Efficacy Of Metoprolol Research Articles

A predictive model of response to metoprolol in children and adolescents with postural tachycardia syndrome

BackgroundThe present work was designed to explore whether electrocardiogram (ECG) index-based models could predict the effectiveness of metoprolol therapy in pediatric patients with postural tachycardia syndrome (POTS).MethodsThis study consisted of a training set and an external validation set. Children and adolescents with POTS who were given metoprolol treatment were enrolled, and after follow-up, they were grouped into non-responders and responders depending on the efficacy of metoprolol. The difference in pre-treatment baseline ECG indicators was analyzed between the two groups in the training set. Binary logistic regression analysis was further conducted on the association between significantly different baseline variables and therapeutic efficacy. Nomogram models were established to predict therapeutic response to metoprolol. The receiver-operating characteristic curve (ROC), calibration, and internal validation were used to evaluate the prediction model. The predictive ability of the model was validated in the external validation set.ResultsOf the 95 enrolled patients, 65 responded to metoprolol treatment, and 30 failed to respond. In the responders, the maximum value of the P wave after correction (Pcmax), P wave dispersion (Pd), Pd after correction (Pcd), QT interval dispersion (QTd), QTd after correction (QTcd), maximum T-peak-to-T-end interval (Tpemax), and T-peak-to-T-end interval dispersion (Tped) were prolonged (all P < 0.01), and the P wave amplitude was increased (P < 0.05) compared with those of the non-responders. In contrast, the minimum value of the P wave duration after correction (Pcmin), the minimum value of the QT interval after correction (QTcmin), and the minimum T-peak-to-T-end interval (Tpemin) in the responders were shorter (P < 0.01, < 0.01 and < 0.01, respectively) than those in the non-responders. The above indicators were screened based on the clinical significance and multicollinearity analysis to construct a binary logistic regression. As a result, pre-treatment Pcmax, QTcmin, and Tped were identified as significantly associated factors that could be combined to provide an accurate prediction of the therapeutic response to metoprolol among the study subjects, yielding good discrimination [area under curve (AUC) = 0.970, 95% confidence interval (CI) 0.942–0.998] with a predictive sensitivity of 93.8%, specificity of 90.0%, good calibration, and corrected C-index of 0.961. In addition, the calibration curve and standard curve had a good fit. The accuracy of internal validation with bootstrap repeated sampling was 0.902. In contrast, the kappa value was 0.769, indicating satisfactory agreement between the predictive model and the results from the actual observations. In the external validation set, the AUC for the prediction model was 0.895, and the sensitivity and specificity were 90.9% and 95.0%, respectively.ConclusionsA high-precision predictive model was successfully developed and externally validated. It had an excellent predictive value of the therapeutic effect of metoprolol on POTS among children and adolescents.

FAILURE TO CONSIDER FUTURE ATRIAL FIBRILLATION RATE CONTROL NEEDS AFTER PRESENTATION TO THE EMERGENCY DEPARTMENT WITH RAPID RATE

Atrial fibrillation (AF) usually presents to the emergency room (ED) with a rapid ventricular rate, which commonly, but not always, is symptomatic. Rate control is usually easily managed with diltiazem (DTZ) and beta blockers (BBs), typically metoprolol (MTP). Sinus rhythm is frequently restored within 48 hours by means of spontaneous conversion, electrical cardioversion, or medications. However, AF recurs within one year in 60-80% of these subjects. There are little data describing doses of DTZ and MTP used for AF rate control at discharge. A retrospective study of 576 patients presenting with acute AF were evaluated for admission and discharge rate control medications (RCMs). For the 319 (68%) patients with a ventricular rate ≥110bpm the admission and discharge dose of MTP was 61mg and 63mg and DTZ was 195mg and 204mg, respectively. Those who remained in AF had a modest increase in the two medications compared to the patients who converted to sinus rhythm. Current guidelines recommend DTZ up to 300 to 400mg and MTP up to 300mg for rate control for select patients. Concerns about high doses of MTP are mitigated by the MERIT-HF Trial demonstrating improved mortality and symptoms with doses of MTP up to 200mg demonstrating the safety and efficacy of MTP in high risk patients. Lack of follow-up of future AF recurrences is a limitation of the study. For those patients with acute AF and a heart rate (HR) &gt;110bpm, a minimal increase in RCMs for those in AF at discharge was noted.

Efficacy of Metoprolol Combined with Trimetazidine in the Treatment of Coronary Heart Disease and Heart Failure

Efficacy of Metoprolol Combined with Trimetazidine in the Treatment of Coronary Heart Disease and Heart Failure

FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers.&#x0D; Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin.&#x0D; Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability.&#x0D; Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.

Twenty-four-hour urine NE level as a predictor of the therapeutic response to metoprolol in children with recurrent vasovagal syncope.

Vasovagal syncope (VVS) is a heterogeneous disorder that creates challenges for treatment. Metoprolol is an important therapeutic option for children with VVS. The study examined the predictive value of 24-h urine norepinephrine (NE) levels in the assessment of the therapeutic efficacy of metoprolol for recurrent VVS in children. Thirty-eight children with recurrent VVS and 20 healthy children were enrolled in our study. Twenty-four-hour urine NE levels were measured by LC-MS-MS. VVS children were diagnosed by BHUTT and/or SNHUTT, and received metoprolol treatment for 3months. Symptom scoring was utilized to evaluate the therapeutic effect. A ROC curve was used to investigate the predictive value of 24-h urine norepinephrine levels. There exists significant correlation between 24-h urine NE levels and supine systolic and diastolic blood pressures. The 24-h urine NE levels of responders (40.75 ± 12.86μg/24h) were higher than those of nonresponders (21.48 ± 6.49μg/24h), and there was a significant difference between the two groups (P < 0.001). A ROC curve of the predictive value of 24h urine NE levels revealed that the area under the curve was 0.926. A cutoff value for 24-h urine NE level of 34.84μg/24h produced both high sensitivity (70%) and specificity (100%) in predicting the efficacy of metoprolol therapy for VVS. Patients with high 24-h urine NE levels have higher supine systolic and diastolic pressures and more effective responses to metoprolol. A 24-h urine norepinephrine level of > 34.84μg/24h was an indicator of the effectiveness of metoprolol therapy for VVS in children.

Search of substances with the cardioprotective activity in the series of derivatives of halogenides 1-alkyl- and carboxyalkyl-4-ylideneamino-1,2,4-triazole

In spite of achievements in the sphere of highly effective drugs creation for treating cardiovascular diseases the problem is still urgent since mortality is high because of these diseases, and it takes the 2-nd – 3-d place among the population of industrially developed countries. In the Research and Production Association “Pharmatron” a new approach concerning creation of new effective anti-anginal drugs has been developed; it is a chemical modification of position 1 and 4 of 1,2,4-triazole molecule by introduction of the structural fragments of the most active medicines and structures imitating sites of adrenergic receptors. Bromides of 1-(alkyl) carboxyalkyl-4-ylideneamino-1,2,4-triazole have been synthesized at the Pharmaceutical Chemistry department of Zaporizhzhia State Medical University under the supervision of professor I.A.Mazur. The cardioprotective activity of 12 compounds – derivatives of 1-carboxyalkyl-4-ylideneamino-1,2,4-triazole bromides and 1-alkyl-4-ylidenamino-1,2,4-triazole bromides has been investigated. The experiments were conducted in 510 white outbred male rats weighing 120-130 g from the mouse bank of the Institute of Pharmacology and Toxicology of the AMS of Ukraine. Determination of acute toxicity of the compounds investigated was conducted according to Kerber method. It has been found that LD50 of these compounds when introduced intraabdominally to rats is within 29.5-295 mg/kg. It allows to refer the compounds under research to the III and IV classes of toxicity (moderate or low toxic). The model of acute myocardial infarction in rats was used for studying the cardioprotective activity of the compounds, the infarction was modeled by staged introduction of isadrin and pituitrin. It has been found that intraabdominal introduction of 8 compounds of 12 ones in the dose of 1/100 LD50 to rats with myocardial infarction leads to decrease of hyperenzymemia of cardiospecific isoenzymes of creatine phosphokinase (MB CPK) and lactate dehydrogenase (LDH-1), which play the role of biochemical markers of the myocardium damage, and decrease of electrophysiological marker ΣΔST during electrocardiography. The structural fragments of the molecule, which play a determinative role in manifestation of the cardioprotective effect of such series as β-phenylethyl, carboxy propyl, octyl in position 1 and the presence of amino- and n-methoxybensilidenamino-groups in position 4, have been revealed. It has been determined that compound MT significantly exceeds the therapeutical efficacy of metoprolol by decrease of MB CPK and LDH-1 activity in the blood serum of rats with myocardial infarction, as well as decrease of ECG ST amplitude.

The clinical efficacy of metoprolol combined with trimetazidine for cardiac failure due to coronary heart disease

Objeective To investigate the clinical efficacy of combination therapy with metoprolol and trimetazidine in the treatment of cardiac failure due to coronary heart disease (CHD).Meyhods 96 patients with cardiac failure due to CHD divided study group and control group,48 for each group.The control group received routine comprehensive treatment,while the study group received metoprolol combined with trimetazidine.The clinical efficacy and improvement in cardiac function were observed in the two groups.Results The total effectiveness rate was significantly higher in the study group than in the control group (95.83％ vs.83.33％,P＜0.05).Six months after treatment,LVEF was significantly greater while LVESD and LVEDD were markedly smaller in the study group than in the control group (P＜0.05 for all comparisons).Conclusions Combination therapy with metoprolol and trimetazidine is efficacious and has a rapid onset of action and a longer-lasting action.It can be used as an ideal therapeutic regimen for cardiac failure due to coronary heart disease. Key words: Metoprolol; Trimetazidine; Coronary heart disease; Cardiac failure

Comparison of the efficacy of metoprolol and nifedipine in the treatment of asymptomatic myocardial ischemia for the elderly

Objective To explore the clinical value of application of metoprolol and nifedipine in the treatment of asymptomatic myocardial ischemia for the elderly.Methods 56 cases of elderly patients with silent myocardial ischemia were chosen.They were randomly divideded into the metoprolol group of 28 cases and nifedipine group with 28 cases according to the number table.The incidence of complications during treatment in the metoprolol and nifedipine group were analyzed.The seizure frequency and onset time in the two groups of patients were compared before and after treatment.Results The onset time in the two groups,before treatment had no statistically significant difference[the number of attacks:(19.6±3.2) times/week compared with(18.9±2.8) times/week;attack time:(5131±352)s vs (5130 ± 348 ) s,all ( P ＞ 0.05 ).After treatment,there were statistically significant differences for the number of attacks and attack time [the number of attacks:(4.6 ± 2.1 ) times/week compared with ( 7.4 ± 2.1 )times/week,onset tine:(900 ± 140) s vs ( 1440 ± 240 ) s ( all P ＜ 0.05 ).All patients can tolerate the treatment period,there was no cases of myocardial infarction occurs.Conclusion The metoprolol and nifedipine for the elderly treatment of silent myocardial ischemia was more secure,and metoprolol was more effective than nifedipine. Key words: Metoprolol; Nifedipine treatment ; Silent myocardial ischemia

Efficacy of metoprolol in treatment and preventive of cardiovascular diseases

Efficacy of metoprolol in treatment and preventive of cardiovascular diseases

RATIONAL CHOICE OF Β-ADRENOBLOCKERS IN CHRONIC HEART FAILURE THERAPY

There were presented results of clinical trials on β-adrenoblockers usage in patients with chronic heart failure (CHF) as well as data of own study on nebivolol efficacy and tolerability in 113 patients with ischemic heart disease, complicated with CHF. It is emphasized that therapy with β-adrenoblockers positively influences on cardiac hemodynamics and CHF symptoms, significantly reduces mortality risk and the frequency of hospitalizations. The usage of β-adrenoblockers is indicated in CHF of any stage. Efficacy of metoprolol, bisoprolol and carvedilol had been proven in CHF therapy. Nebivolol was effective in elderly patients with CHF.

Short-term and long-term hemodynamic and clinical effects of metoprolol alone and combined with amlodipine in patients with chronic heart failure

Background Initiation of β-blocker therapy is often limited by worsening congestive heart failure, which may manifest as worsening hemodynamics. Deleterious hemodynamic effects might be mitigated with the vasodilation of combined calcium channel/β-blocker therapy. Methods and Results This prospective, randomized study assessed the safety and efficacy of metoprolol alone or combined with amlodipine on hemodynamic parameters at baseline, 2 hours after the first dose of study medication, and after 12 weeks of therapy in patients receiving background triple therapy for mild to severe heart failure. Functional, exercise, and hormonal status were assessed at baseline and end of study. Twenty-nine patients (mean age 50 ± 12.1 years) were enrolled; 21 completed 12 weeks of treatment. Mean ejection fraction at baseline was 13.4% ± 5.7%; 79% of patients had heart failure classified as New York Heart Association class III, and 66% had heart failure of idiopathic origin. Heart rate and blood pressure did not change with short-term therapy in either group. The first dose of both regimens produced significant increases in systemic vascular resistance and significant decreases in cardiac output and index and stroke volume and stroke work indexes; combination therapy acutely yielded small but statistically significant increases in pulmonary artery, pulmonary capillary wedge, and right atrial pressures. Long-term therapy with both regimens produced significant decreases in heart rate, systemic vascular resistance, and pulmonary capillary wedge pressure and significant increases in cardiac output and index and stroke volume and stroke work indexes. Combination therapy produced significant long-term decreases in blood pressure. Conclusions There was no further measurable benefit with the addition of amlodipine to metoprolol compared with the effects of metoprolol alone. Therapy with metoprolol alone and the combination of metoprolol and amlodipine was well tolerated in patients with mild to severe heart failure, as evidenced by a lack of adverse effects on hemodynamic parameters over the short term and clinical and hemodynamic improvement with long-term treatment. (Am Heart J 1999;138:261-8.)

No effect of prophylactic treatment with metoprolol on cerebrovascular CO2 reactivity in migraineurs.

The prophylactic effect of metoprolol in the treatment of migraine is well known, but its mode of action is still unclear. In the past, increased CO2 reactivity has been reported as one pathognomic finding in interictal migraineurs. Using transcranial Doppler we assessed CO2 reactivity in 20 migraineurs before and 3 h after the first intake of 50 mg metoprolol, and subsequently twice after 1 and 8 weeks of continuous therapy with 150 mg metoprolol/d. Before initiation of therapy, migraineurs as a group had increased CO2 reactivity (p=0.07) compared to 20 age- and sex-matched volunteers. While treatment with metoprolol has been reported to affect amplitudes of increased contingent negative variation or visual evoked potentials in interictal migraineurs, it had no influence on enhanced CO2 reactivity in the present study. Moreover, the pretreatment value of CO2 reactivity did not correlate with the clinical efficacy of metoprolol after a 2-month treatment period.

The Efficacy of Low Dose Metoprolol CR/ZOK in Mild Hypertension and in Elderly Patients with Mild to Moderate Hypertension

In two separate but similarly designed placebo-controlled studies, the efficacy of metoprolol CR/ZOK 50 mg once daily was evaluated in 64 patients (mean age 53 years) with mild hypertension (Study I) and in 34 elderly patients (mean age 68 years) with mild to moderate hypertension (Study II). Both studies were of randomized, double-blind, parallel-group design, the entry criteria for diastolic blood pressure being greater than or equal to 90 less than 105 mm Hg in Study I and greater than or equal to 95 less than 110 mm Hg in Study II. Study I: The impact of metoprolol CR/ZOK 50 mg once daily for 4 weeks compared with placebo 24 hours post dosing was to produce a significant reduction in supine (P = .0001), and standing (P less than .0001) systolic blood pressures and the standing diastolic pressure (P = .035). The supine diastolic pressure was lower after metoprolol CR/ZOK but not significantly so. Study II: Metoprolol CR/ZOK 50 mg daily given to elderly hypertensives when compared with placebo 24 hours post dosing produced a significant fall in supine (P = .022) and standing (P = .022) diastolic pressure. Systolic pressure and heart rate were not significantly reduced. One patient in Study II had a nonfatal myocardial infarct whilst receiving placebo. There were no other serious adverse effects in either study and no patients were withdrawn from the trial because of drug related unwanted events. The studies indicate that 50 mg metoprolol CR/ZOK may be an effective antihypertensive agent which may prove useful in the treatment of mild to moderate hypertension, particularly in the elderly.

Medikamentöse Migräneprophylaxe

If migraine attacks occur more frequently than 2 times a month, treatment of the acute attack with analgesics and ergotamine becomes problematic. An acute relief of migraine symptoms will be achieved only at the risk of developing a drug-induced chronic headache. Therefore, if migraine attacks occur frequently prophylactic treatment should be considered. A bewildering variety of drugs have been discussed for migraine prophylaxis in the past few decades. Only a few of them can be accepted to be effective on the basis of reliable clinical studies. Others have failed to show any superiority to placebo treatment when tested in controlled drug trials for a period long enough to rule out the placebo response, which may simulate effectiveness at the beginning of the trial. The efficacy of metoprolol and propranolol has been demonstrated beyond any doubt. It seems, however, that other beta-blocking drugs are less effective or even ineffective. In more than 20% of patients even prolonged treatment with metoprolol or propranolol does not provide sufficient relief. Flunarizine may be tried in these patients, as long as side effects do not occur or can be tolerated by the patient. Whether non-steroidal antirheumatics and dihydroergotamine can be considered as an effective and safe alternative in migraine prophylaxis is still not well established. There is, however, convincing evidence that neither clonidine, nor anti-histamines, nor barbiturates, nor antiepileptic drugs, nor anxiolytics are effective in the prophylactic treatment of migraine. Successful prophylactic treatment cannot be achieved by drug therapy alone. Any form of drug treatment should be complemented by providing the patient with detailed information about the nature of the disease and the properties of the prescribed drugs, as well as careful investigation of the patient's situation and habits and a careful search for precipitants, combined with an attempt to change the patient's habits and to avoid factors that trigger the attacks.

Efficacy of Metoprolol in Anxiety Disorders

Efficacy of Metoprolol in Anxiety Disorders

Metoprolol for hypertension Open trial in general practice

The results of an uncontrolled and open study of a once-a-day dosage of metoprolol (Betaloc) in the management of mild to moderate hypertension are described. The study was conducted by a group general practice. The trial was designed to test if metoprolol taken only once a day, could improve patient compliance. This would also result in less expense to the patient. Of the 161 patients who started the trial, 144 patients remained in it. Hypertension was fully controlled in 84 patients, but 33 failed to respond to metoprolol therapy. Because of side effects, 27 abandoned the trial. The remaining 17 patients withdrew from the drug trial for reasons unrelated to metoprolol. The efficacy of metoprolol was not influenced by a person's sex, but the number of side effects was significantly increased in older patients.

An Open Study of the Antihypertensive Efficacy of Metoprolol

An open study of the effectiveness of metoprolol in reducing the blood pressures of 13 hypertensive patients was conducted. It was found that metoprolol reduced the patients' blood pressure satisfactorily, and is well tolerated within the dose range of 100 mg to 400 mg daily.