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PubMed1999

Central nervous system and plasma lipid profiles associated with carteolol and timolol in postmenopausal black women.

PURPOSE: Among ocular hypotensive agents, intrinsic sympathomimetic activity (ISA) is unique to carteolol hydrochloride. This study was conducted to evaluate the central nervous system (CNS) and plasma lipid profiles associated with timolol maleate and carteolol hydrochloride in postmenopausal black women with primary open-angle glaucoma (POAG) or ocular hypertension. METHODS: One hundred subjects met the inclusion and exclusion criteria for this randomized, double-masked, multicenter, parallel-group study. After completion of informed consent and complete ophthalmic examination, eligible patients entered a washout period, during which no topical ophthalmic medications were used. Blood samples were obtained for hematology and blood chemistry evaluations. Vital signs, ocular symptoms, Symptom Checklist-90-R (SCL-90-R) evaluation, intraocular pressure (IOP) measurements, and slit-lamp examinations were performed before randomization to treatment with either topical carteolol hydrochloride 1.0% or topical timolol maleate 0.5%. Patients received active medications twice daily and were monitored at 4 weeks and 12 weeks. At the conclusion of treatment, vital signs, ocular symptoms, SCL-90-R evaluation, IOP, slit-lamp examinations, and blood samples were obtained. RESULTS: Compared with baseline, high-density lipoprotein (HDL) cholesterol was significantly decreased (worsened) in the timolol group but did not change significantly in the carteolol group. The between-group difference was statistically significant. Total cholesterol to HDL ratio significantly increased (worsened) in the timolol group compared with baseline but did not change in the carteolol group. The difference between groups was statistically significant. No significant differences were observed between groups in SCL-90-R results for either somatization or depression. CONCLUSIONS: These results suggest that topical carteolol hydrochloride may have a more favorable blood lipid profile than topical timolol maleate in postmenopausal black women with POAG or ocular hypertension. Carteolol and timolol appear to have similar CNS side effect profiles.

Adrenergic beta-Antagonists↗
PubMed2000

[A comparison between latanoprost and timolol in treatment of patients with primary open-angle glaucoma and ocular hypertension].

OBJECTIVE: To evaluate the therapeutic value of latanoprost on glaucoma. METHODS: In an open-label fashion, multicenter, randomized control clinical trial, the efficacy and adverse drug reactions of topical application of 0.005% latanoprost once daily were compared with that of 0.5% timolol twice daily for 12 weeks in patients with open-angle glaucoma or ocular hypertension. RESULTS: The study included 128 patients (63 patients in latanoprost group and 65 patients in timolol group) and 117 patients remained at the end of the study (60 cases in latanoprost group and 57 cases in timolol group). Comparing 12 weeks with baseline diurnal intraocular pressure (IOP), the IOP reduction (mean +/- standard deviation) in latanoprost group was (7.5 +/- 0.3) mm Hg (1 mm Hg = 0.133 kPa) (32%, t = 22.73, P < 0.0001) greater than the reduction in timolol group (6.1 +/- 0.3) mm Hg (26%, t = 17.94, P < 0.0001), the difference between the two groups being significant (F = 9.54, P = 0.0026). Two patients treated with timolol and none treated with latanoprost were withdrawn from the study because of inadequate IOP control; 3 patients with latanoprost had foreign body sensation. In latanoprost group, there was one patient whose eyelashes became darker and longer at the last visit (the 12th week). No ocular and systemic adverse events related to the two drugs were found. CONCLUSION: It is demonstrated that 0.005% latanoprost topically applied once daily is well tolerated and more effective in reducing IOP than 0.5% timolol topically applied twice daily. Thus, latanoprost has the potential to be a new first-line antiglaucoma drug.

Adrenergic beta-Antagonists↗
PubMed1992

[Transdermal properties of timolol and factors affecting its permeability in vitro].

V-C horizontal diffusion cell has been used to carry out the initial study of timolol across intact and stripped hairless mouse skin and human cadaver skin. Also, we have systematically studied the effect of some factors such as hydration time, medium pH value as well as various transdermal enhancers on the permeability of timolol in vitro. We investigated the determination method of timolol by RP-HPLC using YWG-C18 column with water-acetonitrile-triethylamine (87:13:1) as the mobile phase. The results indicated the feasibility of transdermal absorption of timolol. The permeabilities of timolol raised significantly with properly extending of hydration time, increasing of medium pH and with presence of various kinds of transdermal enhancers. With 10% propylene glycol and 1% azone were used conjunctly, they showed obviously synergistic effects. All these studies contributed theoretically and practically to the further development and utilization of timolol in the form of transdermal patch.

Administration, Cutaneous↗
PubMed2003

A study of replacement of timolol-pilocarpine with latanoprost in pseudoexfoliation glaucoma.

The aim of the study was to evaluate the efficacy of replacing current dual local therapy (timolol and pilocarpine) with latanoprost 0.005% in 71 pseudoexfoliation glaucoma patients with controlled intraocular pressure (IOP). 39 patients switched to latanoprost 0.005%) and 32 patients continued timolol-pilocarpine therapy. Mean diurnal (IOP) was measured at baseline, after 0.5, 1, 3 and 6 months of treatment. After 6 months 38 patients with latanoprost and 30 patients with timolol-pilocarpine had completed the study. At baseline the mean diurnal IOP was 20.4 +/- 2.0 mmHg for patients in latanoprost treatment group and 21.4 +/- 2.1 mmHg for patients in timolol-pilocarpine group. At the end of the study, after 6 months of treatment, the mean diurnal IOP values were 16.6 +/- 2.4 and 17.9 +/- 2.0 mmHg respectively. IOP was statistically significantly reduced from baseline (p < 0.001). The mean diurnal IOP change from baseline was -3.3 +/- 0.5 mmHg (mean +/- SEM, ANCOVA) for the patients treated with latanoprost and -3.2 +/- 0.4 mmHg for the patients treated with timolol + pilocarpine. This difference in IOP reduction between groups was not statistically significant (z = 0.69; p = 0.49). This study showed that combination therapy (timolol plus pilocarpine) in pseudoexfoliation glaucoma can effectively be replaced by latanoprost monotherapy.

Aged↗
PubMed1991

Improving the ocular to systemic ratio of topical timolol by varying the dosing time.

This study was performed to determine whether the ratio of ocular to systemic absorption of topically applied timolol in the pigmented rabbit can be maximized by varying the time of drop instillation. Twenty-five microliters of 0.65% timolol maleate solutions were instilled into the pigmented rabbit eye at 6 AM, 12 PM, 6 PM, or 12 AM. The time course of timolol concentration in plasma and various eye tissues (conjunctiva, sclera, corneal epithelium, corneal stroma, aqueous humor, iris-ciliary body, and lens) was monitored with the use of reversed phase high-performance liquid chromatography (HPLC). Ocular timolol concentrations were approximately twice as high when the drug was administered at 12 PM than at 6 AM, 6 PM, or 12 AM, whereas timolol concentration in plasma was lowest when the drug was administered at 12 PM. It may, therefore, be possible to maximize the therapeutic index of topically applied timolol by administering the drug at 12 PM. Moreover, the possible influence of dosing time on the extent of ocular and systemic drug absorption must be considered when planning dosing schedules for topically applied ophthalmic drugs.

Absorption↗
PubMed1991

Effect of two weeks of timolol maleate treatment on the normal retinal circulation.

The effect of 2 weeks of topical treatment with timolol maleate 0.5% ophthalmic solution on the retinal circulation was investigated using bidirectional laser Doppler velocimetry and monochromatic fundus photography. Fifteen normal healthy volunteers were included in this study. In a double-masked, randomized design one eye of each received one drop of timolol maleate 0.5% twice daily for 14 days, and the fellow eye received placebo. Vessel diameter (D), maximum erythrocyte velocity (Vmax), and volumetric blood flow rate (Q) were determined in one major retinal vein of each eye before treatment, and then, 2 hr after the instillation of drops on the morning of the 15th day of treatment. After treatment, the average change from baseline in D (+0.7%), Vmax (-8.2%) and Q (-7.7%) were not statistically significant in the placebo-treated eyes. In the timolol-treated eyes, the average increase from baseline in D (+0.1%) and Q (+10%) were not statistically significant. Average Vmax, on the other hand, increased significantly from baseline (P less than 0.05) by 9.6%. In comparison to the placebo-treated eyes, Vmax and Q were significantly increased in the timolol-treated eyes (P less than 0.0005 and P less than 0.01, respectively). These results are similar to those reported previously in a study of the effect of a one-time instillation of timolol and, therefore, suggest that the effect of timolol on the retinal circulation is maintained over a 2-week period.

Administration, Topical↗
PubMed1977

Comparison of the effects of timolol and other adrenergic agents on intraocular pressure in the rabbit.

The effect of timolol, propranolol, epinephrine, and isoproterenol on intraocular pressure (IOP) (measured by tonometry) were compared after topical administration in conscious rabbits. Epinephrine and isoproterenol decreased IOP in normotensive rabbits, whereas propranolol had no effect. Timolol produced only a slight and inconsistent lowering of IOP in normotensive rabbits. All four agents reduced IOP elevated by an oral water load; the adrenergic agonists were substantially more active than the two beta-adrenergic blocking agents. In alpha-chymotrypsin-induced ocular hypertension, epinephrine, isoproterenol, and timolol were essentially equally effective, whereas propranolol exhibited only weak activity. In this latter model, timolol did not lose its effectiveness after multiple instillations (three/day) over an 8-day period. The concentration of timolol in the acqueous humor after topical application of effective hypotensive doses was relatively high as compared to that found in plasma. In addition, topical doses of timolol required to lower IOP were considerably greater than those needed to reduce or block the ocular hypotensive activity of isoproterenol. The mode of action and therapeutic implications of beta-adrenergic blocking agents in glaucoma are discussed.

Adrenergic beta-Antagonists↗
PubMed1979

Modification by timolol of catecholamine stimulation of chloride transport in isolated corneas.

In the isolated frog cornea, 10(-5)M timolol completely blocked the stimulation of chloride transport by 10(-6)M isoproterenol. In this preraration, timolol inconsistently modified the response to epinephrine. In some experiments, epinephrine added to the bathing medium after timolol caused a smaller than normal increase in chloride transport, but in other instances, epinephrine caused a decrease in chloride transport. In the isolated rabbit cornea, 10(-5)M timolol totally blocked the stimulation of chloride transport by 10(-6)M epinephrine. In vivo, topical treatment of rabbit eyes with 0.5% timolol resulted in corneas from these eyes having an inhibited response to epinephrine when incubated in vitro. This inability to stimulate chloride transport persisted for several days following termination of topical treatment with timolol.

Administration, Topical↗
PubMed1985

Timolol-related reduction in mortality and reinfarction in diabetic patients surviving acute myocardial infarction.

The long-term effect of timolol treatment (20 mg daily) on mortality and reinfarction was evaluated in 99 diabetic patients (placebo 46, timolol 53) surviving acute myocardial infarction. During the follow-up period of mean 17 months (12-33 months) there were 13 cardiac deaths in the placebo group and 5 in the timolol group, a reduction of 66.6% (p less than 0.05). The number of non-fatal reinfarctions was 10 in the placebo group and 2 in the timolol group, a reduction of 82.7% (p less than 0.05). The timolol treatment was well tolerated. However, in patients not suffering from diabetes mellitus, long-term timolol treatment was related to a slight increase in new onset diabetes mellitus and in fasting blood sugar levels.

Blood Glucose↗
PubMed1979

[Comparative study between timolol and pilocarpine in the treatment of open-angle glaucoma (author's transl)].

Timolol, a beta-blocker with special influence on aqueous humor production and less influence on outflow facility lowered the intraocular pressure after one single local application for more than 12 hours. Normal diurnal variations of the intraocular pressure were also observed. Fifty open-angle glaucoma patients from the University of Münster, Eye Clinic, took part in a comparative study between Timolol and Pilocarpine. For a period of 17 weeks the patients were given various concentrations of Timolol ophthalmic solution. The continual lowering of the intraocular pressure following Timolol application was noted in 88% of the patients, whereas the rate of success on only 56% could be recorded with Pilocarpine. Side-effects, which for the Pilocarpine-treated patients were very irritating, e. g. miosis with possible night-blindness, accommodation spasms, myopia, etc. were not observed with Timolol. Pupil diameter and pupillary reaction remained unchanged with the application of Timolol. Changes of blood pressure and pulse were not evident. A detrimental influence on the corneal transparency could not be observed in any patient.

Double-Blind Method↗
PubMed1983

The Norwegian Multicenter Study of Timolol after Myocardial Infarction.

In this study, 1884 patients who were selected from 3647 consecutive patients who survived at least 6 days after an acute myocardial infarction were randomized to double-blind treatment with either placebo or timolol and followed for 12-33 months. One hundred fifty-two patients in the placebo group and 98 in the timolol group died. The life-table cumulative probability of total death was 21.9% in the placebo group and 13.3% in the timolol group, corresponding to a relative reduction of 39.4% (p = 0.0003). One hundred thirty-one nonfatal reinfarctions were confirmed in the placebo group and 90 were confirmed in the timolol group, including events among withdrawn patients. The life-table probability rate of reinfarction was 16.4% in the placebo and 11.8% in the timolol group (p = 0.001). We conclude that chronic treatment with timolol in survivors of acute myocardial infarction who can tolerate beta-adrenergic blockade is effective in reducing both total mortality and reinfarction over 33 months.

Adult↗
PubMed1981

[Timolol reduces mortality and reinfarct in patients surviving an acute myocardial infarct. The Norwegian Multicenter Study Group].

A multicenter double-blind randomized study was carried out to compare the effect of timolol (10 mg twice daily) with that of placebo in patients surviving acute myocardial infarction. Treatment was started seven to 28 days after infarction in 1884 patients (945 taking timolol, and 939 placebo), who represented 52 per cent of those evaluated for entry; the patients were followed for 12 to 33 months (mean, 17). There were 152 deaths in the placebo group and 98 in the timolol group. When deaths that occurred during treatment or within 28 days of withdrawal were considered, the cumulated sudden-death rate over 33 months was 13.9 per cent in the placebo group and 7.7 per cent in the timolol group--a reduction of 44.6 per cent (P = 0.0001). The cumulated reinfarction rate was 20.1 per cent in the placebo group and 14.4 per cent in the timolol group (P = 0.0006). We conclude that long-term treatment with timolol in patients surviving acute myocardial infarction reduces mortality and the rate of reinfarction.

Acute Disease↗
PubMed1980

[Experiences in a double-blind study with different concentrations of timolol and pilocarpine (author's transl)].

Fifty patients with chronic open-angle glaucoma were studied in a double-blind study with Timolol ophthalmic solution, in a concentration of 0.1%, 0.2% and 0.5%, and Pilocarpine eye drops 1%, 2% and 4% over a period of seventeen weeks. Timolol was instilled twice daily into the conjunctival sack, or Pilocarpine four times daily. The results of the investigations may be summarised as follows: Timolol (0.1%-0.5%) achieved a mode-rate reduction in I.O.P. of 29%, compared to a 10.3% drop with Pilocarpine (1%-4%). Under treatment with Timolol, there was a statistically significant reduction in pulse rate of 12%, also a slight drop in blood-pressure of 3.5% systolic and 2.5% diastolic. During this study, those treated with Timolol showed no statistical changes of visual acuity, visual field, or on slit lamp examination and ophthalmoscopy of the optic disk and retina. The average pupillary diameter and tear flow (Schirmer Test), were little changed in the group of patients treated with Timolol, whereas in the Pilocarpine group, the size of the pupil decreased by 30.5% as expected.

Adult↗
PubMedDate not supplied

Effects of D-timolol on intraocular pressure, heart rate, cardiac contractility, and tracheal muscle function.

Introduction of L-timolol maleate into the clinics for glaucoma treatment has been a great success as it produces relatively few side effects, such as miosis, ciliary spasm and headache, which are associated with the use of pilocarpine. Recent reports indicated, however, that L-timolol produces asthmatic attacks, cardiovascular suppression and central depression. D-Timolol was found to be as effective as L-timolol in lowering the intraocular pressure and aqueous humor production. However it was much less potent than L-timolol in inhibiting cardiac contractility and heart rate stimulated by isoproterenol and was less active in blocking beta-adrenergic receptors in tracheal muscle. It is suggested that the D-isomer of timolol could be used to treat glaucoma instead of L-isomer without producing untoward side effects in cardiovascular and bronchial tissues.

Animals↗
PubMed1993

The analysis of plasma kinetics and beta-receptor binding and -blocking activity of timolol following its small intravenous dose.

Plasma kinetics and beta-receptor blocking and -binding activity of timolol was studied in six healthy volunteers following its intravenous 0.25 mg dose. Timolol concentrations were measured using radioreceptor assay (RRA), blocking activity by comparing the dose ratios (DRs) of the infusion rates of isoprenaline required to increase heart rate by 25 bpm (I25) and binding activity by determining the extent to which timolol occupied beta 1-receptors of rabbit lung and beta 2-receptors of rat reticulocytes in undiluted plasma samples. Timolol was eliminated from plasma with a mean half-life for the elimination phase of 2.6 hours. The dose antagonized potently isoprenaline-induced tachycardia at least for four hours. The effect was excellently correlated with the estimated beta 2-receptor binding activity of timolol in the circulating plasma. In conclusion, the small intravenous timolol dose was eliminated from plasma by a fashion, which was very similar to its eighty-fold higher oral doses reported earlier in the literature. The 0.25 mg dose was of considerable systemic beta-receptor blocking and -binding activity, that may help to explain its reported side-effects following ocular drug administration. The extent to which beta-blocking agents occupy rabbit lung beta 1- and rat reticulocyte beta 2-receptors in the circulation appears to predict the intensity and selectivity of their beta-blocking effects in healthy volunteers.

Adrenergic beta-Antagonists↗
PubMed1993

Double-masked comparative study of UF-021 and timolol ophthalmic solutions in patients with primary open-angle glaucoma or ocular hypertension.

A double-masked comparative clinical study of UF-021 (Rescula), a unique prostaglandin-related compound, was carried out at 18 centers with timolol maleate 0.5% ophthalmic solution as an active reference drug. After a wash-out period, UF-021 (0.12%) or timolol (0.5%) was given topically twice a day for 12 weeks to 158 patients with primary open-angle glaucoma or ocular hypertension, in a randomized double-masked manner. Both groups showed a significant reduction in intraocular pressure from the second week to the end of the study. In overall improvement rating, 91.4% of the cases (64/70) in the UF-021 group and 88.3% (68/77) in the timolol group were judged to be "Extremely improved" or "Improved". Five and 4 cases reported having side effects in the UF-021 and timolol groups, respectively, but none of the cases required any change or discontinuation of treatment. While UF-021 did not affect blood pressure, both systolic and diastolic blood pressures in the timolol group were significantly decreased. These results suggest that UF-021 (0.12%) has the potential to lower intraocular pressure equivalent to timolol (0.5%), while having no effect on cardiovascular functions.

Administration, Topical↗
PubMed1998

Bioavailability of timolol and aceclidine after ocular instillation in the rabbit.

The bioavailability of timolol and aceclidine after the ocular instillation of each drug (timolol 0.5% or aceclidine 2%) or both combined (timolol 0.5% + aceclidine 2%) has been evaluated in rabbits. 15 male albino rabbits were treated by the instillation of timolol and aceclidine alone or combined in the conjunctival sac of the right eye. Timolol concentrations in humor aqueous were assayed at 10 min, 30 min, 1 hr, 2 hr, 4 hr and 6 hr after instillation by high-performance liquid chromatography (HPLC). Aceclidine was assayed by a pharmacodynamic method: pupillary diameter at the following time intervals 0 (basal value), 1 min, 5 min, 30 min, 1 hr, 2 hr, 4 hr, 6 hr after treatment. Our results demonstrated that no differences in timolol and aceclidine bioavailability were found between simple-drug preparations and their combination.

Administration, Topical↗
PubMed1998

The efficacy and safety of dorzolamide as adjunctive therapy to timolol maleate gellan solution in patients with elevated intraocular pressure. Additivity Study Group.

PURPOSE: Two parallel, randomized, double-masked, placebo-controlled studies were conducted to assess the efficacy and safety of 2% dorzolamide hydrochloride as adjunctive therapy to 0.5% timolol maleate ophthalmic gellan (gel-forming) solution in patients with elevated intraocular pressure (IOP) that was inadequately controlled with 0.5% timolol maleate gellan solution alone. METHODS: Both studies began with an open-label 2-week run-in period on 0.5% timolol maleate gellan solution once a day. The only variation in method between the two studies was the dosage of 2% dorzolamide. In one study, 202 patients received 0.5% timolol maleate gellan solution once daily plus either 2% dorzolamide or placebo three times daily. In the other study, 181 patients received 0.5% timolol maleate gellan solution once daily plus either 2% dorzolamide or placebo twice daily. RESULTS: After 85 days, additional mean percent reductions in IOP from baseline at morning trough for the groups receiving 2% dorzolamide three times daily and placebo three times daily were 12.5% and 8.4%, respectively. Mean percent reductions for the groups receiving 2% dorzolamide twice daily and placebo twice daily were 13.1% and 6.5%, respectively. Burning and/or stinging on instillation were the only adverse experiences that affected significantly more of the patients receiving 2% dorzolamide twice or three times daily than those receiving placebo. CONCLUSION: When administered concomitantly with 0.5% timolol maleate gellan solution, 2% dorzolamide three times daily or twice daily produced a statistically significant reduction in IOP at morning trough and peak and was generally well tolerated.

Adrenergic beta-Antagonists↗