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PubMed1975

Effects of several antianginal agents on pacing-induced S-T Segment depression in the atherosclerotic rabbit.

Several agents used clinically in the treatment of angina pectoris were studied in an atherosclerotic rabbit model previously shown to be useful in differentiating antianginal drug activity. Intravenously administered isosorbide dinitrate afforded protection against pacing-induced S-T segment depression in a dose-related manner. Drugs with no protective effect included pentaerythritol tetranitrate, chromonar, and papaverine. Propranolol also did not prevent pacing-induced S-T segment depression, due in part to the overriding of the beneficial negative chronotropic effect of this drug by pacing.

Angina Pectoris↗

PubMed2005

Nitroester drug's effects and their antagonistic effects against morphine on human sphincter of Oddi motility.

AIM: To evaluate the effects of nitroester drugs on human sphincter of Oddi (SO) motility and their antagonistic effects against morphine which shows excitatory effect on Oddi's sphincter motility. METHODS: The effects of these drugs on SO were evaluated by means of choledochofiberoscopy manometry. A total of 67 patients having T-tubes after cholecystectomy and choledochotomy were involved in the study, they were randomly divided into glyceryl trinitrate (GTN) group, isosorbide dinitrate (ISDN) group, pentaerythritol tetranitrate (PTN) group, morphine associated with GTN group, morphine associated with ISDN group and morphine associated with PTN group. Basal pressure of Oddi's sphincter (BPOS), amplitude of phasic contractions (SOCA), frequency of phasic contractions (SOF), duration of phasic contractions (SOD), duodenal pressure (DP) and common bile duct pressure (CBDP) were scored and analyzed. Morphine was given intramuscularly while nitroester drugs were applied sublingually. RESULTS: BPOS and SOCA decreased significantly after administration of ISDN and GTN, BPOS reduced from 10.95+/-7.49 mmHg to 5.92+/-4.04 mmHg (P<0.05) evidently after application of PTN. BPOS increased from 7.37+/-5.58 mmHg to 16.60+/-13.87 mmHg, SOCA increased from 54.09+/-38.37 mmHg to 100.70+/-43.51 mmHg, SOF increased from 7.15+/-3.20 mmHg to 10.38+/-2.93 mmHg and CBDP increased 3.75+/-1.95 mmHg to 10.49+/-8.21 mmHg (P<0.01) evidently after injection of morphine. After associated application of ISDN and GTN, the four indications above decreased obviously. As for application associated with PTN, SOCA and SOF decreased separately from 100.64+/-44.99 mmHg to 66.17+/-35.88 mmHg and from 10.70+/-2.76 mmHg to 9.04+/-1.71 mmHg (P<0.05) markedly. CONCLUSION: The regular dose of GTN, ISDN and PTN showed inhibitory effect on SO motility, morphine showed excitatory effect on SO while GTN, ISDN and PTN could antagonize the effect of morphine. Among the three nitroester drugs, the effect of ISDN on SO was most significant.

Adult↗

PubMed1975

Savings from generic prescriptions. A study of 33 pharmacies in Rochester, New York.

Brand name and gereric prescriptions for 12 drugs were surveyed at 33 pharmacies in the Rochester, New York, area to determine how frequently generic prescriptions were filled with a product other than the major brand, and at a savings to the consumer. Generic prescriptions for ampicillin, erythromycin, propoxyphene, and dioctyl sodium sulfosuccinate were often filled at prices lower than comparable brand name prescriptions. Occasional, but often substantial, savings were obtained for papaverine, pentaerythritol tetranitrate, and conjugated estrogens. No savings were obtained for penicillin V, chlorpheniramine, diphenylhydantoin, sulfisoxazole, or methenamine mandelate. The pharmacists included in the survey identified correctly a mean of 18.5 out of 22 drugs as to whether products other than the major brand were available. A sample of physicians identified correctly a mean of 14.1 drugs. Pharmacists who were better informed as to which drugs were available generically were more likely to stock alternative products and more likely to charge lower prices on generic prescriptions than on brand name prescriptions.

Alkanesulfonates↗

PubMed2002

[Comparative evaluation of the clinical effectiveness and the adverse effects of three different forms of nitrates in high oral doses in patients with stable angina pectoris].

UNLABELLED: The aim of this study was the comparative evaluation of antianginal efficacy and the adverse effects of 3 nitrates in oral doses: isosorbide dinitrate 80 mg in slow release form (ISDN-80), nitroglycerin 15 mg--slow release (NITRO-15) and pentaerythritol tetranitrate 100 mg in normal tablets (PENTA-100) in patients (pts) with stable angina pectoris. In a randomized, double-blind, cross-over and placebo (P) controlled study 15 men, with mean age 54.8 +/- 8.0 years, with stable angina, received single doses of: ISDN-80, NITRO-15, PENTA-100 or P. Clinical efficacy of the drugs was evaluated by analysis of the walking times: total (TT), to angina (TA), and to ischemia (TI) on treadmill during stress tests performed 2 and 6 hours (h) after drug ingestion; the adverse effects were registered during 6 h follow up. RESULTS: 2 h after ingestion all 3 study drugs improved significantly: TT, TA and TI in comparison to P. After 6 h the same parameters were improved by: ISDN-80 and NITRO-15, but PENTA-100 improved only TT and TA. After 6 h ISDN-80 significantly improved in comparison to NITRO-15: TT by 19.7% (p < 0.01), TA by 21.2% (p < 0.01) ant TI by 25.0% (p < 0.05), and in comparison to PENTA-100: TT by 32.1% (p < 0.001), TA by 33.4% (p < 0.001) and TI by 41.1% (p < 0.01). After 6 h NITRO-15 significantly improved TI in comparison to PENTA-100 by 13.1% (p < 0.05). The headaches, the most frequent adverse effects, occurred after ingestion of ISDN-80 in 6 pts, NITRO-15 in 4 pts, PENTA-100 in 3 pts and P in 1 pt. Among three evaluated nitrates ISDN-80 significantly improved the effort tolerance and the coronary reserve in the strongest way, NITRO-15 was intermediate in the clinical efficacy, but PENTA-100, the drug with the weakest antianginal efficacy, was the reason of the least number of the adverse effects.

Angina Pectoris↗

PubMedDate not supplied

[Drug consumption by the patients with ischemic heart disease (IHD) studied by the Pol-Monica Warsaw and the effect of selected factors on the treatment of IHD].

As part of a multicentre WHO MONICA-Project the present drug consumption by Warsaw population was assessed (evaluated by DDD). In Warsaw population 2646 inhabitants aged 35-64 years were examined. Ischaemic heart disease was diagnosed in 30% screened persons. Only 39% of subjects were involved in taking cardiovascular drugs. In ischaemic heart disease the drugs used most frequently were pentaerythritol tetranitrate and dipyridamole. The influence of several psychosocial factors on the fact of undertaking of pharmacological therapy was analysed using multivariant logistic function method. Significant relationships were found for age, health self-care self-estimation of health status and fact of medical consultation. Persons with high values of MLF (fifth quintile) underwent drug treatment six time more often, then persons with low values of MLF (first quintile).

Adult↗

PubMed2005

[Effects of different drugs on the sphincter of Oddi motility: study with choledochoscope manometry].

OBJECTIVE: This study assessed the effects of narcotic analgesics, nitrates drugs, somatostatin analogues on human sphincter of Oddi motility and the antagonistic effects of nitrates drugs and anticholinergic agents against morphine measured by choledochoscope manometry. METHODS: 157 patients who had a T tube after cholecystectomy and choledochotomy were assessed by choledochoscope manometry. They were randomly divided into 5 groups. Sphincter of Oddi basal pressure (SOBP), amplitude (SOCA), frequency of contractions (SOF), duration of contractions (SOD), duodenal pressure (DP), common bile duct pressure (CBDP) were scored and analyzed. RESULTS: SOBP, SOCA and SOF increased after injection of morphine and Ap-237, CBDP increased after intramuscular administered morphine. No apparent change occurred after intramuscularly administered pethidine. SOBP and SOCA decreased after tramadol. After intravenous administration of stilamin in a dose of 250 microg/h, SOCA increased. After administration stilamin of 500 microg/h dose, SOCA and SOBP declined. After intravenous administration of sandostatin, CBDP increased obviously. BPOS and SOCA decreased significantly after administration of isosorbide dinitrate (ISDN) and glyceryl trinitrate (GTN), SOBP reduced evidently after application of pentaerythritol tetranitrate (PTN). SOBP, SOCA, SOF and CBDP increased evidently after injection of morphine. After associated application of ISDN and GTN, the four indications above decreased. As to associated application with PTN, SOCA and SOF decreased. After associated application of anisodamine or atropine, SOCA, SOBP declined, after injected buscopan, SOCA, SOBP, SOF all declined. CONCLUSION: The regular dose of morphine and Ap-237 shows excitatory effect on the sphincter of Oddi motility. Tramadol shows inhibitory effect on the sphincter of Oddi. The regular dose of pethidine and sandostatin shows no apparent effect on the sphincter of Oddi. Stilamin in low dose shows excitated effect on the sphincter of Oddi. Nitrates drugs show inhibited effects on SO motility. Nitrates drugs and anticholinergic agents can antagonize the excitated effect of morphine.

Adult↗

PubMed1978

Effects of some coronary vasodilator drugs on collateral hemodynamics after chronic myocardial ischemia in the anesthetized dog: appropriate or inappropriate redistribution?

These effects of dipyridamole, carbochromen, pentaerythritol tetranitrate (PETN), papaverine and ethaverine on collateral hemodynamics were investigated in anesthetized dogs 5 weeks after experimental coronary occlusion. The retrograde pressure, flow and resistance (RP, RF and RR) and the pressure, flow and resistance of the nonoccluded artery (CP, CF and CR) were measured; the pressure, flow and resistance ratios, i.e., the circulatory relationships which appeared between areas localized on both sides of the well-developed collateral channels, were calculated. Dipyridamole and carbochromen provoked an inappropriate and long-lasting redistribution to the detriment of ischemic areas: RF and RP decreased, whereas CF increased; RP/CP and RF/CF decreased; RR/CR increased. PETN provoked a redistribution in favor of ischemic areas: RF increased and RR decreased; RP/CP and RF/CF increased; RR/CR decreased. These main effects of PETN appeared after a first short period during which the changes in normal and ischemic areas were almost identical. Like PETN, papaverine and ethaverine provoked an appropriate redistribution during a second period. These results are discussed in terms of the selectivity of coronary dilator action on large or small vessels. The methodology used appears to be adequate to evaluate the activities of various drugs on a well-developed collateral coronary circulation.

Animals↗

PubMed1980

[Comparative study of three oral nitrate derivatives. A hemodynamic assessment in 10 patients with chronic heart failure (author's transl)].

The efficacy of three long-acting, orally administered nitrate derivatives was assessed in 10 patients with chronic heart failure. The compounds were: isosorbide dinitrate (ID) 5 mg, nitroglycerin microcapsules (NGMC) 7.5 mg and pentaerythritol tetranitrate (PETN) 160 mg. Pulmonary blood pressures were measured at regular intervals until the 6th hour following oral administration of all three compounds successively to 7 patients and of two compounds (ID and NGMC) to 3 patients. In addition, a hemodynamic study was performed in 3 of these patients while under placebo. The results showed a significant decrease in pulmonary artery diastolic pressure with all three compounds. The effects appeared after 30 minutes with ID and NGMC and after 1 hour with PETN. They lasted 1 hour with ID and 3 to 4 hours with NGMC and PETN. Maximal effect occured at 1 hour with ID (-28%; p < 0.001), at 1.5 hour with NGMC (-18%; p (< 0.01) and at 3 hours with PETN (-21%; p <0.01).

Administration, Oral↗

PubMed1980

Determination of ejection fraction by echocardiography in patients treated with P.E.T.N.

The purpose of this single-blind study carried out on 20 patients was to assess the effects of a long-acting nitrate derivative on the stroke index, which reflects left ventricular function. Following a 4 weeks' period of observation without any treatment (except for sublingual nitroglycerin during anginal attacks), an echocardiographic study of the left ventricle was performed. The distance between the endocardium lining the interventricular septum and that lining the posterior wall of the left ventricle was measured at the end of the diastole (R wave of the ECG) and at the end of the systole (shortest measurable distance). The rule of cubes was used to determine the ventricular volume and to calculate the stroke index. The patients then received pentaerythritol tetranitrate in daily doses of 240 mg for 30 consecutive days, after which a new echocardiographic study was done and the stroke index calculated again. The improvement in stroke index was more than three times the standard deviation before treatment in 15 patients (75%) and even six times greater in 8 of these (40%). No improvement was observed in the remaining 5 patients. In the group as a whole the stroke index increased from 0.418 +/- 0.135 to 0.504 +/- 0.115.

Adult↗

PubMed2001

Molecularly imprinted microparticles for capillary electrochromatography: studies on microparticle synthesis and electrolyte composition.

The use of molecularly imprinted polymer (MIP) microparticles in a partial filling application of capillary electrochromatography (CEC) has previously been shown successful for the enantiomer separation of propranolol. In this investigation, the influence of some important parameters in the preparation protocol, i.e., template to monomer ratio, type of cross-linker and functional monomers, and the effect of separation condition, i.e., organic modifier content, pH and the temperature of the column, on the electrochromatographic behavior of the MIP microparticles were studied. It was found that ethyleneglycol dimethacrylate (EDMA), having two reactive double bonds, was superior in terms CEC performance to trimethylpropane trimethacrylate (TRIM) and pentaerythritol tetraacrylate (PETEA) having three and four double bonds, respectively. The use of weak functional monomers, i.e., monomers lacking a strong interaction with the template, was shown to increase the separation efficiency. It was found that the template to functional monomer ratio had a pronounced influence on the MIP microparticle partial filling CEC performance as well as the size of the obtained microparticles. The use of a partial filling technique realizes the use of a new MIP phase in every new separation as well as the ability of altering the selectivity of the separation column and length of the MIP without the need for column switching.

Adrenergic beta-Antagonists↗

PubMed2002

Capillary electrochromatography with monolithic stationary phases: 1. Preparation of sulfonated stearyl acrylate monoliths and their electrochromatographic characterization with neutral and charged solutes.

A novel monolithic stationary phase having long alkyl chain ligands (C17) was introduced and evaluated in capillary electrochromatography (CEC) of small neutral and charged species. The monolithic stationary phase was prepared by the in situ copolymerization of pentaerythritol diacrylate monostearate (PEDAS) and 2-acrylamido-2-methyl-1-propanesulfonic acid (AMPS) in a ternary porogenic solvent consisting of cyclohexanol/ethylene-glycol/water. While AMPS was meant to support the electroosmotic flow (EOF) necessary for transporting the mobile phase through the monolithic capillary, the PEDAS was introduced to provide the nonpolar sites for chromatographic retention. Monolithic columns at various EOF velocities were readily prepared by conveniently adjusting the amount of AMPS in the polymerization solution as well as the composition of the porogenic solvent. The monolithic stationary phases thus obtained exhibited reversed-phase chromatography behavior toward neutral solutes and yielded a relatively strong EOF. For charged solutes (e.g., dansyl amino acids), nonpolar as well as electrostatic interaction/repulsion with the monoliths were observed in addition to electrophoretic migration. Therefore, for charged solutes, selectivity and migration can be readily manipulated by changing various parameters including the nature of the monolith and the composition of the mobile phase (e.g., pH, ionic strength and organic modifier). Ultrafast separation on the time scale of seconds of 17 different charged and neutral pesticides and metabolites were performed using short capillary columns of 8.5 cm x 100 microm ID.

Acrylic Resins↗

PubMed2006

Theoretical analysis of the terahertz spectrum of the high explosive PETN.

The experimental solid-state terahertz (THz) spectrum (3 to 120 cm(-1)) of the high explosive pentaerythritol tetranitrate (PETN, C(5)H(6)N(4)O(12)) has been modeled using solid-state density functional theory (DFT) calculations. Solid-state DFT, employing the BP density functional, is in best qualitative agreement with the features in the previously reported THz spectrum. The crystal environment of PETN includes numerous intermolecular hydrogen-bonding interactions that contribute to large (up to 80 cm(-1)) calculated shifts in molecular normal-mode positions in the solid state. Comparison of the isolated-molecule and solid-state normal-mode calculations for a series of density functionals reveals the extent to which the inclusion of crystal-packing interactions and the relative motions between molecules are required for correctly reproducing the vibrational structure of solid-state THz spectra. The THz structure below 120 cm(-1) is a combination of both intermolecular (relative rotations and translations) and intramolecular (torsions, large amplitude motions) vibrational motions. Vibrational-mode analyses indicate that the first major feature (67.2 cm(-1)) in the PETN THz spectrum contains all of the optical rotational and translational cell modes and no internal (molecular) vibrational modes.

Journal Article↗

PubMed2005

Capillary electrochromatography with monolithic stationary phases. 4. Preparation of neutral stearyl-acrylate monoliths and their evaluation in capillary electrochromatography of neutral and charged small species as well as peptides and proteins.

A neutral, nonpolar monolithic capillary column having a relatively strong electroosmotic flow (EOF) yet free of electrostatic interactions with charged solutes was developed for the reversed-phase capillary electrochromatography (RP-CEC) of neutral and charged species including peptides and proteins. The neutral nonpolar monolith is based on the in situ polymerization of pentaerythritol diacrylate monostearate (PEDAS) in a ternary porogenic solvent composed of cyclohexanol, ethylene glycol, and water. PEDAS plays the role of both the cross-linker and the ligand provider, generating a macroporous nonpolar monolith having C17 chains as the chromatographic ligands. Despite the fact that the neutral PEDAS monolith is devoid of fixed charges, the monolithic capillary columns exhibited a relatively strong EOF due to the ability of PEDAS to adsorb sufficient amounts of electrolyte ions from the mobile phase. The adsorbed ions imparted the neutral PEDAS monolith the zeta potential necessary to support the EOF required for mass transport across the monolithic column. The absence of fixed charges on the surface of the neutral PEDAS monolith and in turn the adsorption sites for electrostatic attraction of charged solutes allowed the rapid and efficient separations of proteins and peptides at pH 7.0, with an average plate number of 255,000 and 121,000 plates/m, respectively. To the best of our knowledge, this constitutes the first report on the separation of proteins at neutral pH by RP-CEC using a neutral monolithic column.

Chromatography, Micellar Electrokinetic Capillary↗

PubMedDate not supplied

Dependence of curing time, peak temperature, and mechanical properties on the composition of bone cement.

Commercial bone cements usually contain hydroquinone as the polymerization inhibitor and N,N-dimethyl-p-toluidine as the accelerator in the benzoyl peroxide-initiated redox polymerization. The former compounds have certain shortcomings in their biocompatibility profile. Measurements of the setting times, polymerization exotherms, and postpolymerization strengths of the cured monomer-polymer compositions show that the hydroquinone can be replaced by food grade di-tert-butyl-p-cresol (BHT). The more reactive 4-N,N-(dimethylamino)phenethanol can replace 4-N,N-dimethyl-p-toluidine, yielding cements with shorter setting times and increased strengths. Excessive heat liberated on polymerization can be reduced by partial substitution of higher-molecular-weight methacrylates, e.g., dicyclopentenyloxyethyl methacrylate for methyl methacrylate, but there is a decrease in strength of the resulting polymer. More successful has been the addition to the monomer of 1% or 2% of the chain transfer agent pentaerythritol tetra(3-mercaptopropionate), which lowers the peak temperature without changing the physical properties of the cement. Compositions with short curing times, lower exotherms, and mechanical properties that exceed those of a commercial material have been formulated.

Acrylates↗

PubMed1990

Acrylated phosphonate esters containing 1,3-dioxane and 1,3-dioxolane moieties as adhesion-promoting agents for dentin and hard tissues, I.

Novel acrylated phosphonate esters containing 1,3-dioxane and 1,3-dioxolane moieties derived from polyols such as glycerol, D-mannitol, D-sorbitol, pentaerythritol, and dipentaerythritol have been evaluated in vitro for their role as adhesion-promoting agents in composites employed for restorative dentistry. Some of the acrylated phosphonate esters have been found to promote strong bonding to dentin; the dipentaerythritol derivative exhibits a bond strength of approximately 960 psi (7 MPa) which compares favorably to commercial dentin adhesive systems. The bonding agents appear to act in multifunctional ways: the phosphonate group of the monomer chelates the calcium ions of hydroxyapatite at the dentin surface, ethereal oxygen atoms of 1,3-dioxolane or 1,3-dioxane moieties interact with the proteinaceous content of collagen, and the methacrylic fragment copolymerizes concomitantly with the other comonomers of the restorative composite material. Methods of preparing radiopaque adhesion-promoting acrylated phosphonates are also discussed.

Acrylates↗

PubMed2007

Novel biopolymers as implant matrix for the delivery of ciprofloxacin: biocompatibility, degradation, and in vitro antibiotic release.

The purpose of this study was to investigate the in vitro-in vivo degradation and tissue compatibility of three novel biopolymers viz. polymerized rosin (PR), glycerol ester of polymerized rosin (GPR) and pentaerythritol ester of polymerized rosin (PPR) and study their potential as implant matrix for the delivery of ciprofloxacin hydrochloride. Free films of polymers were used for in vitro degradation in PBS (pH 7.4) and in vivo in rat subcutaneous model. Sample weight loss, molecular weight decline, and morphological changes were analyzed after periodic intervals (30, 60, and 90 days) to monitor the degradation profile. Biocompatibility was evaluated by examination of the inflammatory tissue response to the implanted films on postoperative days 7, 14, 21, and 28. Furthermore, direct compression of dry blends of various polymer matrices with 20%, 30%, and 40% w/w drug loading was performed to investigate their potential for implant systems. The implants were characterized in terms of porosity and ciprofloxacin release. Biopolymer films showed slow rate of degradation, in vivo rate being faster on comparative basis. Heterogeneous bulk degradation was evident with the esterified products showing faster rates than PR. Morphologically all the films were stiff and intact with no significant difference in their appearance. The percent weight remaining in vivo was 90.70 +/- 6.2, 85.59 +/- 5.8, and 75.56 +/- 4.8 for PR, GPR, and PPR films respectively. Initial rapid drop in Mw was demonstrated with nearly 20.0% and 30.0% decline within 30 days followed by a steady decline to nearly 40.0% and 50.0% within 90 days following in vitro and in vivo degradation respectively. Biocompatibility demonstrated by acute and subacute tissue reactions showed minimal inflammatory reactions with prominent fibrous encapsulation and absence of necrosis demonstrating good tissue compatibility to the extent evaluated. All implants showed erosion and increase in porosity that affected the drug release. Increase in drug loading significantly altered the ciprofloxacin release in extended dissolution studies. PPR produced drug release >90% over a period of 90 days promising its utility in implant systems. The results demonstrated the utility of novel film forming biopolymers as implant matrix for controlled/sustained drug delivery with excellent biocompatibility characteristics.

Animals↗

PubMed2005

Extending the array of crosslinkers suitable for the preparation of polymethacrylate-based monoliths.

The in situ preparation of monolithic capillary columns comprising copolymers of butyl methacrylate with ethylene dimethacrylate, diethylene glycol dimethacrylate, triethylene glycol dimethacrylate, and pentaerythritol tetraacrylate using thermal polymerization within 250 microm ID capillaries and their application for micro-HPLC separations of proteins has been studied. For all crosslinkers, optimization of the porogenic mixture consisting of 1-propanol and 1,4-butanediol yielded monoliths with pore sizes above 1 microm suitable for rapid separations at low back pressure. Very good separations were achieved for a protein mixture consisting of ribonuclease A, cytochrome c, myoglobin, and ovalbumin with all tested columns.

Chromatography, High Pressure Liquid↗

PubMed2002

A rapid and efficient mass spectrometric method for the analysis of explosives.

The high explosives trinitrotoluene, nitroglycerine, pentaerythritol tetranitrate and hexahydro-1,3,5-trinitro-1,3,5-triazine are efficiently ionised under negative ion atmospheric pressure chemical ionisation (APCI) conditions. The limit of detection is improved, in some cases by several orders of magnitude, by complexation with chlorine demonstrating this to be a highly suitable method for enhancing the detection capabilities for explosives. The spectra produced from introduction of the analytes in a liquid matrix, with and without chlorine present, contain a number of ions that arise through secondary processes including breakdown and adduct formation. Sample introduction into an APCI source in air, via a heated-plate inlet with a supplementary feed of dichloromethane, produces improved response for the chloride adducts of the analytes and minimises their decomposition during analysis. The tandem mass spectra produced from the chloride adducts are simple. Optimisation of the trapping parameters of the ion trap detector enhances selected transitions, yields highly reproducible spectra and improves the limits of detection for MS/MS analysis.

Journal Article↗