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At least 739 records · Page 41Linked to original sources

PubMed1985

Levobunolol vs timolol for open-angle glaucoma and ocular hypertension.

A group of 162 patients with chronic open-angle glaucoma or ocular hypertension were treated twice daily for up to 15 months with one of the following topical ophthalmic solutions: 0.5% levobunolol, 1% levobunolol, or 0.5% timolol. Overall mean reductions in intraocular pressure were 8 mm Hg for patients receiving 0.5% levobunolol or timolol and 8.2 mm Hg for patients receiving 1% levobunolol. There were no significant differences between levobunolol and timolol in mean reductions in intraocular pressure, percent of patients with adequately controlled intraocular pressure, or life-table estimates of the probability of successful treatment.

Clinical Trials as Topic↗

PubMed1991

Influence of betaxolol and timolol on the visual fields of patients with glaucoma.

In a double-masked study, 40 patients with primary open-angle glaucoma were randomly assigned to treatment with betaxolol 0.5% or timolol 0.5% in both eyes twice daily. Visual fields and intraocular pressures were studied. Perimetry was performed with the Octopus G1 program two weeks after a washout period and three, six, 12, and 18 months after initiation of treatment. Both drugs reduced intraocular pressure. The reduction in intraocular pressure in the timolol-treated group was more pronounced than that in the betaxolol-treated group; the difference, however, was not statistically significant. In both treatment groups, the visual fields tended to improve during the first six months of treatment and remained stable or tended to deteriorate thereafter. The treatment effect on the visual field was better in the betaxolol-treated group than it was in the timolol-treated group (P = .041).

Aged↗

PubMed1992

Therapeutic index of pilocarpine, carbachol, and timolol with nasolacrimal occlusion.

We assessed the effect of nasolacrimal occlusion on the therapeutic index of various antiglaucoma medications in healthy volunteers and patients with glaucoma. Nasolacrimal occlusion used with pilocarpine 2% every 12 hours gave the maximal ocular hypotensive response. Carbachol 1.5% every 12 hours with nasolacrimal occlusion gave the maximal response for this drug. For timolol, nasolacrimal occlusion collapsed the dose-response curve and extended the duration of action. A final trial of carbachol added to timolol with nasolacrimal occlusion showed that timolol 0.25% and carbachol 1.5% every 12 hours gave the maximal response for this combination. Our findings suggest that most of the commercially used ocular hypotensive agents can achieve the same maximal effect with lower concentrations and less frequent administration (never exceeding every 12 hours) than are currently recommended should nasolacrimal occlusion be performed. Furthermore, nasolacrimal occlusion should markedly decrease the systemic absorption of topical ocular drugs and lessen the chance of systemic side effects.

Absorption↗

PubMedDate not supplied

Effect of topical latanoprost-timolol combined therapy on retinal blood flow and circulation of optic nerve head tissue in cynomolgus monkeys.

PURPOSE: To evaluate the effects of topical latanoprost and timolol in combined therapy on retinal blood flow and tissue circulation in the optic nerve head (ONH) of the cynomolgus monkey. METHODS: Latanoprost (30 microL, 0.005%) was instilled once daily and timolol (30 microL, 0.5%) twice daily for 6 days into 1 eye, and physiological saline into the other eye to serve as control. Blood velocity through retinal veins was determined using Kowa Laser Speckle Blood Flow Meter. The ONH tissue blood velocity (NB(ONH)) was determined using the Laser Speckle Tissue Circulation Analyzer. Retinal blood flow and NB(ONH) determinations were carried out before the first instillation and 4 hours after the first instillation on the 2nd experimental day, and the last instillation at the same sites at the same time of day. The intraocular pressure (IOP) was also measured periodically. RESULTS: After the first instillation, on the 2nd experimental day, the retinal blood flow decreased compared with the baseline, but 6-day instillation caused no significant change from the baseline. Six-day instillation increased the NB(ONH) in the treated eyes by 10% from the baseline and by 7% from that in the fellow control eye. After 6-day instillation, the IOP was lowered by 7.8+/-2.7 mm Hg and 3.6+/-4.3 mm Hg in the treated and control eyes, respectively. CONCLUSIONS: Combined 6-day instillation of latanoprost once daily and timolol twice daily has no significant effect on the retinal blood flow, but significantly increases the ONH tissue blood velocity in monkey eyes. Jpn J Opthalmol 2000;44:227-234

Animals↗

PubMed1999

Periocular accumulation of timolol and betaxolol in glaucoma patients under long-term therapy.

PURPOSE: To determine if betaxolol or timolol is present in measurable concentration in the Tenon capsule in patients under long-term topical therapy. METHODS: Small (1-cc) specimens of Tenon capsule were removed at the time of filtering surgery from 15 glaucoma patients under long-term preoperative topical therapy, nine of whom had been treated with timolol and six of whom had been receiving betaxolol. Methanol extracts of these tissue samples were analyzed quantitatively for the presence of either beta-adrenergic antagonist by high-performance liquid chromatography. RESULTS: Drug was detected in every specimen. A mean total of 2.6 (range, 0.1-30.0) microg of betaxolol was detected per 1-cc specimen. CONCLUSION: Timolol and betaxolol penetrate the conjunctiva and accumulate in the Tenon capsule. In patients under long-term therapy, the periocular tissue can accumulate a greater quantity of beta-antagonist than is present in a daily dosage of applied eyedrops, manyfold higher than the maximal intraocular concentration.

Adrenergic beta-Antagonists↗

PubMed2004

Comparison of latanoprost with fixed-combination dorzolamide and timolol in adult patients with elevated intraocular pressure: an eight-week, randomized, open-label, parallel-group, multicenter study in Latin America.

BACKGROUND: The newer ocular hypotensive agents available to treat glaucoma and ocular hypertension (OHT) include latanoprost, a prostaglandin F(2alpha) analogue, and the fixed combination of dorzolamide hydrochloride, a carbonic anhydrase inhibitor, and timolol maleate, a beta-blocker. OBJECTIVE: The aim of this study was to compare the efficacy and tolerability of latanoprost with that of the fixed combination of dorzolamide and timolol over 8 weeks. METHODS: This interventional, 8-week, randomized, open-label, parallel-group study was conducted at 18 centers in 6 Latin American countries. Patients with unilateral or bilateral primary open-angle, pigmentary, or exfoliative glaucoma or OHT were randomized to receive latanoprost, 1 drop in the affected eye QD (evening), or fixed-combination dorzolamide/timolol, 1 drop in the affected eye BID (morning and evening). Medications were self-administered, 1 drop per affected eye. At baseline and week 8, intraocular pressure (IOP) was measured 3 times each at 8:30 am, 10:00 am, 2:00 pm, and 5:00 pm and after the water-drinking test, which estimates the IOP peak of diurnal tension curve, performed following the 5:00 pm IOP assessment. The primary efficacy outcome was change in diurnal IOP (the mean of IOP measurements) from baseline to week 8. Adverse effect (AE) data were recorded at each visit. RESULTS: A total of 229 patients were randomized (latanoprost, n = 112; dorzolamide/timolol, n = 117). Mean baseline diurnal IOP values were similar between the 2 groups. Mean (SD) diurnal IOP reductions at week 8 before the water-drinking test were 6.9 (3.0) mm Hg for the latanoprost group and 6.4 (3.2) mm Hg for the dorzolamide/timolol group. Mean IOP values were similar at all time points except at 5:00 pm, when levels were significantly lower in latanoprost-treated patients (P = 0.025). After the water-drinking test, the increase in IOP values was similar between groups at baseline but lower in latanoprost-treated patients at week 8 (adjusted difference, 1.08 mm Hg; P = 0.012). Fewer patients treated with latanoprost reported ocular or systemic AEs (P = 0.025 and P < 0.001, respectively). CONCLUSIONS: In this study of patients with unilateral or bilateral primary open-angle, pigmentary, or exfoliative glaucoma or OHT IOP reductions generally were similar between treatment groups, except at 5:00 pm, when the mean IOP level was significantly lower in latanoprost-treated patients. Latanoprost was better tolerated than fixed-combination dorzolamide and timolol.

Adult↗

PubMed1993

Comparison of apraclonidine and timolol in chronic open-angle glaucoma. A three-month study.

PURPOSE: To compare the safety and efficacy of apraclonidine ophthalmic solution 0.25% and 0.5% (both given 3 times daily) to timolol maleate (0.5%) given twice daily, in primary open-angle glaucoma or ocular hypertension. METHODS: This study was a 90-day prospective, multicenter, double-masked, randomized, parallel group trial. Intraocular pressure (IOP) measurements were made between 8:00 and 10:00 AM before the morning dose (i.e., up to 12 hours after the evening dose of glaucoma medication) and at 4:00 PM (i.e., 8 hours after the morning dose of glaucoma medication). Patients with off-therapy IOP of greater than 22 mmHg and less than 35 mmHg were entered into the study and were assessed 14, 30, and 90 days after treatment. RESULTS: Sixty-nine patients were enrolled; there were no significant demographic differences among the three study groups. All three treatments significantly reduced IOP over 90 days (P < 0.011). For apraclonidine 0.5%, IOP reductions from 25.8 +/- 3.2 mmHg (pretreatment) to 20.4 +/- 4.00 mmHg (day 90) were observed; for apraclonidine 0.25%, from 25.7 +/- 3.05 mmHg (pretreatment) to 22.1 +/- 4.24 mmHg (day 90); and for timolol 0.5% from 26.1 +/- 3.79 mmHg to 21.1 +/- 5.91 mmHg (day 90). The 90-day period of therapy was completed by 12 patients treated with apraclonidine 0.5%, 21 patients treated with apraclonidine 0.25%, and 23 patients treated with timolol 0.5%. There were no serious adverse events. Fourteen of 22 patients (0.5% apraclonidine) and 21 of 23 patients (0.25% apraclonidine) tolerated the drug well; ocular allergy developed in the remaining patients treated with apraclonidine, which resolved upon discontinuation. CONCLUSIONS: Apraclonidine effectively lowers IOP associated with open-angle glaucoma or ocular hypertension; these pilot results will need to be confirmed by a larger pivotal study. Long-term therapy for some patients may be inhibited by ocular allergy for which there was a higher incidence to the 0.5% apraclonidine solution than to the 0.25% solution in this study. Apraclonidine may be of value as an additional therapy for open-angle glaucoma in selected patients.

Adult↗

PubMed1979

Timolol: its effectiveness in different types of glaucoma.

A study is presented on the effectiveness of timolol maleate in the treatment of 76 cases of various types of glaucoma. Timolol lowered intraocular pressure significantly in almost every diagnostic category, although there was marked variability within the diagnostic categories themselves. The therapeutic trial approach is suggested as an aid in selecting persons who will respond adequately to timolol drops.

Glaucoma↗

PubMed1981

Timolol and pediatric glaucomas.

Thirty-eight eyes were treated by adding timolol to the medical regimen. After a suitable trial, attempts were made to reduce other glaucoma medications. Fifteen eyes with infantile glaucoma treated surgically at birth, experienced elevated intraocular pressure later in life. Another 15 eyes had glaucoma associated with congenital anomalies such as aniridia, Sturge-Weber syndrome, and mesodermal malformations. The group with infantile glaucoma demonstrated an average drop in pressure of 24% and 22% after one and three months, respectively. Six of the 15 eyes were controlled at 22 mm Hg or less. In the other group, intraocular pressure fell 30% after one month and 12% after three months. Five of the 15 eyes were controlled. Adverse effects occurred in five patients, timolol therapy was discontinued in two (7%). The IOP was not controlled in any of the eyes with timolol alone.

Adolescent↗

PubMed1989

Adjunctive glaucoma therapy. A comparison of apraclonidine to dipivefrin when added to timolol maleate.

The authors compared the additive intraocular pressure (IOP)-lowering effects of two different topical medications, apraclonidine hydrochloride and dipivefrin hydrochloride, when used in conjunction with timolol maleate. Eighteen patients with elevated IOPs entered a randomized, double-masked, cross-over study. Each used apraclonidine 1.0%, dipivefrin 0.1%, or placebo, twice daily for 3 weeks each, in addition to timolol 0.5% twice daily. Only apraclonidine produced a significant additional IOP lowering over timolol treatment alone at all time intervals (P less than 0.001). Its additive effect was significantly greater than that seen with dipivefrin at all time intervals (P less than 0.01), with the exception of day 22 (P = 0.061). No significant change in pulse rate or blood pressure was seen during apraclonidine administration. Apraclonidine may be a useful adjunctive agent in patients with poorly controlled glaucoma.

Adult↗

PubMed2000

Comparison of the efficacy of betaxolol-brinzolamide and timolol-dorzolamide as suppressors of aqueous humor flow in human subjects.

OBJECTIVE: To compare the efficacy of combinations of betaxolol-brinzolamide and timolol-dorzolamide as suppressors of aqueous humor flow and ocular hypotensive agents. DESIGN: Placebo-controlled, masked comparison of the two drug combinations. PARTICIPANTS: Twenty-five normal human volunteers with the fellow eye serving as control. METHODS OR TESTING: Fluorophotometric measurement of aqueous humor flow and pneumatonometric measurement of intraocular pressure. MAIN OUTCOME MEASURES: Aqueous humor flow and intraocular pressure. RESULTS: The betaxolol-brinzolamide combination lowered aqueous flow 39% to 44%, and the timololdorzolamide combination lowered aqueous flow 51%. The betaxolol-brinzolamide combination lowered intraocular pressure 14% to 19%, and the timolol-dorzolamide combination lowered it 18% to 24%. CONCLUSIONS: Both drug combinations were effective; the timolol-dorzolamide combination appeared to be the more effective of the two after short-term exposure (24 hours).

Adrenergic beta-Antagonists↗

PubMed2003

Transdermal delivery of timolol and atenolol using electroporation and iontophoresis in combination: a mechanistic approach.

PURPOSE: The purpose of this work was to study the effect of electroporation on iontophoretic transport of two beta-blockers, timolol (lipophilic) and atenolol (hydrophilic), and to have a better understanding of the mechanism of combination. METHODS: The transdermal delivery of these beta-blockers through human stratum corneum was studied in three-compartment diffusion cells. The transport of mannitol was evaluated to assess the electroosmotic flow. RESULTS: The iontophoretic transport of timolol was decreased by electroporation because the high accumulation of the lipophilic cation timolol in the stratum corneum resulted in a decrease of electroosmosis. In contrast, electroosmosis was not affected by atenolol, and the iontophoretic transport of atenolol was increased by electroporation. CONCLUSIONS: Using two different beta-blockers, we showed that lipophilicity and positive charges affect the electrotransport of drugs. Understanding the effect of the physicochemical properties of the drug, as well as the electrical parameters, is thus essential for the optimization of transdermal drug delivery by a combination of electroporation and iontophoresis.

Administration, Cutaneous↗

PubMed1985

Pharmacokinetics and beta-blocking effects of timolol in poor and extensive metabolizers of debrisoquin.

We studied the pharmacokinetics and beta-blocking effects of a single, oral 20 mg dose of timolol in six poor metabolizers (PMs) and six extensive metabolizers (EMs) of debrisoquin. The plasma timolol concentration was significantly higher in PMs than in EMs. There was a fourfold difference in mean AUC (1590 +/- 1133 vs. 394 +/- 239 ng X hr/ml; P less than 0.01) and a twofold difference in mean t1/2 (7.5 +/- 3 vs. 3.7 +/- 1.7 hours; P less than 0.01), reflecting differences in oral clearance (13.1 +/- 7.8 vs. 48.5 +/- 23.2 L/hr; P less than 0.01). The degree of beta-blockade was greater in PMs than in EMs at 12 hours (30.9% vs. 18.2%; P less than 0.05) and at 24 hours (28.3% vs. 13.1%; P less than 0.05). In the group as a whole the metabolic ratio correlated positively with both kinetic data and beta-blockade, but some overlap was observed. Hence timolol metabolism appears to be subject to debrisoquin-type polymorphism, which results in interphenotypic variation in plasma concentration and beta-blocking effect.

Absorption↗

PubMed1989

Timolol-induced up-regulation of polymorphonuclear leukocyte beta 2-adrenergic receptors in the elderly.

Drug-induced up-regulation of beta-adrenergic receptors is impaired in the brains of aged rats but not in myocardia. To investigate age-related changes in receptor regulation in human beings, young (24 to 35 years of age) and elderly (62 to 78 years of age) healthy volunteers were treated with the beta-adrenergic receptor blocking agent timolol maleate (10 mg b.i.d.) for 8 days. Baseline densities of beta 2-adrenergic receptors on polymorphonuclear leukocyte (PMNL) membranes and heart rates were the same in the two age groups. However, systolic blood pressures were higher in the elderly subjects. Administration of timolol produced similar plasma levels in the two groups. In response to timolol, the density of PMNL beta-adrenergic receptors increased at a similar rate and to the same extent (threefold) in both age groups. Likewise, hemodynamic changes were not related to age. These results suggest that up-regulation of peripheral beta 2-adrenergic receptors in human beings is not impaired with aging.

Adult↗

PubMed1994

Clinical experience with a fixed dose combination therapy of timolol and pilocarpine used twice daily in the management of chronic open angle glaucoma.

Twenty-five eyes of 25 patients with primary chronic open angle glaucoma deemed controlled for 12 months were converted from timolol 0.25% or 0.5% b.d. and pilocarpine 2% q.i.d. to a combination drop (TP2) of combined timolol 0.5% and pilocarpine 2% given b.d. Mean intraocular pressures (IOP) were 18.68 +/- 2.84 mmHg at 1 month, 18.81 +/- 2.56 mmHg at 3 months and 18.56 +/- 2.01 mmHg at 6 months. These values were significantly higher than the initial IOP of 17.48 +/- 2.2 mmHg (p values 0.0006, 0.0001 and 0.0004 respectively). However, 1 month following reconversion to initial therapy the IOP was 17.68 +/- 2.67 mmHg, which was not significantly higher than the initial IOP (p = 0.46). In addition, of 8 eyes uncontrolled during the course of the study, 6 became controlled following reconversion to initial treatment. Combination therapy of TP2 b.d. cannot be recommended to control IOP satisfactorily in patients maintained on timolol 0.25% or 0.5% b.d. and pilocarpine 2% q.i.d.

Aged↗

PubMed1998

Compliance with timolol treatment in glaucoma.

PURPOSE: To assess levels of compliance in elderly patients on timolol eyedrops for glaucoma. METHODS: A postal questionnaire was sent from the general practitioner to 86 patients over 55 years of age on repeat prescriptions for timolol eyedrops. The questionnaire asked details about the duration of treatment, family history, the level of understanding of the disease and the importance of treatment, other regular medication, side-effects attributed to the drops and how often patients omitted their drops. A search of practice and local hospital dispensing data was carried out to assess how frequently monthly repeat prescriptions for timolol eyedrops were dispensed over a 12 month period. This allowed a total volume to be calculated for each patient. RESULTS: Twenty-four per cent of patients admitted to omitting eyedrops either occasionally or frequently. Fifty-one per cent were found to have had insufficient drops dispensed to comply with treatment as prescribed. In non-complaint patients the mean period without drops was 85 days of the year, with a maximum of 165 days. CONCLUSION: Compliance with treatment is poor and patients underestimate their level of defaulting when questioned.

Aged↗

PubMed2005

A 6-month assessment of bimatoprost 0.03% vs timolol maleate 0.5%: hypotensive efficacy, macular thickness and flare in ocular-hypertensive and glaucoma patients.

AIM: To compare 6 months of treatment with bimatoprost and timolol in terms of their hypotensive efficacy and secondary effects, including changes in macular thickness and the inflammatory reaction induced in the anterior chamber. METHODS: A prospective, randomized, parallel-group trial performed on 30 eyes of 30 patients per group. The main outcome measure was the difference between the IOP value taken between the baseline visit and the 6-month-visit. Macular thickness determined through optical coherence tomography and anterior chamber inflammation estimated using the laser flare meter was also evaluated. Adverse events were recorded during the study period. RESULTS: Bimatoprost treatment gave rise to a significantly lower mean IOP than timolol in all follow-up visits as from the first month (P<0.05). Bimatoprost achieved high percentage IOP reductions from baseline in a significantly higher proportion of patients (P<0.05). Macular thickness and anterior chamber flare failed to vary significantly both between the two groups and within each group during the 6-month evaluation (P>0.05). CONCLUSIONS: Bimatoprost 0.03% once daily showed a greater efficacy then timolol 0.05% twice daily in patients with elevated IOP. No significant differences were detected in macular thickness or anterior uveitis using optical coherence tomography and laser flare photometry.

Adult↗

PubMed1989

Interaction of naloxone and timolol on maximal exercise capacity and the subjective perception of fatigue.

The effect on exercise performance and on the subjective perception of fatigue of the opioid receptor blocker naloxone, the nonselective beta-blocker timolol, and the combination of these two was studied in a double-blind randomized cycle ergometry test in healthy young men. Cumulative work at exhaustion was reduced by 25% after timolol (P less than 0.002) and by 34% after naloxone/timolol (P less than 0.02) but not after naloxone, compared with placebo. Naloxone alone had no influence on the subjective perception of fatigue (Borg scale rating), but significantly higher ratings were obtained by timolol and by naloxone/timolol. The present study does not support the hypothesis that opioid peptides are of importance for maximal exercise capacity and subjective perception of fatigue during short-term dynamic exercise in healthy young men.

Adult↗