Literature DB >> 2411566

Effect of ophthalmic administration of S-596 (Arotinolol) on intraocular pressure and haemodynamics in health volunteers: comparison with timolol.

M Nakashima, T Uematsu, Y Takiguchi, H Hashimoto, I Watanabe, S Morioka, T Hibino.   

Abstract

The effects on intraocular pressure (IOP) and haemodynamics of two beta-blockers, arotinolol and timolol, administered topically to the eye, were studied in 6 healthy volunteers in a cross-over trial. 0.5% timolol or 0.5% arotinolol ophthalmic solutions drop was instilled in both eyes of the volunteers at an interval of 48 hours. Timolol lowered IOP by about 31.9% 1 hour after administration and the effect continued until 3 h, whilst arotinolol lowered it significantly 2 h after instillation and the same maximum effect as that of timolol was obtained after 3 h. Arotinolol was detected in blood in all subject and timolol in blood in one subject, although it was found in all subjects in urine. Both drugs lowered heart rate at rest and attenuated the increase in the double product (products of blood pressure and heart rate) at exercise. The effect of timolol on the double products was larger. Thus, arotinolol and timolol decreased IOP to similar extent, although the maximal effect of arotinolol was delayed. Arotinolol as well as timolol affected haemodynamics through absorption into circulation, but the former had less effect on haemodynamics during exercise.

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Year:  1985        PMID: 2411566     DOI: 10.1007/bf00544356

Source DB:  PubMed          Journal:  Eur J Clin Pharmacol        ISSN: 0031-6970            Impact factor:   2.953


  15 in total

1.  Physiological disposition and metabolism of timolol in man and laboratory animals.

Authors:  D J Tocco; A E Duncan; F A Delauna; H B Hucker; V F Gruber; W J Vandenheuvel
Journal:  Drug Metab Dispos       Date:  1975 Sep-Oct       Impact factor: 3.922

2.  Synthesis and beta-adrenergic blocking action of a new thiazolylthiopropanolamine derivative.

Authors:  Y Hara; E Sato; A Miyagishi; A Aisaka; T Hibino
Journal:  J Pharm Sci       Date:  1978-09       Impact factor: 3.534

3.  Timolol and epinephrine. Comparisin of efficacy and side effects.

Authors:  J R Sonntag; G O Brindley; M B Shields; N I Arafat; C D Phelps
Journal:  Arch Ophthalmol       Date:  1979-02

4.  Cardiac effects of topical timolol.

Authors:  N A Britman
Journal:  N Engl J Med       Date:  1979-03-08       Impact factor: 91.245

5.  Allergic conjunctivitis associated with timolol therapy in an adult.

Authors:  J A Baldone; J S Hankin; T J Zimmerman
Journal:  Ann Ophthalmol       Date:  1982-04

6.  [Pharmacological properties of dl-2-(3'-t-butylamino-2'-hydroxypropylthio)-4-(5'-carbamoyl-2'-thienyl) thiazole hydrochloride (S-596), a new beta-adrenergic blocking agent (author's transl)].

Authors:  Y Hara; E Sato; A Miyagishi; S Aono; H Nakatani
Journal:  Nihon Yakurigaku Zasshi       Date:  1979-10

7.  Timolol, dose response and duration of action.

Authors:  T J Zimmerman; H E Kaufman
Journal:  Arch Ophthalmol       Date:  1977-04

8.  Absorption of ocular timolol.

Authors:  G Alvan; B Calissendorff; P Seideman; K Widmark; G Widmark
Journal:  Clin Pharmacokinet       Date:  1980 Jan-Feb       Impact factor: 6.447

9.  Dynamics and kinetics of ophthalmic timolol.

Authors:  M B Affrime; D T Lowenthal; J A Tobert; J Shirk; B Eidelson; T Cook; G Onesti
Journal:  Clin Pharmacol Ther       Date:  1980-04       Impact factor: 6.875

10.  Long-term treatment of glaucoma with systemic propranolol.

Authors:  A Ohrström; M Pandolfi
Journal:  Am J Ophthalmol       Date:  1978-09       Impact factor: 5.258

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  1 in total

1.  Apraclonidine hydrochloride: an evaluation of plasma concentrations, and a comparison of its intraocular pressure lowering and cardiovascular effects to timolol maleate.

Authors:  A L Robin; A L Coleman
Journal:  Trans Am Ophthalmol Soc       Date:  1990
  1 in total

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