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Timolol | CAS No: 26839-75-8 | GMP-certified suppliers
A medication that treats increased intraocular pressure in ocular hypertension and glaucoma, manages hypertension, and aids in migraine prevention through nonselective beta-adrenergic antagonism.
Therapeutic categories
Primary indications
- Ophthalmic timolol is indicated for the treatment of increased intraocular pressure in patients with ocular hypertension or open-angle glaucoma
- The oral form of this drug is used to treat high blood pressure
- In certain cases, timolol is used in the prevention of migraine headaches
Product Snapshot
- Timolol is available in multiple formulations including ophthalmic solutions and oral tablets
- It is primarily used for managing increased intraocular pressure in ocular hypertension and open-angle glaucoma, with oral forms indicated for hypertension and migraine prevention
- The product is approved for use in key regulatory markets including the US, EU, and Canada
Clinical Overview
Pharmacodynamically, ophthalmic administration of timolol leads to a rapid onset of intraocular pressure reduction, typically within 20 minutes, with effects lasting up to 24 hours at commonly used concentrations (0.25% or 0.5%). Oral timolol decreases blood pressure by reducing heart rate, cardiac output, and sympathetic nervous system activity. It has been shown to lower systolic and diastolic blood pressure and to diminish reflex orthostatic hypotension.
The mechanism of action involves competitive antagonism of beta(1)-adrenergic receptors in cardiac tissue and beta(2)-adrenergic receptors in vascular and bronchial smooth muscle. Beta(1) blockade leads to decreased heart rate and cardiac output, while beta(2) blockade reduces peripheral vascular resistance. The precise mechanism by which timolol reduces intraocular pressure is not fully elucidated but is hypothesized to involve decreased aqueous humor secretion potentially through reduced blood flow to the ciliary body and interference with active transport or prostaglandin biosynthesis.
Key pharmacokinetic considerations reflect its status as a substrate for cytochrome P450 enzymes CYP2C19 and CYP2D6. Timolol is primarily eliminated via renal excretion. Safety considerations include potential bradycardia and bronchospasm due to nonselective beta-blockade, caution in patients with respiratory conditions such as asthma or chronic obstructive pulmonary disease, and monitoring for hypotension during systemic therapy.
Timolol is included in multiple drug categories such as beta-blockers, antiarrhythmic agents, and ophthalmological preparations. Several manufacturers worldwide supply timolol, requiring rigorous quality control to ensure consistent potency, sterility for ophthalmic solutions, and compliance with regulatory standards for both systemic and topical formulations. Sourcing of timolol API should prioritize validated synthetic routes, impurity profiling, and adherence to pharmacopeial monographs to support global registration and patient safety.
Identification & chemistry
| Generic name | Timolol |
|---|---|
| Molecule type | Small molecule |
| CAS | 26839-75-8 |
| UNII | 5JKY92S7BR |
| DrugBank ID | DB00373 |
Pharmacology
| Summary | Timolol is a non-selective beta-adrenergic receptor antagonist targeting beta-1 receptors in cardiac tissue and beta-2 receptors in vascular and bronchial smooth muscle. It decreases heart rate, cardiac output, and peripheral vascular resistance, leading to reduced blood pressure. In ophthalmic applications, timolol lowers intraocular pressure primarily by reducing aqueous humor production, though the precise mechanism remains unclear. |
|---|---|
| Mechanism of action | Timolol competes with adrenergic neurotransmitters for binding to beta(1)-adrenergic receptors in the heart and the beta(2)-receptors in the vascular and bronchial smooth muscle. This leads to diminished actions of catecholamines, which normally bind to adrenergic receptors and exert sympathetic effects leading to an increase in blood pressure and heart rate. Beta(1)-receptor blockade by timolol leads to a decrease in both heart rate and cardiac output during rest and exercise, and a decrease in both systolic and diastolic blood pressure. In addition to this, a reduction in reflex orthostatic hypotension may also occur. The blockade of beta(2) receptors by timolol in the blood vessels leads to a decrease in peripheral vascular resistance, reducing blood pressure. The exact mechanism by which timolol reduces ocular pressure is unknown at this time, however, it likely decreases the secretion of aqueous humor in the eye. According to one study, the reduction of aqueous humor secretion may occur through the decreased blood supply to the ciliary body resulting from interference with the active transport system or interference with prostaglandin biosynthesis. |
| Pharmacodynamics | Timolol, when administered by the ophthalmic route, rapidly reduces intraocular pressure. When administered in the tablet form, it reduces blood pressure, heart rate, and cardiac output, and decreases sympathetic activity.. This drug has a fast onset of action, usually occurring within 20 minutes of the administration of an ophthalmic dose. Timolol maleate can exert pharmacological actions for as long as 24 hours if given in the 0.5% or 0.25% doses. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-1 adrenergic receptor | Humans | antagonist |
| Beta-2 adrenergic receptor | Humans | antagonist |
| Lysozyme | Enterobacteria phage T4 |
ADME / PK
| Absorption | The systemic bioavailability of the ophthalmic eyedrop in one study of healthy volunteers was 78.0 ± 24.5% , indicating that caution must be observed when this drug is administered, as it may be significantly absorbed and have various systemic effects. Another study measured the bioavailability of timolol eyedrops to be 60% in healthy volunteers. The peak concentration of ophthalmic timolol in plasma, Cmax was about 1.14 ng/ml in most subjects within 15 minutes following the administration of timolol by the ophthalmic route. The mean area under the curve (AUC) was about 6.46 ng/ml per hour after intravenous injection and about 4.78 ng/ml per hour following eyedrop administration. |
|---|---|
| Half-life | Timolol half-life was measured at 2.9 ± 0.3 h hours in a clinical study of healthy volunteers. |
| Protein binding | The plasma protein binding of timolol is not extensive and is estimated to be about 10%. |
| Metabolism | Timolol is metabolized in the liver by the cytochrome P450 2D6 enzyme, with minor contributions from CYP2C19. 15-20% of a dose undergoes first-pass metabolism. Despite its relatively low first pass metabolism, timolol is 90% metabolized. Four metabolites of timolol have been identified, with a hydroxy metabolite being the most predominant. |
| Route of elimination | Timolol and its metabolites are mainly found excreted in the urine. |
| Volume of distribution | 1.3 - 1.7 L/kg Timolol is distributed to the following tissues: the conjunctiva, cornea, iris, sclera, aqueous humor, kidney, liver, and lung. |
| Clearance | One pharmacokinetic study in healthy volunteers measured the total plasma clearance of timolol to be 557 ± 61 ml/min. Another study determined the total clearance 751.5 ± 90.6 ml/min and renal clearance to be 97.2 ± 10.1 ml/min in healthy volunteers. |
Formulation & handling
- Timolol is a small molecule suitable for oral and primarily ophthalmic formulations, including solutions, suspensions, gels, and ointments.
- Its moderate water solubility and LogP suggest consideration of solubilization techniques for aqueous ophthalmic dosage forms.
- Formulations should account for stability in aqueous environments given its frequent use in ophthalmic solutions and suspensions.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has patents in the United States with expiry dates ranging from 2010 to 2022, indicating that it has reached market maturity in the US, Canada, and EU regions. Generic competition is likely established in these markets due to the expiration of key patents. |
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| Markets | Canada, EU, US |
|---|
Supply Chain
| Supply chain summary | Timolol is manufactured by a diverse group of originator and generic companies with a broad packaging network, indicating a mature supply landscape. Branded products are available across the US, EU, and Canadian markets, reflecting global market penetration. The listed US patents with expiry dates up to 2022 suggest that generic competition is already established or imminent in these regions. |
|---|
Safety
| Toxicity | The oral LD50 for timolol maleate is 1028 mg/kg in the rat and 1137 mg/kg in the mouse.[MSDS] Symptoms of timolol overdose may include dizziness, headache, shortness of breath, bradycardia, in addition to bronchospasm. Sometimes, an overdose may lead to cardiac arrest. An overdose of timolol can be reversed with dialysis, however, patients with renal failure may not respond as well to dialysis treatment. |
|---|
- Handle timolol maleate with care due to potential systemic toxicity
- The oral LD50 is approximately 1028-1137 mg/kg in rodent models
- Exposure may result in adverse respiratory and cardiovascular effects, including bronchospasm, bradycardia, and risk of cardiac arrest
Timolol 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.
Timolol (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.
Timolol API manufacturers & distributors
Compare qualified Timolol API suppliers worldwide. We currently have 11 companies offering Timolol API, with manufacturing taking place in 6 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 |
|---|---|---|---|---|---|
| Centaur Pharma | Producer | India | India | CEP, CoA, FDA, KDMF, USDMF, WC | 40 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| PCAS | Producer | France | Unknown | CEP, CoA, FDA, GMP, JDMF, KDMF, USDMF | 29 products |
| Quimdis | Distributor | France | Unknown | CoA | 17 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, MSDS | 762 products |
| Syn-tech Chem | Producer | Taiwan | Taiwan | CoA, JDMF, USDMF | 22 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Tianjin Minxiang | Producer | China | China | CoA | 10 products |
| Unnati Pharmaceuticals Pv... | Distributor | India | India | CoA | 70 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 140 products |
| Ven Petrochem & Pharma | Producer | India | India | CEP, CoA, WC | 3 products |
When sending a request, specify which Timolol 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 Timolol 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.
