Carbonic anhydrase inhibitors glaucoma treatment

Therapeutic Function Carbonic anhydrase inhibitor glaucoma treatment Chemical Name 48-Olchloro-m-benzenedisulfonamide Common Name DIclofenamid... 

Therapeutic Function Carbonic anhydrase Inhibitor glaucoma treatment Chemical Name 4,5-Oichloro-m-benzenedisulfonamide Common Name Diclofenamid Structural Formula sOjNH ... 

Therapeutic Function Carbonic anhydrase inhibitor, diuretic, treatment of glaucoma Chemical Name N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl] acetamide Common Name —... 

Carbonic anhydrase inhibitors During treatment for glaucoma, contact the primary health care provider immediately if eye pain is not relieved or if it increases. When a patient with epilepsy is being treated for seizures, a family member of the patient should keep a record of all seizures witnessed and bring this to the primary health care provider at die time of the next visit. Contact the primary healdi care provider immediately if die seizures increase in number. 

Viader MP, McKeever BM, Navia MA. Thienothiopyran-2-sulfonamides novel topically active carbonic anhydrase inhibitors for the treatment of glaucoma. J Med Chem 1989 32 2510-13. 

Acetazolamide is a carbonic anhydrase inhibitor, which reduces intraocular pressure by reducing aqueous humour production. It is used in the treatment of glaucoma. Acetazolamide is administered systemically. Recently newer carbonic anhydrase inhibitors have been developed, which are available as topical agents (for example, dorzolamide). 

Acetazolamide is a carbonic anhydrase inhibitor that is administered orally for the treatment of glaucoma. Topical carbonic anhydrase inhibitors include dorzolamide and brinzolamide. Carbonic anhydrase inhibitors reduce the production of aqueous humour, thereby reducing intraocular pressure. They can be used alone or in addition to beta-blocker therapy in glaucoma patients. 

A variety of thiophene-fused 1,2-thiazines have been prepared as carbonic anhydrase inhibitors for the treatment of glaucoma <2002JME888, 2000BMC957>. The drug brinzolamide (under the trade name Azopt ) 24 has recently been approved by the FDA. 

Table 15-3 Carbonic Anhydrase Inhibitors Used Orally in the Treatment of Glaucoma. ...

Figure 2.6 Dorzolamide 16, a topically active carbonic anhydrase inhibitor, resulted from a structure-based ligand design it is used for the treatment of glaucoma. Sulfaguanidine 17 inhibits thyroid hormone biosynthesis. A phenylog of sulfanilamide 11 (Figure 2.4), dapsone 18, is used for the treatment of leprosy.

Figure 10-15 Mean intraocular pressure (lOP) change (mm Hg) for the various treatment groups by visit and time of day for a 3-month treatment period. Each value represents the least-squares mean of the change from baseline diurnal lOP, and all were significant. (Adapted from Silver LH, Brinzolamide Primary Therapy Smdy Group. Clinical efficacy and safety of brinzolamide [Azopt], a new topical carbonic anhydrase inhibitor for primary open-angle glaucoma and ocular hypertension. Am J Ophthalmol 1998 126 400-408.)...

Carbonic Anhydrase Inhibitors. The CAls (Table 34-8) are aqueous suppressants not typically used as first-line medications in the treatment of glaucoma. 

Carbonic anhydrase inhibitors are used for long-term treatment of open-angle glaucoma, interfering with the production of carbonic acid, which results in decreased IOP. 

An even more extreme situation is found with carbonic anhydrase inhibitors such as ac-etazolamide, ethoxyzolamide, and methazol-amide, which are useful for the treatment cf glaucoma. Because of their limited aqueous solubility or unfavorable lipophilicity,they are not active when given topically to the eye and must be given orally or parenterally. Systemic side effects severely limit this mode of therapy and, consequently, numerous investigations are presently under way to find a new carbonic anhydrase inhibitor that readily penetrates the cornea or to prepare a prodrug with adequate water solubility and lipophilicity combined with the ability to be reconverted to the parent sulfonamide after corneal passage (255-257). 

The final example of a novel process development formulation involves a semi-solid ophthalmic gel containing a carbonic anhydrase inhibitor drug for the treatment of glaucoma. It is administered to the patient by extruding the gel from an ophthalmic tube into the conjunctival sac of the eye. The drug had a very low aqueous solubility. It was necessary to reduce the particle size of the drug to less than 10 pim and suspend it in a very thick carbomer gel vehicle, to increase the residence time of the gel and maximise corneal permeation. The formulation details are given below ... 

The major indication for carbonic anhydrase inhibitors is open-angle glaucoma. Carbonic anhydrase inhibitors also may be employed for secondary glaucoma and preop-eratively in acute angle-closure glaucoma to lower intraocular pressure before surgery. Acetazolamide also is used for the treatment of epilepsy. The rapid development of tolerance, however, may limit the usefulness of carbonic anhydrase inhibitors for epilepsy. 

Brinzolamide is a carbonic anhydrase inhibitor that causes an inhibition of carbonic anhydrase in the cihary processes of the eye deaeases aqueous. It is indicated in the treatment of elevated lOP inpatients with ocular hypertension or open-angle glaucoma. The development of topical carbonic anhydrase inhibitor took many years but was an important event because of the poor side-effect profile of oral carbonic anhydrase inhibitors (CAIs). Dorzolamide (Trusopt) and brinzola-mide both work by inhibiting carbonic anhydrase (isoenzyme n), which is found in the ciliary body epithehum. This reduces the formation of bicarbonate ions, which reduces fluid transport and thus lOP. hi fact, the P-receptor antagonist timolol has been combined with the carbonic anhydrase inhibitor dorzolamide in a single medication (Cosopt). 

Dorzolamide is a carbonic anhydrase inhibitor that inhibits carbonic anhydrase enzyme, reducing the rate of aqueous humor formation and thus lowering intraocular pressure (lOP). It is indicated in the treatment of elevated lOP in patients with ocular hypertension or open-angle glaucoma. 

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