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Biomedical subjects

V I Metelitsa

Publications and source records attributed to V I Metelitsa.

At least 73 records · Page 4Linked to original sources
PubMed1990

[Role of a beta adrenergic blocking agent nadolol (corgard) in prevention of arterial hypertension: a 6-month treatment (cooperative study)].

A comparative study was undertaken to examine the long-acting beta-blocker nadolol without intrinsic sympathomimetic activity and reference agents such as anapriline, a beta-blocker, hypothiazide, a diuretic, and pratsiol, a postsynaptic alpha-adrenoblocker in 361 patients with sustained arterial hypertension (diastolic blood pressure, 95 mm Hg or more) in the randomized groups. The therapy was started with monotherapy of one of these drugs; if ineffective, a combination of two or, if necessary, three agents of different groups was given. The patients' status was monitored at least once monthly for 6 months. Monotherapy with beta-blockers or pratsiol was found to be more effective than that with diuretics. Addition of the second agent was required by 48% of the patients, that of the third agent, by 13%. Nadolol in combination with diuretics and/or pratsiol showed the same effects as did anapriline. The agent possessed a more pronounced negative chronotropic action than did anapriline when it was given alone or in combination. Nadolol caused a decrease in middle and small-sized bronchial patency as did anapriline. A 6-month nadolol therapy resulted in regression of left ventricular hypertrophy.

Adult↗
PubMed1990

[A new antianginal preparation: isosorbide-5-mononitrate].

Repeated treadmill exercise tests were used in 20 patients with stable exercise-induced angina in order to comparatively examine various dosage forms of isosorbide-5-mononitrate (IMN) and isosorbide dinitrate (ID) during their single administration. The antianginal effect of conventional IMN tablets (Monisid, Bulgaria) lasted about 5 hours and 1-2 hours longer than that shown by long-acting tablets (Olicard, FRG) and lasted on an average of 12 hours. There was a correlation between the antianginal effect of IMN and its blood concentration. A significant individual variability was observed in the potency of all the dosage forms of IMN and ID under study. The dosage form of IMN had antianginal effects that were similar and even superior to those exhibited by ID.

Angina Pectoris↗
PubMed1990

[Comparative effectiveness and biological equivalency of new nifedipine preparations in patients with exercise-induced stenocardia].

The effectiveness of fenigidin and cordafen was studied in comparison with placebo and corinfar after a single administration during pharmacodynamic investigations with tredmill in 14 patients with stable exertional angina. Blood nifedipine concentrations were also compared. The potency of fenigidin was shown to be weaker than that of corinfar. The effect of cordafen and corinfar did not differ significantly. The mean concentrations of nifedipine in the blood serum after administration of equal doses of cordafen and corinfar did not differ considerably, either. Thus the findings were indicative of the equal potency of the same single doses of cordafen and corinfar and of less marked potency of fenigidin due to lower bioavailability.

Angina Pectoris↗
PubMed1989

Serum binding of nifedipine and verapamil in patients with ischaemic heart disease on monotherapy.

Serum free fractions of nifedipine, verapamil and some of their metabolites were measured in patients with ischaemic heart disease receiving single oral dose and chronic monotherapy and were compared with those obtained in vitro. The percentages of unbound nifedipine and verapamil in vitro (concentration range 50-200 and 150-400 ng ml-1, respectively) were 2.51 and 7.23%, respectively, and did not differ from those found on monotherapy with these drugs (2.05 and 8.08%, respectively), and after single dosing. It is suggested that, during treatment with nifedipine or verapamil, their serum metabolites do not affect binding of the parent drugs to serum proteins.

Adult↗
PubMed1989

[Effectiveness of intravenous infusion of ethmozin in patients with chronic ventricular arrhythmias].

Intravenous ethmozin in a dose of 270-730 mg for 4 h had pronounced antiarrhythmic effect in 80% of patients with frequent ventricular extrasystoles. In 10-14% of patients it may have arrhythmogenic effect. Positive correlation between duration and degree of the antiarrhythmic effect and dose and plasma ethmozin concentration was found. The character of the effect (antiarrhythmic or arrhythmogenic) did not depend on the dose and concentration of the drug. The indicated doses of intravenous ethmozin produce no serious side effect and may be recommended for treatment of chronic ventricular arrhythmias.

Adult↗
PubMed1989

[Evaluation of the antianginal efficacy of sustonit compared with other nitrate drug forms].

Sustonite, a long-acting nitroglycerin drug for oral use (manufactured in Poland), and some other dosage forms of nitrates were studied and compared. Twenty-one patients with stable angina pectoris of effort, functional classes II-III, were entered into the study. Sustonite was shown to produce an antianginal effect slightly yielding to that of sustac administered in equivalent doses. As to the effectiveness, sustonite appeared inferior to the dosage forms of nitrates such as nitrosorbide tablets, trinitrolong and dinitrosorbilong plates. The effect of sustonite manifested itself much later than that of sustac. As regards the physicochemical properties, sustonite tablets materially differ from sustac tablets in disintegration and solubility which are worse. The content of nitroglycerin in the tablets has turned out lower (1.2-1.4-fold) as compared to that indicated by the manufacturer.

Adult↗
PubMed1989

[Drugs in secondary prevention of ischemic heart disease: achievements, problems and prospects].

The paper provides critical reviews of the progress made in the past 25 years in studies on long-term drug prophylaxis of coronary heart disease. Particular attention is given to general problems, including those in the application of three major groups of antianginal agents, namely, nitrates, beta-adrenoblockers, and calcium antagonists to the prolonged secondary prevention of the disease. It has been shown that there is every prospects of future studies in this area. A general conclusion is drawn from a number of investigations performed at the Preventive Pharmacological Department, All-Union Cardiology Research Center, and in the All-Union Research Center of Preventive Medicine, USSR Ministry of Health over the past 5 years. These involve methodologically complicated matters of choice and long-term usage of drugs, including antianginal drugs within the collaborative studies.

Adrenergic beta-Antagonists↗
PubMed1989

[Evaluation of the efficacy of a course of verapamil and nifedipine in patients with stable stenocardia by daily monitoring of the electrocardiogram].

The daily ECG monitoring was used in 20 patients with stable functional class II-III angina pectoris to study the antianginal and anti-ischemic effects of verapamil and nifedipine during the cross use of the drugs. Verapamil and nifedipine applied in the effective doses provoked a significant decrease of the number and total depth of painful depressions of the ST segment. The effect of verapamil on painful episodes of ST segment depressions was significantly more pronounced than that of nifedipine. At the same time nifedipine significantly reduced the number and total depth of painless episodes of myocardial ischemia whereas verapamil did not cause any significant lowering of these indicators. In cases where the drugs appeared ineffective, verapamil provoked a significant increase of the number of painless episodes of myocardial ischemia. This indicates that the painful threshold of sensitivity may change with the occurrence of myocardial ischemia in patients suffering from angina pectoris. In turn, nifedipine produced no significant effect on the number and intensity of painless episodes of myocardial ischemia.

Adult↗
PubMed1989

[The development of nifedipine tolerance during its regular dosage in patients with stable exertional stenocardia].

The possibility of the development of tolerance to anti-ischemic effects of nifedipine (NF) during chronic administration for 2 months was studied in 15 patients with stable angina pectoris of effort. The duration and degree of the anti-ischemic effect were assessed in terms of similar, individually adjusted exercises performed prior to and repeatedly after NF administration. After acute NF administration the anti-ischemic effect lasting at least 4 h (mean 5.4 +/- 0.4 h) was attained in all the patients. After 2 months of regular NF administration the duration of the NF anti-ischemic effect significantly decreased to 3.9 +/- 0.5 h. In 5 patients, the attenuation of NF efficacy turned out substantial. The study performed 8-10 days after NF withdrawal in those 5 patients revealed partial restoration of the effect. The development of tolerance to NF action was not associated with changes in NF and its metabolite plasma concentrations. NF binding to plasma proteins also remained constant during the study.

Angina Pectoris↗
PubMed1989

[Nifedipine pharmacokinetics in patients with exertion-induced stenocardia after its single and long-term administration].

A study of the causes of tolerance to antianginal effect of nifedipine++, conducted in 12 patients with angina of effort, examined serum pharmacokinetics of nifedipine++ and its primary metabolite (puridine analogue of nifedipine++), after a single 20 or 30 mg dose and at the end of a treatment course (20-40 mg 3-4 times daily for 2 to 6 months). In addition, the effect of nifedipin treatment on nonspecific microsomal hepatic oxidase activity was assessed by means of the antipyrin test. Pharmacokinetics of both unchanged nifedipin and its primary metabolite showed no change through the nifedipin course, suggesting that tolerance to the antianginal effect of nifedipin may be based on altered systemic pharmacologic response rather than altered pharmacokinetics of nifedipin. Nifedipin treatment caused no induction or inhibition of nonspecific microsomal hepatic oxidase activity in the patients so the drug may be expected to have no substantial effect on pharmacokinetics, and hence, efficacy, of combined drugs that are eliminated by oxidation inside the liver.

Administration, Oral↗
PubMed1988

[Molsidomine and isosorbide dinitrate:/their comparative effectiveness in patients with exertion-induced stenocardia].

The markedness and duration of antianginal effects of 2 mg molsidomine and 10 mg isosorbide dinitrate were compared by means of repeated treadmill tests in 37 coronary patients with stable angina of effort. Peak magnitude of the effect was similar with both drugs, while the duration of the effect of isosorbide dinitrate (4.0 +/- 0.3 hrs) was significantly greater than that of molsidomine (3.4 +/- 0.3 hrs). Molsidomine reached its peak effect significantly earlier, as compared to isosorbide dinitrate. There was a significant correlation between the effectiveness of molsidomine and isosorbide dinitrate in the same patients.

Angina Pectoris↗
PubMed1988

[Isosorbide dinitrate: correlations between its anti-anginal effect, dosage form and administration schedule].

The action of various dosage forms of isosorbide dinitrate (ID) was studied with the help of repeated treadmill run in 28 CHD patients with stable angina of effort. The mean duration of the antianginal effect of ID standard tablets (nitrosorbide-NS) at a dose of 10 mg per os was 3.0 +/- 0.4 h. The effect of sublingual NS administration was more marked and the duration slightly less than in NS administration per os. ID of prolonged action isomac-retard containing 40 mg of ID produced an effect, insignificantly exceeding in duration the NS effect. Dinitrosorbilong (DNL) for gingival application produced and effect as marked as that of sublingual NS. The duration of the DNL effect significantly exceeded that of the effect of all ID dosage form under study (over 8 h). An increase in a NS dose per os did not result in an effect of the same degree and duration as that of DNL.

Administration, Buccal↗
PubMed1988

[Relation of the anti-anginal effect of nitroglycerin and its blood level in patients with stable exertion-induced stenocardia].

In 8 patients with coronary heart disease and stable angina pectoris of effort, a relationship was examined between nitroglycerin antianginal effects and blood concentration when it was topically applied to the gum (trinitrolong, TNL) and to the skin (nitroderm, ND). A close correlation was found between the antianginal effects and blood concentration (r = 0.97 for TNL and r = 0.81 for ND). The individual correlation coefficients were 0.61 to 0.84 for TNL and 0.31 to 0.79 for ND). In all cases but one, the antianginal effect was demonstrable when blood NG concentration reached 0.75 ng/ml, while in some cases (23%) at a concentration of 0.5 ng/ml or less.

Administration, Buccal↗
PubMed1988

[Study of anti-ischemic effects of verapamil and nifedipine after long-term treatment of patients with exertion-induced stenocardia].

The effects of verapamil and nifedipine taken as single doses and regular treatment, its mean duration being 2.9 and 2.8 months, respectively, were compared by means of repeated standard treadmill exercise in 22 patients with stable angina of effort. Verapamil taken as a mean standard dose of 413 +/- 18 mg was shown to produce anti-ischemic effect in the whole group that, in most cases, increased in relation to longer duration of treatment. Regular use of nifedipine (a mean daily dose of 86 +/- 5 mg) was associated with decreasing effect of the drug. Moreover, different patients showed different trends in terms of treatment efficiency (constant, growing or declining effect) both with verapamil and nifedipine.

Adult↗
PubMed1987

New transdermal and transmucosal nitroglycerin delivery systems in patients with ischaemic heart disease.

The efficacy of a transdermal (Nitroderm-TTS) and a transmucosal (Trinitrolong) nitroglycerin (NG) formulation has been compared with sublingual NG in 9 patients with ischaemic heart disease and stable angina pectoris. The duration and the degree of anti-ischaemic effect were assessed in terms of similar, individually adjusted work loads performed prior to and repeatedly after drug application in comparison with placebo. The anti-ischaemic effect of nitroderm appeared in 0.5-3 h after administration, reached a maximum in about 3.8 h and persisted for 7.9 h. The maximal nitroderm effect was significantly lower than that of sublingual NG or Trinitrolong. The effect of Trinitrolong was less variable and lasted for 4.6 h. It was evident in all patients 0.5 h after drug administration. Plasma NG levels were monitored in 9 patients after sublingual NG and trinitrolong and in 4 following Nitroderm. The relative bioavailability of Nitroderm and Trinitrolong according to the pharmacokinetic data was 29% and 256%, respectively, of sublingual NG tablets. A therapeutic NG level in blood (0.5 ng/ml) after Trinitrolong appeared much earlier (2 min) than after Nitroderm (1 h). A significant reduction in the effect of sublingual NG was observed during Nitroderm application. Thus, the transdermal NG formulation did not exhibit an antianginal effect lasting for 24 h; transmucosal NG had a relatively short, but more pronounced and stable antianginal effect.

Administration, Cutaneous↗