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At least 19 recordsLinked to original sources
PubMed1981

Tiapamil, a new calcium antagonist. 1. Demonstration of calcium antagonistic activity and related studies.

N-(3,4-Dimethoxyphenethyl)-2-(3,4-dimethoxyphenyl)-N-methyl-m-dithiane-2-propylamine-1,1,3,3-tetraoxide hydrochloride (tiapamil, Ro 11-1781), a new homoveratrylamine derivative, was studied under various experimental conditions which allow the recognition of calcium antagonistic activity, and compared with the reference calcium antagonist verapamil. Similar to verapamil, tiapamil inhibited in a concentration-dependent manner calcium-induced contractions in isolated, potassium-depolarized preparations of rat renal artery, dog coronary artery and rabbit main pulmonary artery. The inhibitory effects of tiapamil and verapamil were overcome by raising the calcium concentration of the bath fluid and a competitive antagonism between calcium ions and both compounds was found. In the rabbit main pulmonary artery both tiapamil and verapamil reduced 45Ca influx into the potassium-depolarized vascular smooth muscle cells. Calcium-mediated slowly rising potentials were evoked in partially depolarized guinea-pig papillary muscles by electrical stimulation in the presence of isoprenaline. Tiapamil, like verapamil, inhibited the slow potentials, an effect which was antagonized by elevation of the concentration of calcium or isoprenaline in the bath fluid. Both tiapamil and verapamil decreased contractile force in isolated guinea-pig atria and papillary muscles as well as in isolated cat hearts. In the last preparation the two compounds also reduced heart rate and increased coronary flow. These results characterize tiapamil as a calcium antagonist in both vascular smooth muscle and cardiac muscle. A comparison between tiapamil and verapamil indicated that both drugs are of approximately equal calcium antagonistic potency in coronary vascular smooth muscle, but verapamil is 5--10 times more potent in smooth muscle of other arterial beds and in cardiac muscle. Thus tiapamil appears to be a calcium antagonist with some preference for coronary vascular smooth muscle.

Anesthetics, Local↗
PubMed2005

A randomized, observer-blind, controlled trial of the traditional Chinese medicine Yi-Gan San for improvement of behavioral and psychological symptoms and activities of daily living in dementia patients.

OBJECTIVE: This randomized, observer-blind, controlled trial examined the efficacy and safety of the traditional Chinese herbal medicine Yi-Gan San (YGS, Yokukan-San in Japanese) in the improvement of behavioral and psychological symptoms of dementia (BPSD) and activities of daily living (ADL). METHOD: Fifty-two patients with mild-to-severe dementia (24 men and 28 women, mean +/- SD age = 80.3 +/- 9.0 years) according to DSM-IV criteria were investigated. Participants were randomly assigned to the YGS group (N = 27) or control (drug-free) group (N = 25) and treated for 4 weeks. The Neuropsychiatric Inventory (NPI) for the assessment of BPSD, the Mini-Mental State Examination (MMSE) for cognitive function, and the Barthel Index for ADL were administered at baseline and the end of the treatment. The frequency of extrapyramidal symptoms (EPS) and other adverse events was recorded. If patients showed insufficient response to treatment after 1 week, tiapride hydrochloride, a dopamine D(1) selective neuroleptic, was added to the regimen. Data were collected from January 2004 to March 2004. RESULTS: All participants in both groups completed the trial. In the control group, 11 patients required treatment with tiapride hydrochloride. Significant improvements in mean +/- SD NPI (from 37.9 +/- 16.1 to 19.5 +/- 15.6) and Barthel Index (from 56.4 +/- 34.2 to 62.9 +/- 35.2) scores were observed in the YGS group, but not in the control group. MMSE results were unchanged in both groups. EPS were not observed in either group, but dizziness and impaired postural sway were observed in 6 patients treated with tiapride hydrochloride. CONCLUSION: Yi-Gan San improves BPSD and ADL. Follow-up studies using a double-blinded, placebo-controlled design are recommended.

Activities of Daily Living↗
PubMed2006

[Facial chorea and hemichorea due to cardiogenic cerebral embolism in the cortex and subcortical white matter].

A 62-year-old man was admitted to our hospital because of suddenly developed bilateral facial chorea and left-sided hemichorea. He had neither hemiparesis nor sensory disturbance. Diffusion-weighted magnetic resonance images of the brain showed acute cortical and subcortical infarctions at the right insula, frontal, temporal and parietal lobes. Tiapride hydrochloride was administered for his chorea. The chorea disappeared on the next day. We diagnosed him as cardiogenic cerebral embolism because he had a paroxysmal atrial fibrillation. We supposed that his chorea was induced by interruption of excitatory output from cerebral cortex to striatum and subthalamic nucleus. Contralateral cortical and subcortical infarction must be considered when a patient suddenly develops hemichorea.

Acute Disease↗
PubMed1982

[Tiapride therapy of centrally produced dyskinesia. Examination of the serum levels of protein, LH and FSH (author's transl)].

The effect of N-(2-diethylaminoethyl)-2-methoxy-5-(methylsulfonyl)-benzamide hydrochloride (tiapride, Tiapridex), a dopamine antagonist, on the serum levels of prolactin, luteinising hormone (LH) and follicle-stimulating hormone (FSH) was studied on 20 healthy individuals and 10 patients with dyskinesia resulting from extrapyramidal disorders. Daily doses of 300 mg in healthy subjects and 300-800 mg in patients with dyskinesia resulted from CNS disorders, were found to increase serum prolactin levels without causing amenorrhoea or galactorrhoea. The drug seemed to have no effect on LH and FSH concentrations in the serum.

Adult↗
PubMed2006

Non-neuroleptic catecholaminergic drugs for neuroleptic-induced tardive dyskinesia.

BACKGROUND: Tardive dyskinesia (TD) is a disabling movement disorder associated with the prolonged use of neuroleptic medication. Several strategies have been examined in the treatment of TD. Currently, however, there is no clear evidence of the effectiveness of these drugs in TD and they have been associated with many side effects. One particular strategy would be to use pharmaceutical agents which are known to influence the catecholaminergic system at various junctures. OBJECTIVES: To determine whether catecholaminergic drugs for people with schizophrenia or other chronic mental illnesses are associated with a reduction in neuroleptic-induced tardive dyskinesia. SEARCH STRATEGY: We searched the Cochrane Schizophrenia Group's Register (January 1996), Biological Abstracts (1982-1995), EMBASE (1980-1995), LILACS (1982-1996), MEDLINE (1966-1995) and PsycLIT (1974-1995). We searched the Cochrane Schizophrenia Group's Register again in December 2002 and September 2005. We also searched references of all relevant studies for further trial citations and contacted principal authors of trials. SELECTION CRITERIA: We selected studies if they were randomised controlled trials focusing on people with schizophrenia or other chronic mental illnesses who also suffered from neuroleptic-induced tardive dyskinesia. We compared the use of catecholaminergic interventions versus placebo or no intervention. DATA COLLECTION AND ANALYSIS: We independently extracted data. For homogenous dichotomous data, we calculated the random effects, relative risk (RR), and 95% confidence interval (CI) and, where appropriate, the numbers needed to treat (NNT) on an intention-to-treat basis. For continuous data, we calculated weighted mean differences (WMD). MAIN RESULTS: We excluded 20 studies, mainly due to an inability to extract data from the first arm of the study crossover. One included study has shown that patients on placebo were no more likely to leave the study early than those on tiapride (n=24). The other included study (n=35) also reported equivocal data (RR 5.28 CI 0.3 to 102.6) for leaving the study early when participants were randomised to either celiprolol or placebo. However, in both studies, sample size was limited. AUTHORS' CONCLUSIONS: Although there has been a large amount of research in this area, most studies were excluded due to inherent problems in the nature of their crossover designs. Usually data are not reported before the crossover and the nature of TD and its likely response to treatments makes it imprudent to use this data. The review provides little usable information for service users or providers and more well designed and reported studies are indicated.

Anti-Dyskinesia Agents↗
PubMed1979

Dimeditiapramine (Ro 11-1781), a new calcium antagonist, in the management of supraventricular tachyarrhythmias in patients with acute myocardial infarction.

18 patients with acute myocardial infarction and sustained arrhythmias were treated with a new Ca2+ antagonist, Ro 11-1781, at the dose of 1.0 mg/kg i.v. The drug was effective in reducing heart rate to less than 90 beats/min in 9/10 patients with atrial fibrillation, in 3/4 patients with atrial flutter and in 3/4 patients with supraventricular tachycardia. The peak effect was observed within 2--5 min after the intravenous administration of Ro 11-1781. In cases with recurring tachyarrhythmias, the drug was also effective in repetitive administration. Systolic blood pressure was reduced, but severe hypotension (less than 90 mm Hg) was not observed. The atrioventricular conduction in these patients remained unimpaired and asystole did not occur. The drug appears to be an effective and a well tolerated antiarrhythmic agent.

Aged↗
PubMed1979

Concealed accessory pathway and dual AV conduction: drug-dependent reentrant tachycardia.

Electrophysiological studies were performed in a patient with paroxysmal supraventricular tachycardia and a normal surface ECG at the time of the study. Premature atrial stimulation revealed dual AV conduction and an echo zone during AV conduction over the fast and the slow pathway. The prolongation of the AV conduction time by a calcium antagonist, Ro 11-1781, permitted the induction of tachycardias via both pathways. Premature ventricular stimulation yielded constant VA conduction times with activation of the low right atrium before the high right atrium before the left atrium. During the tachycardia, premature right ventricular beats conducted to the atrium at a time when the AV node and the His bundle would be refractory. The study suggests the simultaneous occurrence of an occult accessory bundle connecting the right ventricle to the right atrium and dual AV conduction.

Adult↗
PubMed1980

Antiarrhythmic effect of the calcium antagonist tiapamil (Ro 11-1781) by intravenous administration in patients with coronary heart disease.

Twenty coronary patients with a median age of 76 years were treated in the coronary care unit with tiapamil, a new Ca2+ antagonist, by intravenous infusion (until December, 1979, the generic name was dimeditiapramine). The following arrhythmias were identified: atrial fibrillation with ventricular rate greater than 95 beats/min (5 patients); supraventricular premature complexes (SVPC) (4 patients); and ventricular premature complexes (VPC), Lown grades 2-4 (15 patients). Electrocardiograms and hemodynamic parameters were continuously monitored prior to, during, and after the therapy. In patients with atrial fibrillation, sinus rhythm was not restored, but tiapamil decreased the ventricular rate by 54%. In patients with VPC, the median frequency of VPC decreased from 310.5 before tiapamil to 32.5 beats/h at the fourth hour of therapy (p less than 0.01). The median ectopic/sinus beat ratio decreased from 0.083 (pretreatment) to 0.008 at the fourth hour of infusion (p less than 0.10). In one of the patient with an insufficient decrease in the number of VPC, the VPOC changed from class 4a (pretreatment) to class 2 (during the therapy), returning to class 4a after the infusion was stopped. Tiapamil reduced the median systolic and diastolic blood pressures by 8.3 and 7.1%, respectively (p less than 0.05), the third hour. Hypotension and bradycardia were observed in 5/20 patients. The results show that tiapamil is effective against both supraventricular and ventricular arrhythmias, and thus its spectrum of action differs from that of other calcium antagonists.

Adult↗
PubMed1983

Long-term tiapamil treatment of patients with angina pectoris.

The effects of a 12-week oral treatment with tiapamil (200 mg t.i.d.) were compared to those of placebo treatment in a group of 20 men with coronary heart disease. There was a slight reduction of anginal symptoms (p less than 0.05) and a tendency to less nitroglycerin consumption (p less than 0.07). There were no statistically significant differences between the treatments in blood pressure, exercise tolerance during repeated exercise tests, ECG conduction intervals, or routine laboratory tests. No adverse side-effects were encountered. It seems that tiapamil may be beneficial in preventing angina pectoris, but a higher oral dose must be used.

Aged↗
PubMed1984

Pharmacokinetics and hemodynamic effects of tiapamil: exercise performance, thallium stress scintigraphy, and radionuclide ventriculography.

The pharmacokinetic behavior and hemodynamic effects of tiapamil, a calcium antagonist, were studied in 16 cardiac patients during an eight-day treatment course, giving oral doses of 600 mg daily. The hemodynamic effects were investigated using exercise performance tests, thallium stress scintigraphy, and radionuclide ventriculography. The areas under the plasma concentration-time curve after the final dose were greater than after the first dose for both tiapamil (+53 per cent) and its metabolite (+24 per cent). One possible explanation is that tiapamil undergoes saturable intestinal wall metabolism. Alternatively, like verapamil, it may undergo a saturable hepatic elimination process. The hemodynamic test series showed that, despite increasing the exercise tolerance, tiapamil significantly reduced the rate-pressure product, an index of myocardial oxygen requirement. Regional myocardial perfusion clearly improved. Ventriculography showed a significant increase in ejection fraction (+18 per cent), cardiac index (+12 per cent), and stroke volume index (+19 per cent). At the same time, the measured mean arterial pressure decreased significantly by about 10 per cent and the calculated peripheral vascular resistance, by about 19 per cent.

Anti-Arrhythmia Agents↗
PubMed1990

Antihypertensive and metabolic effects of tiapamil.

Tiapamil, a new calcium antagonist, was evaluated for its antihypertensive and metabolic effects in a long-term (58 weeks) drug trial in 20 adult outpatient mild to moderately hypertensive subjects. Baseline systolic and diastolic blood pressure dropped after initiation of treatment and was significantly reduced after 4 weeks of treatment, further improving until the termination of the study. There was no impairment of renal and hepatic functions. Electrolytes, plasma aldosterone, plasma renin activity, as well as plasma lipids were not significantly altered during the course of therapy. Fasting blood sugar determinations and oral glucose tolerance test showed significant reductions from the baseline level as a result of the drug treatment. In conclusion, tiapamil is a metabolically safe and effective antihypertensive drug for long-term use.

Adult↗
PubMedDate not supplied

Weak inhibitors protect cholinesterases from strong inhibitors (paraoxon): in vitro effect of tiapride.

Weak and reversible inhibitors of cholinesterases, when administered before potent organophosphorus inhibitors (pretreatment), have the ability, to a certain extent, to protect enzymes from inhibition. Such a protective effect was demonstrated in vitro for metoclopramide and ranitidine. The putative mode of protective action of these substances is, when administered in excess, competition for the active site of the enzyme with the more potent organophosphate. The present paper presents results using another benzamide with weak cholinesterase inhibitory properties: tiapride (TIA). The purpose of the study was to quantify in vitro the extent that TIA conferred protection, using paraoxon (POX) as an inhibitor, and to compare the results with existing data obtained using TIA as a protective agent against dichlorvos (DDVP). POX is a highly toxic non-neuropathic organophosphate. While the use of parathion (the inactive prodrug which is metabolically converted to POX) has been restricted in most countries, the organophosphate is still responsible for a large number of accidental or suicidal exposures. DDVP is a moderately toxic, non-neuropathic organophosphate. Red blood cell (RBC) acetylcholinesterase (AChE) activities in whole blood and butyrylcholinesterase (BChE) activities in human plasma were measured photometrically in the presence of different POX and TIA concentrations and the IC(50) was calculated. Determinations were repeated in the presence of increasing TIA concentrations. The IC(50) of POX increases with the TIA concentration in a linear manner. The protective effect of tiapride on cholinesterase could be of practical relevance in the pretreatment of organophosphate poisoning. It is concluded that in vivo testing of TIA as an organophosphate protective agent is warranted.

Acetylcholinesterase↗
PubMed1997

Tardive jaw tremor.

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Anti-Dyskinesia Agents↗
PubMed1991

Effect of propionyl-L-carnitine on experimental myocardial infarction in dogs.

Limitation on infarct size, using propionyl-L-carnitine (Sigma-Tau) by itself and with the calcium entry blocker, tiapamil (Hoffmann-LaRoche), was evaluated in two groups of ten dogs each, during chronic (9 days) myocardial infarction. There were eight dogs that served as the control group. A closed-chest model was used to produce the thrombus by placing a helically shaped copper wire in the LAD by catheter technique, under x-ray visualization. Necrotic tissue in serial transventricular sections were delineated by triphenyltetrazolium chloride and measured by computer technique, using an IBM PC interfaced with a digitizing pad, 9 days following occlusion. The mean total amount of necrosis in the propionyl-L-carnitine (7.4%) and the propionyl-L-carnitine/tiapamil (6.7%) groups were significantly less (p less than .01) than found in the control (14.1%) group, reflecting a difference of 50 and 58%, respectively, between the treated groups and control. A number of significant between-group comparisons (p less than .05 to p less than .001), under the same conditions, were found for various ischemia, hemodynamic, and hematologic variables followed before and at 30, 60, 90, 120, and 180 minutes after occlusion, as well as on the second and ninth day. The results of this study strongly suggest that propionyl-L-carnitine and propionyl-L-carnitine with tiapamil has a protective effect on myocardial function, following thrombotic occlusion of the LAD, as well as limiting the resulting infarct size.

Animals↗
PubMed1985

Effects of tiapride in tardive dyskinesia.

Tiapride, a selective D2 dopaminergic receptor blocking agent from the substituted benzamide class, was evaluated in a blind video-controlled trial in 10 psychiatric patients with tardive dyskinesia. There was a significant decrease in dyskinesia with a parallel increase in parkinsonism. This relationship between two opposite effects on movement suggests a common pathophysiological basis lying on a reciprocal hyper- and hypoactivity of the dopaminergic striatal system. Nevertheless, other mechanisms may be involved, for the evolution of individual parkinsonian and dyskinesia scores is not necessarily opposite: the tiapride-induced parkinsonism was generally acceptable and in two cases, the dyskinesia scores were reduced without an increase in parkinsonism. Therefore, more dyskinetic patients have to be evaluated in long-term studies with tiapride, before this drug could be recommended in tardive dyskinesia, when dyskinetic movements become intolerable.

Adult↗
PubMed1981

Acute dyskinesias in monkeys elicited by halopemide, mezilamine and the "antidyskinetic" drugs, oxiperomide and tiapride.

Oxiperomide and tiapride are dopamine receptor antagonists claimed to have "antidyskinetic" properties in animal models and the clinic. Halopemide and mezilamine are other dopamine antagonists predicted to lack extrapyramidal side effects in man on the basis of animal studies. Acute dyskinesias, a neuroleptic-induced acute extrapyramidal syndrome, were elicited in squirrel monkeys by oxiperomide (1 mg/kg), tiapride (30 mg/kg), and halopemide (10 mg/kg). The dyskinesias were virtually indistinguishable from those caused by a standard behaviorally equivalent dose of haloperidol (1.25 mg/kg PO) in the same individual monkeys. Mezilamine (0.3 mg/kg) also induced dyskinesias, which appeared to be less pronounced than those following haloperidol. The antidyskinetic properties of oxiperomide and tiapride evidently do not confer protection against dyskinetic movements induced by dopamine antagonism.

Animals↗