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At least 721 records · Page 40Linked to original sources

PubMed1979

The effects of timolol on cataract extraction and intraocular pressure.

We studied the effect of timolol on post-operative intraocular pressures (IOPs) in a control and experimental group of 30 eyes, each in patients who had uncomplicated intracapsular cataract extractions, most with iris clip lenses. Closure of the eye in each case was with three 6-0 silk sutures preplaced in a morticed incision. Six control eyes had IOP increases of 6 mm Hg or more within 24 hours of surgery. One patient treated with timolol had an IOP increase of 6 mm Hg or more. The differences in IOP between the control and experimental groups were statistically significant at the .01 level. The pressure lowering ability of timolol appears to be prophylactic as well as therapeutic. It is well suited for pseudophakic eyes as pressure reduction is not associated with pupillary alterations.

Cataract Extraction↗

PubMed1979

Evaluation of timolol maleate combination therapy in chronic open-angle glaucoma.

In an eight-week study, timolol maleate ophthalmic solution 0.25% was administered twice daily with either pilocarpine 2% four times a day, epinephrine 2% twice a day, carbachol 1.5% four times a day, or 250 mg of acetazolamide twice a day to 44 patients with chronic open-angle glaucoma. Compared to baseline readings on standard therapy alone, mean intraocular pressure was significantly reduced after addition of timolol maleate to each of the regimens. Mean facility of outflow was unaffected. No clinically significant ocular irritation or changes in visual acuity, pupil size, or vital signs were observed in any patient. Timolol maleate appears to be effective and well tolerated when administered with other antiglaucoma medications in patients with open-angle glaucoma.

Acetazolamide↗

PubMed1979

Adverse effects experienced by patients taking timolol.

Adverse effects involving one or more organ systems occurred in 38 of 165 patients with various types of glaucoma when timolol was added to their glaucoma therapy. It was necessary to discontinue timolol because of these side effects in 15 (9%) of the patients. Double-masked studies will be necessary to clarify the relationship of these adverse effects to the use of timolol.

Aged↗

PubMed1981

Safety and effectiveness of concomitant administration of dipivefrin and timolol maleate.

Dipivefrin, an epinephrine prodromal drug, was used in conjunction with timolol maleate to evaluate the safety and effectiveness of combined therapy. Seventeen patients who had used timolol maleate for at least six months added dipivefrin (Group 1) and seven patients who had used dipivefrin for at least six months added timolol maleate (Group 2). Intraocular pressure decreased further in both groups. Side effects were most prominent in Group 1.

Adult↗

PubMed1984

Effect of indomethacin on the ocular hypotensive action of timolol maleate.

A randomized, double-masked, cross-over study of nine healthy normal subjects was conducted to determine whether indomethacin affected the ocular hypotensive action of timolol maleate. A significant decrease in intraocular pressure occurred with timolol maleate 0.5% eyedrops (used twice a day) alone. Indomethacin (25 mg three times a day, given orally) administered concurrently had no effect on timolol's hypotensive action. No subjective or objective side effects occurred and there were no significant changes in blood pressure, pulse rate, or respiratory rate with either treatment.

Double-Blind Method↗

PubMed1984

Effects of topical betaxolol, timolol, and placebo on pulmonary function in asthmatic bronchitis.

To evaluate the effects of two beta-adrenergic blocking agents on cardiopulmonary function, we investigated two topical ophthalmologic preparations, betaxolol 1% and timolol 0.5%, in nine patients (eight men and one woman, ranging in age from 25 to 69 years) with reactive airway disease. The randomized, double-masked, crossover study used placebo eyedrops as the control, and each drug was tested on separate days. Spirometric measurements, respiratory rate, pulse rate, and blood pressure were observed at frequent intervals for four hours after the test solutions were instilled. At the end of the test, an inhaled beta-adrenergic stimulant (isoproterenol) was administered, and the measurements were repeated. Timolol produced a significant decrease in airflow, measured by forced expiratory volume in one second (FEV1) and the ratio of FEV1 to vital capacity at each observation time beyond 15 minutes. Betaxolol and placebo eyedrops produced no significant change from control values. These results suggested that timolol can adversely affect patients with reactive airway disease. Betaxolol eyedrops, conversely, caused no decrease in airflow in the same patients with proven airway disease.

Administration, Topical↗

PubMed1988

A double-masked comparison of carteolol and timolol in ocular hypertension.

We performed a double-masked study in which 98 patients with ocular hypertension who had been previously treated with timolol received either timolol 0.25% or carteolol 1%, a beta-blocker with intrinsic sympathomimetic activity. The drugs were administered topically twice daily for one month after a one-week washout period. Intraocular pressure was measured at baseline and after one and four weeks of treatment. The appearance of the fundus, external eye, visual fields, tear secretion, blood pressure, and pulse were recorded. Adverse symptoms were elicited using a menu-type questionnaire and an overall judgment of therapy was recorded. Carteolol was as effective as timolol in reducing intraocular pressure. There were significantly fewer patients reporting adverse events overall (P = .019), and eye irritation specifically (P = .02), in the group treated with carteolol.

Administration, Topical↗

PubMedDate not supplied

Experimental studies on the mechanism of action of timolol.

Timolol, which binds to beta-adrenergic receptors, is a potent antagonist of the catecholamine-stimulated synthesis of cyclic AMP. However, the actual mechanism of action by which timolol reduces intraocular pressure is not readily apparent. Compared to its efficacy in human eyes, the drug is relatively ineffective in rabbit eyes. A reasonable postulate is that soon after administration, timolol blocks endogenous adrenergic stimulation contributing to the formation of aqueous humor by the ciliary processes. Nevertheless, the long-lasting reduction of intraocular pressure persists at a time when the drug is no longer bound to beta-adrenergic receptors.

Animals↗

PubMedDate not supplied

Longterm timolol therapy.

Of 145 patients registered for an investigation of timolol, 27 patients were dropped for unrelated reasons. Among the remaining 118 patients (212 eyes), a significant reduction in intraocular pressure resulted from twice-a-day topical instillation of 0.25 or 0.5% timolol to ocular hypertensives, primary open-angle glaucoma or aphakic glaucoma patients. Outflow facility improved only slightly, but remained improved throughout the course of this study. A significant reduction in aqueous secretion, however, was the predominant cause of intraocular pressure reduction. Timolol alone controlled intraocular pressure in 87% of ocular hypertensives, in 68% of patients with chronic open-angle glaucoma and in 68% of patients with angle-unobstructed aphakic glaucomas. The addition of epinephrine brought the intraocular pressure to less than 22 mm Hg in 85% of the total group of patients.

Adolescent↗

PubMed1983

Timolol in childhood glaucoma.

In determining the role of timolol in the treatment of childhood glaucoma, the difficulties of conducting investigational studies in children and the possible delayed appearance of longterm side effects are real concerns. However, an equally important consideration is the fact that young children may face a lifetime of blindness from uncontrolled glaucoma. Timolol is not always successful in lowering intraocular pressure on a longterm basis in severe glaucoma, but it often does help in managing extremely difficult cases. In some respects, the results of using timolol in children are consistent with those achieved with severe adult glaucoma. Although experience with children under one year of age is still extremely limited, theoretical considerations would suggest that children might be particularly vulnerable to the known systemic side effects following local absorption, as well as to longterm side effects that are yet unknown.

Age Factors↗

PubMedDate not supplied

Ophthalmic beta-blockers since timolol.

In the twenty years since beta-blockers were proposed for treatment of glaucoma, use of topical timolol has increased to account for 70% of all glaucoma medications used. The objective of this article is to review the "newer" beta-blockers, and to address the generalization that "all ophthalmic beta-blockers are the same." The review concentrates on agents that have been studied as topical treatments for patients with elevated intraocular pressure. Sections on pharmacology and design of clinical trials are included to aid the ophthalmologist in evaluating the new drugs and published clinical reports. The major questions to consider in evaluating the therapeutic potential of a new beta-blocker for the treatment of glaucoma involve efficacy and safety: Is the drug as effective as timolol? Does it have a duration of action at least as long as timolol? Does it have ocular toxicity? Is it comfortable? What are its systemic effects?

Adrenergic beta-Antagonists↗

PubMed1994

Differences in the longterm effect of timolol and betaxolol on the pulsatile ocular blood flow.

In the past several years the effect of longterm glaucoma therapy on ocular hemodynamics has taken on increased interest. This interest has been sparked by studies demonstrating differential effects of various beta-blockers on visual function, and the possible contributory role of ocular blood flow. In the present study, the pulsatile ocular blood flow (POBF), as derived by the Langham OBF system, was measured prior to treatment and then tracked throughout a one-year period of beta-blocker therapy (betaxolol 0.5% or timolol 0.5%) in 25 glaucoma patients. Results of the two treatments were compared, and indicated that, whereas both betaxolol- and timolol-treated patients had similar significant reductions in the IOP, the effect of the two treatments on the POBF differed. In timolol-treated patients, the POBF decreased significantly over the 12-month observation period, whereas in betaxolol-treated patients it remained stable.

Adult↗

PubMed1985

Once daily timolol in the prophylaxis of angina pectoris.

The clinical efficacy of timolol given once and twice daily was compared in the management of angina pectoris. Following a 2-week entry period, 16 normotensive male subjects with stable angina and proven myocardial ischaemia received timolol 10 mg twice daily, or 20 mg every morning for 1 month followed by 1 month on crossover therapy. All were exercised on separate days in random order 1 hr after administration of 10 mg, 1 hr after administration of 20 mg, 13 hr after administration of 10 mg and 25 hr after administration of 20 mg. In spite of significant differences in the maximum heart rates, rate pressure products and maximum lateral ST segment depression between the once and twice daily regimes, the maximal walking times were not significantly different (P greater than 0.10) and attack rates for angina and trinitrin consumption were similar (P greater than 0.45; P greater than 0.05). This evidence suggests that timolol is as effective in dosage of 20 mg taken once daily as half the dose taken twice daily in the symptom management of angina pectoris.

Adult↗

PubMed1993

Determination of the beta-adrenergic blocker timolol in plasma by liquid chromatography-atmospheric pressure chemical ionization mass spectrometry.

A method based on LC-MS-MS has been developed for the determination of timolol in plasma using the (CD3)3-labelled species as the internal standard. Timolol is isolated from plasma by a simple solid-phase extraction and converted to its oxazolidin-2-one prior to analysis on a 50 x 4.6 mm reversed-phase high-performance liquid chromatography column packed with SynChropak, C18, 5 microns. The column eluate is passed by means of a heated nebulizer interface into a corona discharge atmospheric pressure chemical ionization source where the analyte and its internal standard are detected using multiple reaction monitoring (MRM). The very high specificity of this technique permits chromatographic run times of less than 2 min. The method has a lower quantifiable limit of 0.5 ng ml-1, with intra- and inter-day relative standard deviations less than 10%, and enables the determination of timolol in plasma after ocular administration to volunteers.

Calibration↗

PubMed2005

Effects of antiglaucoma drugs timolol and GLC756, a novel dopamine D2 agonist and D1 antagonist, on endotoxin-induced-uveitis in rats.

Antiglaucoma drugs with anti-inflammatory properties may be of particular value for the long-term treatment of glaucoma since they may reduce the risk for treatment-related inflammatory processes in outer compartments of the eye. The purpose of this study was, to evaluate the effect of systemic and topical administration of GLC756, a novel mixed dopamine D(2) receptor agonist and D(1) receptor antagonist which lowered intraocular pressure in man, and timolol on endotoxin-induced-uveitis (EIU) in rats. For EIU, 8-week-old Lewis rats received an intravenous injection of 160 microg lipopolysaccharide (LPS) from Salmonella typhimurium. GLC756, timolol, or betamethasone, as positive control, were administered either topically (0.4, 0.5, and 0.1%, respectively, 16-times 20 microl eye drops during 48 hr) or systemically (1 mg kg(-1) subcutaneously for 5 days). Protein content, released TNF-alpha, the number of cells as well as cells expressing TNF-alpha were determined in aqueous humor 48 hr after LPS-injection and served as parameters for inflammation. LPS induced an increase of protein content, infiltrating cells and cells expressing TNF-alpha in the aqueous humor. Topical and systemic administration of GLC756 and betamethasone, almost completely suppressed the increase of protein content and betamethasone in addition also suppressed the number of cells in aqueous humor. In conclusion, the almost complete suppression of LPS-induced protein increase in aqueous humor by GLC756 suggests an additional anti-inflammatory potential of dopaminergic compounds in glaucoma treatment. Timolol did not show any effect on EIU in rats.

Administration, Topical↗

PubMed1984

Reduction of infarct size by the early use of intravenous timolol in acute myocardial infarction. International Collaborative Study Group.

One hundred forty-four patients admitted to the hospital within 4 hours after the onset of symptoms of suspected acute myocardial infarction (AMI) were randomly assigned to either intravenous timolol treatment or to matching placebo. Infarct evolution was assessed by continuous vectorcardiography and CK release. Timolol reduced myocardial ischemia and infarct size as measured by an accelerated reduction in ST-vector magnitude, a significant reduction in maximal cumulative CK release (29.5%) and significantly smaller changes in QRS-vector parameters (20 to 25%). Furthermore, the predicted CK release and maximal QRS-vector change for a given initial ST-vector magnitude was significantly reduced by timolol. The drug regimen also caused a significant reduction in pain and the need for analgesic medication.

Administration, Oral↗

PubMed2000

A comparison of dorzolamide-timolol combination versus the concomitant drugs.

PURPOSE: To compare the intraocular pressure (IOP) lowering effect of fixed combination dorzolamide 2% and timolol 0.5% therapy to that of concomitant administration of a topical beta-blocker and dorzolamide. METHODS: Seventy-four consecutive glaucoma patients were changed from a regimen including a topical beta-blocker and dorzolamide to the fixed combination dorzolamide-timolol in 1 eye, with the other eye used as the control. The average IOP readings before and 1 month after the change were compared. RESULTS: The mean baseline IOP in the entire study population was 19.4 +/- 4.2 mm Hg in the study eyes and 16.9 +/- 4.2 mm Hg in the control eyes. Four weeks after the medication change, the mean IOP was 17.3 +/- 3.9 mm Hg in the study eyes (P <.001) and 16.1 +/- 4.1 mm Hg in the control eyes (P =.02). The difference between the mean IOP change of 2.1 mm Hg in the study eyes and 0.8 mm Hg in the control eyes was found to be statistically significant (P =.01). CONCLUSION: These findings suggest that the fixed combination dorzolamide-timolol therapy achieves additional lowering of the intraocular pressure compared with the concomitant administration of a beta-blocker and dorzolamide.

Adrenergic beta-Antagonists↗

PubMed1981

Separate and combined effects of timolol maleate and acetazolamide in open-angle glaucoma.

We compared the intraocular pressure-decreasing effect of timolol maleate alone, acetazolamide alone, and combined timolol and acetazolamide therapy in nine patients with bilateral chronic open-angle glaucoma. Timolol decreased intraocular pressure at least as effectively as acetazolamide. The two medications together were more effective than either medication alone, but they did not have a fully additive effect. Episcleral venous pressures and outflow facilities did not vary significantly with any of the three treatment regimens.

Acetazolamide↗