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PubMed1998

Comparison of the safety and efficacy of the fixed combination of dorzolamide/timolol and the concomitant administration of dorzolamide and timolol: a clinical equivalence study. International Clinical Equivalence Study Group.

AIMS: To compare the tolerability and efficacy of a fixed combination solution of dorzolamide/timolol (Cosopt), administered twice daily with the concomitant administration of its components, dorzolamide (Trusopt) twice daily and timolol (Timoptic) twice daily. METHODS: After a 2 week timolol run in, patients with open angle glaucoma or ocular hypertension were randomised (1:1) to receive treatment with either the dorzolamide/timolol combination solution twice daily (combination) or the dorzolamide solution twice daily plus timolol maleate solution twice daily (concomitant) for 3 months. RESULTS: 299 patients were entered and 290 patients completed the study. Compared with the timolol baseline, additional IOP lowering of 16% was observed at trough (hour 0) and 22% at peak (hour 2) at month 3 in both the concomitant and combination groups. The IOP lowering effects of the two treatment groups were clinically and statistically equivalent as demonstrated by the extremely small point differences (concomitant--combination) observed in this study--0.01 mm Hg at trough and 0.08 mm Hg at peak. The safety variables of the concomitant and combination groups were very similar. Both combination and concomitant therapy were well tolerated and few patients discontinued due to adverse effects. CONCLUSIONS: The dorzolamide/timolol combination solution administered twice daily is equivalent in efficacy and has a similar safety profile to the concomitant administration of the components administered twice daily.

Adult↗

PubMed1987

Fever after acute myocardial infarction in patients treated with intravenous timolol or placebo.

Body temperature was studied in 65 patients admitted to hospital within four hours of the onset of symptoms of acute myocardial infarction. Thirty three patients had been randomly assigned to intravenous timolol treatment and 32 to placebo treatment. Infarct evolution was assessed by continuous vectorcardiography and creatine kinase release. Maximum and mean temperatures during the first eight days were significantly lower in the timolol group, who were discharged from hospital one day earlier. Eight patients in the placebo group had temperatures of greater than 39 degrees compared with one in the timolol group. Both the mean temperature and the maximum temperature correlated significantly with indices of infarct size and ischaemic area as estimated by cumulative creatine kinase release, QRS vector difference, and ST vector magnitude. The results were consistent with the view that reduction of infarct size may partly explain the reduced pyrexial response after timolol treatment. Other mechanisms are probably also involved in larger infarcts. Because high fever has detrimental haemodynamic effects in acute myocardial infarction, reduction of this response may be beneficial. The results support the early use of beta adrenoceptor blockade in acute myocardial infarction.

Body Temperature↗

PubMed1981

Effects of timolol and atenolol on benign essential tremor: placebo-controlled studies based on quantitative tremor recording.

Two different beta-adrenoreceptor antagonists, atenolol and timolol, were separately compared with a placebo in the suppression of essential tremor. In two-week single-blind placebo-controlled studies with cross-over, timolol (5 mg twice daily) and atenolol (100 mg once daily) produced an equal reduction in sitting heart rate and sitting blood pressure. Timolol was effective in reducing tremor while atenolol failed to reduce tremor amplitude. These results indicate that essential tremor can be reduced but not blocked, by the adrenergic blocker timolol with both beta 1 and beta 2 blocking properties; but not by the relatively selective beta 1 blocking drug atenolol. Possibly, the tremor reduction is medicated by a peripheral effect on beta 2 adrenoreceptors.

Adult↗

PubMed1990

Effects of timolol, indomethacin, and MK-571 on bronchoconstriction to infused leukotriene D4 in guinea pigs.

Continuous intravenous infusions of leukotriene D4 produced a prolonged but variable bronchoconstriction (approximately a 200% increase in lung resistance (RL) and a 50% decrease in dynamic compliance (Cdyn] in anesthetized and paralysed guinea pigs that peaked within 1-1.5 min and was followed by a somewhat smaller secondary plateau response. The overall response was delayed (time to peaks) but not significantly reduced by pretreatment with the cyclooxygenase inhibitor indomethacin (1 mg/kg), was markedly potentiated by the beta-adrenoceptor antagonist timolol (5 micrograms/kg), and was partially and completely blocked by pretreatment with 0.1 and 1.0 mg/kg, respectively, of the leukotriene D4 receptor antagonist MK-571. MK-571 prevented the response in indomethacin-treated guinea pigs but was considerably more active at preventing and reversing the potentiated responses (lower dose of leukotriene D4) in animals treated with indomethacin and timolol. Additional studies in indomethacin- and timolol-treated animals demonstrated that MK-571 was active with good duration of action by the aerosol route of administration (30 min and 4 h pretreatment). The technique of infusing leukotrienes into untreated, indomethacin-treated, and indomethacin- and timolol-treated guinea pigs is a useful method to study the action and interaction of leukotriene receptor antagonists.

Aerosols↗

PubMed2000

Oxygen-induced retinopathy in the newborn rat: morphological and immunohistological findings in animals treated with topical timolol maleate.

Oxygen-induced retinopathy (OIR) similar to that seen in premature infants can be produced in newborn rats by exposure to 80% oxygen for the first 5 days of life, with subsequent recovery for 7 days in a room air environment. Previous studies have shown that the latter phase is associated with degeneration of retinal astrocytes. In the absence of astrocytes, the vascular endothelial growth factor (VEGF) is produced by the neurons of the inner retina. In this study, immunohistochemical methods were used to assess retinal expression of VEGF protein in ratlings exposed to the above protocol, with and without simultaneous treatment with topical timolol maleate. Intraocular pressure (IOP) and arterial pressure were measured. The severity of OIR was also evaluated in retinal flat mounts after India ink perfusion. The mean IOP was 8.25 +/- 0.32 mm Hg in untreated ratlings and 5.15 +/- 0.24 mm Hg in timolol-treated animals. OIR in retinas from the timolol group was less severe than that seen in untreated ratlings. VEGF protein expression was almost completely absent in the latter group. Retinas from timolol-treated animals expressed VEGF protein, though the level was inferior to that found in controls raised under room air conditions. In conclusion, these data seem to indicate that experimental OIR can be attenuated by a reduction of the IOP during and after oxygen supplementation. It is possible that these effects are due to improved ocular perfusion pressure, which would mitigate the hypoxic insult to the retina during the room air recovery period.

Administration, Topical↗

PubMed1997

Effect of timolol and UF-021 (a prostaglandin-related compound) on pulsatile ocular blood flow in normal volunteers.

The effects of topically applied timolol (a nonselective beta-blocker) and UF-021 (a prostaglandin-related compound) on pulsatile ocular blood flow (POBF) were investigated in 9 healthy volunteers. One drop of either UF-021 or timolol was instilled in one randomly selected eye and the fellow eye received physiologic saline. Before and 90 min after drop instillation, we measured intraocular pressure (IOP), POBF, heart rate (HR) and blood pressure (BP). After a washout interval of at least 1 week, the other drug was instilled in the previously treated eye. IOP, POBF, HR, and PB were measured following the same protocol. After timolol administration, IOP and POBF decreased significantly in the treated eye (26%, p = 0.01, and 13%, p = 0.02, respectively) and in the fellow eye (11%, p = 0.01, and 11%, p = 0.03, respectively). HR also decreased (10%, p = 0.03), but BP did not change significantly. After UF-021 administration, no significant changes were found in IOP, POBF, HR, or BP. Our results suggest that in normal subjects timolol decreases POBF in both the treated and the untreated eyes, whereas UF-021 has no action on either IOP or POBF.

Administration, Topical↗

PubMed1986

Effect of timolol on optic nerve head autoregulation.

Healthy subjects show, in a special pressure compliance test of the optic nerve head, signs of autoregulation of optic nerve head circulation. In this test visual evoked response (VER) amplitudes were recorded during stepwise increased intraocular pressures. In the resulting VER amplitude/pressure curves glaucoma patients did not show the sign of autoregulation of optic nerve head circulation which is seen in healthy subjects. It is known that topically applied timolol maleate may affect optic nerve head circulation. Therefore the pressure compliance test was performed in 20 healthy eyes before and after 3 days of topically applied timolol maleate 0.5%. The aim of the study was to test the effect of topically applied timolol on optic nerve head autoregulation. In addition we determined the ocular perfusion pressures, heart rate and mean arterial blood pressure. While the ocular perfusion pressures show a slight, but statistically not significant, decrease under timolol, the systemic parameters and the autoregulation behavior did not change.

Adult↗

PubMed1990

[Preservative-free timolol eye drops--surface-anesthetic effect and local compatibility].

0.5% timolol without preservative reduces corneal sensitivity for a shorter period of time than timolol with preservative. The subjective tolerance of unpreserved timolol is much better than that of preserved timolol. The latter and 0.5% levobunolol are significantly more poorly tolerated than buffer solution. The smaller the anesthetic side effects, the better the subjective tolerance of the beta-blockers.

Adolescent↗

PubMed1997

Short-term effect of apraclonidine on intraocular pressure in glaucoma patients receiving timolol and pilocarpine.

A placebo-controlled, prospective study was undertaken to determine whether apraclonidine has an additive effect in eyes treated with timolol and pilocarpine. Twelve patients with primary open-angle glaucoma while on continuing therapy with timolol 0.5% twice daily and pilocarpine 4% four times a day in both eyes for 3 months were included in the study. A single drop of apraclonidine 1% or placebo was added to treatment with timolol and pilocarpine. Intraocular pressure (IOP) was measured on both days before a single drop of test medications in both eyes as well as 2, 4, 6, 8 and 12 h later. The fall in IOP with apraclonidine was significantly greater than with placebo at all time intervals (p < 0.05). This study suggests that apraclonidine provides an additive IOP-lowering effect to timolol and pilocarpine for at least 12 h after single-drop applications.

Administration, Topical↗

PubMed1978

Effect of timolol plus hydrochlorothiazide plus hydralazine on essential hypertension.

The effect on hypertension of hydrochlorothiazide 100 mg daily plus timolol 20-60 mg daily versus hydrochlorothiazide plus placebo and of hydrochlorothiazide plus timolol plus hydralazine 40-200 mg daily versus hydrochlorothiazide plus placebo plus hydralazine was evaluated in a double-blind, randomized, crossover study in 38 patients with hypertension. Hydrochlorothiazide plus timolol was more effective than hydrochlorothiazide plus placebo in lowering both supine and standing systolic and diastolic blood pressures. Hydrochlorothiazide plus timolol plus hydralazine was a very effective regimen in lowering both supine and standing systolic and diastolic blood pressure. The patients tolerated this regimen well with greater hypotensive activity and a lower incidence of side effects than on hydrochlorothiazide plus placebo plus hydralazine.

Adult↗

PubMed1980

The effect of timolol vs placebo on angina pectoris.

The effect of timolol vs placebo on the frequency of anginal episodes, nitroglycerin consumption and exercise performance was investigated in a double-blind, randomized, crossover study in 23 patients with angina pectoris. The optimal dose of timolol (10-30 mg twice daily) for each patient was titrated by exercise studies. Compared with placebo, timolol decreased the weekly number of anginal attacks and the weekly number of nitroglycerin tablets consumed, reduced the resting heart rate, systolic and diastolic blood pressure, and product of systolic blood pressure times heart rate, decreased the heart rate, systolic and diastolic blood pressure, and product of systolic blood pressure times heart rate at the onset of angina pectoris or marked fatigue, prolonged exercise duration, and diminished electrocardiographic evidence of myocardial ischemia. Timolol is an excellent antianginal agent when prescribed twice daily, with the optimal dose titrated by exercise studies.

Angina Pectoris↗

PubMed1980

The beneficial effect of the beta blocker timolol in stable agina pectoris.

Timolol is a new beta blocker with cardioselective properties. A single blind controlled study was performed to assess the efficacy of timolol maleate in doses of 10 to 30 mg per day in 20 patients affected by stable angina pectoris. The patients received a placebo for a baseline period of 2 weeks, followed by 12 weeks of timolol. The number of anginal attacks dropped from 14.9 attacks per week in the baseline period to a minimum of 4.6 attacks per week in the sixth week of treatment (P less than 0.01). The number of tablets of nitroglycerin taken per week was reduced from 6.5 during the baseline period to 2.3 in the sixth week of treatment. Resting heart rate decreased from a baseline mean value of 72 beats per minute to 51.7 and 53.7 per minute at weeks 6 and 12 respectively (P less than 0.01). Blood pressure both at rest and during exercise was significantly reduced. The mean work index measured during bicycle ergometry was 127 units before treatment; it increased by 29.4 units and 36.1 units during week 6 and week 12 respectively (P less than 0.05). There was a marked symptomatic improvement in 50% of the patients. Mild fatigue was a common side effect but it disappeared following reduction of dose. We concluded that timolol maleate significantly reduces the number of anginal attacks and increases the work capacity of patients affected by stable angina pectoris

Adrenergic beta-Antagonists↗

PubMed1977

The management vf essential hypertension with once daily administration of timolol maleate and bendrofluazide.

A placebo controlled-blind study performed on new patients presenting with mild to moderate essential hypertension. A once daily combined dose of timolol maleate and bendrofluazide in a 4:1 ratio was administered ot each patient after a four week placebo period. The starting dose was timolol 10 mg and bendrofluazide 2-5 mg and this dose was increased in steps of timolol 10 mg and bendrofluazide 2-5 mg until blood pressure was controlled. Eleven out of twelve patients achieved normotension, the falls in diastolic and systolic blood pressure being highly significant on active treatment compared with placebo. The once daily regimen of timolol and bendrofluazide resulted in good control of blood pressure with no more side-effects than occurred on the placebo. A combination of these two drugs in one tablet would appear to be both practical and advantageous and should increase patient compliance in taking medication.

Adolescent↗

PubMed2006

Transport of timolol and tilisolol in rabbit corneal epithelium.

The purpose of this study is to characterize the transport of tilisolol and timolol through the corneal epithelium, which is believed to be a tight barrier of ocular drug absorption. Cultured normal rabbit corneal epithelial cells (RCEC) were used to investigate drug transport. Primary RCEC were seeded on a filter membrane of Transwell-COL insert coated with fibronectin and grown in Dulbecco's modified Eagle's medium/nutrient mixture F-12 with various supplements. Beta-blocker permeability through the RCEC layer was measured to assess the transcellular permeability coefficient (P(transcell)) in the absence or presence of inhibitors. The transcellular permeability of tilisolol was dependent on drug concentration although timolol showed no concentration dependency. Tilisolol flux from the apical to the basal side was larger than in the opposite direction although timolol showed no direction dependency. The transcellular permeability of tilisolol from the apical to the basal side was inhibited by sodium azide, tetraethylammonium, quinidine, taurocholic acid, guanidine and carnitine. Tilisolol had an active mechanism in uptake to the corneal epithelium, probably by the organic cation transporter family, although timolol predominantly permeated via passive diffusion. This RCEC system was useful to characterize the ocular permeation mechanism of drugs.

Adrenergic beta-Antagonists↗

PubMed2003

Characteristic effects of alpha1-beta1,2-adrenergic blocking agent, carvedilol, on [Ca2+]i in ventricular myocytes compared with those of timolol and atenolol.

Beta-adrenergic stimulation and the resultant Ca(2+) load both seem to be associated with progression of heart failure as well as hypertrophy. Because the alpha(1)-, beta(1,2)-blocker, carvedilol, has been shown to be outstandingly beneficial in the treatment of heart failure, its direct effects on intracellular calcium ion concentration ([Ca(2+)](i)), including antagonism to isoproterenol, in ventricular myocytes were investigated and then compared with a selective beta(1)-blocker, atenolol, and a non-selective beta(1,2)-blocker, timolol. At 1-300 nmol/L, carvedilol decreased the amplitude of [Ca(2+)] (i) by approximately 20% independently of its concentration, which was a similar effect to timolol. All the beta-blockers at 10 nmol/L decreased the amount of cAMP, but atenolol had the least effect. Carvedilol in the micromol/L order further diminished the amplitude of [Ca(2+)](i) transients, and at 10 micromol/L increased the voltage threshold for pacing myocytes. These effects were not observed with timolol or atenolol. L-type Ca2+ currents (I(Ca)) were decreased by carvedilol in the micromol/L order in a concentration dependent manner. As for the beta-antagonizing effect, the concentrations of carvedilol, timolol, and atenolol needed to prevent the effect of isoproterenol by 50% (IC(50)) were 1.32, 2.01, and 612 nmol/L, respectively. Furthermore, the antagonizing effect of carvedilol was dramatically sustained even after removal of the drug from the perfusate. Carvedilol exerts negative effects on [Ca(2+)](i), including inhibition of the intrinsic beta-activity, reduction of I(Ca) in the micromol/L order, and an increase in the threshold for pacing at > or =10 micromol/L. Data on the IC(50) for the isoproterenol effect suggest that carvedilol could effectively inhibit the [Ca(2+)](i) load induced by catecholamines under clinical conditions.

Adrenergic Antagonists↗

PubMed1983

Effect of timolol on exercise-induced reduction in regional ejection fraction in patients with coronary artery disease.

In order to evaluate the effects of timolol, a new beta-adrenergic blocking agent, on exercise-induced left ventricular wall motion abnormalities, we studied nine patients with chronic, angiographically-documented coronary artery disease. A computerized technique for determining apical, anteroseptal and inferoposterior regional ejection fractions during gated radionuclide ventriculography was used to assess left ventricular dysfunction. During exercise prior to the administration of timolol, the apical regional ejection fraction fell from 0.62 +/- 0.08 to 0.51 +/- 0.08 (p less than .01). The anteroseptal ejection fraction fell from 0.50 +/- 0.08 to 0.41 +/- 0.05 (p less than .05), and the inferoposterior ejection fraction fell from 0.75 +/- 0.10 to 0.59 +/- 0.06 (p less than .05). Three days after beginning therapy with 10-30 mg of timolol, this reduction was markedly attenuated. The apical ejection fraction fell from 0.59 +/- 0.09 to 0.54 +/- 0.08 (p = NS), the anteroseptal ejection fraction fell from 0.49 +/- 0.07 to 0.47 +/- 0.18 (p = NS) and the inferoposterior ejection fraction fell from 0.62 +/- 0.06 to 0.59 +/- 0.07 (p = NS). Furthermore, several individual regions showed increases in ejection fraction. This study demonstrates a previously unreported and beneficial anti-ischemic effect of timolol.

Cardiac Output↗

PubMedDate not supplied

Absorption of ocular timolol.

The absorption of timolol after topical administration to the eye was studied in 11 healthy volunteers and in 5 patients with bilateral open angle glaucoma. The volunteers received 2 drops of 0.5% timolol ophthalmic solution in each eye, equivalent to 0.8 mg of timolol maleate. Overflow was absorbed by paper tissue. The patients received the same dose twice daily for 2 weeks and were then investigated. In the paper tissue, 12 to 88% of the dose administered was recovered. Plasma concentrations were never above 5 ng/ml and not always detectable (detection limit 1 to 2 ng/ml). However, timolol was absorbed as the drug was found in the urine samples from all volunteers and glaucomatous patients.

Absorption↗

PubMed1990

Effects of timolol on terbutaline- and VIP-stimulated aqueous humor flow in the cynomolgus monkey.

The effects of timolol on terbutaline- and VIP-stimulated aqueous humor flow were investigated in cynomolgus monkeys, with a labeled albumin dilution method. The maximal increase in aqueous humor flow caused by intracameral (100 micrograms/ml) or intravenous (0.4 micrograms/kg/min) administration of terbutaline was about 100%. The effect of intravenously infused terbutaline was completely abolished by intracameral administration of timolol, 0.1 mg/ml. The same dose of timolol also abolished the effect of intravenously infused VIP, 50 ng/kg/min. Intravenous administration of timolol, 0.2 mg/kg, had no effect on VIP-stimulated aqueous humor flow, when VIP (90 micrograms) was given intracamerally, but abolished completely the effect of intracameral terbutaline, 100 micrograms/ml. The results suggest that the effect of intravenously infused VIP on aqueous humor flow is secondary to activation of the sympathetic nervous system, while the effect of intracameral administration of VIP is a direct effect on the ciliary epithelium. The maximal aqueous humor flow achieved with terbutaline is comparable to that in conscious cynomolgus monkeys.

Animals↗