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Dorzolamide | CAS No: 120279-96-1 | GMP-certified suppliers
A medication that manages elevated intraocular pressure in ocular hypertension and open-angle glaucoma, alone or combined with timolol, to improve patient responsiveness to treatment.
Therapeutic categories
Primary indications
- Dorzolamide is indicated for the management of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma
- It can also be used in combination with [timolol] for the same indication in patients who are insufficiently responsive to ophthalmic beta-blockers
- Its pre-operative use was also investigated to prevent elevated intraocular pressure after neodynium yttrium aluminum garnet laser posterior capsulotomy
Product Snapshot
- Dorzolamide is an ophthalmic solution formulated as topical eye drops
- It is primarily used to manage elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma, including use in combination with timolol
- Dorzolamide is approved for use in key markets including the United States and Canada
Clinical Overview
Pharmacologically, dorzolamide targets carbonic anhydrase II (CA-II), an enzyme integral to the production of bicarbonate ions within the ciliary processes of the eye. CA-II inhibition diminishes bicarbonate formation, leading to reduced sodium and fluid transport, thereby decreasing aqueous humor secretion and lowering IOP. This effect is achieved with minimal systemic impact due to the drug’s topical administration and negligible systemic bioavailability, avoiding acid-base or electrolyte disturbances commonly associated with systemic carbonic anhydrase inhibitors. The peak ocular hypotensive effect occurs approximately two hours following administration, and combination therapy with topical beta-blockers results in additive IOP reduction.
From a structural perspective, dorzolamide is a sulfonamide derivative classified within 2,3,5-trisubstituted thiophenes. It is primarily metabolized by ocular tissues and exerts its effects locally with minimal systemic absorption. Renal excretion plays a minor role in its elimination due to limited systemic exposure.
Safety considerations for dorzolamide include potential local adverse effects such as ocular burning or stinging upon instillation, and rare instances of sulfonamide-related hypersensitivity reactions. Unlike systemic carbonic anhydrase inhibitors, dorzolamide has a lower risk profile for systemic toxicity, making it suitable for chronic topical use in glaucoma management.
Dorzolamide has been marketed since 1995, commonly available as the ophthalmic solution Trusopt, and in combination with timolol under the brand Cosopt PF. Procurement of dorzolamide API requires adherence to rigorous quality standards, ensuring purity and stability suitable for sterile ophthalmic formulations. Due to its sulfonamide structure, attention should be given to potential cross-reactivity in patients with sulfonamide allergies when evaluating formulation suitability. Certified suppliers with validated manufacturing processes and appropriate documentation are recommended for API sourcing.
Identification & chemistry
| Generic name | Dorzolamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 120279-96-1 |
| UNII | 9JDX055TW1 |
| DrugBank ID | DB00869 |
Pharmacology
| Summary | Dorzolamide is a carbonic anhydrase inhibitor that targets primarily carbonic anhydrase II in ocular ciliary processes to reduce aqueous humor production. By inhibiting this enzyme, it decreases bicarbonate ion formation, thereby reducing sodium and fluid transport and lowering intraocular pressure. It is used to manage elevated intraocular pressure associated with ocular hypertension and open-angle glaucoma. |
|---|---|
| Mechanism of action | Elevated intraocular pressure is a characteristic manifestation of ocular hypertension or open-angle glaucoma. The level of intraocular pressure (IOP) is governed by the balance between the production of aqueous humour (by ocular ciliary processes) and its outflow from the anterior segment of the eye via trabecular (conventional) or uveoscleral (unconventional) pathways. When there is an increase in the resistance to the trabecular outflow of aqueous humour, the intraocular pressure is elevated. Subsequently, optic nerve damage can occur from blood flow restrictions and mechanical distortion of ocular structures. Optic nerve damage can further result in optic disc cupping and progressive visual field loss (and blindness in some cases). Carbonic anhydrase (CA) is a ubiquitous enzyme that catalyzes the reversible hydration of carbon dioxide to bicarbonate ions and dehydration of carbonic acid. In the ocular ciliary processes, the local production of bicarbonate by CAs promotes sodium and fluid transport. CA-II is a key isoenzyme found primarily in red blood cells (RBCs) that regulates aqueous humour production. Dorzolamide is a highly specific CA-II inhibitor, where it displays a 4000-fold higher affinity for carbonic anhydrase II than carbonic anhydrase I. The inhibition of CA-II in the ciliary process disrupts the formation of bicarbonate ions and reduces sodium and fluid transport, which leads to decreased aqueous humour secretion and reduced intraocular pressure. |
| Pharmacodynamics | Dorzolamide is a carbonic anhydrase inhibitor that reduces elevated intraocular pressure in open-angle glaucoma or ocular hypertension. When used in combination with topic beta-adrenergic antagonists, dorzolamide has an additive effect of lowering intraocular pressure. The peak ocular hypotensive effect of dorzolamide is observed at about 2 hours following ophthalmic administration. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Carbonic anhydrase 2 | Humans | inhibitor |
| Carbonic anhydrase 4 | Humans | inhibitor |
| Carbonic anhydrase 1 | Humans | inhibitor |
ADME / PK
| Absorption | Dorzolamide readily penetrated into the eye in animal studies. Upon ophthalmic administration, dorzolamide is absorbed via the cornea and stroma. Dorzolamide is reported to be absorbed systematically following topical administration. The systemic exposure of dorzolamide following long-term administration was assessed in healthy subjects receiving an oral dose of 2 mg dorzolamide twice daily, which equates to the ophthalmic dose of 2% dorzolamide three times daily. In these subjects receiving the treatment for 20 weeks, the steady-state was reached within 8 weeks. |
|---|---|
| Half-life | As the drug administration is stopped, dorzolamide stored in RBCs is washed out of RBCs in a non-linear fashion, with the terminal elimination half-life of ≥120 days in RBCs. This initial rapid decline in drug concentrations is followed by the slow elimination phase, where the elimination half-life of the drug is about >4 months. |
| Protein binding | Dorzolamide is approximately 33% bound to plasma proteins. |
| Metabolism | Dorzolamide is slowly metabolised to N-desethyldorzolamide, which has a less potent pharmacological activity on CA-II and some inhibitory effect on CA-I. Like the parent drug, N-desethyldorzolamide is also stored in RBCs, where it binds to CA-I. The findings of an _in vitro_ study using liver microsomes from Sprague-Dawley rats suggest the involvement of CYP2B1, CYP2E1, and CYP3A2 in the metabolism of dorzolamide in rat liver. |
| Route of elimination | Dorzolamide is primarily excreted unchanged in the urine; however, N-desethyldorzolamide is also detected in the urine. |
| Volume of distribution | There is limited information on the volume of distribution of dorzolamide; however, the plasma concentrations of dorzolamide and its main metabolite are generally below the assay limit of quantitation, which is 15nM. Dorzolamide accumulates in red blood cells following chronic administration as a result of binding to CA-II, which is contained in peripheral red blood cells (RBCs). |
| Clearance | There is limited information on the clearance rate of dorzolamide. |
Formulation & handling
- Dorzolamide is a small molecule API formulated exclusively for ophthalmic administration as solutions or suspensions.
- Its moderate water solubility and near-neutral LogP support formulation in aqueous ophthalmic solutions without extensive solubilizers.
- Handling considerations should include protection from microbial contamination due to its use in multi-dose ophthalmic preparations.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has had patent protection in Canada that expired in May 2011. It is currently marketed in Canada and the US, representing a mature product in these markets. |
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| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Dorzolamide includes multiple originator companies with a significant presence in North American markets, particularly the US and Canada. Branded products are marketed primarily in these regions, with several suppliers and packagers involved, indicating an established supply network. The patent expiration in Canada as of 2011 suggests that generic competition is established or imminent in these markets. |
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Safety
| Toxicity | The oral LD<sub>50</sub> of dorzolamide is 1927 mg/kg in rats and 1320 mg/kg in mice. The subcutaneous LD<sub>50</sub> is >2 g/kg in both rats and mice. Overdose may result in electrolyte imbalance, acidosis, and possibly central nervous system effects; these symptoms should be responded with appropriate supportive treatment. It is advised that the patient's serum electrolyte (particularly potassium) levels and blood pH levels are monitored in the case of a suspected overdose. |
|---|
- Dorzolamide exhibits moderate acute toxicity with oral LD50 values of 1927 mg/kg in rats and 1320 mg/kg in mice
- Subcutaneous administration shows LD50 values exceeding 2 g/kg in rodent models, indicating lower systemic toxicity via this route
- Overdose may induce electrolyte disturbances, metabolic acidosis, and central nervous system effects
Dorzolamide is a type of Carbonic anhydrase(II) inhibitors
Carbonic anhydrase (CA) inhibitors are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that specifically target the enzyme carbonic anhydrase II (CAII). CAII is a zinc metalloenzyme that plays a crucial role in the regulation of acid-base balance and fluid secretion in various tissues and organs.
These inhibitors are designed to selectively bind to CAII and inhibit its enzymatic activity. By doing so, they disrupt the conversion of carbon dioxide (CO2) to bicarbonate ions (HCO3-) and protons (H+), which is a fundamental process in many physiological functions.
The inhibition of CAII has been found to be useful in the treatment of several medical conditions. One of the most common applications is in the management of glaucoma, a condition characterized by increased intraocular pressure. By inhibiting CAII in the ciliary body of the eye, these inhibitors reduce the production of aqueous humor, thus lowering the intraocular pressure.
In addition to glaucoma, CAII inhibitors have shown promise in the treatment of other disorders such as epilepsy, edema, and certain types of cancer. Their ability to modulate the pH and ion balance in tissues makes them potential therapeutic agents in a wide range of conditions.
The development of CAII inhibitors involves extensive structure-activity relationship studies and optimization of chemical properties to enhance potency, selectivity, and pharmacokinetic properties. Various structural classes of CAII inhibitors have been synthesized and tested, providing a rich pool of potential drug candidates.
In conclusion, carbonic anhydrase II inhibitors are a valuable subcategory of pharmaceutical APIs that hold promise for the treatment of various medical conditions. Continued research and development in this field may lead to the discovery of novel and effective therapies in the future.
Dorzolamide (Carbonic anhydrase(II) inhibitors), classified under Anticoagulants
Anticoagulants are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used to prevent and treat blood clotting disorders. These medications play a crucial role in various medical conditions, including deep vein thrombosis (DVT), pulmonary embolism (PE), and atrial fibrillation (AF). Anticoagulants work by inhibiting the formation of blood clots or by preventing existing clots from getting larger.
There are different types of anticoagulants available, including direct thrombin inhibitors, vitamin K antagonists, and factor Xa inhibitors. Direct thrombin inhibitors, such as dabigatran, directly target the enzyme thrombin to hinder clot formation. Vitamin K antagonists, like warfarin, interfere with the production of clotting factors that rely on vitamin K. Factor Xa inhibitors, such as rivaroxaban and apixaban, inhibit the activity of factor Xa, a crucial component in the clotting cascade.
Anticoagulants are commonly prescribed to patients at risk of developing blood clots or those with existing clotting disorders. They are often used during surgeries, such as hip or knee replacements, to minimize the risk of post-operative clot formation. Patients with AF, a condition characterized by irregular heart rhythm, may also be prescribed anticoagulants to prevent stroke caused by blood clots.
While anticoagulants offer significant benefits in preventing and treating clot-related conditions, they also carry potential risks, including bleeding complications. Patients taking anticoagulants require careful monitoring to ensure the right dosage is administered, as excessive anticoagulation can lead to hemorrhage. Regular blood tests and close medical supervision are essential to manage the delicate balance between preventing clots and avoiding excessive bleeding.
In conclusion, anticoagulants are a crucial category of pharmaceutical APIs used to prevent and treat blood clotting disorders. They function by inhibiting clot formation or preventing existing clots from enlarging. While highly beneficial, their use requires careful monitoring to minimize the risk of bleeding complications.
Dorzolamide API manufacturers & distributors
Compare qualified Dorzolamide API suppliers worldwide. We currently have 11 companies offering Dorzolamide API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| AXXO GmbH | Distributor | Germany | European Union | CoA, EDMF/ASMF, GMP, GDP, MSDS | 243 products |
| Bakul Pharma Private Limi... | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, MSDS | 52 products |
| Curia | Producer | United States | Spain | CEP, CoA, GMP, JDMF, MSDS, USDMF | 106 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hetero Drugs | Producer | India | India | CEP, CoA, GMP, USDMF, WC | 98 products |
| Indoco Remedies | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 19 products |
| Micro Labs | Producer | India | India | CEP, CoA, FDA, GMP, JDMF, USDMF, WC | 38 products |
| PCAS | Producer | France | Unknown | CEP, CoA, FDA, GMP, USDMF | 29 products |
| Quimdis | Distributor | France | Unknown | CoA | 17 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
When sending a request, specify which Dorzolamide 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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