Abstract: Provided are compositions and methods for treating or preventing nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery.

Abstract: A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.

Abstract: Provided are methods for treating nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery, comprising the co-administration of netupitant, palonosetron and dexamethasone.

Abstract: The present invention relates to novel benzylpiperazine derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.

Abstract: This invention provides compositions for treating and preventing nausea and other disorders, the compositions comprising vitamins as active ingredients, including vitamin B6, vitamin K, and vitamin C, and a method for treating nausea or morning sickness with the oral compositions.

Abstract: A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.

Abstract: Methods and apparatus are provided to prevent, treat, and cure chemotherapy induced nausea in human beings. The inhalation of an effective amount of vaporized essential oil from Mentha piperita (peppermint oil) has been shown in practice to prevent, treat, and cure chemotherapy induced nausea. A simple hand-held apparatus provides the vapors to be inhaled through the nostril to prevent, treat, and cure chemotherapy induced nausea.

Abstract: There invention discloses aqueous dispersions of nanoparticulate aerosol formulations, dry powder nanoparticulate aerosol formulation, propellant-based aerosol formulations, methods of using the formulations in aerosol delivery devices, and methods of making such formulations. The nanoparticles of the aqueous dispersions or dry powder formulations comprise insoluble drug particles having a surface modifier on the surface thereof.

Abstract: Methods and apparatus are provided to prevent, treat, and cure chemotherapy induced nausea in human beings. The inhalation of an effective amount of vaporized essential oil from Mentha piperita (peppermint oil) has been shown in practice to prevent, treat, and cure chemotherapy induced nausea. A simple hand-held apparatus provides the vapors to be inhaled through the nostril to prevent, treat, and cure chemotherapy induced nausea.

Abstract: A composition and method for cleansing a colon prior to endoscopic procedure. More particularly, a combination of bisacodyl, metoclopramide, sodium, and/or a phosphorus containing composition administered in sequential doses for preparing a colon prior to colonoscopy.

Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(O)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

Abstract: A composition and method for cleansing a colon prior to endoscopic procedure. More particularly, a combination of bisacodyl, metoclopramide, sodium, and/or a phosphorus containing composition administered in sequential doses for preparing a colon prior to colonoscopy.

Abstract: Generally, the method for preventing or relieving discomfort in the ears arising from congestion and/or obstruction of in the eustachian tubes comprising or changes in middle ear pressure relative to atmospheric pressure arising from environmental conditions in an individual need of prevention or relief from discomfort in the ears comprises the steps of: 1) administering a solution of 1.5%-3.5% (preferably 2-3%) sodium chloride solution having a pH of about 6 to 7.8 (preferably 6.5-7.5) in an aqueous solution as a spray or mist into the nose, 2) minimizing discharge of the solution from the nose for at least 5 seconds, then 3) evacuating the nose under pressure.

Abstract: The present invention relates to a novel process for preparing and resolving 3-amino-2-phenylpiperidine and for synthesizing from the enantiomers of such compound certain pharmaceutically active substituted 2-phenyl-3-benzylaminopiperidines. The substituted 2-phenyl-3-benzylaminopiperidines that can be prepared by the processes of this invention are substance P receptor antagonists and are useful in the treatment and prevention of inflammatory and central nervous system disorders, as well as several other disorders.

Abstract: The present invention relates to the use of certain tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis.

Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(O)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

Abstract: An injectable slow-release naltrexone formulation is provided comprising naltrexone in a poly(D,L-lactide) matrix with a small amount of residual ethyl acetate. Upon intramuscular injection of the composition, naltrexone is released in a controlled manner over an extended period of time. The composition finds use in the treatment of heroin addicts and alcoholics to reduce consumption of the abused substances.

Abstract: Invented are improved multidose aqueous formulations of endo-N-(9-methyl-9-azabicyclo[3.3.1.]non-3-yl)-1-methyl-1H-indazole-3-carboxamide hydrochloride.

Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: The present disclosure is directed to novel nutritional anti-nausea compositions, anti-emetic compositions, and methods of using same. The compositions provide improved relief from nausea and/or vomiting. The compositions are particularly useful for pregnant women.

Abstract: A non-sedating anti-emetic composition in oral unit dosage form comprising from 1 to 5 mg of methotrimeprazine per unit dosage, or in unit dosage form for parenteral administration comprising from 1 to 5 mg of methotrimeprazine in each unit dosage.

Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: CRF-antagonists are useful in the treatment of emesis.

Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. ##STR1## wherein R represents the ring A ##STR2## or 2-pyridinyl or 2-pyridinyl-N-oxide; R.sup.1 is selected from halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, and S(O).sub.n C.sub.1-4 alkyl groups;R.sup.2 and R.sup.3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and cyano groups;n represents zero, 1 or 2;and pharmaceutically acceptable salts and solvates thereof.

Abstract: The invention relates to an anti-emetic composition that comprises dexamethasone (DEX), metoclopramide (MTC) and an antihistamine or an anticholinergic agent. In a particular embodiment, a composition containing DEX:MTC:diphenhydramine in a relative weight ratio of about 1:1:2.5, respectively, is found to be effective in providing relief from the discomfort caused by symptoms of both vomiting and nausea in all patients receiving the composition. Alternatively, an effective composition may contain DEX:MTC:scopolamine in a relative weight ratio of about 1:1:0.025, respectively. Other effective compositions and methods of their use are also disclosed.

Abstract: A method of treating emesis in a warm blooded animal by administering an anti-emesis effective amount of a nitric oxide synthase inhibitor and compositions containing the same.

Abstract: Compounds of formula I, ##STR1## wherein R.sup.1 represents hydrogen; R.sup.2 represents hydrogen, halogen, cyano, OR.sup.4, --(CH.sub.2).sub.m CONR.sup.5 R.sup.6, --(CH.sub.2).sub.m SO.sub.2 NR.sup.5 R.sup.6, --(CH.sub.2).sub.m NR.sup.7 COR.sup.8, --(CH.sub.2).sub.m S(O).sub.x R.sup.8, --(CH.sub.2).sub.m NR.sup.7 CONR.sup.5 R.sup.6, --(CH.sub.2).sub.m NR.sup.7 COOR.sup.9 or --CH.dbd.CH(CH.sub.2).sub.y R.sup.10 ; R.sup.3 represents hydrogen or C.sub.1-6 alkyl; R.sup.4 represents hydrogen, C.sub.1-6 alkyl or aryl; R.sup.5 and R.sup.6 are independently represent hydrogen, C.sub.1-6 alkyl, aryl or (C.sub.1-3 alkyl)aryl; or R.sup.5 and R.sup.6 taken together may form a 4-, 5- or 6-membered ring; R.sup.7 and R.sup.8 independently represent hydrogen, C.sub.1-6 alkyl, aryl or (C.sub.1-3 alkyl)aryl; R.sup.9 represents hydrogen, C.sub.1-6 alkyl, aryl or (C.sub.1-3 alkyl)aryl; R.sup.10 represents --CONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --NR.sup.7 COR.sup.8, --NR.sup.7 SO.sub.2 R.sup.8, --NR.sup.7 CONR.sup.

Abstract: The present invention relates to a method of treating or preventing emesis in a mammal, including a human, by administering to the mammal a 5HT.sub.3 receptor antagonist and an NK-1 receptor antagonist (e.g., a substance P receptor antagonist). It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5HT.sub.3 receptor antagonist and an NK-1 receptor antagonist.

Abstract: The present invention relates to the use of certain tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis.

Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. ##STR1## wherein R represents the ring A ##STR2## or 2-pyridinyl or 2-pyridinyl-N-oxide; R.sup.1 is selected from halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, and S(O).sub.n C.sub.1-4 alkyl groups;R.sup.2 and R.sup.3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and cyano groups;n represents zero, 1 or 2;and pharmaceutically acceptable salts and solvates thereof.

Abstract: Methods are disclosed utilizing the optically pure R(+) isomer of ondansetron. This compound is a potent drug for the treatment of nausea and vomiting associated with chemotherapy and radiation therapy, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ondansetron. The R(+) isomer of ondansetron is also useful for the treatment of behavioral disorders such as mood anxiety and schizophrenia, and such other conditions as may be related to R(+) ondansetron's activity as a competitive antagonist of serotonin receptor subtype 5-HT.sub.3 such as disorders of gastrointestinal motility, depression, migraine, and as an aid for alcohol withdrawal, nicotine withdrawal, and drug (benzodiazepine et al.) withdrawal, without the concomitant liability of adverse effects associated with the racemic mixture of ondansetron.

Abstract: The present invention relates to a method of treating or preventing emesis in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives and related compounds.

Abstract: Derivatives of 2,3,3a,4-tetrahydro-2-azabicyclo alkyl-1H-imidazo[5,1,-c][1,4]benzoxazin-1-one are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addiction agents and analgesic.

Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. ##STR1## wherein R represents the ring A ##STR2## or 2-pyridinyl or 2-pyridinyl-N-oxide; R.sup.1 is selected from halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, and S(O).sub.n C.sub.1-4 alkyl groups;R.sup.2 and R.sup.3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and cyano groups;n represents zero, 1 or 2;and pharmaceutically acceptable salts and solvates thereof.

Abstract: An oral composition comprising in combination acetaminophen, dimenhydrinate and one or more antacid ingredients has been shown to be effective in the treatment of acute migraine attacks.

Abstract: Derivatives of 1-phenyl-3-azabicycloalkylimidazolidin-2-ones are provided of general formula (1) ##STR1## in which inter alia R represents a group ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof. which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addition agents and analgesic.

Abstract: This invention provides novel 3-quinuclidinyl benzamides and benzoates which have utility as therapeutical agents which exhibit anxiolytic, antipsychotic, cognition improvement, antiemetic and gastric prokinetic effects in warm blooded animals.The compounds useful in the methods and composition of this invention are represented by the formula: ##STR1## where X is oxygen or sulfur; Y is --NH or --O--; when Y is --O--, R.sup.1 is ##STR2## and when Y is --NH, R.sup.1 is ##STR3## and R.sup.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkenyl; the geometrical and optical isomers, or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of Formula I: ##STR1## in which Z is CH.sub.2 or C.dbd.O;X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino; and R.sup.1 is a group selected from Formulae (a), (b), (c) (d) and (e): ##STR2## in which p is 0 or 1;n is 1, 2 or 3;R.sup.2 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.12 alkyl, or a group R.sup.6 -C.sub.1-2 alkyl in which R.sup.6 is thienyl, pyrrolyl or furyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy;each R.sup.

Abstract: Compounds of the formula I ##STR1## wherein n is 1 or 2, R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sub.2 represents a hydrogen atom and R.sub.3 represents a hydrogen atom or a hydroxy group or R.sub.2 and R.sub.3 together represent a chemical bond, R.sub.4 represents a hydrogen atom, or a phenyl or C.sub.1 -C.sub.4 alkyl group, R.sub.5 represents a C.sub.1 -C.sub.4 alkyl group or an alkyl group and R.sub.6 represents a hydrogen or halogen atom, and the pharmaceutically acceptable salt thereof, are useful for the manufacture of a pharmaceutical composition useful in the treatment of emesis.

Abstract: The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond;n is 1, 2 or 3;p is 0, 1, 2 or 3;q is 0, 1 or 2;each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino;each R.sup.2 is lower alkyl; andR.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1;z is 1, 2 or 3; andR.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.

Abstract: A dosage form is disclosed comprising an antiemetic and antinausea drug for treating vomiting and nausea.

Abstract: Shipping fever, and other stress-related diseases in livestock, are treated by administration of a microencapsulated composition comprising IL-2 conjugated with a polyoxyethylene polymer, and mixed with a release-modulating amount of humen serum albumin. The microcapsules are administered parenterally, and release an effective amount of conjugated IL-2 continuously over a period of 14-30 days. These microcapsules are also effective in the treatment of cancer in mammals.

Abstract: Vasopressin derivatives having V.sub.1 antagonist activity which alleviate the symptoms of motion sickness. More specifically, the vasopressin V.sub.1 antagonists of this invention are employed to prevent nausea and emesis associated with motion. The antagonists may also be employed for preventing nausea and emesis due to other etiologies.

Abstract: This invention relates to a method and a class of pharmaceutical agents for suppressing vomiting, nausea, and other emetic symptoms. The method involves administering to a susceptible mammal a glutamate (EAA) receptor antagonist at an anti-emetically effective dose which does not cause undesirable side effects. Preferred EAA antagonists include those that do not readily cross blood-brain barriers (BBB). One suitable formulation comprises a broad-spectrum antagonist such as kynurenic acid or 7-chlorokynurenate. Other formulations include EAA antagonists that preferentially block NMDA receptors (such as D-AP5) or non-NMDA receptors (such as CNQX), or mixtures thereof that can block both classes of EAA receptors. In lab tests, the agents of this invention were shown to reduce or entirely block the effects of several emetic agents, including cisplatin.

Abstract: Microbially-stable liquid pharmaceutical suspensions for oral administration comprising a bismuth-containing pharmaceutical agent, benzoic acid, sorbic acid, a suspension system and water, and wherein said compositions have a pH within the range of from about 3.0 to about 5.5. These compositions are efficacious, and have good aesthetics and good storage stability.

Abstract: A liquid composition for the relief of premenstrual and menstrual discomfort comprising, as active pharmaceutical agents, an effective amount of an analgesic, an antihistamine, and a diuretic, said active agents being dissolved in a liquid vehicle, said composition containing 5-25 percent by volume alcohol and being flavored with active flavoring elements selected from the group consisting of citrus, vanilla, and mint, said active flavoring ingredients being present in an amount sufficient to mask the unpleasant taste of the pharmaceutically active agents.

Abstract: New N-(2-cycloalkylamino)ethyl-substituted benzamides having a powerful stimulating activity on gastric motility and with a low central anti-dopaminergic activity are described. The synthesis and the pharmaceutical preparation for therapeutical use are also described.

Abstract: A method for the alleviation of both motion sickness and chemically-induced emesis is provided which includes the administration of a nontoxic, therapeutically effective amount of a composition which stimulates serotonin-1A receptors in a mammal in need of such treatment. The preferred compounds for use are buspirone and 8-hydroxy-2(di-n-propylamino)-tetralin (8-OH-DPAT).

Abstract: The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group; and one of the groups represented byR.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl or phenyl - C.sub.1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage in radiological examination procedures.

Abstract: Quaternary derivatives of noroxymorphone are used to prevent or relieve nausea and emesis associated with the use of narcotic analgesics without interfering with the analgesic activity of the drugs. A particularly preferred compound is methylnaltrexone. The compound is administered in a concentration between 0.05 mg/kg and 1.0 mg/kg prior to or concurrently with the administration of the narcotic analgesic.