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PubMedDate not supplied

Bioequivalency and dose proportionality of three tableted promethazine products.

Data from a five-way crossover study in human subjects using four talented promethazine products and a promethazine solution are presented. All products were administered as a single oral dose. The five objectives of the study were to investigate bioequivalency, to estimate dose proportionality at two dose levels, to establish validity of a reference production solution for future bioequivalency studies, to estimate intersubject variation, and to compare bioavailability/tablet dissolution data. Blood samples were collected at given intervals over a 24-hour period and analysed for promethazine using an HPLC technique. Pharmacokinetic parameters were calculated using standard procedures and a two-way analysis of variance (ANOVAR) was used to assess whether the differences were statistically significant. The AUC0----infinity data from the ANOVAR analysis showed that the 50 mg innovator and generic products and the 50 mg solution were not significantly different. However, the innovator product had a significantly lower Cmax and longer tmax than the solution. The generic product did not differ significantly from the solution. Promethazine was found to exhibit linear dose proportionality in the range and product studied. Intersubject variation was high for all parameters (23 to 63 per cent) and the in vivo and in vitro data showed a positive relationship.

Adolescent↗
PubMed1994

Use of promethazine to hasten adaptation to provocative motion.

In an earlier study, the authors found that severely motion sick individuals could be greatly relieved of their symptoms by intramuscular injections of promethazine (50 mg) or scopolamine (.5 mg). Comparable 50-mg injections of promethazine also have been found effective in alleviating symptoms of space motion sickness. The concern has risen, however, that such drugs may delay or retard the acquisition of adaptation to stressful environments. In the current study, we controlled arousal using a mental arithmetic task and precisely equated the exposure history (number of head movements during rotation) of a placebo, control group and an experimental group who had received promethazine. No differences in total adaptation or in rates of adaptation were present between the two groups. Another experimental group also received promethazine and was allowed to make as many head movements as they could, before reaching nausea, up to 800. This group showed a greater level of adaptation than the placebo group. These results suggest a strategy for dealing with space motion sickness that is described.

Adaptation, Physiological↗
PubMedDate not supplied

Reduction of erythema in hairless guinea pigs after cutaneous sulfur mustard vapor exposure by pretreatment with niacinamide, promethazine and indomethacin.

Erythema is the initial symptom that occurs after sulfur mustard (HD) cutaneous exposure. The time course of HD-induced erythema is similar to that observed after UV irradiation, which can be reduced by indomethacin. Sulfur mustard lethality is decreased by using promethazine, which is an antihistamine. Niacinamide can reduce microvesication after HD vapor exposure in hairless guinea pig (HGP) skin. The present study examines the effect of the combined administration of niacinamide, indomethacin and promethazine used alone or in all possible combinations on the degree of erythema and histopathologic skin damage after HD exposure in HGP. Niacinamide (750 mg kg-1, i.p.), promethazine (12.5 mg kg-1, i.m.) or indomethacin (4 mg kg-1, p.o.) used singly or in combination was given as a 30-min pretreatment before an 8-min HD vapor cup skin exposure. Using a combination pretreatment of niacinamide, promethazine and indomethacin, erythema was reduced at 4 (91%) and 6 (55%) h, but not 24 h after HD. The incidence of histopathological skin changes (microvesicles, follicular involvement, epidermal necrosis, intracellular edema and pustular epidermatitis) 24 h after HD was not reduced. This study indicates that HD-induced erythema may result from several different mechanisms, including inflammation, histamine release and DNA damage. It is suggested that two phases of inflammation may occur: an early phase sensitive to antihistamines and non-steroidal antiinflammatory drugs and a late phase of extensive cell damage that was not sensitive to these drug pretreatments.

Animals↗
PubMed1985

Promethazine both facilitates and inhibits nociception in rats: effect of the testing procedure.

The present study demonstrates that low doses of promethazine (1.25-5 mg/kg SC) dose-dependently facilitate nociception in the vocalization test in rats. However, this effect disappeared gradually with increasing dose, and in contrast, high doses (20-40 mg/kg SC) induced an antinociceptive effect. This indicates that promethazine, depending upon the biophase concentration, has the potential to interact with separate antagonizing or opposing functional systems, producing contrasting effects on nociception. The sigmoid Emax model was fitted to the observed composite effect, and dose-response characteristics for two opposite effects were described. In addition, when suprathreshold stimulation was used to evoke nociception, the stimulus amplified the hyperalgesic efficacy of promethazine but left the potency of this effect unaltered. In this experimental situation only negligible antinociception was observed. Our data thus show that for promethazine, the net effect on nociception in rats is not absolute but is balanced both by the biophase concentration and by the effectiveness of the stimulation used to evoke nociception.

Animals↗
PubMed1990

Synergistic effect of promethazine with gentamycin in frequently recurring pyelonephritis.

The effects of promethazine were studied in children with frequently recurring pyelonephritis which was not associated with urological abnormalities. The results of three methods of treatment were compared: 10 children were given a combination of gentamycin and promethazine for 7 days (Group 1), 11 received gentamycin treatment alone for 10 days (Group 2), and 19 (Group 3) were on long-term oral antibiotic prophylaxis (5.6 +/- 2.1 years) with episodes of intensive treatment of recurrences. In a 3-year follow-up period, the number of pyelonephritis recurrences was significantly lower in Group 1 than in Groups 2 and 3. Six out of 19 children in Group 3 had renal scarring. The authors suggest a synergistic effect between gentamycin and promethazine therapy. Promethazine increases antibiotic sensitivity, which could contribute to the elimination of recurring urinary tract infections.

Adolescent↗
PubMed1999

Post discharge nausea and vomiting after ambulatory laparoscopy is not reduced by promethazine prophylaxis.

PURPOSE: To determine the incidence of post-discharge nausea and vomiting (PDNV) following outpatient laparoscopic procedures in women, and to assess the efficacy of the prophylactic administration of promethazine prior to discharge from hospital. METHODS: Ninety-five healthy women scheduled for ambulatory laparoscopic cholecystectomy or gynecological surgery completed this double blind, placebo controlled study. A standardized fentanyl-propofol-nitrous oxide-isoflurane anesthetic was used, and all patients received 0.5 mg droperidol i.v., intraoperatively. Subjects were randomized to receive 0.6 mg x kg(-1) promethazine or placebo i.m. prior to transfer from the post-anesthetic recovery (PAR) unit. The incidence and severity of nausea, pain, and drowsiness were documented using patient diaries at four time intervals during the first 24 hr postoperatively using four-point self-assessment scales. RESULTS: After discharge home, the overall incidence of nausea was 48%, moderate to severe nausea 30%, vomiting 17% and rescue antiemetic use 28%, with no difference between those receiving saline or promethazine. The need for antiemetics in the PAR was associated with subsequent PDNV, with those requiring PAR antiemetics being four times as likely to vomit after discharge (P = 0.008). CONCLUSION: Despite the prophylactic administration of 0.5 mg droperidol i.v., patients undergoing ambulatory laparoscopic surgery reported a high incidence of nausea after discharge. Patients requiring antiemetics in the PAR were at higher risk for PDNV. The incidence of nausea was not altered by prophylactic administration of 0.6 mg x kg(-1) promethazine i.m. before discharge.

Adult↗
PubMed1996

Blocking effects of promethazine, triprolidine and their analogues on the excitation caused by the peptide, achatin-I.

An Achatina endogenous tetrapeptide, achatin-I (Gly-D-Phe-Ala-Asp), applied by brief pressure, produced an inward current (Iin) on an Achatina giant neurone type, PON (periodically oscillating neurone). Promethazine, triprolidine and their analogues tested, applied by perfusion, showed a tendency to inhibit the Iin, suggesting that the effective structures vary to a wide extent. With respect to promethazine and its analogues, the presence of 2-bromo, 5-oxo, 3-dimethylsulfamido and 2-methoxy weakened the effects. 10-(2-methylamino-2-methylethyl) instead of 10-(2-dimethylamino-2-methylethyl) of promethazine and the azepine ring instead of phenothiazine ring potentiated the effects. From the dose (pressure duration)-response study of achatin-I, the two promethazine analogues, RP 6497 and RP 6549 (the structures are shown in Fig. 1), inhibited the Iin in partly competitive and partly noncompetitive manners. Regarding triprolidine and its analogues, the compounds in Z-configuration seemed to be more effective than those in E-configuration. The presence of 4-methyl in 1-phenyl, and 1-(4-pyridyl) instead of 1-(2-pyridyl) potentiated the effects. 3-Dimethylamino instead of 3-pyrrolidino weakened the effects. The two triprolidine analogues, Trip Der 3 and Trip Der 6 (the structures in Fig. 2), inhibited the Iin in an uncompetitive manner.

Animals↗
PubMed1999

Effects of promethazine on porcine gastroduodenal function: a sonographic study.

This sonographic study was aimed at examining the effect of sedation with promethazine (1.5 mg x kg(-1)), on gastroduodenal function in neonatal piglets. On 3 consecutive days, observations of gastroduodenal motility during the first 3 postprandial h were made in 13 animals (3 to 5 days old; 7 sleeping naturally and 6 sedated 2 h prior to feeding). Promethazine significantly reduced both the closures per min of the terminal part of the pyloric antrum and pyloric canal and the percentage of gastric contractions that were followed by closure of the terminal pyloric antrum and canal. Such actions of promethazine on motility of the gastroduodenal junction could lead to a delay in gastric emptying of ingesta with a consequent increased risk of reflux of gastric contents into the esophagus. Because gastroesophageal reflux has been associated with the pathogenesis of sudden infant death syndrome (SIDS), care should be taken if promethazine is to be used as a sedative in neonates.

Animals↗
PubMed2001

Quantitation of promethazine and metabolites in urine samples using on-line solid-phase extraction and column-switching.

A chromatographic method for the quantitation of promethazine (PMZ) and its three metabolites in urine employing on-line solid-phase extraction and column-switching has been developed. The column-switching system described here uses an extraction column for the purification of PMZ and its metabolites from a urine matrix. The extraneous matrix interference was removed by flushing the extraction column with a gradient elution. The analytes of interest were then eluted onto an analytical column for further chromatographic separation using a mobile phase of greater solvent strength. This method is specific and sensitive with a range of 3.75-1400 ng/ml for PMZ and 2.5-1400 ng/ml for the metabolites promethazine sulfoxide, monodesmethyl promethazine sulfoxide and monodesmethyl promethazine. The lower limits of quantitation (LLOQ) were 3.75 ng/ml with less than 6.2% C.V. for PMZ and 2.50 ng/ml with less than 11.5% C.V. for metabolites based on a signal-to-noise ratio of 10:1 or greater. The accuracy and precision were within +/- 11.8% in bias and not greater than 5.5% C.V. in intra- and inter-assay precision for PMZ and metabolites. Method robustness was investigated using a Plackett-Burman experimental design. The applicability of the analytical method for pharmacokinetic studies in humans is illustrated.

Humans↗
PubMed2003

The effects of acute doses of fexofenadine, promethazine, and placebo on cognitive and psychomotor function in healthy Japanese volunteers.

BACKGROUND: Genetic variations in cross-cultural metabolic capability may attenuate the lack of central nervous system effects of fexofenadine. OBJECTIVE: To compare the pharmacodynamics of fexofenadine and promethazine versus placebo in Japanese volunteers. METHODS: In this randomized, crossover, double-blind study, 24 subjects received single doses of fexofenadine 60 mg and 120 mg, promethazine 25 mg, and placebo, with a 6-day washout period between treatments. Objective measures included critical flicker fusion, choice reaction time, and a compensatory tracking task. A line analog rating scale evaluated self-rated sedation. A rapid visual information-processing task evaluated vigilance at baseline and at 2 hours. RESULTS: Fexofenadine was not significantly different from placebo on any test at any timepoint. In contrast, promethazine impaired critical flicker fusion thresholds (F[3,63] = 5.37, P = 0.0023); increased recognition reaction time (F[3,63] = 13.63, P < 0.0001) and total reaction time (F[3,63] = 12.23, P < 0.0001) components of the choice reaction time test; reduced tracking accuracy (F[3,63] = 14.25, P < 0.0001) and increased reaction times to peripheral stimuli (F[3,63] = 9.29, P < 0.0001) in the compensatory tracking task; reduced the number of valid responses (F[3,63] = 14.86, P < 0.0001) and impaired reaction times (F[3,63] = 12.02, P < 0.0001) in the rapid visual information-processing task test; and impaired subjective ratings of sedation (F[3,63] = 7.55, P = 0.0002), compared with placebo. CONCLUSIONS: A battery of tests sensitive to impairment by promethazine failed to show any negative cognitive or psychomotor effects with fexofenadine 60 and 120 mg. Fexofenadine is an intrinsically non-impairing antihistamine in Japanese subjects.

Adult↗
PubMed1969

The effects of carbon tetrachloride on rat liver microsomes during the first hour of poisoning in vivo, and the modifying actions of promethazine.

The effects of an oral administration of carbon tetrachloride on various liver microsomal and supernatant components were studied 1hr. and 2hr. after dosing. The modifications of such early changes resulting from a concomitant administration of promethazine together with the carbon tetrachloride were also investigated. The microsomal components studied were: cytochromes P-450 and b(5); inorganic pyrophosphatase; NADH- and NADPH-cytochrome c reductases; NADH- and NADPH-neotetrazolium reductases; a lipid-peroxidation system associated with the oxidation of NADPH and stimulated by ADP and Fe(2+). NAD- and NADP- DT-diaphorases were measured in the supernatant solution remaining after isolation of liver microsomes, and the distribution of RNA phosphorus between the microsomes and supernatant solution was also determined. Carbon tetrachloride produced a rapid fall in inorganic pyrophosphatase activity, a rather slower decrease in cytochrome P-450 content of the microsomes and small increases in the activities of NADH-cytochrome c reductase and neotetrazolium reductases. The activities of NADPH-cytochrome c reductase, the NADPH-ADP/Fe(2+)-linked lipid-peroxidation system, DT-diaphorases and the content of cytochrome b(5) in the microsomes were unchanged. There was also a loss of RNA phosphorus from the microsomes into the supernatant solution. The RNA phosphorus redistribution, the decrease in inorganic pyrophosphatase and the increases in neotetrazolium reductase activities were at least partially prevented by a concomitant dosing with promethazine. However, the decrease in cytochrome P-450 was not affected by promethazine treatment. These early changes are discussed in terms of the liver necrosis produced by carbon tetrachloride and which is greatly retarded in its onset by the administration of promethazine.

Animals↗
PubMed1986

The hypnotic effects of an antihistamine: promethazine.

Twelve volunteer poor sleepers of mean age 59 years took placebo on one night, promethazine 20 mg on one night and promethazine 40 mg on one night, in a double-blind balanced order study. Sleep in the EEG laboratory was increased by nearly 1 h after either dose of promethazine, and sleep interruptions were reduced. Slow-wave sleep was unaffected, but the larger dose reduced the percentage of sleep spent as REM sleep. Sleep was improved subjectively by both doses of promethazine which appears to be an effective hypnotic.

Aged↗
PubMed1988

Effects of promethazine on ischemic and reperfusion arrhythmias in rat heart.

The effects of the H1-receptor antagonists promethazine, mepyramine, and chlorpheniramine on ischemic and reperfusion arrhythmias were studied in the isolated perfused rat heart. Promethazine reduced both ischemic and reperfusion arrhythmias (2 x 10(-6)M-7.5 x 10(-6)M). Mepyramine and chlorpheniramine decreased these arrhythmias but at concentrations about 10 times higher. The H2-blockers cimetidine and ranitidine had no antiarrhythmic effect. Promethazine also: (i) increased release of noradrenaline by the heart; and (ii) increased coronary flow in the reperfusion period and in some mildly ischemic zones. It is proposed that promethazine exerts most of its antiarrhythmic effects by a nonspecific mechanism, possibly membrane stabilization; in addition, enhanced coronary flow may play a role.

Animals↗
PubMed1999

Tardive dyskinesia: probing abnormal metabolism with promethazine.

Ten in-patients with tardive dyskinesia (TD) (mean AIMS score 16.7) and 8 controls were recruited to the study, and 3 h after oral administration of promethazine a blood sample was taken for assay of levels of promethazine and its immediate metabolites by high-performance liquid chromatography (HPLC). The TD group had a variety of indicators of impaired or slow metabolism compared to the controls. There was a significant difference in the ratio of promethazine to promethazine sulphoxide (P < 0.05) between patients with TD and the control group. The TD group but not the controls showed increasing metabolic impairment with age. This small study confirms the previous reports of impaired neuroleptic metabolism in TD, particularly in the elderly.

Adult↗
PubMed1977

A sex difference in the interaction between promethazine and morphine in the mouse.

The effects of promethazine on the antinociceptive and respiratory actions of morphine have been examined in the mouse. Moderate doses of promethazine (5 and 10 mg kg-1) potentiated morphine's action in male mice but inhibited it in female mice. Gonadectomy abolished the interaction between promethazine and morphine in both sexes, although the intensity and duration of morphine's activity was greatly enhanced in these mice. Replacement of oestradiol in ovariectomized mice restored morphine's activity to intact female control values. However, interactions between promethazine and morphine required progesterone, as well as oestradiol, replacement to obtain results approaching those obtained in intact female mice.

Animals↗
PubMed1981

Drug treatment of breathlessness: contrasting effects of diazepam and promethazine in pink puffers.

Fifteen out of 18 "pink and puffing" patients completed a double-blind, placebo-controlled cross-over trial of diazepam and promethazine for breathlessness and reduced exercise tolerance. Dosages were 25 mg and 125 mg daily, respectively, and each course lasted two weeks. Patients with psychiatric or other major medical histories were excluded. Of the three patients who did not complete the trial, one died during an exacerbation of breathlessness while taking diazepam, one was withdrawn because of mild hypercapnia while taking placebo, and one suffered intolerable drowsiness while taking diazepam. Of the remaining 15 patients, six needed a reduction in dosage because of drowsiness: one of these was taking promethazine and five diazepam. Diazepam had no effect on breathlessness and noticeably reduced exercise tolerance. Promethazine reduced breathlessness and improved exercise tolerance without altering lung function. From these results diazepam is contraindicated for breathlessness and reduced exercise tolerance in fixed airways obstruction, but promethazine may be beneficial.

Adult↗
PubMed2000

Zolpidem and promethazine in pre-anaesthetic medication. A pharmacopsychological approach.

This study dealt with the question: What are the effects of different doses of the benzodiazepine-like agent zolpidem and the phenothiazine derivative promethazine on mood in pre-anaesthetic medication? Subjects were 192 female and male patients awaiting elective surgery. Two drugs were administered to the patients in the evening before anaesthesia according to a 3 x 2 factorial randomized double-blind design. The first drug factor was zolpidem (8.03 vs. 16.06 mg) versus placebo. These drugs were combined with the second drug factor, either promethazine (50 mg) or placebo. In summary, the results confirm the hypothesis that zolpidem 8.03 mg can induce paradoxical effects, especially of anxiety, 1 h after application. When the dosage is doubled, no adverse effects are found, but there are no effects different from placebo either. Men could probably be described as a risk population for the adverse effects of zolpidem 8.03 mg. Furthermore, selective deactivating effects of promethazine 50 mg were shown in this study. In addition to these anaesthesiological aspects, this study showed promethazine to be useful as a research tool, suitable as a reference drug to detect deactivating effects. The multidimensional self-report inventory BSKE(EWL) (Befindlichkeitsskalierung durch Kategorien und Eigenschaftswörter) detected the expected drug effects, indicating that this instrument is suitable for further pharmacopsychological research.

Adult↗
PubMed1988

Effects of promethazine HCl on osteoporotic femora of adult castrated male rats.

Promethazine HCl (Phenergan) was added to the drinking water (2.4-9.6 mg/kg/day) of castrated adult male Holtzman rats. One group of castrates and a group of normal rats received no drug and served as controls. Treatment was started at castration and continued for 4 months. After controlling for body weight, analyses of covariance and Student-Newman-Keuls tests revealed that promethazine did not prevent the development of femoral osteoporosis in the castrate rats. However, control rats (normal and untreated castrates) had significantly wider femora and thicker cortices at midshaft than did promethazine-treated animals. The results indicated that promethazine HCl had no effect on the development of femoral osteoporosis and retarded normal femoral expansion in the adult castrate male rats.

Animals↗