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Biomedical subjects

G D Novack

Publications and source records attributed to G D Novack.

70 records · Page 4Linked to original sources

Levobunolol compared with timolol for the control of elevated intraocular pressure.

Two concentrations of levobunolol (0.5% and 1%) and one concentration of timolol (0.5%) were evaluated for the control of elevated intraocular pressure (IOP) in a double-masked, randomized study. Fifty-one patients received one of the three study treatments in both eyes bid for one year. Both drugs were equally effective in reducing IOP: The overall reduction in mean IOP was slightly more than 9 mm Hg in all three treatment groups. Levobunolol was as safe and effective as timolol for the long-term control of elevated IOP.

Clinical Trials as Topic↗

Levobunolol. A three-month efficacy study in the treatment of glaucoma and ocular hypertension.

The ocular hypotensive effect and the safety of levobunolol hydrochloride (0.5% and 1%) were compared with vehicle in this double-masked study of 42 patients with chronic open-angle glaucoma or ocular hypertension. After a washout of ocular hypotensive medication, patients received one of the three test treatments in both eyes twice daily for three months. Both concentrations of levobunolol produced significant reductions in intraocular pressure, while decreases in vehicle-treated patients were minimal. Over the three-month study period, average pressure reductions were approximately 9.0 mm Hg in patients receiving either concentration of levobunolol and 0.5 mm Hg in patients receiving vehicle. Fewer patients were terminated from the study for inadequately controlled intraocular pressure in the levobunolol groups than in the vehicle group. No patients were terminated for drug-related adverse experiences.

Adult↗

Levobunolol compared with timolol for the long-term control of elevated intraocular pressure.

Levobunolol hydrochloride (0.5% and 1%) and timolol maleate (0.5%) are being compared in an ongoing, double-masked, randomized study of 141 patients with ocular hypertension or chronic open-angle glaucoma. Baseline intraocular pressure (IOP) in the three treatment groups ranged from 26 to 27 mm Hg. During the first 15 months of the study, the two drugs have not proved to be significantly different in ocular hypotensive efficacy, with overall mean IOP decreases of 6.8 to 7.6 mm Hg. In addition, the two concentrations of levobunolol have been equally effective in controlling IOP. Neither drug has been associated with any significant ocular side effects. Both drugs have produced significant decreases (five to ten beats per minute) in mean heart rate. The effect on mean blood pressure has been less pronounced: overall decreases have been less than 4 mm Hg for both systolic and diastolic blood pressure. The results of this ongoing study suggest that levobunolol is as effective and as safe as timolol for the long-term control of IOP.

Adult↗

Long-term ocular hypotensive effect of levobunolol: results of a one-year study.

Data for the first 12 months are reported for an ongoing, multicentre, clinical study comparing the long-term, ocular hypotensive efficacy and safety of topical levobunolol (0.5% and 1%) and timolol (0.5%). This study was a double-masked trial testing 88 patients with chronic open angle glaucoma or ocular hypertension. During the 12-month period drops were instilled twice daily into both eyes after a washout of prestudy ocular hypotensive medication. The effect of the three treatments in reducing intraocular pressure (IOP) was similar. Mean IOP reductions over the 12 months averaged 7.2 mmHg for the 0.5% levobunolol group, 6.2 mmHg for the 1% levobunolol group, and 6.0 mmHg for the timolol group. Decreases in mean heart rate of up to 5 beats per minute were observed in the 0.5% levobunolol group, up to 8 beats per minute in the 1% levobunolol group, and up to 4 beats per minute in the timolol group. Several patients were removed from the study owing to side effects possibly related to levobunolol treatment.

Adult↗

Flurazepam and triazolam: dose-response and time-response evaluation on cat sleep.

A window discrimination method is presented for the continuous monitoring of sleep-wakefulness cycles in cats. Window discrimination permits the recording of the frequency of firing of multiple units, while filtering out movement artifacts and low-level noise. Records of reticular formation multiple unit activity (MUA) and EMG from cats with chronically implanted electrodes were quantified by window discrimination and displayed on a strip chart recorder. The frequency of firing of large reticular multiple units was highest in states of high CNS excitation (i.e., REM), and the lowest in states of low CNS excitation (i.e., SWS). Comparison of recording of reticular MUA by window discrimination and rectification-integration indicated that sleep-wakefulness states were more easily distinguished with the former method. The effects of flurazepam, 1.25-5 mg/kg i.p., and triazolam, 0.01-0.05 mg/kg i.p., on reticular MUA were observed for 24-72 h of continuous recording. Both benzodiazepines depressed reticular MUA by up to 50% in a dose-related fashion. Flurazepam was effective for 72 h or more, and triazolam for 24-48 h. Flurazepam was also much longer lasting than triazolam when administered for 3 days at 24 h intervals. As evidence by our evaluation of flurazepam and triazolam, it appears that evaluation of the effects of sedative-hypnotics on the CNS excitation level of the cat, and the duration of these effects, can be readily performed and these results generalized to the clinical experience. This should prove useful in the evaluation of novel sedative-hypnotics.

Animals↗

Predictive value of muscle relaxant models in rats and cats.

A number of clinically effective muscle relaxants and structurally related compounds were examined in three animal models of muscle relaxant activity in order to determine the utility of these models in predicting clinical activity. The methods used were attenuation of morphine-induced rigidity in rats, decerebrate rigidity in cats, and the polysynaptic linguomandibular reflex in cats. Specificity of the compounds was assessed by comparing these data to the ability of the compounds to induce rotarod failure in rats and to inhibit the monosynaptic patellar reflex in cats. Diazepam and chlordiazepoxide were of limited potency in morphine-induced rigidity and decerebrate rigidity, but were potent on the polysynaptic reflex. Mephenesin, cyclobenzaprine, and the newer benzodiazepine, midazolam, were effective and moderately specific in all three models. Baclofen and dantrolene were effective but were of little or no specificity in all models. Analysis of the data yielded poor correlation between clinical muscle relaxant potency and the potencies obtained in these animal models. The correlation coefficients of 0.54, 0.50, and 0.70 for the linguomandibular reflex, decerebrate rigidity, and morphine rigidity, respectively, were not statistically significant, in contrast with a coefficient of 1.0 using previously reported data on these compounds in inhibiting morphine-induced Straub tail in mice. Thus, the three models used in this study may possess utility in the study of sites and mechanisms of action and structure-activity relationships of potential muscle relaxants, but they do not appear to be as useful as morphine-induced Straub tail in potency comparisons between different chemical classes.

Amitriptyline↗

Anticonvulsant effects of benzhydryl piperazines on maximal electroshock seizures in rats.

The anticonvulsant effects of four benzhydryl piperazines, SC-13504 (ropizine, an anticonvulsant), hydroxyzine (HDX, an anxiolytic), chlorcyclizine (CCZ, an antihistaminic) and buclizine (BUC, an antihistaminic), were investigated utilizing a modified maximal electroshock seizure test in rats. In addition to detecting the presence or absence of tonic hindlimb extension, the modified method quantified various phases of the seizure. All four benzhydryl piperazines exhibited anticonvulsant activity in maximal electroshock seizure, but SC-13504 was similar in efficacy to phenobarbital and phenytoin, and much more effective than HDX, CCZ or BUC. Additionally, SC-13504 possessed a therapeutic index much greater than any of the compounds tested. The duration of action of the benzhydryl piperazines, in hours was: SC-13504, 0.5 to 8; HDX, 0.5 to 2; CCZ, 0.5 to 16; and BUC, 2 to 8. Buc and CCZ are postulated to be converted to active anticonvulsant metabolites.

Animals↗

Ophthalmic beta-blockers since timolol.

In the twenty years since beta-blockers were proposed for treatment of glaucoma, use of topical timolol has increased to account for 70% of all glaucoma medications used. The objective of this article is to review the "newer" beta-blockers, and to address the generalization that "all ophthalmic beta-blockers are the same." The review concentrates on agents that have been studied as topical treatments for patients with elevated intraocular pressure. Sections on pharmacology and design of clinical trials are included to aid the ophthalmologist in evaluating the new drugs and published clinical reports. The major questions to consider in evaluating the therapeutic potential of a new beta-blocker for the treatment of glaucoma involve efficacy and safety: Is the drug as effective as timolol? Does it have a duration of action at least as long as timolol? Does it have ocular toxicity? Is it comfortable? What are its systemic effects?

Adrenergic beta-Antagonists↗

[Dipivefrin: its mechanism of action, clinical efficacy and good tolerance].

Dipivefrin (DPE) is the first prodrug in general use in ophthalmology. We will discuss the metabolism of DPE to epinephrine within the eye, and the efficacy and safety of DPE in the treatment of elevated intraocular pressure. In addition, we will address the incidence of adverse systemic effects, ocular tolerance and allergy, and the ocular hypotensive efficacy when DPE is used alone or in combination with other antiglaucoma medications.

Epinephrine↗