but by 24 h, these parameters had returned close to the baseline values. Chlorpheniramine maleate (0.3 mg/kg, i.v.) produced a 12-fold shift in the histamine bronchoconstrictor dose-response curve. Pretreatment of monkeys with chlorpheniramine maleate (0.3 mg/kg, i.v.) attenuated the increase in airway resistance induced by Ascaris challenge, but had only a small effect on the increase in G and the reductions in PaO2 and FRC after antigen. CONCLUSIONS: These results demonstrate that airway closure occurs immediately after the antigen challenge in allergic cynomolgus monkeys and that histamine H1 receptors contribute very minimally to this response.

Airway Obstruction↗
PubMed1979

The effects of ergonovine maleate on coronary arterial size.

Changes in coronary arterial size due to ergonovine maleate are described and quantitated in 90 patients--18 with typical angina pectoris, 56 with atypical chest pain, nine with variant angina pectoris, and seven heart transplant (allograft) recipients. We observed two angiographic changes in the diameter of coronary arteries: 1) spasm, which was characterized by occlusion or marked (greater than 85%) focal or diffuse vessel narrowing, or 2) relatively mild and diffuse vessel narrowing, which was interpreted as the normal pharmacologic response to the drug. Serial bolus injections of 0.05 mg, 0.10 mg and 0.25 mg of ergonovine maleate produced diffuse narrowing of the diameter of coronary arteries of 10 +/- 1.5%, 16 +/- 1.4% and 20 +/- 1.3% (mean +/- SEM), respectively, in the 72 patients with anginal syndromes who did not develop coronary spasm. The degree of coronary arterial narrowing was the same in heart transplant recipients and in patients with normally innervated hearts who did not develop coronary spasm. We believe the normal pharmacologic response to ergonovine maleate was due to a direct vasoconstrictor action of the drug; this action was independent of neural control extrinsic to the heart.

Adult↗
PubMedDate not supplied

Perhexiline maleate in the treatment of angina pectoris in patients awaiting coronary artery bypass surgery.

Twenty-five patients with angina pectoris due to coronary artery disease who had not responded to other medical therapy and on the waiting list for coronary bypass surgery were treated over a period of 4 weeks with perhexiline maleate (100 mg to 400 mg/day) in addition to their other therapy. There was an 80% reduction in the average number of both anginal attacks and nitroglycerin requirement when the pre-treatment week and the 4th week of perhexiline maleate therapy were compared (p less than 0.0001). Six of the patients had no anginal attacks at all and did not require sublingual nitro glycerin tablets during the 4th week of perhexiline maleate therapy.

Aged↗
PubMed2003

Rapid and sensitive HPLC method for the simultaneous determination of dorzolamide hydrochloride and timolol maleate in eye drops with diode-array and UV detection.

A rapid and sensitive HPLC method has been developed for the simultaneous determination of dorzolamide hydrochloride and timolol maleate. The drugs were monitored with a diode-array detector at two fixed wavelengths (lambda = 250.0 nm for dorzolamide hydrochloride and 300.0 nm for timolol maleate). Liquid chromatography was performed on a RP-YMC pack ODS A-132 C18 (5 microm, 15 cm x 6.0 mm) column and the mobile phase consisted of an acetonitrile: phosphate buffer (pH 2.5): methanol (5:85:10 v/v/v) mix and a flow rate of 1.2 ml x min(-1). The linearity of the method ranged between 4.0-45.0 microg x ml(-1) for dorzolamide hydrochloride and and 2.0-20.6 microg x ml(-1) for timolol maleate in binary mixture. The procedure was successfully applied to the determination of these compounds in pharmaceutical preparations and gave a high recovery, good accuracy and precision without any interference by the excipients.

Adrenergic beta-Antagonists↗
PubMed1991

[Methylergometrine Maleate Reference Standard (Control 891) of National Institute of Hygienic Sciences].

The raw material of methylergometrine maleate was examined for the preparation of the "Methylergometrine Maleate Reference Standard". Analytical data obtained were as follows: melting point, 181.7 degrees C; ultraviolet spectrum, lambda max = 313 nm; absorbance, E1%1cm (313 nm) = 181.3; infrared spectrum, 3406, 2962, 2928, 1645, 1574 cm-1; thin-layer chromatography, 6 impurities were detected; high-performance liquid chromatography, no impurities were detected; loss on drying, 0.02%; optical rotation, [alpha]20D = + 44.04 degrees; assay, 99.5% against Ergometrine Maleate Reference Standard (Control 755). Based on the above results, this raw material was authorized to be the Reference Standard of the National Institute of Hygienic Sciences.

Chromatography, High Pressure Liquid↗
PubMed2006

Promoting effect of borneol on the permeability of puerarin eye drops and timolol maleate eye drops through the cornea in vitro.

Studies on the influence of borneol on the penetration of puerarin eye drops and timolol maleate eye drops through the cornea, and evaluation of the ocular irritability were conducted to provide a theoretical basis for the application of borneol in enhancing corneal permeability. The cornea penetrative experiment in vitro was conducted to observe the quantitative change of puerarin and timolol maleate penetrated through the cornea after administering different dosages of borneol. The corneal hydration level and blinking frequency were recorded as irritability indexes in vitro and in vivo. The steady-flow J of high, middle and low dosage groups of puerarin eye drops with borneol were increased by 49%, 32%, 5% respectively, and permeability parameter Kp increased by 49%, 32%, 5% respectively, as compared to that of the control group. The steady-flow J of high dosage group of timolol maleate eye drops with borneol was increased by 5%; middle and low dosage groups with borneol were decreased by 6%, 3% respectively. The permeability parameter Kp of high dosage group increased by 5%, while middle and low dosage groups with borneol were decreased by 6%, 3% respectively, as compared to that of the control group. Evaluation showed no ocular irritability caused by borneol. The results of this study suggest that the promoting effect of borneol on the permeability of drugs through the cornea in vitro is selective, which indicates that borneol has the potential to be used as an ophthalmic penetration enhancer.

Adrenergic beta-Antagonists↗
PubMedDate not supplied

[Effect of treatment with enalapril maleate on the levels of circulating catecholamines, beta endorphins, prostaglandins, and concentration of sodium in erythrocytes in patients with essential hypertension].

An effect of enalapril maleate on the activity of renin-angiotensin-aldosterone system and sympathetic reactivity, erythrocyte prostaglandin and sodium levels as well as blood beta-endorphin was investigated in 28 patients with the essential arterial blood hypertension. It was found that enalapril maleate significantly increased plasma renin activity, decreased plasma norepinephrine and its 24-hour excretion, and decreased erythrocyte beta-endorphin and sodium levels. Blood epinephrine and aldosterone levels and their daily excretion remained unchanged similarly to prostaglandins. The above results suggest that a decrease in sympathetic system activity and intracellular sodium concentration may play a role in the hypotensive action of enalapril maleate related to the inhibition of angiotensin II formation.

Adult↗