Abstract: Ischemic disorders of the retina and associated tissues of the posterior segment of the eye are treated by topical administration to the eye of an amount of a calcium channel blocking agent effective to increase blood flow to those tissues. Calcium channel blocking agents of Class I are especially useful, and among these a preferred agent is verapamil hydrochloride.

Abstract: A composition for use in hair growth stimulant and blood circulation stimulant, which contains as active ingredient an extract fraction containing non-aconitine type alkaloidal components which is obtained by extracting Aconitum roots with water or alcohol and removing aconitine type alkaloidal components from the resultant aqueous or alcoholic extract.

Abstract: Mixed ligand metal complexes of nitric oxide-nucleophile adducts, useful as cardiovascular agents of the formula KA, wherein A is[(M).sub.x.sup.x' (L).sub.y (R.sup.1 R.sup.2 N-N.sub.2 O.sub.2).sub.x ], andK is a pharmaceutically acceptable counterion present in the composition when the overall charge of A is not zero, counterion K being present only in an amount to neutralize A. Methods of treating mammals with such compounds are provided. Pharmaceutical compositions containing such compounds are also provided.

Abstract: Method for prophylaxis and treatment of heart diseases using a carbostyril derivative-of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cycloalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonylalkyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoylalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A--NR.sup.4 R.sup.5 (R.sup.4 and R.sup.

Abstract: The invention provides a topical composition for rejuvenating skin texture, comprising a first topically applicable component for stimulating the flow of blood in the arteries leading to, and capillaries feeding the muscles adjacent the skin; and a second topically applicable component for stimulating the flow of blood in the capillaries adjacent skin cells.

Abstract: The present invention provides a new medical use for 3-[2-(dimethylamino)-ethyl]-N-methyl-1H-indole-5-methanesulphonamide and physiologically acceptable salts and solvates thereof in the treatment of tension-type headache and headache associated with substances or their withdrawal.

Abstract: There are disclosed cardiovascularly active compounds possessing antihypertensive properties, and pharmaceutical compositions containing these agents and a method of treating cardiovascular disorders with the compounds. The active components of the pharmaceutical compositions are compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from straight chain and branched chain alkyl and olefinic groups, which may be unsubstituted or substituted; or R.sub.1 and R.sub.2 together with the nitrogen atom they are bonded to form a heterocyclic group; and R.sub.3 is a pharmaceutically acceptable organic group selected from alkyl and olefinic groups which may be unsubstituted or substituted, acyl, a sulfonyl, sulfinyl, sulfenyl, carbonate, or carbamate derivative; or R.sub.3 is a group of the formula--(CH.sub.2).sub.n ONN(O)NR.sub.1 R.sub.2, wherein n is 2-8, and R.sub.1 and R.sub.2 are as described above. Novel compounds are disclosed wherein at least one of R.sub.1, R.sub.2 and R.sub.

Abstract: Optically pure (S) metoprolol, which is substantially free of the (R) enantiomer, is a potent beta-blocker for treating myocardial infarction and for relieving the symptoms of angina pectoris, cardiac arrhythmia and hypertension in individuals. A method is disclosed utilizing the optically pure (S) configurational enantiomer of metoprolol for treating cardiovascular disorders while reducing undesirable side effects associated with the administration of beta-blockers.

Abstract: The invention relates to a matrix tablet for the sustained release of indapamide which ensures a continuous and uniform release of the active principle after oral administration.

Abstract: The composite membrane is disclosed having a microporous support which is coated with a polymer composition and a contact adhesive layer applied to said polymer. A process for making and a process for using the membrane is also disclosed.

Abstract: An anti-hypotensive formulation comprising an essentially arginine-free or low arginine (less than about 0.1%, most preferably, about 0.01%) containing mixture of amino acids is provided. The invention in particular embodiments of the anti-hypotensive formulation includes ornithine, citrulline or both. A method for prophylaxis and treatment of systemic hypotension in an animal is provided. Most particularly, a method for treating hypotension caused by nitric oxide synthesis through administering a low or essentially arginine-free parenteral formulation to an animal, so as to reduce or eliminate nitric oxide synthesis is described. A method for treating an animal in septic shock is also disclosed, comprising administering to the animal an anti-hypotensive formulation comprising a mixture of amino acids, which is essentially arginine free.

Abstract: Improved oral formulations are prepared by admixing gemfibrozil with from 1 to 4%, by weight, of a pharmaceutically acceptable surfactant having an HLB value of from about 10 to about 50.

Abstract: A family of compounds effective in inhibiting interleukin-1 (IL-1) activity, tumor necrosis factor (TNF) activity, and the activity of other leukocyte derived cytokines is comprised of 7-(oxoalkyl) 1,3-dialkyl xanthines of the formula ##STR1## in which R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of straight-chain or branched alkyl radicals with 2 to 6 carbon atoms, cyclohexyl, alkoxyalkyl and hydroxyalkyl radicals, and A represents a hydrocarbon radical with up to 4 carbon atoms which can be substituted by a methyl group. Another family of effective compounds is identified as ##STR2## The inhibition of IL-1, TNF, and other cytokines in mammals is implicated in alleviation of a wide variety of disease conditions.

Abstract: Polypeptides called receptor mediated permeabilizers (RMP) increase the permeability of the blood-brain barrier to molecules such as therapeutic agents or diagnostic agents. These receptor mediated permeabilizers are more efficacious than bradykinin in causing the blood-brain barrier to become more permeable. The permeabilizer A-7 or conformational analogues can be intravenously co-administered to a host together with molecules whose desired destination is the cerebrospinal fluid compartment of the brain. The permeabilizer A-7 or conformational analogues allow these molecules to penetrate the blood-brain barrier and arrive at this destination.

Abstract: A sustained-release coating composition is described that contains an ethylcellulose and/or a methacrylic methylester together with a plasticizer and a detackifying agent. Sized drug granules are coated with this composition and then mixed with a polymeric composition containing at least one viscosity agent and formed into drug dosage units for the administration and sustained release of the drug in a patient.The sustained-release drug dosage units described produce a continuous, slow release of the drug at a therapeutically effective dosage level when administered to a patient.

Abstract: A pharmaceutical composition which comprises a mixture of an alpha-2 adrenoceptor antagonist, preferably idazoxan, or a pharmaceutically acceptable salt thereof, and either a catecholamine precursor or an inhibitor of aromatic L-amino acid decarboxylase, preferably carbidopa. The compositions can be used for treatment of endogenous depression or low blood pressure.

Abstract: The present invention provides a novel pharmaceutically acceptable gel containing minoxidil for topical application.

Abstract: This invention concerns antihypertensive compositions and a method of lowering blood pressure in mammals. The active component of the compositions is a compound of the formula: ##STR1## wherein J is an organic or inorganic moiety, M.sup.+x is a pharmaceutically acceptable cation and the compound decomposes under physiological conditions to release nitric oxide (NO).

Abstract: A method is disclosed for reducing cardiovascular damage caused by hypoxic or ischemic events such as heart attack and cardiac arrest. This method involves the administration of disulfiram, or a suitable salt or analog of disulfiram, to a mammal in need of such treatment. Disulfiram can inhibit enzymes such as xanthine oxidase which would otherwise generate oxygenated free radicals, which are highly reactive chemical compounds that non-specifically attack and damage essential molecules and cells. It can also chelate copper and iron, thereby suppressing lipid peroxidation and protecting cell membranes from destruction. It also generates metabolites such as tryptophol which reduce the rate of metabolic activity in neurons and affected tissue, which can be useful during cytotoxic events. This invention also discloses injectable formulations that rapidly release disulfiram into the circulating blood.

Abstract: A family of compounds effective in inhibiting interleukin-1 (IL-1) activity, tumor necrosis factor (TNF) activity, and the activity of other leukocyte derived cytokines is comprised of 7-(oxoalkyl) 1,3-dialkyl xanthines of the formula ##STR1## in which R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of straight-chain or branch alkyl radicals with 2 to 6 carbon atoms, cyclohexyl, alkoxyalkyl and hydroxyalkyl radicals, and A represents a hydrocarbon radical with up to 4 carbon atoms which can be substituted by a methyl group. Another family of effective compounds is identified as ##STR2## The inhibition of IL-1, TNF, and other cytokines in mammals is implicated in alleviation of a wide variety of disease conditions.

Abstract: A family of compounds effective in inhibiting interleukin-1 (IL-1) activity, tumor necrosis factor (TNF) activity, and the activity of other leukocyte derived cytokines is comprised of 7-(oxoalkyl) 1,3-dialkyl xanthines of the formula ##STR1## in which R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of straight-chain or branched alkyl radicals with 2 to 6 carbon atoms, cyclohexyl, alkoxyalkyl and hydroxyalkyl radicals, and A represents a hydrocarbon radical with up to 4 carbon atoms which can be substituted by a methyl group. Another family of effective compounds is identified as ##STR2## The inhibition of IL-1, TNF, and other cytokines in mammals is implicated in alleviation of a wide variety of disease conditions.

Abstract: Anthraquinone compounds of the formula: ##STR1## wherein: R.sup.1 is hydrogen, hydroxy or acyloxy,R.sup.2 is hydrogen or acyl,R.sup.3 is acyl,R.sup.4 is hydrogen or acyl,R.sup.5 is hydrogen or acyl,R.sup.6 is hydrogen or acyl, andR.sup.7 is hydrogen or acylhave been found to possess endothelin antagonistic properties and are producible by various synthetic and fermentation processes.

Abstract: A method of using certain thiazolidine-2,4-diones in the treatment of hypertension.

Abstract: Peptides comprising the tripeptide sequence of arginine-tyrosine-aspartic acid, linked from amino- to carboxy-terminus, are inhibitors of fibrinogen binding, platelet aggregation, glycoprotein IIb-IIIa binding and related aberrant and normal physiological conditions.

Abstract: The present invention is directed to a material and method for the stimulation of the production of cytokines. Several polysaccharides, including polymers of different size of .sym.1-4 linked D-mannuronic acid (poly-M and M-blocks), chitosan and cellulose oxidized in C-6 position C60XY) induce human monocytes to produce the cytokines. Preferably, the molecular weights of poly-M and chitosan are above 50,000 and 20,000 respectively. Pretreatment of the monocytes with IFN-.gamma. increases the cytokine production from monocytes stimulated with all polysaccharides tested. The subject polysaccharides worked in vivo and in vitro.The present invention has therapeutic utility as vaccine adjuvants and components. Therapeutic compositions comprising biologically active quantities of the compositions of the present invention may be employed to potentiate antibody production in response to vaccine antigens. Anti-tumor, anti-bacteriological, anti-fungal and anti-viral effects may be expected.

Abstract: The present invention pertains to a new class of compounds which can be characterized as 1,4-disubstituted piperidinyl compounds useful as antiarrhythmics, analgesics, and serotonin 5HT.sub.2 antagonists.

Abstract: A controlled-release pharmaceutical preparation of 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine. The controlled-release preparation is in the form of powder or granule containing 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine, coated with medically non-active substance or in the form of rectal suppository containing 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine. Further the controlled-release is prepared by implanting 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine in fatty materials, or granulating it and coating the resultant particles with medically non-active substance.

Abstract: The invention pertains to the field of vasoactive medicines.The vasoactive medicine, of the type composed of a combination of main active ingredients with papaverine, is characterized by the fact that it comprises at least one alpha blocker and a phosphodiasterase inhibitor representing a total of 5 to 20% by weight of the papaverine.Application to treatment of impotence in men.

Abstract: A controlled-release organic nitrate formulation for once-per-day oral administration is provided by spheres having a core which includes an organic nitrate, and a membrane surrounding the core composed of a pharmaceutically acceptable, film forming polymer. The film forming polymer is effective to permit release of the organic nitrate from the spheres, over a daily dosing period, at a rate that achieves a therapeutically effective level of the organic nitrate, while effecting a drug holiday towards a latter portion of the daily dosing period so as not to induce tolerance.

Abstract: Cyclic pentapeptides of the formula:cyclo (-X.sup.1 -X.sup.2 -X.sup.3 -X.sup.4 -X.sup.5 -) (I)wherein X.sup.n (n=1-5) represents amino acid residues. These compounds are useful as hypotensive drugs.

Abstract: A new compound, which we have named "Leualacin" has the formula (I): ##STR1## and may be prepared by cultivation of a microorganism of the genus Hapsidospora, especially Hapsidospora irregularis. The compound may be used for the treatment and prophylaxis of cardiovascular diseases and disorders, especially hypertension.

Abstract: The permeability of the blood-brain barrier to endogenous or exogenous neuropharmaceutical or diagnostic agents in an individual's blood stream is increased by administering a bradykinin agonist of blood-brain barrier permeability, such as N-acetyl [Phe.sup.8 (CH.sub.2 -NH)Arg.sup.9 ] bradykinin, to the individual. The bradykinin agonist of blood-brain barrier permeability is co-administered with the agent of interest into a blood vessel such as a vein. This co-administration allows the agent of interest to pass the blood-brain barrier into the brain compartment.

Abstract: The invention relates to combinations of angiotensin-converting enzyme inhibitors with calcium antagonists, processes for their preparation and their use as medicaments.

Abstract: A family of compounds effective in inhibiting interleukin-1 (IL-1) activity, tumor necrosis factor (TNF) activity, and the activity of other leukocyte derived cytokines is comprised of 7-(oxoalkyl) 1,3-dialkyl xanthines of the formula ##STR1## in which R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of straight-chain or branched alkyl radicals with 2 to 6 carbon atoms, cyclohexyl, alkoxyalkyl and hydroxyalkyl radicals, and A represents a hydrocarbon radical with up to 4 carbon atoms which can be substituted by a methyl group. Another family of effective compounds is identified as ##STR2## The inhibition of IL-1, TNF, and other cytokines in mammals is implicated in alleviation of a wide variety of disease conditions.

Abstract: Cell-stimulating composition having hair-growing effect and skin-vivifying effect. The composition comprising as an effective ingredient an aliphatic alcohol having odd number of carbon atoms or a derivative thereof in a cosmetically acceptable carrier.

Abstract: There is described a new inclusion complex of nicardipine or its hydrochloride with beta-cyclohdextrin, which is prepared by admixing nicardipine or its hydrochloride with beta-cyclodextrin in a molar ratio of the compounds 1:0.9-1.1 under stirring at a temperature from about room temperature to the boiling temperature of the reaction mixture in an aqueous or ethanolic medium, cooling the reaction mixture to 0.degree. to 5.degree. C. and isolating the desired complex.The inclusion complex of nicardipine or its hydrochloride posesses cerebrovascular-vasodilatory and coronary-vasodilatory properties, which are equally well expressed as those of nicardipine or its hydrochloride themselves, yet owing to the better solubility of the complex at a higher pH range, such as it exists e.g. in the intestinal tract, the manufacture of sustained release pharmaceutical forms is made possible, whereby a greater extent of dissolution of the active substance is provided also in the intestinal juice.

Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbozole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.

Abstract: This invention provides a hair enrichment composition which includes a hair-sorbable bulking agent, a blood vessel dilator, and a scalp stimulant, together with a method of using the composition.

Abstract: A method and composition for inhibition of abnormal postnatal ocular growth are disclosed. The composition comprises vasoactive intestinal peptide (VIP), PHI or a analogue of these peptides. The method for inhibition of abnormal postnatal ocular growth comprises administering to the eye of an animal effective amount of VIP, PHI or analogue of these peptides.

Abstract: A pharmaceutical composition comprises (a) a pharmacologically effective amount of bunazosin or a pharmacologically acceptable salt thereof and (b) a monoglyceride of a fatty acid having 8 to 12 carbon atoms and/or a lactic acid ester of an aliphatic alcohol having 12 to 18 carbon atoms and is improved in percutaneous administration.

Abstract: 1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C.sub.1 to C.sub.7 alkyl, C.sub.3 to C.sub.6 cycloalkyl, aryl, heteroaryl or heterocycloalkyl group at the 1-position and an amino, a dialkylamino, a piperidyl, a pyrrolidyl or a hexahydroazepinyl group at the 7-position are disclosed which may have one or two substituents in addition to the phenyl group at the 1-position and also may have a p-fluoro substituent on the phenyl group. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one, 1-cyclobutyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one and 1-cyclo-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one.The compounds are highly specific M.sub.1 -AChR antagonists with relatively prolonged duration of activity.

Abstract: A method of treating injuries in a patient associated with spinal cord trauma is disclosed. The method comprises administering to the patient a therapeutically effective amount of (S)-emopamil or a physiologically acceptable salt thereof.

Abstract: A pharmaceutical composition which comprises a mixture of an alpha-2 adrenoceptor antagonist, preferably idazoxan, or a pharmaceutically acceptable salt thereof, and either a catecholamine precursor or carbidopa.

Abstract: Pharmaceutical compounds and compositions for injectable use in the treatment of thromboxane A.sub.2 mediating diseases, comprising a pharmaceutical carrier and a pharmacologically effective amount of a compound of the formula: ##STR1## wherein R.sup.1 is carboxyl or 5-tetrazolyl; R.sup.2 is hydrogen, methyl, hydroxy, chloro, or bromo; or a pharmaceutically acceptable ester or salt thereof, together with one or more non-toxic pharmaceutically acceptable carriers; and methods for treating thromboxane A.sub.2 mediating diseases.

Abstract: The present invention relates to a pharmaceutical composition in the form of a multiple-compression tablet comprising(a) a discrete zone made with Formulation (A) which comprises a carrier base material combined with a therapeutically effective decongestant amount of a sympathomimetic drug, or a pharmaceutically acceptable salt thereof, the carrier base material being a mixture of (i) one or more pharmaceutically acceptable water-soluble nonionic cellulose ethers in an amount from about 18% to about 50% by weight of Formulation (A), (ii) one or more pharmaceutically acceptable anionic surfactants in an amount from about 2% to about 20% by weight of Formulation (A), and (iii) one or more other pharmaceutically acceptable excipients, and(b) a discrete zone made with Formulation (B) which comprises a second carrier base material combined with a therapeutically effective antihistaminic amount of a piperidinoalkanol, or a pharmaceutically acceptable salt thereof, the second carrier base being a mixture of (i) calc

Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.

Abstract: A family of compounds effective in inhibiting interleukin-1 (IL-1) activity, tumor necrosis factor (TNF) activity, and the activity of other leukocyte derived cytokines is comprised of 7-(oxoalkyl) 1,3-dialkyl xanthines of the formula ##STR1## in which R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of straight-chain or branched alkyl radicals with 2 to 6 carbon atoms, cyclohexyl, alkoxyalkyl and hydroxyalkyl radicals, and A represents a hydrocarbon radical with up to 4 carbon atoms which can be substituted by a methyl group. The inhibition of Il-1, TNF, and other cytokines in mammals is implicated in allerviation of a wide variety of disease conditions.

Abstract: A medical bandage is disclosed comprising a reservoir containing a gelled fluid, rheological agent and a drug. A method of using the bandage for producing a beneficial effect is disclosed also.

Abstract: A solid dosage form having a fill composition encased in a shell composition; the fill composition comprising(a) 5-60 mg of nifedipine;(b) a 5-7 membered cyclic pharmaceutically acceptable ingestible carbonate of the formula ##STR1## where A is an alpha,omega-C.sub.2 -C.sub.4 alkylene which is unsubstituted or substituted by at least one C.sub.1 -C.sub.4 alkyl; and(c) a pharmaceutically acceptable ingestible surfactant having a total of d ring members and being of the formula ##STR2## wherein B is a C.sub.1-4 -alpha,omega-alkylene;n is an integer from 0 up to d-1;m is an integer from 0 up to (d-n-1);each R is independently H or a C.sub.1-4 alkyl which is unsubstituted or substituted by at least one R';each R' is independently a hydroxy which is free, etherified by R.sup.2, or esterified by R.sup.3 ;each R.sup.2 is a C.sub.2-4 straight or branched oxyalkylene or a poly (C.sub.2-4 straight or branched oxyalkylene), the terminal oxygen of which is bound to hydrogen or R.sup.3 ; and each R.sup.

Abstract: Nifedipine is formulated into a reactally administrable composition for administration to humans and animals to effect coronary dilation and for hypotensive effect.