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1.
Am J Cardiol ; 53(6): 684-8, 1984 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-6367415

RESUMO

A new calcium ion antagonist, gallopamil, 150 mg/day, was compared with propranolol, 240 mg/day, in 20 patients with stable chronic angina. The patients were studied in a randomized, placebo-controlled, double-blind, crossover trial. Multistage treadmill exercise with computer-assisted electrocardiographic analysis was performed after 2 weeks of placebo therapy and at the end of each 4-week active treatment period. The mean (+/- standard error of the mean) exercise time to development of angina was 5.4 +/- 0.3 minutes with placebo; this increased to 9.4 +/- 0.7 minutes with propranolol (p less than 0.001) and 10.1 +/- 0.7 minutes with gallopamil (p less than 0.001 vs placebo; difference not significant vs propranolol). Both drugs significantly prolonged the time to development of 1 mm of ST depression. Five patients became free of angina during treadmill testing with gallopamil therapy and 2 with propranolol. Both drugs decreased the heart rate at rest; propranolol also decreased the maximal exercise heart rate, which was slightly increased with gallopamil. With the exception of 1 patient in whom raised liver enzymes developed, gallopamil was well tolerated. Thus, gallopamil is an effective antianginal agent that has few of the unwanted effects associated with other calcium channel-blocking drugs.


Assuntos
Angina Pectoris/tratamento farmacológico , Galopamil/uso terapêutico , Propranolol/uso terapêutico , Verapamil/uso terapêutico , Idoso , Ensaios Clínicos como Assunto , Método Duplo-Cego , Eletrocardiografia , Teste de Esforço , Feminino , Galopamil/efeitos adversos , Frequência Cardíaca/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Propranolol/efeitos adversos , Distribuição Aleatória
2.
Drugs ; 47(1): 93-115, 1994 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-7510624

RESUMO

Gallopamil is a methoxy derivative of verapamil. As is typical of the phenylalkylamine class of calcium antagonists, it acts on the vascular system, and on the heart and its nodal structures. In the treatment of stable angina pectoris, gallopamil is at least as effective as nifedipine and diltiazem, though apparently better tolerated than nifedipine. Typical of calcium antagonists there is little or no tolerance to the antiischaemic effects of gallopamil. Preliminary studies indicate that gallopamil, like other calcium antagonists, has cardioprotective potential. However, further investigation is required to explore the clinical relevance of the improved myocardial regional perfusion and free fatty acid utilisation in reversibly ischaemic regions, and the potential of delayed ischaemia during angioplasty that is observed during gallopamil administration. Gallopamil is well tolerated, exhibiting a low propensity for causing cardiovascular and gastrointestinal adverse effects, thus making it a suitable alternative to other calcium antagonists for the treatment of patients with ischaemic heart disease.


Assuntos
Galopamil/farmacologia , Galopamil/uso terapêutico , Isquemia Miocárdica/tratamento farmacológico , Animais , Galopamil/efeitos adversos , Galopamil/farmacocinética , Humanos
3.
Int J Cardiol ; 19(3): 315-25, 1988 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-3294189

RESUMO

In a randomized double-blind crossover trial 30 patients with chronic stable angina were studied to compare the antianginal actions of gallopamil (150 mg/day) and nifedipine. With the initial nifedipine dose of 60 mg/day, the trial had to be stopped because of severe exacerbation of angina in 3 patients of the nifedipine group. Twenty-one patients were entered into a second protocol with the nifedipine dose reduced to 30 mg/day. Compared to the preceding placebo period, the exercise time to onset of angina (+ 30%, P less than 0.01) and the total exercise time (+ 18%, P less than 0.01) were prolonged by gallopamil but not by nifedipine (+ 20 and 13%, respectively, not significant) with no significant difference between the test drugs. Four patients became free of angina during exercise testing with gallopamil therapy and one patient with nifedipine. Both agents significantly reduced ST depression at maximal comparable workload by 77% (gallopamil) and 52% (nifedipine) compared with placebo; the difference between the drugs reached borderline significance (P = 0.055). The increase in heart rate and the rate-pressure product at maximal comparable workload was less with gallopamil than with nifedipine (P less than 0.01). In contrast to nifedipine, very few side effects were reported with gallopamil. Thus, gallopamil is an effective antianginal agent whose therapeutic to toxic ratio appears to be superior to that of nifedipine.


Assuntos
Angina Pectoris/tratamento farmacológico , Eletrocardiografia , Teste de Esforço , Galopamil/uso terapêutico , Nifedipino/uso terapêutico , Adulto , Idoso , Ensaios Clínicos como Assunto , Circulação Coronária/efeitos dos fármacos , Método Duplo-Cego , Feminino , Galopamil/efeitos adversos , Sistema de Condução Cardíaco/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Nifedipino/efeitos adversos , Distribuição Aleatória
5.
Z Kardiol ; 72(12): 746-54, 1983 Dec.
Artigo em Alemão | MEDLINE | ID: mdl-6421002

RESUMO

The effects of the calcium-channel-blocking agent Gallopamil (D 600) were assessed in 20 patients with stable exertional angina pectoris in a randomized placebo-controlled double-blind protocol using serial exercise tests. Both after a single oral dose and during long-term treatment over 3 weeks, Gallopamil caused a dose-dependent increase in exercise duration and a reduction in ischemic ST segment depression that became clinically relevant using single doses of 50 mg. Since the rate-pressure product was not significantly affected by Gallopamil, its anti-anginal action cannot adequately be explained by a reduction in myocardial oxygen consumption as a result of this mechanism. The only side effects observed were asymptomatic second-degree sinoatrial block in one and first-degree atrioventricular block in another patient, each on 150 mg gallopamil daily. It thus seems justifiable to study the effectiveness of higher doses.


Assuntos
Angina Pectoris/tratamento farmacológico , Galopamil/uso terapêutico , Verapamil/uso terapêutico , Adulto , Idoso , Ensaios Clínicos como Assunto , Método Duplo-Cego , Eletrocardiografia , Feminino , Galopamil/efeitos adversos , Humanos , Assistência de Longa Duração , Masculino , Pessoa de Meia-Idade , Distribuição Aleatória
6.
Eur J Clin Pharmacol ; 42(3): 271-3, 1992.
Artigo em Inglês | MEDLINE | ID: mdl-1577045

RESUMO

The clinical efficacy of a new slow release preparation of the calcium antagonist gallopamil was assessed in 20 patients by diary cards and treadmill exercise tests. A single blind phase of two week periods of placebo, gallopamil 100 mg o.d. and gallopamil 100 mg b.i.d., blinded to the patient, was followed in 18 patients by a double blind comparison of gallopamil 100 mg od versus 100 mg b.i.d. Angina frequency and trinitrin consumption per week were both significantly less on high dose (2.7 and 1.7) than on low dose (5.4 and 3.4) respectively. Treadmill total exercise time was longer on high dose (523s) than low dose (449s). Other exercise test parameters showed similar improvements on high dose treatment. Gallopamil was well tolerated. PR interval correlated best with plasma gallopamil level, while exercise test parameters correlated best with the log plasma level of its major metabolite nor-gallopamil.


Assuntos
Angina Pectoris/tratamento farmacológico , Galopamil/administração & dosagem , Adulto , Idoso , Angina Pectoris/fisiopatologia , Doença Crônica , Preparações de Ação Retardada , Método Duplo-Cego , Exercício Físico/fisiologia , Feminino , Galopamil/efeitos adversos , Humanos , Masculino , Pessoa de Meia-Idade , Fatores de Tempo
7.
Z Kardiol ; 78 Suppl 5: 25-8, 1989.
Artigo em Alemão | MEDLINE | ID: mdl-2698563

RESUMO

Severe adverse effects associated with the use of calcium channel blockers do not occur very often. Sometimes nifedipin produces hypotension, tachycardia, and headache, whereas verapamil, gallopamil, and dilitiazem show more negative chronotropic effects such as bradycardia or sinuatrial and atrioventricular nodal conduction disturbances. Gastrointestinal side effects are constipation after verapamil and stomach problems after gallopamil.


Assuntos
Bloqueadores dos Canais de Cálcio/efeitos adversos , Galopamil/efeitos adversos , Arritmias Cardíacas/induzido quimicamente , Humanos , Contração Miocárdica/efeitos dos fármacos , Relação Estrutura-Atividade , Vasodilatação/efeitos dos fármacos
8.
Arzneimittelforschung ; 41(8): 789-93, 1991 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-1781798

RESUMO

In order to assess the efficacy and tolerability of gallopamil (D-600, CAS 16662-47-8) by long-term venous infusion in the treatment of spontaneous angina, 15 consecutive patients were studied in a single-blind, self-controlled trial versus placebo. Following a 24-h Holter ECG recording of the patients receiving a saline infusion (run-in phase), i.v. administration of gallopamil was started at a dose of 0.02 mg/kg/h preceded by a 0.03 mg/kg bolus. After 24 h, the dosage was increased to 0.03 mg/kg/h and the infusion was maintained for another 48 h. The Holter ECG recording was repeated in the last 24 h of treatment and after 6 h from withdrawal (washout phase). The reduction in the number of angina attacks, as shown by a comparison between the average of the two placebo periods (run-in and washout phases) and the three days of treatment, was 68.2%, 92.5%, and 87%, respectively. Consumption of glyceryl trinitrate decreased by 92.5% on each one of the three days of treatment. The reduction in the number of ischemic episodes (IEs) with symptomatic (-91.6%) and silent (-98.0%) ST elevation, and with symptomatic (-100%) and silent (-90%) ST depression, also proved significant. Heart rate decreased only moderately. One patient showed a mild first-degree heart block, while another suffered a transient episode of isorhythmic A-V dissociation. In conclusion, when administered by venous infusion, gallopamil has been found to be well tolerated and highly effective in the treatment of spontaneous angina.(ABSTRACT TRUNCATED AT 250 WORDS)


Assuntos
Angina Pectoris/tratamento farmacológico , Galopamil/uso terapêutico , Adulto , Pressão Sanguínea/efeitos dos fármacos , Angiografia Coronária , Eletrocardiografia Ambulatorial , Feminino , Galopamil/administração & dosagem , Galopamil/efeitos adversos , Frequência Cardíaca/efeitos dos fármacos , Humanos , Infusões Intravenosas , Masculino , Pessoa de Meia-Idade , Nitroglicerina/uso terapêutico , Método Simples-Cego
9.
J Cardiovasc Pharmacol ; 20 Suppl 7: S57-63, 1992.
Artigo em Inglês | MEDLINE | ID: mdl-1284158

RESUMO

Symptomatic and asymptomatic episodes of transient myocardial ischemia are well-known risk factors in patients with coronary artery disease. In a single-blind, randomized, and placebo-controlled study, the efficacy and safety of gallopamil was studied during a 1-week treatment period in 25 patients with high-grade coronary artery stenosis and frequent, exercise-induced episodes of myocardial ischemia. Eighteen patients were men, and seven patients were women; the mean age +/- SD was 59 +/- 7 years. After a 1-week run-in period (days 1-7), all patients were treated with gallopamil 50 mg t.i.d. (days 8-14) and placebo t.i.d. (days 15-21) or vice versa. Twenty-four-hour Holter monitoring, exercise testing, and adverse effects were controlled at days 7, 14, and 21. During the run-in period, all patients suffered a mean of 5.9 +/- 2.9 episodes of transient myocardial ischemia, mean ischemic duration was 38 +/- 29 min/day. Gallopamil increased exercise tolerance from 7.9 to 9.8 min (+24%, p < 0.05) and resulted in reduction of the weekly usage of short-acting nitrates by 45% compared to placebo. During 24-h Holter monitoring, mean heart rate at the onset of ST-segment depression increased from 106 to 118 beats/min (p < 0.05). The frequency of daily ischemic episodes was reduced after gallopamil administration from 6.1 to 3.9 episodes/day (-37%, p < 0.05), the total ischemic burden decreased for symptomatic episodes by -54% (p < 0.05) and for asymptomatic episodes by 29% (p < 0.05). Gallopamil modified the circadian distribution of ischemic episodes by modifying the morning peak of transient myocardial ischemia.(ABSTRACT TRUNCATED AT 250 WORDS)


Assuntos
Doença das Coronárias/tratamento farmacológico , Exercício Físico , Galopamil/uso terapêutico , Idoso , Arritmias Cardíacas/prevenção & controle , Ritmo Circadiano/efeitos dos fármacos , Doença das Coronárias/etiologia , Doença das Coronárias/fisiopatologia , Eletrocardiografia , Eletrocardiografia Ambulatorial , Teste de Esforço , Feminino , Galopamil/efeitos adversos , Humanos , Masculino , Pessoa de Meia-Idade
10.
J Cardiovasc Pharmacol ; 20 Suppl 7: S88-94, 1992.
Artigo em Inglês | MEDLINE | ID: mdl-1284163

RESUMO

The anti-ischemic properties and tolerability of a slow-release formulation (SR) of gallopamil were investigated in 118 patients with exercise-inducible ST-segment depression and stable angina pectoris in this double-blind, randomized, placebo-controlled, multicenter study. After a placebo run-in period (A) of 2-7 days and a 7-day open therapy period (B) with gallopamil SR, the patients were randomized to a double-blind 7-day period (C) to receive placebo or gallopamil SR 100 mg twice a day. Each patient was submitted to gradual upright bicycle ergometry and electrocardiography (ECG) at rest on the last 2 days of each period at 6 and 12 h postadministration (p.a.) In period C, exercise time and exercise tolerance remained significantly prolonged at 6 and 12 h after gallopamil SR administration in comparison with the placebo values. Additionally the sum of ST-segment depression and maximal ST-segment depression were significantly reduced by gallopamil SR at 6 h p.a. as were the frequency of angina attacks and nitroglycerin consumption. Four patients were withdrawn from the study because of gallopamil-related adverse events, which, however, were not serious. Constipation was noted in 2.5% of the patients. These data suggest that gallopamil SR is effective in reducing exercise-inducible ST-segment depression and increasing exercise tolerance with no serious adverse effects in patients with stable angina pectoris.


Assuntos
Angina Pectoris/tratamento farmacológico , Exercício Físico , Galopamil/uso terapêutico , Adulto , Idoso , Angina Pectoris/fisiopatologia , Preparações de Ação Retardada , Eletrocardiografia , Feminino , Galopamil/administração & dosagem , Galopamil/efeitos adversos , Hemodinâmica/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade
11.
Arzneimittelforschung ; 34(11): 1587-94, 1984.
Artigo em Alemão | MEDLINE | ID: mdl-6543136

RESUMO

Efficacy and tolerance of gallopamil (Procorum) were investigated over a period of 1 year under practice conditions in a total of 455 patients (254 male, 201 female), aged 62 years (male) and 66 (female) on an average, with electrocardiographically confirmed coronary heart disease. The most frequently applied dosage was 1 film-coated tablet of gallopamil 50 mg 2-3 times daily. Frequency of attacks and nitro consumption as criteria of efficacy decreased by an average of approx. 80% in comparison to the placebo period. Full effectiveness was usually reached 4 weeks after start of therapy. ST-depression under exercise diminished by approx. 50%. An improved exercise tolerance was likewise observed, especially in patients who only tolerated up to 100 Watt prior to therapy. Therapeutic success was defined as good in 73% of the cases, satisfactory in 17.3% and insufficient in 6.7% by the trial physicians - the patient's opinion also being taken into consideration. A decrease of effectiveness was not observed during the one-year therapy. No uniform influence on the laboratory parameters could be revealed. The most frequent side-effects were: gastric discomfort (13 patients), bradycardia (7 patients) and AV-prolongation (3 patients). A total of 77 patients (16.9%) had to discontinue therapy. 29 out of these discontinuations were not therapy-related (drop-outs); 12 were based on an insufficient therapeutic success, 13 on hospitalization, 11 on extracardiac, 4 on cardiac adverse reactions and 8 patients (1.8%) died during the study. In a global assessment the trial physicians described the tolerability as good in 92% of the patients, fair in 2.9% and poor in 2.4%.(ABSTRACT TRUNCATED AT 250 WORDS)


Assuntos
Doença das Coronárias/tratamento farmacológico , Galopamil/uso terapêutico , Verapamil/uso terapêutico , Adulto , Idoso , Angina Pectoris/tratamento farmacológico , Pressão Sanguínea/efeitos dos fármacos , Eletrocardiografia , Feminino , Galopamil/efeitos adversos , Frequência Cardíaca/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Fatores de Tempo
12.
Cardiologia ; 35(5): 407-14, 1990 May.
Artigo em Italiano | MEDLINE | ID: mdl-2125241

RESUMO

The efficacy of a new calcium channel blocker, gallopamil, has been tested via a single blind, self-controlled versus placebo protocol in 9 consecutive patients admitted to our Coronary Care Unit because of repeated daily attacks of Prinzmetal variant angina. Exclusion criteria were age (greater than 65 years) bradycardia (less than 50 beats/min), recent myocardial infarction, heart failure, sinoatrial or atrioventricular block. After a 24 hours run-in period on saline drip, gallopamil was administered as 0.03 mg/kg bolus followed by continuous infusion at 0.02 mg/kg/h for the first 24 hours and 0.03 mg/kg/h for the last 48 hours. Treatment was then stopped and the patients were again kept on saline infusion for the next 30 hours. Holter monitoring was recorded during run-in, on third day of treatment and 6 hours after gallopamil withdrawal. Anginal attacks were significantly reduced in number by therapy (-63%, -91%, -84% in the 3 days of treatment). Holter monitoring during gallopamil infusion showed a statistically significant reduction in silent (-98%) and symptomatic (-93%) ischemic episodes (IE). During the last 24 hours of the washout period we observed a statistically significant increase in silent ischemic episodes. While no transient ST segment elevation was recorded in 3 patients, in 1 patient symptomatic IE were increased of 150% with respect to the run-in period. On the whole we observed complete suppression of IE in 7 patients (78%) at the third day of treatment with gallopamil. In 2 patients (22%) a greater than 75% reduction was observed.(ABSTRACT TRUNCATED AT 250 WORDS)


Assuntos
Angina Pectoris Variante/tratamento farmacológico , Galopamil/uso terapêutico , Adulto , Doença das Coronárias/complicações , Doença das Coronárias/fisiopatologia , Eletrocardiografia Ambulatorial , Feminino , Galopamil/administração & dosagem , Galopamil/efeitos adversos , Frequência Cardíaca/efeitos dos fármacos , Humanos , Infusões Intravenosas , Masculino , Pessoa de Meia-Idade , Nitroglicerina/administração & dosagem , Nitroglicerina/uso terapêutico , Recidiva , Método Simples-Cego
13.
Cardiology ; 88(4): 353-60, 1997.
Artigo em Inglês | MEDLINE | ID: mdl-9197430

RESUMO

We evaluated the efficacy and safety of daily administration of gallopamil 150 mg/day and its effects on myocardial perfusion in a medium-term, randomized, double-blind, cross-over, placebo-controlled trial. We studied 19 patients (17 males and 2 females; mean age 57 +/- 6.8 years) with stable effort angina, angiographically documented coronary artery disease and reversible perfusion defects during exercise thallium-201 myocardial scintigraphy of at least one segment of the left ventricle. After 2 weeks of a single-blind placebo run-in period, during which each patient underwent at least 2 exercise tests and a 48-hour Holter ECG recording, all patients were treated with either placebo or gallopamil 50 mg t.i.d. for 28 days. At the end of this period, patients crossed over to the alternate regimen. This phase was double blind. After treatment with placebo or gallopamil, patients underwent exercise tests, 24-hour Holter ECG recording and thallium-201 myocardial scintigraphy. Weekly angina frequency and trinitroglycerin (TNT) consumption and safety were also evaluated. No patients dropped out of the study because of major side effects. The number of total ischemic and symptomatic events recorded at 24-hour ECG monitoring, weekly angina frequency and TNT consumption were significantly reduced during gallopamil treatment. After gallopamil administration, exercise duration significantly increased (run-in: 419 +/- 116 s, placebo: 420 +/- 118 s, gallopamil: 511 +/- 144 s; p < 0.05), and ST segment depression was significantly reduced (run-in: -1.3 +/- 0.3 mm, placebo: -1.3 +/- 0.3 mm, gallopamil: -0.94 +/- 0.68 mm; p < 0.01), while heart rate, systolic blood pressure and rate-pressure product were unchanged at rest, at submaximal and at peak exercise. Qualitative and quantitative evaluation of myocardial perfusion and the myocardial uptake percentage of thallium-201 in ischemic zones were significantly improved by gallopamil treatment. These findings demonstrate that gallopamil can improve myocardial perfusion and reduce myocardial oxygen consumption.


Assuntos
Angina Pectoris/tratamento farmacológico , Bloqueadores dos Canais de Cálcio/uso terapêutico , Circulação Coronária/efeitos dos fármacos , Galopamil/uso terapêutico , Idoso , Angina Pectoris/diagnóstico por imagem , Angina Pectoris/fisiopatologia , Bloqueadores dos Canais de Cálcio/efeitos adversos , Angiografia Coronária , Estudos Cross-Over , Método Duplo-Cego , Eletrocardiografia Ambulatorial , Teste de Esforço , Feminino , Seguimentos , Galopamil/efeitos adversos , Hemodinâmica , Humanos , Masculino , Pessoa de Meia-Idade , Cintilografia , Segurança , Radioisótopos de Tálio , Resultado do Tratamento
14.
Cardiologia ; 38(7): 455-62, 1993 Jul.
Artigo em Italiano | MEDLINE | ID: mdl-8221740

RESUMO

In the setting of stable effort angina a single-blind, randomized, cross-over study to evaluate the effects of gallopamil (GAL) and amlodipine (AML) on exercise tolerance and ischemic ST depression was conducted. Fifteen outpatients, 12 males and 3 females, aged 40-65 years (57 +/- 9), with documented coronary atherosclerosis and reproducible ST-segment depression on 2 consecutive baseline exercise stress tests, completed the study, which consisted of 4 periods: 1 and 3 placebo, 2 and 4 at random GAL (50 mg tid) and AML (10 mg/daily). At the end of each period a multistage treadmill exercise stress test (Bruce protocol) was performed. Both drugs significantly (p = 0.0001) increased the ischemia time (IT) (0.1 mV ST depression) as compared to placebo, from 416 +/- 165 s to 635 +/- 161 s (GAL) and 607 +/- 152 s (AML) with significant difference (p = 0.2) between the 2 drugs, and reduced significantly (p = 0.001) the maximal ST depression from -0.25 +/- 0.09 mV to -0.11 +/- 0.08 mV (GAL) and -0.12 +/- 0.09 mV (AML). At the IT, the systolic blood pressure increased from 178 +/- 23 mmHg to 185 +/- 20 mmHg (GAL) and remained unchanged during AML treatment (178 +/- 15 mmHg); similarly, the heart rate increased from 126 +/- 22 b/min to 139 +/- 21 b/min (GAL) and 138 +/- 19 b/min (AML). In conclusion, both GAL and AML showed a good anti-ischemic effect (IT = +52.6% during GAL and +45.9% during AML), even if GAL proved to be significantly more effective than AML.


Assuntos
Anlodipino/uso terapêutico , Angina Pectoris/tratamento farmacológico , Teste de Esforço/métodos , Galopamil/uso terapêutico , Isquemia Miocárdica/tratamento farmacológico , Esforço Físico/efeitos dos fármacos , Adulto , Idoso , Anlodipino/efeitos adversos , Análise de Variância , Angina Pectoris/diagnóstico , Angina Pectoris/epidemiologia , Teste de Esforço/estatística & dados numéricos , Feminino , Galopamil/efeitos adversos , Humanos , Masculino , Pessoa de Meia-Idade , Isquemia Miocárdica/diagnóstico , Isquemia Miocárdica/epidemiologia , Método Simples-Cego
15.
Eur Heart J ; 13(4): 526-30, 1992 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-1600993

RESUMO

Anti-ischaemic properties and tolerability of the calcium antagonist gallopamil were compared with those of nifedipine in a double-blind cross-over study performed in 20 patients affected by effort or mixed angina. The patients were of both sexes and aged 43-66 years; coronary angiography performed on 18 of them revealed at least one-vessel disease (stenosis greater than 70%). After a one week wash-out period the patients received placebo for 2 weeks; thereafter 10 patients were treated orally with gallopamil 150 mg daily and 10 patients with nifedipine 60 mg daily for 4 weeks. Before crossing-over to the alternate therapy a 2-week placebo period was allowed. The patients underwent cycloergometric exercise tests after each phase of treatment; workload was increased by 25 W every 3 min and the test was stopped in the presence of a typical angina or ST segment depression or age-predicted maximal heart rate. The results show that both exercise time and maximal workload were significantly increased by gallopamil and by nifedipine in comparison with placebo; also the maximal ST segment depression was significantly reduced by the two drugs. The number of patients developing angina and/or segment depression during exercise test was significantly reduced by both drugs compared to placebo. Time to onset of angina and time to ST depression greater than or equal to 1 mm were increased, though not significantly, by both calcium antagonists. No side effects were recorded with gallopamil while with nifedipine six patients reported side effects.(ABSTRACT TRUNCATED AT 250 WORDS)


Assuntos
Doença das Coronárias/tratamento farmacológico , Eletrocardiografia/efeitos dos fármacos , Teste de Esforço/efeitos dos fármacos , Galopamil/uso terapêutico , Nifedipino/uso terapêutico , Adulto , Idoso , Angina Pectoris/tratamento farmacológico , Pressão Sanguínea/efeitos dos fármacos , Método Duplo-Cego , Feminino , Galopamil/efeitos adversos , Frequência Cardíaca/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Nifedipino/efeitos adversos
16.
Eur Heart J ; 13(3): 404-10, 1992 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-1597229

RESUMO

The aim of this study was to evaluate the efficacy and possibly the mechanism of action of gallopamil and diltiazem in a double-blind crossover trial in patients with effort ischaemia. Twenty male patients (mean age 57 +/- 6 years) with documented coronary atherosclerosis and exercise-induced ischaemia (ST depression greater than or equal to 0.15 mV) completed the study, which consisted of four 7 day periods. At the end of each period a multistage bicycle exercise stress test was performed under placebo (first and third periods) and randomly under gallopamil (50 mg t.i.d.) or diltiazem (90 mg t.i.d.) in the second and fourth periods. Both drugs significantly increased time to ischaemia (0.15 mV ST depression) as compared to placebo, from 7.9 +/- 1.7 min to 8.9 +/- 1.1 min (diltiazem) and 9.1 +/- 1.6 min (gallopamil) with no significant difference between the two drugs, and reduced the maximal extent of ST shift from 0.18 +/- 0.08 mV to 0.13 +/- 0.04 mV (diltiazem) and 0.12 +/- 0.05 mV (gallopamil). Analysis of the results from the whole population showed that the beneficial effect did not appear to be related to any specific parameter. Individual analysis showed that 13/20 patients under gallopamil and 13/20 under diltiazem increased time to ischaemia, while this was unchanged or reduced in the remainder. A positive correlation between changes in time to ischaemia and changes in rate x pressure product at ischaemia was found in both those administered gallopamil (R 0.80, P less than 0.01) and diltiazem (R 0.65, P less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)


Assuntos
Angina Pectoris/tratamento farmacológico , Diltiazem/uso terapêutico , Galopamil/uso terapêutico , Adulto , Angina Pectoris/etiologia , Pressão Sanguínea/efeitos dos fármacos , Diltiazem/efeitos adversos , Diltiazem/farmacologia , Método Duplo-Cego , Exercício Físico , Teste de Esforço/efeitos dos fármacos , Galopamil/efeitos adversos , Galopamil/farmacologia , Frequência Cardíaca/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Análise de Regressão , Fatores de Tempo
17.
Z Kardiol ; 73(9): 578-85, 1984 Sep.
Artigo em Alemão | MEDLINE | ID: mdl-6391005

RESUMO

UNLABELLED: In 12 male patients with angiographically confirmed coronary heart disease and stable angina the antianginal effects of 50 mg Gallopamil have been studied in comparison with 10 mg Nifedipine and placebo. The study has been carried out using a double-blind cross-over protocol with standardized exercise stress tests. Patients underwent 5 exercise step tests, without any medication and 120 minutes after randomized drug administration (placebo, placebo, Gallopamil, Nifedipine). Both Gallopamil and Nifedipine had good antianginal effects. Following 50 mg Gallopamil, ischemic ST-depression was reduced by 45% compared to placebo and by 50% compared to ergometry without any medication. The reduction of ST-depression after 10 mg Nifedipine was 26% compared to placebo and 31% compared to a drug-free exercise test. Due to the negative chronotropic effects, Gallopamil led to a slight but significant reduction of heart rate at rest and during exercise of about 5%. In contrast, after Nifedipine administration, a reflex-mediated increase in heart rate could be seen. In normotensive patients both channel-blocking agents showed a slight reduction of arterial blood pressure. CONCLUSIONS: The results indicate a considerable antianginal effect of a single oral dose of 50 mg Gallopamil. In comparison to 10 mg Nifedipine this effect is more pronounced.


Assuntos
Angina Pectoris/tratamento farmacológico , Galopamil/uso terapêutico , Nifedipino/uso terapêutico , Verapamil/uso terapêutico , Adulto , Idoso , Pressão Sanguínea/efeitos dos fármacos , Ensaios Clínicos como Assunto , Doença das Coronárias/tratamento farmacológico , Método Duplo-Cego , Eletrocardiografia , Teste de Esforço , Galopamil/efeitos adversos , Galopamil/sangue , Frequência Cardíaca/efeitos dos fármacos , Humanos , Cinética , Masculino , Pessoa de Meia-Idade , Infarto do Miocárdio/tratamento farmacológico , Nifedipino/efeitos adversos , Nifedipino/sangue
18.
Z Kardiol ; 83 Suppl 2: 27-36, 1994.
Artigo em Alemão | MEDLINE | ID: mdl-8091822

RESUMO

When enoximone is acutely administered to patients with stable angina and angiographically proven relevant coronary stenosis i.v. application of 0.75 mg/kg exhibits pronounced antiischemic effects. This could be observed in patients during exercise and in those in whom the ischemia was provoked by rapid cardiac stimulation. The antiischemic effects were documented by relief of symptoms, reduction of ST-depression, improvement of impaired myocardial wall motion, decrease to normalization of pathologically elevated filling pressure, amelioration of coronary blood flow as evidenced by myocard scintigraphy and washout time of an intracoronarily injected echo-contrast medium. There was also a definite improvement of ischemia-caused mitral regurgitation. Similar observations were found when the drug was injected in the diseased coronary arteries in a small dose (0.075 mg/kg) so that peripheral effects were not present. In comparison to the Ca(++)-blocker Gallopamil the antiischemic effects of Enoximone were more pronounced, a synergistic action was, however, observed. Negative dromotropic effects of Gallopamil could be abolished by Enoximone. With oral administration of the drug over a period of one week antiischemic effects could also be documented with Holter monitoring as well as during exercise. There was a reduction of ST-depression both at spontaneously occurring ischemic episodes and during exercise, in the number and duration of episodes of silent ischemia, particularly, however, a decrease in symptomatic episodes. In none of the patients under study proarrhythmic effects were observed.


Assuntos
Doença das Coronárias/tratamento farmacológico , Enoximona/administração & dosagem , Isquemia Miocárdica/tratamento farmacológico , Administração Oral , Cálcio/metabolismo , Circulação Coronária/efeitos dos fármacos , Doença das Coronárias/fisiopatologia , AMP Cíclico/metabolismo , Relação Dose-Resposta a Droga , Eletrocardiografia Ambulatorial/efeitos dos fármacos , Enoximona/efeitos adversos , Teste de Esforço/efeitos dos fármacos , Galopamil/administração & dosagem , Galopamil/efeitos adversos , Hemodinâmica/efeitos dos fármacos , Hemodinâmica/fisiologia , Humanos , Infusões Intravenosas , Contração Miocárdica/efeitos dos fármacos , Contração Miocárdica/fisiologia , Isquemia Miocárdica/fisiopatologia
19.
Z Kardiol ; 83(6): 431-8, 1994 Jun.
Artigo em Alemão | MEDLINE | ID: mdl-7915067

RESUMO

To compare the hemodynamic, antiischemic, metabolic, and neurohumoral effects of intravenous esmolol (beta 1 blocking agent) and gallopamil (verapamil-like calcium channel blocker), 14 patients with angiographically proven CAD and reproducible ST segment depression were studied at rest and during exercise under control conditions and after an intravenous bolus injection of esmolol (0.5 mg/kg/1 min, followed by an infusion with 0.2 mg/kg/min) or gallopamil (0.025 mg/kg/3 min). In contrast to gallopamil, esmolol significantly reduced systolic blood pressure (175.7 vs. 160 mm Hg) and heart rate (107.4 vs. 96.9 min-1) during exercise as well as cardiac output (11.57 vs. 9.38 l/min) and significantly enhanced systemic vascular resistance both at rest (1241 vs. 1479 dynes.s.cm-5) and during exercise (805 vs. 947 dynes.s.cm-5). On the other hand, exercise filling pressures and lactate levels (3.66 vs. 3.05 mmol/l) were significantly reduced by gallopamil only. Thus, the significant improvement of exercise tolerance by both esmolol and gallopamil is based on different mechanisms of action: esmolol improves myocardial ischemia by appreciably reducing myocardial oxygen consumption, whereas gallopamil primarily improves oxygen supply and ventricular performance. Plasma catecholamines, atrial natriuretic factor, and aldosterone levels as well as plasma renin activity were identically influenced by esmolol and gallopamil, respectively. A reflex activation of the sympathetic system did not occur.


Assuntos
Antagonistas Adrenérgicos beta/administração & dosagem , Doença das Coronárias/tratamento farmacológico , Galopamil/administração & dosagem , Isquemia Miocárdica/tratamento farmacológico , Propanolaminas/administração & dosagem , Antagonistas Adrenérgicos beta/efeitos adversos , Idoso , Aldosterona/sangue , Fator Natriurético Atrial/sangue , Angiografia Coronária/efeitos dos fármacos , Circulação Coronária/efeitos dos fármacos , Circulação Coronária/fisiologia , Doença das Coronárias/fisiopatologia , Quimioterapia Combinada , Eletrocardiografia/efeitos dos fármacos , Teste de Esforço/efeitos dos fármacos , Feminino , Galopamil/efeitos adversos , Hemodinâmica/efeitos dos fármacos , Hemodinâmica/fisiologia , Humanos , Infusões Intravenosas , Lactatos/sangue , Ácido Láctico , Masculino , Pessoa de Meia-Idade , Isquemia Miocárdica/fisiopatologia , Norepinefrina/sangue , Propanolaminas/efeitos adversos , Renina/sangue , Método Simples-Cego
20.
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