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PubMed1987

[Concentration-time profile of isosorbide dinitrate and its metabolites in plasma following percutaneous resorption of a transdermal therapeutic system].

Percutaneous absorption of isosorbide dinitrate (ISDN), determined from plasma concentrations of ISDN and its metabolites isosorbide 2-mononitrate (IS-2-MN) and isosorbide 5-mononitrate (IS-5-MN), was studied in 8 healthy subjects aged 19 to 25 years following application of a single plaster containing 40 mg ISDN to the hairless skin on the left side of the chest for 72 h. ISDN and mononitrates were measurable in plasma 2 h after application and maximal concentrations for ISDN and mononitrates occurred after 12-16 h and 16 h, respectively. Mean areas under the curves values corrected for the body surface (BS) (AUC0-72 h.BS of 1074, 815 and 3584 nmol.m2.h/l for ISDN, IS-2-MN and IS-5-MN are equivalent to area ratios of 1, 0.8 and 3.3. ISDN metabolism following transdermal application is less extensive than after oral application. The molar nitrate concentration including metabolites, however, is comparatively low reaching approximately 60-80 nmol/l.

Administration, Cutaneous↗
PubMed1987

Veterans Administration Cooperative Study on Vasodilator Therapy of Heart Failure: influence of prerandomization variables on the reduction of mortality by treatment with hydralazine and isosorbide dinitrate.

The Veterans Administration Cooperative Study on Vasodilator Therapy of Heart Failure was designed to determine whether vasodilator drugs could alter the survival of patients with chronic congestive heart failure treated with digoxin and diuretics. Among the 642 patients entered into the study, 273 were randomly assigned to placebo, 186 were randomly assigned to the combination of hydralazine and isosorbide dinitrate, and 183 patients were randomly assigned to prazosin; all patients were followed for periods ranging from 6 months to 5.7 years. Treatment with hydralazine-nitrate produced a 28% reduction in mortality compared with that in patients receiving placebo (95% confidence interval, 3% to 46%), whereas prazosin exerted no apparent beneficial effect. Data were further examined to determine if any baseline variables had an impact on the response to treatment. Mortality in the placebo group was higher in those with coronary artery disease, with a history of antiarrhythmic drug use, and with values lower than the median for ejection fraction and exercise tolerance. A reduction in mortality with hydralazine-isosorbide dinitrate was observed in all of the above pairs of subgroups as well as in those above and below 60 years of age and those with and without a history of hypertension or excess alcohol ingestion. The benefit of hydralazine and isosorbide dinitrate was particularly prominent in younger patients with a lower ejection fraction and those with a history of hypertension and without an alcoholic history.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1978

Plasma concentrations of isosorbide dinitrate after administration of increasing doses of a sustained-release formulation to human subjects.

Plasma concentrations of isosorbide dinitrate have been measured after administration of increasing doses in the range 20--100 mg as sustained-release tablets (Isoket retard) containing 20 mg to human subjects. Means of peak concentrations of 4.2 ng/ml, 13.1 ng/ml, 20.7 ng/ml, 36.8 ng/ml, and 34.9 ng/ml were measured after doses of 20 mg, 40 mg, 60 mg, 80 mg and 100 mg, respectively. In the plasma of individual subjects, peak concentrations of isosorbide dinitrate increased in proportion to the dose administered. Areas under the plasma isosorbide dinitrate concentration-time curves also increased in proportion to the dose administered. Bioavailability parameters were better correlated to the dose over the range 20--60 mg than over the range 20--100 mg.

Adult↗
PubMed1982

Effect of isosorbide and hydralazine in painful primary esophageal motility disorders.

Five patients with painful primary esophageal motility disorders underwent pharmacologic testing with isosorbide and hydralazine. While neither agent affected baseline amplitude or duration of distal esophageal contractions, pretreatment with hydralazine significantly blunted the response to bethanechol (mean esophageal contraction duration, 31.4 +/- 4.8 s after bethanechol alone vs. 12.7 +/- 1.8 s after bethanechol and hydralazine p less than 0.005). Premedication with isosorbide was significantly less effective. In addition, while all 5 patients experienced chest pain in response to bethanechol alone, only 1 of 5 experienced chest pain in response to bethanechol after previous hydralazine administration; 3 patients had chest pain after previous administration of isosorbide. Patients who were placed on long-term oral hydralazine therapy experienced improvement in chest pain and dysphagia with concomitant decrease in amplitude and duration of esophageal contractions on repeat motility study (176.5 +/- 23.8 mmHg to 97.3 +/- 27.0 mmHg, p less than 0.05, 7.5 +/- 0.8 s to 5.2 +/- 0.5 s, p less than 0.005). Hydralazine appears to be of value in the treatment of diffuse esophageal spasm and other painful primary esophageal motility disorders.

Adult↗
PubMed1983

Fate of orally given isosorbide dinitrate in man: factors of variability.

After oral administration of isosorbide dinitrate, plasma concentrations of isosorbide dinitrate and mononitrates can be measured. An attempt was made to identify a number of factors which influence these plasma concentrations. Presence of renal failure, acute or chronic treatment with beta-blocking agents, and chronic cimetidine treatment did not influence the plasma concentrations. In a number of patients with cirrhosis, however, plasma concentrations of isosorbide dinitrate were found to be higher than in noncirrhotic patients.

Administration, Oral↗
PubMed1983

Acute and chronic isosorbide dinitrate therapy in congestive heart failure: demonstration of improved exercise capacity and differing arterial and venous tolerance during chronic administration.

Thirty patients with congestive heart failure underwent a double-blind study after randomization into either isosorbide dinitrate or placebo. The initial dose (40 mg orally) of isosorbide dinitrate reduced resting and exercise pulmonary artery, pulmonary capillary wedge, and systemic blood pressure and pulmonary and systemic vascular resistance without improving exercise tolerance. Chronic dosing (40 mg orally every 6 h for 3 months) increased exercise tolerance and maintained a reduction in resting and exercise pulmonary artery and pulmonary capillary wedge pressures and pulmonary resistance, while systemic pressure and resistance returned to baseline. Chronic oral isosorbide dinitrate (40 mg every 6 h) improves exercise capacity over a 3-month period with disparate tolerance effects on systemic arterial, systemic venous, and pulmonary vasculature.

Heart Failure↗
PubMed1983

Single administration of atenolol does not influence the kinetics of orally given isosorbide dinitrate.

In eight subjects, plasma concentrations of isosorbide dinitrate and its mononitrates after oral administration of 10 mg isosorbide dinitrate were measured on two occasions, once with and once without previous administration of a single dose of atenolol 100 mg. There were no significant changes either in plasma concentration at different times after administration, or in peak plasma concentrations or in area under the curve of the isosorbide dinitrate and mononitrates.

Administration, Oral↗
PubMed1983

Efficacy of isosorbide dinitrate tape on exercise tolerance of patients with angina pectoris.

Evaluation was made on the efficacy of isosorbide dinitrate tape (ISDN tape, TY-0081, Frandol Tape), a preparation newly developed in Japan, regarding the relationship between the exercise tolerance in patients with stable effort angina pectoris and plasma concentrations of ISDN. Placebo(s) or one to three pieces of isosorbide dinitrate tape (10 cm x 10 cm in size, containing 40 mg/tape) were applied to the patients and ISDN plasma concentrations were measured every 6th(15:00) and 24th (9:00) h after each application (9:00). Treadmill tests were repeated for the measurement of exercise tolerance according to a prescribed protocol where the exercise endpoint was the occurrence of chest pain. Correlation was found between the number of ISDN tape applied and the plasma concentrations, as well as between the isosorbide dinitrate plasma concentration and treadmill exercise time in 7 cases out of 10. Exercise time was increased significantly by the application of one piece of ISDN tape or two to three pieces of the tape, compared to the control or placebo study, respectively. The duration of actions lasted more than 24 h. These results suggest the efficacy of ISDN tape on angina pectoris, especially in its durability of action which lasts over 24 h.

Aged↗
PubMed1982

[Hemodynamic effects of a transdermal formulation of isosorbide dinitrate and its pharmacokinetics in conscious dogs].

Transdermal application of isosorbide dinitrate (ISDN) in the form of a tape (ISDN-Tape) to conscious dogs, in a dose of 40 mg/dog, caused a slow decrease in pulse pressure. The maximum effect was obtained 12 hour after application. The pulse pressure was still under the initial level even after 48 hours of application. In contrast, a sustained-release tablet of ISDN (ISDN-SR-Tablet), given in a dose of 40 mg/dog, significantly decreased the pulse pressure of conscious dogs by reducing systolic pressure and slightly elevating diastolic pressure. The plasma concentrations of ISDN and its two metabolites, isosorbide 2-mononitrate (2-ISMN) and isosorbide 5-mononitrate (5-ISMN), were measured by gas chromatography after application of ISDN-Tape or ISDN-SR-Tablets. The time course pattern of the plasma concentration of ISDN after application of the both preparations ran quite parallel with their decreasing effect on the pulse pressure. After application of the ISDN-Tape, the plasma concentration of ISDN was maintained at a higher level than after the application of the ISDN-SR-Tablet. The maximum plasma concentrations of the two metabolites, however, were considerably lower in the case of the ISDN-Tape than in the case of the ISDN-SR-Tablet. These results were ascribed to the fact that ISDN given through the transdermal route, in contrast to that given by the peroral route, does not undergo the first-pass effect in the liver. It was concluded that the transdermal dosage form of ISDN, which possesses a more prolonged pharmacologic effect than the oral dosage form, may be useful in the prevention and cure of angina pectoris.

Administration, Topical↗
PubMed1981

Relationship between the pharmacodynamics and pharmacokinetics of two oral sustained-release formulations of isosorbide dinitrate in normal man.

The relationship between the pharmacodynamics and pharmacokinetics of isosorbide dinitrate (ISDN) following oral administration of 40 mg of two different models. A model assuming an additive contribution of all active drug-related substances in plasma to pharmacological effect, i.e., finger pulse plethysmograph, resulted in estimates of relative potencies of ISDN:2-MN:5-MN (2-MN:2-isosorbide mononitrate; 5-MN:5-isosorbide mononitrate) as being 1:0.1:0.025. The data analysis using a receptor model (plasma concentration-effect curves) yielded sigmoid curves yielded sigmoid curves for 2-MN and 5-MN with similar relative potencies in the range of 20-80% of maximum response providing an upper limit for the pharmacodynamic effect due to ISDN, 2-MN or 5-MN in healthy volunteers.

Delayed-Action Preparations↗
PubMed1981

[Intermittent claudication: topical treatment with isosorbide dinitrate ointment. Preliminary results].

Following the casual observation reported by one anginal patient of ours, of improvement of its claudicatio intermittens with application of isosorbide dinitrate ointment directly on the leg suffering pain, we undertook a study to assess the possible use of the drug in peripheral vascular disease in a group of 10 patients suffering of a severe form of claudicatio intermittens. The effect of the drug was tested 1) by the subjective valuation of the patient itself 2) by treadmill stress tests performed at constant rate. In this case were used as reference parameters the distance walked without any symptoms and the maximal distance reached by each patient. The treadmill stress test was performed in basal condition and after longterm administration of isosorbide dinitrate ointment 100 mg three times a day for 30-45 days. In 5 patients the control test was repeated twice in different days to evaluate the reproducibility of the measure that resulted good, while other 5 patients performed the test one hour following the application of the drug in order to assess a possible acute effect of the drug that was not present in any patient. All the patients noted an improvement in their walking capacity but only after 15-20 days of treatment. In basal condition the distance walked without any symptoms by the patients was on the average m. 51 (+/- 52) and the maximal distance reached was m. 143 (+/- 111), while after the treatment were m. 151 (+/- 136) and m. 384 (+/- 203) with a difference highly significative (p less than 0.05 and p less than 0.01 respectively). From our data although preliminary, it is apparent that longterm local application of isosorbide dinitrate is effective in the treatment of patients with peripheral vascular disease and that the action of the drug seems to be related to a local effect.

Administration, Topical↗
PubMed1995

[Intra-anal application of isosorbide dinitrate in chronic anal fissure].

OBJECTIVE: To evaluate the effect of intra-anal application of isosorbide dinitrate on the healing rate of chronic anal fissure. DESIGN: Prospective, descriptive. SETTING: Outpatient clinic of the department of Surgery, University Hospital Dijkzigt, Rotterdam. METHOD: Sixteen patients with chronic (more than three months' duration) anal fissure were treated by intra-anal application of isosorbide dinitrate ointment every 3 hours, except during the night. The maximal duration of therapy was 12 weeks. Every three weeks the following aspects were investigated: clinical symptoms, side-effects and fissure healing. RESULTS: All patients experienced mild and transient headache shortly after the beginning of the treatment. At three weeks the fissure-related pain was resolved in all patients. At 6, 9 and 12 weeks the fissure was completely healed in 9, 11 and 15 patients respectively. CONCLUSION: The majority of chronic anal fissures can be treated effectively by local application of isosorbide dinitrate. This new and simple treatment modality appears to be an attractive alternative to the currently available surgical procedures.

Administration, Topical↗
PubMedDate not supplied

Isosorbide dinitrate or nifedipine: which is preferable in the medical therapy of achalasia?

Oesophageal motor activity was recorded manometrically with a low compliance system in 16 patients with achalasia and a slightly dilated oesophagus. After a basal recording period, nifedipine 20 mg was given sublingually to 9 patients and isosorbide dinitrate 5 mg to another 7 patients. Lower oesophageal sphincter pressure (LESp) and oesophageal body pressure wave amplitude were measured for 60 min after drug administration. Both drugs decreased LESp and pressure wave amplitude, but the effect of isosorbide dinitrate was faster and more intense than that of nifedipine. There was a lower inhibitory effect of nifedipine on the amplitude of pressure waves than on LESp, while isosorbide dinitrate inhibited with a similar intensity both LESp and pressure waves.

Esophageal Achalasia↗
PubMed1995

Reduction of exercise-induced myocardial perfusion defects by isosorbide-5-nitrate: assessment using quantitative Tc-99m-MIBI-SPECT.

BACKGROUND: Although nitrates were introduced more than 100 years ago and have been used for the treatment of angina pectoris, there are still some open questions concerning the mechanism of their action on myocardial ischemia. There are also insufficient data regarding the influence of any anti-ischemic medication on the results of myocardial perfusion scintigraphy. METHODS: To assess the influence of a mononitrate, 30 patients with stable angina pectoris, coronary stenosis > or = 70% and normal left ventricular function were examined using quantitative Tc-99m-MIBI exercise-single photon emission computed tomography (SPECT). On the same day, 5 h after a randomized double-blind dose of 60 mg sustained-release isosorbide-5-nitrate or placebo, SPECT was repeated with identical stress protocol. The results were analyzed using a semi-automatic polar coordinate program that allows definition of areas with significant decreased blood flow expressed as a percentage of standard vessel area. RESULTS: In the vessel areas with the largest perfusion defects, the mean defect size decreased after isosorbide-5-nitrate from 38.2 +/- 31.0% to 29.1 +/- 33.8% (reduction by 24%; P < 0.05) and increased from 35.2 +/- 27.6% to 36.6 +/- 27.4% after placebo (increase by 4%; P = NS). The difference between defect size changes was also significant (P < 0.05). CONCLUSION: Acute administration of sustained-release isosorbide-5-nitrate significantly reduces the size of exercise-induced perfusion defects as assessed using quantitative Tc-99m-MIBI-SPECT.

Adult↗
PubMed1994

[Antianginal effect of transdermal isosorbide dinitrate (multicenter study)].

Efficacy of transdermal isosorbid-dinitrate spray was investigated in 167 of 254 patients with stable angina pectoris. The transdermal application of isosorbid-dinitrate decreased successfully the number of anginal attacks and the sublingual nitroglycerin or isosorbid-dinitrate consumption. Very few side effects were observed and the patients well-being was good during treatment.

Administration, Cutaneous↗
PubMed1993

Renal effects of acute isosorbide-5-mononitrate administration in cirrhosis.

The aim of this study was to assess the effects of an oral dose (20 mg) of isosorbide-5-mononitrate on systemic hemodynamics, kidney function, plasma renin activity and plasma aldosterone and atrial natriuretic peptide concentrations in 16 nonazotemic cirrhotic patients. Isosorbide-5-mononitrate significantly reduced cardiopulmonary pressures, cardiac output, peripheral vascular resistance, mean arterial pressure, renal plasma flow, glomerular filtration rate, free water clearance, sodium excretion and atrial natriuretic peptide concentration and significantly increased renin and aldosterone values. Cardiopulmonary pressures, atrial natriuretic peptide, cardiac output and mean arterial pressure decreased to a similar extent in patients with (n = 9) and without ascites (n = 7). In patients with ascites we noted marked increases in plasma renin activity (3.7 +/- 1.1 ng/ml/hr to 6.4 +/- 1.8 ng/ml/hr; p = 0.01) and aldosterone level (61.1 +/- 17.5 ng/dl to 108.4 +/- 36.1 ng/dl; p = 0.01). In contrast, in patients without ascites the elevation of plasma renin activity (0.5 +/- 0.16 ng/ml/hr to 0.95 +/- 0.27 ng/ml/hr; p = 0.02) and aldosterone level (5.9 +/- 1.3 ng/dl to 12.3 +/- 3.8 ng/dl; p = 0.02) was mild, and in no case did these parameters increase over the upper normal limit. Isosorbide-5-mononitrate produced a significantly greater reduction of glomerular filtration rate (-21.4% +/- 3.3% vs. -8.9% +/- 4.2%; p = 0.03) and free water clearance (-82.4% +/- 16.1% vs. -34.5% +/- 12.3%; p = 0.03) in patients with ascites than in those without.(ABSTRACT TRUNCATED AT 250 WORDS)

Aldosterone↗
PubMed1995

ITF 296, a new endothelium-independent vasodilator: comparison with nitroglycerin and isosorbide dinitrate.

The effects of a new nitrate ester derivative, ITF 296, on large conductance and small resistance coronary arteries were investigated and compared with those of nitroglycerin and isosorbide dinitrate in chronically instrumented conscious dogs with an intact or with a deendothelialized large coronary artery. In a wide range of doses, ITF 296 (0.3-3 micrograms/kg), nitroglycerin (0.1-0.3 micrograms/kg), and isosorbide dinitrate (0.3-10 micrograms/kg) induced a highly selective dilatation of the large conductance vessels, an effect that was dose-dependent. At 30-fold higher doses, the three drugs also dilated coronary arterioles, an effect that preceded dilatation of large arteries but was transient. Qualitatively, ITF 296 therefore exhibits the same pattern of coronary effects as nitroglycerin and isosorbide dinitrate. Quantitatively, ITF 296 was 6.6-fold less potent than nitroglycerin at dilating large coronary arteries, but its effects on these vessels were of longer duration. Three days after endothelium removal, the vasodilation observed during reactive hyperemia or induced by acetylcholine were almost completely abolished. In contrast, the vasodilating effects of ITF 296 (30-100 micrograms/kg) and nitroglycerin (1 microgram/kg) were not significantly different from those observed before endothelium removal, thus indicating that these two drugs dilate the large conductance coronary arteries through an endothelium-independent mechanism.

Animals↗
PubMed1997

[Influence of combination therapy (isosorbide dinitrate and molsidomine) on the incidence of angina pectoris in patients with coronary heart disease].

UNLABELLED: Angina pectoris in patients with severe 3-vessel-disease refractory to treatment is a challenge for the treating physician. We have therefore tested the treatment efficacy of isosorbide dinitrate combined with molidomine on the frequency of angina pectoris in patients with symptoms refractory to treatment. PATIENTS AND METHODS: 15 patients with severe coronary heart disease were included in the study. The protocol included a 2-weeks stabilisation phase, followed by a 4-weeks treatment phase with 100 mg isosorbide dinitrate in the morning as well as 8 mg slow-release molsidomine at 6 p.m. RESULTS: Initially all of the 15 patients reported about daily angina pectoris attacks. After 4 weeks of treatment 4 out of 15 patients became free of symptoms. From the other 11 patients 6 reported an improvement, 5 an unchanged frequency of attacks. DISCUSSION: Combination treatment with isosorbide dinitrate with molsidomine in a slow-release form (in the nitrate free interval) showed a distinct improvement in patients with angina pectoris refractory to treatment with reduction of complaints. The effect of the combination is possibly based on a prolonged vasodilatation of the stenosed vessels and a prolonged reduction of filling pressure (reduction of preload).

Aged↗