Perhexiline maleate induced cirrhosis.
Perhexiline maleate is a potent anti-anginal drug which may cause alcoholic-type hepatitis and cirrhosis. We report a case of a patient who developed cirrhosis on a relatively low dose within 16 mth.
Aged↗
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The effects of separate and combined topical treatment with timolol maleate and trifluormethazolamide on the intraocular pressure in normal rabbits.
The effects of separate and combined topical treatment with timolol maleate and trifluormethazolamide (TFM) on the intraocular pressure (IOP) were studied in normotensive rabbits. Timolol had a distinct, albeit small, dose related hypotensive effect. Unilateral application of timolol resulted in dose related decrease in IOP in the untreated fellow eye. These effects could be observed only by using a protocol that reduces the contribution of individual and diurnal variations to the overall variability in IOP in the rabbit. Topical treatment with TFM caused a reduction in the calculated outflow pressure of 32%, similar to that observed after systemic administration of acetazolamide and methazolamide. At the concentration and dosage employed here there was no significant difference between the hypotensive effects of timolol and TFM. The maximal decrease in the calculated outflow pressure for the different doses of timolol varied between 24% to 37%. The hypotensive effect of the combined timolol and TFM treatment (delta IOP = -2.4 +/- 0.4 mmHg, n = 12) was greater than that observed in rabbits treated with TFM alone (delta IOP = -1.6 +/- 0.5 mmHg, n = 12). The increment was smaller than the initial effect of either drug alone.
Administration, Topical↗
Enalapril maleate (MK-421), a potent, nonsulfhydryl angiotensin-converting enzyme inhibitor: absorption, disposition, and metabolism in man.
Animal studies (particularly in dogs) on enalapril maleate have served to predict the patterns of absorption and elimination observed in man. Enalapril is more readily absorbed in man than the active inhibitor form MK-422. Estimates of minimum absorption of enalapril are of the order of 60-70%, based on urinary recovery. Metabolism of enalapril to MK-422 appears to be largely a postabsorptive process. From urinary recovery data, a minimum of 43% of a 10-mg dose of enalapril is available as MK-422. Excretion of enalapril and MK-422 is principally renal. The excellent mass balance obtained in human studies precludes extensive metabolism beyond hydrolysis to MK-422. Data in hand suggest that any metabolism other than to MK-422 is of a trace nature.
Absorption↗
Effects of enalapril maleate on plasma level of inactive renin in renovascular hypertension.
Changes in plasma levels of active and inactive renin after the treatment with enalapril maleate (MK-421), a new angiotensin converting enzyme inhibitor, were studied in five patients with renovascular hypertension (RVH) due to unilateral renal artery stenosis. The dosage was increased when the blood pressure (BP) was not normalized for more than 3 days. Blood sampling was performed before, and 5 hours and 24 hours after the first administration, and on the 3rd day with each dosage. Active and inactive renin concentrations (ARC and IRC) showed a reciprocal change in 4 cases, 5 hours after the first dose. In the chronic treatment, ARC and IRC before the morning dose did not change apparently until the BP was normalized, when both ARC and IRC were evidently increased. It was suspected that a conversion from inactive to active renin may occur in the patients with RVH, when the active renin secretion is stimulated suddenly by the first dose of MK-421. The chronically diminished perfusion pressure in the kidney may stimulate the secretion of inactive renin, but the decrease in endogenous angiotensin II may not.
Adolescent↗
[Chronic administration of lisuride hydrogen maleate increases muscarinic acetylcholine receptor binding in aged rat brain].
Changes in the distribution and densities of muscarinic acetylcholine receptors (mACh-R) in young adult and aged rat brain, and the effects of chronic administration of lisuride hydrogen maleate (lisuride) on these changes were studied by in vitro quantitative autoradiography of [3H] quinuclidinyl benzilate binding. mACh-R was relatively higher in the striatum, hippocampus and cerebral cortex in the young adult rats. In contrast, mACh-R binding was markedly reduced in the striatum, accumbens nucleus, amygdaloid nucleus and frontal cerebral cortex of aged rats compared to young adult rats. However, chronic administration of lisuride significantly increased mACh-R binding in the parietal cerebral cortex as well as in the above-mentioned regions in aged rats. This lisuride-induced increase in mACh-R of aged rat brain is considered to have important implications concerning the mechanism of therapeutic efficacy of lisuride.
Aging↗
A retrospective study on the use of acepromazine maleate in dogs with seizures.
Use of acepromazine (i.e., acetylpromazine) maleate in dogs with a history of seizures is reportedly contraindicated because of the risk of decreasing the seizure threshold in these animals. In this retrospective study, acepromazine was administered for tranquilization to 36 dogs with a prior history of seizures and to decrease seizure activity in 11 dogs. No seizures were seen within 16 hours of acepromazine administration in the 36 dogs that received the drug for tranquilization during hospitalization. After acepromazine administration, seizures abated for 1.5 to 8 hours (n=6) or did not recur (n=2) in eight of 10 dogs that were actively seizing. Excitement-induced seizure frequency was reduced for 2 months in one dog.
Acepromazine↗
Perhexiline maleate neurotoxicity and weight loss.
Ten Caucasian patients with perhexiline maleate neurotoxicosis and weight loss are presented. Weight loss preceded symptomatic neuropathy which was detected on electromyography in one patient. Weight loss and neuropathy may be marked, but clinical improvement follows drug withdrawal.
Aged↗
[Coronary artery spasm induced by the somministration of ergonovine maleate in subjects with spontaneous angina (author's transl)].
In 6 patients affected by spontaneous angina with S-T elevation and coronariographic findings of obstruction, intravenous administration of ergonovine maleate determined the same clinical and ECG patterns of spontaneous episodes. The coronary arteriography during pain showed a marked spasm with occlusion of a large coronary vessel in four patients. In 2 patients with atypical chest pain and normal coronariogram, E.M. did not induce pain, ECG abnormality or coronariographic alterations. The role of spasm in spontaneous angina is discussed.
Adult↗
Diversity of response of optic nerve head circulation to timolol maleate in gel-forming solution.
PURPOSE: This randomized, double-masked, placebo-controlled, two-period crossover study was conducted to investigate the effects of 0.5% timolol maleate in gel-forming solution on intraocular pressure (IOP) and blood circulation in the optic nerve head in patients with untreated ocular hypertension. METHODS: The effects of 0.5% timolol in gel-forming solution on IOP and optic nerve head capillary blood speed were studied in 12 patients with untreated ocular hypertension. Optic nerve capillary blood speed was measured using the laser Doppler technique before and at the end of each treatment period. RESULTS: In each patient, IOP decreased after treatment with timolol (mean decrease 16.8% versus placebo). Systemic blood pressure and pulse rate did not differ significantly after treatment with topical timolol from values after placebo. The mean change from baseline in Doppler broadening was 10.6% greater after treatment with timolol than after placebo. There was no significant change in mean Doppler broadening from baseline after treatment with either timolol or placebo. However, optic nerve head capillary blood speed increased in six patients, and was within the range of placebo response in six patients after treatment with timolol. Spearman correlation analysis of the baseline with Doppler broadening measurements after treatment showed a correlation for placebo but not for timolol. The percent change in Doppler broadening after timolol treatment was correlated with iris color. CONCLUSION: These results indicate that administration of timolol for 4 weeks reduces IOP in patients with ocular hypertension and generally does not change the blood circulation in the optic nerve head. Individual patients, however, showed variable changes in optic nerve head circulation after topical administration of timolol. Although the sample size was small, these changes in optic nerve head circulation were correlated with iris color.
Adrenergic beta-Antagonists↗
[Methyl-ergometrin maleate test during coronary arteriography in spontaneous chest pain].
This coronary spasm provocation test with methyl-ergometrine maleate was carried out during coronary arteriography in 47 patients presenting with spontaneous chest pain. Coronary spasm was triggered in 16 cases, reproducing the chest pain in 11 patients, and accompanied by electrical changes in 15 cases, 12 subepicardial ischaemias and 3 subendocardial ischaemias. This test is not without danger to the patient as arrhythmias and conduction defects were recorded in 6 cases although the spasm was readily reversible on injection of intravenous glyceryl trinitrate. Of 7 patients with Prinzmetal variant angina, the test was positive 6 times, in three of which on pre existing severe organic lesions, so confirming the mechanism of this syndrome and the reliability of the test. Of 40 patients presenting with spontaneous chest pain, 10 had a positive test. In 2 of these cases the chest pain was subsequently observed with subepicardial ischaemic electrical changes, so confirming the screening value of this test. In the 7 cases where coronary spasm gave rise to electrical changes with or without pain, the logical diagnosis would appear to be spastic angina. In the 30 cases where the test was negative the subsequent outcome did not provide any proof in favour of a coronary origin of the chest pain.
Adult↗
Prediction of psychotropic properties of lisuride hydrogen maleate by quantitative pharmaco-electroencephalogram.
Based on "quantitative pharmaco-EEG" using computer-analyzed EEG (CEEG) measurements, unknown CNS effects of lisuride hydrogen maleate (LHM) were established. CEEG profiles of LHM in low dosages (less than or equal to 10 mcg) are similar to CNS "inhibitory" compounds, while in higher dosages (25 mcg to 100 mcg) they resemble "psychostimulant" compounds. By measuring the brain function using computer period analysis of cerebral biopotentials, dose-efficacy relations were found (in the range of 25-75 mcg) which suggest the bioavailability of LHM at the CNS level. By comparing the CEEG profiles of LHM with the previously studied compounds, five different clinical uses of LHM were predicted. The pilot trials suggest that LHM may have therapeutic potentials in patients with "aging" and/or organic brain syndromes, and in children with behavioral disturbances.
Adolescent↗
[Clinical trial by perexiline maleate in treatment of angina pectoris (author's transl)].
A controlled double blind clinical trial has been conducted in 16 patients with "angina pectoris" in order to investigate the effect of Perexiline maleate as compared with prenilamine. Perexiline at the dose of 400 mg/die and prenilamine at the dose of 120 mg/die have been administered over a period of 4 weeks each. Between these periods placebo has been administered for two weeks. The number of attacks of angina and the number of tablets of nitroglycerine used per week by the patient during each period has been used for the evaluation. Furthermore ECG at rest and after exercise has been performed every two weeks. Our results statistically evaluated show a definite antianginal effect of Perexiline. According to our experience Perexiline should be considered the drug of choise in the treatment of angina complicated by bradicardia, left ventricular failure, bronchospasm, and in angina unresponsive to other drugs.
Angina Pectoris↗
[Effects of nebivolol, metoprolol and enalapril maleate on the state of endothelium-dependent arteriolar vasodilation in patients with essential hypertension].
Effects were studied of nebivolol, metoprolol and enalapril maleat on the state of endothelium-dependent vasodilatation of arterioles in patients with essential arterial hypertension. Nebivolol has been shown to effectively decrease blood pressure and restore endothelium-dependent vasodilatation to a grater degree, than enalapril or metoprolol.
Adult↗
Pharmacokinetic study of maleate acid of 2-(N,N-dimethylaminoethanol-14C1)-cyclohexylpropionate (cyprodenate) and of N,N-dimethylaminoethanol-14C1 in animals.
The localization, distribution, and elimination of maleate acid 2-(N,N-dimethylaminoethanol-14C1)-cyclohexylpropionate (14C-cyprodenate, Actebral) was studied in rats and pigs. Beside this, dimethylaminoethanol-14C (DMAE) was also administered to rats enabling a comparison of the pharmacokinetics of the two 14C-labelled molecules to be made. The study of the localization by autoradiography and the study of the quantitative distribution of the radioactivity showed that cyprodenate, a psychotonic drug, diffused more rapidly than DMAE through the hemo-encephalic barrier. However, it was also observed that the radioactivity found in the brain rises continually as a function of time, regardless of the product administered. The two labelled products were primarily excreted in the urine (30-35 per cent of the dose in 72 h in rats and 6 per cent of the dose in 48 h in pigs) following oral administration of cyprodenate. Radioactivity found in the feces was practically nil and in rats the biliary elimination of the drug was very weak. Thus, whichever animal is used, it was found that 14C-cyprodenate is totally absorbed. Radioactivity expired as 14CO2 was negligible (around 1 per cent of the administered dose in 8 h), however, this value increases as a function of time, becoming 4 per cent in 24 h. In rats the maximum radioactivity in the blood was found at 45 min to 1 h after oral administration of 14C-cyprodenate. These values decrease slowly until 3 h when they begin to increase again. The rising of the blood level values is practically the same for pigs, the maximum being attained at 1 h. Therefore, whatever route of administration, whichever dose or animal, we always found a progressive elevation of the protein binding to the plasma proteins for these two labelled products in vivo.
Animals↗
[Effect of pH on the permeability of timolol maleate across isolated rabbit cornea].
AIM: To study the effect of pH on the transcorneal permeability of timolol maleate (TM). METHODS: The apparent distribution coefficients of TM were determined. The permeability of TM across isolated rabbit cornea was measured using in vitro method at various pH. RESULTS: The partition coefficient and pKa of TM were 63.63 and 9.17 respectively. At neutral pH, the apparent permeation coefficient of TM was 1.43 x 10(-5) cm.s-1. When the pH varied from 6.65 to 9.20, the cumulative amount for timolol transcorneal penetration increased 1.3 times and the lag time decreased more than 19-folds. The calculated permeability coefficients of ionized and un-ionized timolol were 1.29 x 10(-5) cm.s-1 and 4.22 x 10(-5) cm.s-1, respectively. CONCLUSION: Timolol penetrated corneal membrane mainly as free base by intracellular pathway, and corneal epithelium was the rate-limiting barrier.
Animals↗
[Effect of combined therapy with enalapril maleate and hypothiazide on the structuro-functional status of erythrocyte membranes in hypertensive patients].
AIM: To characterize changes in erythrocytic membranes (ErM) structure and function in patients with essential hypertension (EH) due to combined therapy with enalapril maleate (EM) and hypothiazide. MATERIAL AND METHODS: Polypeptide and lipid spectra of ErM were studied by electrophoresis in polyacrylamide gel and thin-layer chromatography, respectively, the activity of transport ATP, lipid peroxidation (LPO) and antioxidant defense were studied with standard techniques in 32 EH patients before and 4 weeks after combined therapy with EM and hypothiazide. RESULTS: If previous EM therapy failed, combined treatment's effect was 62.5%. Molecular effects of the treatment consisted of decreased concentrations of actin and blend 5 protein, increased levels of spectrin in EM polypeptide composition, correction of phopholipid fractions imbalance, gluthationperoxidase. Transport ATP activity and chholesterin level remained unchanged. CONCLUSION: EH treatment with EM + hypothiazide is both clinically effective and beneficial for physico-chemical properties of the cell membranes.
Adult↗
[The Raman spectra study on crystal-octadecyl hydrogen maleate (OHM)].
Raman spectra of crystal-octadecyl hydrogen maleate (OHM), whose geometric disposition of the experiment has y (zx) y y(zz)y, and y(xz)y, y(xx)y respectively, have been recorded and analyzed with the purpose of understanding the structure of OHM crystal. It shows that some of the Raman-active modes of alkyl chain appear polarization. The analysis for crystal structure indicates that the molecular of OHM arrange in layers along [100] and [001] by the mode of dimers, and the molecular layers of chain pile up along [010]. The other groups of OHM corresponding Raman vibration peaks have been analysed as well.
English Abstract↗
Effects of chronic administration of lisuride hydrogen maleate on aromatic amine and metabolite levels in the gerbil brain following bilateral common carotid ligation.
Cerebral monoaminergic neurotransmitters and their metabolites show various concentration changes in gerbils following bilateral carotid ligation. The present study evaluated the effect of chronic administrations of lisuride hydrogen maleate (lisuride) on these changes. Lisuride (0.01 mg/kg or 0.05 mg/kg) or vehicle was intraperitoneally administered to gerbils for 14 consecutive days before the induction of a 30 min ischemia by bilateral carotid ligation. Animals were sacrified immediately and the levels of dopamine, DOPAC, homovanillic acid, noradrenaline, serotonin and 5-hydroxyindoleacetic acid determined by HPLC in the striatum, cortex, hippocampus and diencephalon/midbrain. Lisuride itself had no effect on any compound determined in any region. In the carotid-ligated gerbil brain, however, lisuride corrected the reduction of dopamine in the striatum, normalized or reduced increases in the (DOPAC+homovanillic acid)/dopamine ratio in the striatum, hippocampus and diencephalon/midbrain, and increased the levels of serotonin in all four regions. The present study, together with previous reports, indicate that lisuride may interfere with ischemia-induced cerebrovascular disturbances and, in such a way, improve some pathological sequelae of cerebrovascular disease.
Animals↗