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Journal of Veterinary Cardiology : the... Mar 2024A nine-year-old spayed female domestic shorthair cat with a previous diagnosis of hypertrophic cardiomyopathy and treated for one month with atenolol (6.25 mg q 12 h)...
A nine-year-old spayed female domestic shorthair cat with a previous diagnosis of hypertrophic cardiomyopathy and treated for one month with atenolol (6.25 mg q 12 h) was referred for respiratory distress and anorexia. The cat was diagnosed with pulmonary oedema secondary to obstructive hypertrophic cardiomyopathy. After stabilisation, she was discharged with furosemide (1 mg/kg q 12 h), clopidogrel (18.75 mg q 24 h), atenolol (6.25 mg q 12 h), and mirtazapine (2 mg/cat q 24 h) to increase appetite. At recheck, the cat was lethargic and presented with severe bradycardia with a junctional escape rhythm and ventriculoatrial conduction. The mirtazapine was discontinued due to its possible side-effects on cardiac rhythm. After three days, the atenolol was halved because the bradyarrhythmia was still present. After 10 days, the rhythm returned to sinus; atenolol was reintroduced twice daily with no further side-effects. The absence of a sinus rhythm with a junctional escape rhythm and P' retroconduction is compatible with a third-degree sinus block or a sinus standstill; the differentiation of these rhythm disturbances is impossible, based on the surface electrocardiogram (ECG). The sinus rhythm was restored after mirtazapine was withdrawn. However, it is not possible to rule out the role of the atenolol or the combined effect of the two drugs. The cat was affected by hypertrophic cardiomyopathy, and the role of myocardial remodelling cannot be excluded. This is the first time that a bradyarrhythmia consequent to the treatment with atenolol and mirtazapine was described in a cat.
PubMed: 38735230
DOI: 10.1016/j.jvc.2024.03.003 -
European Journal of Pharmaceutical... Jul 2022Swallowing oral solid dosage forms is challenging in patients with dysphagia who are at risk of aspiration or choking. The most common method to facilitate drug...
Swallowing oral solid dosage forms is challenging in patients with dysphagia who are at risk of aspiration or choking. The most common method to facilitate drug administration in dysphagia patients is to mix the powdered drug with a small amount of thickened water, however little is known about the effects of this method on in vivo bioavailability of drugs. This study aimed to evaluate the impact of thickened liquids on dissolution rate and bioavailability of levetiracetam as a model drug. Powdered commercial tablets of levetiracetam, carbamazepine, atenolol and cefixime were mixed with water thickened with two commercial thickeners, modified maize starch (MS) and xanthan gam (XG), at three thickness levels: nectar, honey and pudding in test groups, and mixed with only water in the control group. At the first stage, the effects of thickened water on in vitro drug release of 4 drugs (levetiracetam, carbamazepine, atenolol and cefixime) were tested by using dialysis membrane method. Addition of both thickeners significantly reduced the release of three drugs compared to the control group, except carbamazepine. Levetiracetam which had the highest solubility was chosen as the model drug for in vivo experiments. In the second stage, New Zealand albino female rabbits (n=24) were divided into two groups as: control group (water+drug, n=6) and test group (thickened water+drug, n=18). Powdered levetiracetam tablets were mixed with water thickened with XG (n=9, 1.2%, 2.4%, 3.6%) and MS (n=9, 4%, 6%, 8%) at three thickness levels and administered to the rabbits by intragastric gavage. Blood samples were collected at 9 time points following administration. After two-weeks of wash-out, test groups were crossed over and sample collection was repeated. Blood samples were analysed using liquid chromatography with tandem mass spectrometry (LC-MS/MS). An in vitro-in vivo correlation (IVIVC) model was developed using in vitro drug dissolution (%) and in vivo plasma concentrations of levetiracetam for control group and test groups. The peak plasma concentration (C) was lower and time to reach C (t) was relatively higher in test groups compared to control group. The lowest C was detected at the highest thickness level, however, the differences between groups were not statistically significant (p=0.117 and p=0.495 for C and t, respectively). No significant difference in total amount of levetiracetam absorbed (AUC) was found between groups (p=0.215 and p=0.183 for AUC and AUC, respectively). The comparisons according to the type of thickener also revealed that pharmacokinetic parameters did not significantly differ between groups, except for a significantly lower C when drug was mixed with MS-thickened water at nectar consistency (1.2%) compared to drug mixed with XG (4%) at the same thickness level (p=0.038). A good correlation was observed between in vitro and in vivo data, which was characterized by higher r values as the concentration of the thickening agents was increased, but not for all thickness levels studied, indicating an inability of this in vitro model to fully predict the in vivo response. These results suggest that regardless of the thickness level, the administration of levetiracetam with two commercial thickening agents commonly used in dysphagia for safe swallowing, do not affect the pharmacokinetic efficiency and thus, the bioavailability of the drug.
Topics: Animals; Atenolol; Biological Availability; Carbamazepine; Cefixime; Chromatography, Liquid; Deglutition Disorders; Diet; Food Additives; Humans; Levetiracetam; Plant Nectar; Rabbits; Starch; Tablets; Tandem Mass Spectrometry; Viscosity; Water
PubMed: 35489612
DOI: 10.1016/j.ejps.2022.106197 -
Cureus Dec 2020Subacute thyroiditis is usually a self-limiting inflammatory condition. The clinical presentation varies from person to person, but usually includes neck pain or...
Subacute thyroiditis is usually a self-limiting inflammatory condition. The clinical presentation varies from person to person, but usually includes neck pain or discomfort and a painful diffuse goiter. There is at times a transient episode of hyperthyroidism followed by euthyroidism and sometimes hypothyroidism. We describe the case of a previously healthy 29-year-old female presenting with symptoms consistent with subacute thyroiditis. The patient had recently recovered from a mild episode of COVID-19 infection. Labs and imaging were consistent with the clinical diagnosis of subacute thyroiditis. The patient was provided symptomatic treatment with prednisone and atenolol and had an uneventful recovery.
PubMed: 33510992
DOI: 10.7759/cureus.12301 -
European Stroke Journal Mar 2023Hypertension is the leading modifiable risk factor for cerebral small vessel diseases (SVDs). Yet, it is unknown whether antihypertensive drug classes differentially...
The EffecTs of Amlodipine and other Blood PREssure Lowering Agents on Microvascular FuncTion in Small Vessel Diseases (TREAT-SVDs) trial: Study protocol for a randomised crossover trial.
BACKGROUND
Hypertension is the leading modifiable risk factor for cerebral small vessel diseases (SVDs). Yet, it is unknown whether antihypertensive drug classes differentially affect microvascular function in SVDs.
AIMS
To test whether amlodipine has a beneficial effect on microvascular function when compared to either losartan or atenolol, and whether losartan has a beneficial effect when compared to atenolol in patients with symptomatic SVDs.
DESIGN
TREAT-SVDs is an investigator-led, prospective, open-label, randomised crossover trial with blinded endpoint assessment (PROBE design) conducted at five study sites across Europe. Patients aged 18 years or older with symptomatic SVD who have an indication for antihypertensive treatment and are suffering from either sporadic SVD and a history of lacunar stroke or vascular cognitive impairment (group A) or CADASIL (group B) are randomly allocated 1:1:1 to one of three sequences of antihypertensive treatment. Patients stop their regular antihypertensive medication for a 2-week run-in period followed by 4-week periods of monotherapy with amlodipine, losartan and atenolol in random order as open-label medication in standard dose.
OUTCOMES
The primary outcome measure is cerebrovascular reactivity (CVR) as determined by blood oxygen level dependent brain MRI signal response to hypercapnic challenge with change in CVR in normal appearing white matter as primary endpoint. Secondary outcome measures are mean systolic blood pressure (BP) and BP variability (BPv).
DISCUSSION
TREAT-SVDs will provide insights into the effects of different antihypertensive drugs on CVR, BP, and BPv in patients with symptomatic sporadic and hereditary SVDs.
FUNDING
European Union's Horizon 2020 programme.
TRIAL REGISTRATION
NCT03082014.
Topics: Humans; Amlodipine; Antihypertensive Agents; Blood Pressure; Atenolol; Losartan; Cross-Over Studies; Prospective Studies; Randomized Controlled Trials as Topic
PubMed: 37021189
DOI: 10.1177/23969873221143570 -
Comparative Analysis on Single- and Multiherb Strategies in Coronary Artery Atherosclerosis Therapy.Cardiology Research and Practice 2021Herbal medicine unswervingly serves human health by modernizing preparation and administration. Coronary artery atherosclerosis is a serious threat to human health and...
Herbal medicine unswervingly serves human health by modernizing preparation and administration. Coronary artery atherosclerosis is a serious threat to human health and survival all over the world. Following experimental and clinical evidence, we collected four herbal treatments containing herbal strategy I (San Qi), II (Injectio Salvia Miltiorrhizae), III (Danhong injection), and IV (Taoren Honghua Jian granule) against coronary artery disease. In order to analyze their similarities and differences in controlling coronary artery atherosclerosis, we investigated each herb of four strategies and revealed that the number of active components and molecule targets is increasing with the herb category of herbal strategy. Nitric oxide-associated carbonate dehydratase activity and nitrogen metabolism are tacitly enriched by target corresponding genes with statistical significance in four strategies. The herbal strategy with multiherb not merely possesses more amounts and interactions of target proteins than the strategy with single-herb but also enlarges interaction partners of target proteins like PTPN11 and STAT3 in strategy II, III, and IV. Whereas single-herb also involves regulating network core proteins in consistent with compatibility, such as SRC and PIK3R1 that are mostly targeted by strategy I, III, and IV. Comparing the targets of the herbal strategies and three existing drugs (atenolol, pravastatin and propranolol) and the symbols of coronary artery atherosclerosis, we discovered that MAOA, HTR1A, and ABCG2 are overlapping in the three groups. Hence, our work enables people to better understand the connections and distinctions of single- and multiherb on the healing of coronary artery atherosclerosis.
PubMed: 34012683
DOI: 10.1155/2021/6621925 -
Clinical Journal of the American... Apr 2018There is a paucity of data available to describe drug dialyzability. Of the available information, most was obtained before implementation of modern hemodialysis... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND AND OBJECTIVES
There is a paucity of data available to describe drug dialyzability. Of the available information, most was obtained before implementation of modern hemodialysis membranes. Our study characterized dialyzability of the most commonly prescribed -blockers in patients undergoing high-flux hemodialysis.
DESIGN, SETTING, PARTICIPANTS, & MEASUREMENTS
Patients on hemodialysis (=8) were recruited to an open label, pharmacokinetic, four-way crossover trial. Single doses of atenolol, metoprolol, bisoprolol, and carvedilol were administered on separate days in random order to each patient. Plasma and dialysate drug concentrations were measured, and dialyzability was determined by the recovery clearance and arterial venous difference methods.
RESULTS
Using the recovery clearance method, the dialytic clearance values for atenolol, metoprolol, bisoprolol, and carvedilol were 72, 87, 44, and 0.2 ml/min, respectively (<0.001). Applying the arterial venous difference method, the dialytic clearance values of atenolol, metoprolol, bisoprolol, and carvedilol were 167, 114, 96, and 24 ml/min, respectively (<0.001).
CONCLUSIONS
Atenolol and metoprolol are extensively cleared by hemodialysis compared with the negligible dialytic clearance of carvedilol. Contrary to estimates of dialyzability on the basis of previous literature, our data indicate that bisoprolol is also dialyzable. This finding highlights the importance of conducting dialyzability studies to definitively characterize drug dialytic clearance.
Topics: Adrenergic beta-Antagonists; Adult; Aged; Aged, 80 and over; Atenolol; Bisoprolol; Carvedilol; Cross-Over Studies; Dialysis Solutions; Female; Humans; Male; Metoprolol; Middle Aged; Renal Dialysis
PubMed: 29519953
DOI: 10.2215/CJN.07470717 -
The Journal of Physiology Feb 2018While values of arterial pressure during sleep are predictive of cardiovascular risk, the autonomic mechanisms underlying the cardiovascular effects of sleep remain...
KEY POINTS
While values of arterial pressure during sleep are predictive of cardiovascular risk, the autonomic mechanisms underlying the cardiovascular effects of sleep remain poorly understood. Here, we assess the autonomic mechanisms of the cardiovascular effects of sleep in C57Bl/6J mice, taking advantage of a novel technique for continuous intraperitoneal infusion of autonomic blockers. Our results indicate that non-REM sleep decreases arterial pressure by decreasing sympathetic vasoconstriction, decreases heart rate by balancing parasympathetic activation and sympathetic withdrawal, and increases cardiac baroreflex sensitivity mainly by increasing fluctuations in parasympathetic activity. Our results also indicate that REM sleep increases arterial pressure by increasing sympathetic activity to the heart and blood vessels, and increases heart rate, at least in part, by increasing cardiac sympathetic activity. These results provide a framework for generating and testing hypotheses on cardiovascular derangements during sleep in mouse models and human patients.
ABSTRACT
The values of arterial pressure (AP) during sleep predict cardiovascular risk. Sleep exerts similar effects on cardiovascular control in human subjects and mice. We aimed to determine the underlying autonomic mechanisms in 12 C57Bl/6J mice with a novel technique of intraperitoneal infusion of autonomic blockers, while monitoring the electroencephalogram, electromyogram, AP and heart period (HP, i.e. 1/heart rate). In different sessions, we administered atropine methyl nitrate, atenolol and prazosin to block muscarinic cholinergic, β -adrenergic and α -adrenergic receptors, respectively, and compared each drug infusion with a matched vehicle infusion. The decrease in AP from wakefulness to non-rapid-eye-movement sleep (N) was abolished by prazosin but was not significantly affected by atropine and atenolol, which, however, blunted the accompanying increase in HP to a similar extent. On passing from N to rapid-eye-movement sleep (R), the increase in AP was significantly blunted by prazosin and atenolol, whereas the accompanying decrease in HP was blunted by atropine and abolished by atenolol. Cardiac baroreflex sensitivity (cBRS, sequence technique) was dramatically decreased by atropine and slightly increased by prazosin. These data indicate that in C57Bl/6J mice, N decreases mean AP by decreasing sympathetic vasoconstriction, increases HP by balancing parasympathetic activation and sympathetic withdrawal, and increases cBRS mainly by increasing fluctuations in parasympathetic activity. R increases mean AP by increasing sympathetic vasoconstriction and cardiac sympathetic activity, which also explains, at least in part, the concomitant decrease in HP. These data represent the first comprehensive assessment of the autonomic mechanisms of cardiovascular control during sleep in mice.
Topics: Animals; Anti-Arrhythmia Agents; Arterial Pressure; Cardiovascular System; Heart Rate; Humans; Male; Mice; Mice, Inbred C57BL; Sleep; Sympathetic Nervous System; Vasoconstriction; Wakefulness
PubMed: 29266348
DOI: 10.1113/JP275353 -
Brazilian Oral Research 2020This study evaluates how atenolol affects dental mineralization in offspring of female spontaneously hypertensive rats (fSHR) and normotensive Wistar rats (fW). fSHR and...
This study evaluates how atenolol affects dental mineralization in offspring of female spontaneously hypertensive rats (fSHR) and normotensive Wistar rats (fW). fSHR and fW were treated with atenolol (100 mg/Kg/day, orally) during pregnancy and lactation. Non-treated fSHR and fW were the control groups. Enamel and dentin hardness were analyzed (Knoop, 15 g load, 10s) in mandibular incisor teeth (IT) and molar teeth (MT) obtained from the male offspring of atenolol-treated and non-treated fWistar and fSHR. Data were analyzed by ANOVA, followed by Tukey post hoc test (p < 0.05). Atenolol reduced the arterial blood pressure (SBP) in fSHR, but it did not change the SBP in fW. The offspring of non-treated fSHR had lower enamel (IT and MT) and dentin (IT) hardness than the offspring of non-treated fW (p < 0.05). Atenolol increased enamel and dentin hardness in the IT obtained from the offspring of fSHR and fW (p<0.05), but the offspring of fSHR presented higher values (p < 0.05). Atenolol did not alter enamel width in the IT obtained from any of the groups, but it increased enamel and dentin hardness in the IT obtained from the offspring of fSHR and fW. Atenolol affected the IT obtained from the offspring of fSHR. Atenolol increased only enamel hardness in the MT obtained from the offspring of fW. In conclusion, maternal hypertension reduces tooth hard tissues, and treatment with atenolol increases tooth hardness in male offspring of hypertensive and normotensive female rats.
Topics: Animals; Atenolol; Dental Enamel; Dentin; Female; Hardness; Hypertension; Male; Pregnancy; Rats; Rats, Wistar
PubMed: 32785480
DOI: 10.1590/1807-3107bor-2020.vol34.0086 -
International Journal of Molecular... Jan 2022MATE1 (multidrug and toxin extruder 1) and OCT2 (organic cation transporter 2) play critical roles in organic cation excretion by the human kidney. The transporter...
MATE1 (multidrug and toxin extruder 1) and OCT2 (organic cation transporter 2) play critical roles in organic cation excretion by the human kidney. The transporter turnover rate (TOR) is relevant to understanding both their transport mechanisms and interpreting the in vitro-in vivo extrapolation (IVIVE) required for physiologically-based pharmacokinetic (PBPK) modeling. Here, we use a quantitative western blot method to determine TORs for MATE1 and OCT2 proteins expressed in CHO cells. MATE1 and OCT2, each with a C-terminal V-5 epitope tag, were cell surface biotinylated and the amount of cell surface MATE1 and OCT2 protein was quantified by western analysis, using standard curves for the V5 epitope. Cell surface MATE1 and OCT2 protein represented 25% and 24%, respectively, of the total expression of these proteins in CHO cells. The number of cell surface transporters was ~55 fmol cm for MATE1 and ~510 fmol cm for OCT2. Dividing these values into the different J values for transport of MPP, metformin, and atenolol mediated by MATE1 and OCT2 resulted in calculated TOR values (±SE, = 4) of 84.0 ± 22.0 s and 2.9 ± 0.6 s; metformin, 461.0 ± 121.0 s and 12.6 ± 2.4 s; atenolol, 118.0 ± 31.0 s, respectively. These values are consistent with the TOR values determined for a variety of exchangers (NHEs), cotransporters (SGLTs, Lac permease), and uniporters (GLUTs, ENTs).
Topics: Animals; CHO Cells; Cricetulus; Gene Expression; Humans; Organic Cation Transport Proteins; Organic Cation Transporter 2; Protein Transport
PubMed: 35163393
DOI: 10.3390/ijms23031472 -
Experimental and Therapeutic Medicine Aug 2020Infantile haemangioma (IH) is a benign vascular tumour type that occurs in 3-10% of infants. In the present meta-analysis, previous studies comparing clinical outcomes,...
Infantile haemangioma (IH) is a benign vascular tumour type that occurs in 3-10% of infants. In the present meta-analysis, previous studies comparing clinical outcomes, including the recovery rate and haemangioma activity score (HAS), adverse effects and relapse rates, were compared between patients treated with atenolol and those treated with propranolol for IH. A systematic search in various databases, including Medline, Cochrane Controlled Register of Trials, ScienceDirect and Google Scholar from inception until July 2019 was performed. The Cochrane risk of bias tool was used to assess the quality of published trials. A meta-analysis with a random-effects model and reported pooled mean differences (MD) or odds ratios (OR) with 95% CIs was performed. In total, 8 studies including 608 participants were analyzed. Only 2 studies were randomized controlled trials, while the majority of studies had low or unclear bias risks. Except for the response to medication (pooled OR=1.49; 95% CI, 0.85-2.18), all other outcomes (HAS, adverse reactions and relapse rate) were better for the atenolol group than the propranolol group. Atenolol resulted in better HAS (pooled MD=0.16; 95% CI, -0.42 to 0.73). Propranolol had more adverse reactions (pooled OR=2.17; 95% CI, 0.93-5.06) and a higher relapse rate (pooled OR, 1.67; 95% CI, 0.44-6.41) when compared to atenolol. However, these findings were not statistically significant. The results of this analysis suggest that atenolol may be non-inferior to propranolol and may offer advantages, including lower adverse reactions and relapse rates.
PubMed: 32742396
DOI: 10.3892/etm.2020.8842