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Nadolol | CAS No: 42200-33-9 | GMP-certified suppliers
A medication that treats angina pectoris and hypertension by providing consistent beta-blockade to reduce cardiac workload and manage blood pressure effectively.
Therapeutic categories
Primary indications
- Nadolol is indicated to treat angina pectoris and hypertension
- Another product formulated with [bendroflumethiazide] is indicated to treat hypertension
Product Snapshot
- Nadolol is available as oral tablets, including standard and delayed-release formulations
- It is primarily used for the treatment of angina pectoris and hypertension
- Nadolol products have regulatory approval in the US and Canadian markets
Clinical Overview
Pharmacodynamically, nadolol exerts its antihypertensive and antianginal effects primarily through nonselective blockade of beta-1 and beta-2 adrenergic receptors. By antagonizing beta-1 receptors in the myocardium, nadolol reduces cyclic AMP signaling, resulting in decreased cardiac contractility, heart rate, conduction velocity, and oxygen demand. Blockade of beta-2 receptors in vascular smooth muscle inhibits vasodilation, thereby increasing peripheral vascular resistance which moderates the risk of hypotension. Inhibition of beta-1 receptors in the juxtaglomerular apparatus reduces renin release, leading to downstream reduction of angiotensin II-mediated vasoconstriction and aldosterone-driven sodium and water retention. Additionally, beta-2 antagonism in the liver, skeletal muscle, lungs, and pancreas contributes to reduced glycogenolysis, limited bronchodilation, and decreased insulin secretion, which may adversely affect insulin sensitivity.
Nadolol does not interact significantly with beta-3 adrenergic receptors. It has a long half-life permitting once-daily dosing over a wide therapeutic range, typically initiated at 40 mg daily and titrated up to 240 mg as clinically indicated. Abrupt withdrawal is contraindicated due to risk of exacerbation of ischemic heart disease symptoms.
The compound undergoes minimal hepatic metabolism, with predominant renal excretion of the unchanged drug. It is a substrate for cytochrome P450 CYP2D6 enzymes and transporter proteins including P-glycoprotein and multidrug and toxin extrusion (MATE) transporters.
Safety considerations include the potential for bradycardia, bronchospasm especially in patients with reactive airway disease, and alterations in glucose metabolism. Nadolol is also classified among agents causing hyperkalemia and inadvertent photosensitivity reactions. Combination formulations with bendroflumethiazide extend its indication for hypertension management.
For API procurement, quality evaluation should confirm chemical identity, assay purity, and compliance with pharmacopoeial standards. Given nadolol’s primary renal elimination and potential for drug interactions via CYP2D6 and efflux transporters, sourcing from reliable manufacturers with validated control of impurities and batch-to-batch consistency is critical to ensure therapeutic safety and efficacy.
Identification & chemistry
| Generic name | Nadolol |
|---|---|
| Molecule type | Small molecule |
| CAS | 42200-33-9 |
| UNII | FEN504330V |
| DrugBank ID | DB01203 |
Pharmacology
| Summary | Nadolol is a nonselective beta-1 and beta-2 adrenergic receptor antagonist that reduces myocardial contractility, heart rate, and conduction velocity, thereby decreasing cardiac workload. It also inhibits renin release from the kidneys and modulates vascular smooth muscle tone, resulting in lowered blood pressure. Additionally, nadolol impacts glycogenolysis, bronchodilation, and insulin secretion due to beta-2 receptor blockade in peripheral tissues. |
|---|---|
| Mechanism of action | Although nadolol is described as a non selective beta blocker, it does not interact with beta 3 adrenal receptors. Antagonism of beta-1 and beta-2 adrenoceptors in the heart inhibits cyclic AMP and its signalling pathway, decreasing the strength and speed of contractions as well as the speed of relaxation and conduction. Antagonism of beta-2 adrenoceptors in the smooth muscle cells of the vasculature inhibits their relaxation, leading to an increase in peripheral vascular resistance and reducing the risk of severe hypotension. The increase in peripheral vascular resistance may contribute to the decrease in insulin sensitivity associated with nadolol use. Antagonism of beta-1 adrenoceptors in the juxtaglomerular apparatus of the kidney inhibits the release of renin, and therefore angiotensin II mediated vasoconstriction, aldosterone mediated water retention, and the release of epinephrine. Antagonism of beta-2 adrenoceptors in the liver and skeletal muscle inhibits glycogenolysis, in the lungs prevents bronchodilation, and in the pancrease inhibits insulin release. |
| Pharmacodynamics | Nadolol is a nonselective beta adrenal receptor blocker that is used to lower blood pressure. It has a long duration of action as it is usually taken once daily and a wide therapeutic index as patients start at doses of 40mg daily but may be increased to doses as high as 240mg daily. Patients taking nadolol should not aburptly stop taking it as this may lead to exacerbation of ischemic heart disease. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-1 adrenergic receptor | Humans | antagonist |
| Beta-2 adrenergic receptor | Humans | antagonist |
ADME / PK
| Absorption | Oral doses of nadolol are approximately 30% absorbed. In healthy subjects, nadolol has a T<sub>max</sub> of 2.7h with a C<sub>max</sub> or 69±15ng/mL following a 60mg oral dose and 132±27ng/mL after a 120mg oral dose. The AUC following a 60mg oral dose was 1021ng\*h/mL and following a 120mg oral dose was 1913±382ng\*h/mL. |
|---|---|
| Half-life | The half life of nadolol is 20 to 24 hours. |
| Protein binding | Nadolol is approximately 30% bound to plasma protein. Nadolol binds to alpha-1-acid glycoprotein in plasma. |
| Metabolism | Nadolol is not metabolized by the liver in humans. |
| Route of elimination | Nadolol is not metabolized in the liver and excreted mainly in the urine. In healthy subjects, following intravenous dosing, 60% of a dose is eliminated in the urine and 15% in the feces after 72 hours. The remainder of the dose is expected to be eliminated in the feces afterwards. |
| Volume of distribution | In healthy subjects, the volume of distribution of nadolol is 147-157L. |
| Clearance | In healthy subjects, the total body clearance of nadolol is 219-250mL/min and the renal clearance is 131-150mL/min. |
Formulation & handling
- Nadolol is a small molecule API intended for oral administration in tablet form with multiple dosage strengths available.
- The compound exhibits moderate water solubility and low lipophilicity (LogP 0.87), supporting oral bioavailability without significant food effect.
- Formulation should consider stability in solid state and the absence of peptide or biologic sensitivities, with handling focused on standard solid API precautions.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient’s patent protection has expired in both Canada and the US, resulting in established generic competition and a mature market environment. Product availability is stable across these regions with ongoing manufacturing and distribution. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Nadolol is manufactured by multiple originator and generic companies, reflecting a diverse supply base. Its branded products have a significant presence primarily in the US and Canada markets. Patent expiration has allowed for extensive generic competition, as indicated by the numerous generic packagers operating in these regions. |
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Safety
| Toxicity | The oral LD<sub>50</sub> in mice is 4500mg/kg. Patients experiencing an overdose may present with bradycardia, cardiac failure, hypotension, and bronchospasm. An overdose may be treated with atropine for bradycardia, digitalis and diuretics for cardiac failure, vasopressors for hypotension, and beta-2 stimulants for bronchospasms, as well as gastric lavage and hemodialysis. |
|---|
- Oral LD50 in mice is 4500 mg/kg, indicating low acute toxicity
- Overdose potential includes bradycardia, cardiac failure, hypotension, and bronchospasm
- Handle with appropriate controls to prevent exposure
Nadolol 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.
Nadolol (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.
Nadolol API manufacturers & distributors
Compare qualified Nadolol API suppliers worldwide. We currently have 5 companies offering Nadolol API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Biophore India | Producer | India | India | CEP, CoA, GMP, USDMF | 46 products |
| Fermion | Producer | Finland | Finland | Other, BSE/TSE, CoA, GDP, GMP, Other, MSDS, USDMF | 29 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Mylan | Producer | India | India | CEP, CoA, WC | 201 products |
| Signa | Producer | Mexico | Mexico | CoA, USDMF | 42 products |
When sending a request, specify which Nadolol 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.).
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