PMID: 9527641Apr 4, 1998Paper

Systemic and ocular absorption and antagonist activity of topically applied cyclopentolate in man

Pharmacology & Toxicology
M HaagaP Ylitalo

Abstract

Ocular and systemic absorption and antagonist activity of topical 1% cyclopentolate were studied in 11 elderly patients undergoing extracapsular cataract extraction, and in 8 healthy female volunteers. The patients received two 35 microl drops of cyclopentolate unilaterally and the healthy volunteers one 30 microl drop bilaterally to the lower conjunctival cul-de-sac of the eye. The drug concentrations were measured with radioreceptor assay and receptor occupancies with radiooccupancy assay using isolated rat brain muscarinic cholinoceptors. In the patient group, cyclopentolate concentrations in aqueous humour were approximately 3000 times higher than those in plasma. Muscarinic cholinoceptors were occupied totally (more than 99.9%) by aqueous humour and 3-18% by plasma taken at 55-125 min. after the drug application. In healthy volunteers peak plasma concentration of cyclopentolate, 2.06+/-0.86 (mean+/-S.D.) nM, occurred at 53 min., maximum receptor occupancy being 5.9+/-2.1%. The maximum pupillary dilatation occured at 30 min. after the drug application. At the same time the near point of vision was extended to more than 50 cm in all subjects. After topical application plasma receptor occupancy was not high enough to cause an...Continue Reading

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Citations

Jan 8, 2004·Journal of Cataract and Refractive Surgery·Björn Lundberg, Anders Behndig
Nov 16, 2007·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Anders Behndig
Oct 30, 2010·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Eun Chul KimMan Soo Kim
Feb 13, 2010·Cutaneous and Ocular Toxicology·Hasan Basri CakmakSaban Simsek
Aug 27, 2013·American Journal of Ophthalmology·Daniel J SalchowFangyong Li
Mar 27, 2004·Acta Ophthalmologica Scandinavica·Anders Behndig, Anders Eriksson
Nov 26, 2015·Journal of Cataract and Refractive Surgery·Fatemeh ShamsDavid Mansfield
Aug 20, 2015·Journal of Cataract and Refractive Surgery·Anders Behndig, Jean-François Korobelnik
May 10, 2016·Current Eye Research·Anita MitchellHoward Hendrickson
Dec 7, 2017·Indian Journal of Ophthalmology·Boris Malyugin
Sep 18, 2017·Journal of Cataract and Refractive Surgery·Amelia Lim Lay SuanVanessa Naseem Mansurali
Dec 27, 2006·Journal of Cataract and Refractive Surgery·Aminollah NikeghbaliMohsen Bahmani Kashkouli
Sep 17, 2019·Clinical & Experimental Ophthalmology·Luzia MüllerAnthony P Wells
Nov 7, 2019·Current Opinion in Ophthalmology·Neal H Shorstein, William G Myers
Jun 6, 2017·Asia-Pacific Journal of Ophthalmology·Li Sar TeohMae-Lynn Catherine Bastion

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