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Results for “Timolol”

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At least 919 records · Page 51Linked to original sources

PubMed1981

[Timolol in combination with other glaucoma drugs (author's transl)].

In 39 selected patients with open-angle glaucoma, in whom pressure regulation with Timolol alone was inadequate, success was achieved by using this drug in combination with various other glaucoma drugs over treatment periods of 12 to 18 months. In all cases, Timolol had had a significant, thought inadequate pressure-lowering effect; only by adding either 0.5%-2% pilocarpine. 0.75-2.25% carbachol, 2% aceclidine, 0.1% epinephrine or 250 mg of acetazolamide could IOP be lowered effectively to an acceptable level.

Acetazolamide↗

PubMed1981

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

In a randomized, double-blind, cross-over study lasting eight months and involving 40 patients with primary open-angle glaucoma, the pressure-lowering effects of 0.25-0.5% timolol maleate were compared those of 0.1% epinephrine hydrochloride and 1% epinephrine. Timolol maleate was significantly more effective in reducing elevated IOP, both before cross-over and overall at both the lowest and highest concentrations of drug used; it was also without adverse side effects. The observed and reported adverse reactions during the epinephrine treatment period, such as blepharoconjunctivitis, burning and stinging after drug instillation, occurred less frequently with 0.1% epinephrine hydrochloride than with 1% epinephrine, whereas reduction of IOP was almost the same.

Adult↗

PubMed1981

[Results of treatment with timolol in problematic cases (author's transl)].

The authors report on the effect of timolol in cases of secondary glaucoma and buphthalmus in 143 eyes. Constant regulation of intraocular pressure was achieved by treatment with timolol in 67 eyes. A remarkable effect was observed in cases of complicated buphthalmus. The results were least favorable in cases of hemorrhagic secondary glaucoma.

Glaucoma↗

PubMed1980

[Effect of timolol and acetazolamide on intraocular hypertension after intracapsular lens extraction with alpha-chymotrypsin (author's transl)].

After intracapsular lens extraction with alpha-chymotrypsin three groups of 14 patients were formed. The first group was given Timolol 0.25% 2 x 1 drops, the second acetazolamide in sustained release form 1 x 500 mg and the third served as control. In all three groups the postoperatively elevated pressure diminished significantly in the first five postoperative days. The pressure diminution on the fourth and fifth postoperative day was accelerated by Timolol but not by acetazolamide.

Acetazolamide↗

PubMed1980

[Cadiovascular effects of local timolol therapy (author's transl)].

In a double-blind study, a significant blockade of the beta-adrenergic system was verified on 20 healthy volunteers after instillation of 4 drops of Timolol maleate 0.5% daily. The systemic blocking effect is obvious after stimulation of the sympathetic system by physical activity. Under these conditions the blood pressure and the heart rate of volunteers treated with Timolol rise less than those of volunteers given a placebo. A theoretical explanation is given and possible clinical implications are discussed.

Adult↗

PubMed1980

[Is timolol effective in neovascular glaucoma? (author's transl)].

Timolol lowered intraocular pressure in six patients with severe neovascular glaucoma only from about 45 mmHg to about 38 mmHg. The intense pain suffered by five patients was not alleviated. Hence, Timolol treatment does not seem very effective in neovascular glaucoma, although it may be of some value as a supplement to surgical treatment, which is only indicated where the patient still has useful vision. In the absence of an effective therapy for neovascular glaucoma priority must be given to its prevention.

Glaucoma↗

PubMed1987

Nasal and conjunctival contributions to the systemic absorption of topical timolol in the pigmented rabbit: implications in the design of strategies to maximize the ratio of ocular to systemic absorption.

The primary purpose of this study was to determine the relative contribution of the nasal and the conjunctival mucosae to the systemic absorption of topically applied timolol in the pigmented rabbit. The nasal mucosa was found to be about 2.5 times more efficient than the conjunctival mucosa in contributing to systemic timolol absorption, which occurred to the extent of 74% of the instilled dose. In addition, a minimum of 5-10 min prolongation of ocular contact time was determined to be necessary for significantly reducing systemic drug absorption and indirectly enhancing ocular drug absorption. The pharmaceutical implication of this finding is that ophthalmic vehicles such as polymeric inserts and gels would provide more favorable ocular to systemic drug absorption ratios than vehicles such as aqueous solutions and low-viscosity polymer solutions.

Absorption↗

PubMed1990

The effect of timolol, betaxolol, and placebo on corneal sensitivity in healthy volunteers.

This study in sixty healthy volunteers investigated the effect of a single drop of either 0.5% timolol ophthalmic solution, 0.5% betaxolol ophthalmic solution, or placebo on corneal sensitivity as measured by the Cochet-Bonnet anesthesiometer. Corneal sensitivity was measured immediately prior to the drop and then 1, 3, 6, 10, 15 and 30 minutes after drop instillation. The timolol treated eyes showed a significant decrease at one minute after instillation. An increase in sensitivity occurred in the placebo group at 15 and 30 minutes. In the eyes treated with betaxolol, a significant reduction in corneal sensitivity was seen at every time point through the 10-minute measurement.

Administration, Topical↗

PubMed1992

The inhibition of Na, K-ATPase, and Mg-ATPase by timolol maleate in cultured non-pigmented epithelial cells of the ciliary body.

Bovine, non-pigmented, ciliary body epithelial cells were isolated and grown in culture to determine whether timolol maleate might affect the activity of their plasma membrane ATPases. The possible effects were tested in drug concentrations in a range of 5 x 10(-19) to 5 x 10(-5) M over an incubation period of 30 min at 37 degrees. Assays of specific activity showed that the drug significantly (p less than .001 for most concentrations) inhibited both Na,K-ATPase and Mg-ATPase. However, the inhibition was partially reversed in concentrations greater than 10(-6) M for Na,K-ATPase and 10(-5) M for Mg-ATPase. The latter enzyme also indicated a second partial reversal in activity at concentrations between 10(-12) and 10(-9) M. These reversals in activity suggest that more than one binding site is involved in the inhibition of both enzymes. Since Na,K-ATPase in non-pigmented, ciliary body cells is responsible for the generation of aqueous fluid and the intraocular pressure (IOP), this inhibition demonstrates a possible mechanism for the pharmacological action of timolol maleate in lowering IOP.

Amino Acid Sequence↗

PubMed1997

Ocular-specific delivery of timolol by sequential bioactivation of its oxime and methoxime analogs.

S-(-)- Timolol maleate was oxidized, using the modified Pfitzner-Mofatt method, to the corresponding keto analog, which was then coupled with either hydroxylamine or methoxyamine in the same reaction medium. The products separated, timolone oxime (TO) or timolone methoxime (TMO), were found to be a mixture of both E and Z isomers with the Z isomer in higher concentration. Both isomers could be separated on silica column. No isomerization of any of the isomers could be detected whether in buffers or biological fluids. TMO salts were found to be stable in slightly acidic buffer. The Z isomer of TMO is more stable than the E isomer. Both TO and TMO showed pronounced reduction of the intraocular pressure (IOP) in normotensive rabbits, when instilled into the conjunctival sac. Reduction of IOP caused by either TO or TMO was higher than the reduction produced with the same dose of timolol maleate. Equal doses of any of the TMO isomers or the mixture of isomers gave almost the same percent reduction of IOP. TMO and TO did not show cardiovascular effects when administered intravenously to rabbits or rats. Both are good candidates to be used for topical management of glaucoma without producing systemic side effects.

Administration, Topical↗

PubMed2005

The efficacy and ocular discomfort of substituting brinzolamide for dorzolamide in combination therapy with latanoprost, timolol, and dorzolamide.

PURPOSE: The aim of this study was evaluate the efficacy and ocular discomfort of substituting brinzolamide for dorzolamide in patients with glaucoma treated by latanoprost, timolol, and dorzolamide. METHODS: An 8-week, prospective, randomized, open-label, comparative study was performed in 58 patients with primary open-angle glaucoma treated by latanoprost, timolol, and dorzolamide. These patients were randomly enrolled into two groups: (1) dorzolamide three times daily was substituted with brinzolamide twice-daily (substituting group); and (2) dorzolamide three times daily was continued (control group). Intraocular pressure (IOP) was measured at baseline, 4, and 8 weeks after the enrollment. Subjective ocular discomfort (irritation and blurred vision) at the time of the instillation of the patient was noted with interview. RESULTS: The IOPs at baseline, 4 and 8 weeks after the enrollment were 17.7 +/- 2.7 mmHg, 17.5 +/- 2.6 mmHg, and 17.4 +/- 2.9 mmHg in the substituting group, and 18.0 +/- 2.5 mmHg, 17.8 +/- 2.5 mmHg, and 17.9 +/- 2.6 mmHg in the control group, respectively. There were no significant differences in IOP changes between the two groups (P = 0.74). In the substituting group, ocular irritation was decreased significantly (P = 0.0014) from 63% to 20%. The slight increase of blurred vision from 27% to 37% that occurred in the substituting group was not significant (P = 0.58). In the control group, neither ocular irritation (P = 0.58, from 68% to 57%) nor blurred vision (P = 0.99, from 25% to 21%) was changed. CONCLUSIONS: Substituting brinzolamide for dorzolamide maintained stable IOP with improvement in ocular comfort in patients with glaucoma.

Aged↗

PubMed1994

Unsuspected bronchospasm in association with topical timolol--a common problem in elderly people: can we easily identify those affected and do cardioselective agents lead to improvement?

The extent of impairment of respiratory function in a group of 52 elderly, glaucomatous patients receiving topical timolol therapy was investigated. To predict those patients who were likely to benefit from changing therapy, symptoms were elicited by direct questioning, and lung spirometry was measured before and after inhalation of salbutamol. Changing from timolol to either pilocarpine or the cardioselective betaxolol produced improvement in lung function tests. Mean peak flow increased from 278 l/min to 328 l/min (p < 0.001), forced expiratory volume in 1s (FEV1) from 1.66 l to 1.85 l (p < 0.001) and forced vital capacity (FVC) from 2.41 to 2.64 l (p < 0.001). Spirometry in a control group of 20 subjects was unchanged. Nineteen of 47 patients demonstrated a clinically significant (defined as 15% or more) increase in all values of lung function tests. Change to pilocarpine or betaxolol was equally effective in producing improvement but betaxolol had fewer side-effects. The presence of exertional dyspnoea, cough with sputum, raised dyspnoea score and improved lung function tests after salbutamol identified those patients experiencing clinically significant bronchospasm with an 89% specificity and 74% sensitivity.

Aged↗

PubMed1984

The action of beta-adrenoceptor antagonists on rat heart mitochondrial function in vitro: a comparison of propranolol, timolol, and atenolol.

The effect of beta-adrenoceptor antagonists, propranolol, timolol and atenolol on functions of rat heart mitochondria in vitro was investigated. Concentrations of all three drugs less than 2 mmol X litre-1 did not affect rates of respiration of uncoupled intact mitochondria supported by substrates of alpha-oxoglutarate, pyruvate-malate or succinate. Inhibition was observed if mitochondria were broken to allow access of substrates and drugs into the mitochondria. Studies of the effect of drug concentration on NADH-supported oxygen uptake and NADH oxidase activity of submitochondrial particles produced from rat heart mitochondria showed a marked inhibition by propranolol: the effect of timolol and atenolol were much less marked and inhibition was only observed at relatively high concentrations of these drugs. Transfer of electrons through Complex I measured by the rate of reduction of ferricyanide by submitochondrial particles inhibited by rotenone and the lack of specific inhibition by propranolol of succinate supported respiration indicated that one site of drug action was between NADH dehydrogenase and its associated flavoprotein, possibly close to the site of rotenone inhibition.

Animals↗

PubMed1996

Cardiac failure aggravated by timolol eye drops: preoperative improvement by changing to pilocarpine.

A 73-year-old woman with cardiac dysfunction had several episodes of severe bradycardia and pulmonary oedema when waiting for peripheral vascular surgery. She used timolol eye drops for primary open-angle glaucoma. The first episode of pulmonary oedema occurred two weeks prior to and the second on the day before the planned surgery. There were another two episodes of pulmonary oedema before she was transferred to the Department of Internal Medicine where she had a further two episodes of cardiac failure. After changing timolol to pilocarpine eye drops, the patient's condition was stabilized, and two weeks later surgery and postoperative recovery were uneventful.

Adrenergic beta-Antagonists↗

PubMed1982

Timolol and dipivalyl epinephrine combination therapy.

Combination therapy with timolol 0.25% eye drops and dipivalyl epinephrine (DPE) 0.1% eye drops twice daily is an acceptable form of medication for both chronic simple glaucoma and ocular hypertension. A group of eighteen patients using this combination therapy have been followed up for a period of two years with satisfactory control of intraocular pressure in the majority of cases. An additive effect in lowering intraocular pressure when the two drugs were used in combination was confirmed. Two patients developed a sensitivity reaction to DPE and were able to continue on timolol alone. There was a slight rise in the intraocular pressure between the sixth and ninth months of therapy, but following this the mean intraocular pressure was remarkably stable. Patient acceptance of this twice daily regime was excellent and compliance with the drug therapy was also good.

Aged↗

PubMed1983

Excretion of oxprenolol and timolol in breast milk.

The excretion of oxprenolol and timolol in breast milk was examined by comparing their concentrations in milk with those in plasma. The mean milk to plasma ratio of oxprenolol was 0.29 (SD 0.14; that for timolol was 0.80 (SD 0.21). The total quantity of either drug ingested by a fully breast-fed infant is unlikely to be therapeutically significant.

Adult↗

PubMed1976

Investigations on the antihypertensive activity of timolol and bendroflumethiazide and the combination in dogs and rats.

The effects of timolol and bendroflumethiazide, either alone or combined in a fixed ratio of 4:1, on blood pressure, plasma renin activity, and plasma potassium concentration, have been investigated in normotensive and renal hypertensive dogs, and in normotensive and spontaneously hypertensive rats. In addition, the urinary kallikrein excretion has been measured in normotensive and hypertensive rats. When administered to hypertensive dogs and rats, the drug combination significantly reduced the blood pressure. Marginal reductions were observed in normotensive animals or after the administration of the single drugs. The thiazide-induced hypokalaemia and hyperreninaemia were almost completely antagonised by the concomitant administration of timolol in both animal species. A highly significant elevation of urinary kallikrein excretion was also observed in rats treated with the drug combination. A less marked increase of kallikrein excretion was noted in the bendroflumethiazide treated rats. The possibility that renal haemodynamic changes, in addition to the inhibition of the increase in plasma renin, play a role in the observed antihypertensive effects is discussed.

Animals↗

PubMed1978

The effect of 1.5% timolol maleate on intraocular pressure.

A controlled trial was instituted to compare the effect on intraocular pressure of topical administration of timolol maleate with epinephrine hydrochloride. A bottling error by the manufacturer resulted in the placebo bottles containing 1.5% timolol maleate. This drug given twice a day for two weeks significantly reduced intraocular pressure and produced no side effects.

Administration, Topical↗