dorzolamide and Eye-Diseases

To characterize and compare the ocular comfort and symptoms of dorzolamide and tear-replacement drops (placebo) in healthy volunteers.. Subjects were randomized in a double-masked fashion to receive each medicine for 6 days twice daily. Patients used a visual analog scale to assess the quality and intensity of pain temporally after initial (acute) dosing and after 6 days of chronic dosing. The visual analog scale, an objective measure of pain, allows a subject to grade their perceived intensity of pain on a line between 0 and 100 mm.. Of 28 subjects enrolled in the study, 27 completed the protocol (1 subject was lost to follow-up). Dorzolamide demonstrated statistically greater peak ocular pain (21.4 +/- 22.3 mm) compared with placebo (1.9 +/- 4.4 mm) (P<0.0001) after chronic dosing. Time of mean peak pain for dorzolamide products was 15 seconds after dosing. The pain was statistically greater with dorzolamide compared with placebo for 50 seconds after dosing. On average the discomfort associated with dorzolamide lasted 38.9 +/- 17.9 seconds after dosing. The average pain per second for the first minute was 7.1 +/- 10.1 mm for dorzolamide. No differences in pain intensity were observed after acute and chronic dosing. The discomfort with dorzolamide was characterized after chronic dosing as "burning" (14.8 +/- 25.0 mm) and was associated with tearing (1.9 +/- 5.2 mm).. Dorzolamide caused more ocular pain after instillation than placebo. However, the pain was characterized as mild and quickly resolved.

Topics: Acute Disease; Adult; Carbonic Anhydrase Inhibitors; Chronic Disease; Double-Blind Method; Eye Diseases; Female; Humans; Male; Ophthalmic Solutions; Pain; Pain Measurement; Sulfonamides; Thiophenes; Time Factors

Ocular diseases are very common in many of the systemic diseases such as sarcoidosis, and may sometimes be the presenting symptom of the disease. In this case report, we present an unusual reaction of the sarcoid granuloma to carbonic anhydrase enzyme inhibitors (CAIs), which was encountered in a patient with ocular sarcoidosis. This observation was taken after a 2-week interval between a CT scan orbits and an MRI orbits which showed a decrease in size from 4×3×4 cm to 2.5×2.5×2 cm, respectively. We suspected the dorzolamide CAI to have had a significant role in the reduction in size. It is suggested that acidotic changes that occur due to the effect of the carbonic anhydrase inhibitor causes electrolyte imbalance, intracellular as well as extracellular, which lead to the reduction in the size of the granuloma.

Topics: Carbonic Anhydrase Inhibitors; Eye Diseases; Female; Humans; Magnetic Resonance Imaging; Middle Aged; Sarcoidosis; Sulfonamides; Thiophenes

Dilutable nanoemulsions are potent drug delivery vehicles for ophthalmic use due to their numerous advantages as sustained effect and high ability of drug penetration into the deeper layers of the ocular structure and the aqueous humor. The aim of this article was to formulate the antiglaucoma drug dorzolamide hydrochloride as ocular nanoemulsion of high therapeutic efficacy and prolonged effect. Thirty-six systems consisting of different oils, surfactants, and cosurfactants were prepared and their pseudoternary-phase diagrams were constructed by water titration method. Seventeen dorzolamide hydrochloride nanoemulsions were prepared and evaluated for their physicochemical and drug release properties. These nanoemulsions showed acceptable physicochemical properties and exhibited slow drug release. Draize rabbit eye irritation test and histological examination were carried out for those preparations exhibiting superior properties and revealed that they were nonirritant. Biological evaluation of dorzolamide hydrochloride nanoemulsions on normotensive albino rabbits indicated that these products had higher therapeutic efficacy, faster onset of action, and prolonged effect relative to either drug solution or the market product. Formulation of dorzolamide hydrochloride in a nanoemulsion form offers, thus, a more intensive treatment of glaucoma, a decrease in the number of applications per day, and a better patient compliance compared to conventional eye drops.

Topics: Animals; Aqueous Humor; Carbonic Anhydrase Inhibitors; Cornea; Drug Delivery Systems; Drug Stability; Emulsions; Eye Diseases; Glaucoma; Hydrogen-Ion Concentration; Irritants; Male; Nanoparticles; Ophthalmic Solutions; Osmolar Concentration; Particle Size; Rabbits; Rheology; Solubility; Sulfonamides; Surface Tension; Thiophenes; Viscosity

Topics: Aged; Critical Care; Drug Therapy, Combination; Eye Diseases; Female; Glaucoma, Open-Angle; Humans; Metronidazole; Ophthalmic Solutions; Pheniramine; Prednisolone; Stevens-Johnson Syndrome; Sulfonamides; Thiophenes