dorzolamide and apraclonidine

Significant advances have recently been achieved in the development of topical glaucoma medications. The primary advantage of a topical preparation is the reduced incidence of adverse systemic effects attributable to a given drug compared to its systemically administered counterpart. However, the strong protective barrier of the eye forces topical ophthalmic preparations to be highly concentrated and in some cases, they have the potential to produce unwanted systemic effects, particularly in smaller animals. Oral carbonic anhydrase inhibitors are commonly associated with adverse effects in both humans and animals. Two recently developed topical carbonic anhydrase inhibitors, dorzolamide and brinzolamide, have shown promise in reducing intraocular pressure in animals and systemic side effects are apparently limited with their use. The topical alpha2-agonist apraclonidine, on the other hand, effectively reduces intraocular pressure in cats and dogs, but in its currently available form is likely to induce unwanted systemic effects. Latanoprost is a topical prostaglandin F2alpha analog that has proven effective in reducing intraocular pressure in dogs and horses, but while systemic side effects have not yet been reported, this topical preparation may exacerbate pre-existing or concurrent ocular inflammatory disease.

Topics: Administration, Topical; Animals; Cat Diseases; Cats; Clonidine; Dog Diseases; Dogs; Glaucoma; Humans; Latanoprost; Ophthalmic Solutions; Prostaglandins F, Synthetic; Sulfonamides; Thiazines; Thiophenes

Primary open-angle glaucoma is a condition associated with an elevated intraocular pressure (IOP) that is defined as optic degeneration with a slowly progressive deterioration of the visual field that may lead to blindness. More than 1 million Americans are being treated for glaucoma, and 80,000 are legally blind as a result of the disease. Glaucoma has its highest prevalence among the elderly population, with an incidence of approximately 1% in those older than 60 years, 3% in those between the ages of 70 and 80 years, and more than 9% in those older than 80 years. Treatment is directed at lowering high ocular pressures. The initial treatment, in most cases topical therapy with a beta-adrenergic blocking agent, reduces the IOP to help preserve sight. But such topical agents may also have adverse systemic effects on cardiac, pulmonary, central nervous system (CNS), and endocrine functions.

Topics: Adrenergic beta-Antagonists; Brimonidine Tartrate; Cardiovascular System; Central Nervous System; Clonidine; Glaucoma, Open-Angle; Humans; Intraocular Pressure; Latanoprost; Neurosecretory Systems; Ophthalmic Solutions; Prostaglandins F, Synthetic; Quinoxalines; Respiratory System; Sulfonamides; Thiophenes

Glaucoma is in most of cases initially treated with drugs, viz. beta-blocking agents, miotics, sympathicomimetics and carbonic anhydrase inhibitors. The therapy of first choice is a beta-blocking agent, but in approximately 50% of the patients treated the effect becomes inadequate with time and combination therapy is necessary. Recently, four new antiglaucomatous agents have become available: apraclonidine, brimonidine, dorzolamide and latanoprost. Apraclonidine, an alpha 2-adrenergic agonist, is indicated for brief episodes of postlaser rise of the intraocular pressure. Longer treatment may lead to tolerance. Brimonidine, another alpha 2-adrenergic agonist, is indicated for long-term treatment of glaucoma; tolerance does not often occur. Dorzolamide is a local carbonic anhydrase inhibitor which lacks the systemic side effects seen after oral administration of carbonic anhydrase inhibitors. Latanoprost, a prostaglandin F2 alpha-derivative induces an effective decrease of the intraocular pressure if administered as monotherapy and has a good efficacy when combined with other drugs lowering the intraocular pressure. The new antiglaucomatous agents are a welcome addition to the pharmacotherapy, since in many cases they make it possible to postpone or avoid surgery.

Topics: Administration, Oral; Administration, Topical; Adrenergic alpha-Agonists; Brimonidine Tartrate; Carbonic Anhydrase Inhibitors; Clonidine; Drug Therapy, Combination; Female; Glaucoma; Humans; Latanoprost; Male; Prostaglandins F, Synthetic; Quinoxalines; Sulfonamides; Thiophenes

Topics: Adrenergic alpha-Agonists; Carbonic Anhydrase Inhibitors; Clonidine; Glaucoma, Open-Angle; Humans; Intraocular Pressure; Latanoprost; Prostaglandins F, Synthetic; Sulfonamides; Thiophenes; Treatment Outcome

Glaucoma is a potentially blinding disease. The goal of glaucoma therapy is to reduce intraocular pressure to a predetermined target level. There are currently 5 classes of compounds used for the medical management of glaucoma. Four classes that appear promising for the long term management of glaucoma are in different phases of clinical investigation, and include the topically active carbonic anhydrase inhibitors, selective alpha 2-adrenergic agonists, prostaglandins and ethacrynic acid. The topically active carbonic anhydrase inhibitor dorzolamide (MK-507) is effective and well tolerated in clinical trials of up to 1 year's duration. Animal studies have demonstrated that this drug lowers intraocular pressure by reducing aqueous humour formation. The selective alpha 2-adrenergic agonists, brimonidine and apraclonidine, have been shown to be effective in reducing intraocular pressure in the short term. Long term effectiveness of these agents is under investigation. Prostaglandins (PG) of the PGF2-alpha isopropylester series caused marked reductions of intraocular pressure in laboratory and clinical trials. The newest prostaglandin analogue, latanoprost (PhXA41), effectively lowered intraocular pressure and was well tolerated in clinical trials of up to 4 weeks' duration. Prostaglandins reduce intraocular pressure by enhancing uveoscleral outflow. Ethacrynic acid enhanced traditional outflow facility and lowered intraocular pressure when applied topically or intracamerally in laboratory studies and clinical trials. Corneal adverse effects of ethacrynic acid have been noted. Reformulation of ethacrynic acid ointment may resolve this problem. These 4 classes of compounds will enhance our options for the medical management of glaucoma. They may be used instead of or in combination with some of the drugs currently in use, and may be better tolerated.

Topics: Administration, Topical; Adrenergic alpha-Agonists; Brimonidine Tartrate; Carbonic Anhydrase Inhibitors; Clonidine; Ethacrynic Acid; Glaucoma; Humans; Latanoprost; Prostaglandins; Prostaglandins F, Synthetic; Quinoxalines; Sulfonamides; Thiophenes

Topics: Administration, Topical; Antihypertensive Agents; Betaxolol; Clonidine; Epinephrine; Glaucoma; Humans; Intraocular Pressure; Levobunolol; Prospective Studies; Sulfonamides; Thiophenes; Visual Field Tests

To evaluate the efficacy of dorzolamide compared to apraclonidine, in the prevention of the intra-ocular pressure (IOP) spike after Nd :YAG laser posterior capsulotomy. SITE: Department of Ophthalmology, State University of Campinas (UNICAMP) General Hospital, Campinas, São Paulo, Brazil.. In a double masked prospective clinical trial, 217 eyes from 217 patients were randomly assigned to receive either dorzolamide 2 h before and placebo 1 h before Nd : YAG laser capsulotomy or placebo 2 h before and apraclonidine 1 h before the procedure. Inclusion criteria were secondary cataracts with reduction in best corrected visual acuity (BCVA < 20/40), absence of manifest or suspected glaucoma and no known hypersensitivity to the study drugs. IOP was measured 2 h and 1 h before applying the laser, and 1 h, 2 h, 3 h and 7 days after.. There were no statistically significant differences between the two groups regarding the IOP 2 h and 1 h before the procedure, and 1 h, 2 h, 3 h and 7 days after the laser treatment (p values, respectively: 0.077, 0.21, 0.085, 0.36, and 0.60).. The results of this study suggest that dorzolamide is as safe and effective as apraclonidine in the prevention of the IOP elevation after Nd : YAG laser posterior capsulotomy. Synopsis. The efficacy of dorzolamide was compared to apraclonidine in the prevention of the intraocular pressure spike after Nd : YAG laser posterior capsulotomy in 217 patients and the results were similar with both drugs.

Topics: Adrenergic alpha-Agonists; Adult; Aged; Aged, 80 and over; Carbonic Anhydrase Inhibitors; Clonidine; Double-Blind Method; Female; Humans; Intraocular Pressure; Laser Therapy; Male; Middle Aged; Ocular Hypertension; Prospective Studies; Sulfonamides; Thiophenes; Time Factors

To determine whether topical aqueous suppressant therapy applied after pars plana vitrectomy with gas tamponade prevents postoperative intraocular pressure (IOP) elevation.. Prospective, nonrandomized comparative study.. Forty-one patients who met inclusion criteria and underwent pars plana vitrectomy with gas tamponade (SF6 18%-20% or C3F8 12%-16%) over a 1-year period.. Treatment eyes received topical aqueous suppressants at the end of surgery.. Postoperative IOP at 4 to 6 hours, 1 day, and 1 week.. Twenty-one control and 20 treatment eyes met the inclusion criteria. The IOP (in mmHg) measured at 4 to 6 hours (23.05 [control, 14.73 [treatment]) and 1 day (23.24 [control], 17.28 [treatment]) postoperatively showed a statistically significant difference between the groups (P = 0.0038) at 4 to 6 hours and a trend toward significance (P = 0.057) at 1 day. Eleven control and three treatment eyes had an IOP spike above 25 mmHg at 4 to 6 hours or 1 day postoperatively (P = 0.02), and six control eyes and one treatment eye had postoperative IOP greater than 30 mmHg. A pressure rise greater than 40 mmHg was seen in two control eyes and no treatment eyes.. Use of topical aqueous suppressants after pars plana vitrectomy with long-acting gas tamponade is effective in preventing significant postoperative IOP elevation in most cases.

Topics: Administration, Topical; Antihypertensive Agents; Aqueous Humor; Brimonidine Tartrate; Clonidine; Fluorocarbons; Humans; Intraocular Pressure; Ocular Hypertension; Prospective Studies; Quinoxalines; Sulfonamides; Sulfur Hexafluoride; Thiophenes; Timolol; Vitrectomy

To compare the effectiveness of 2% dorzolamide and 0.5% apraclonidine on intraocular pressure (IOP) following phacoemulsification cataract surgery.. This prospective, randomised study comprised 54 eyes of 27 consecutive patients with age-related cataract scheduled for cataract surgery in both eyes. In each patient the eye with the higher degree of cataract was randomly assigned to receive one drop of either dorzolamide or apraclonidine immediately after surgery. The fellow eye was operated on later and received the other treatment. Cataract surgery was performed with a superior 6.0 mm sutureless frown incision, phacoemulsification and implantation of a three-piece PMMA intraocular lens. The IOP was measured pre-operatively as well as 6 h and 20-24 h and 1 week post-operatively.. The mean pre-operative IOP was not significantly different between the groups (dorzolamide group, 14.9 +/- 2.3 mmHg; apraclonidine group, 14.6 +/- 2.5 mmHg; p = 0.450). At 6 h post-operatively, the mean IOP was significantly lower in the dorzolamide than in the apraclonidine group (15.6 +/- 3.9 mmHg vs 18.0 +/- 4.0 mmHg; p < 0.001). An IOP increase of more than 5 mmHg at 6 h post-operatively occurred in 3 (12%) eyes in the dorzolamide group and in 9 (36%) eyes in the apraclonidine group (p = 0.034). At 20-24 h post-operatively and at 1 week post-operatively no difference was found between the groups.. 2% Dorzolamide is more effective than 0.5% apraclonidine in preventing the early post-operative IOP increase following phacoemulsification cataract surgery.

Topics: Adrenergic alpha-Agonists; Aged; Aged, 80 and over; Antihypertensive Agents; Carbonic Anhydrase Inhibitors; Clonidine; Female; Humans; Male; Middle Aged; Ocular Hypertension; Phacoemulsification; Prospective Studies; Sulfonamides; Thiophenes

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Capecitabine; Carbamates; Ceftriaxone; Clonidine; Deoxycytidine; Diagnosis, Differential; Drug Eruptions; Ethacridine; Female; Fluorouracil; Humans; Immunosuppressive Agents; Indapamide; Isotretinoin; Isoxazoles; Leflunomide; Male; Middle Aged; Nelfinavir; Phenylcarbamates; Rivastigmine; Salicylates; Severity of Illness Index; Sulfonamides; Thiophenes

Topics: Adrenergic alpha-Agonists; Brimonidine Tartrate; Carbonic Anhydrase Inhibitors; Clonidine; Drug Approval; Female; Glaucoma; Humans; Intraocular Pressure; Latanoprost; Male; Netherlands; Prostaglandins F, Synthetic; Quinoxalines; Sulfonamides; Thiophenes

To evaluate the effect of topical aqueous humor suppressants on the absorption of intravitreal perfluorocarbon gases.. Sulfur hexafluoride or perfluoropropane was injected intravitreally in five rabbits. Time to gas disappearance was measured in eyes treated with topical aqueous humor suppressants and in those not treated.. The mean time (+/- SD) to disappearance of 0.4 cc of sulfur hexafluoride was 5.6 +/- 0.9 days, which was prolonged by 43% to 8.0 +/- 0.7 days with topical aqueous humor suppressants (P = .009). The mean time (+/- SD) to disappearance of 0.2 cc of perfluoropropane was 18.4 +/- 1.9 days, which was prolonged by 55% to 28.6 +/- 2.7 days with topical aqueous humor suppressants (P = .009).. Aqueous suppressants prolong sulfur hexafluoride and perfluoropropane intravitreal gas bubble duration in rabbits.

Topics: Absorption; Administration, Topical; Animals; Aqueous Humor; Clonidine; Fluorocarbons; Injections; Intraocular Pressure; Rabbits; Sulfonamides; Sulfur Hexafluoride; Thiophenes; Time Factors; Timolol; Vitreous Body

To report a case of glaucomatocyclitic crisis (Posner-Schlossman syndrome) in a child.. Case report. A 13-year-old boy presented with decreased vision, photophobia, halos, and pain in the right eye.. Findings in this child were consistent with a diagnosis of Posner-Schlossman syndrome.. Glaucomatocyclitic crisis can occur in a child and must be included in the differential diagnosis of uveitis and glaucoma in pediatric patients.

Topics: Adolescent; Clonidine; Corneal Edema; Diagnosis, Differential; Drug Therapy, Combination; Glaucoma; Humans; Intraocular Pressure; Male; Pain; Prednisolone; Sulfonamides; Syndrome; Thiophenes; Timolol; Uveitis, Intermediate; Vision Disorders; Visual Acuity

Topics: Adrenergic alpha-Agonists; Antihypertensive Agents; Brimonidine Tartrate; Carbonic Anhydrase Inhibitors; Clonidine; Drug Therapy, Combination; Glaucoma, Open-Angle; Humans; Latanoprost; Prostaglandins F, Synthetic; Quinoxalines; Sulfonamides; Thiophenes; Treatment Outcome

To measure under carefully controlled conditions the effects in the rabbit eye of commonly used therapeutic agents for glaucoma.. Rabbits were outfitted in one eye with an implantable telemetric pressure transducer and monitored for several months under controlled conditions of light/ dark and handling. Effects of tonometry, handling, water drinking, and instillation of topical ophthalmic medications on intraocular pressure were recorded during each 24-hour day/night cycle.. Pneumatonometry, animal handling, and water drinking all had an effect on intraocular pressure that in many instances was of the same magnitude as the effects of pharmacologic agents. Dorzolamide and timolol caused a sustained reduction of intraocular pressure during the nocturnal period. Epinephrine had a biphasic effect, causing an immediate pressure elevation followed by a prolonged depression. Apraclonidine, latanoprost, and pilocarpine had no measurable effect.. Continuous telemetric measurement of intraocular pressure in rabbits permits the measurement of uncontrollable artifacts that occur with tonometric measurements and animal handling. If environmental conditions are rigidly controlled, this method is very sensitive for detecting therapeutic effects of candidates for ocular hypotensive drugs. When healthy animals are used, the method appears to be more sensitive for drugs that affect aqueous humor formation than for drugs that affect aqueous humor outflow resistance.

Topics: Animal Husbandry; Animals; Circadian Rhythm; Clonidine; Epinephrine; Intraocular Pressure; Latanoprost; Ophthalmic Solutions; Pilocarpine; Prostaglandins F, Synthetic; Rabbits; Sulfonamides; Telemetry; Thiophenes; Timolol; Tonometry, Ocular