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Metoprolol | CAS No: 51384-51-1 | GMP-certified suppliers
A medication that treats cardiovascular diseases by managing angina, heart failure, myocardial infarction, arrhythmias, and hypertension to reduce morbidity and mortality.
Therapeutic categories
Primary indications
- Metoprolol is indicated for the treatment of angina, heart failure, myocardial infarction, atrial fibrillation, atrial flutter and hypertension
- Some off-label uses of metoprolol include supraventricular tachycardia and thyroid storm
Product Snapshot
- Metoprolol is available primarily as oral tablets and capsules in immediate and extended-release formulations, as well as intravenous injection
- It is indicated for cardiovascular conditions including angina, heart failure, myocardial infarction, atrial fibrillation, atrial flutter, and hypertension
- Metoprolol is approved for use in major regulatory markets including the United States and Canada
Clinical Overview
Pharmacologically, metoprolol exerts a negative chronotropic and inotropic effect by selectively inhibiting beta-1 adrenergic receptors predominantly located in cardiac tissue. This selective receptor blockade results in decreased heart rate, reduced myocardial contractility, and attenuation of myocardial oxygen demand. The compound does not exert significant beta-2 receptor activity, minimizing pulmonary side effects typical of non-selective beta blockers. In arrhythmia management, metoprolol reduces pacemaker potential slope and slows atrioventricular conduction.
Key findings from clinical trials—including the Metoprolol Atherosclerosis Prevention in Hypertensives (MAPHY) trial—demonstrate a reduction in sudden cardiac death and myocardial infarction when metoprolol is administered compared to alternative treatments such as diuretics. Chronic administration post-myocardial infarction has been associated with a 17% reduction in mortality and reinfarction rates.
Metoprolol is available predominantly as succinate and tartrate salts, with succinate favored in extended-release formulations due to its lower systemic bioavailability relative to the tartrate derivative, which is typically formulated for immediate release. The compound undergoes hepatic metabolism primarily via cytochrome P450 CYP2D6, with renal excretion representing a notable elimination pathway.
Safety considerations include monitoring for bradycardia, hypotension, and exacerbation of heart failure symptoms. Metoprolol’s profile as a moderate CYP2D6 inhibitor warrants caution when co-administered with substrates of this enzyme. Photosensitivity reactions and potential for hyperkalemia are also reported.
From an API sourcing perspective, the quality of metoprolol is critical in ensuring consistent release profiles, particularly given the formulation-dependent differences between succinate and tartrate salts. Compliance with pharmacopeial standards and thorough impurity profiling are essential, particularly monitoring for residual solvents and related substances. Reliable supply chains and validated analytical methods support regulatory submissions and maintain therapeutic consistency across global markets.
Identification & chemistry
| Generic name | Metoprolol |
|---|---|
| Molecule type | Small molecule |
| CAS | 51384-51-1 |
| UNII | GEB06NHM23 |
| DrugBank ID | DB00264 |
Pharmacology
| Summary | Metoprolol is a selective beta-1 adrenergic receptor antagonist targeting cardiac cells, resulting in decreased heart rate, myocardial contractility, and oxygen demand. Its pharmacodynamic effects include negative chronotropic and inotropic actions, which reduce cardiac output and suppress arrhythmic activity by modulating pacemaker potential and atrioventricular conduction. Metoprolol is primarily used in cardiovascular conditions such as angina, heart failure, myocardial infarction, and arrhythmias. |
|---|---|
| Mechanism of action | Metoprolol is a beta-1-adrenergic receptor inhibitor specific to cardiac cells with negligible effect on beta-2 receptors. This inhibition decreases cardiac output by producing negative chronotropic and inotropic effects without presenting activity towards membrane stabilization nor intrinsic sympathomimetics. |
| Pharmacodynamics | Administration of metoprolol in normal subjects is widely reported to produce a dose-dependent reduction on heart rate and cardiac output. This effect is generated due to a decreased cardiac excitability, cardiac output, and myocardial oxygen demand. In the case of arrhythmias, metoprolol produces its effect by reducing the slope of the pacemaker potential as well as suppressing the rate of atrioventricular conduction. The Metoprolol Atherosclerosis Prevention in Hypertensives (MAPHY) trial showed a significant improvement in sudden cardiac death and myocardial infarction when patients were given with metoprolol as compared with diuretics. As well, in clinical trials performed in 1990, metoprolol reduces mortality and re-infarction in 17% of the individuals when administered chronically after an episode of myocardial infarction. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-1 adrenergic receptor | Humans | antagonist |
| Beta-2 adrenergic receptor | Humans | antagonist |
| Beta adrenergic receptor | Humans | inhibitor |
ADME / PK
| Absorption | When metoprolol is administered orally, it is almost completely absorbed in the gastrointestinal tract. The maximum serum concentration is achieved 20 min after intravenous administration and 1-2 hours after oral administration. The bioavailability of metoprolol is of 100% when administered intravenously and when administered orally it presents about 50% for the tartrate derivative and 40% for the succinate derivative. The absorption of metoprolol in the form of the tartrate derivative is increased by the concomitant administration of food. |
|---|---|
| Half-life | The immediate release formulations of metoprolol present a half-life of about 3-7 hours. |
| Protein binding | Metoprolol is not highly bound to plasma proteins and only about 11% of the administered dose is found bound. It is mainly bound to serum albumin. |
| Metabolism | Metoprolol goes through significant first-pass hepatic metabolism which covers around 50% of the administered dose. The metabolism of metoprolol is mainly driven by the activity of CYP2D6 and to a lesser extent due to the activity of CYP3A4. The metabolism of metoprolol is mainly represented by reactions of hydroxylation and O-demethylation. |
| Route of elimination | Metoprolol is mainly excreted via the kidneys. From the eliminated dose, less than 5% is recovered unchanged. |
| Volume of distribution | The reported volume of distribution of metoprolol is 4.2 L/kg. Due to the characteristics of metoprolol, this molecule is able to cross the blood-brain barrier and even 78% of the administered drug can be found in cerebrospinal fluid. |
| Clearance | The reported clearance rate on patients with normal kidney function is 0.8 L/min. In cirrhotic patients, the clearance rate changes to 0.61 L/min. |
Formulation & handling
- Metoprolol is a small molecule drug available in oral and intravenous formulations with extended and delayed release oral dosage forms.
- Due to moderate water solubility and LogP of 1.76, formulations should consider solubility enhancement for consistent bioavailability.
- Avoid concomitant administration with alcohol and natural licorice, and oral doses should be taken with food to minimize gastrointestinal side effects.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is protected by patents in the United States until July 9, 2035, indicating market exclusivity in both the US and Canada during this period. Following patent expiry, the product is expected to enter a mature market phase with potential for generic competition. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Metoprolol is manufactured by a diverse range of originator and generic companies with global manufacturing and packaging capabilities, including major firms such as Novartis, AstraZeneca, Sandoz, and Teva. Branded metoprolol products are primarily marketed in North America, including the US and Canada. Existing patents with expiry dates in 2035 indicate that generic competition is currently limited, with patent protection extending into the mid-2030s. |
|---|
Safety
| Toxicity | Oral administration of metoprolol to rats presents an LD50 in the range of 3090 to 4670 mg/kg. Cases of overdose have reported bradycardia, hypotension, bronchospasm, and cardiac failure. In the case of an overdose, gastric lavage is recommended followed by specific treatment according to symptoms. Metoprolol is not reported to be carcinogenic nor mutagenic nor to impair fertility. The only event registered is the increase of macrophages in pulmonary alveoli and slight biliary hyperplasia. When metoprolol was given for long periods of time on the highest dose, there was evidence of small benign lung tumors. |
|---|
- Metoprolol demonstrates an oral LD50 in rats between 3090 and 4670 mg/kg, indicating moderate acute toxicity
- Overdose symptoms observed include bradycardia, hypotension, bronchospasm, and cardiac failure
- Stringent handling to prevent exposure is advised
Metoprolol is a type of Beta blockers
Beta blockers are a subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the medical field. These medications work by blocking the effects of adrenaline and other stress hormones on the beta receptors in the body. This action helps to reduce the heart rate and blood pressure, making them effective in treating various cardiovascular conditions.
Beta blockers are commonly prescribed to manage conditions such as hypertension (high blood pressure), angina (chest pain), arrhythmias (irregular heart rhythms), and certain types of heart failure. They can also be used in the prevention of migraines and to alleviate symptoms associated with anxiety disorders.
By targeting the beta receptors, these APIs provide a significant impact on the sympathetic nervous system, reducing the fight-or-flight response and promoting a state of calmness. This mechanism of action allows beta blockers to be effective in controlling heart-related conditions.
Some well-known beta blockers include metoprolol, propranolol, atenolol, and carvedilol. These APIs are available in various forms such as tablets, capsules, and injectables, allowing for flexibility in administration and dosage.
It is important to note that the use of beta blockers should be done under medical supervision due to potential side effects and contraindications. Common side effects may include fatigue, dizziness, cold hands and feet, and sexual dysfunction. Patients with certain conditions like asthma or diabetes may require cautious monitoring while using beta blockers.
In conclusion, beta blockers are a vital subcategory of pharmaceutical APIs used to treat cardiovascular conditions by blocking the effects of stress hormones. Their effectiveness and versatility make them a valuable tool in managing various medical conditions, enhancing the well-being of patients.
Metoprolol (Beta blockers), classified under Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Metoprolol API manufacturers & distributors
Compare qualified Metoprolol API suppliers worldwide. We currently have 23 companies offering Metoprolol API, with manufacturing taking place in 8 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Aarambh Life Science | Producer | India | India | CoA, GMP | 19 products |
| AXXO GmbH | Distributor | Germany | World | CEP, CoA, EDMF/ASMF, GMP, GDP, MSDS, USDMF | 243 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CEP, CoA, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| HEC Pharm | Producer | Germany | China | CEP, CoA, FDA, GMP, USDMF | 31 products |
| Ipca Labs. | Producer | India | Unknown | CEP, CoA, FDA, GMP, JDMF, USDMF, WC | 69 products |
| Iwaki Seiyaku | Producer | Japan | Japan | CoA, JDMF | 21 products |
| Medichem | Producer | Spain | Unknown | CoA, USDMF | 39 products |
| Moehs | Producer | Spain | Spain | CEP, CoA, EDMF/ASMF, GMP, JDMF, USDMF | 50 products |
| Prachi Pharmaceuticals | Producer | India | India | CoA, FDA, GMP, ISO9001, USDMF, WHO-GMP | 12 products |
| S.I.M.S. | Producer | Italy | Italy | CEP, CoA, FDA, GMP, USDMF | 18 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, MSDS, USDMF, WC | 762 products |
| Sun Pharma | Producer | India | India | CEP, CoA, USDMF, WC | 219 products |
| Syn-tech Chem | Producer | Taiwan | Taiwan | CoA, USDMF | 22 products |
| Unichem Labs. | Producer | India | India | CoA, USDMF | 62 products |
| Watson Pharma | Producer | India | India | CEP, CoA, FDA, GMP, WC | 5 products |
| Xellia (Taizhou) | Producer | China | China | CoA, WC | 8 products |
| Yung Zip Chemical | Producer | Taiwan | Taiwan | CoA, USDMF | 12 products |
| Zhejiang Apeloa Tospo-Jia... | Producer | China | China | CEP, CoA, FDA, USDMF, WC | 15 products |
| Zhejiang Hisoar | Producer | China | China | CEP, CoA, FDA, GMP, USDMF | 10 products |
| Zhejiang Huahai Zhicheng | Producer | China | China | CEP, CoA | 1 products |
| Zhejiang Yongtai Pharma | Producer | China | China | CoA, USDMF | 5 products |
When sending a request, specify which Metoprolol API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Metoprolol API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
