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At least 757 records · Page 42Linked to original sources
PubMed1982

[General pharmacology of lisuride hydrogen maleate--actions on isolated organs, especially on smooth muscles].

Pharmacological actions of lisuride hydrogen maleate (lisuride) were studied by using isolated organs. 1) Lisuride at 2.2 microM exerted a negative chronotropic effect on guinea-pig atria, the effect being antagonized completely by 2.9 microM sulpiride. 2) alpha-Adrenolytic action of lisuride was observed in the rat vas deferens and beta-adrenolytic action in the rabbit trachea, respectively. The former (ID50 = 64 nM) was potent and equivalent to that of phentolamine, whereas the latter (ID50 = 26 microM) was only 1/30 as compared to that of propranolol. 3) Anti-5-hydroxytryptamine action (ID50 = 11 nM) was detected in the rat stomach and anti-histamine (ID50 = 15 nM) in the guinea-pig ileum, respectively. In these respective activities, lisuride was equipotent to methysergide and diphenhydramine. 4) Lisuride showed a spasmodic action, which may be categolized as an ergot alkaloid action, on the guinea-pig ileum and on rabbit renal artery. A weak positive inotropic action of lisuride was also observed in guinea-pig atria. In the rat uterus, however, no uterotonic action of lisuride was detected. It is concluded that, in addition to its known effects on the central nervous system, lisuride possesses potent peripheral anti-5-hydroxytryptamine and anti-histamine activities.

Animals↗
PubMed1982

[Effects of trimebutine maleate (TM-906) on the spontaneous contraction of the isolated guinea pig stomach].

Effects of trimebutine maleate (TM-906) on the spontaneous contraction were investigated in the isolated circular smooth muscle of the antrum region of the guinea pig stomach. TM-906 dose-dependently reduced the amplitude of the regular spontaneous contraction without any marked change in its frequency and basal tension. This effect of TM-906 was also observed in the presence of phentolamine, propranolol, atropine, and tetrodotoxin. However, the inhibitory effect of TM-906 was overcome by increasing the extracellular concentration of CaCl2. On the other hand, in preparations which exhibited irregular spontaneous contraction, TM-906 regularized it, and spontaneous contraction with regular frequency and amplitude was elicited. In addition, this regularizing effect of TM-906 was also observed in the presence of atropine and tetrodotoxin. It was concluded that TM-906 has dual effects on the spontaneous contraction, reducing the amplitude of regular contraction and regularizing the irregular contraction. These effects of TM-906 may be attributed to the direct action on the smooth muscle.

Animals↗
PubMed1981

The importance of ergonovine maleate provocation in the diagnosis of coronary artery spasm. A case report.

Ergonovine maleate produced transient vasospastic occlusion of the entire left anterior descending coronary artery in a young woman with atypical angina pectoris and normal coronary arteries. Electrocardiographic evidence of extensive anterior subendocardial ischaemia persisted for days after an episode of spontaneous pain, suggesting that the patient was at risk of developing completed infarction due to coronary spasm.

Adult↗
PubMed1981

Determination of blood pressure by indirect methods in dogs given acetylpromazine maleate.

This study was designed to monitor and compare indirect blood pressures by two methods (ultrasonic Doppler and photoelectric) after intravenous acetylpromazine maleate at three different doses (0.11, 0.55, and 1.10 mg/kg). Sixteen unanesthetized dogs were placed in right lateral recumbency and pressures estimated from the left hind leg at two preinjection times and at 3, 15, 60 and 120 minutes postinjection. This procedure was followed for each dog for each of the three doses. Preinjection ultrasonic mean values and standard deviations were similar to published values. Photoelectric systolic pressures were lower and diastolic pressures higher than ultrasonic systolic and diastolic pressures. The decrease in blood pressure was detected by both methods. Neither method revealed a dose related response.

Acepromazine↗
PubMed1980

Inhibitory effect of lidoflazine on contractions of isolated canine coronary arteries caused by norepinephrine, 5-hydroxytryptamine, high potassium, anoxia and ergonovine maleate.

Experiments were performed on isolated coronary arteries to determine whether or not lidoflazine, an agent reported to be beneficial in the treatment of angina pectoris, is effective in antagonizing coronary vasoconstriction. Segments of canine circumflex and right coronary arteries were suspended in organ chambers filled with aerated Krebs-Henseleit solution (37 degrees C) for continuous isometric tension recordings. Dose-dependent contractions were obtained with norepinephrine (in presence of propranolol) and 5-hydroxytryptamine; these contractile responses were antagonized by phentolamine and methysergide, respectively. Lidoflazine caused long-lasting, and dose-dependent inhibition of the responses to both norepinephrine and 5-hydroxytryptamine. High K+ solution (30 mM) caused sustained contraction of the coronary segments; these responses were depressed in a dose-dependent manner by lidoflazine. Lidoflazine slightly augmented relaxations caused by adenosine. Addition of Ca++ to the bath solution partially reversed the inhibitory effect of lidoflazine, which indicates that the compounds acts by inhibiting the influx of extracellular Ca++. Segments incubated in solution containing 20 mM K+ and subjected to anoxia exhibited transient contractions which were inhibited by lidoflazine. Ergonovine maleate caused contractures of the coronary arteries which also were antagonized in a dose-dependent manner by lidoflazine. These experiments demonstrate the ability of lidoflazine to counteract contractions of coronary vascular smooth muscles caused by factors which may be involved in the etiology of coronary vasospasm.

Animals↗
PubMed1980

[Preliminary study of acidification of the pH of the aqueous humor in rats treated with timolol maleate].

The Authors have studied in a homogeneous group of rabbits the variations of intraocular pressure and of aqueous humour pH caused by instillation of timolol maleate at different concentrations. In the animals treated with drug concentration of 0,25% and 0,5% a constant reduction of IOP has been observed in comparison with controls, associated to acidification of aqueous humour: no evidence of this correlation it seems to be at low doses of timolol. Further studies are in course to indicate an eventual action of intermediate substances in the mechanism of IOP depression caused by timolol.

Acid-Base Equilibrium↗
PubMed1995

Stimulatory effect of perhexiline maleate on the basal and LHRH-stimulated luteinizing hormone release from rat pituitary cell aggregates in vitro.

Perhexiline maleate (PM) is an anti-anginal agent of amphiphilic character involved in lipidosis disorders. Experiments were carried out to study PM action on LH release from rat anterior pituitary cell aggregates. PM caused significant and dose-dependent increases of basal LH release when the aggregates had been previously treated with PM for 20 min, then incubated for 30 min with the same concentration of drug after renewal of the culture medium. The increases of basal LH secretion induced by PM were 69% (p < 0.001) at a concentration of 10(-7)M, 130% (p < 0.001) at a concentration of 10(-5)M and 250% (p < 0.001) at a concentration of 10(-4)M. PM also increased the LHRH-stimulated LH release by 25.5% (p < 0.05) at a concentration of 10(-5)M and by 74.5% (p < 0.01) at the concentration of 10(-4)M. The results showed that PM was more potent on basal LH release than on LH stimulated by LHRH. The mechanism of this action remains unclear. It may be due to the lipidosis property of the drug.

Animals↗
PubMed1994

Cardiac effects of the novel pyridazinone derivative 6-[4-[2-[3-(5-chloro-2-cyanophenoxy)-2-hydroxypropylamino]- 2- methylpropylamino]phenyl]-4,5-dihydro-5-methyl-3(2H) pyridazinone monoethyl maleate and its metabolite in isolated heart preparations of guinea pigs and dogs.

The cardiovascular effects of 6-[4-[2-[3-(5-chloro-2-cyanophenoxy)-2- hydroxypropylamino]-2-methylpropylamino]phenyl]-4,5-dihydro- 5-methyl-3(2H) pyridazinone monoethyl maleate (salt) (TZC-5665, CAS 114856-47-2) and its main metabolite in human, M-2, were investigated in isolated atrial and ventricular muscles of guinea pigs and dogs, in guinea pig atrial and right ventricular papillary muscles. TZC-5665 showed negative chronotropic and inotropic effects, whereas M-2 showed a potent positive inotropic effect with a slight positive chronotropic effect. The positive inotropic effect of M-2 was not modified by phentolamine, propranolol and cimetidine, but completely depressed by carbachol. In blood-perfused dog heart preparations, M-2 increased the contractile force and coronary blood flow of paced papillary muscles and sinus rate. Although TZC-5665 scarcely affected the contractile force and sinus rate, it increased coronary blood flow. TZC-5665 scarcely affected atrio-ventricular (AV) conduction time, whereas M-2 slightly shortened AV conduction time. The rate of ventricular automaticity was slightly increased by M-2, but suppressed by TZC-5665 at higher doses. TZC-5665 showed a non-selective beta-adrenoceptor blocking activity comparable to that of propranolol in guinea-pig atrial and tracheal preparations. In enzyme preparations, TZC-5665 and M-2 were more potent and selective inhibitors of phosphodiesterase (PDE) III than milrinone. Combination of beta-adrenoceptor blocking effect of TZC-5665 and positive inotropic effect of M-2 could be useful in the treatment of congestive heart failure by mutual prevention of undesirable effects.

Adrenergic beta-Antagonists↗
PubMedDate not supplied

Effects of enalapril maleate on heart rate variability: a pilot study.

The effects of enalapril maleate on heart rate variability, an indicator of cardiac autonomic function, were evaluated by nonspectral analysis in 12 patients with standard deviation in the R-R interval for each 5-minute period for 24 hours (SDANN) of 80 msec or less. A 24-hour electrocardiogram was recorded before treatment and after 2 weeks of treatment with enalapril. No significant difference was observed in the mean R-R interval on 24-hour electrocardiography between the pretreatment and the posttreatment periods (824 +/- 84 msec vs 834 +/- 83 msec). The SDANN increased significantly (P < 0.01) between the pretreatment period (62.8 +/- 13.7 msec) and the posttreatment period (87.1 +/- 31.2 msec), as did the standard deviation of the R-R interval during the two monitoring periods (P < 0.001). However, no significant difference was observed in the mean value of the standard deviations of the R-R interval for 5 minutes; the proportion of adjacent R-Rs with a difference of more than 50 msec; or the root-mean square of the difference in successive R-Rs in the pretreatment period as compared with the posttreatment period. Causal blood pressure at rest decreased significantly (P < 0.05) after treatment with enalapril (124 +/- 17/66 +/- 7 mmHg) as compared with the pretreatment period (140 +/- 24/75 +/- 13 mmHg). Enalapril may be useful for maintaining normal autonomic nerve activity, preventing sudden cardiac death, and enhancing quality of life in our stressful society.

Aged↗
PubMed1993

[Value of the methylergometrin maleate test in recurrent cardio-circulatory arrests].

A 56-year-old man, with no particular past history, sustained two cardio-circulatory arrests preceded by constrictive chest pain. Coronary arteriography was normal during etiological investigations. The methylergometrine maleate (Méthergin (tm)) test enabled the diagnosis of severe spastic angina and guided appropriate management of this patient.

Angina Pectoris, Variant↗
PubMed1995

Imidapril hydrochloride in essential hypertension: a double-blind comparative study using enalapril maleate as a control.

OBJECTIVE: To assess the value of using imidapril hydrochloride (ACE/TA-6366), a long-acting angiotensin converting enzyme (ACE) inhibitor developed in Japan, to treat patients with essential hypertension. PATIENTS AND METHODS: A double-blind, comparative, phase III study was carried out using enalapril maleate as a control, with a 4-week observation period and a 12-week treatment period. Both drugs were started at a dose of 5 mg once a day, increasing to 10 mg in patients whose antihypertensive response was insufficient after 4 weeks. The study included 231 outpatients aged 30-74 years; of these, 108 in the imidapril group and 115 in the enalapril group were assessed. There were no differences in background factors between groups. RESULTS: An adequate antihypertensive effect was observed in 71.3% (77/108) in the imidapril group in in 66.1% (76/115) in the enalapril group, with no significant difference between groups. The pulse rate was unchanged in both groups. The drug had no adverse effects in 86.1% (93/108) of the imidapril group and 79.1% (91/115) of the enalapril group, with no significant difference between groups. Adverse drug effects were observed din 5.6% (6/108) of the imidapril group and 12.2% (14/115) of the enalapril group. Cough was the most frequent side effect, reported in 0.9% (1/108) of the imidapril group and 7.0% (8/115) of the enalapril group. Other side effects were reported in 4.6% (5/108) of the imidapril group and 5.2% (6/115) of the enalapril group. Abnormal laboratory values were observed in 3.7% (4/108) of the imidapril group and 0.9% (1/115) of the enalapril group. CONCLUSIONS: Imidapril showed excellent clinical efficacy and safety compared to enalapril. The low incidence of cough is of particular interest.

Adult↗
PubMed1977

[Hypoglycemia in 2 patients treated with perhexiline maleate].

Hypoglycaemia occurred in two patients treated with perhexiline maleate. The responsibility of the medication is discussed in each case. Blood insulin levels were increased. Blood perhexiline levels decreased very rapidly in the first patient, though much more slowly in the second.

Aged↗
PubMed1996

Inhibition of lipid hydroperoxidation of low density lipoprotein by the Ca(2+)-channel and alpha 1-adrenoceptor antagonist monatepil maleate.

The antioxidative effect of monatepil maleate (CAS 103379-03-9, AJ-2615), a new antihypertensive agent, was investigated by measuring its ability to inhibit copper-induced lipid hydroperoxidation of low density lipoprotein (LDL) and was compared with those of diltiazem (Ca(2+)-channel antagonist), prazosin (alpha 1-adrenoceptor antagonist), and probucol. The concentration of AJ-2615 required to inhibit copper-induced lipid hydroperoxidation of LDL by 50% (IC50) was 28 mumol/l. The IC50 values for diltiazem, prazosin, and probucol were > 1 mmol/l, > 1 mmol/l, and 17 mumol/l, respectively. These results indicate that AJ-2615 has the same potent antioxidative effect as probucol and suggest that a previously reported ability of AJ-2615 to inhibit the progression of atherosclerosis may be due to this antioxidative property. In addition, the dihydrodibenzothiepine ring of AJ-2615 may have an antioxidative functions.

Adrenergic alpha-1 Receptor Antagonists↗
PubMed1996

Efficacy of intranasally applied dimethindene maleate solution as spray in adult volunteers with symptoms of seasonal allergic rhinitis in the Vienna challenge chamber.

Twelve asymptomatic subjects (4 female, 8 male), being allergic to grass pollen proved by positive anamnesis, positive Prick-test and positive nasal provocation test, were challenged under controlled conditions with purified airborne grass pollen of Dactylis glomerata in the Vienna Challenge Chamber (VCC), located at the Universitätsklinik für Hals-Nasen-Ohrenheilkunde, Allgemeines Krankenhaus (AKH), der Stadt Wien, Vienna (Austria) by means of a double-blind, randomised, cross-over design, with 2 weeks wash-out periods between. Efficacy and safety of 2 concentrations of dimethindene (dimethindene maleate; DMM, CAS 3614-69-5, Fenistil resp. Foristal) 0.025% DMM, 0.1% DMM) were tested vs placebo as negative control and vs 0.1% azelastine as positive control, as topical nasal sprays. The tested nasal sprays were applied as single doses in the morning (2 puffs = 0.28 ml of the respective solution) to each nostril 15 min before the start of the 4 h lasting provocation procedure in the VCC, thus representing a total daily dose of 0.14 mg resp. 0.56 mg DMM and 0.56 mg azelastine, respectively. Compared to placebo, the objective variables nasal flow (150 Pa., measured by active anterior rhinomanometry) and nasal secretion (g), showed similar onset of antiobstructive and antisecretory effects in the nose after 0.1% DMM and 0.1% azelastine, respectively. The same applied for the subjective nasal symptom complex and for nasal symptom scores, evaluated by Visual Analog Scale (VAS): Time curves showed statistically significant and clinically relevant superiority of 0.1% DMM and 0.1% azelastine vs placebo, during the 4 h lasting provocation period. 0.025% DMM was not significantly different from placebo. No systemic adverse events were reported after the 4 tested preparations. Only a total of 3 subjects reported very slight local irritations (1 subject after placebo, 1 subject after 0.025% DMM and 1 subject after 0.1% azelastine). However, after 0.1% DMM no local adverse events were reported. It is concluded from this study that 0.1% DMM as nasal spray, is an efficient and safe galenical formulation for nasal spray application for patients suffering from seasonal allergic rhinitis (SAR).

Administration, Intranasal↗
PubMed1977

[Hepatic overload of gangliosides after perhexiline maleate. Morphological and biochemical course (author's transl)].

A 72 years old man treated with perhexiline maleate (400 mg during 15 months) complained of skin rash, sensitive neuropathy, liver damage and mild renal insufficiency. Clinical status improved when the treatment was stopped, but liver size and renal status remained inchanged. Liver biopsy were performed at 0,6 and 15 months after the end of treatment. Inflammation and hepatocyte necrosis, seen on the first specimen, disappeared latter. Steatosis and voluminous, swollen, foamy liver seen were present in the three biopsies. Sclerosis had increased in the last one in spite of treatment arrest. Histochemical study exhibited liver storage of triglycerides, fatty acids, phospholipids, and gangliosides. Cytoplasmic glycogen was increased and some nuclei were glycogenated. Enzymatic pattern suggests a minor form of type I glycogen storage or increased neoglycogenesis. Perhexiline relation to this complex liver storage is discussed.

Aged↗
PubMed1997

Persistent penile prolapse associated with acute blood loss and acepromazine maleate administration in a horse.

Prolonged penile prolapse in horses has been reported in association with administration of phenothiazine tranquilizers, trauma, neuropathies, severe general debilitation or exhaustion, starvation, rabies, herpes myeloencephalitis, equine infectious anemia, and purpura hemorrhagica. A 5-year-old gelding was admitted for treatment of prolonged penile prolapse of 12 days' duration that developed after acepromazine maleate was administered to allow examination of a laceration that had resulted in severe blood loss. The horse was sedated, and the penis was replaced in the preputial cavity by use of a combination of massage and bandaging. Treatment was successful, and recovery was complete.

Acepromazine↗
PubMedDate not supplied

Determination of pseudoephedrine hydrochloride and carbinoxamine maleate in combination drug formulation by liquid chromatography.

An isocratic, reversed-phase liquid chromatographic (LC) method was developed for simultaneous determination of pseudoephedrine hydrochloride (I) and carbinoxamine maleate (II) in a pharmaceutical dosage form. Analysis was conducted on a CN column (10 microns), with a mobile phase consisting of acetonitrile-methanol-phosphate buffer (pH 5.3)-water (140 + 170 + 40 + 100) and at a detection wavelength of 262 nm. The method was validated for linearity, precision, system reproducibility, and accuracy. Recoveries at 80-120% of labeled claim ranged from 97.4 to 100.7% and from 98.5 to 100.2% for I and II, respectively. Results were linear (correlation coefficient, r > 0.9995 for I in the range 250-750 micrograms/mL and r > 0.9999 for II in the range 20-60 micrograms/mL.

Antitussive Agents↗
PubMed1998

Restraint of the paca (Agouti paca) with ketamine hydrochloride, acetylpromazine maleate, and atropine sulfate.

The paca (Agouti pace) is a neotropical rodent that requires chemical restraint for handling due to its aggressive nature and susceptibility to stress. Eighteen adult pacas (seven males and 11 females) weighing 6.25+/-2.22 (mean +/- SD) kg were given ketamine hydrochloride (25.0 mg/kg), acetylpromazine maleate (0.125 mg/kg), and atropine sulfate (0.05 mg/kg) combined by i.m. injection during field procedures that included sexing, marking, translocations, physical examinations, and minor surgeries. In all individuals, the induction of anesthesia was rapid and uneventful. Righting reflexes were abolished after 5.95+/-3.56 min, and all animals ceased to react to manipulation after 9.55+/-3.48 min. Response to interdigital and pinnal painful stimuli disappeared after 10.67+/-3.46 min and 11.11+/-3.83 min. respectively. Analgesia and depth of anesthesia were excellent in 61.0% of the animals and good in 39.0%. Muscle relaxation was excellent in 77.8% and good in 22.2%. Duration of anesthesia was 57.33+/-31.10 min. Recovery occurred without psychomotor disturbances, and every animal remained calm until normal ambulation resumed 115.00+/-37.00 min postinjection. The anesthetic protocol was safe for both the animal and the human personnel and is recommended for routine management and medical procedures, including minor surgeries, in A. paca.

Acepromazine↗