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At least 703 records · Page 39Linked to original sources
PubMed1990

Apraclonidine hydrochloride: an evaluation of plasma concentrations, and a comparison of its intraocular pressure lowering and cardiovascular effects to timolol maleate.

We performed a prospective, placebo-controlled, cross-over study in 20 young healthy female volunteers. We evaluated both the cardiovascular and IOP effects of both timolol maleate and apraclonidine hydrochloride. In addition, we evaluated the plasma levels of various apraclonidine concentrations. We utilized 0.5% timolol and both the 0.25% and 0.50% concentrations of apraclonidine. Both timolol and apraclonidine lowered IOP comparably. Timolol lowered the resting pulse rate and blunted exercise-induced tachycardia. Apraclonidine did not affect blood pressure or heart rate any differently than placebo. We detected plasma levels of apraclonidine in many individuals for up to 8 hours. These serum levels were variable and did not appear to relate to the quantity of IOP lowering.

Adrenergic alpha-Agonists↗
PubMed1977

[Oedematous optic neuropathy from Perhexilline maleate associated with peripheral polyneuropathy (author's transl)].

The authors report on a polyradiculoneuropathy related to long-term treatment with Perhexiline maleate (a drug used in France since 1973 for coronary insufficiency) whose presenting sign is a bilateral aedematous optic neuropathy. The mechanism of this effect on the optic nerves and on papilloedema is discussed; it seems not to be caused by a direct toxic action on the optic fibres but by the existence of chronic intracranial hypertension.

Humans↗
PubMed1978

[Diffuse polymorphous inclusions in a patient treated with perhexiline maleate (author's transl)].

Case report of polyneuritis and liver dysfunction induced by perhexiline maleate in a 64 years old male patient. The ultrastructural study of nerve, liver, muscle and skin biopsies shows polymorphous, membrane bound, often multilamellar, lysosome-like inclusions, the content of which is probably complex lipids. The histochemical study of liver reveals a lipid storage, consisting mainly of triglycerides and of smaller amount of phospholipids and free fatty acids, the pattern of which is abnormal. The biochemical study of nerve tissue shows a decrease of phospholipids levels and some qualitative disturbances in gangliosides. These changes, some of which are similar to those reported in amphiphilic drug intoxications, are prevalent in high lipid metabolism cells such as hepatic and Schwann cells.

Biopsy↗
PubMedDate not supplied

[Pharmacological basis for a fixed association of hydrochlorothiazide, amiloride hydrochloride, and timolol maleate (author's transl)].

The treatment of hypertension requires in many cases a therapeutic combination. This survey, carried out in 96 cases, shows the interest of a fixed combination including a thiazide diuretic (hydrochlorothiazide), a potassium sparing (chlorhydrate of amiloride) and a beta-blocking agent (timolol maleate) as compared to therapy with a beta-blocking agent or diuretic alone. This combination, logical from a pharmacological view point, has proved significantly more effective (81% of patients were normalized) and as well tolerated (none additional side effect) as each of its components. As it simplifies prescription by reducing the number of tablets, it appears a considerable contribution to hypertension therapy.

Amiloride↗
PubMed1990

Efficacy of chlorpheniramine maleate for management of pruritus in cats.

Chlorpheniramine maleate was administered orally (2 mg, q12 h) to 26 cats with pruritic skin disease. Pruritus was completely eliminated in 19 cats, and was reduced by 50% in 1 cat. Six cats had no response to treatment. Serious or long-lasting clinical side effects were not observed in any cat.

Animals↗
PubMed1985

[Evaluation of the clinical effect of lisuride hydrogen maleate (SH-1072) on benign prostatic hypertrophy: on the clinical results and mechanism of action].

Lisuride hydrogen maleate (LHM, SH-1072), a dopaminergic agonist and therefore an inhibitor of prolactin (PRL) secretion, were administered to 12 patients with mild to moderate BPH in order to evaluate the clinical effectiveness. LHM was administered 75 or 150 mcg/day, po, for 20 weeks on the average. The status of micturition evaluated by score points and nocturnal frequency of urination was significantly improved, whereas objective responses such as on the amount of residual urine, size of the prostate gland, findings of urethrocystography and the length of prostatic urethra measured on the film were minimal. Serum PRL level have been reduced significantly through the therapy, and testosterone were unchanged. The mechanism of action of the agent on BPH and the surrounding tissue was discussed; reduced androgen effect on the prostate through lowering of PRL and anti-alpha-adrenergic activity or the effect through prostaglandin on the gland, the bladder neck and the posterior urethra would mitigate the symptoms.

Aged↗
PubMed1985

Captopril versus enalapril maleate: a comparison of antihypertensive and hormonal effects.

The antihypertensive effects of captopril and enalapril maleate were studied over a 10-week period in 24 hypertensive patients randomized into captopril or enalapril treatment groups. Prestudy blood pressure was 171 +/- 4/109 +/- 1 mm Hg and after 4 weeks of hydrochlorothiazide 160 +/- 4/103 +/- 1 (p less than 0.05). With the addition of converting enzyme inhibitor to hydrochlorothiazide the blood pressure decreased at 3 h to 132 +/- 3/87 +/- 2 in the subjects. The diastolic blood pressure decreased acutely more with captopril (-24) than with enalapril (-17) (p less than 0.05). After 10 weeks of combined therapy the depressor response was maintained (134 +/- 3/83 +/- 1) and there was no difference between the diastolic blood pressure in the two groups treated with captopril and enalapril. Acute and chronic responses of plasma renin activity, plasma aldosterone, and converting enzyme to the angiotensin-converting enzyme inhibitor were determined. There was a significant correlation between the acute fall in diastolic blood pressure and rise in plasma renin activity in patients treated with captopril but not with enalapril. In conclusion, there is an acute depressor response with converting enzyme inhibition which is more pronounced with captopril than with enalapril and which correlates with an increase in plasma renin activity. With more prolonged treatment, the two drugs show equivalent efficacy in reducing blood pressure, inhibiting angiotensin-converting enzyme, reducing aldosterone, and stimulating plasma renin activity.

Adult↗
PubMed1989

Metabolic fate of the new Ca++-channel blocking agent (+)-(2S,3S)-3-acetoxy-8-chloro-(2-(dimethylamino)ethyl)-2,3-dihydro- 2-(4-methoxyphenyl)-2,5-benzothiazepin-4-(5H)-one maleate. Distribution, excretion and protein binding in rats and dogs.

Distribution, excretion and protein binding of (+)-(2S,3S)-3-acetoxy-8-chloro-(2-(dimethylamino)ethyl)-2,3-dihydro- 2-(4-methoxyphenyl)-2,5-benzothiazepin-4-(5H)-one maleate (TA-3090) in rats and dogs were investigated after oral (30 mg/kg (rats), 2 mg/kg(dogs] and intravenous (3 mg/kg (rats), 0.2 mg/kg (dogs) administration of 14C-TA-3090. Plasma level of radioactivity in rats reached plateau (6.04 micrograms equiv. of TA-3090 free base/ml) 1 h after oral administration. The plateau level continued at least up to 6 h. The plasma concentration of the unchanged drug (free base) reached the maximum (425 ng/ml) at 45 min after oral administration, and then decreased with a half-life of 1.16 h. Plasma level of radioactivity after intravenous administration to rats rose gradually up to 1 h and thereafter it was kept constant for 6 h. Plasma concentration of the unchanged drug decreased with half-lives of 0.43 h (alpha phase) and 1.33 h (beta phase) after intravenous administration. In dogs, the peak level of plasma radioactivity after oral administration was 227 ng/ml at 1 h. The Cmax, Tmax and t1/2 of unchanged drug were 31 ng/ml, 1.34 h and 4.13 h, respectively. The plasma levels of total radioactivity and unchanged drug after intravenous administration to dogs were 146 and 142 ng/ml at 1 min, respectively. The t1/2 of the plasma radioactivity were 0.02 h (alpha) and 4.02 h (beta). Those of unchanged drug were 0.03 h (alpha) and 1.66 h (beta).(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1989

Effects of perhexiline maleate on asialo-orosomucoid receptor endocytosis and recycling in HTC cells.

Perhexiline is a lysosomotropic agent which has proved to be very valuable to certain patients suffering from angina pectoris. However long-term administration of the drug may induce hepato- and neuro-toxicity. Using HTC cells (a rat hepatoma-derived cell line) whose plasma membranes were labeled with NaB[3H]4 after oxidation by NaIO4, endocytosis and recycling of labeled asialo-orosomucoid (ASOR) receptors were investigated in the presence of 50 mumols/l perhexiline maleate. The results demonstrate that the drug induces a significant decrease of the rate of both the internalization and the recycling of ASOR receptors. The mechanisms responsible for these effects have not yet been elucidated. However, the current findings may be related to the previously observed inhibitory effect of perhexiline on cellular (Na+, K+)-ATPase and Mg++-ATPase activities. Our findings would then reflect insufficient cellular energy production, resulting from depressed ATP hydrolysis in the presence of perhexiline.

Animals↗
PubMed1989

[Administration of uterotonic drugs at the end of the expulsion stage. Comparison of the use of oxytocin and ergometrine maleate].

In spite of the large diffusion of uterotonic drugs some doubts persist about which preparation and which dosage are the most suitable. For such a reason a group of pregnant women, to whom ergometrine maleate was administered at the delivery of the anterior shoulder of the fetus, was compared by the authors to an analogous group formed by pregnant women to whom oxytocin was administered under the same conditions. Pregnant women not submitted to a pharmacologic control of the third stage of labour served as a control group. Each study group was thereafter divided into 2 subgroups: the former is composed by patients submitted to episiotomy and the latter by patients not submitted to this procedure. Our results have shown the usefulness of both drugs in the active management of the third stage of labour, whereas different side effects may occur.

Episiotomy↗
PubMedDate not supplied

Effects of lisuride hydrogen maleate on ischemia-induced depletion of brain acetylcholine levels in gerbils.

Effects of several cerebral metabolic activators on ischemia-induced decrease in brain acetylcholine levels were studied in gerbils. Single administration of lisuride hydrogen maleate (lisuride) significantly inhibited ischemia-induced decreases in acetylcholine in the hippocampus among various regions of the brain in 46 gerbils; however, single administration of idebenone and indeloxazine hydrochloride did not affect the ischemia-induced decreases in acetylcholine. When lisuride was intraperitoneally administered to gerbils at low doses once daily for 14 days, ischemia-induced decreases in acetylcholine were inhibited dose-dependently in all the evaluated regions of the brain. The effects of lisuride were much more marked following consecutive administration than single administration. No changes in brain acetylcholine were observed following the 14-day administration of lisuride alone without induction of ischemia. These results suggest that lisuride is not only useful for treating sequelae of cerebrovascular diseases but, when administered consecutively, is also useful for preventing ischemia-induced cerebral disturbances.

Acetylcholine↗
PubMed1988

Local actions of trimebutine maleate in canine small intestine.

A study of the local actions of trimebutine (TMB) maleate and its N-diesmethyl metabolite (TMB-M) was carried out in the gastrointestinal tract of anesthetized dogs. In the unstimulated small intestine, but not in the stomach or colon, i.a. TMB and TMB-M caused activation of circular muscle. Like the activation by i.a. [Met5]-enkephalin, this was antagonized by naloxone. In field-stimulated segments of stomach and small intestine circular muscle, TMB or TMB-M, like dynorphin-1-13 or [Met5]-enkephalin, inhibited the phasic and tonic contractions which were mediated mostly by cholinergic, postganglionic nerves. However, the inhibitory effects of dynorphin-1-13 or [Met5]-enkephalin on small intestine were antagonized by naloxone whereas those of TMB sometimes or those of TMB-M usually were not. TMB or TMB-M did not affect responses to i.a. acetylcholine, but high doses reduced the contractile responses to subsequent field stimulation and excitatory responses to [Met5]-enkephalin. We concluded that the excitatory local actions of TMB or TMB-M on small intestine involved opioid receptors probably of the mu or delta types. Inhibitory local actions on nerve-mediated responses, however, may not have involved opioid receptors. Comparison of these data to results when TMB or TMB-M were given i.v. suggests that these agents also have peripheral actions to affect gastrointestinal motility at sites outside the gastrointestinal tract.

Animals↗
PubMed1977

[Influence of perhexiline maleate on the electrocardiographic signs of myocardial ischemia. Ergometric study].

The improvement in the electrocardiographic signs of coronary insufficiency under the influence of perhexiline maleate is the object of an ergometric study in 28 patients. Ergometric tests repeated at regular over an average period of 8.3 months show a rapid ECG improvement, sustained over the period of the study. The heart rate, registered while at rest, which diminshes between that noted at the beginning of the study and that noted at the first registration under treatment, remains stable during the three following registrations. At the end of the effort, on the other hand, a significant reduction in tachycardia is observed during all the registrations.

Coronary Disease↗
PubMed1988

Management of ovarian hyperstimulation syndrome with chlorpheniramine maleate, mannitol, and invasive hemodynamic monitoring.

Ovarian hyperstimulation syndrome due to exogenous gonadotropin administration is life-threatening in its most severe form. Profound fluid shifts may occur, with concomitant cardiovascular changes. We present a case of severe ovarian hyperstimulation syndrome managed with chlorpheniramine maleate (previously shown to be effective in animal models) and invasive hemodynamic monitoring. Mannitol and albumin infusions were also used to maintain urine output and intravascular volume.

Adult↗
PubMed1988

[Coronary artery tone assessed by the administration of ergonovine maleate and nitrates].

Angiographic changes caused by administering ergonovine maleate (EM) and nitrates were quantitated in 136 patients without significant coronary artery disease. Percent coronary artery (CA) narrowing was calculated in 67 patients with a negative EM test (Group A) and 69 patients with a positive EM test (Group B) as follows: (Formula; see text) In both groups, coronary artery narrowing before and after EM did not differ among the proximal, middle or distal segments of each coronary artery. The measurements of the right coronary artery were greater than those of the left anterior descending artery (p less than 0.01 after EM, p less than 0.05 before EM), and those of the left main trunk were markedly less than those of the other coronary arteries (p less than 0.01). In both groups, coronary narrowing after EM administration was greater than before administration (p less than 0.01). Initial coronary narrowing in Group B was also greater than in Group A (p less than 0.01), similar to the responses for EM. In 19 patients with coronary artery spasm provoked by EM coronary artery narrowing before and after EM was 37 +/- 12% and 69 +/- 23% for coronary arteries with spasm, and 30 +/- 13% and 42 +/- 16% for those without spasm. Not only after, but also before EM administration, coronary narrowing was greater in the arteries with spasm than in those without spasm (p less than 0.01). Furthermore, the arteries without spasm showed greater sensitivity to EM and nitrates than did the arteries of the control patients.(ABSTRACT TRUNCATED AT 250 WORDS)

Coronary Vessels↗
PubMed1987

[Coronary arterial spasm and symptomatology in ischemic and non-ischemic heart diseases: study of the ergonovine maleate provocative test in 3,000 consecutive patients].

We performed coronary angiography and ergonovine maleate provocative tests (EM test) for 3,000 consecutive patients to clarify 1) the incidence of coronary arterial spasm and significant fixed organic stenosis in ischemic and non-ischemic heart diseases, and 2) the relation of these angina-inducing mechanism(s) to rest (R), effort and rest (E & R), and effort (E) angina. Coronary arterial spasm was defined as total or subtotal occlusion induced by ergonovine test, and fixed stenosis was defined as stenosis with more than 70% narrowing of luminal diameter measured after administration of isosorbide dinitrate. Subjects consisted of 3,000 consecutive patients and were categorized in four groups including 1,145 patients who had typical angina pectoris (Group I: rest angina 653, effort angina 230, and combined rest and effort angina 262), 398 patients with myocardial infarction (Group II), 648 patients with atypical chest pain (Group III), and 809 patients who eventually had diagnostic catheterization for heart diseases other than of ischemic nature (Group IV). Results were as follows: 1. The incidence of coronary artery spasm was 22.2% in Group I, 22.9% in Group II, 1.2% in Group III, and 3.7% in Group IV. 2. In Group I, there was a close relationship between the mechanism of angina and the type of occurrence of typical chest pain; coronary artery spasm was more likely observed in rest angina, organic stenosis was observed in effort angina, and the combined type was observed in cases with both spasm and organic stenosis. Furthermore, the occurrence of coronary artery spasm was significantly more frequent in cases with single vessel disease compared with those with multivessel disease (50.7% vs. 26.7%, p less than 0.005). 3. In Group II, the most frequent angiographic evidence was fixed organic stenosis, and there was no relationship between spasm and the numbers of diseased vessels. 4. In Groups III and IV, the most common entity causing coronary artery spasm was hypertrophic cardiomyopathy. In conclusion, two major mechanisms of angina pectoris, i.e., coronary artery spasm and organic stenosis, are closely related to the symptomatology of this disease, such as rest, effort and combined rest and effort types.

Adult↗
PubMed1978

Long-term effect of perhexiline maleate on ventricular ectopic activity.

The effectiveness of perhexiline maleate in the suppression of ventricular ectopic activity has been studied in 10 patients after myocardial infarction. Before treatment all patients exhibited frequent ectopic beats, i.e. more than 8 per hour. Numerous Holter magnetic tape recordings were made over a 9 - 10-month period of treatment. During the entire period of monitoring significant suppression of ectopic activity was observed in 5 patients and transient suppression in 4, of whom 3 subsequently showed a transient increase. The drug was discontinued in 1 patient because of nausea, anorexia and weight loss. No other adverse effects were encountered.

Anti-Arrhythmia Agents↗