Antiglaucoma agent

Use beta blocking agent, antiglaucoma agent, antianginal, antiarrhythmic... 

In the synthesis of Travoprost, an antiglaucoma agent, a bicyclo[2.2.1]heptan-2-one is converted to a lactone.240 The commercial process uses peroxyacetic acid as the oxidant and gives a 40% yield. The regioselectivity in this case is only 3 1 but the unwanted isomer can be removed by selective hydrolysis. 

Glaucoma Initial therapy or as an adjunct with other antiglaucoma agents for the control of intraocular pressure (lOP) in chronic open-angle glaucoma. 

Timolol, Ophthalmic (Timoptic) [Antiglaucoma Agent/Beta Blocker] Uses Glaucoma Action BB Dose 0.25% 1 gt bid T to daily when controlled use 0.5% if needed 1 gtt/d gel Caution [C (1st tri D 2nd or 3rd), /+] Disp Sohi, gel SE Local irritation Interactions See Timolol EMS See Timolol OD Unlikely from ophthalmic form... 

B. Resul, J. Stjernschantz, K. No, C. Liljebris, G. Selen, M. Astin, M. Karlsson, L.Z. Bito, Phenyl-substituted prostaglandins Potent and selective antiglaucoma agents, J. Med. Chem. 36 (1993) 243. 

Mechanism of Action An antihypertensive and antiglaucoma agent that blocks beta,-adrenergic receptors in cardiac tissue. Reduces aqueous humor production. Therapeutic Effect Slows sinus heart rate, decreases BP, and reduces intraocular pressure (lOP). 

Vision-Novartis (phase III completed in 1999 for age-related macular degeneration also in trial for psoriasis and leukemia) (see also timolol above, an antiglaucoma agent)... 

Pilocarpine is the active ingredient in Ocusert , an antiglaucoma agent, which can be inserted behind the lower eyelid. 

The Schedule I designation of marijuana has been disputed over the past 15 or more years. Some physicians would like to see it as a Schedule II drug so that it could be used therapeutically in the treatment of the nausea, vomiting and anxiety caused by cancer chemotherapy and as an antiglaucoma agent (lowers intraocular pressure). It should be noted that the neuroleptic prochlorperazine is an effective antinausea drug which can be used without producing the psychoactive effects of marijuana. 

The initial increase followed by a prolonged decrease has not been observed previously with cannabinoids and may represent a serious drawback in the eventual clinical use of anandamides as antiglaucoma agents. This bi-phasic effect is reminiscent of the same phenomenon seen with anandamide in blood pressure measurements (see above). 

Maestrclli, E, Mura, R, Casini, A., Mincione, F., Scozzafava, A., and Supuran.C.T. (2002), Cyclodextrin complexes of sulfonamide carbonic anhydrase inhibitors as long-lasting topically acting antiglaucoma agents,/. Pharm. Sci., 91(10), 2211-2219. 

Of the commonly used therapeutic drugs, the greatest risks are encountered when clinicians prescribe topical steroids (for extended periods), systemic steroids, P blockers, miotic antiglaucoma agents, and oral carbonic anhydrase inhibitors (CAIs). Optometrists should be aware of the adverse effects that attend the use of these drugs and should warn patients accordingly. Disclosures should be documented in the patient record. 

Woodward DF, Phelps RL, Krauss AFI, et al. Bimatoprost a novel antiglaucoma agent. Cardiovasc Drug Rev 2004 22 103-120. Woodward DF, Krauss AH, Chen J, et al. The pharmacology of bimatoprost (Lumigan). Surv Ophthalmol 2001 45(suppl 4) S337-S345. 

The beneficial action of triamcinolone appears to be related to its inhibition of synthesis of inflammatory mediators (prostaglandins and interleukins), inhibition of the VEGF gene, and improved stability of the blood-retinal barrier. The rise in intraocular pressure typically occurs in 40% to 50% of patients but is controllable with one or two topical antiglaucoma agents. Other complications of IVTA include ptosis, endophthalmitis, accelerated development of cataract, and retinal detachment. The most worrisome compUcation is infectious endophthalmitis, but the incidence of cases is quite low. 

Catecholamines are sympathomimetic drugs. Dopamine and norepinephrine are used as vasopressors (antihypotensives). Epinephrine is used as a vasoconstrictor, cardiac stimulant, or bronchodilator to counter allergic reaction, anesthesia, and cardiac arrest. It is also an antiglaucoma agent. 

Resul, B., Stjemschantz, J., No, K., et al. (1993) Phenyl-substituted prostaglandins Potent and selective antiglaucoma agents. Journal of Medicinal Chemistry, 36, 243-248. 

Yu DY, Su EN, Cringle SJ, et al. Systemic and ocular vascular roles of the antiglaucoma agents beta-adrenergic antagonists and Ca + entry blockers. Surv Ophthalmol 1999 43(Suppl l) S214-222. 

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