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PubMed1979

[Effects on the systemic and coronary circulation of 2 nitrate derivatives, intravenous trinitrin and sublingual isosorbide dinitrate, administered during atrial pacing].

The changes in the systemic and coronary circulations produced by intravenous trinitrin 0.38 +/- 0.125 mg/hour and sublingual isosorbide dinitrate 5 mg were studied in 24 patients with coronary artery disease. When given during rapid atrial pacing both drugs decreased pulmonary capillary pressures (p less than 0.001), cardiac and coronary output (p less than 0.001 and p less than 0.01) and myocardial oxygen consumption (p less than 0.01). At these dosages, intravenous trinitrin has no significant effect on average systemic blood pressure or left ventricular work index; the coronary arterial resistances increased (p less than 0.005). Isosorbide dinitrate significantly decreased average systemic blood pressure and the left ventricular work index (p less than 0.001); there was no significant difference in the coronary arterial resistances; the decrease in coronary blood flow observed after sublingual isosorbide dinitrate seems partly due to a decreased perfusion pressure. The beneficial effect of these nitrite derivatives seems to be mainly related to a reduced preload.

Administration, Oral↗
PubMed2002

[Effect of isosorbide mononitrate on hypotensive action of enalapril in patients with mild and moderate hypertension].

The aim of the study was to compare hypotensive reaction after treatment with enalapril and enalapril with isosorbide mononitrate in patients with mild and moderate hypertension. Investigations were carried out in 49 patients. In every patient at baseline and after 3 hours from oral administration of enalapril or enalapril and isosorbide mononitrate plasma renin activity, plasma angiotensin converting enzyme activity, plasma aldosterone concentration and blood pressure were estimated. All measurements were repeated after 7 days of treatment. Adding a nitric oxide donor--isosorbide mononitrate--to enalapril does not enhance decrease in blood pressure nor influence plasma renin activity, plasma ACE activity nor plasma aldosterone concentration in patients with mild and moderate hypertension.

Administration, Oral↗
PubMed2002

[Development of nitrate tolerance in individual patients with stable angina pectoris in various phases of therapy with oral isosorbide dinitrate].

The aim of the work was an individual assessment of the effect on coronary reserve exerted by the widely used drug from the group of nitrates--isosorbide dinitrate (ISDN) in conventional and slow-release (SR) presentations, in various doses. The patients--38 males with stable coronary disease were given orally, by randomised double blind method, conventional isosorbide dinitrate (ISDN) in 10 and 20 mg doses, and slow-release isosorbide dinitrate in 20 mg SR, 40 mg SR, 80 mg SR and 120 mg SR doses, or placebo for the first time and for 7 days: four times daily, three times daily (with a 12-hour break), twice daily (with an 18-hour break) and once daily. In each of the therapeutic methods, walking times were analysed during exercise test six hours following drug administration, that is total time (TT), time to angina (TA) and time to ischaemia (TI). A prolongation by > or = 20% of walking times after ISDN administration as compared to placebo in > 50% of patients was accepted as significant improvement. Six hours after the first administration, a significant improvement of TT, TA and TI as compared to placebo was observed in the case of ISDN 20 mg, 40 mg SR, 80 mg SR and 120 mg SR. After administration of the drugs four times daily no significant improvement was observed after any dose. After administration of the drugs thrice daily, significant improvement was found in the case of TA (80 mg SR) and TI (20 mg SR, 40 mg SR and 120 mg SR), after twice daily administration--in the case of TI (40 mg SR and 80 mg SR) and after once daily administration--in the case of TT (80 mg SR), TA (120 mg SR) and TI (40 mg SR, 80 mg SR and 120 mg SR). In > 50% of patients, the coronary activity of ISDN in higher doses persists for six hours in the case of the first time administration; continuous therapy leads to tolerance development and intermittent therapy makes possible to avoid it. Tolerance does not depend on patients' sensitivity to nitrates.

Administration, Oral↗
PubMed2003

[Favorable results of conservative treatment with isosorbide dinitrate in 25 patients with fourth-degree hemorrhoids: a pilot study].

OBJECTIVE: To evaluate application of isosorbide dinitrate 1% ointment in the treatment of fourth-degree haemorrhoids. DESIGN: Prospective pilot study. METHOD: Twenty-five consecutive patients, 12 men and 13 women, with a median age of 48 years (range: 30-78), presenting in the period October 1999-December 2001 with fourth-degree haemorrhoids, were treated with isosorbide dinitrate 1% ointment. RESULTS: In 24 out of 25 patients (96%) the objective, reduction of the stangulated haemorrhoids and relief of pain, was achieved. In one patient the haemorrhoids were not reduced. This patient was cured after classic haemorrhoidectomy. Two patients interrupted the treatment because of severe headache, but after renewed instructions they continued the therapy and were cured. CONCLUSION: Isosorbide dinitrate 1% ointment gave good results in the treatment of fourth-degree haemorrhoids, with only few side effects.

Administration, Topical↗
PubMed1992

Bioavailability and metabolism of isosorbide dinitrate from a transdermal spray.

The plasma pharmacokinetics of isosorbide dinitrate (ISDN), isosorbide-2-nitrate (IS-2-N) and isosorbide-5-nitrate (IS-5-N) were investigated in 12 healthy volunteers after a single cutaneous administration of 60 mg ISDN (CAS 87-33-2) in the form of a solution sprayed onto the skin (TD Spray Iso Mack), in comparison with an intravenous infusion of 5 mg ISDN. After the intravenous dose, the apparent steady state volume of ISDN distribution came to 179.9 l, total body clearance was 3.14 l min-1, and terminal half-life was 79 min, on average. The transdermal absorption resulted in an average peak plasma concentration of 6.9 ng ISDN ml-1 at 5 h after the administration. ISDN concentrations between 1 and 5 ng ml-1 were maintained over at least 15 h. On average, 16.5% of the topically applied ISDN reached the systemic circulation. Total variations in Cmax (CV = 47.9%) and AUC (CV = 36.0%) of transdermal ISDN were similar to those usually observed after oral ISDN.

Administration, Cutaneous↗
PubMed1992

Reduction of portal pressure by chronic administration of isosorbide dinitrate in patients with cirrhosis: effects on systemic and splanchnic hemodynamics and liver function.

We investigated the chronic effects of isosorbide dinitrate on systemic and splanchnic hemodynamics and liver function in 13 patients with liver cirrhosis and portal hypertension. Placebo administration for 4 wk (n = 4) had no significant effects on these parameters. In contrast, oral administration of 40 mg/day of isosorbide dinitrate for 4 wk (n = 9) caused a significant fall in portal pressure (-18%, p less than 0.02), as evaluated by measurements of the hepatic venous pressure gradient with no modification in hepatic blood flow (from 0.72 +/- 0.29 to 0.71 +/- 0.34 L/min, NS), suggesting decreased intrahepatic or collateral vascular resistance. On the other hand, there was no significant correlation between the changes in mean arterial pressure and hepatic venous pressure gradient (r = 0.42). Thus, it seems unlikely that a reduction in portal blood inflow by baroreceptor-mediated reflex splanchnic vasoconstriction contributed to the fall in portal pressure. In addition, this drug had no adverse effects on liver function, as evaluated by measurements of the intrinsic clearance. These results suggest that chronic administration of isosorbide dinitrate could be a potentially useful and associated with cirrhosis.

Adult↗
PubMed1978

A patient with repeated syncopal attacks after using isosorbide dinitrate.

The case of a patient with repeated attacks of collapse induced by sublingual isosorbide dinitrate is reported. The patient was an 81 year-old female who was admitted to Yura Hospital because of attacks of precordial pain. Several minutes after the sublingual administration of isosorbide dinitrate (10 mg) for an anginal attack, she developed a sensation of general weakness, and thereafter because unconscious. Arterial blood pressure fell and became unmeasurable. Electrocardiograms recorded during the syncopal attack showed sinus tachycardia and significant elevation of ST-segment in right precordial leads. In response to a drip infusion of noradrenaline, arterial blood pressure returned to normal with recovery of consciousness. Two similar syncopal attacks induced by sublingual isosorbide dinitrate occurred in the next three days. These attacks were not due to augmentation of the vagal reflex. Decrease of venous return probably was the primary etiological factor.

Aged↗
PubMed1992

[Pharmacokinetics of low-dose isosorbide dinitrate and metabolites after buccal or oral administration].

The kinetics of isosorbide dinitrate (ISDN; CAS 87-33-2) and its metabolites isosorbide-5-mononitrate (IS-5-MN) and isosorbide-2-mononitrate (IS-2-MN) were examined after buccal and oral administration of 5 mg ISDN. Twelve healthy volunteers were included in a randomized cross-over study. The mean dose-corrected AUCs for total nitrate in serum after the two different preparations were in the same range. The relative bioavailability of ISDN applied buccally, however, was more than twice that after oral application. The metabolism of ISDN differed depending on the route of administration, where the AUC-ratios ISDN: IS-2-MN: IS-5-MN were 1:2.7:19.4 after buccal and 1:5.7:53.4 after oral application respectively. The absorption rate constants Ka for ISDN and the MRT after buccal and oral application did not differ significantly. The same holds for the mean residence time.

Administration, Buccal↗
PubMed1991

[Bioavailability and bioequivalence of organic nitrates. Isosorbide dinitrate--a study of sustained-release preparations].

Assessment of Bioavailability of Organic Nitrates/Comparative bioavailability study of sustained-release isosorbide dinitrate preparations. Relative bioavailabilities of isosorbide dinitrate (ISDN, CAS 87-33-2) and the metabolite isosorbide-5-mononitrate (IS-5-MN, CAS 16051-77-7) were studied after application of Maycor retard 40 (sustained-release capsules, multiple unit formulation, test preparation) in comparison to sustained-release tablets (single unit formulation, reference preparation) with 16 healthy male volunteers in a two-way crossover design. Test and reference formulations were previously characterised in vitro by dissolution tests. ISDN, IS-5-MN (IS-2-MN) plasma concentrations were determined using a selective and sensitive GLC-method with ECD-detection. As pharmacokinetic parameters AUC, Cmax and half value duration (HVD) were evaluated. Bioequivalence was assessed by calculating 90%-confidence intervals (ANOVA, ANOVAlog, Mann-Whitney-test) for ISDN and IS-5-MN. Bioequivalence was accepted if due to the inclusion rule one of the calculated intervals fulfill the requirements of 80 and 120% (AUC) or 70 and 130% (Cmax, HVD), respectively. Relative bioavailability of the test formulation was calculated as 94% (ISDN) and 96% (IS-5-MN). Maximum plasma concentrations of ISDN (IS-5-MN) were determined for the test preparation as 14.3 +/- 3.1 ng/ml (265 +/- 45 45 ng/ml) and as 22.8 +/- 12.6 ng/ml (287 +/- 59 ng/ml) for the reference product. HVD-values were for the test preparation 4.5 +/- 1.3 h (ISDN) and 8.5 +/- 1.3 h (IS-5-MN) and for the reference formulation 3.1 +/- 1.2 h (ISDN) and 8.1 +/- 1.4 (IS-5-MN).(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1990

[Changes in exercise capacity and in induced ischemia with an oral dose of 5 isosorbide mononitrate in patients with stable angina pectoris].

In order to establish the effects of 5-isosorbide mononitrate on: the exercise capacity, the onset period of angina and ischemia along with the degree and on whether the duration time was prolonged up to 5 hours after the oral administration of 20 mg of this drug, we compare this drug against a placebo in a group of 15 patients with stable angina pectoris developed by effort who performed an exercise test using a bicycle ergometer. After the administration of 20 mg of 5-isosorbide mononitrate it was observed that onset time of angina (p less than 0.001), the onset time of ST decrease (p less than 0.002) and total time of exercise attained were significantly superior to those found in patients with placebo administration. Moreover, for the same degree of EKG ischemia (ST decrease) showed a superior exercise time was registered (p less than 0.002) after the administration of 5-isosorbide mononitrate (5-IM). Our results show that an oral dosage of 20 mg of 5-IM given to patients with stable angina pectoris increased the capacity and exercise tolerance delaying significantly the onset time of angina, the onset time of EKG ischemia and its decree induced by the effort up to 5 hours after its administration.

Administration, Oral↗
PubMed1989

[Determination of isosorbide dinitrate and its degradation products in pharmaceuticals by gradient RP-HPLC].

Isosorbide dinitrate (ISDN) and its degradation products isosorbide-5-mononitrate (5-ISMN) and isosorbide-2-mononitrate (2-ISMN), in a spray formulation were separated and determined by step gradient RP-HPLC within 8 minutes. A Shimadzu LC-4A liquid chromatograph, Nucleosil C18 5 microns 150 X 4.6 mm (ID) column, SPD 2AS spectrophotometric detector at 220 nm with variable attenuation were used, the sensitivity was kept at 0.16 AUFS in the first 4.5 min and changed to 2.56 AUFS during 4.5-12 min. Solution A (70% methanol) and solution B (5% methanol) were employed as mobile phase at a flow rate of 1.0 ml/min in gradient elution. Good results could be obtained by CR 3A data module using external standard method. The recoveries were 98.20% (ISDN), 96.92% (5-ISMN) and 95.83% (2-ISMN) and the coefficients of correlation were 0.9990 (ISDN), and 0.9994 (5-ISMN and 2-ISMN).

Chromatography, High Pressure Liquid↗
PubMed1989

[Pharmacokinetic profile and bioavailability of a new pharmaceutical formulation of isosorbide-5-mononitrate sustained-release formulation].

The pharmacokinetic profile and the bioavailability of a new galenic formulation of isosorbide-5-mononitrate sustained released capsules (Olicard 40 retard) was tested under standardized conditions. 12 healthy, male volunteers (mean age 24.9 +/- 3.0 years) in a randomized, intraindividual crossover design (wash-out phase: 6 days) received the isosorbide-5-mononitrate sustained-release capsules (testformulation) and a standard-release formulation of the same active substance as single dose (40 mg each). Venous blood sampling for analysing the plasma concentration of isosorbide-5-mononitrate was done before and at 21 fixed times after medication. The AUC0----36h of the concentration/time curve was calculated using the linear trapezoidal rule and the AUC0----infinity extrapolated after computing the half-life of the terminal elimination phase. The leading variable was the AUC0----infinity. For the sustained-release preparation an AUC0----36h of 5764.5 +/- 909 ng/ml.h was measured, an AUC0----infinity of 5863.9 +/- 981.9 ng/ml.h was calculated, with a peak maximum (Cmax) of 472.5 +/- 29.7 ng/ml after 2.9 +/- 0.5 h (tmax). For the standard-release formulation an AUC0----36h of 5679.8 +/- 690.3 ng/ml.h was measured, an AUC0----infinity of 5688.7 +/- 695.7 ng/ml.h was calculated, with a peak maximum (Cmax) of 842.4 +/- 100.2 ng/ml after 1.2 +/- 0.2 h (tmax). The bioavailability of the standard-release formulation was postulated to be 100%. The non-parametric calculation of the bioavailability-ratio (geometric Walsh-averages) was 101.47% (95% confidence limits 85.24% to 121.09%). There was no statistically significant difference between the both galenical formulations, the sustained-release preparation has no influence on the total amount of resorption.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1989

[Comparison of isosorbide dinitrate and nifedipine in the treatment of variant angina pectoris. Randomized study].

The effects of isosorbide dinitrate single dose 120 mg daily and nifedipine 20 mg twice daily were studied in 17 patients with variant angina pectoris due to coronary artery spasm. After a placebo phase the patients were randomized to treatment with either isosorbide dinitrate or nifedipine. After six weeks the patients were crossovered for another six weeks period of treatment. There was significant decrease of number of angina attacks during both treatment regimens. Using 24 hours Holter monitoring we also proved significant decrease of number of ST segment elevation or depression, either symptomatic or asymptomatic. There was increase of performed work during exercise tests after both treatment periods. The efficacy of Isoket 120 mg and Adalat Retard 2 x 20 mg daily in the treatment of patients with active variant angina pectoris was comparable in our study. 3 patients suffered untolerable headache during isosorbide dinitrate phase and had to terminate treatment after first day only.

Adult↗
PubMed1989

[Effect of isosorbide dinitrate (sorbonit) on the exercise reaction in patients with coronary disease and in healthy individuals].

The study aimed at evaluating an effect of a single dose of isosorbide dinitrate (Sorbonit) on the exercise reaction in the patients with coronary disease of various degree and in healthy individuals. The study involved 20 male patients of mean age 54.0 +/- 4.5 years with history of myocardial infarction and 12 healthy males of mean age 45.6 +/- 5.0 years. Ergometric test has been performed twice: prior to and 15 minutes after sublingual administration of isosorbide dinitrate in the dose of 10-15 mg. The first test has been interrupted when horizontal ST load exceeded 1 mm or contractions rate was 60% of the maximum value. Similar loads have been used after the administration of Sorbonit. The following parameters have been evaluated: heart rate (HR), systolic blood pressure (BPS), HR x BPS, lactate level (LA), and cardiac index. The value of the load has been measured with the aid of oxygen consumption (VO2). Significant depression of ST segment (less than 3 mm) in the exercise ECG has been noted in 8 patients following isosorbide dinitrate. Exercise tolerance has increased in these patients - CI increased during exercise following drug administration (VO2 the same as prior to the drug administration), and VO2/CI has became closer - physiological.

Coronary Disease↗
PubMed1987

In vitro evidence of an endothelial cell-dependent antiplatelet activity for isosorbide dinitrate, but not for its 2- and 5-mononitrate metabolites.

In an experimental model in which cultured endothelial cells (EC) and platelets were incubated with autologous plasma, we investigated the pharmacological modulations by isosorbide nitrates (ISN) [isosorbide dinitrate (ISDN) + 2-isosorbide mononitrate (2-ISMN) + 5-ISMN] of the EC-induced inhibition of platelet aggregation; and the associated changes in prostanoid profile of these mixed EC-platelet suspensions. ISDN antiplatelet activities were found to be magnified profoundly by EC, being dependent upon both ISDN concentration and EC number, e.g., 5.10(-5) M ISDN in the presence of 2.10(4) cells, fully arrested ADP-induced aggregation, whereas the same ISDN concentration induced 30% inhibition in control platelet activities. In contrast, there were no significant changes in 2- and 5-ISMN antiaggregating properties, whether incubated in the presence or absence of EC. Thromboxane B2 accumulated noticeably after aggregation, whereas 6-keto-prostaglandin (PG) F1 alpha and PGE2 accumulated poorly in the medium. In the presence of EC, thromboxane B2 accumulation fell in parallel to the extent of aggregation, whereas 6-keto-PGF2 alpha and PGE2 accumulated in the medium. Aspirin-treated, washed ECs still inhibited platelet aggregation. ISDN was the only ISN capable of inducing PG-accumulation profile changes. These results demonstrate the existence of an endothelium-dependent ISDN antiplatelet activity. Furthermore, this effect is specific to ISDN not being shown by its mononitrate metabolites. These results suggest that PG accumulation changes may be a consequence rather than a cause of the inhibition of platelet activity by (ISDN-stimulated) EC.

6-Ketoprostaglandin F1 alpha↗
PubMed1988

Effect of isosorbide dinitrate and atropine on the lower esophageal sphincter pressure in Chagasic patients.

The effect of isosorbide dinitrate (5 mg, sublingually) and of atropine (12 micrograms/kg i.v.) on the lower esophageal sphincter pressure of chagasic patients with esophageal involvement and of control subjects was studied by the manometric method. The pressure was measured at 5 minute intervals for 60 minutes after drug administration. When the effect of isosorbide dinitrate was studied, basal sphincter pressure (mean +/- SEM) was 15.3 +/- 1.9 mmHg in chagasic patients (N = 15) and 25.4 +/- 5.6 mmHg in controls (N = 9) (P greater than 0.05). Isosorbide dinitrate reduced sphincter pressure between 10 and 20 minutes and at 40 minutes in controls, and froM 5 to 60 minutes in chagasics (P less than 0.05). The reduction was more intense in chagasics throughout the time of measurement (P less than 0.05). When the effect of atropine was studied, basal sphincter pressure was 20.6 +/- 1.8 mmHg in chagasic patients (N = 14) and 23.7 +/- 2.5 mmHg in controls (N = 9) (P greater than 0.05). Atropine reduced sphincter pressure both in chagasics and controls, but more intensely so in controls during the first 30 minutes of the study (P less than 0.05). The action of the musculature itself may be the main factor in the maintenance of sphincter pressure in chagasics, with secondary participation of the cholinergic excitatory system.

Administration, Sublingual↗
PubMedDate not supplied

[Effect of isosorbide dinitrate on the lower esophageal sphincter pressure in patients with Chagas' disease].

The effect of 5 mg of sublingual isosorbide dinitrate on the lower esophageal sphincter pressure of 28 chagasic patients with esophageal involvement, was studied by continuous perfusion manometry. The pressure was measured at 5 minute intervals for 60 minutes after drug administration. Isosorbide dinitrate reduced sphincter pressure from 5 to 60 minutes (p less than 0.01). Only two patients hadn't sphincter pressure reduced lower than 50% of initial value at 20 minutes after drug administration. These results indicate that isosorbide dinitrate may be useful to reduce lower esophageal sphincter pressure in chagasic megaesophagus.

Adult↗
PubMed1988

Effects of isosorbide dinitrate on thromboxane A2 synthesis in carbon dioxide exposed platelets.

Isosorbide dinitrate (Nitorol R, 100 nmol/l) blocked an increase in thromboxane B2 concentration in human platelet-rich plasma caused by exposure to high CO2 tension, in the presence of arachidonic acid. Thromboxane B2 concentrations obtained at 1 or 2 mmol/l or arachidonic acid were not influenced by isosorbide dinitrate at low CO2 tension. Inhibitory action of isosorbide dinitrate on the thromboxane A2 synthesis appears to have a close relation to the site of CO2 action.

Blood Platelets↗