Abstract: Combinations of at least one clonidine derivative and at least one prostaglandin are used to treat glaucoma and ocular hypertension without some of the side effects typically associated with topical administration of prostaglandins.

Abstract: The present invention provides a novel use of a compound of formula I ##STR1## or a pharmaceutically and/or physiologically acceptable salt or solvate thereof for the manufacture of a pharmaceutical composition useful for lowering intraocular pressure.

Abstract: Methods for the treatment of glaucoma are described. The compounds described cause a perturbation of cell adhesions in the trabecular meshwork, mainly via disruption of the associated cytoskeletal structures or the modulation of their interactions with the underlying membrane. Perturbation of these adhesions reduces the resistance of the trabecular meshwork to fluid flow and thereby reduces intraocular pressure.

Abstract: Methods and kits for treatment of glaucoma are disclosed. In general, the methods of the invention include administering a therapeutically effective amount of a deprenyl compound to a subject such that the subject is treated for glaucoma.

Abstract: A medicament for reduction of intraocular pressure comprises both carbachol and a locally applicable betablocker.

Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are encompassed by the following structure formula I: ##STR1## wherein wavy line attachments indicate either the alpha (a) or beta (b) configuration; hatched lines indicate a configuration, solid triangles are used to indicate b configuration, dashed bonds represent a double bond, or a single bond; n is 0, or an integer of from 1 to 3; X is NH.sub.2 or OR; R is hydrogen, R.sub.4 or a --(CO)R.sub.4 group; R.sub.1, R.sub.2, and R.sub.3 independently are hydroxyl, or --O(CO)R.sub.5 groups, wherein R.sub.4 and R.sub.5 independently stand for saturated or unsaturated acyclic hydrocarbon having from 1 to 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.6 where m is 0-10 and R.sub.6 is an aliphatic, aromatic or heteroaromatic ring, R.sub.7 and R.sub.8 together are .dbd.

Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is is two or three; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl;, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

Abstract: Disclosed are pharmaceutical compositions comprising dipivefrin and levobunolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.

Abstract: The present invention provides a sustained-release delivery composition for ophthalmic drugs comprising cross-linked hydrogel microspheres having a binding affinity for the drug.

Abstract: 9-Halo-13,14-dihydroprostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.

Abstract: The subject invention involves methods of treating nasal congestion comprising administration, to a human or lower animal in need of such treatment of a safe and effective amount of a compound having the following structure: ##STR1## wherein: (a) R is unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; and(b) R' is selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl or alkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thiol; cyano; and halo.The subject invention also involves the use of such compounds for preventing or treating other respiratory, ocular and/or gastrointestinal disorders. The subject invention also involves novel compounds having the above structure wherein R' is hydrogen or fluoro or cyano.

Abstract: In a preferred embodiment, drugs having pharmacological properties which are useful in the medicinal therapy of fibrotic disease for the reparation and prevention of fibrotic lesional tissues, such drugs including as active ingredient(s) one or more N-substituted 2-(1H) pyridone(s) and/or N-substituted 3-(1H) pyridones. The composition of this invention is novel as an anti-fibrotic drug, namely, as an agent for treating fibrosis. Any existing compounds have not been shown to be effective for the reparation and prevention of fibrotic lesions.

Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains as the active ingredient one or more muscarinic antagonist compounds. Examples of muscarinic antagonists utilized in the pharmaceutical composition and method of treatment are: 10H-thieno(3,4-b)(1,5)benzodiazepin-10-one 4,9-dihydro-3-methyl-4-((4-methyl-1-piperazinyl)acetyl) (telenzepine); 5,11-dihydro-11?4'-methyl-1'-piperazinyl)-acetyl!-6H-pyrido?2,3-b!?1,4!ben zodiazepin-6-one (pirenzepine); racemic 11-??2-(Diethylamino)methyl!-1-piperidinyl!-acetyl!-5,11-dihydro-6H-pyrido ?2,3-b!?1,4!benzodiazepin-6-one (AF-DX 116); dextrorotatory 11-??2-(Diethylamino)methyl!-1-piperidinyl!-acetyl!-5,11-dihydro-6H-pyrido ?2,3-b!?1,4! benzodiazepin-6-one (AF-DX 250); an ophthalmically acceptable salt of 4-diphenylacetoxy-1,1-dimethyl piperidine (4-DAMP); .alpha.-cyclohexyl, -.alpha.

Abstract: Polyamine antagonists are found to be effective in preventing or reducing visual field loss associated with glaucoma. Especially preferred are certain 1-phenyl-2-piperidinoalkanol derivatives, such as eliprodil and ifenprodil.

Abstract: The use of certain dopaminergic compounds for controlling elevations of intraocular pressure is disclosed. The compounds are ergoline derivatives. The most preferred compound is cabergoline. The compounds have been found to produce a significant reduction of intraocular pressure.

Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains, as the active ingredient, one or more compounds having chloride channel blocking activity. Examples of chloride channel blockers utilized in the pharmaceutical composition and method of treatment are: ##STR1## wherein R is hydrogen or a pharmaceutically-acceptable cation, e.g. an alkali or alkaline earth metal, or a quaternary amine; or R represents a ester-forming moiety, e.g. a lower alkyl radical, having up to six carbon atoms, that may be derived from a lower alkanol.

Abstract: A method for treating or preventing anoxic or ischemic brain injury that includes administering melatonin to a person who is suffering from or has a high risk of suffering from an anoxic or ischemic insult or injury. The method may also include administering complementary agents.

Abstract: Compositions containing 3-Oxa-D-prostaglandins and methods of their use in treating glaucoma or ocular hypertension are disclosed.

Abstract: The invention relates to the use of EP.sub.2 receptor agonists as potent ocular hypotensives, and are particularly suitable for the management of glaucoma. In particular said compounds are represented by the formulae: ##STR1## wherein the broken line attachment to the cyclopentane ring or the omega chain indicates the .alpha. configuration and the solid line attachment to the cyclopentane ring or the omega chain indicates the .beta. configuration, R is hydrogen or a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.1 wherein m is 0-10, and R.sub.1 is an aliphatic ring having from about 3 to about 7 carbon atoms, or an aryl or heteroaryl ring having from about 4 to about 10 carbon atoms and wherein the heteroatom is selected from the group consisting of N, O and S.

Abstract: The intraocular use of combinations of lens epithelial cell growth stimulators (e.g., TGF-.beta.) and antimetabolites (e.g., mitomycin C) is described. The combination is applied to the capsular bag to prevent or retard the formation of secondary cataracts following cataract surgery. The lens epithelial cell stimulators activate DNA synthesis in dormant lens epithelial cells, and thereby make those cells susceptible to the anti-metabolites. This enables the antimetabolites to suppress the proliferation of lens epithelial cells to a much greater extent, relative to the proliferation observed when the metabolites alone are utilized. The increased suppression of the growth of lens epithelial cells results in a significant improvement in the ability to prevent or retard the formation of opacities on the lens capsule (i.e., secondary cataracts).

Abstract: This invention relates to a new medical use for compounds having selective agonist activity at 5-HT.sub.1 -like receptors and to pharmaceutical compositions containing them. In particular it relates to a new medical use of 3-?2-(dimethylamino)ethyl!-N-methyl-1H-indole-5-methanesulphonamide and physiologically acceptable salts and solvates thereof for the treatment or prevention of elevated intraocular pressure, in particular glaucoma.

Abstract: The present invention relates to ophthalmo-logical pharmaceutical compositions comprising a renin inhibitor and to methods for using said composition in the treatment of glaucoma.

Abstract: Methods for controlling IOP with compositions of HGF Receptor Activators are disclosed.

Abstract: Compositions and methods for reducing the decomposition rate of polymeric bioadhesives and viscosity enhancers, such as poly(acrylic acids). The compositions include at least one strong, stable chelating agent, preferably an organophosphorous compound such as diethylene triamine penta(methylene phosphonic acid). These biocompatible compositions are especially useful in the ophthalmic field.

Abstract: Methods of facilitating surgical operations that involve the eye or eye area comprise introducing an opthalmologically acceptable composition containing hyaluronic acid into the site of the surgical operation. The hyaluronic acid comprises a chemically unmodified sterilized hyaluronic acid substance having a weight average molecular weight of from 4,500,000 to 12,000,000 daltons, a zero shear viscosity of from 1,000 to 80,000 Pas as measured on a 1.3-1.6% (wv) solution of hyaluronic acid substance in physiological phosphate buffer, and an absorbance at 257 nm of less than 3.5 when measured on a 1% solution of hyaluronic acid substance in sodium chloride buffer in a 10 mm cuvette. Preferred sterilized solutions of hyaluronic acid comprise hyaluronic acid which is chemically unmodified from the naturally occurring hyaluronic acid and has a weight average molecular weight of from 4,500,000 to 8,000,000 daltons, a zero shear viscosity of from 1,000 to 20,000 Pas and an absorbance at 257 nm of less than 3.5.

Abstract: The present invention provides a method for identifying a compound having muscarinic agonist activity that will lower intraocular pressure without causing miosis which comprises measuring the activity of the compound at the m.sub.3 and m.sub.5 muscarinic receptors and determining from the activity measurement a compound having at least twice the agonist activity at the m.sub.5 receptor as compared to the m.sub.3 receptor. Preferably, the method of measuring said muscarinic agonist activity comprises eliciting phosphoinositide hydrolysis in CHO-K1 cells stably expressing the m.sub.3 and m.sub.5 muscarinic receptor subtypes. The present invention also provides a method of lowering the intraocular pressure in a mammal which comprises administering to said mammal a compound that has been determined to have at least twice the agonist activity at the m.sub.5 receptor as compared to the m.sub.3 receptor.

Abstract: A pharmaceutical composition for use in glaucoma treatment which contains as an active ingredient 5-[1-hydroxy-2-[2-(2-methoxyphenoxyl)ethylamino]ethyl]-2-methylbenzenesulf onamide of the formula: ##STR1## or its acid salt. This agent is free from side effects and stable and has an excellent intraocular pressure reducing activity at its low concentrations, thus being useful as a pharmaceutical composition for use in glaucoma treatment.

Abstract: The present invention relates to therapeutically active azacyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.

Abstract: The present invention provides a novel drug for treating glaucoma.The present invention relates to a therapeutic agent for glaucoma and an ocular hypotensive agent, which comprise an aminoalkoxybibenzyl represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkoxy group, etc.; R.sup.2 represents a hydrogen atom, a halogen atom, etc.; R.sup.3 represents a hydrogen atom, a hydroxyl group, --O--CO--(CH.sub.2).sub.I --COOH (wherein I is an integer of 1 to 3), etc.; and R.sup.4 represents --NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 independently represent a hydrogen atom or a C.sub.1 -C.sub.8 alkyl group), etc.or a salt thereof as an active ingredient.

Abstract: The invention relates to the use of alcohol derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are encompassed by the following structure formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched lined indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond; n is 0, or an integer of from 1 to 3; R is hydrogen or a --(CO)R.sub.4 group; R.sub.1, R.sub.2, and R.sub.3 independently are hydroxyl, or --O(CO)R.sub.5 groups, wherein R.sub.4 and R.sub.5 independently stand for saturated or unsaturated acyclic hydrocarbon having from 1 to 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.6 where m is 0-10 and R.sub.6 is an aliphatic, aromatic or heteroaromatic ring, R.sub.7 and R.sub.8 independently are hydrogen or alkyl of 1 to 6 carbon atoms or pharmaceutically acceptable salts thereof.

Abstract: The present invention provides an ophthalmic preparation for reducing intraocular pressure comprising 2-[3-dimethyl-amino-2-(2-carboxyethoxy)propionyloxy]-2'-methoxybibenzyl or a salt thereof, which preparation exhibits intraocular pressure reducing activity, without exerting effects on the central nervous system, and can advantageously be used as a prophylactic and therapeutic agent for ocular hypertension and glaucoma bringing about elevated intraocular pressure.

Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains as the active ingredient one or more compounds having guanylate cyclase inhibition activity. Examples of guanylate cyclase inhibitors utilized in the pharmaceutical composition and method of treatment are methylene blue, butylated hydroxyanisole and N-methylhydroxylamine.

Abstract: Methods for treating angiogenesis, tumors, and ocular hypertension with steroids are disclosed herein. The steroids have angiostatic activity with reduced glucocorticoid activity.

Abstract: Compositions comprising cationic polysaccharide polymers and anionic therapeutic agents which can have enhanced substantivity to mucosal surfaces are disclosed. These compositions are well suited, for example, for the delivery of anionic ophthalmic pharmaceuticals because they can provide clear solution in addition to substantivity.

Abstract: Disclosed are nonstinging, sustained release ophthalmic formulations to control intraocular pressure in antiglaucoma therapy comprising a basic active, a cation exchange resin, and, inter alia, an acidic, mucomimetic polymer. Also disclosed are methods of treatment comprising administering such formulations topically to the eye when indicated for control and lowering of intraocular pressure.

Abstract: Anandamides useful for the treatment of intraocular hypertension, as well as ophthalmic compositions comprising the same and a cyclodextrin, and methods of use of these compounds to treat intraocular hypertension.

Abstract: ATP-sensitive K.sup.+ channel modulating compounds are incorporated into ophthalmically acceptable carriers for administration to the eye in order to affect intraocular pressure. Such formulations including compounds which inhibit the channel are particularly suitable for treating glaucoma and other disorders related to elevated intraocular pressure. Such formulation which potentiates the channel are particularly suitable for treating hypotonia and other depressed intraocular pressure conditions.

Abstract: 9-Haloprostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.

Abstract: The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in which the omega chain contains a ring structure, in an ophthalmologically compatible carrier. The invention further relates to the preparation of said compositions and their use for treatment of glaucoma or ocular hypertension.

Abstract: The present invention is directed to topical ophthalmic formulations of carbonic anhydrase inhibitors and polyethoxylated derivatives of castor oil. Methods for using the formulations for treating and controlling glaucoma and ocular hypertension are also disclosed.

Abstract: Drug delivery vehicles which reversibly increase in either loss modulus or storage modulus, or both, upon contact with the eye, skin, mucous membrane or body cavity are disclosed. The vehicles contain one or more nonionic substituted cellulose ethers and do not require a charged surfactant or a pH-sensitive polymer for such increase in loss modulus or storage modulus, or both, upon administration. In one embodiment, the vehicles gel upon instillation in the eye.

Abstract: Compositions containing, and methods for controlling intraocular pressure with, substantially pure apraclonidine are disclosed.

Abstract: Combinations of at least one clonidine derivative and at least one prostaglandin are used to treat glaucoma and ocular hypertension without some of the side effects typically associated with topical administration of prostaglandins.

Abstract: Disclosed are storage-stable preserved ophthalmic compositions containing acidic drugs in combination with polymeric quaternary ammonium compounds and boric acid.

Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains as the active ingredient one or more compounds having guanylate cyclase inhibition activity. Examples of guanylate cyclase inhibitors utilized in the pharmaceutical composition and method of treatment are: ##STR1## and pharmaceutically acceptable salts thereof.

Abstract: Reversibly gel-forming compositions for sustained delivery of bio-affecting substances are disclosed. The compositions exhibit significant changes in viscosity in response to changes in pH. The compositions contain relatively low concentrations of a stable combination of at least one pH-responsive gelling polymer and at least one other thermally nonresponsive polymer. The compositions are preferably formulated to include one or more therapeutic or diagnostic agents for administration as a liquid that will gel in situ or for topical application as a pre-formed gel.

Abstract: The invention concerns the recognition that certain non-steroidal anti-inflammatory agents produce cytoprotective effects on trabecular cells, and thus can be used to prevent injury to the cells and treat the loss of trabecular cells caused by oxidative or other forms of injury to the cells. Such treatment can ameliorate the severity, or prevent, glaucoma.

Abstract: Balanced pH, hyperosmotic, hypoosmotic, or isoosmotic gels are ideal vehicles for drug delivery. They are especially suited for topical body cavity or injection application of drugs or diagnostic agents; for drug or diagnostic agent delivery to the eye of a mammal; as protective corneal shields; or as ablatable corneal masks useful in laser reprofiling of the cornea. The compositions without the addition of a drug or diagnostic agent are useful as medical devices, for instance, in separating surgically or otherwise injured tissue as a means of preventing adhesions.

Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains, as the active ingredient, one or more compounds having potassium channel blocking activity. Examples of potassium channel blockers utilized in the pharmaceutical composition and method of treatment are quinine, tremogenic indole alkaloids, such as Penitrem A and paspalicine, and insect toxins such as charybdotoxin and iberiotoxin.

Abstract: Disclosed is the use of combinations of F and E series prostaglandins and their respective derivatives and analogues, as well as pharmaceutically acceptable salts and esters thereof in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising said combinations.