Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0085631 (agitation)
 12,064 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Predictable hydrolysis of [3H]digoxin-12alpha occurred in vitro with incubation in HCl or gastric juice. Hydrolysis varied with pH, time, temperature and agitation. Digoxin, the bis- and mono-digitoxosides of digoxigenin and digoxigenin were separated by silica gel thin-layer chromatography using chloroform-ethyl acetate-glacial acetic acid (25:25:1 v/v) and were quantitated by liquid scintillation spectrometry. Hydrolysis with incubation at 37 degrees and pH 3 for 90 min was minimal, but increased with increasing acidity until greater than 70% was hydrolysed at pH 1-2 after 30 min and greater than 96% after 90 min incubation. At pH 0-9, 87% was hydrolysed after 30 min. In vitro hydrolysis in gastric fluid was slightly less than in HCl at the same pH. A volunteer was given 150 muCi[3H]digoxin-12alpha by nasogastric tube during a pentagastrin infusion when gastric pH was 0-94. He remained on his left side and samples were aspirated at intervals and immediately neutralized. Ethanol-chloroform 50-50 (v/v) extracts of the gastric fluid aspirated after 90 min and of all the urine specimens collected for 5 days were applied to a DEAE Sephadex LH-20 column. The radioactivity appeared in a single peak as digoxigenin in the 90 min gastric aspirate and in all urine specimens. Extensive intragastric hydrolysis of digoxin may occur under conditions of maximum acid output.
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PMID:Hydrolysis of digoxin by acid. 1 78

Self-emulsifying drug delivery systems (SEDDSs) represent a possible alternative to traditional oral formulations of lipophilic compounds. In the present study, a lipophilic compound, WIN 54954, was formulated in a medium chain triglyceride oil/nonionic surfactant mixture which exhibited self-emulsification under conditions of gentle agitation in an aqueous medium. The efficiency of emulsification was studied using a laser diffraction sizer to determine particle size distributions of the resultant emulsions. An optimized formulation which consisted of 25% (w/w) surfactant, 40% (w/w) oil, and 35% (w/w) WIN 54954 emulsified rapidly with gentle agitation in 0.1 N HCl (37 degrees C), producing dispersions with mean droplet diameters of less than 3 microns. The self-emulsifying preparation was compared to a polyethylene glycol 600 (PEG 600) solution formulation by administering each as prefilled soft gelatin capsules to fasted beagle dogs in a parallel crossover study. Pharmacokinetic parameters were determined and the absolute bioavailability of the drug was calculated by comparison to an i.v. injection. The SEDDS improved the reproducibility of the plasma profile in terms of the maximum plasma concentration (Cmax) and the time to reach the maximum concentration (tmax). There was no significant difference in the absolute bioavailability of WIN 54954 from either the SEDDS or the PEG formulations.
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PMID:Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound. 158 15

The possibility of prolonging the effect of intrathecally injected meperidine by the use of a lipid solution was examined in this study. An aqueous solution of 5% meperidine HCl, 250 micrograms/kg, and an equimolar solution of meperidine dissolved in iophendylate (Pantopaque) were injected subarachnoidally in two groups of rabbits (n = 9 in each) with chronically implanted catheters in the subarachnoid space at the level of L7-8. The effect of each injection was assessed by evaluation of the pain threshold in the animal's hind limbs and of the degree of motor blockade produced. The duration of analgesia and of motor blockade were significantly longer when the lipid solution was used. Six of nine animals that received the aqueous solution of 5% meperidine HCl exhibited temporary signs of agitation (i.e., biting of hind limbs). None of the animals given the lipid solution of the drug did. The findings are attributed to the slow release of meperidine from the lipid phase that serves as a drug depot in the cerebrospinal fluid. The approach presented is suggested as a basis for the development of lipid solutions that might prolong the duration of spinal analgesia produced by a single intrathecal injection.
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PMID:Prolongation of the pharmacologic effect of intrathecal meperidine by the use of a lipid solution of it. 201 21

Constant drug release was achieved from theophylline tablets coated with a multiporous membrane in an aqueous environment. The tablets were coated with an aqueous acrylic latex containing a dispersed pore-forming agent with pH-dependent solubility characteristics. The pore former, dibasic calcium phosphate, was insoluble in the latex but leached out rapidly in 0.1 M HCl. Theophylline was then released at a constant rate through the multiporous membrane. The drug release was a function of the level of the pore-forming agent and the membrane thickness, but independent of the pH of the dissolution medium and the degree of agitation.
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PMID:Theophylline tablets coated with aqueous latexes containing dispersed pore formers. 228 Mar 64

Morphine sulfate in doses of 90 to 150 micrograms/3 microliters evoke a prominent behavioral syndrome characterized by 1) periodic bouts of spontaneous agitation during which the rat scratches and bites at the skin of the caudal dermatomes and 2) vigorous agitation, vocalization and coordinated efforts to bite and escape evoked by a light tactile stimulus applied to the flank, suggestive of a pain state (allodynia). The phenomenon is not reversed by naltrexone or is it subject to tolerance. The ordering of activity of an opioid alkaloid related agent in producing this touch-evoked agitation is: noroxymorphone-3-glucuronide, morphine-3-glucuronide, morphine-3-ethereal sulfate, dihydromorphine, noroxymorphone dihydrate, hydromorphone, dihydrocodeine tartrate, morphine sulfate, dihydroisomorphine, morphine-HCl, 6-acetylmorphine, N-normorphine-HCl and (+)-morphine. The following agents were essentially without effect at the highest doses examined: 3,6-diacetylmorphine, N-normeperidine-HCl, nalorphine-HCl, alfentanil, sufentanil, naloxone, naltrexone, methadone, dextrorphan tartrate, meperidine-HCl, oxycodone, levorphanol, oxymorphone, codeine phosphate, thebaine, nalbuphine and naltrexone-3-glucuronide. The observations that the sulfated and conjugated metabolites are 10 to 50 times more potent than their unmetabolized precursor suggest the possibility that, in high concentrations certain phenanthrene opioid alkaloids with a free 3-OH position, an ether bridge and no N-methyl extension will be subject to conjugation and this metabolite will alter the processing of otherwise innocuous tactile stimuli. The fact that the phenomenon appeared at least partially stereospecific may reflect upon the fact that other laboratories have shown that glucuronyl transferase may preferentially convert (-)-morphine to the 3-glucuronide and (+)-morphine to the 6-glucuronide which may be less active.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacology of the allodynia in rats evoked by high dose intrathecal morphine. 334 33

A novel method for the preparation of theophylline granules coated with a polyelectrolyte complex of sodium tripolyphosphate and chitosan was developed. The theophylline granules containing sodium tripolyphosphate were stirred in an HCl solution of chitosan. During the mixing, the dissolved sodium tripolyphosphate in the granule moved to the surface and reacted with the chitosan, resulting in the formation of the polyelectrolyte complex film. The factors affecting the drug content, the particle size, and the coating-film thickness of the resultant coated granules were determined. The theophylline content in the coated granule decreased with increasing content ratio of sodium tripolyphosphate to theophylline in the original granule and with increasing chitosan concentration in the coating solution. The coated granule size increased with increasing chitosan concentration in the coating solution and with decreasing agitation speed. The coating-film thickness increased with an increase in the chitosan concentration, the pH of the coating solution, and the sodium tripolyphosphate to theophylline content ratio in the original granule. The drug-release pattern of the coated granules followed zero-order kinetics and the release rates were significantly reduced compared with that of the original granule.
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PMID:Novel method for the preparation of controlled-release theophylline granules coated with a polyelectrolyte complex of sodium polyphosphate-chitosan. 400 32

Pili separated from the cells of Corynebacterium renale strain 46 (type II) by agitation at high speed in a homogenizer were purified by repeated cycles of ammonium sulfate precipitation, sonic treatment, and centrifugation. The preparation of purified pili formed a single antigen-antibody line in agar gel and showed an absorption maximum at 275 nm. The pili subjected to dodecyl sulfate-polyacrylamide gel electrophoresis formed a main band and corresponded to the molecular weight of 19,000. The fact that the total nitrogen of the amino acids of the pili was nearly equal to its nitrogen content, together with the absence of detectable carbohydrate, has led to the conclusion that the pili are protein. The pilial protein was composed of 20 amino acids. Preparations of pili which had been treated with 0.5 n NaOH, but not with 1 n HCl, no longer appeared filamentous and failed to form a precipitate with the antibody in agar gels. A comparison has been made of the amino acid composition and certain properties of the pili of C. renale and type I pili and F pili of gram-negative bacteria.
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PMID:Chemical properties of the pili of Corynebacterium renale. 463 66

We have developed a preparation of hexamethylmelamine (HMM), dissolved in a fat emulsion Intralipid 20%, that is potentially satisfactory for parenteral administration to man. Solid HMM can be dissolved in Intralipid 20% up to 5 mg/ml, with extensive agitation. Solubilization of HMM is facilitated first by dissolving the drug in ethanol or in dimethylacetamide and then by adding the solution to Intralipid 20%. The disposition of HMM in rabbits after iv administration of HMM dissolved in Intralipid 20% was similar to the disposition of the drug following iv administration of HMM dissolved in 0.1 N HCl.
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PMID:Parenteral formulation of hexamethylmelamine potentially suitable for use in man. 680 43

The ideal of periodontal surgery is the total regeneration of the lost periodontal complex. A promising new osseous grafting material is Dental Matrix Gelation (DMG). DMG was prepared by a method similar to that of Conover and Urist (1979). This consisted of sequential extraction in 1:1 chloroform-methanol, 25 degrees C for 1 hour; 0.6 N HCl, 2 degrees C for 24 hours with constant agitation; 2 M CaCl2, 2 degrees C for 1 hour; 0.5 M EDTA pH 7.4, 2 degrees C for 1 hour; washed in distilled water 1 hour. Twelve rats were anesthetized, had heads shaved, midline flaps reflected, and 2 mm holes drilled through the right and left parietal bones. This type of osseous defect normally heals only by fibrous scarring and has been used to define osteoinductive materials. The DMG was cut into pieces about 1 mm square and placed into the right side defect while the left side remained open as a control. The animals were sacrificed on a schedule of two rats every 2 weeks until the 10th week when four rats were killed. The results showed complete osseous closure of the DMG site while the control healed by fibrous scarring. DMG seems to have strong osteoinductive power, and used allogenically has great potential as a commercially viable implant material.
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PMID:Dentin matrix gelatin (DMG) as a possible "universal" grafting material in periodontics. 694 46

Dextrorphan HCl (Ro 01-6794/706) is an NMDA receptor antagonist with clinical potential for administration in an elderly population of acute ischemic stroke patients. In vivo experience with such patients demonstrated a consistent pharmacologic effect/adverse experience profile that is typical of an NMDA receptor antagonist (e.g., nystagmus, nausea, vomiting, agitation, somnolence, hallucinations and hypertension). For the most part, these pharmacologic effects were mild to moderate in severity; short-lived; reversible; not life-threatening and subjectively tolerated. The most serious pharmacologic effect produced by dextrorphan administration was hypotension, which occurred within a well-defined window of 90 minutes from the start of the loading dose infusion in patients who received 200 mg/hr or greater loading dose infusions. In all cases it was reversible without neurologic sequelae. Careful review of demographic and pharmacokinetic parameters did not demonstrate any overriding factor(s) to the production of hypotension other than the rate of the loading dose infusion. Severe hypotension, severe decreased levels of consciousness and respiratory depression should not be generally expected at loading doses less than 200 mg/hr. In summary, dextrorphan can be safely given to an elderly population of ischemic stroke patients as a loading dose rate below 200 mg/hr and as a maintenance dose rate between 50-90 mg/hr for 24 hours when patients are monitored carefully for pharmacologic effects.
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PMID:Safety, tolerability and pharmacokinetics of the N-methyl-D-aspartate antagonist Ro-01-6794/706 in patients with acute ischemic stroke. The Dextrorphan Study Group and Hoffmann-La Roche. 748 11


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