OBJECTIVE: The noradrenaline system is involved in the reward effects of various kinds of abused drugs. Betaxolol (BTX) is a highly selective β1-antagonist. In the present study, we evaluated the effect of BTX on methamphetamine (MAP)-induced conditioned place preference (CPP) and hyperactivity in mice. METHODS: The mice (n=72) were treated with MAP or saline every other day for a total of 6 days (from day 3 to day 8; 3-times MAP and 3-times saline). Each mouse was given saline (1 mL/kg) or MAP (1 mg/kg, s.c.) or BTX (5 mg/kg, i.p.) or MAP with BTX (5 mg/kg, i.p.) 30 min prior to the administration of MAP (1 mg/kg, s.c.) every other day and paired with for 1 h (three-drug and three-saline sessions). We then compared the CPP score between the two groups. After the extinction of CPP, the mice were given BTX (5 mg/kg, i.p.) or saline (1 mL/kg) 24 h prior to a priming injection of MAP, and were then immediately tested to see whether the place preference was reinstated. RESULTS: The repeated administration of BTX 30 min prior to the exposure to MAP significantly reduced the development of MAP-induced CPP. When BTX was administered 24 h prior to the CPP-testing session on day 9, it also significantly attenuated the CPP, but did not result in any change of locomotor activity. In the drug-priming reinstatement study, the extinguished CPP was reinstated by a MAP (0.125 mg/kg, s.c.) injection and this was significantly attenuated by BTX. CONCLUSION: These findings suggest that BTX has a therapeutic and preventive effect on the development, expression, and drug-priming reinstatement of MAP-induced CPP.
Animals ; Betaxolol* ; Methamphetamine* ; Mice* ; Motor Activity ; Norepinephrine ; Reward

We investigated the acute effects of timolol (beta-adrenergic non-selective) and betaxolol (beta1-adrenergic selective) on the retinal and optic nerve head (ONH) microcirculation in healthy subjects with Heidelberg Retina Flowmeter (HRF). Intraocular pressure (IOP), heart rate, blood pressure, and retinal and ONH microcirculation were measured in 7 healthy subjects (3 F/ 4 M; mean age=27.2 +/- 1.1 years) before and 90 minutes after instillation of each drug on separate occasions at 2 weeks apart. Volume, flow, and velocity of microcirculation in the peripapillary retina and neural rim of ONH were measured using HRF. Both drugs significantly reduced IOP (Wilcoxon signed rank test; p=.03) without affecting heart rate or blood pressure. It had no effect on the volume, flow, and velocity of blood flow in the peripapillary retina and ONH (Wilcoxon signed rank test; p>.1), From the above results, we concluded that both timolol and betaxolol did not alter retinal and ONH microcirculation.
Betaxolol* ; Blood Pressure ; Flowmeters ; Heart Rate ; Intraocular Pressure ; Microcirculation ; Optic Disk* ; Optic Nerve* ; Retina ; Retinaldehyde* ; Timolol*

Betaxolol Hydrochloride was compared with Timolol in view of the hypotensive effect. Thirty five normal volunteers(70 eyes) of the third decade were enrolled in this study. Thirty volunteers of experimental group were devided into three groups, -0.5% Betaxolol group, 0.25% Timolol group and 0.5% Timolol group. The remaining five volunteers(10 eyes) were used as control group. Double masked single dose study was done by instillating each eye solution into the randomly selected one eye. The intraocular pressure(IOP), Pupil size, Visual acuity, blood pressure, and pulse rate were measured before the instillation of eye solution at first and 30 minutes. 1,2,4,6,12, and 24 hours after the and the statistical significance was estimated by using the paired t-test. The following results were obtained: 1. 0.5% Betaxolol showed a significant reduction of IOP from 30 minutes to 12 hours after the instillation and maximum IOP reduction(18.9 +/- 3.4%) was noted at 4 hours after the instillation. 2. Statistically significant IOP reduction was noted in the contralateral eyes of both Betaxolol and Timolol groups. 3. After the treatment with Betaxolol, the pupil size, visual acuity, blood pressure, and pulse rate were not significantly changed. Transient mild stinging sensation was noted as a local side effect after the instillation of the Betaxolol.
Betaxolol* ; Bites and Stings ; Blood Pressure ; Healthy Volunteers* ; Heart Rate ; Masks ; Pupil ; Sensation ; Timolol* ; Visual Acuity ; Volunteers

To evaluate the clinical usefulness of a newly developed beta-one selective blocker. Betaxolol hydrochloride(Betoptice(R)), seven patients(14 eyes) with primary open-angle glaucoma who were instilled twice a day with a drop of 0.5% Betoptic were enrolled in this study. Intraocular pressure(IOP), systolic and diastolic blood pressure, pulse rate and pupil size were measured with the evaluation on the local adverse reaction before and after the Betoptic treatment of 1, 2, 4, 8 and 12 weeks. The following results were obtained: 1. Significant reduction of IOP was noted at all intervals examined after the treatment of 0.5% Betoptic and it had the additive effect on pilocarpine. 2. The systemic side reaction of Betoptic on either pulse rate or blood pressure was not significant and pupil size was not changed by Betoptic. 3. The local transient and mild stinging sensation with tearing was followed after the instillation of 0.5% Betoptic eye solution.
Betaxolol* ; Bites and Stings ; Blood Pressure ; Glaucoma* ; Glaucoma, Open-Angle ; Heart Rate ; Humans ; Pilocarpine ; Pupil ; Sensation

PURPOSE: To evaluate the neuroprotective effects of betaxolol (betaxolol hydrochloride) under hypoxic conditions using retinal ganglion cells (RGC-5) and determine whether heme oxygenase-1 (HO-1) expression exerts cytoprotective effects. METHODS: In this study, cultured RGC-5 cells were incubated with different concentrations of betaxolol hydrochloride (0.1 microM, 1 microM or 5 microM) and with 10 microM zinc protoporphyrin (ZnPP), in a hypoxia incubator (1% O2, 5% CO2, 94% N2) for 48 hours and the cell viability of each group was determined. Additionally, cell viability was measured after RGC-5 cells were incubated with 5 microM of brinzolamide (Azopt(R)), brimonidine tartrate (Alphagan(R)) or travoprost (Travatan(R)). RGC-5 cells were divided into three groups and incubated under three different conditions, normoxia group (20% O2, 5% CO2), hypoxia group (1% O2, 5% CO2) and the group with 5 microM of Betoptic S(R) treated under hypoxic conditions (hypoxia, Betoptic S(R)). After incubation for 4, 8, 12 and 24 hours, HO-1 expression was analyzed using Western blotting. RESULTS: Cell viability significantly increased in RGC-5 cells treated with Betoptic S(R) compared with other antiglaucoma agents. Increased levels of HO-1 expression indicate its relevance in cell viability. Furthermore, increased RGC-5 cell viability by Betoptic S(R) was significantly reduced in the HO-1 inhibitor ZnPP-treated group. CONCLUSIONS: We reaffirmed the known cytoprotective effects of Betoptic S(R) and the results suggests that HO-1 expression exerts cytoprotective effects against hypoxia.
Anoxia ; Betaxolol* ; Blotting, Western ; Cell Survival ; Heme Oxygenase-1* ; Heme* ; Incubators ; Neuroprotective Agents* ; Retinal Ganglion Cells ; Zinc ; Brimonidine Tartrate ; Travoprost

The effect of betaxolol and dipivefrin on microcirculation of peripapil lary reina and optic disc in normal tension glaucoma was assessed. Betaxolol, selective beta-1 blocker, was known to improve the blood flow of retrobulbar arteries, and dipivefrin was known to decrease the flow of ciliary body. Total subjects were 29 normal tension glaucoma patients; 18 subjects with no previous IOP reducing eye drops during 4 weeks were assigned for betaxolol group, and 11 subjects with using timolol for dipivefrin group. The intraocular pressure was significantly reduced after instillation in betaxolol group(p<0.01), and in dipivefrin group(p<0.05). But systemic blood pressure and pulse rate were not changed after instillations in both groups. Blood flow, volume, velocity of optic disc and peripapillary retina of betaxolol group and dipivafrin group were not significantly changed. From the above results, we concluded that betaxolol and dipiverin with timolol did not influenced the microcirculation of peripapillary retina and opit disc.
Arteries ; Betaxolol* ; Blood Pressure ; Ciliary Body ; Heart Rate ; Humans ; Intraocular Pressure ; Low Tension Glaucoma* ; Microcirculation ; Ophthalmic Solutions ; Optic Disk* ; Optic Nerve* ; Retina ; Retinaldehyde* ; Timolol

Normal tension glaucoma (NTG) is a disorder showing the characteristic optic nerve head damage and visual field defect with a normal intraocular pressure (IOP) and open anterior chamber angle, without any other disorders that may induce a damage to the optic nerve head and visual field. A disturbance in the vascular supply to the optic nerve head is thought to be the main etiologic factor in this disorder. A thirty percent reduction of IOP from the baseline can delay or prevent the disease progress of glaucoma, and the treatment of NTG is focused on relieving any vascular disturbance to the optic nerve head and reducing IOP. The target pressure in NTG should be individualized in each patient by age, presence of any systemic vascular disorder, the degree of optic disc damage, and response to anti-glaucoma medications. It should also be carefully and regularly re-evaluated during follow-up. Since most patients with NTG are old, the selection of anti-glaucoma medication needs a careful consideration of the systemic status of the patient. Pilocarpine effectively reduces IOP, but has limitations from side effects including miosis. Nonselective beta-blocking agents may induce serious systemic side effects and can reduce the perfusion pressure to the optic nerve head. Brimonidine reduces the aqueous inflow, increases the uveoscleral outflow, and is known to have a potential neuroprotective effect. Betaxolol and dorzoldamide are known to increase the ocular blood flow and have a protective effect from optic nerve damage. Oral carbonic anhydrase inhibitor may be effective, if systemic adverse effects can be tolerated. Prostaglandins may reduce IOP below the level of episcleral venous pressure, but their long-term side effects have not been fully evaluated to date. Laser trabeculoplasty can reduce IOP, but not sufficiently in many instances. To reduce IOP sufficiently enough to halt the progression of glaucoma, filtering surgery assisted by mitomycin-C and 5-FU may be recommended, when the IOP reduction is not satisfactory with anti-glaucoma medications.
Anterior Chamber ; Betaxolol ; Brimonidine Tartrate ; Carbonic Anhydrases ; Filtering Surgery ; Fluorouracil ; Follow-Up Studies ; Glaucoma* ; Humans ; Intraocular Pressure ; Low Tension Glaucoma ; Miosis ; Mitomycin ; Neuroprotective Agents ; Optic Disk ; Optic Nerve ; Perfusion ; Pilocarpine ; Prostaglandins ; Trabeculectomy ; Venous Pressure ; Visual Fields

PURPOSE: Although the economic and mortality burden of atrial fibrillation (AF) is substantial, it remains unclear which treatment strategies for rate and rhythm control are most cost-effective. Consequently, economic factors can play an adjunctive role in guiding treatment selection. MATERIALS AND METHODS: We built a Markov chain Monte Carlo model using the Korean Health Insurance Review & Assessment Service database. Drugs for rate control and rhythm control in AF were analyzed. Cost-effective therapies were selected using a cost-effectiveness ratio, calculated by net cost and quality-adjusted life years (QALY). RESULTS: In the National Health Insurance Service data, 268149 patients with prevalent AF (age ≥18 years) were identified between January 1, 2013 and December 31, 2015. Among them, 212459 and 55690 patients were taking drugs for rate and rhythm control, respectively. Atenolol cost $714/QALY. Among the rate-control medications, the cost of propranolol was lowest at $487/QALY, while that of carvedilol was highest at $1363/QALY. Among the rhythm-control medications, the cost of pilsicainide was lowest at $638/QALY, while that of amiodarone was highest at $986/QALY. Flecainide and propafenone cost $834 and $830/QALY, respectively. The cost-effectiveness threshold of all drugs was lower than $30000/QALY. Compared with atenolol, the rate-control drugs propranolol, betaxolol, bevantolol, bisoprolol, diltiazem, and verapamil, as well as the rhythm-control drugs sotalol, pilsicainide, flecainide, propafenone, and dronedarone, showed better incremental cost-effectiveness ratios. CONCLUSION: Propranolol and pilsicainide appear to be cost-effective in patients with AF in Korea assuming that drug usage or compliance is the same.
Amiodarone ; Atenolol ; Atrial Fibrillation ; Betaxolol ; Bisoprolol ; Compliance ; Cost-Benefit Analysis ; Diltiazem ; Flecainide ; Humans ; Insurance, Health ; Korea ; Markov Chains ; Mortality ; National Health Programs ; Propafenone ; Propranolol ; Quality-Adjusted Life Years ; Sotalol ; Verapamil