Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Promethazine”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 37 records · Page 2Linked to original sources

Changes in the disposition of promethazine during multiple dosing in the rabbit.

During a multiple dosing regimen, the area under the promethazine blood concentration-time profile progressively decreased indicating auto-induction of metabolism. The increase in promethazine clearance (mean 35%) was not reflected in changes in either elimination half-life or minimum blood concentrations during the dosing interval. This was attributed to a deep compartment in the disposition of promethazine in the rabbit. The changes in promethazine clearance were accompanied by proportionally larger changes in the clearance of the monodesmethylpromethazine metabolite. The effect of promethazine pretreatment on the clearance of antipyrine was also studied and was found to be significantly increased by a mean of 17% following pretreatment with promethazine. However, the changes in the clearance of antipyrine did not highly correlate with those of promethazine and monodesmethylpromethazine. This may indicate that promethazine induces metabolic systems in the rabbit for which antipyrine is not a good substrate.

Animals↗

Suggestion of a role for calmodulin and phosphorylation in regulation of rabbit ileal electrolyte transport: effects of promethazine.

Suggestion of a role for protein phosphorylation in the regulation of intestinal active NaCl transport was found by studying the effects of low concentrations of promethazine on Ca2+-calmodulin (CaM)-dependent protein phosphorylation of ileal microvillus membranes and on active ileal electrolyte transport. Ca2+-CaM increased the phosphorylation of six microvillus peptides (Mr 137,000, 116,000, 77,000, 58,000, 53,000, and 50,000) in a concentration-dependent manner. Promethazine inhibited the Ca2+-CaM-induced increases in each of these phosphorylations. The effect of promethazine was concentration dependent, with concentrations of 5-12 microM (mean 8 microM) causing 50% inhibition. Promethazine also caused a concentration-dependent increase in net Cl absorption and decrease in the ileal short-circuit current, with 9 microM promethazine causing a change in short-circuit current 50% of maximum. The promethazine effect on microvillus membrane phosphorylation was specific, since neither cAMP- and cGMP-induced phosphorylation in the microvillus membrane nor the stimulation by Ca2+-CaM of myosin light chain kinase phosphorylation of myosin light chain were affected by promethazine. The similar, and unusual sensitivity to low concentrations of promethazine on ileal microvillus membrane phosphorylation increased by Ca2+-CaM and on ileal electrolyte transport is consistent with Ca2+-CaM-dependent microvillus membrane phosphorylation being involved in the regulation of active electrolyte transport in ileal absorptive cells.

Animals↗

No more than necessary: safety and efficacy of low-dose promethazine.

BACKGROUND: Limitations in antiemetic options have resulted in increased use of intravenous promethazine. However, this drug has significant sedative effects with its standard dosage of 25 mg, especially when used in conjunction with narcotic analgesics. While studies have revealed the bioavailability of enteric promethazine to be 25%, current dosing references suggest identical dosing regardless of the route of administration. OBJECTIVE: To compare the antiemetic efficacy and sedative effects of low-dose intravenous promethazine (6.25 or 12.5 mg) with intravenous ondansetron 4 mg. METHODS: We assessed inpatients with noncritical conditions at Anne Arundel Medical Center who were treated for nausea or vomiting from any cause except chemotherapy or pregnancy. Forty-six patients received low-dose promethazine and 41 received ondansetron. Statistical analysis was carried out for significant differences in efficacy and sedation. RESULTS: For patients who received intravenous promethazine 6.25 or 12.5 mg, nausea and vomiting were relieved at one hour in 74% and 68%, respectively, compared with 59% for intravenous ondansetron 4 mg. Results at 3 hours were 67% and 80% for promethazine and 71% for ondansetron. Median sedation scores at one hour were equal at 3 for promethazine and ondansetron (4 = fully awake); at 3 hours, the median scores were 4 and 3.5, respectively. There were no statistically significant differences among any of these results. CONCLUSIONS: Low-dose (6.25 mg) intravenous promethazine relieves nausea and vomiting as effectively as intravenous ondansetron 4 mg.

Antiemetics↗

Effects of promethazine on nocturnal sleep in normal man.

The effects of a phenothiazine, on sleep in ten healthy volunteers were investigated in two double blind polygraphic studies. The first part consisted of a single dose study with promethazine 50, 100, and 200 mg, using pentobarbital 100 mg as a reference substance. In the second part, four subjects spent 20 consecutive nights with nine drug nights (promethazine 100 mg), followed by a placebo withdrawal period of six nights, in the sleep laboratory. Promethazine showed a dose related REM-depressing effect with a greater decrease, the higher the dose. The placebo value was 20.7% REM of total sleep time and gave 16.3, 13.5 and 11.4 respectively, for promethazine 50, 100 and 200 mg. Pentobarbital gave 16.2% REM. There was also an increase of stage II and with the highest dose an increase of stage III + IV. An increase of REM-latency together with a decrease of REM-periods was also seen, and while pentobarbital gave a decrease in REM-density, promethazine did not cause any changes in the phasic REM-component. A REM-rebound was seen in the first night of withdrawal with an increase of per cent REM from 19.9%-25.1%. The mean for the whole withdrawal period was 23.1%. Promethazine in the highest dose, 200 mg, gave drowsiness and hangover effects in 14 nights out of 20. The REM-depressing effect of promethazine together with its relatively weak REM-rebound effect may explain its value in the treatment of withdrawal symptoms following abuse of alcohol and barbiturates.

Adult↗

Antiemetic prophylaxis with promethazine or droperidol in paediatric outpatient strabismus surgery.

This randomized, double-blind study evaluated the antiemetic efficacy and the side-effects of promethazine pretreatment (0.5 mg.kg-1 IV + 0.5 mg.kg-1 IM) versus droperidol + placebo pretreatment (droperidol, 0.075 mg.kg-1 IV + physiological saline, 0.02 ml.kg-1 IM). One hundred unpremedicated ASA physical status I children ranging from two to ten years, and undergoing outpatient strabismus surgery were studied. All children received inhalational anaesthesia with halothane, nitrous oxide and oxygen. Neither opioids nor muscle relaxants were used. The incidence of vomiting and/or retching and the incidence of side-effects were determined in the post-anaesthesia recovery room (PARR), in the short-stay surgical unit (SSSU), and after discharge from the hospital (including the journey and the stay at home during the first postoperative day). Promethazine and droperidol were equally effective in reducing the incidence of vomiting before discharge to two and eight per cent respectively. On the contrary, the incidence of vomiting after discharge and overall were significantly less with promethazine (ten and ten per cent) than with droperidol pretreatment (54 and 56 per cent) (P less than 0.0001). Promethazine permitted the time to discharge from the hospital to be reduced to an average of three hours, without increasing the incidence of vomiting postdischarge. Promethazine pretreatment is much less expensive than droperidol pretreatment. The incidence of restlessness was significantly less with droperidol (eight per cent) than with promethazine (36 per cent) (P less than 0.001). Promethazine pretreatment demands the use of an analgesic like acetaminophen in order to reduce the incidence of postoperative pain and restlessness.(ABSTRACT TRUNCATED AT 250 WORDS)

Ambulatory Surgical Procedures↗

Sedation with promethazine profoundly affects spontaneous airway protection in sleeping neonatal piglets.

1. Phenothiazine use in infants has been implicated in apparent life-threatening events, sleep apnoea and Sudden Infant Death Syndrome. 2. The aim of this study was to investigate the cumulative effects of a commonly used antihistamine medication containing promethazine on airway protective mechanisms and cardiorespiratory responses in 42 healthy neonatal piglets (21 naturally sleeping, 21 sedated sleeping). 3. Sedated piglets were given 1.5 mg/kg, p.o., promethazine 2 h prior to each recording session. Control animals slept naturally with no sedative given. On three consecutive days in all piglets, physiological recordings were made during sleep; on at least one of these days, simultaneous physiological and radiological observations were made. 4. Following sedation, sleep time and time in active sleep were increased significantly (P < 0.01). The spontaneous occurrence of swallowing, arousal, body movement, gastrooesophageal reflux and apnoea was compared between naturally and sedated sleeping piglets. Sedation with promethazine significantly decreased the spontaneous occurrence of swallowing (P < 0.05) and arousal (P < 0.05) and increased the occurrence of both central (P < 0.05) and obstructive sleep apnoea (P < 0.0001). 5. By the third day, a cumulative effect of promethazine was seen; the rate of swallowing and body movement significantly decreased (P < 0.01). 6. In summary, a low dose of promethazine profoundly altered sleep characteristics, airway protective mechanisms and cardiorespiratory responses in normal healthy sleeping piglets. Continued use of promethazine over several days may attenuate airway protective mechanisms to a potentially life-threatening degree. Our findings support continued caution in the use of promethazine-containing medications for the sedation of infants.

Animals↗

Prochlorperazine versus promethazine for uncomplicated nausea and vomiting in the emergency department: a randomized, double-blind clinical trial.

STUDY OBJECTIVE: Nausea and vomiting related to gastritis or gastroenteritis are common complaints in the emergency department. The most effective antiemetic agent is yet undetermined. This study was conducted to compare the efficacy of prochlorperazine versus promethazine for uncomplicated nausea and vomiting in the ED. METHODS: The study was a randomized, double-blind comparison of prochlorperazine (Compazine) and promethazine (Phenergan) for acute ED treatment of gastritis or gastroenteritis. We studied patients 18 years or older with presumed uncomplicated gastritis or gastroenteritis who presented to 2 academic EDs. Patients were randomly assigned to receive either prochlorperazine, 10 mg intravenously, or promethazine, 25 mg intravenously. Visual analog scale readings of patient comfort were obtained at baseline and at 30- and 60-minute intervals. The primary endpoint was degree of relief at 30 and 60 minutes. Secondary endpoints were time to complete relief, need for further antiemetic medication (treatment failures), and side effects. Statistical analysis was performed using the Mann-Whitney U test for nonparametric analysis and repeated-measures analysis of variance (ANOVA). RESULTS: Eighty-four patients were enrolled in the study; 42 received prochlorperazine and 42 received promethazine. There were no differences in demographics in the 2 groups. At baseline (time 0), there was no difference in symptoms (P =.23). At 30 and 60 minutes after receiving medication, prochlorperazine worked significantly better than promethazine (P =.004 and P <.001 using nonparametric analysis). Using repeated-measures ANOVA, there was a significant difference in symptoms over time for both groups (P <.001) and a significant difference in prochlorperazine versus promethazine (P =.002). Time to complete relief was significantly shorter with prochlorperazine (P =.021). There were significantly fewer treatment failures with prochlorperazine (P =.03, 9.5% versus 31%; difference 21%, 95% confidence interval 5 to 38). There was no difference in incidence of extrapyramidal effects. Prochlorperazine caused significantly fewer complaints of sleepiness (P =.002, 38% versus 71%; difference 33%, 95% confidence interval 13 to 53; P =.002). CONCLUSION: Prochlorperazine works significantly better than promethazine for relieving symptoms of nausea and vomiting more quickly and completely in ED patients with uncomplicated nausea and vomiting.

Adolescent↗

Study of the prophylactic effect of droperidol, alizapride, propofol and promethazine on spinal morphine-induced pruritus.

BACKGROUND: We have compared the use of alizapride, propofol, droperidol and promethazine for the prevention of spinal morphine-induced pruritus. METHODS: Three hundred ASA I or II women undergoing Caesarean section under spinal anaesthesia, in which morphine 0.2 mg was added to a local anaesthetic, were assigned randomly to receive i.v., in the operating room, just after delivery of the baby, alizapride 100 mg, propofol 20 mg, droperidol 1.25 mg, promethazine 50 mg or saline 2 ml (control group). In the postoperative period, the women were assessed for pruritus (absent, mild, moderate or severe) or other untoward symptoms by blinded observers. We used 95% confidence limits (95% CI) for the cumulative incidence of moderate and severe pruritus to compare the groups, and the NNT and 95% CI to compare droperidol, propofol and alizapride as for their effectiveness in preventing pruritus. For other untoward effects, the chi(2)-test was used, results being considered significant when P<0.05. RESULTS: The droperidol, propofol and alizapride groups had significantly lower incidences of pruritus compared with the control and promethazine groups, while the incidence of pruritus was similar among the patients assigned to the promethazine and control groups. As for the prevention of moderate and severe pruritus, droperidol had the lowest NNT (3.52; 95% CI: 3.37-3.67), followed by propofol (4.61; 95% CI: 4.45-4.77) and alizapride (5.43; 95% CI: 5.27-5.59). As for untoward effects, droperidol and promethazine increased the incidence of somnolence, which seemed more severe with promethazine. Otherwise, there were no differences between the groups. CONCLUSION: Droperidol, propofol and alizapride, in a decreasing order of effectiveness in the doses used in this study, reduced the incidence of pruritus induced by the use of morphine 0.2 mg intrathecally. On the other hand, promethazine 50 mg was shown to be ineffective.

Adolescent↗

CYP2D6 is the principal cytochrome P450 responsible for metabolism of the histamine H1 antagonist promethazine in human liver microsomes.

To determine which cytochrome P450 form is involved in the promethazine [10-(2-dimethylaminopropyl) phenothiazine] metabolism, in vitro analysis using human liver microsomes were performed. Promethazine was mainly biotransformed to ring-hydroxylated, S-oxidized and N-demethylated metabolites. The promethazine hydroxylase in human liver microsomes was inhibited by SKF-525A, propranolol, sparteine, quinidine and anti-CYP2D6 serum suggesting involvement of a P450 related to CYP2D6. Lineweaver-Burk plots for the hydroxylation, S-oxidation and N-demethylation indicated that the hydroxylation occurred with a low K(m) value in human liver microsomes. Microsomes from genetically-engineered human B-lymphoblastoid cells expressing CYP2D6 hydroxylated promethazine most efficiently as compared to other P450 forms, indicating that it was the principal P450 responsible for the metabolism of promethazine in human liver microsomes. The inhibition of CYP2D6-catalysed bufuralol 1'-hydroxylase by various histamine H3 antagonists including promethazine suggested that promethazine and some other histamine H1 antagonists could be inhibitors of this P450 in human liver microsomes.

Antibodies↗

Promethazine for the treatment of agitation after electroconvulsive therapy: a case series.

OBJECTIVES: Agitation after electroconvulsive therapy (ECT) is observed in approximately 7% of patients. Promethazine is an antihistamine with sedative properties that has no antiseizure effects and therefore can be administered before ECT to prevent the onset of agitation. In the current study, we present a series of 8 patients who reacted to ECT with severe agitation and improved under the treatment of promethazine. METHODS: Eight patients were included (5 women, 3 men), ages 22 to 77 years. All patients showed severe post-ECT agitation as demonstrated by severe restlessness, crying, or mumbling loudly. Seven of them required the administration of intravenous midazolam. ECT was given according to established clinical protocols at the Sheba Medical Center. All patients were prescribed either 25 to 50 mg of promethazine 2 hours before the treatment to avoid agitation. RESULTS: All 8 patients suffered from extreme agitation after ECT treatment, and 7 required the administration of intravenous midazolam. After a clinical protocol, these patients were prescribed 25-50 mg of promethazine orally 60-120 minutes before the ECT. Improvement was observed in all patients both immediately post-ECT and also in their overall sense of well-being after the ECT. No patient complained of adverse reactions to the promethazine. Most patients reported a relief in pre-ECT fears. CONCLUSION: In this small case series, we found that promethazine can be used to prevent post-ECT agitation. Further double-blind controlled studies are needed to better evaluate the usefulness and appropriateness of promethazine in the prevention of pre-ECT fears and post-ECT agitation.

Adult↗

Premedication with promethazine and transdermal scopolamine reduces the incidence of nausea and vomiting after intrathecal morphine.

Intrathecal morphine provides effective postoperative pain relief in major orthopaedic surgery. In use, however, is associated with unpleasant side effects like nausea and vomiting. The effect of different premedications on postoperative emetic sequelae induced by intrathecal morphine was studied in a prospective, double blind study. Sixty patients scheduled for arthroplasty surgery of the lower extremity were anaesthetized with spinal anaesthesia with a combination of isobaric bupivacaine 20 mg and morphine 0.3 mg. For premedication the patients were randomised to three groups of equal size. They received either oral diazepam (5-15 mg), oral promethazine (10 mg) or a combination of promethazine and transdermal scopolamine (1.5 mg). Sixty percent of the patients with both promethazine and transdermal scopolamine were totally free from postoperative nausea and vomiting (PONV) symptoms compared to those premedicated with diazepam (40%) or promethazine alone (30%). Promethazine together with transdermal scopolamine reduced significantly the number of patients with vomiting (to 25%) and also vomiting episodes. This combination was also more efficient in reducing the incidence of nausea (to 25%) and nausea episodes than promethazine along (P < 0.05). Combination also reduced the requests for additional pain relief (P < 0.05). PONV occurred in a majority of patients during the first 12 hours of the 24 hour study period and the need for additional analgesics thereafter. The incidence of itching (50-65%) and urinary catheterisation (55-70%) was similar in all groups. In conclusion, the combination of oral promethazine and transdermal scopolamine was most effective in reducing PONV symptoms and also reduced the need for postoperative pain treatment.

Administration, Cutaneous↗

Blockade of Na+ current by promethazine in guinea-pig ventricular myocytes.

1. To elucidate the antiarrhythmic mechanism of promethazine, its effects on the fast Na+ current (INa) were examined in single guinea-pig ventricular myocytes by whole-cell voltage clamp methods. 2. Promethazine blocked INa with a KD of 42.6 microM and Hill's coefficient of 1.1 at a holding potential of -140 mV. 3. The INa blockade was enhanced at a less negative holding potential of -80 mV with a change of KD to 4.4 microM. Although 10 microM promethazine did not change the inactivation time constants of INa, it shifted the steady-state inactivation curve (h infinity curve) toward more negative potentials by 19.5 mV with the slope factor unaffected. 4. Double pulse experiments revealed that the development of blockade followed two-exponential functions having time constants of 7 and 220 ms at -20 mV. 5. Promethazine slowed the repriming of INa. This was associated with the development of slow phase having a time constant of 1160 +/- 59 ms. 6. Promethazine produced a profound use-dependent block when the cell was repeatedly stimulated with interpulse intervals shorter than 1 s. However, short pulses of 2 ms duration hardly produced such a use-dependent block. Hence, open channel blockade is considered to play a minor role in the promethazine action on INa. 7. These results suggest that promethazine blocks cardiac INa in a manner similar to class I antiarrhythmic drugs and that this effect may account for its antiarrhythmic action.

Algorithms↗

Multiple effects of promethazine in Staphylococcus aureus.

The antibiotic resistance of 6 Staphylococcus aureus strains was eliminated with a frequency from 1.2 to 10% in the presence of subinhibitory concentrations of promethazine. The pigment production of the cells was also eliminated by the promethazine to an extent of 0 to 5%. The cell size was increased and the protein A production was markedly decreased in S. aureus cells cultured in the presence of promethazine. Complex formation between protein A and promethazine was detected by differential spectrophotometry. The biological activity of staphylococcus protein A was abolished by promethazine in the passive haemagglutination of rabbit antiserum treated sheep red blood cells. Evidence has been found that plasmid-encoded functions of S. aureus cells can be altered in the presence of promethazine, and the chromosomally controlled synthesis of protein A, one of the weakest virulence factor of S. aureus is also lowered by promethazine.

Drug Resistance, Microbial↗

Haloperidol plus promethazine for psychosis induced aggression.

BACKGROUND: Health services often manage agitated or violent people and for emergency psychiatric services such behaviour is particularly prevalent (10%). The drugs used in this situation should ensure that the person swiftly and safely becomes calm. OBJECTIVES: To examine whether haloperidol plus promethazine is an effective treatment for psychosis induced agitation/aggression. SEARCH STRATEGY: We searched the Cochrane Schizophrenia Group's Register (July 2004). SELECTION CRITERIA: We included all randomised clinical trials involving aggressive people with psychosis for which haloperidol plus promethazine was being used. DATA COLLECTION AND ANALYSIS: We reliably selected, quality assessed and extracted data from all relevant studies. For binary outcomes we calculated standard estimations of risk ratio (RR) and their 95% confidence intervals (CI). Where possible we estimated weighted number needed to treat or harm (NNT/H). MAIN RESULTS: We identified two relevant high quality studies. One compared the haloperidol plus promethazine mix with midazolam (n=301) and one with lorazepam (n=200). The combined results were largely heterogeneous. In Brazil, haloperidol plus promethazine was an effective means of tranquillisation with over two thirds of people being tranquil or sedated by 30 minutes, but midazolam was more swift (n=301, RR 2.9 CI 1.75 to 4.80, NNH 5 CI 3 to 12). In India, however, 95% of people were tranquil or sedated by 30 minutes if allocated to the combination treatment (vs lorazepam, n=200, RR 0.26 CI 0.10 to 0.68, NNT 8 CI 6 to 17). Over the next few hours of treatment reported differences are negligible. One person given midazolam had respiratory depression (reversed by flumazenil), one given lorazepam had respiratory difficulty. A single person given haloperidol plus promethazine had an epileptic fit. Once the initial tranquillisation was administered, few needed additional medications for continued agitation (n=501, 2 RCTs, RR needing additional tranquillising drugs by four hours 1.67 CI 0.62 to 4.54, 4% vs 2%, I squared 50%) and there were no differences in the low levels of use of restraints. About 28% of people in Brazil in both groups had another episode of aggression in the first day after the initial injection (n=301, RR 0.89 CI 0.62 to 1.29). About half of all people in the Indian study were discharged by four hours (n=200, RR 1.13 CI 0.85 to 1.50) and a similar proportion in Brazil by 15 days (n=301, RR 1.05 CI 0.84 to 1.29). Both studies attained 99% follow up for their primary outcomes. Even by two weeks only 4% of people could not be accounted for (n=501, 2 RCTs, RR 0.91 CI 0.38 to 2.17). AUTHORS' CONCLUSIONS: This review suggests that both benzodiazepines work, but that midazolam has a faster onset and thereby reduces the risk of exposure to violence. Both benzodiazepines have the potential to cause respiratory depression, probably midazolam more so than lorazepam, and we would question the use of this group of drugs outside of those services fully confident of observing for and managing the consequences of respiratory distress. Most evidence, however, exists for the haloperidol plus promethazine mix, with currently more than 400 people randomised to the combination. The onset of action is swift and faster than lorazepam. The combination also seems safe with no clear longer term consequences. We would expect policy makers recommending other drug managements to have equally compelling evidence to support their guidance and hope that this would not be founded in conjecture or consensus, which may be more difficult to defend than evidence from high quality studies.

Aggression↗

A retrospective study of promethazine and its failure to produce the expected incidence of sedation during space flight.

Since March 1989, intramuscular (IM) promethazine has been successfully used to treat the symptoms of space motion sickness. The incidence of sedation associated with promethazine administration on the ground is large and may result in operational impact. The authors undertook a retrospective study to quantify the incidence of sedation from promethazine use during Space Shuttle flights. Crew medical debriefings from 14 shuttle missions were reviewed for crew members who had been treated with IM promethazine and their corresponding symptoms were identified. Twenty-one crew members received IM promethazine (25-50 mg), and only one experienced any associated sedation with no operational impact. This sedation incidence of less that 5% is in stark contrast to the 60 to 73% incidence of sedation seen in ground-based studies. The incidence of sedation during space flight from IM promethazine is substantially less than that seen on the ground and does not present an operational problem during Space Shuttle flights. Future investigations of environmental stressors and pharmacodynamic changes associated with space flight may explain the huge disparity between the space-flight and ground-based data.

Humans↗

Oxidative degradation of pharmaceutically important phenothiazines III: Kinetics and mechanism of promethazine oxidation.

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.

Antioxidants↗

Human whole blood and parotid saliva concentrations of oral and intramuscular promethazine.

Ten healthy male subjects received 25 mg of promethazine intramuscularly, followed within 3 weeks by oral administration of 25 mg. Whole blood and parotid saliva were collected over a 12-hr period after drug administration. Promethazine was quantitated by high-performance liquid chromatography. After intramuscular administration, the promethazine concentrations were 3.0-22.4 ng/ml in blood and 0.9-2.8 ng/ml in parotid saliva. After oral administration, the promethazine concentrations were 1.4-5.5 ng/ml in blood and 0.2-0.8 ng/ml in parotid saliva. The peak blood promethazine concentration after the intramuscular dose was four times higher than that following the oral dose, which indicates that promethazine possesses an extensive first-pass effect. The mean parotid saliva to whole blood ratio (S/B) was calculated to be 0.24 after the intramuscular route an 0.20 after the oral route over the 12-hr period. The calculated percentage of free drug in the blood was 20-24% of the whole blood concentration determined from the S/B ratio.

Administration, Oral↗

[Multidimensional psychometric assessment of preoperative mood. Effects of zolpidem compared to phenobarbital combined with promethazine as premedication].

The following double-blind, randomised study dealt with three questions: (1) Is a multidimensional psychometric rating scale suitable for the measurement of mood before anaesthesia? (2) What are the effects of the new benzodiazepine-like drug zolpidem on preoperative mood compared with phenobarbital? (3) Is the combination with Promethazine suggestive? METHODS. Three hundred and four patients were assigned to four groups (group 1: zolpidem 8.03 mg/promethazine 50 mg; group 2: zolpidem 8.03 mg/placebo; group 3: phenobarbital 100 mg/promethazine 50 mg; group 4: phenobarbital 100 mg/placebo). The drugs were given the evening before anaesthesia (09:30-10:00 p.m.). The sample was shifted by age and sex. Mood was measured by a multidimensional rating scale, which assessed aspects of elated mood, anxiety, hostility, deactivation, vigilance, and introversion. Statistics were performed using analysis of variance (ANOVA). RESULTS. Zolpidem led to significantly higher expressions of hostility (negative mood, irritability, aggressiveness) than phenobarbital. Compared with placebo, promethazine led to greater deactivation (more tiredness and numbness, lower level of wakefulness). Specific emotions and somatic aspects were not affected. Patients who had received promethazine received a lower dose of thiopentone for induction of anaesthesia than patients with placebo. CONCLUSIONS. Zolpidem and phenobarbital have many common effects on preoperative mood. Differences were found in the unspecific emotional aspects of agitation and hostility. These negative effects must be weighed against the pharmacokinetic and pharmacodynamic advantages of zolpidem when this drug is administered for premedication. The effects of zolpidem seem to be more sedative than anxiolytic. The study shows that a combination with promethazine is suggestive, because promethazine has a selective deactivating effect. The finding that promethazine lowers the dose of thiopentone required for induction of anaesthesia is an additional interesting point. The results of this study highlight the importance of using multidimensional rating scales for the measurement of mood before anaesthesia.

Adolescent↗