*For medical professionals only
This article fully teaches you the difference
Beta-blockers are commonly used drugs in cardiology and are widely used in hypertension, coronary heart disease, arrhythmia, chronic heart failure, etc.
Metoprolol and bisoprolol are the most commonly used members of the “lool” family. Metoprolol tartrate and metoprolol succinate, the two seem to be similar, only the “prefix” is different?
Metoprolol and bisoprolol are both highly selective beta1 receptor blockers. What is the difference between them? Let’s take a look with Jie Xiaoyao!
Metoprolol tartrate vs
Metoprolol succinate,
How to tell the difference?
There are currently two types of metoprolol in clinical use, Metoprolol tartrate and Metoprolol succinate, Both have similar medicinal effects. But the time of action and the way of action are different.
1
Different dosage forms
Metoprolol tartrate has a high solubility in water at 37°C, making it difficult to prepare film-forming controlled-release pellets, which are ordinary tablets, and are also called “flat tablets” by doctors;
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The solubility of metoprolol succinate is significantly lower than that of metoprolol tartrate, and it can be prepared into film-controlled sustained-release pellets, which are sustained-release tablets.
2
Different processes in the body
Metoprolol tartrate tablets will be rapidly absorbed after taking, reaching the peak blood concentration, and the half-life is about 3-5h.
After taking metoprolol succinate sustained-release tablets, it is released at an almost constant rate for about 20 hours, and the effect lasts for more than 24 hours. , the absorption is stable.
3
Frequency and doses vary[1]
Metoprolol tartrate tablets: should be taken on an empty stomach. The treatment of hypertension is 100-200 mg per day, divided into 1 to 2 times.
Metoprolol succinate extended-release tablets: once a day, preferably in the morning, the treatment of hypertension is 47.5-95mg, patients who fail to take 95mg can be combined with other antihypertensive drugs, or Increase the dose. Break apart, but not chew or crush.
4
Food Impact
Metoprolol tartrate when taken with food will increase the absorption rate by 40% and increase adverse reactions, so it should be taken on an empty stomach.
Metoprolol succinate extended-release tablets are not affected by diet, and can be taken before or after meals. It is worth noting that at least half a glass of liquid should be taken when taking this medicine.
Table 1 Differences between metoprolol tartrate and metoprolol succinate[2]
Metoprolol vs Bisoprolol,
How do I choose?
Non-selective beta-blockers can block both beta1 and beta2 receptors, which can easily cause bronchospasm[1], and both metoprolol and bisoprolol are highly selective Sex β1 receptor blockers, we look at the similarities and differences between the two from the following points.
1
Comparison of pharmacological characteristics and pharmacokinetics
■Receptor selectivity
Bisoprolol and metoprolol are β1-receptor blockers and have little effect on β2 receptors, but, compared with metoprolol, bisoprolol is more selective for β1 receptors Sex is higher, about 2 times higher than that of metoprolol [3].
■Solubility
Bisoprolol is water-lipid dual-soluble, which has the advantages of low first-pass effect of water-soluble beta-blockers and high oral absorption rate of fat-soluble beta-blockers. Advantage. Metoprolol is only fat-soluble and can easily enter the central nervous system through the blood-brain barrier.
■Bioavailability
Metoprolol has a greater first-pass elimination effect, with a bioavailability of 40%-50%, while the bioavailability of bisoprolol is about 90%.
■Speed of action
Metoprolol tartrate tablets work faster and work more quickly if neededTo slow down your heart rate, you can choose metoprolol tartrate.
■Half-life and duration
Bisoprolol has a half-life of 10-12h, and its efficacy can last for 24h. Metoprolol tartrate has a short half-life of 3-5h and a short duration of efficacy, while metoprolol succinate has a short half-life of 3-5h. The drug effect of Lorol sustained-release tablets lasted for more than 24 hours.
■Metabolic pathways
Metoprolol is mainly eliminated by the liver, and bisoprolol is eliminated by both liver and kidney channels in the same proportion.
■Drug interactions
Metoprolol is mainly metabolized by the liver enzyme CYP2D6. Drugs that inhibit CYP2D6 enzyme such as paroxetine, fluoxetine, sertraline, celecoxib, diphenhydramine, propafenone Ketones etc.
If the patient is taking these drugs in combination, the dose of metoprolol should be appropriately reduced to avoid bradycardia. Bisoprolol has little effect on liver drug-enzyme-mediated drug interactions.
■Gene polymorphism[4]
Gene polymorphisms have less effect than Soprolol. Metoprolol is metabolized by the liver enzyme CYP2D6. The mutation rate of this enzyme in the human body is relatively high. Therefore, individuals with Metoprolol big different.
2
Clinical application
■Lower blood pressure and control heart rate
A study on Chinese patients with mild to moderate hypertension showed [5]: the antihypertensive efficacy of bisoprolol fumarate and metoprolol extended-release tablets were comparable; Bisoprolol once a day is more effective for sustained heart rate control than troporol extended-release tablets.
■Anti-Heart Failure
Metoprolol and bisoprolol both improve cardiac function and are prognostic. Classical large clinical trials for HFrEF patients (MERIT-HF, CIBIS II, US Carvedilol HF Study, COPERNICUS) have confirmed this.
Beta-blockers (metoprolol, bisoprolol) reduce the risk of all-cause death by 34%-65% and sudden death by 41%-44 compared to placebo %, reduce the risk of cardiovascular death or hospitalization by 27%-38%, and improve the patient’s cardiac function classification and quality of life [6].
■Medication for special patients
Metoprolol: In patients with renal impairment, no dose adjustment is required; in patients with hepatic impairment, the dose of metoprolol usually used in patients with cirrhosis is related to liver function Normal is the same. Dose reduction should only be considered in very severely impaired liver function (eg, patients undergoing bypass surgery).
Bisoprolol: Patients with mild to moderate hepatic or renal insufficiency usually do not require dose adjustment. For patients with severe renal failure (creatinine clearance <20ml/min) and severe liver dysfunction, the daily dose should not exceed 10mg.
3
Adverse reactions
■Effects on the central nervous system
Drugs with high lipid solubility can easily pass through the blood-brain barrier and cause corresponding adverse reactions. Metoprolol is moderately fat-soluble, so it can cause adverse reactions such as headache and dizziness.
Bisoprolol is difficult to penetrate the blood-brain barrier, so there are fewer central nervous symptoms. If you have adverse reactions such as headache and dizziness after taking metoprolol, you can switch to bisoprolol.
■Effects on respiratory system
Bisoprolol is more selective for beta1 receptors and has less effect on the respiratory system than metoprolol. Studies have shown that bisoprolol can significantly increase the forced expiratory volume in one second and improve lung function [7].
Finally special reminder: β-blockers should be slowly reduced, and the drug must be stopped slowly, not suddenly, otherwise it may cause heart failure. Worsening failure and increased risk of sudden myocardial infarction.
What other drug comparisons would you like to see? Welcome to leave a message in the comment area~
References:
[1] Feng Yingqing, Li Yong, Zhang Yuqing, et al. Expert consensus on the application of beta-blockers in hypertension [J]. Chinese Journal of Medical Frontiers: Electronic Edition, 2013 ( 4):9.
[2] Tong Rongsheng, Liu Yuejian, Yang Yong. Drug comparison and clinical rational selection [M]. People’s Health Publishing House, 2013.
[3]Smith C,Teitler M.Beta-Blocker Selectivity at Cloned Human Beta1-and Beta2-Adrenergic Receptors[J].Cardiovascular Drugs&Therapy,1999,13(2):123-126 .
[4]Grandsonloyal. Pharmacogenomics and rational application of β-blockers[J]. Chinese Journal of Hypertension, 2011, 19(5): 409-412.
[5]Zhou,Shuxian,Ma,et al.Comparison of bisoprolol to a metoprolol CR/ZOK tablet for control of heart rate and blood pressure in mild-to-moderate hypertensive patients:the CREATIVE study[J].Hypertension Research Official Journal of the Japanese Society of Hypertension,2017.
[6] Guidelines for Rational Drug Use in Heart Failure (2nd Edition). National Health and Family Planning Commission Rational Drug Use Expert Committee, Chinese Pharmacists Association.
[7]BMLA,CMP,DDK,et al.Differences between bisoprolol and carvedilol in patients with chronic heart failure and chronic obstructive pulmonary disease: a randomized trial[J].Respir Med,2011 ,105(1):S44-S49.
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