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Journal of Vestibular Research :... 1998Space motion sickness is a well-recognized problem for space flight and affects 73% of crewmembers on the first 2 or 3 days of their initial flight. Illness severity is... (Review)
Review
Space motion sickness is a well-recognized problem for space flight and affects 73% of crewmembers on the first 2 or 3 days of their initial flight. Illness severity is variable, but over half of cases are categorized as moderate to severe. Management has included elimination of provocative activities and delay of critical performance-related procedures such as extra-vehicular activity (EVA) or Shuttle landing during the first three days of missions. Pharmacological treatment strategies have had variable results, but intramuscular promethazine has been the most effective to date with a 90% initial response rate and important reduction in residual symptoms the next flight day. Oral prophylactic treatment of crewmembers with difficulty on prior flights has had mixed results. In order to accommodate more aggressive pharmacologic management, crew medical officers receive additional training in parenteral administration of medications. Preflight medication testing is accomplished to reduce the risk of unexpected performance decrements or idiosyncratic reactions. When possible, treatment is offered in the presleep period to mask potential treatment-related drowsiness. Another phenomenon noted by crewmembers and physicians as flights have lengthened is readaptation difficulty or motion sickness on return to Earth. These problems have included nausea, vomiting, and difficulty with locomotion or coordination upon early exposure to gravity. Since landing and egress are principal concerns during this portion of the flight, these deficits are of operational concern. Postflight therapy has been directed at nausea and vomiting, and meclizine and promethazine are the principal agents used. There has been no official attempt at prophylactic treatment prior to entry. Since there is considerable individual variation in postflight deficit and since adaptation from prior flights seems to persist, it has been recommended that commanders with prior shuttle landing experience be named to flights of extended duration.
Topics: Antiemetics; Humans; Promethazine; Space Motion Sickness
PubMed: 9416592
DOI: No ID Found -
Infection and Immunity Mar 1973Promethazine hydrochloride at a concentration of 0.033 mg/ml has pronounced effects on leukocyte metabolism and function. The drug inhibits the phagocytosis-induced...
Promethazine hydrochloride at a concentration of 0.033 mg/ml has pronounced effects on leukocyte metabolism and function. The drug inhibits the phagocytosis-induced increases in O(2) consumption and hexose monophosphate shunt activity. Associated with these effects is an inhibition of the iodination of zymosan particles and an inhibition of bacterial killing by the cell. At least two mechanisms appear to be involved. Many of the effects can be explained by an inhibition of phagocytosis, but promethazine also inhibits the decarboxylation of amino acids and iodide fixation in a cell-free system, indicating a specific effect on metabolism. These results may partially account for the action of the drug in ameliorating the effects of erythroblastosis.
Topics: Cell Nucleus; Hexosephosphates; Humans; Leukocytes; Oxygen Consumption; Phagocytosis; Promethazine
PubMed: 4713692
DOI: 10.1128/iai.7.3.403-408.1973 -
Canadian Medical Association Journal Nov 1958
Topics: Analgesia; Anesthesia; Anesthesia and Analgesia; Female; Humans; Hypnotics and Sedatives; Labor, Obstetric; Pain Management; Pregnancy; Promethazine
PubMed: 13596915
DOI: No ID Found -
Anesthesiology 1957
Topics: Blood Circulation; Humans; Male; Promethazine; Respiration
PubMed: 13458866
DOI: 10.1097/00000542-195709000-00005 -
Die Pharmazie Nov 1979
Topics: Animals; Biotransformation; Male; Promethazine; Rats
PubMed: 545346
DOI: No ID Found -
Nature Jan 1966
Clinical Trial
Topics: Adult; Humans; Male; Motor Skills; Placebos; Promethazine; Visual Perception
PubMed: 5919589
DOI: 10.1038/209516a0 -
Biophysical Chemistry Feb 2006In this work the interaction of Hydroxyzine, Promethazine and Thioridazine with Langmuir films of dipalmitoylphosphatidylcholine (dpPC) and dipalmitoylphosphatidic acid...
In this work the interaction of Hydroxyzine, Promethazine and Thioridazine with Langmuir films of dipalmitoylphosphatidylcholine (dpPC) and dipalmitoylphosphatidic acid (dpPA), is studied. Temporal variations in lateral surface pressure (pi) were measured at different initial pi (pi(i)), subphase pH and drug-concentration. Drugs with the smallest (PRO) and largest (HYD) molecular size exhibited the lowest adsorption (k(a)) and the highest desorption (k(d)) rate constant values, respectively. The affinity binding constants (K(b)) obtained in monolayers followed the same profile (K(b,PRO) < K(b,HYD) < K(b,THI)) of the egg-PC/water partition coefficients (P) determined in bilayers. The drug concentration required to reach the half-maximal Deltapi at pi(i) = 14 mN/m (K(0.5)), was very sensitive to pH. The maximal increment in pi upon drug incorporation into the monolayer (deltapi(max)) will depend on the phospholipid collapse pressure (pi(c)), the monolayers's compressibility and drug's size, shape and charge. The higher pi(c) of dpPC lead to higher pi(cut-off) values (maximal pi allowing drug penetration), if compared with dpPA. In dpPC and dpPA pi(cut-off) decreased as a function of the molecular size of the uncharged drugs. In dpPA, protonated drugs became electrostatically trapped at the monolayer surface hence drug penetration, monolayer deformation and pi increase were impaired and the correlation between pi(cut-off) and drug molecular size was lost.
Topics: 1,2-Dipalmitoylphosphatidylcholine; Air; Hydroxyzine; Lipid Bilayers; Phosphatidic Acids; Promethazine; Surface Properties; Thioridazine; Water
PubMed: 16233945
DOI: 10.1016/j.bpc.2005.09.006 -
Journal of Pharmaceutical Sciences Aug 1978The kinetics of the thermal degradation of promethazine in an acidic medium under various conditions were investigated. The degradation of promethazine and the formation...
The kinetics of the thermal degradation of promethazine in an acidic medium under various conditions were investigated. The degradation of promethazine and the formation of some degradation products were studied under aerobic and anaerobic conditions. The influence of pH, metal ions such as copper(II) and iron (III), and antioxidants was investigated. In an oxygen-saturated medium, promethazine generally followed first-order kinetics. Increasing the pH increased the degradation rate to a limiting value at pH 5. Addition copper (II) increased the degradation rate over the whole process, while iron (III) caused an increase for only a short time. Ascorbic acid sometimes increased the degradation rate, while higher concentrations of hydroquinone also accelerated the degradation. Pyrosulfite did not have any influence. Under anaerobic conditions, promethazine degraded only in the presence of copper (II) and iorn (III) ions. As a result of the studies on the qualitative and quantitative aspects of the oxidation process, a mechanism for the oxidative degradation of promethazine is suggested. Promethazine 5-oxide and a number of degradation products without intact side chains are formed via a semiquinone free radical. The influence of several factors on the degradation process is discussed.
Topics: Antioxidants; Chemical Phenomena; Chemistry; Drug Stability; Hydrogen-Ion Concentration; Kinetics; Metals; Oxidation-Reduction; Oxygen; Promethazine; Temperature
PubMed: 27627
DOI: 10.1002/jps.2600670828 -
Xenobiotica; the Fate of Foreign... Sep 19811. Incubation of promethazine (Ia) and desmethylpromethazine (Ib) with 9000g supernatant fractions of rabbit liver homogenate resulted in formation of N-dealkylated,...
1. Incubation of promethazine (Ia) and desmethylpromethazine (Ib) with 9000g supernatant fractions of rabbit liver homogenate resulted in formation of N-dealkylated, N-oxygenated and ring-hydroxylated products. 2. The N-oxidation products identified by t.l.c. and mass spectra using synthetic reference products are promethazine-N-oxide (IX) and the nitrone (VIII), which is believed to be formed chemically and metabolically from the metabolite N-hydroxydesmethylpromethazine (VII).
Topics: Animals; Chromatography, Thin Layer; Gas Chromatography-Mass Spectrometry; Liver; Male; Oxidation-Reduction; Promethazine; Rabbits
PubMed: 7314643
DOI: 10.3109/00498258109045872 -
Aviation, Space, and Environmental... Mar 1993Intramuscular promethazine and its efficacy in the treatment of Space Motion Sickness (SMS) were evaluated using standardized questions administered during postflight...
Intramuscular promethazine and its efficacy in the treatment of Space Motion Sickness (SMS) were evaluated using standardized questions administered during postflight debriefings to crewmembers immediately after their first Shuttle flight. Space Motion Sickness was graded as none, mild, moderate, or severe, based on published criteria. Immediate symptom relief (within 1-2 h) was evaluated by subjective reports; medication efficacy was based on scores derived from the four most frequently reported symptoms of SMS: nausea, vomiting, loss of appetite, and stomach awareness. Scores were given for each symptom, mild = 1, moderate = 2, and severe = 3, and added for a total score for each flight day. Following intramuscular (IM) promethazine on flight day 1, the scores were used to determine if the crewmembers were "sick" or "not sick" on flight day 2. On the basis of the scoring criteria, any subject with a score adding to greater than three, with any severe symptom, or with vomiting was defined as "sick." The comparison showed that 25% of crewmembers treated with IM promethazine were "sick" on flight day 2, compared to 50% of crewmembers who did not receive promethazine (p = 0.046). Of crewmembers treated with IM promethazine, 90% reported immediate symptom relief as well. Untreated crewmembers typically have slow symptom resolution over 72-96 h, and those treated with oral scopolamine/dextroamphetamine show delayed symptom development. This study suggests that intramuscular promethazine is an effective treatment for SMS and merits continued use and further controlled investigations.
Topics: Female; Humans; Injections, Intramuscular; Male; Motion Sickness; Promethazine; Space Flight
PubMed: 8447805
DOI: No ID Found