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GLAUCOMA
ABSTRACTS

Aqueous humour and serum zinc and copper concentrations of patients with glaucoma and cataract
Akyol N.; Deger O.; Keha E.E.; Kilic S.
Dept of Ophthalmology, Faculty of Medicine, Karadeniz Tech University,61080 Trabzon Turkey
British Journal of Ophthalmology (United Kingdom) 1990, 74/11 (661-662)

Serum and aqueous humour zinc and copper concentrations of 44 patients with glaucoma and cataract were determined. Serum values were found within normal ranges. The highest mean copper concentration was seen in the glaucoma group. In addition there was a significant negative correlation between the aqueous humour levels of zinc and copper in patients with glaucoma. It was concluded that an increased copper value together with a low zinc value might be of importance in patients with glaucoma.

Analysis of the medical use of marijuana and its societal implications
Taylor HG
Sparrow Hospital, Lansing, Michigan 48826, USA
hgtaylor@pilot.msu.edu
J Am Pharm Assoc (Wash) (U S) Mar-Apr 1998, 38 (2) p220-7

OBJECTIVE: To review the pharmacology, therapeutics, adverse effects, and societal implications of the medical use of marijuana.

DATA SOURCES: MEDLINE and manual searches of English-language marijuana literature, supplemented with interviews of scientists currently conducting cannabinoid research. Search terms included pain OR palliative care AND cannabis or ALL marijuana; cachexia OR appetite OR appetite stimulants; muscle spasticity OR spasm; immune system and cannabis; nausea and vomiting and cancer and cannabis. MEDLINE search terms: cannabis OR marijuana smoking OR marijuana abuse; all glaucoma ; multiple sclerosis AND cannabis OR marijuana smoking OR marijuana abuse.

STUDY SELECTION: Studies on pharmacology, risks, and medical potential of marijuana.

DATA EXTRACTION: Not applicable.

DATA SYNTHESIS: The most prominent effects of marijuana are mediated by receptors in the brain. Acute intoxication is characterized by euphoria, loss of short-term memory, stimulation of the senses, and impaired linear thinking. Depersonalization and panic attacks are adverse effects. Increased heart rate and reddened conjunctivae are common physical effects. Chronic, high doses may cause subtle impairment of cognitive abilities that are appear to be long-term, but of unknown duration. Marijuana may be a risk factor for individuals with underlying mental illness. It causes dependence, but compared with cocaine, alcohol, heroin, and nicotine, marijuana has little addictive power and produces only mild withdrawal symptoms. Marijuana shows clinical promise for glaucoma, nausea and vomiting, analgesia, spasticity, multiple sclerosis, and AIDS wasting syndrome.

CONCLUSION: As a recreational drug, marijuana poses dangers, particularly to social and emotional development during adolescence and young adulthood. As a medical drug, marijuana should be available for patients who do not adequately respond to currently available therapies. (57 Refs.)

Glycerol: Biochemistry, pharmacokinetics and clinical and practical applications
Robergs R.A.; Griffin S.E.
Dr. R.A. Robergs, Ctr. Exercise Applied Human Physiol., Johnson Center, University of New Mexico, Albuquerque, NM 87131 United States
Sports Medicine (New Zealand), 1998, 26/3 (145-167)

Glycerol is a naturally occurring 3-carbon alcohol in the human body. It is the structural backbone of triacylglycerol molecules, and can also be converted to a glycolytic substrate for subsequent metabolism. Serum glycerol concentrations approximate 0.05 mmol/L at rest, and can increase to 0.30 mmol/L during increased lipolysis associated with prolonged exercise or caloric restriction. When glycerol is ingested or infused at doses greater than 1.0 g/kg bodyweight, serum concentrations can increase to approximately 20 mmol/L, resulting in more than a 10 mOsmol/kg increase in serum osmolality. Glycerol infusion and ingestion have been used in research settings for almost 60 years, with widespread clinical use between 1961 and 1980 in the treatment of cerebral oedema resulting from acute ischaemic stroke, intraocular hypertension ( glaucoma ), intracranial hypertension, postural syncope and improved rehydration during acute gastrointestinal disease. Since 1987, glycerol ingestion with added fluid has been used to increase total body water (glycerol hyperhydration) by up to 700 ml, thereby providing benefits of improved thermoregulation and endurance during exercise or exposure to hot environments. Despite the small number of studies on glycerol hyperhydration and exercise, it appears to be an effective method of improving tolerance to exercise and other heat-related stressors.

Medicinal marijuana: A comprehensive review
Gurley R.J.; Aranow R.; Katz M.
Dr. R.J. Gurley, San Francisco Dept. of Public Health, 25 Van Ness, San Francisco, CA 94102
Journal of Psychoactive Drugs (United States), 1998, 30/2 (137-147)

Considerable controversy exists regarding the role of marijuana as a therapeutic agent; however, many practitioners are taught very little about existing marijuana data. The authors therefore undertook a comprehensive literature review of the topic. References were identified using textbooks, review and opinion articles, and a primary literature review in MEDLINE. Sources were included in this review based primarily on the quality of the data. Some data exists that lends credence to many of the claims about marijuana's properties. In general, however, the body of literature about marijuana is extremely poor in quality. Marijuana and/or its components may help alleviate suffering in patients with a variety of serious illnesses. Health care providers can best minimize short term adverse consequences and drug interactions for terminally ill patients by having a thorough understanding of the pharmacology of marijuana, potential adverse reactions, infection risks, and drug interactions (along with on-going monitoring of the patient). For chronic conditions, the significance and risk of short and long term adverse effects must be weighed against the desired benefit. Patients who are best suited to medicinal marijuana will be those who will gain substantial benefit to offset these risks, and who have failed a well- documented, compliant and comprehensive approach to standard therapies.

Vitamins Binf 1 and PP in treating glaucomatous patients (Russian)
Zhukovsky V.S.
Kaf. Glazn. Bol., Fak. Usover. Vrachej, Med. Inst., L'vov Russia
Vestnik Oftalmologii 1974, No.3/- (19-21)

The supply of and demand for thiamine were studied in 142 glaucomatous patients. Thiamine deficiency was found in all these patients, being however more pronounced in cases of secondary and congestive glaucoma and after antiglaucomatous operations. Seasonal fluctuations in the supply were recorded. In winter and spring the thiamine dosages administered daily were 8 mg parenterally and 12 mg orally, while in summer and fall they were 6 and 10 mg, respectively. With these doses saturation of the body supervened on the 2nd to 4th day in cases of simple glaucoma and on the 4th to 6th day during glaucoma attacks and after surgery. An improvement of visual functions could then be observed.

Blood levels of thiamine and ascorbic acid in chronic open-angle glaucoma.
Asregadoo ER
Ann Ophthalmol (United States) Jul 1979, 11 (7) p1095-1100

Blood levels of thiamine and ascorbic acid in chronic open-angle glaucoma are determined in this study. Dietary vitamin intake was compared with thiamine and ascorbic acid blood levels in a sample of 38 patients with glaucoma and 12 controls. These patients had a statistically significant lower thiamine blood level than controls (P less than 0.001), but no significant difference was found for ascorbic acid blood levels. Poor absorption of thiamine occurred in the glaucomatous patients in this study.

Glaucoma, capillaries and pericytes 3. Peptide hormone binding and influence on pericytes
Ferrari-Dileo G.; Davis E.B.; Anderson D.R.
Bascom Palmer Eye Institute, PO Box 016880, Miami, FL 33101-6880 USA
Ophthalmologica (Switzerland), 1996, 210/5 (269-275)

To test the potential for vasoactive neuropeptide receptors to affect capillary resistance, we have begun to study the plausibiIity that pericytes might be equipped to respond to a representative peptide vasoconstrictor and a representative peptide vasodilator. Pericytes cultured from the bovine retinal vasculature specifically bind the angiotensin II (Ang II) antagonist saralasin (1 nM 125I-saralasin bound at 2.2plus or minus0.41 fmol/mg protein) and 125I-vasoactive intestinal peptide (VIP; K(d) of 0.5 nM with a population of 30 fmol/mg protein). Incubation with 100 microM Ang II induced minimal cAMP synthesis, while VIP (1 microM, 100 microM) did not induce any change in cAMP concentration. Ang II (10 microM and 100 microM) caused contraction of pericytes cultured on an elastic silicone surface. Circulating or locally produced vasoactive neuropeptides might affect pericyte contractile tone via several intracellular pathways, moderated by indirect effects of these peptides through endothelial stimulation, with the net effect on local blood flow resulting from the effects on arteries and veins as well as capillaries.

Cultured human trabecular meshwork cells express functional alpha 2A adrenergic receptors.
Stamer WD; Huang Y; Seftor RE; Svensson SS; Snyder RW; Regan JW
Department of Pharmacology/Toxicology, University of Arizona, Tucson 85721, USA.
Invest Ophthalmol Vis Sci (United States) Nov 1996, 37 (12) p2426-33

PURPOSE: For the treatment of glaucoma, alpha-2 adrenergic receptor (alpha 2-AR) agonists are thought to lower intraocular pressure primarily by decreasing aqueous humor production. Effects on the outflow pathways, however, also may occur. To begin to examine this possibility, the authors characterized the alpha 2-AR subtypes present in cultures of human trabecular meshwork (HTM) cells using both immunofluorescence microscopy and functional measures of alpha 2-AR activation.

METHODS: For immunofluorescence microscopy, subtype-specific polyclonal antibodies that recognize each of the human alpha 2-AR subtypes (alpha 2A, alpha 2B, alpha 2C) were used. Functional studies involved the inhibition of forskolin-stimulated cyclic adenosine monophosphate (cAMP) production, the stimulation of mitogen-activated protein (MAP) kinase activity, and the stimulation of mitotic activity as reflected by the expression of proliferating cell nuclear antigen (PCNA).

RESULTS: From the immunofluorescence microscopy, there was evidence for the presence of the alpha 2A subtype, but not alpha 2B or alpha 2C subtype, on HTM cells. The administration of the alpha 2-agonist, dexmedetomidine, to HTM cells resulted in a 90% inhibition of forskolin-stimulated cAMP formation, a twofold stimulation of MAP kinase activity, and a threefold increase in the expression of PCNA. Additionally, preincubation of cells with either of the alpha 2-AR-selective antagonists, rauwolscine or atipamezole, reversed the functional effects of dexmedetomidine.

CONCLUSIONS: Functional alpha 2A-ARs are present on HTM cells where they may affect the outflow pathway during the treatment of glaucoma with alpha 2-AR agonists.

Neurotransmitters and intraocular pressure
Lapalus P.; Elena P.P
Fundam. Clin. Pharmacol. (France), 1988, 2/4 (305-325)

The role of the ocular autonomic nervous system in IOP regulation has been well established. Pharmacological and autohistoradiographic studies confirmed the high density of beta2 and alpha2 receptors on ciliary processes and iris epithelium. Their respective pharmacological activation or blockade is discussed. The role of other ocular neurotransmitters is also complex, as shown by the paradoxical similar action of dopamine agonists and antagonists on IOP. Concerning the cholinergic system, ocular muscarinic receptors are pharmacologically not well documented. Numerous other neurotransmitters may modulate IOP without necessarily leading to the development of new drugs. Drugs of the future will probably concentrate on dopaminergic agonists, cAMP-stimulators such as forskolin, prostaglandins, and cannabinoids.

HP 663: A novel compound for the treatment of glaucoma
Hartman H.B.; Roehr J.E.; Kotyuk B.L.; Kosley R.W. Jr.; Cherill R.J.; Petko W.W.; Conway P.G.
Department of Biological Research, Hoechst-Roussel Pharmaceuticals, Somerville, NJ 08876 USA
Drug Dev. Res. (USA), 1988, 12/3-4 (197-209)

Various studies suggest that the 7-dihydroxypropionyl derivative of forskolin, HP 663, effectively lowers intraocular pressure (IOP) by a novel mechanism. Biochemically, HP 663 stimulates rat striatal adenylate cyclase and displays an affinity for forskolin binding sites similar to that of forskolin. Following topical administration this compound lowers IOP in both New Zealand White (NZW) and Dutch Belt (DB) rabbits. In NZW rabbits, concentrations from 0.05 to 2.0% in a buffered hydroxypropylmethylcellulose (HPMC) vehicle produce significant reductions in outflow pressures of 35-45% for 5-6 hr. Additionally, HP 663 is soluble in this vehicle up to a concentration of 0.25%. As mentioned, HP 663 also reduces IOP in DB rabbits; however, this response is not significant until a concentration of 1% is attained. The effect on aqueous humor inflow was indirectly determined by studying the rate of IOP recovery following rapid i.v. infusion of 20% NaCl. In NZW rabbits, HP 663 significantly reduced aqueous humor inflow as shown by a 40% decrease in the IOP recovery rate compared to control. Tolerance also does not appear to develop to the IOP lowering effects of HP 663 in NZW rabbits. This compound is still capable of significantly lowering IOP following twice daily treatment for 21 consecutive days. Following topical administration of concentrations which effectively lower IOP, HP 663 exhibits no significant effects on heart rate or blood pressure of NZW rabbits. Therefore, this compound does not appear to exhibit a potential for peripheral side effects after topical application. Based on the results of the present study, HP 663 appears to be a potent activator of adenylate cyclase and may provide a novel and effective treatment for glaucoma

Intraocular pressure effects of multiple doses of drugs applied to glaucomatous monkey eyes
Lee P.-Y.; Podos S.M.; Serle J.B.; et al.
Department of Ophthalmology, Mount Sinai School of Medicine, New York, NY 10029 USA
Arch. Ophthalmol. (USA), 1987, 105/2 (249-252)

The effects of multiple dosing with 0.5% timolol maleate, 2% epinephrine hydrochloride, 4% pilocarpine hydrochloride, 1% vanadate, 1% forskolin (nonproprietary name, colforsin), or 0.5% prostaglandin F(2alpha) on intraocular pressure (IOP) were each tested on eight cynomolgus monkey eyes in which glaucoma was induced by photocoagulating the trabecular meshwork with the argon laser. The week prior to drug therapy, baseline IOP measurements were carried out at hourly intervals from 9:30 AM to 3:30 PM on three days. One to two days later, therapy was initiated. Each drug was applied topically to both eyes of each monkey twice daily for at least four days. The IOP was measured with a calibrated pneumatonometer at the same hourly intervals on treatment days as on the baseline days. The IOP at each time of day on treatment days was compared with the average baseline IOP measured at the corresponding time of day. Topical application of timolol, epinephrine, pilocarpine, vanadate, and prostaglandin F(2alpha) significantly reduced IOP without evidence of tolerance or tachyphylaxis during the course of therapy. Forskolin did not significantly decrease IOP after the second day of treatment.

Laser-induced glaucoma in rabbits
Gherezghiher T.; March W.F.; Nordquist R.E.; Koss M.C. Dean A.
McGee Eye Institute, Oklahoma City, OK 73104 USA
Exp. Eye Res. (UK), 1986, 43/6 (885-894)

Argon laser energy was applied to the trabecular meshwork of pigmented rabbits in an attempt to develop an animal model of 'glaucoma'. Laser energy was varied to determine the optimal level needed to produce sustained ocular hypertension. An initial response of ocular hypertension followed by hypotension was observed in all of the animals tested. Approximately half of the laser-treated rabbits developed a secondary buphthalmus and sustained ocular hypertension. In these animals outflow facility was decreased by approximately 60%. Histologic examination at 4-and 8 weeks after laser treatment demonstrated a wound-healing response resulting in closure of the intertrabecular spaces and obstruction of outflow to injected carbon particles. Optic nerve cupping and a loss of ganglion cells were also observed. Topical application of L-timolol (0.5%), pilocarpine (2.0%) and forskolin (1.0%) were found to be effective in decreasing intraocular pressure in the laser-treated, hypertensive eye with no significant effect in control non-laser-treated eyes, suggesting that this model can be a useful tool for screening potential antiglaucoma medications.

Regulation of aqueous flow by the adenylate cyclase receptor complex in the ciliary epithelium
Sears M.L.
Department of Ophthalmology and Visual Science, Yale University School of Medicine, New Haven, CT 06510 USA
Am. J. Ophthalmol. (USA), 1985, 100/1 (194-198)

The answer to how beta-adrenergic receptor mediates a fall in intraocular pressure has been elusive. Methods of measurement have not been refined sufficiently. The separate changes after adrenergic treatment frequently are small, and the tissue effects are multiple. On a molecular basis, stimulation of the beta-adrenergic receptor activates intracellular adenylate cyclase to produce increased cyclic adenosine monophosphate. Acting by different cell-receptor mechanisms, but nonetheless potent, nonadrenergic stimulators of adenylate cyclase in the ciliary epithelium, such as cholera toxin and organic fluorides, have been studied in experimental animals. They reduce intraocular pressure by reducing net aqueous flow. When forskolin, a diterpene and potent stimulator of adenylate cyclase, became available, it was used in noninvasive topical form in the human eye to clarify the question of whether increased cyclic adenosine monosphosphate reduces intraocular pressure and aqueous flow. Noninvasive studies in human eyes have demonstrated a 35% reduction in outflow pressure after the administration of forskolin in a 1% topical suspension, matched by a corresponding reduction in aqueous flow. Tonographic outflow facility was unaltered. Thus, the entire reduction in intraocular pressure can be accounted for by a reduction in net aqueous flow.

Forskolin suppresses sympathetic neuron function and causes ocular hypotension
Potter D.E.; Burke J.A.; Temple J.R.
Department of Pharmacology, Texas Tech University Health Sciences Center, Lubbock, TX 79430 USA
Curr. Eye Res. (England), 1985, 4/2 (87-96)

No abstract.

Forskolin lowers intraocular pressure by reducing aqueous inflow
Caprioli J.; Sears M.; Bausher L.; et al.
Department of Ophthalmology and Visual Science, Yale University School of Medicine, Box 3333, New Haven, CT 06510 USA
Invest. Ophthalmol. Visual Sci. (USA), 1984, 25/3 (268-276)

Forskolin is a diterpene derivative of the plant Coleus forskohlii that stimulates adenylate cyclase activity without interacting with cell surface receptors. Forskolin lowers the intraocular pressure of rabbits, monkeys, and humans. In rabbits, net aqueous humor inflow decreases, outflow facility remains unchanged, and ciliary blood flow increases. Tolerance to the intraocular pressure lowering effect did not occur in rabbits after topical doses given every 6 hr for 15 days. In vitro forskolin activates adenylate cyclase of crude particulate homogenates prepared from cultured human ciliary epithelia or from dissected ciliary epithelial processes of rabbit or human eyes. This activation is not blocked by timolol. The stimulation of adenylate cyclase by isoproterenol in vitro is potentiated in the presence of forskolin. Forskolin represents a potentially useful class of antiglaucoma agents differing in molecular mechanism of action from previously used drugs.

Indomethacin and epinephrine effects on outflow facility and cyclic adenosine monophosphate formation in monkeys
Crawford K.S.; Gange S.J.; Gabelt B.T.; Heideman W.; Robinson J.C.; Hubbard W.C.; Kaufman P.L.
Ophthalmology/Visual Sciences Dept., University of Wisconsin, 600 Highland Avenue, Madison, WI 53792-3220 USA
Investigative Ophthalmology and Visual Science (USA), 1996, 37/7 (1348-1359)

Purpose. To investigate the effect of indomethacin inhibition of prostanoid production on the epinephrine-stimulated increase in outflow facility and cyclic adenosine monophosphate (cAMP) production in the anterior segment of the monkey eye.

Methods. Topical indomethacin was given 1 hour before the intracameral administration of epinephrine to living cynomolgus monkeys. Outflow facility was measured for 45 to 60 minutes, beginning 3 hours after epinephrine administration, by two-level constant pressure perfusion of the anterior chamber. Cyclic adenosine monophosphate formation was measured in cell membranes isolated from rhesus monkey ciliary muscle, ciliary muscle, ciliary processes, trabecular meshwork, and iris in the presence of forskolin, indomethacin, epinephrine, or indomethacin and epinephrine combined.

Results. Three hours after the intracameral administration of 5.5 microg epinephrine, facility increased by similar40%, a putatively maximal response, at which time the intracameral epinephrine concentration was similar15 microM. Pretreatment with topical indomethacin produced a dose-dependent inhibition of epinephrine's facility-increasing effect; the maximum inhibition of 50% to 70% occurred at an indomethacin dose of 50 to 125 microg. Doubling the indomethacin dose (250 microg) produced no further inhibition, whereas a fivefold larger epinephrine dose (27.5 microg) did not overcome the inhibition. Forskolin and epinephrine both stimulated cAMP production in vitro, whereas (indomethacin) greater than or equal to 10-4 M partially inhibited both basal and epinephrine-stimulated cAMP production in all four tissues.

Conclusions. Approximately half of the epinephrine-induced facility increase is inhibited by indomethacin, but it is unclear whether the indomethacin- inhibitable fraction is mediated by epinephrine-stimulated prostanoid production or release.


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