Timolol Ophthalmic

WL Nelson, FT Fraunfelder, JM Sills, JB Arrowsmith, JN Kuritsky. (1986). Adverse respiratory and cardiovascular events attributed to timolol ophthalmic solution. Am J Ophthalmol 102 606-611. 

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... 

I Brand Name(s) Betimol, Blocadren, Istalol, Timolol Ophthalmic, Timoptic, Timoptic OccuDose, TimopticOcumeter, TimopticOcumeter Plus, TimopticXE... 

Shedden, A., Laurence, I, and Tipping, R. (2001), Efficacy and tolerability of timolol maleate ophthalmic gel-forming solution versus timolol ophthalmic solution in adults with open-angle glaucoma or ocular hypertension A six-month, double-masked, multicenter study, Clin. Then, 23(3), 440 150. 

MA-MVE isopropyl ester timolol (ophthalmic use, reduced high blood pressure) 156... 

When a -adrenergic blocking ophthalmic preparation, such as timolol, is administered to patients with glaucoma, it is important to insist that they have periodic follow-up examinations by an ophthalmologist. At these examinations, the intraocular pressure should be measured to determine the effectiveness of drug therapy. 

Co-administration of ofloxacin and chitosan in eyedrops increased the bioavailabUity of the antibiotic [290]. Trimethyl chitosan was more effective because of its solubility (plain chitosan precipitates at the pH of the tear fluid). On the other hand, N-carboxymethyl chitosan did not enhance the corneal permeability nevertheless it mediated zero-order ofloxacin absorption, leading to a time-constant effective antibiotic concentration [291]. Also W,0-carboxymethyl chitosan is suitable as an excipient in ophthalmic formulations to improve the retention and the bioavailability of drugs such as pilocarpine, timolol maleate, neomycin sulfate, and ephedrine. Most of the drugs are sensitive to pH, and the composition should have an acidic pH, to enhance stability of the drug. The delivery should be made through an anion exchange resin that adjusts the pH at around 7 [292]. Chitosan solutions do not lend themselves to thermal sterilization. A chitosan suspension, however. 

Hyaluronic acid is a linear polysaccharide found in the highest concentrations in soft connective tissues where it fills an important structural role in the organization of the extracellular matrix (23,24). It has been used in ophthalmic preparations to enhance ocular absorption of timolol, a beta blocker used for the treatment of glaucoma (25), and in a viscoelastic tear formulation for conjunctivitis (26). The covalent binding of adriamycin and daunomycin to sodium hy-aluronate to produce water-soluble conjugates was recently reported (27). 

Other quaternary ammonium germicides, ben-zethonium chloride and benzalkonium bromide, have been used in several ophthalmic solutions. While these have the advantage of not being a chemical mixture, they do not possess the bactericidal effectiveness of benzalkonium chloride and are subject to the same incompatibility limitations. In addition, the maximum concentration for benzethonium chloride is 0.01%. Several new products that form gels in the eye, like Timolol Gel Forming Solution and Timoptic-XE, employ another quaternary preservative, BDAB, in the formulation. 

TIMOLOL MALEATE OPHTHALMIC SOLUTION USP 5ML BOTTLE WITH TIP 6505010696519 BT 3.20 ... 

A large number of (3-blockers are on the market in the United States. Of these, propranolol, a nonselective (3-antagonist, was the first to be introduced and is the prototypical drug with which the others are compared. Metoprolol was the hrst (3i-selective drug and timolol the hrst (3-blocker approved for ophthalmic use. 

Nadolol is noteworthy for its very long duration of action its spectrum of action is similar to that of timolol. Timolol is a nonselective agent with no local anesthetic activity. It has excellent ocular hypotensive effects when administered topically in the eye. Levobunolol (nonselective) and betaxolol (E -selective) are also used for topical ophthalmic application in glaucoma the latter drug may be less likely to induce bronchoconstriction than nonselective antagonists. Carteolol is a nonselective 13-receptor antagonist. 

Rimexolone (Vexol Ophthalmic) Timolol, Ophtlialmic (Timoptic)... 

Salminen, L., and Urtti, A. Disposition of ophthalmic timolol in treated and untreated rabbit eyes. A multiple and single dose study. Exp. Eye Res. 38(2) 203—206, 1984. 

Shibuya,T., Kashiwagi, K., and Tsukahara, S. (2003), Comparison of efficacy and tolerability between two gel-forming timolol maleate ophthalmic solutions in patients with glaucoma or ocular hypertension, Ophthalmologica, 217(1), 31-38. 

Shedden, A. H., Laurence, J., Barrish, A., and Olah, T. V. (2001), Plasma timolol concentrations of timolol maleate Timolol gel-forming solution (TIMOPTIC-XE) once daily versus timolol maleate ophthalmic solution twice daily, Doc. Ophthalmol., 103(1), 73-79. 

Rozier, A., Mazuel, C., Grove, J., and Plazonnet, B. (1989), Gelrite(R) A novel, ion-activated, in-situ gelling polymer for ophthalmic vehicles. Effect on bioavailability of timolol, Int. J. Pharm., 57(2), 163-168. 

Aggarwal, D., and Kaur, I. P. (2005), Improved pharmacodynamics of timolol maleate from a mucoadhesive niosomal ophthalmic drug delivery system, Int. I. Pharm., 290(1-2), 155-159. 

Saettone, M. F., Chetoni, P, Bianchi, L. M., Giannaccini, B., Conte, U., and Sangalli, M. E. (1995), Controlled release of timolol maleate from coated ophthalmic mini-tablets prepared by compression, Ini. J. Pharm., 126(1-2), 79-82. 

When topical ophthalmic drugs must be administered to patients who are pregnant, the medications should be administered at minimally effective doses and for as short a time as possible.The use of nasolacrimal occlusion (see Chapter 3) after the instillation of eye medications minimizes systemic drug absorption and should always be recommended. Patients who take medications should also be advised about the potential risks to newborns during breast-feeding (Figure 1-2). Timolol, for example, has been shown to be concentrated in breast milk. 

Rozier A, Mazuel C, Grove J, et al. Gelrite a novel ion-activated, in-sim geUing polymer for ophthalmic vehicles. Effect on bioavailabUity of timolol. Int J Pharmacol 1989 57 163-168. 

Figure 10-7 Mean change in forced expiratory volume in 1 second (FEVi) after instillation of timolol, betaxolol, or placebo (vehicle). Timolol induced a significant decrease in airflow, whereas betaxolol produced values no different from those for the placebo. (Reprinted with permission from Am J Ophthalmol 1984 97 86-92. Copyright by the Ophthalmic Publishing Company.)...

Bamebey HS, Orengo-Nania S, Flowers BE, et al.The safety and efficacy of travoprost 0.004%/timolol 0.5% fixed combination ophthalmic solution.Am J Ophthalmol 2005 140 1-7. Bartlett JD, Olivier M, Richardson T, et al. Central nervous system and plasma lipid profiles associated with carteolol and timolol in postmenopausal black women.) Glaucoma 19S>9 8 388-395. Becker B. Use of mettiazolamide (Neptazane) in the therapy of glaucoma comparison with acetazolamide (Diamox). Am ) Ophthalmol 1960 49 1307-1311. 

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