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Bisoprolol and Hydrochlorothiazide [keywords]
- Comparative effectiveness of a fixed-dose combination of losartan + HCTZ versus bisoprolol + HCTZ in patients with moderate-to-severe hypertension: results of the 6-month ELIZA trial. [Journal Article, Research Support, Non-U.S. Gov't]
- Vasc Health Risk Manag 2013.:535-49.
The aim of this study was to compare the antihypertensive efficacy of losartan 100 mg + hydrochlorothiazide (HCTZ) 25 mg versus bisoprolol 10 mg + HCTZ 25 mg and their influence on arterial stiffness and central blood pressure (BP).Of 60 patients with a mean BP of 173.3 ± 1.7/98.4 ± 1.2 mmHg, 59 were randomized to losartan + HCTZ (n = 32) or bisoprolol + HCTZ (n = 27). Amlodipine was added if target BP was not achieved at 1 month, and doxazosin was added if target BP was not achieved after 3 months. Body mass index, office and 24-hour ambulatory BP, pulse wave velocity (carotid-femoral [PWVE] and radial [PWVM]), noninvasive central systolic BP, augmentation index (AIx), laboratory investigations, and electrocardiography were done at baseline and after 6 months of treatment.Losartan + HCTZ was as effective as bisoprolol + HCTZ, with target office BP achieved in 96.9% and 92.6% of patients and target 24-hour BP in 75% and 66.7% of patients, respectively, after 6 months. Effective treatment of BP led to significant lowering of central systolic BP, but this was decreased to a significantly (P < 0.05) greater extent by losartan + HCTZ (-23.0 ± 2.3 mmHg) than by bisoprolol + HCTZ (-15.4 ± 2.9 mmHg) despite equal lowering of brachial BP. Factors correlated with central systolic BP and its lowering differed between the treatment groups. Losartan + HCTZ did not alter arterial stiffness patterns significantly, but bisoprolol + HCTZ significantly increased AIx. We noted differences in ΔPWVE, ΔPWVM, and ΔAIx between the groups in favor of losartan + HCTZ. Decreased heart rate was associated with higher central systolic BP and AIx in the bisoprolol + HCTZ group, but was not associated with increased AIx in the losartan + HCTZ group.Although both treatments decreased both office and 24-hour BP, losartan + HCTZ significantly decreased central systolic BP and had a more positive influence on pulse wave velocity, with a less negative effect of decreased heart rate on AIx and central systolic BP.
- Heart rate variability on antihypertensive drugs in Black patients living in sub-Saharan Africa. [JOURNAL ARTICLE]
- Blood Press 2013 Sep 25.
Background. Compared with Caucasians, African Americans have lower heart rate variability (HRV) in the high-frequency domain, but there are no studies in Blacks born and living in Africa. Methods. In the Newer versus Older Antihypertensive agents in African Hypertensive patients trial (NCT01030458), patients (30-69 years) with uncomplicated hypertension (140-179/90-109 mmHg) were randomized to single-pill combinations of bisoprolol/hydrochlorothiazide (R) or amlodipine/valsartan (E). 72 R and 84 E patients underwent 5-min ECG recordings at randomization and 8, 16 and 24 weeks. HRV was determined by fast Fourier transform and autoregressive modelling. Results. Heart rate decreased by 9.5 beats/min in R patients with no change in E patients (- 2.2 beats/min). R patients had reduced total (- 0.13 ms²; p = 0.0038) and low-frequency power (- 3.6 nu; p = 0.057), higher high-frequency (+ 3.3 nu; p = 0.050) and a reduced low- to high-frequency ratio (- 0.08; p = 0.040). With adjustment for heart rate, these differences disappeared, except for the reduced low-frequency power in the R group (- 4.67 nu; p = 0.02). Analyses confined to 39 R and 47 E patients with HRV measurements at all visits or based on autoregressive modelling were confirmatory. Conclusion. In native Black African patients, antihypertensive drugs modulate HRV, an index of autonomous nervous tone. However, these effects were mediated by changes in heart rate except for low-frequency variability, which was reduced on beta blockade independent of heart rate.
- A report from the American Society of Hypertension 28th Annual Scientific Meeting and Exposition (May 15-18, 2013 - San Francisco, California, USA). [Journal Article]
- Drugs Today (Barc) 2013 Jul; 49(7):463-70.
A wide selection of antihypertensive drugs are currently available for managing hypertension, with distinct advantages and disadvantages in selected patient populations. However, many patients require combination approaches for effective control of blood pressure, and new drugs are required for reaching target blood pressure values in difficult-to-treat subjects. Indeed, initial use of combination therapies more effectively lowered blood pressure, resulting in a further decreased risk of stroke compared to antihypertensive monotherapy (Yu, J. et al., Abst PO-13). Nevertheless, novel drugs and new fixed-drug combinations are being developed, as reported in the following report from this year's American Society of Hypertension meeting. As exemplified by a comparison of newer versus older antihypertensive drugs in Sub-Saharan African countries that demonstrated the superiority of valsartan/amlodipine versus bisoprolol/hydrochlorothiazide (M'Buyamba-Kabangu, J.R. et al., Abst PO-86), newer drugs are beating the efficacy of older agents, and drugs currently in development may eventually demonstrate greater benefits that drugs considered new today. Research continues, as the morbidity and mortality associated with hypertension is better recognized as a threat in aging populations worldwide.
- What can we do to make antihypertensive medications taste better for children? [Journal Article]
- Int J Pharm 2013 Nov 30; 457(1):333-6.
More and more data indicate the importance of palatability when selecting drugs for children. Since hypertension is uncommon in children, no child-friendly palatable formulations of these agents are currently available. As a consequence, in everyday practice available tablets are crushed and administered mixed with food or a sweet drink. We started investigating the issue of palatability of drugs among children in 2004 using smile-face scales. In the first trial we compared taste and smell acceptability of pulverized angiotensin receptor antagonists among nephropathic children and found that the score assigned to candesartan was significantly higher than that assigned to irbesartan, losartan, telmisartan and valsartan. In the second trial we compared the taste of pulverized amlodipine and lercanidipine among children and found that the score assigned to lercanidipine was significantly higher. Our third trial was performed using pulverized β-adrenoceptor blockers, angiotensin-converting enzyme inhibitors, calcium-channel antagonists and diuretics among medical officers and pediatricians. The palatability scores assigned to chlorthalidone, hydrochlorothiazide and lisinopril were significantly higher to those assigned to atenolol, bisoprolol, enalapril and ramipril. In conclusion pulverized amlodipine, atenolol, bisoprolol, enalapril, irbesartan, losartan, ramipril, telmisartan and valsartan are poor tasting. From the child's perspective, lercanidipine, candesartan, chlorthalidone, hydrochlorothiazide and lisinopril are preferable.
- Efficacy of newer versus older antihypertensive drugs in black patients living in sub-Saharan Africa. [Journal Article]
- J Hum Hypertens 2013 Dec; 27(12):729-35.
To address the epidemic of hypertension in blacks born and living in sub-Saharan Africa, we compared in a randomised clinical trial (NCT01030458) single-pill combinations of old and new antihypertensive drugs in patients (30-69 years) with uncomplicated hypertension (140-179/90-109 mm Hg). After 4 weeks off treatment, 183 of 294 screened patients were assigned to once daily bisoprolol/hydrochlorothiazide 5/6.25 mg (n=89; R) or amlodipine/valsartan 5/160 mg (n=94; E) and followed up for 6 months. To control blood pressure (<140/<90 mm Hg), bisoprolol and amlodipine could be doubled (10 mg per day) and α-methyldopa (0.5-2 g per day) added. Sitting blood pressure fell by 19.5/12.0 mm Hg in R patients and by 24.8/13.2 mm Hg in E patients and heart rate decreased by 9.7 beats per minute in R patients with no change in E patients (-0.2 beats per minute). The between-group differences (R minus E) were 5.2 mm Hg (P<0.0001) systolic, 1.3 mm Hg (P=0.12) diastolic, and 9.6 beats per minute (P<0.0001). In 57 R and 67 E patients with data available at all visits, these estimates were 5.5 mm Hg (P<0.0001) systolic, 1.8 mm Hg (P=0.07) diastolic and 9.8 beats per minute (P<0.0001). In R compared with E patients, 45 vs 37% (P=0.13) proceeded to the higher dose of randomised treatment and 33 vs 9% (P<0.0001) had α-methyldopa added. There were no between-group differences in symptoms except for ankle oedema in E patients (P=0.012). In conclusion, new compared with old drugs lowered systolic blood pressure more and therefore controlled hypertension better in native African black patients.
- Bioequivalence study of 2 formulations of film-coated tablets containing a fixed dose combination of bisoprolol fumarate 5 mg and hydrochlorothiazide 6.25 mg in healthy subjects. [Journal Article, Randomized Controlled Trial]
- Drug Res (Stuttg) 2013 May; 63(5):243-9.
The present study was conducted to compare the bioavailability of 2 formulations of fixed-dose combination of bisoprolol fumarate 5 mg and hydrochlorotiazide (HCT) 6.25 mg film-coated tablet (test and reference formulations).This study was a randomized, single-blind, 2-period, 2-sequence cross-over study which included 18 healthy adult male and female subjects under fasting condition. The pharmacokinetic parameters, AUCt, AUCinf, Cmax, tmax, and t½ were determined based on the concentrations of bisoprolol (CAS 66722-44-9) and HCT (CAS 58-93-5), using ultra-performance liquid chromatography with tandem mass spectrometer detector (UPLC-MS/MS). In each of the 2 study periods (with a washout of 1 week) a single dose of test or reference product was administered.The geometric mean ratios (90% CI) of the test drug/reference drug for bisoprolol were 97.22% (93.75-100.83%) for AUCt(0-48), 97.20% (93.97-100.54%) for AUCinf, and 100.36% (93.83-107.34%) for Cmax; while those for HCT were 93.22% (84.72-102.57%), 93.39% (85.43-102.10%) and 99.39% (85.45-115.61%), for AUCt(0-24), AUCinf, and Cmax, respectively. The differences between the test and reference drug products for tmax values of bisoprolol as well as t½ values of both bisoprolol and hydrochlorothiazide were not statistically significant; yet, the difference was statistically significant for the tmax values of hydrochlorothiazide. There was no adverse event encountered during this bioequivalence test.It was concluded that the 2 formulations of fixed dose combination of bisoprolol fumarate 5 mg and hydrochlorotiazide (HCT) 6.25 mg film-coated tablet (the test and reference products) were bioequivalent.
- Fully validated simultaneous determination of bisoprolol fumarate and hydrochlorothiazide in their dosage forms using different voltammetric, chromatographic, and spectrophotometric analytical methods. [Journal Article, Validation Studies]
- J AOAC Int 2013 Jan-Feb; 96(1):42-51.
Voltammetric, chromatographic, and spectrophotometric methods were developed for the simultaneous determination of bisoprolol fumarate (BIS) and hydrochlorothiazide (HCZ). Differential pulse and square wave voltammetry techniques were used to analyze BIS and HCZ simultaneously by measuring at about 1400 and 1100 mV, respectively. RP-HPLC was the second method for simultaneous analysis of the compounds. The mixture of BIS, HCZ, and moxifloxacin as an internal standard was separated on an RP Zorbax Eclipse XDB-C18 column (150 x 4.6 mm, id, 5 microm particle size) using acetonitrile-15 mM phosphate (25+75, v/v) mobile phase at a 1.0 mL/min flow rate. The third method was based on first derivative of the ratio-spectra method obtained from the measurements of the amplitudes at 246 and 257 nm for BIS and HCZ, respectively. All the proposed methods were effectively applied for the simultaneous determination of BIS and HCZ in tablet dosage forms without any time-consuming extraction, sample preparation, or derivatization procedures.
- [Telangiectasia during amlodipine therapy]. [Case Reports, English Abstract, Journal Article]
- Ann Dermatol Venereol 2013 Mar; 140(3):202-5.
Calcium inhibitors are recommended as first-line treatment in hypertension. We report the development of telangiectasia on the trunk and upper limbs in a female patient on amlodipine (Amlor(®)) that subsided on treatment discontinuation.A 63-year-old woman consulted for numerous asymptomatic stellate telangiectasias on her upper trunk and shoulders, with sparing of the face. No Darier's sign was seen and clinical examination was otherwise normal. The patient had been treated with amlodipine (Amlor(®)) and a combination of bisoprolol and hydrochlorothiazide (Lodoz(®)) for 5years for essential hypertension. Laboratory tests, which included serum tryptase assay, were normal. Histological analysis showed a normal epidermis with dilated superficial dermal capillaries and no inflammatory infiltrate or dermal elastosis. Amlodipine was discontinued and replaced with ramipril (an ACE inhibitor). The other treatments were changed over and the telangiectasias regressed spontaneously within several months, with no relapse being seen at one year of follow-up.Reports of telangiectasia associated with calcium inhibitors most commonly involve the dihydropyridine family, of which amlodipine is a member. Inhibition of muscular contraction induced by this treatment results in vasodilatation, accounting for the associated antihypertensive properties, and this could play a role in telangiectasia formation. The literature contains reports of cases of photo-distributed telangiectasia, suggesting that as well as vasodilatation, calcium inhibitors may in certain cases cause abnormal sensitivity of blood vessels to ultraviolet radiation. The absence of facial lesions rules out the hypothesis of photo-induced lesions in our patient.
- Monitoring drug residues in donor blood/plasma samples using LC-(MS)/MS--a pilot study. [Letter, Research Support, Non-U.S. Gov't]
- Drug Test Anal 2013 May; 5(5):380-3.
Quality assurance of pharmaceutical products is of particular importance and thoroughly controlled. Among these, the preparation of human plasma follows strict guidelines from the point of donor selection to product processing. While various precautions particularly concerning antiviral treatment as well as quality assessment are standard procedure, tests for drug residues are rarely, if at all, conducted with fresh frozen plasma products. With the constantly increasing sensitivity and specificity of modern analytical instruments, the detection of trace amounts of therapeutics in plasma is feasible and can be applied to blood products where considered appropriate. To estimate the prevalence of a selection of commonly prescribed and over-the-counter drugs (including diuretics, beta-receptor blocking agents, contraceptives, β2 -agonists, antibiotics, antidepressants, analgesics, opioids, glucocorticosteroids, benzodiazepines, stimulants, and oral anti-diabetics) as well as cannabinoids in human donor plasma, a total of 100 specimens (61 female, 39 male) collected at the German Red Cross Organization in 2012 was subjected to an established analytical approach. The methodology was based on protein precipitation followed by liquid chromatographic-high resolution/high accuracy mass spectrometric analysis. Following initial test results, confirmatory analyses were conducted with respective reference substances employing a conventional liquid chromatography-triple-quadrupole mass spectrometer (LC-MS/MS) apparatus. Out of one hundred samples, five were found to contain diuretics (four hydrochlorothiazide and one torasemide), five contained beta-receptor blocking agents (four bisoprolol and one metoprolol), one was found with residues of pseudoephedrine (stimulant) and one with drosperinone (contraceptive). Overall, 12% of samples yielded detectable amounts of drug residues at concentrations estimated to levels common to individuals under therapeutic treatment. In addition, six aliquots of different lots of commercially available plasma preparations with solvent-detergent processing were tested. Here, no drug residues of the targeted therapeutics were detected.
- Simultaneous acquisition of the dissolution curves of two active ingredients in a binary pharmaceutical association, employing an on-line circulation system and chemometrics-assistance. [Journal Article, Research Support, Non-U.S. Gov't]
- J Pharm Biomed Anal 2013 Jan.:51-8.
The association of an on-line circulation system with a chemometrics-assisted UV detection strategy is described as a useful system to continuously monitor the dissolution of a pharmaceutical preparation containing two active ingredients, and as a tool for the simultaneous determination of the dissolution curves and dissolution profiles of the latter. Multivariate curve resolution with alternating least squares (MCR-ALS) was used as the chemometric tool to quantitate the analytes, while the hydrochlorothiazide-bisoprolol fumarate (HCT-BIS) association was employed as a model for method development. The experiments were carried out with a dissolution tester configured as apparatus II (paddles), under USP 32 official conditions. The suitability of the calibration procedure for quantitating the dissolved drugs was assessed according to ICH guidelines, with regards to linearity in the working range, specificity, accuracy and precision. Figures of merit, including limits of detection and quantitation were also determined, as well as the method's robustness with regards to detection wavelength range. The system was able to consistently provide very reproducible dissolution curves of commercial tablets, which were statistically similar to those furnished by a manual sampling technique, followed by HPLC analysis. To demonstrate the usefulness of the proposed system, the dissolution profiles of different lots of HCT-BIS tablets were acquired and three of them were conveniently compared at a 31 data point level, employing the f(1) and f(2) ("difference" and "similarity") indexes. Use of multiple data points for comparison ensured reliability of the results.