Abstract: Hydroxyalkyl-phenoxy-propan-2-ol-3-amines are oculoselective .beta.-blockers useful in the treatment of elevated intraocular pressure with little or no effect on the pulmonary or cardiovascular system.

Abstract: The invention disclosed is a composition and method for the slow sustained ocular delivery of a prophylactic agent contained in liposome vesicles. The liposome vesicles are composed of phospholipid and cholesterol in a molar ratio of phospholipid to cholesterol of 8:2 to 1:1. Preferably, stearylamine is included in the liposome composition.

Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is a substituted amino group; or pharmaceutically acceptable salts or esters thereof.

Abstract: The prostaglandin 1,11-lactone PGF.sub.2.alpha. is disclosed for lowering intraocular pressure.

Abstract: An antiglaucoma composition containing as the active component a s-/-/-2,3 dihydroxy-9,10,11-trimethoxy-5,8,13,13a-tetrahydro-6H-dibenzo (a,f) quinolizine hydrochloride of the general formula: ##STR1## where R.sub.1 .dbd.R.sub.2 .dbd.R.sub.3 .dbd.R.sub.4 .dbd.H.dbd.R.sub.5 .dbd.R.sub.6 .dbd.R.sub.7 .dbd.CH.sub.3 OThe composition is used as an ophthalmic solution in a method for treating glaucoma by administering a therapeutic dose of 2 to 3 drops two to four times daily to a host such as a warm-blooded animal having glaucoma.

Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents (i)--CH.sub.3, (ii)--CH.sub.2 OH or (iii) ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.7 is branched alkyl having 4-12 atoms.

Abstract: Protein hydrolysates are described; they may be obtained by the enzymatic decomposition of whey protein, lactalbumin, .alpha.-lactalbumin, .beta.-lactoglobulin, lysozyme, lactoferrin or serum albumin. These products are suitable for pharmaceutical purposes.

Abstract: The use of an angiotensin converting enzyme inhibitor for reducing and controlling the elevation of intraocular pressure associated with the use of corticosteroids is disclosed. Also disclosed are the use of the combination of an angiotensin converting enzyme inhibitor and a steroid, and pharmaceutical compositions comprising the combination.

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: A method for treating glaucoma consisting of exposing the eye to a corticosteroid and a beta adrenergic agent to the eye which acts to decrease ocular pressure. Useful adrenergic agents include beta agonists antagonists, including, for example, epinephrine, dipivalyl epinephrine, betaxolol, levobunolol, and timolol. Useful steroids, which are preferably applied topically, include dexamethasone, prednisolone, cortisone, and triamcinolone. The beta adrenergic agent is administered at a concentration between about 10% and 20% of the concentration that the agent is administered in its normal use. The corticosteroid is administered at a concentration between 5% and 10% of the concentration that the corticosteroid is administered in its normal use.

Abstract: Herein is described an ocular composition comprising an ocular decongestant such as phenylephrine and certain labdane derivatives which are intraocular pressure lowering agents. The composition not only markedly reduces the ocular reddening otherwise produced by such labdane compounds, but also unexpectedly prolongs and frequently potentiates their intraocular pressure lowering effect. Both of these effects are very beneficial to the use of such labdanes for the treatment of glaucoma.

Abstract: There is provided a stable, ophthalmic aqueous composition for topical administration, comprising (a) acetazolamide and either (b) a pre-formed, pharmaceutically acceptable, aqueous gel or (c) an aqueous gel-forming liquid capable of forming a pharmaceutically acceptable gel in situ when applied topically to a patient; said composition having a pH of less than 5.0.

Abstract: Pharmaceutical compositions and a method for reducing intraocular pressure by topically applying a carboxyalkyl dipeptide are disclosed.

Abstract: This invention provides a method for treating hypertension or glaucoma in a subject's eye which comprises contacting the surface of the eye with an effective intraocular pressure reducing amount of one or more prostaglandins selected from the group consisting of prostaglandin A (PGA), prostaglandin B (PGB), prostaglandin C (PGC), derivatives of PGA, PGB, and PGC, conjugates of PGA and conjugated derivatives of PGA, so as to reduce the intraocular pressure of the eye and maintain such reduced intraocular pressure. Also provided is a composition for topical treatment of hypertension or glaucoma in the eye of a subject which comprises an effective intraocular pressure reducing amount of one or more prostaglandins selected from the group consisting of PGA, PGB and PGC, derivatives of PGA, PGB and PGC and conjugates of PGA and an opthalmically compatible carrier.

Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for their preparation, and methods for reducing intraocular pressure utilizing the compounds or compositions are disclosed.

Abstract: The invention relates to a process for the treatment of glaucoma comprising administering to a human in need thereof an effective amount of a compound selected from the inhibitors of xanthine-oxidase.

Abstract: This invention relates to a pharmaceuticals which contains thyroid hormones and improved method which extracts thyroid hormones from animal thyroid gland. The pharmaceuticals of this invention is used to treat senile cortical cataract. There are some effect of long term on other cataract except subcapsular cataract. The pharmaceuticals of this invention is applied in the form of eyedrops or injection.

Abstract: Pharmaceutical compositions comprising tetrahydrocortisol and method of using same in the control of intraocular pressure are disclosed.

Abstract: Methods and compositions are described for the preparation of alpha-tocopherol vesicles, the bilayers of which comprise a salt form of an organic acid derivative of alpha-tocopherol such as the Tris salt form of alpha-tocopherol hemisuccinate. The method is rapid and efficient and does not require the use of organic solvents. The alpha-tocopherol vesicles may be used to entrap compounds which are insoluble in aqueous solutions. Such preparations are especially useful for entrapping bioactive agents of limited solubility, thus enabling administration in vivo.

Abstract: The present invention relates to a pharmaceutical composition intended for contacting with a physiological liquid characterized in that said composition is intended to be administered as a non-gelled liquid form and is intended to gel in situ, this composition containing at least one polysaccharide in aqueous solution, of the type which undergoes liquid-gel phase transition gelling in situ under the effect of an increase in the ionic strength of said physiological liquid.

Abstract: A method of lowering intraocular pressure in the eye of a human or an animal, the method involving administering to the eye, an agent comprising an amount of tetracycline or a tetracycline related compound, such as demeclocycline, sufficient to achieve a significant lowering of intraocular pressure.

Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, whereinR.sub.1 is alkyl of two to four carbon atoms; andR.sub.2 is alkyl of three or four carbon atoms; orR.sub.1 and R.sub.2 taken together with N form ##STR2## wherein n is 0, 1, or 2 and R.sub.5 and R.sub.6 are each independently lower alkyl or hydro;R.sub.3 is hydro or hydroxy;R.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.

Abstract: A method for reducing intraocular pressure by topically applying 7-{N-[1(S)-Carboxy-3-phenylpropyl]-(S)-alanyl}-1,4-dithia-7-azaspiro[4.4]n onane-8(S)-carboxylic acid is disclosed.

Abstract: An ocular antihypertensive composition for topical use which contains an effective amount of a compound represented by the formula ##STR1## or a salt thereof having, in low concentrations, intraocular pressure lowering activity in mammals, low toxicity and no influence on the pupil size and, therefore, is useful as a therapeutic agent for glaucoma, for instance.Furthermore, since the compound is effective in low concentrations, the possibility of tolerance development is considered to be scarce.

Abstract: Trifluoromethanesulfonamide and salts thereof are active as antiglaucoma agent and may be administered topically to the eye. Pharmaceutical formulations of such compounds are also described.

Abstract: Method of treatment of ocular hypertension and glaucoma which comprises administering an effective amount of prostaglandin D.sub.2 -active substance to a subject in need of such treatment.

Abstract: Disclosed is the use of trimoprostil, and its derivatives, such as, 15-acetyl trimoprostil and pharmaceutically acceptable salts and esters thereof in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising trimoprostil and its derivatives.

Abstract: Disclosed is the use of Tri-methyl PG-F.sub.2 a, and its derivatives, such as, 15-acetyl Tri-methyl PG-F.sub.2 a and pharmaceutically acceptable esters thereof in the treatment of glaucoma and intraocular hypertension. Also disclosed are ophthalmic pharmaceutical compositions comprising Tri-methyl PG-F.sub.2 a and its derivatives.

Abstract: The hyaluronidase, which is a hyaluronic acid-specific endo-.beta.-glucuronidase, having a molecular weight of about 28,500 in non-reduced form, is derived from buffalo leeches (that is, leeches of the sub-family Hirudinariinae, such as the species Hirudinaria manillensis or Poecilobdella granulosa).The hyaluronidase, which cleaves hyaluronic acid, but not chondroitin, chondroitin -4- sulphate, chondroitin -6- sulphate or heparin, is considerably more stable at high temperatures and extremes of pH than known leech hyaluronidase. It has a wide range of uses where breakdown of hyaluronic acid is required; of particular interest is in pharmaceutical or veterinary formulations, either as an active agent or a spreading or percutaneous factor. The hyaluronidase is useful for stimulating flow of physiological fluids in the eye (for example, in the treatment of glaucoma).

Abstract: A novel pharmacologic therapy for treatment of idiopathic primary open angle glaucoma, drug-induced glaucoma and elevated intraocular pressure is disclosed. The pharmacologic therapy consists of a novel composition comprised of 17-alpha-methyl-testosterone and a physiologically tolerable carrier. In accordance with a method aspect of this invention, the active ingredient is administered to the eye of a warm blooded animal in such a manner as to maintain physiologic or normal intraocular pressure, or to return elevated intraocular pressure to normal levels. The method aspect of this invention may also be employed to ameliorate drug induced elevated intraocular pressure.

Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Abstract: The present invention relates to ophthalmological pharmaceutical compositions comprising (benzothiadiazine, benzamide and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds and to methods for using said composition in reducing intraocular pressure, e.g., in the treatment of glaucoma.

Abstract: Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.

Abstract: Topical ocular administration of a dopamine agonist is effective in lowering abnormally elevated intraocular pressure and is useful in the prevention and treatment of glaucoma and related ocular diseases.

Abstract: Aqueous humor formation and intraocular pressure in mammals having ocular hypertension or glaucoma may be reduced by topically administering to a hypertensive eye an ophthalmologically acceptable amount of certain dopamine antagonists or acid addition salts thereof. A preferred group of dopamine antagonists is the 4-piperidino-4'-fluoro-butyrophenones, especially haloperidol, trifluperidol, and moperone. The phenothiazines are another suitable group of dopamine antagonists. An ophthalmic composition for topically treating glaucoma may comprise an aqueous solution containing 0.01% to 5% by weight of a water-soluble ophthalmologically acceptable acid addition salt of such dopamine antagonist.

Abstract: A target-entrapped drug comprising three chemically joined components(1) the active drug component;(2) a linking chain; and(3) an activatable group;the activatable group on exposure of the drug to activation liberating components (1) and (2) so that the drug component (1) is bound to a selected target site through the linking chain (2). The drug is administered and then activated by exposure to electromagnetic radiation or other energy such as thermal energy at the anatomic target site.

Abstract: Glaucoma can be treated by the application to the eye of a physiologically active amount of a compound of the formula ##STR1## in which: each of R.sub.3 and R.sub.4 is selected from hydrogen, and alkyl, alkenyl and cycloalkyl radicals, or R.sub.3 and R.sub.4 together with the carbon between them are a cycloalkylidene radical,R.sub.2 is a lower alkyl radical, and the salts thereof with pharmaceutically acceptable acids, in an opthamologically accepted carrier therefor, which when liquid and an isotonic agent is present can have the form of an eye lotion. The 1-N-tert.-butylamino derivatives of 3-(cyclopropyl-methyl-ketone-oximino)-propan-2-ol, 3-(dicyclopropyl-ketone-oximino)-propan-2-ol, and 3-(3,3,5-trimethylcyclohexane-1-ketone-oximino)-propan-2-ol are novel compounds within such formula specifically useful for such treatment.

Abstract: A method of increasing aqueous humor outflow in the eye of a human patient including topically administering to the eye an outflow increasing amount of a compound characterized in that it contains one or more groups capable of reacting with sulfhydryl groups in the trabecular meshwork of the eye, and it has a margin of safety of at least 2.0.

Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms;R.sub.2 is --(CH.sub.2).sub.n --C.sub.6 H.sub.4 --R.sub.5 ; wheren is an integer from 1 to 4; andR.sub.5 is --H, --OH, halo, lower alkyl, lower alkoxy, ureido, lower alkyl-ureido, lower alkyl-amido, or formamido;R.sub.3 is hydro or hydroxy; andR.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.

Abstract: Novel pharmaceutical compositions containing norepinephrine releasers such as alpha-adrenergic agonists, para-sympathomimetic agonists and carbonic anhydrase inhibitors in combination with a potentiating amount of norepinephrine are disclosed. Use of such compositions, exemplified by the combination of norepinephrine and epinephrine, in an ophthalmic solution for the treatment of glaucoma is also disclosed, as well as the use of the combination of norepinephrine and a norepinephrine releaser in the treatment of congestion in the upper respiratory tract.

Abstract: A sustained-release polymeric hydrogel dosage form useful for topical, systemic or transdermal administration of a medicinal agent comprising a cross-linked, polymerized hydrophilic polymer, an amino acid polymer, a cross-linking agent, and an optional hydrophobic monomer and/or a chain regulator in conjunction with a lower alkyl (C.sub.1 -C.sub.4), polar solvent and said medicinal agent in a therapeutically effective amount.

Abstract: Fatty acid salts of betaxolol, a cardioselective beta-blocker, and ophthalmic compositions containing these salts are described. These new salts have an aqueous solubility significantly less than that of betaxolol hydrochloride. This relatively poor aqueous solubility enables the salts to be slowly released from a suitable ophthalmic vehicle when placed in the aqueous environment of the eye. The salts also exhibit a significantly lower incidence of ocular irritation, as compared to ophthalmic solutions containing betaxolol hydrochloride.

Abstract: A sustained-release polymeric hydrogel dosage form useful for topical, systemic or transdermal administration of a medicinal agent comprising a cross-linked, polymerized hydrophilic polymer, an amino acid polymer, a cross-linking agent, an optional hydrophobic polymer and said medicinal agent in a therapeutically effective amount.

Abstract: Hydroxyalkyl-phenoxy-propan-2-olamines and novel esters thereof are oculoselective .beta.-blockers useful in the treatment of elevated intraocular pressure with little or no effect on the pulmonary or cardiovascular system.

Abstract: Lyophylisates comprising bromocriptine or an acid addition salt thereof capable of reconstitution in an isotonic vehicle to provide a stable formulation for occular instillation, useful e.g. in the treatment of glaucoma. Typical lyophylisates in accordance with the invention comprise: a lyophylisable acid, e.g. methane sulfonic acid, an acid addition salt of bromocriptine with said acid, e.g. bromocriptine mesylate, benzalkonium chloride and a lyophylisate matrix material.

Abstract: A method of lowering the intraocular pressure in a human having abnormally high intraocular pressure, comprisingadministering systemically thereto an amount of melatonin effective to lower the intraocular pressure.

Abstract: A method of decreasing the intraocular pressure in the eye of an animal which comprises administering to the animal an intraocular pressure decreasing amount of a beta.sub.2 adrenergic receptor antagonist having a .beta..sub.2 /.beta..sub.1 potency ratio of at least 10. The method is particularly useful for the treatment of glaucoma in humans.

Abstract: This invention relates to dihydropyridazinone compounds having a cyclopropylmethoxyethyl group in the 6-substituent. These compounds are vasodilators and .beta.-adrenoceptor antagonists. A particular compound of the invention is 6-[4-[3-[2-hydroxy-3-[4-(2-(cyclopropylmethoxy) ethyl)phenoxy]propylamino]propionamido]phenyl]-5-methyl-4,5-dihydro-3 (2H)-pyridazinone.

Abstract: 1-moprolol is instilled locally in the form of an opthalmic pharmaceutical composition to treat glaucoma.

Abstract: 3-chloro-4-(4,5-dihydro-1H-imidazao-2-yl)-amino-5-alkylbenzoic acid, its pharmaceutically acceptable metal salts and esters are useful in treating glaucoma by virtue of the effect in lowering intraocular pressure when administered systemically or topically to the eye. Also disclosed are processes for preparing the compounds, pharmaceutical compositions comprising the disclosed compounds; and methods of treatment comprising administering said compositions when a lowering of intraocular pressure is indicated.