Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

For a period of six months, we collected 12 cases of nocturnal asthmatics (7 males, 5 females); their ages ranged from 20 to 66 (the average age is 49). We found that administration of Uniphyllin (10 mg/kg) once a day at 6 PM could maintain the blood level of theophylline within therapeutic range at least 12 to 24 hrs. The peak expiratory flow rate of the 6 cases we collected, were significantly improved. The result of pharmokinetic parameters: 1) The average of a single dose (12 cases) is AUC (ug. hr/ml) 275.1 +/- 62. k; Kel (hr-1) 0.068 +/- 0.019; Ka (hr-1) 0.33 +/- 0.07); Tmax (hr) 6.3 +/- 1.4; T 1/2 (hr) 11.2 +/- 4.4; Clearance/F (ml/kg/hr) 37.9 +/- 9.0.2). The average of steady state (12 cases) is Css (mg/L) 5. 7 +/- 2.6; Cmax-Cmin (mg/L) 10.09 +/- 1.46.3). The average of relative bioavailability (3 cases) is 82%, 83%, 102%. However, the extent of absorption data is available for only 3 subjects. There are too few subjects to draw any meaningful conclusions about this relative bioavailability. Four cases show slight symptoms, including 1 case of dizziness, 2 cases of nausea, and 1 case gaseousness. It is suggested that the drug be administered at about 6-8 PM to coincide peak levels in the early morning in nocturnal asthmatics.
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PMID:Sustained-release theophylline-uniphyllin in nocturnal asthmatics. 276 61

In a randomized, multiple-dose, cross-over study, serum theophylline concentrations (STC) were compared in 12 healthy volunteers for 24 hours after the first and seventh administration of two sustained-release formulations. The preparations tested were the new encapsulated micro-osmotic system Euphylong (E) and the tablet Uniphyllin (U). Daily doses of 800 mg were administered at 7 p.m., half an hour after a standardized evening meal. The relative bioavailability of E with respect to U under steady-state conditions is 93 (83-105)%. In contrast to U, E markedly truncates the high peak concentrations and leads to a sustained, plateau-like concentration throughout the night. Therefore prediction of individual maximum serum levels becomes possible for E on the basis of one blood sample taken in the morning. The significantly improved in vivo performance of E in comparison with U is reflected in a 50% reduction of the swing, a 60% increase in the plateau time, and a substantial reduction of theophylline-specific side effects such as nausea, palpitations and increased diuresis.
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PMID:Once daily theophylline: multiple-dose comparison of an encapsulated micro-osmotic system (Euphylong) with a tablet (Uniphyllin). 375 79

We evaluated an oral theophylline loading-dose procedure that was designed to rapidly achieve and sustain theophylline serum concentrations of approximately 10 to 12 micrograms/mL. Ten healthy adults were given an oral loading dose of approximately 6 mg/kg of aminophylline, (Aminophyllin) (ie, 4.8 mg/kg of theophylline). Two hours later, each subject was given approximately 6 mg/kg of a sustained-release theophylline tablet (Theo-Dur). Serum samples were collected at 1/2, 1, 2, 3, 6, 9, and 12 hours, then assayed for theophylline concentration. The mean theophylline concentration (+/- SD) one hour after the initial loading dose was 10.5 +/- 2.3 micrograms/mL. Subsequent theophylline concentrations demonstrated minimal fluctuation, with means ranging from 10.7 +/- 1.6 to 13.6 +/- 2.8 micrograms/mL. Four of the subjects reported headache; none vomited or experienced severe nausea. We conclude that this method of oral theophylline loading can be effective in achieving prompt and sustained therapeutic theophylline levels without significant side effects and that this may provide a valuable therapeutic alternative in those asthmatic patients who do not clearly require intravenous aminophylline therapy.
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PMID:Rapid and sustained oral theophylline loading. An alternative to intravenous aminophylline therapy. 683 1

This multicenter, randomized, investigator-blinded, parallel group study compared the effects of converting patients from a q12h extended-release theophylline preparation (Theo-Dur) to a q24h extended-release product (Uni-Dur). Patients (n = 133) first received open-label Theo-Dur treatment with dosage titrated to achieve peak serum theophylline concentrations of 10-20 micrograms/ml. Patients then were randomized to continue Theo-Dur (n = 64) or to convert to Uni-Dur (n = 60) with peak serum theophylline concentrations maintained in the desired range. Pulmonary function tests were performed during the open-label and blinded periods; patients maintained diaries and performed peak flow measurements before each dose of study treatment. Adverse events were recorded throughout the study. Respiratory status during blinded treatment was rated as the same or improved compared with open-label treatment by > 87% of evaluable patients and physicians, regardless of treatment group. There were no significant differences in mean peak serum theophylline concentrations at baseline, at the final evaluation, or at any point during the study. Few dosage adjustments were necessary (5/52, Uni-Dur; 9/57, Theo-Dur). There were no significant changes in pulmonary function test results or patient diary entries between the open-label and blinded periods. Headache and nausea were the most commonly reported adverse events. In conclusion, converting patients from twice- to once-daily theophylline treatment resulted in no significant changes in any measures of pulmonary function, and there were no significant differences between the groups during the blinded treatment period.
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PMID:Conversion from twice- to once-daily extended-release theophylline treatment in patients with reversible airway obstruction. 762 3

Many attempts have been made to achieve good selectivity to targeted tumor cells by preparing specialized carrier agents that are therapeutically profitable for anticancer therapy. Among these, liposomes are the most studied colloidal particles thus far applied in medicine and in particular in antitumor therapy. Although they were first described in the 1960s, only at the beginning of 1990s did the first therapeutic liposomes appear on the market. The first-generation liposomes (conventional liposomes) comprised a liposome-containing amphotericin B, Ambisome (Nexstar, Boulder, CO, USA), used as an antifungal drug, and Myocet (Elan Pharma Int, Princeton, NJ, USA), a doxorubicin-containing liposome, used in clinical trials to treat metastatic breast cancer. The second-generation liposomes ("pure lipid approach") were long-circulating liposomes, such as Daunoxome, a daunorubicin-containing liposome approved in the US and Europe to treat AIDS-related Kaposi's sarcoma. The third-generation liposomes were surface-modified liposomes with gangliosides or sialic acid, which can evade the immune system responsible for removing liposomes from circulation. The fourth-generation liposomes, pegylated liposomal doxorubicin, were called "stealth liposomes" because of their ability to evade interception by the immune system, in the same way as the stealth bomber was able to evade radar. Actually, the only stealth liposome on the market is Caelyx/Doxil (Schering-Plough, Madison NJ, USA), used to cure AIDS-related Kaposi's sarcoma, resistant ovarian cancer and metastatic breast cancer. Pegylated liposomal doxorubicin is characterized by a very long-circulation half-life, favorable pharmacokinetic behavior and specific accumulation in tumor tissues. These features account for the much lower toxicity shown by Caelyx in comparison to free doxorubicin, in terms of cardiotoxicity, vesicant effects, nausea, vomiting and alopecia. Pegylated liposomal doxorubicin also appeared to be less myelotoxic than doxorubicin. Typical forms of toxicity associated to it are acute infusion reaction, mucositis and palmar plantar erythrodysesthesia, which occur especially at high doses or short dosing intervals. Active and cell targeted liposomes can be obtained by attaching some antigen-directed monoclonal antibodies (Moab or Moab fragments) or small proteins and molecules (folate, epidermal growth factor, transferrin) to the distal end of polyethylene glycol in pegylated liposomal doxorubicin. The most promising therapeutic application of liposomes is as non-viral vector agents in gene therapy, characterized by the use of cationic phospholipids complexed with the negatively charged DNA plasmid. The use of liposome formulations in local-regional anticancer therapy is also discussed. Finally, pegylated liposomal doxorubicin containing radionuclides are used in clinical trials as tumor-imaging agents or in positron emission tomography.
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PMID:From conventional to stealth liposomes: a new frontier in cancer chemotherapy. 1290 76

A 48-year-old woman presented to the Accident and Emergency department with a 4 month history of headaches, nausea and dizziness. She was found to have severe hypertension and hypokalaemia. Extensive investigations did not find any secondary cause for hypertension. The patient was discharged with oral doxazosin therapy which controlled the blood pressure. Before the follow-up appointment at the hypertension clinic, the patient and her husband identified that her headaches coincided with liquorice tea consumption of up to three cups per day. This information was not obtained in the clinical assessment. The patient is now headache and medication free after cessation of liquorice tea. Liquorice ingestion is often a forgotten reversible cause of hypertension. A good history is key to this diagnosis.
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PMID:All sorts of tests, only one question: an unexpected cause of hypertension. 2912 28