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At least 19 recordsLinked to original sources
PubMed1992

[A program for continuous infusion of cardiovascular agents (CIRCULATION)--how to derive the algorithm and how to use the mathematical formula in this program].

Recently, many cardiovascular agents came to be administered to serious or perioperative cases continuously, and difficult calculation became necessary. For continuous infusion of cardiovascular agents, we devised a personal computer program (CIRCULATION) to avoid difficult calculation for PC-9801 series (NEC) by a C language (Turbo-C, Version 2.0). It is easy to use the program, and it calculates the algorithm for many cardiovascular agents in a second. The program is very useful for anesthesiologists and for other doctors when they administer various cardiovascular agents.

Algorithms↗
PubMed1994

Intranasal delivery of cardiovascular agents: an innovative approach to cardiovascular pharmacotherapy.

The intranasal administration of drugs has long been used for the topical treatment of various nasal disorders. Many features of the intranasal mucosa also make it useful for delivery of systemically active agents. It has been shown that intranasal drug administration can provide plasma drug levels similar to those observed with comparable doses of parenteral drugs. The feasibility of intranasal administration of propranolol, nifedipine, and nitroglycerin has been investigated in several small clinical studies. Intranasal propranolol has been shown to improve exercise tolerance in patients with angina pectoris. Intranasal nifedipine has been used to treat patients with perioperative hypertension and hypertensive crisis. Intranasal administration of nitroglycerin was shown to blunt the hypertensive response to endotracheal intubation. These studies and others suggest that intranasal delivery of cardiovascular drug treatment could be used in those clinical situations where a rapid or intermittent drug effect is desired and can potentially serve as an alternative to parenteral drug administration.

Absorption↗
PubMed2000

Recent advances in biotransformation of CNS and cardiovascular agents.

Compound biotransformation is a very important research area for drug discovery and development. In this review, publications from the metabolism studies of ten compounds, seven CNS and three cardiovascular agents, from the Johnson & Johnson Corp. were reviewed. The seven CNS compounds are: three antipsychotic agents, mazapertine (arypiperazine analog), RWJ-46344 (arypiperidine analog) and risperidone (aryisoxazole-piperidine analog), one antidepressant, etoperidone (arypiperazine analog), one anxiolytic agent, fenobam (aryimidazole urea analog), one muscle relaxant, xilobam (pyrrolidinylidene urea analog), and one antiepileptic agent, topiramate (fructopyranose sulfamate analog). The three cardiovascular agents are: two arylalkylamine calcium channel blockers, bepridil and RWJ-26240, and one thioindolaminidine antianginal agent, RWJ-34130. Other antipsychotic and antidepressant agents with similar analogs (ziprasidone, trazodone and nefazodone) as well as other similar analogs of calcium channel blockers (verapamil) are discussed. In this article, excretion and metabolism (in vitro, in vivo) of compounds are reviewed from the CNS agents to the cardiovascular agents, including structures of parent compounds, their metabolites, metabolic pathways, and methods for the isolation, profiling, quantification and structural identification of unchanged compounds and metabolites. Pharmacological activities of parent compounds and their metabolites are also briefly discussed.

Animals↗
PubMed2004

Evaluation of synergism between the aminoglycoside antibiotic streptomycin and the cardiovascular agent amlodipine.

Amlodipine, a cardiovascular drug, exhibited remarkable antibacterial action in vitro against 504 bacterial strains belonging to both Gram positive and Gram negative genera, as well as in vivo against a mouse-virulent bacterium. Based on such findings, the present study was undertaken to determine whether the efficacy of this non-antibiotic drug could be enhanced in the presence of any antibiotic. Twelve bacterial strains, sensitive to amlodipine as well as to 6 antibiotics, viz., benzyl penicillin, streptomycin, chloramphenicol, tetracycline, erythromycin and ciprofloxacin were chosen. Disc diffusion test with amlodipine and streptomycin revealed marked synergism between the combination, compared with their individual effects. The synergism was found to be statistically significant (p<0.01). To assess the degree of synergy, the checkerboard analysis was performed. The fractional inhibitory concentration (FIC) index of this combination turned out to be 0.24, which confirmed synergism. This antibiotic-non-antibiotic pair was then administered to mice, challenged with S. typhimurium to determine whether this was effective in vivo. Statistical analysis of the mouse protection tests suggested that the combination was highly synergistic (p<0.001), according to Student's t-test. This synergistic drug combination may help us in enhancing the scope of prolonged antibiotic therapy in various types of infections, and might open a new therapeutic approach to combat drug resistance in bacterial diseases.

Aminoglycosides↗
PubMed1993

Feasibility of use of several cardiovascular agents in transdermal therapeutic systems with l-menthol-ethanol system on hairless rat and human skin.

Effect of the simultaneous use of l-menthol and ethanol on the skin permeation of six potent cardiovascular agents: nicardipine hydrochloride, atenolol, captopril, nifedipine, vinpocetine and nilvadipine (in hydrophilic order) was investigated to evaluate the feasibility of their use in a transdermal therapeutic system (TTS). In vitro diffusion experiments were carried out using excised hairless rat and human skin, and the application area of TTS required for the minimum therapeutic effect was estimated by a simple pharmacokinetic calculation. Marked enhancing effect by the l-menthol-ethanol system was found independent of drug lipophilicity, but the mode of action was dependent on the lipophilicity of the drug. The action of the system on lipophilic drugs (nifedipine, vinpocetine and nilvadipine) was mainly due to their increase in solubility in the system, while that on hydrophilic (or water soluble) drugs (nicardipine hydrochloride, atenolol and captopril) was the result of increase in their skin permeability coefficient. This enhancing effect was adequate to assure their minimum effective concentration (MEC) in human. The area of application of a drug to maintain the MEC was calculated to be 0.15 cm2 for hydrophilic or water soluble drugs and 3.7-13 cm2 for lipophilic drugs.

Administration, Cutaneous↗
PubMed1994

Carvedilol, a novel cardiovascular agent, inhibits development of vascular and ventricular hypertrophy in spontaneously hypertensive rats.

The effects of carvedilol, a novel cardiovascular agent, were evaluated in developing spontaneously hypertensive rats (SHR) for effects on hemodynamics, and the ability to effect the development of left ventricular, and vascular hypertrophy associated with chronic hypertension. Chronic oral administration of low dose carvedilol (20 mg/kg/day) was initiated when rats were 5 weeks of age, and experiments progressed until 14 weeks of age. Carvedilol-treated SHR had significantly reduced systolic blood pressures and heart rates throughout the duration of the experiment, and had significantly reduced ventricle/body weights by approximately 9.0%. Morphologic analysis of tertiary branches of the mesenteric artery revealed that carvedilol-treated SHR had significant reductions in medial cross-sectional area. Carvedilol produced concentration-dependent inhibition of basal [3H]thymidine incorporation in cultured SHR vascular smooth muscle cells, as well as by stimulation produced by PDGF (1 nM), EDGF (1 nM), thrombin (0.5 U/ml), or endothelin-1 (1 nM), indicating that carvedilol had direct anti-mitogenic activity. The present studies demonstrate that low dose carvedilol produced sustained reductions in blood pressure and heart rate in developing SHR that were accompanied by significant inhibition in the development of vascular and myocardial hypertrophy. The morphological changes induced by carvedilol may be mediated by a combination of hemodynamic effects, as well as by direct anti-mitogenic effects on vascular smooth muscle.

Administration, Oral↗
PubMed1987

Pharmacological profiling of cardiovascular agents in healthy volunteers by means of non-invasive methods.

In a placebo-controlled study the hemodynamic effects of single doses of oxprenolol, metoprolol, prenalterol, phentolamine, nifedipine, nitroglycerin, angiotensin II and frusemide have been investigated in 9 healthy volunteers by means of the combined measurement of heart rate, blood pressure, pre-ejection period (systolic time intervals) and stroke volume (impedance cardiography) in the supine and tilted positions (70 degrees). Each cardiovascular agent exhibited its characteristic pharmacodynamic profile, which allowed a clear-cut discrimination. The effects of oxprenolol and metoprolol, however, could not be distinguished by this procedure. The pre-ejection period, although not a very specific parameter, proved to be most sensitive to the pharmacological interventions, whereas stroke volume was less often influenced. It is concluded that the proposed selection of non-invasive parameters is a very suitable and simple means for early cardiovascular drug testing in man.

Adrenergic beta-Agonists↗
PubMedDate not supplied

[Acute poisoning with cardiovascular agents].

In order to determine the frequency, severity of poisoning, and the efficacy of the applied therapeutic measures, retrospective study of 391 patients treated for acute drug poisoning was performed during one-year period at the Clinic for Emergency and Clinical Toxicology and Pharmacology. In 49 (12.5%) patients cardiovascular agents were the cause of poisoning, most frequently beta-blockers and calcium antagonists (77.5%). Poisoning with antihypertensive agents was registered in 12.2% of patients, antiarrhythmics in 8.2%, and cardiotonics in 2.1%. Beta-blockers and calcium antagonists caused severe poisoning in over 40% of cases. Predominant clinical manifestations were registered on cardiovascular system, while central nervous system effects occurred secondary to cardiotoxicity. Symptomatic and supportive measures were performed most frequently, while specific agents, glucagon, calcium salts, and others, were used less often.

Acute Disease↗
PubMed2002

[Clinical proarrhythmias induced by anti-arrhythmic drugs, non-cardiovascular agents and implantable cardioverter-defibrillators].

The authors survey the electrophysiological mechanisms and clinical spectrum of the aggravation of cardiac arrhythmias provoked by antiarrhythmic drugs, non-cardiovascular agents and implantable cardioverter-defibrillators. The main aspects of the recognition, the differential diagnostics and the therapy are discussed. It is demonstrated that prevention of drug-induced arrhythmogenesis necessitates a fundamental understanding of the risk factors of proarrhythmias and of the clinical pharmacological properties of the drugs that are intended to be used, including proarrhythmic drug interactions. A systematic account is presented of those drugs prescribed in non-arrhythmic diseases which may lead to out-of-hospital cardiac arrest. The proarrhythmias that may be observed in recipients of implantable cardioverter-defibrillators are discussed, as are the undesirable interactions between these devices and antiarrhythmic drugs in such patients.

Anti-Arrhythmia Agents↗
PubMed1980

Studies on cardiovascular agents. 6. Synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to heterocyclic systems.

The synthesis and coronary vasodilating and antihypertensive activities of 1,2,4-triazolo[1,5-a]pyrimidines fused to pyrrole, thiophene, pyran, pyridine, and pyridazine are described. Among these compounds, 8-tert-butyl-7,8-dihydro-5-methyl-6H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-a]pyrimidine (23) was found to be the most promising potential cardiovascular agent, having been shown to be more potent in coronary vasodilating activity than trapidil [7-diethylamino)-5-methyl-1,2,4-triazolo[1,5-a]pyrimidine] and approximately equipotent to guanethidine sulfate in antihypertensive activity.

Animals↗