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Levobunolol | CAS No: 47141-42-4 | GMP-certified suppliers
A medication that lowers intraocular pressure to manage chronic open-angle glaucoma and ocular hypertension, supporting ophthalmic use with consistent quality and safety standards.
Therapeutic categories
Primary indications
- For lowering intraocular pressure (IOP) and may be used in patients with chronic open-angle glaucoma or ocular hypertension
Product Snapshot
- Levobunolol is formulated as an ophthalmic liquid solution for topical administration
- It is primarily indicated for lowering intraocular pressure in conditions such as chronic open-angle glaucoma and ocular hypertension
- Levobunolol holds approved regulatory status in key markets including the United States and Canada
Clinical Overview
Pharmacodynamically, levobunolol acts as an ophthalmic beta-blocker exhibiting similar affinity for both β1- and β2-adrenergic receptors. It effectively lowers elevated IOP and can also reduce normal IOP levels. In clinical settings, levobunolol reduces mean IOP by approximately 25-40% from baseline in patients with elevated pressure. Due to its nonselective beta-blocking activity, topical ocular administration may lead to systemic effects including bronchoconstriction, increased airway resistance, decreased blood pressure, and bradycardia.
The precise mechanism by which levobunolol decreases IOP has not been fully elucidated; however, it is generally attributed to inhibition of endogenous catecholamine-induced increases in cyclic adenosine monophosphate (cAMP) within the ciliary body processes. This reduction in cAMP results in decreased aqueous humor production and subsequent lowering of IOP.
Key ADME parameters for levobunolol are not extensively characterized in the literature, though it is recognized as a substrate of cytochrome P450 enzymes including CYP2D6, which may influence its metabolism. Systemic absorption following ophthalmic administration warrants consideration particularly in patients with respiratory or cardiovascular comorbidities.
Safety considerations involve monitoring for pulmonary adverse effects such as bronchospasm, especially in patients with pre-existing reactive airway disease, and cardiovascular effects including bradycardia and hypotension. Due to these risks, levobunolol use requires caution, and contraindications include asthma and severe chronic obstructive pulmonary disease.
Levobunolol is marketed under various ophthalmic formulations globally and is utilized predominantly in glaucoma management protocols.
For API sourcing, stringent quality controls are essential to ensure purity, consistent potency, and compliance with pharmacopeial standards. Given its classification as a cytochrome P450 substrate and potential for systemic effects, impurities or variability could impact clinical safety. Procurement should prioritize manufacturers with validated synthesis processes, robust analytical characterization, and adherence to Good Manufacturing Practice (GMP) requirements.
Identification & chemistry
| Generic name | Levobunolol |
|---|---|
| Molecule type | Small molecule |
| CAS | 47141-42-4 |
| UNII | G6317AOI7K |
| DrugBank ID | DB01210 |
Pharmacology
| Summary | Levobunolol is a nonselective beta-adrenergic antagonist targeting both β1- and β2-receptors in ocular tissues. It reduces intraocular pressure primarily by inhibiting catecholamine-induced cyclic AMP production in ciliary processes, thereby decreasing aqueous humor formation. Its pharmacodynamic effects include lowering elevated and normal IOP, with potential systemic cardiovascular and pulmonary impacts following ocular administration. |
|---|---|
| Mechanism of action | Levobunolol's mechanism of action in reducing IOP is not clearly defined, but is believed to be due to a reduction of the production of aqueous humor via blockage of endogenous catecholamine-stimulated increases in cyclic adenosine monophosphate (AMP) concentrations within the ciliary processes. |
| Pharmacodynamics | Levobunolol is an ophthalmic beta-blocker, equally effective at β(1)- and β(2)-receptor sites. Levobunolol reduces both elevated and normal IOP in patients with or without glaucoma. In patients with elevated IOP, levobunolol reduces mean IOP by approximately 25-40% from baseline. As the drug is a nonselective &beta-adrenergic blocking agent, it can produce both systemic pulmonary and cardiovascular effects following topical application to the eye. These effects include adverse pulmonary effects (eg. bronchoconstriction, increased airway resistance), and a decrease in blood pressure and heart rate. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-1 adrenergic receptor | Humans | antagonist |
| Beta-2 adrenergic receptor | Humans | antagonist |
ADME / PK
| Absorption | 80% |
|---|---|
| Half-life | 20 hours |
| Metabolism | Hepatic |
Formulation & handling
- Levobunolol is formulated exclusively for ophthalmic use, typically as aqueous solutions or drops.
- As a small molecule with moderate lipophilicity (LogP 2.18) and low water solubility, solubilization strategies may be required for stable ophthalmic formulations.
- Stable handling recommendations should consider protection from light and controlled storage conditions to maintain solution integrity.
Regulatory status
| Lifecycle | The API is currently marketed in both Canada and the US, with key patent protections having expired or approaching expiry, indicating a transition into the mature phase of its product lifecycle in these regions. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Levobunolol is manufactured and supplied by multiple companies including both originators and generic manufacturers, reflecting a competitive supply landscape. Branded products such as Betagan have established presence primarily in North American markets, including the US and Canada. The availability of generics like Apo-levobunolol suggests that patent protection has expired or is near expiration, allowing for generic competition. |
|---|
Safety
| Toxicity | Bradycardia, hypotension, bronchospasm, and acute cardiac failure, LD<sub>50</sub>=700 mg/kg (orally in rat). |
|---|
- Potential for bradycardia, hypotension, bronchospasm, and acute cardiac failure upon exposure
- Oral LD50 in rat model is 700 mg/kg, indicating moderate acute toxicity
- Handle with appropriate personal protective equipment to prevent systemic absorption
Levobunolol 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.
Levobunolol (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.
Levobunolol API manufacturers & distributors
Compare qualified Levobunolol API suppliers worldwide. We currently have 3 companies offering Levobunolol API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Medichem | Producer | Spain | Unknown | CoA, USDMF | 39 products |
| Piramal Healthcare | Producer | United Kingdom | India | CoA, GMP, WC | 31 products |
| Piramal Pharma Solutions | Producer | India | India | CoA, USDMF, WC | 44 products |
When sending a request, specify which Levobunolol 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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