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PubMed1993

Inhibition of angiotensin converting enzyme with enalapril maleate in infants with congestive heart failure.

We studied the inhibition of angiotensin converting enzyme (ACE) in eight infants with congestive heart failure (CHF) poorly controlled with digoxin and diuretics, treated orally with 0.25 mg kg-1 enalapril maleate once a day. Baseline ACE activities were compared between these infants and control children without CHF or ACE inhibitor. Except for one infant who vomited, inhibition of ACE activity was 75.5 +/- 12.2%, 75.5 +/- 10.5% and 51.7 +/- 12.2%, at 4, 12 and 24 h after drug intake respectively. There was no correlation between postnatal age and inhibition of ACE activity. In infants with CHF, mean baseline ACE activity was significantly higher than in control infants (36.4 +/- 7.2 mu ml-1 vs 26.9 +/- 6.9 mu ml-1, P < 0.05). These results were very similar to those seen in adults.

Aging↗
PubMed1979

The effect of lisuride hydrogen maleate, an ergot derivative on anterior pituitary hormone secretion in man.

The effects of single oral doses of 0.2 mg of lisuride hydrogen maleate, a semisynthetic ergot derivative, on serum levels of prolactin (PRL), growth hormone (GH), thyroid stimulating hormone (TSH), luteinizing hormone (LH), follicle stimulating hormone (FSH), cortisol and blood glucose were studied in six normal males. Lisuride effectively inhibited basal PRL secretion as well as the PRL response to TRH given 3 h later. In addition, the drug raised basal GH levels and decreased basal and TRH stimulated TSH secretion. No significant differences between lisuride and control were observed in basal LH and FSH, LHRH stimulated gonadotrophins or in cortisol. Drowsiness was noted by all subjects, one became nauseated and another vomited, 60 and 90 min respectively after administration of lisuride. No changes were seen in pulse rate and blood pressure. The endocrine effects of lisuride were attenuated by the prior administration of the dopamine antagonist metoclopramide. These results suggest that lisuride acts as a long-acting dopamine agonist and that therefore this drug could be of therapeutic use in hyperprolactinaemic states and acromegaly.

Adult↗
PubMed2005

Pharmacokinetics and pharmacodynamics profiles of enalapril maleate in healthy volunteers following determination of enalapril and enalaprilat by two specific enzyme immunoassays.

BACKGROUND AND OBJECTIVES: Most of the pharmacokinetic (PK) parameters for enalapril and enalaprilat were established following determination of the drug and its metabolite, using angiotensin converting enzyme (ACE) inhibition assays. In these methods, enalapril has to be hydrolysed to enalaprilat first and then assayed. The purpose of this study was to re-estimate the PK parameters of enalapril and enalaprilat in healthy volunteers using two specific enzyme immunoassays for enalapril and enalaprilat. METHODS: The rate and extent of absorption of enalapril and enalaprilat from a 10-mg dose of two enalapril maleate commercial brands (Renetic and Enalapril) were estimated using a two-way-cross over design with 1-week washout period. Blood pressure was also measured at specified time intervals and correlated to enalaprilat plasma concentrations. RESULTS: For enalapril, the AUC(o-->infinity) values (Mean+/-SD) were 450.0+/-199.5 and 479.6+/-215.6 ng h/mL, Cmax values were 313.5+/-139.6 and 310.1+/-186.6 ng/mL, Tmax values were 1.06+/-0.30 h and 1.13+/-0.22 h, and t1/2 ranged between 0.3 to 6.1 h (1.6+/-1.5) and 0.40 to 5.05 h (1.3+/-1.0), for the two brands. For enalaprilat, the AUC(o-->infinity) values were 266.9+/-122.7 and 255.9+/-121.8 ng h/ml, Cmax values were 54.8+/-29.5 and 57.2+/-29.0 ng/mL, Tmax values were 4.6+/-1.6 h and 4.3+/-1.45 h, and t1/2 ranged between 1.1 to 10.5 h (4.5+/-2.9) and 0.6 to 9.4 h (3.5+/-2.5) for the two brands. CONCLUSIONS: Cmax values for enalapril are about 10 times those published in the literature and the rate and extent of absorption of the two brands of enalapril and their deesterification to enalaprilat following the administration of either brand were bioequivalent. Secondly, enalaprilat concentrations at 12-24 h following a single oral dose of enalapril in healthy volunteers were lower than those reported in the literature. The values reported here correlated with the return of blood pressure to predose level. Thirdly, enzyme immunoassays for enalapril and enalaprilat are better than ACE inhibition assays and can be used in bioequivalence assessment of enalapril and enalaprilat and for therapeutic drug monitoring in a clinical laboratory setting.

Absorption↗
PubMed2005

Serum concentration of potassium in chronic heart failure patients administered spironolactone plus furosemide and either enalapril maleate, losartan potassium or candesartan cilexetil.

OBJECTIVE: To retrospectively investigate elevation of serum potassium when spironolactone (25 or 50 mg/day) and furosemide were administered concomitantly with an angiotensin II converting enzyme inhibitor (ACE-I) or angiotensin II receptor blocker (ARB) to patients with chronic heart failure for 12 months and occurrence of hyperkalemia and hypokalemia because of concomitant administration of spironolactone plus an ACE-I or ARB and furosemide. METHODS: Patients with chronic heart failure, who visited departments of cardiovascular internal medicine and cardiovascular surgery at the National Hospital Organization Osaka Medical Center, were enrolled for this study. Serum potassium, blood urea nitrogen (BUN), serum creatinine, uric acid, and serum sodium were determined in every patient at the time of start of treatment and at 3 and 12 months of treatment. Data from patients in Groups A (25 mg/day spironolactone + 40 mg/day furosemide + an ACE-I or ARB) and B (50 mg/day spironolactone + 40 mg/day furosemide + an ACE-I or ARB) were analysed for differences with respect to the ACE-I and ARB used. RESULTS: When 50 mg/day spironolactone plus 5 mg/day enalapril maleate (enalapril) or 50 mg/day losartan potassium (losartan) or 8 mg/day candesartan cilexetil (candesartan) plus 40 mg/day furosemide were concomitantly used, the mean value of serum potassium was significantly elevated only in the group treated with 50 mg/day spironolactone regardless of the concomitant drug. The number of patients with hyperkalemia (>5.5 mEq/L) at 12 months of treatment was 12 (8.8%), while the number of patients with hypokalemia (<or=3.5 mEq/L) was 7 (5.1%). However, the occurrence of hyperkalemia was almost the same regardless of the dose of spironolactone or the ACE-I or ARB concomitantly administered. Therefore, if enalapril, losartan, or candesartan is concomitantly used, it is necessary to monitor the serum concentration of potassium, even if spironolactone is administered at a dose of 25 mg/day. CONCLUSION: The occurrence of hyperkalemia in patients administered spironolactone is influenced by the dose, but when it is used concomitantly with enalapril, losartan or candesartan, the occurrence of hyperkalemia exceeding 5.5 mEq/L may increase even if the dose of spironolactone is as low as 25 mg. Thus it is essential to always monitor serum potassium.

Adult↗
PubMed2006

Carvedilol accelerate elevation of serum potassium in chronic heart failure patients administered spironolactone plus furosemide and either enalapril maleate or candesartan cilexetil.

OBJECTIVE: To retrospectively investigate the effect of carvedilol and spironolactone plus furosemide, administered concomitantly with an angiotensin II converting enzyme inhibitor (ACE-I) or an angiotensin II receptor blocker (ARB) to patients with chronic heart failure (CHF). METHODS: Patients with CHF, who visited Departments of Cardiovascular Internal Medicine at the National Hospital Organization Osaka Medical Center, were enrolled for this study. Serum potassium, blood urea nitrogen (BUN), serum creatinine (Scr) and serum sodium were measured in every patient at the time of start of treatment and after 3 and 12 months of treatment. Data from patients in groups A (20 mg/day carvedilol + 25 mg/day spironolactone + 40 mg/day furosemide + an ACE-I) and B (20 mg/day carvedilol + 25 mg/day spironolactone + 40 mg/day furosemide + ARB) were compared. RESULTS: When 20 mg/day carvedilol plus 25 mg/day spironolactone plus 5 mg/day enalapril maleate (enalapril, group A) or 8 mg/day candesartan cilexetil (candesartan, group B) plus 40 mg/day furosemide were used concomitantly, the mean serum potassium increased significantly in both groups of patients. Seven of 59 (11.9%) patients had hyperkalemia (>5.5 mEq/L) during 12 months of treatment whereas 8.5% of patients (five of 59) had hypokalemia (< or =3.5 mEq/L). CONCLUSION: When carvedilol is used concomitantly with spironolactone, furosemide and enalapril or candesartan, it is necessary to monitor serum potassium concentration, even if spironolactone is administered at a low dose of 25 mg/day.

Adult↗
PubMed1983

Influence of acepromazine maleate on the equine haematocrit.

The effect of acepromazine maleate (ACP) on the equine venous haematocrit and total plasma protein concentration was studied in six clinically normal horses. Total plasma protein concentration was not appreciably influenced by ACP. However, the haematocrit decreased with the duration, but not the degree, of the decrease being dose-related. Mean haematocrit values returned to control levels by 12 h after 0.05 mg ACP/kg body weight and 21 h after 0.15 mg ACP/kg body weight.

Acepromazine↗
PubMed1983

A comparative study of dexchlorpheniramine maleate sustained release tablets and budesonide nasal spray in seasonal allergic rhinitis.

It was the aim of the study to compare the efficacy and side effects of oral antihistamine and nasal glucocorticoid therapy in seasonal allergic, rhinitis. In a double blind, double-dummy, group-comparative study, 61 adult grass pollen allergic patients were either treated with dexchlorpheniramine maleate sustained release tablets (6 mg b.d.), or with budesonide nasal spray (200 micrograms b.d.). After a 1-week run-in period, treatment was given for 3 weeks in the grass pollen season. Patients treated with budesonide showed significantly less nasal blockage than those who received dexchlorpheniramine (P less than 0.05), but there was no difference in the number of sneezes and nose blowings. Patients treated with budesonide and a larger quantity of antihistamine-vasoconstrictor eye drops (P less than 0.01). Drowsiness occurred in the group that was treated with dexchlorpheniramine, but mainly during the first week of treatment. The side effects caused by the budesonide spray were few and insignificant. The patients' overall assessment of the treatment favoured the glucocorticoid spray (P = 0.06).

Administration, Intranasal↗
PubMed2004

Efficacy and pharmacokinetics of fluvoxamine maleate in patients with mild depression undergoing hemodialysis.

Seven Japanese patients on maintenance hemodialysis who were comorbid with mild depression were medicated with 50 mg/day fluvoxamine maleate for 28 days. Effectiveness was obtained in four out of seven patients (57%). The plasma fluvoxamine concentrations were examined in three patients. The plasma fuvoxamine concentration decreased by 22% by hemodialysis. There is a tendency for the dialyzed rate of fluvoxamine to become lower if the plasma albumin concentration is higher. The half-life of fluvoxamine was possibly shortened more in the patient with hypoalbuminaemia. The plasma fluvoxamine concentration reached a steady state 8 days after the start of medication and thereafter. The time required to reach steady state was lengthened when compared with the results in normal Japanese volunteers.

Antidepressive Agents, Second-Generation↗
PubMed1983

Timoptol--three years on. A study of timolol maleate drops over a longer period.

A group of 130 patients with chronic glaucoma has been followed from one to more than three years on timolol maleate drops; this confirms that these drops remain effective in long-term therapy through added therapy is usually needed. Of 54 patients originally controlled by timolol alone or in combination, only four were not controlled more than three years later, though some needed further additional therapy. Of 35 patients followed for two to three years, only six could not be controlled by timolol alone or in combination; and of 41 followed for one to two years, 18 were controlled on timolol alone while 23 needed additional therapy. Attention is drawn to side effects including a mild keratopathy and in particular the occurrence of bronchospasm or other severe respiratory disease in 10 patients, not all of whom had a previous history of respiratory disease. Great care should be exercised with timolol in the presence of present or past respiratory disease as the complication is not generally recognised and it falls to the ophthalmologist to act to stop the drop.

Drug Therapy, Combination↗
PubMed1987

Therapeutic response interactions between timolol maleate and dipivefrin hydrochloride.

Twenty-one patients on long-term treatment with topical timolol maleate and dipivefrin hydrochloride were studied to assess the effect of each agent when used in combined therapy. The two agents are partially additive in most patients, but the relative contribution of each agent varies widely in individual patients and in separate diagnostic categories.

Aged↗
PubMed1990

Torsade de pointes associated with perhexiline maleate therapy.

Multiform ventricular tachycardia (torsade de pointes) is a recognised proarrhythmic effect of drugs which prolong the QT interval. A case is now described for the first time where torsade de pointes occurred with the administration of the anti-anginal agent perhexiline maleate.

Aged↗
PubMed1996

A cost-effectiveness analysis of enalapril maleate in the management of congestive heart failure in Australia.

BACKGROUND: This study is motivated by the results of the SOLVD treatment trial (N Engl J Med 1991; 325: 293-302) which demonstrated the clinical efficacy of enalapril in the treatment of congestive heart failure but did not undertake an economic evaluation of enalapril therapy. AIMS: To undertake a cost-effectiveness analysis of enalapril maleate versus placebo, in conjunction with conventional treatment, in the management of congestive heart failure in Australia. METHODS: The published results from the SOLVD treatment trial are used to estimate the increase in survival, and the reduction in the number of hospitalisations, arising from the use of enalapril in the management of congestive heart failure. The costs of enalapril therapy are estimated using Australian data on the drug and non-drug costs of enalapril therapy and the costs of hospitalisation. RESULTS: Enalapril therapy increases mean survival in heart failure patients by 1.68 to 1.80 months. The average additional drug and non-drug cost of enalapril therapy is estimated to be $1890 over a four year period, against which must be offset cost savings from a reduction in hospitalisations of $2060 to $2140. On balance, therefore, enalapril is cost saving, reducing health care costs for a congestive heart failure patient on average by $170 to $250 over a four year period. This value is sensitive to estimates of cost offsets and of improved survival which can result in either a net cost saving with enalapril of approximately $1200 per patient or a net additional cost of up to $3000 per patient (over four years) or greater than $20,000 per life-year saved. CONCLUSIONS: The addition of enalapril to conventional management of congestive heart failure in Australia should improve survival and may provide a net reduction in treatment costs compared with conventional management alone.

Angiotensin-Converting Enzyme Inhibitors↗
PubMed1979

The long-term hypotensive effect of timolol maleate compared with the effect of pilocarpine in simple and capsular glaucoma.

The long-term intraocular pressure (IOP) lowering effect of a beta-adrenergic blocking agent, timolol maleate, in topical administration was compared with the effect of pilocarpine on simple and capsular glaucoma by means of diurnal pressure curves during a six-month follow-up. In simple glaucoma timolol was more effective than pilocarpine in lowering IOP. In the follow-up a significant but not marked increase of the IOP was observed. In capsular glaucoma timolol was not effective enough, but when it was co-administered with miotics the IOP lowering effect was better than with either substance alone. Timolol induced no accomodative myopia, miosis, reduction of tear flow or other side effects. It increased the outflow facility in simple glaucoma but not in capsular glaucoma. During the trial, the anterior chamber depth increased while the corneal thickness remained unchanged. Four out of the six eyes included in a previous report of secondary glaucoma due to chronic uveitis are still, after one year of therapy, controlled with timolol.

Adrenergic beta-Antagonists↗
PubMedDate not supplied

Acute and short-term hemodynamic, echocardiographic, and clinical effects of enalapril maleate in dogs with naturally acquired heart failure: results of the Invasive Multicenter PROspective Veterinary Evaluation of Enalapril study. The IMPROVE Study Group.

The efficacy of enalapril maleate in dogs with naturally acquired class III or class IV heart failure was evaluated in a multicenter study. Fifty-eight dogs with dilated cardiomyopathy (35 dogs), mitral regurgitation (22 dogs), or aortic regurgitation (1 dog) receiving conventional therapy for heart failure (furosemide with or without digoxin) were included in a randomized double-blind study. Thirty-one dogs received enalapril tablets PO at approximately 0.5 mg/kg body weight bid, and 27 dogs received placebo tablets PO bid. Physical, electrocardiographic, hemodynamic, echocardiographic, radiographic, and clinical examinations were performed on each dog before treatment and at the end of the approximately 21-day study. After treatment on day 0, the enalapril-treated dogs had significantly (P < .05) lower heart rate, mean systemic arterial blood pressure, and mean pulmonary arterial blood pressure than the placebo-treated dogs. Pulmonary capillary wedge pressure was marginally decreased (P = .0567) in the enalapril-treated dogs. When compared with those in the placebo-treated dogs, scores for pulmonary edema were significantly (P < .05) decreased on day 2 in the enalapril-treated dogs. At the end of the study, enalapril-treated dogs had significantly (P < .05) greater decreases in class of heart failure, pulmonary edema score, and mobility score relative to baseline, and had significantly (P < .05) better overall evaluation scores when compared with the placebo-treated dogs. This study shows the beneficial hemodynamic and clinical effects of adding enalapril to conventional therapy for dogs with heart failure.

Angiotensin-Converting Enzyme Inhibitors↗
PubMed1991

Release of chlorpheniramine maleate from fatty acid ester matrix disks prepared by melt-extrusion.

Chlorpheniramine maleate was incorporated into disks consisting of glyceryl fatty acid esters, polyethylene glycol fatty acid esters or a combination of the two. A melt-extrusion process was used to prepare the matrix disks containing the drug. The release of the drug into distilled water, pH 1.2 buffer, and pH 7.5 buffer showed the expected square root of time dependence. An increase in the fatty acid ester hydrophilic-lipophilic balance (HLB) from 1 to 14 resulted in a 10-fold increase in the drug release rate from 0.25 +/- 0.01 to 25.84 +/- 1.29 mg cm-2 h-1/2. The maximum release rate was seen from the fatty acid ester with a melting point of 44 degrees C. The pH of the dissolution medium had a small impact on the rate of drug release, but the rate of agitation had no significant influence on the rate of drug release. By blending a fatty acid ester of a high melting point (64 degrees C) and a low HLB value of 2 with esters of lower melting points (33 to 50 degrees C) or higher HLB values (10 to 14), it was possible to modify the release from 10.0 +/- 0.70 to 21.5 +/- 0.57 mg cm-2 h-1/2.

Chemistry, Pharmaceutical↗
PubMed1980

Addition of timolol maleate to routine medical therapy: a clinical trial.

A double-blind cross-over trial of timolol maleate (Timoptol) while routine medical therapy was continued gave the result that pressure was reduced by 3.22 mmHg is compared to placebo and 5.01 compared to pre-timolol levels in 24 patients. There was also a small (1.858 mmHg) drop in pressure in placebo treated eyes, a small and statistically significant drop in resting pulse rate, 76.67 to 71.39/min, and a small but not statistically significant drop in diastolic blood pressure.

Adult↗
PubMed1979

Liver damage associated with perhexiline maleate.

Two patients who developed biochemical and histological evidence of hepatitis while taking the anti-anginal drug perhexiline maleate are described. The pathological changes were those of mild to moderate fatty change together with a hepatitis which resembled alcoholic hepatitis, including in one patient the presence of material which by light microscopy was indistinguishable from Mallory's alcoholic hyalin. However, the predominantly periportal location of this material contrasted with the centrilobular distribution of Mallory's hyaline. One patient showed, in addition, severe atypia of the hepatocytes which was still present in less pronounced form 10 weeks after stopping perhexiline. The other patient had advanced hepatic fibrosis.

Aged↗