Basic treatment: Establish a patent airway. Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with normal saline during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poison A and B/
Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in respiratory arrest. Positive pressure ventilation techniques with a bag valve mask device may be beneficial. Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start an IV with D5W /SRP: "To keep open", minimal flow rate/. Use lactated Ringer's if signs of hypovolemia are present. Watch for signs of fluid overload. Consider drug therapy for pulmonary edema ... . For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam (Valium) ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poison A and B/
/LABORATORY ANIMALS: Acute Exposure/ Using the hepatic macrophage system of the rat, cell alteration was examined by magnetometry after intravenous application of various perfluorochemicals (emulsified perfluorodecalin (C10F18), perfluorooctane (C8F17Br) and Fluosol-DA (corresponding to a 20% emulsion of 70% perfluorodecalin and 30% perfluorotripropylamine, C9F21N)). After administration of high doses, all perfluorochemicals led to cytoskeleton alteration. This alteration, expressed as retardation of the relaxation period of ferromagnetic iron oxide particles, was most pronounced after administration of Fluosol-DA.
/LABORATORY ANIMALS: Acute Exposure/ The effect of an emulsion of perfluorochemicals (PFC) (7 parts perfluorodecalin and 3 parts perfluorotripropylamine, 4.4 g PFC/kg bw) on organ function was determined. Whereas maximal storage of PFC was reached in the spleen as early as 12 hr after PFC administration, the liver attained a maximal PFC content only after 2 days. The increase in weight also differed: a maximum occurred in the spleen on the 4th day, in the liver on the 8th day. Indocyanine green (ICG) clearance showed a small decrease, statistically significant after 12 and 24 hr. Colloidal carbon clearance, used as a measure of the function of the reticuloendothelial system (RES) decreased instantly after PFC to less than half the control value; after full recovery a second decrease was seen which lasted till the 4th day after PFC. Pretreatment with C 48/80 or with increasing doses of E. coli endotoxin could largely obviate the depressive effect of PFC-loading on carbon clearance. Serum transaminases increased to about twice the control levels but were normal by the 2nd day, and thereafter. Alkaline phosphatase showed a 2.5 fold increase but returned to control level after the 2nd day. It is concluded that while a severe disturbance of liver function did not occur, the reduction in the capacity of the RES can become a serious factor in the defense against a simultaneously appearing infection if not compensated by activating the RES. /Perfluoro chemical emulsion/
/LABORATORY ANIMALS: Acute Exposure/ Because of uncertainty about the mechanism by which fluorocarbons ameliorate myocardial ischemia, the effects of a fluorocarbon emulsion, perfluorodecalin and perfluorotripropylamine (Fluosol-DA 20% TM) with and without 100% O2 inhalation, on cardiac hemodynamics and energetics were studied in the anesthetized dog. Left ventricular (LV) intramural partial pressure of oxygen (PmO2) was measured by before and after iv infusion of Fluosol-DA 20% (40 ml/kg), and was compared with measurements made in another group of dogs receiving the volume expander dextran (36 ml/kg). Both groups of dogs were then ventilated with 100% O2 and repeat measurements were performed. In the 11 animals receiving fluorocarbons, there were increases in left atrial pressure, LV myocardial blood flow, and LV myocardial O2 consumption (MVO2) compatible with volume expansion. After 100% O2, LV MVO2 decreased to control values, while PmO2 increased to 127 +/- 48 mm Hg (p<0.001). There were no significant changes in heart rate, arterial pressure or first derivative of LV pressure (dP/dt) during the study. In 10 dogs treated with dextran there was no change in heart rate or dP/dt, but arterial and left atrial pressures were higher after dextran infusion and remained elevated after 100% O2 inhalation. LV MVO2 increased with volume expansion, and remained increased after 100% O2. PmO2 (66 +/- 18 mm Hg) after 100% O2 was lower (p<0.02) than in the fluorocarbon-treated dogs after O2 inhalation.
The decline of the concentration of perfluorochemicals (PFC) after a single injection of three different doses was studied in the circulation of rats. The doses used amounted to 4.4, 10 and 14 g/kg body weight of Fluosol-DA, an emulsion of 7 parts of perfluorodecalin (FDC) and 3 parts of perfluorotripropylamine (FTPA). This also allowed testing of the composition of the emulsion remaining in the circulation and of that found in the liver. After two days a decrease of the half life from 34.0 +/- 0.7 to 17.1 +/- 4.3 h was found within the circulation at the highest dose. At the same time a change in the composition of the emulsion in the blood stream occurred, favouring the fraction of FTPA. FTPA increased from 28.3 +/- 1.4 to 54.4 +/- 8.1% on the fourth day. Whereas in the cells of the liver PFC droplets may be broken up, freed from their surfactant layer and handled according to their individual components, for PFC in the blood stream an unchanged composition should be assumed. Both results, the decreasing half life and the change in composition of the circulating emulsion may best be explained by a shrinking and instability of the emulgator film, showing the necessity for development of a superior surfactant. /Fluosol-DA/
The effect of an emulsion of perfluorochemicals (PFC) (7 parts perfluorodecalin and 3 parts perfluorotripropylamine, 4.4 g PFC/kg body weight) on organ function was determined. Whereas maximal storage of PFC was reached in the spleen as early as 12 h after PFC administration, the liver attained a maximal PFC content only after 2 days.
A pharmaceutical preparation has a ligand structure specifically recognizing a target site and an amphiphilic compound having a hydrophobic or amphiphilic group. The pharmaceutical preparation employs an amphiphilic compound of specific structure obtained by introducing a chained hydrophilic group with an appropriate flexibility, and thus becomes a fine particle suited for drug targeting.
The pharmaceutical preparation is expected to give a prolonged pharmacological effect. A particulate preparation exhibiting a remarkable site targeting property can be formed. Further, according to the selection of matrix forming material, the drug releasing property can be controlled.
The invention relates to an oil-in-water nanoemulsion for MRI, including:
an aqueous phase,
a fluorinated phase including at least one fluorinated oil,
a surfactant at the interface between the aqueous and fluorinated phases, the surfactant comprising:
at least one amphiphilic targeting ligand,
at least one amphiphilic lipid, and
at least one diblock or triblock fluorophilic compound,
as well as to the use thereof as a contrast agent.
Electrochemical fluorination of 2-methoxy-1,1,1-trifluoro-2-(F-methyl) octane gave the corresponding perfluorinated ether in 27% yield, along with cyclic by-products in 9%. A mixture of partly fluorinated tertiary amines, consisting of 1-dipropylamino-F-1-propene and 1-dipropylamino-2-hydryl-F-propane, did not afford a superior yield of tri(F-propyl)amine compared to the unfluorinated tripropylamine
[EN] TREPROSTINIL DERIVATIVE COMPOUNDS AND METHODS OF USING SAME<br/>[FR] COMPOSÉS DE DÉRIVÉS DE TRÉPROSTINIL ET LEURS PROCÉDÉS D'UTILISATION
申请人：CORSAIR PHARMA INC
公开号：WO2016010538A1
公开（公告）日：2016-01-21
Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
[EN] PRODRUGS OF TREPROSTINIL<br/>[FR] PROMÉDICAMENTS DE TRÉPROSTINIL
申请人：THERATROPHIX LLC
公开号：WO2014110491A1
公开（公告）日：2014-07-17
Prodrugs of treprostinil are provided which can be used in the treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
