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The mechanisms of drug clearance from the aqueous humor are poorly defined. In this study, a cocktail approach was used to simultaneously determine the pharmacokinetics of three beta blocker agents after intracameral (i.c.) injection into the rabbit eyes. Aqueous humor samples were collected and analyzed using LC-MS/MS to determine drug concentrations. Pharmacokinetic parameters were obtained using a compartmental fitting approach and the estimated clearance, volume of distribution and half-life values were: atenolol (6.44 µL/min, 687µL and 73.87 min), timolol (19.30 µL/min, 937 µL and 33.64 min) and betaxolol (32.20 µL/min, 1421 µL and 30.58 min). Increased compound lipophilicity (atenolol < timolol < betaxolol) resulted in higher clearance and volume of distributions in the aqueous humor. Clearance of timolol and betaxolol is about ten times higher than the aqueous humor outflow, demonstrating the importance of other elimination routes (e.g. uptake to iris and ciliary body, and subsequent elimination via blood flow).
This article was published in the following journal.
Name: Molecular pharmaceutics
Preclinical in vivo tests of retinal drug responses are carried out in mice and rats, often after intravitreal injections. However, quantitative pharmacokinetics in the mouse eye is poorly understood....
There is a limit beyond which increasing either the concentration of a prostaglandin analog (PGA) or its dosing frequency fails to produce increases in ocular hypotensive efficacy with topical dosing....
PRéCIS:: Noninferiority of efficacy was demonstrated for a preservative-free latanoprost-timolol fixed combination compared with a BAK-containing formulation at 84 days after treatment in patients wi...
Glaucoma is a group of irreversible ocular diseases which result in damage to the optic nerve and vision loss. The objective of the present work was to develop micelles-laden contact lenses (CLs-M) th...
Background Subtenon anticancer drugs are given as an adjunct to systemic chemotherapy for conditions like retinoblatoma. This study evaluated the ocular kinetics of nano-emulsion formulation of etopos...
To evaluate the safety and efficacy of BETOPTIC S and Timolol Gel-forming solution in pediatric patients. Patients will dose with study drug at 8 am and 8 pm daily for twelve weeks. Patien...
Eligible patients will be randomized in a 1:1 ratio to receive Travoprost 0.004% / Timolol, once daily or Timolol 0.5%, twice-daily, for a total of twelve weeks. The study treatments will...
The purpose of this study is to demonstrate that fixed combination of latanoprost and timolol (PhXA41) has better IOP lowering effect than the individual monotherapies.
Study PhXA41 for its non-inferiority compared with timolol in lowering intra-ocular pressure
Safety and efficacy study comparing between fixed combination latanoprost-timolol and its component parts.
A beta-adrenergic antagonist similar in action to PROPRANOLOL. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
A pharmaceutical preparation of brimonidine tartrate and timolol maleate. The combined ADRENERGIC ALPHA2 RECEPTOR AGONIST and ADRENERGIC BETA-ANTAGONIST activity of these drugs reduce INTRAOCULAR PRESSURE in GLAUCOMA patients.
Ocular manifestations secondary to various NEOPLASMS in which antibodies to antigens of the primary tumor cross-react with ocular antigens. This autoimmune response often leads to visual loss and other ocular dysfunctions.
The dioptric adjustment of the EYE (to attain maximal sharpness of retinal imagery for an object of regard) referring to the ability, to the mechanism, or to the process. Ocular accommodation is the effecting of refractive changes by changes in the shape of the CRYSTALLINE LENS. Loosely, it refers to ocular adjustments for VISION, OCULAR at various distances. (Cline et al., Dictionary of Visual Science, 4th ed)
Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...
Ophthalmology is the branch of medicine that is devoted to the study and treatment of eye diseases. As well as mild visual defects correctable by lenses, ophthalmology is concerned with glaucoma, uveitis and other serious conditions affecting the eye, ...
Multiple Sclerosis MS
Multiple sclerosis (MS) is the most common disabling neurological condition affecting 100,000 young adults in the UK. The condition results from autoimmune damage to myelin, causing interference in nerve signaling. Symptoms experienced depend on the pa...