-
International Journal of Analytical... 2018Hypertension or high blood pressure is a harbinger of cardiovascular diseases. There are several classes of drugs used to treat hypertension. This review discusses the... (Review)
Review
Hypertension or high blood pressure is a harbinger of cardiovascular diseases. There are several classes of drugs used to treat hypertension. This review discusses the use of dried blood spots (DBSs) for the quantification by mass spectrometry (MS), tandem mass spectrometry (MS/MS), or, in some cases, by fluorescence detection methods the following antihypertensive medications: angiotensin-converting enzyme inhibitors (ramipril, ramiprilat, captopril, and lisinopril); angiotensin II receptor antagonists (valsartan, irbesartan, losartan, and losartan carboxylic acid); calcium channel blockers (verapamil, amlodipine, nifedipine, pregabalin, and diltiazem); blockers (guanfacine, doxazosin, and prazosin); blockers (propranolol, bisoprolol, atenolol, and metoprolol); endothelin receptor antagonists (bosentan and ambrisentan); and statins (simvastatin, atorvastatin, and rosuvastatin).
PubMed: 30154849
DOI: 10.1155/2018/3235072 -
Molecules (Basel, Switzerland) Jul 2017Our research to discover potential new multitarget agents led to the synthesis of 10 novel derivatives of cinnamic acids and propranolol, atenolol, 1-adamantanol,...
Our research to discover potential new multitarget agents led to the synthesis of 10 novel derivatives of cinnamic acids and propranolol, atenolol, 1-adamantanol, naphth-1-ol, and (benzylamino) ethan-1-ol. The synthesized molecules were evaluated as trypsin, lipoxygenase and lipid peroxidation inhibitors and for their cytotoxicity. Compound derived from phenoxyphenyl cinnamic acid and propranolol showed the highest lipoxygenase (LOX) inhibition (IC = 6 μΜ) and antiproteolytic activity (IC = 0.425 μΜ). The conjugate of simple cinnamic acid with propranolol showed the higher antiproteolytic activity (IC = 0.315 μΜ) and good LOX inhibitory activity (IC = 66 μΜ). Compounds and , derived from methoxylated caffeic acid present a promising combination of in vitro inhibitory and antioxidative activities. The isomer of also presented an interesting multitarget biological profile in vitro Molecular docking studies point to the fact that the theoretical results for LOX-inhibitor binding are identical to those from preliminary in vitro study.
Topics: Animals; Cell Line; Cinnamates; Lipoxygenase; Lipoxygenase Inhibitors; Mice; Propranolol; Protease Inhibitors; Soybean Proteins; Glycine max
PubMed: 28757554
DOI: 10.3390/molecules22081247 -
BMJ Case Reports Jul 2018An older male patient with a history of tachycardia treated with atenolol presented to an outside hospital on 22 February 2017 with acute right flank pain. He had a CT...
An older male patient with a history of tachycardia treated with atenolol presented to an outside hospital on 22 February 2017 with acute right flank pain. He had a CT scan which revealed a large right renal mass with acute haemorrhage. He was initially managed with interventional radiology guided embolism on 25 February 2017 due to the ongoing bleeding and haemodynamic instability. He was then transferred to our institution. He underwent right radical nephrectomy on 13 March 2017. His pathology revealed a 12.5×6×4.5 cm mass consistent with angiosarcoma of the right kidney with negative margins. Final pathology was pT2b with extension of the mass into the renal vein and perirenal adipose tissue. He was discharged soon after surgery. He was recommended to undergo adjuvant chemotherapy.
Topics: Aged; Chemotherapy, Adjuvant; Fatal Outcome; Flank Pain; Hemangiosarcoma; Humans; Image-Guided Biopsy; Kidney Neoplasms; Male; Nephrectomy; Renal Veins
PubMed: 30061122
DOI: 10.1136/bcr-2017-222672 -
BMJ Clinical Evidence Nov 2014Acute atrial fibrillation is rapid, irregular, and chaotic atrial activity of recent onset. Various definitions of acute atrial fibrillation have been used in the... (Review)
Review
INTRODUCTION
Acute atrial fibrillation is rapid, irregular, and chaotic atrial activity of recent onset. Various definitions of acute atrial fibrillation have been used in the literature, but for the purposes of this review we have included studies where atrial fibrillation may have occurred up to 7 days previously. Risk factors for acute atrial fibrillation include increasing age, cardiovascular disease, alcohol, diabetes, and lung disease. Acute atrial fibrillation increases the risk of stroke and heart failure. The condition resolves spontaneously within 24 to 48 hours in more than 50% of people; however, many people will require interventions to control heart rate or restore sinus rhythm.
METHODS AND OUTCOMES
We conducted a systematic review and aimed to answer the following clinical questions: What are the effects of interventions to prevent embolism, for conversion to sinus rhythm, and to control heart rate in people with recent-onset atrial fibrillation (within 7 days) who are haemodynamically stable? We searched: Medline, Embase, The Cochrane Library, and other important databases up to April 2014 (Clinical Evidence reviews are updated periodically; please check our website for the most up-to-date version of this review). We included harms alerts from relevant organisations such as the US Food and Drug Administration (FDA) and the UK Medicines and Healthcare products Regulatory Agency (MHRA).
RESULTS
We found 26 studies that met our inclusion criteria. We performed a GRADE evaluation of the quality of evidence for interventions.
CONCLUSIONS
In this systematic review, we present information relating to the effectiveness and safety of the following interventions: amiodarone, antithrombotic treatment before cardioversion, atenolol, bisoprolol, carvedilol, digoxin, diltiazem, direct current cardioversion, flecainide, metoprolol, nebivolol, propafenone, sotalol, timolol, and verapamil.
Topics: Acute Disease; Anti-Arrhythmia Agents; Atrial Fibrillation; Electric Countershock; Humans; Safety
PubMed: 25430048
DOI: No ID Found -
Frontiers in Cardiovascular Medicine 2016It is surprising that only about 50 years ago hypertension was considered an essential malady and not a treatable condition. Introduction of thiazide diuretics in late... (Review)
Review
It is surprising that only about 50 years ago hypertension was considered an essential malady and not a treatable condition. Introduction of thiazide diuretics in late 50s made some headway in successful treatment of hypertension and ambitious multicenter VA co-operative study (phase 1 and 2) started in 1964 for diastolic hypertension ranging between 90 and 129 mmHg and completed by 1971 established for the first time that treating diastolic hypertension reduced CV events such as stroke and heart failure and improved mortality. In the following decade, these results were confirmed for the wider US and non-US population, including women and goal-oriented BP treatment to diastolic 90 became the standard therapy recommendation. But isolated systolic hypertension (accounting for two-thirds of the 70 million hypertensive population in USA alone) was not considered treatable until 1991 when SHEP study (systolic hypertension in elderly program) was completed and showed tremendous benefits of treating systolic BP over 160 mmHg using only a simple regimen using small dose chlorthalidone with addition of atenolol if needed. In the next two decades, ALLHAT and other studies examined the comparability of outcomes with use of different classes and combinations of antihypertensive drugs. Although diastolic BP goal was established as 90 in the late 70s and later confirmed by HOT study, the goal BP for systolic hypertension was not settled until very recently with completion of SPRINT study. ACCORD study showed no significant difference in outcome with sys 140 vs. 120 in diabetics. But recently completed SPRINT study with somewhat similar protocol as in ACCORD but in non-diabetic showed almost one-quarter reduction in all-cause mortality and one-third reduction of CV events with systolic BP goal 120.
PubMed: 26942184
DOI: 10.3389/fcvm.2016.00003 -
World Journal of Cardiology Jan 2016Since the introduction of propranolol in the treatment of complicated infantile hemangiomas (IH) in 2008, other different beta-blockers, including timolol, acetabutolol,... (Review)
Review
Since the introduction of propranolol in the treatment of complicated infantile hemangiomas (IH) in 2008, other different beta-blockers, including timolol, acetabutolol, nadolol and atenolol, have been successfully used for the same purpose. Various hypotheses including vasoconstriction, inhibition of angiogenesis and the induction of apoptosis in proliferating endothelial cells have been advanced as the potential beta-blocker-induced effect on the accelerated IH involution, although the exact mechanism of action of beta-blockers remains unknown. This has generated an extraordinary interest in IH research and has led to the discovery of the role of the renin-angiotensin system (RAS) in the biology of IH, providing a plausible explanation for the beta-blocker induced effect on IH involution and the development of new potential indications for RAS drugs such as angiotensin-converting enzyme inhibitors and angiotensin-receptor blockers in the treatment of IH. This review is focused on the current use of cardiovascular drugs in the treatment of IH.
PubMed: 26839658
DOI: 10.4330/wjc.v8.i1.74 -
Veterinary Record Open Dec 2022Ivabradine is used to treat tachycardia; unlike atenolol, it does not affect blood pressure or myocardial contractility. This study compared the impact of ivabradine and...
BACKGROUND
Ivabradine is used to treat tachycardia; unlike atenolol, it does not affect blood pressure or myocardial contractility. This study compared the impact of ivabradine and atenolol on heart rate (HR) and HR variability (HRV) during a 24 h period, feeding and sleeping times, via a Holter electrocardiogram in healthy cats. We hypothesised that ivabradine and atenolol would lower the HRs equally well, even at times of excitement and rest, such as during feeding and sleep; that ivabradine, unlike atenolol, would have an effect on HRV.
METHODS
Five clinically healthy cats were used in the prospective blinded crossover study receiving 3 days of ivabradine (0.30 mg/kg per os twice daily) followed by atenolol (6.25 mg/cat per os twice daily, range 1.3-2.0 mg/kg) or receiving atenolol followed by ivabradine. A placebo period was initiated before the start of the crossover test, data obtained during that period were used as a baseline (BL). Evaluation parameters included HR and HRV, for the whole 24 h period and for feeding and sleeping times, comparing the effect of ivabradine and atenolol with BL.
RESULTS
The HR for the whole 24 h, feeding and sleeping times, were significantly lower with ivabradine and atenolol, compared to BL ( < 0.05). The HRV for the whole 24 h and sleeping time were significantly higher after ivabradine compared with BL and after atenolol.
CONCLUSIONS
In healthy cats, ivabradine and atenolol significantly reduced the HR regardless of excitement and rest; their effects were comparable. Ivabradine significantly increased HRV in comparison to BL whereas atenolol did not.
PubMed: 35154785
DOI: 10.1002/vro2.28 -
Microorganisms Oct 2022The targeting of bacterial virulence is proposed as a promising approach to overcoming the bacterial resistance development to antibiotics. is one of the most important...
The targeting of bacterial virulence is proposed as a promising approach to overcoming the bacterial resistance development to antibiotics. is one of the most important gut pathogens that cause a wide diversity of local and systemic illnesses. The virulence is controlled by interplayed systems namely Quorum sensing (QS) and type three secretion system (T3SS). Furthermore, the spy on the host cell via sensing the adrenergic hormones enhancing its virulence. The current study explores the possible anti-virulence activities of β-adrenoreceptor blocker atenolol against serovar Typhimurium in vitro, in silico, and in vivo. The present findings revealed a significant atenolol ability to diminish the biofilm formation, invasion into HeLa cells, and intracellular replication inside macrophages. Atenolol significantly downregulated the encoding genes of the T3SS-type II, QS receptor Lux analogs , and norepinephrine membranal sensors qseC and qseE. Moreover, atenolol significantly protected mice against . For testing the possible mechanisms for atenolol anti-virulence activities, an in silico molecular docking study was conducted to assess the atenolol binding ability to QS receptor SdiA and norepinephrine membranal sensors QseC. Atenolol showed the ability to compete on the targets. In conclusion, atenolol is a promising anti-virulence candidate to alleviate the pathogenesis by targeting its QS and T3SS systems besides diminishing the eavesdropping on the host cells.
PubMed: 36296252
DOI: 10.3390/microorganisms10101976 -
Journal of Pharmaceutical Analysis Dec 2021Enantioseparation of three β-blockers, i.e., atenolol, metoprolol and propranolol, was studied on amylose tris(3-chloro-5-methylphenylcarbamate) immobilized chiral...
Enantioseparation of three β-blockers, i.e., atenolol, metoprolol and propranolol, was studied on amylose tris(3-chloro-5-methylphenylcarbamate) immobilized chiral stationary phase using supercritical fluid chromatography (SFC). The effect of organic modifiers (methanol, isopropanol and their mixture), column temperature and back pressure on chiral separation of β-blockers was evaluated. Optimum chromatographic separation with respect to resolution, retention, and analysis time was achieved using a mixture of CO and 0.1% isopropyl amine in isopropanol: methanol (50:50, ), in 75:25 () ratio. Under the optimized conditions, the resolution factors ( ) and separation factors (α) were greater than 3.0 and 1.5, respectively. Further, with increase in temperature (25-45 °C) and pressure (100-150 bars) there was corresponding decrease in retention factors (), α and . However, a reverse trend (α and ) was observed for atenolol with increase in temperature. The thermodynamic data from van't Hoff plots revealed that the enantioseparation was enthalpy driven for metoprolol and propranolol while entropy driven for atenolol. To understand the mechanism of chiral recognition and the elution behavior of the enantiomers, molecular docking studies were performed. The binding energies obtained from simulation studies were in good agreement with the elution order found experimentally and also with the free energy values. The method was validated in the concentration range of 0.5-10 μg/mL for all the enantiomers. The limit of detection and limit of quantitation ranged from 0.126 to 0.137 μg/mL and 0.376-0.414 μg/mL, respectively. The method was used successfully to analyze these drugs in pharmaceutical preparations.
PubMed: 35028180
DOI: 10.1016/j.jpha.2020.12.005 -
Circulation Journal : Official Journal... Mar 2023α/β- and β-blockers are essential in pregnant women's perinatal congenital heart disease management. Nevertheless, data on the effects of α/β- and β-blockers on...
BACKGROUND
α/β- and β-blockers are essential in pregnant women's perinatal congenital heart disease management. Nevertheless, data on the effects of α/β- and β-blockers on pregnant women and fetuses are limited. We examined the risks of neonatal hypoglycemia and small for gestational age (SGA) associated with maternal exposure to α/β- and β-blockers.Methods and Results: All consecutive pregnant women with heart disease admitted to our hospital between January 2014 and October 2020 were included. Of 306 pregnancies (267 women), 32 were in the α/β-blocker group, 11 were in the β-blocker group, and 263 were in the control group. All 32 pregnancies in the α/β-blocker group were treated with carvedilol. In the β-blocker group, 4 women were treated with bisoprolol, 3 were treated with propranolol, 2 were treated with atenolol, 1 was treated with metoprolol, and 1 was treated nadolol. The incidence of neonatal hypoglycemia was higher in pregnant women taking carvedilol than in the control group (P=0.025). SGA was observed significantly more frequently in pregnant women taking β-blockers than in the carvedilol and control groups (P<0.001).
CONCLUSIONS
Carvedilol administration during pregnancy was associated with neonatal hypoglycemia; however, it did not occur in a time- or dose-dependent manner. Routine monitoring of blood glucose levels in newborns exposed to α/β- and β-blockers is essential.
Topics: Female; Infant, Newborn; Humans; Pregnancy; Carvedilol; Gestational Age; Adrenergic beta-Antagonists; Metoprolol; Hypoglycemia
PubMed: 36823100
DOI: 10.1253/circj.CJ-22-0647