Antiglaucoma drugs

Multifluorinated aromatics also play a significant role within bioactive compounds. Difluoroaromatics have already been discussed in Chapter 3. Bioactive tetrafluorobenzene derivatives are exemplified by the pyrethroid insecticides transfluthrin (6-9) and tefluthrin (6-10), whereas there are numerous pentafluorobenzene compounds that have proved of interest as potential insecticides, anticancer or antiglaucoma drugs (6-11,6-12, and 6-13) (Fig. 6.5). 

W.M. Grant and I.H. Leopold, Antiglaucoma Drugs Problems with a Carbonic Anhydrase Inhibition , in Symposium on Ocular Therapy, C.V. Mosby, ed., St. Louis, 1973, pp. 19-38. 

Other Medical Conditions. Other systemic disorders can be affected by or contraindicate the use of topically applied medications. Examples include myasthenia gravis, which can be worsened with topical timolol, and erythema multiforme (Stevens-Johnson syndrome), which can be caused or exacerbated by topical ocular sulfonamides and related antiglaucoma drugs such as carbonic anhydrase inhibitors. 

Baudouin C, Pisella P, Eillacier K, et al. Ocular surface inflammatory changes induced by topical antiglaucoma drugs. Ophthalmology 1999 106 556-563. 

The ophthalmic drugs that have been the most frequent causes of product liability and negligence claims are antiglaucoma drugs (i.e., acetazolamide, echothio-phate iodide) and steroids (i.e., hydrocortisone, dexa-methasone sodium phosphate, and prednisolone acetate). 

A. J. Blacker, R. A. Holt, Development of a Multistage Chemical and Biological Process to an Optically Active Intermediate for an Antiglaucoma Drug, in A. N. Collins, G. N. Sheldrake and J. Crosby (eds.), Chirality In Industry II, John Wiley Sons, New York 1997, 246-261. 

Three subtypes of 02-adrenoceptors, 02A, Q2B, and 02c, are recognized. Each plays a role in the different clinical applications of a2-agonists, which include use as antihypertensives (see Chapter 29), antiglaucoma drugs, and analgesics. The first of these drugs, clonidine, was introduced as an antihypertensive, an effect attributed to central a2A-adrenoceptors in cardiovascular control areas of the brain (18). 

The effects of antiglaucoma drugs (epinephrine, timolol, and pilocarpine) on the glycosaminoglycans of the rabbit trabecular meshwork were examined by organ culture. Treatment with epinephrine significantly reduced hyaluronan and increased chondroitin sulfate in the radiolabeled precursor incorporation rate, but the other drugs had little effect (25). 

Kadam, R. Jadhav, G. Kompella, U.B. Yang, H. Polyamidoamine dendrimer hydrogel for enhanced delivery of antiglaucoma drugs. Nanomed. Nanotechnol. 2012, 8 (5), 776-783. 

Muchtar et at. (35) have demonstrated that submicron emulsions can also be used as an ocular delivery system for the lipophilic antiglaucoma drug. A"-tetrahydrocannabinol. They showed that the emulsion was able to achieve a long-lasting antidepressant effect on the intraocular pressure of rabbits following a single Instillation. 

Rescula, the isopropyl ester of unoprostone, is an antiglaucoma drug used to treat ocular hypertension. Compare the structural formula of this synthetic prostaglandin with that of PGF2a-... 

Sensory systems Eyes In a retrospective case series in 84 consecutive patients with uveitis, prostaglandins did not increase the frequency of anterior uveitis or cystoid macular edema compared with other antiglaucoma drugs [35. ... 

An intermediate for the antiglaucoma drug dorzolamide was synthesized in 67% ee through asymmetric conjugate addition of thiophene-2-thiol to E)-3-crotonoyloxazolidin-2-one catalyzed by Sc(OTf)3 and Ph-pybox [126]. In addition, this catalytic system was proved to be successful in the Michael addition of thiophenol to the previous substrate (66% ee). 

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