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PubMed1989

Promethazine inhibits the formation of aldehydic products of lipid peroxidation but not covalent binding resulting from the exposure of rat liver fractions to CCl4.

Promethazine is known to have protective activity in relation to CCl4-induced liver necrosis. This hepatoprotective property has been investigated with regard to the free radical scavenging and antioxidant properties of promethazine using isolated hepatocytes and microsomal suspensions. CCl4 is activated in both systems to free radical metabolites that bind covalently to lipid and protein, and initiate lipid peroxidation. A large number of carbonyl products is produced during CCl4-induced lipid peroxidation; promethazine strongly inhibits the production of all classes of carbonyl compounds in both microsomal suspensions and isolated hepatocytes. In contrast, promethazine is a very weak inhibitor of the covalent binding of metabolites of CCl4. We conclude that promethazine acts by scavenging the trichloromethylperoxyl radical and lipid peroxyl radicals, and is a weak scavenger of the trichloromethyl radical. These data, when considered together with the hepatoprotective effects of promethazine, suggest that lipid peroxidation is of relatively more importance than covalent binding in the pathogenesis of CCl4-induced liver necrosis.

Aldehydes↗
PubMed1999

A double-blind, placebo-controlled investigation of the effects of fexofenadine, loratadine and promethazine on cognitive and psychomotor function.

AIMS: To assess whether fexofenadine in a range of doses from 80 to 180 mg has any disruptive effects on aspects of psychomotor and cognitive function in comparison with placebo, loratadine and promethazine, an antihistamine known to produce psychomotor and cognitive impairment. METHODS: Twenty-four healthy volunteers received fexofenadine 80 mg, 120 mg and 180 mg, loratadine 10 mg, promethazine 30 mg (as a positive internal control) and placebo in a six-way crossover, double-blind study. Following each dose, subjects were required to perform a series of tests of cognitive function and psychomotor performance at 1.5, 3, 6, 9, 12 and 24 h post dose. The test battery included critical flicker fusion (CFF), choice reaction time (CRT) and assessment of subjective sedation (LARS). Overall levels of activity were monitored by means of wrist mounted actigraphs throughout each of the 24 h experimental periods. RESULTS: Fexofenadine at all doses tested was not statistically different from placebo in any of the tests used and loratadine did not cause any significant impairment of cognitive function. Significant impairments were found following promethazine. Promethazine caused a significant reduction in CFF threshold and this effect was evident up to 12 h post dose (P<0.05). There was a significant increase in recognition reaction time at 3 and 6 h post promethazine administration, and the drug caused a significant (P<0. 002) increase in the percentage of 'sleep-like' activity from actigraph records during the daytime. CONCLUSIONS: Fexofenadine at doses up to 180 mg appears free from disruptive effects on aspects of psychomotor and cognitive function in a study where the psychometric assessments have been shown to be sensitive to impairment, as evidenced by the effects of the verum control promethazine 30 mg.

Adult↗
PubMed1997

[Optimizing anesthesiologic premedication with reference to biopsychological theories. Exemplified by the effect of dipotassium clorazepate and zolpidem in combination with promethazine].

UNLABELLED: The following double-blind randomized placebo-controlled study dealt with three questions: 1. Are differentiated psychometric test systems suitable measuring emotions before anaesthesia? 2. What are the effects of different doses of zolpidem (8.03 mg vs. 16.06 mg) compared with dipotassiumclorazepat (10 mg vs. 20 mg) on emotions in premedication? 3. Is the combination with Promethazin suggestive? METHOD: 320 patients were randomly assigned to different regimes of preanaesthetic medication. As primary premedication they received either zolpidem 8.03 mg or zolpidem 16.06 mg or dipotassium clorazepate 10 mg or dipotassium clorazepate 20 mg or placebo. The secondary premedication was either promethazine 50 mg or placebo. The tablets/dragees were given in the evening before surgery (09.00 p.m.-10.00 p.m.). Every cell of the 5 x 2-factorial design contained 16 men and 16 women. Emotions were measured by a multidimensional rating scale, comprising the aspects elated mood, anxiety, hostility, deactivation, vigilance and introversion. In addition, somatic symptoms and the quality of sleep were measured. Statistics were performed using multivariate analysis of variance. RESULTS: No differing effects of zolpidem and dipotassium clorazepate on preoperative mood were found. There was also no difference compared with placebo. Compared with placebo, promethazin leads to greater deactivation. Specific emotions were not affected. In somatic aspects there was a greater amount of cholinergic effects under promethazine, which was mainly expressed by a higher intensity of a dry mouth and weakness in general. Compared with placebo all of the tested drugs led to a better quality of sleep. CONCLUSIONS: Using multidimensional rating scales and considering emotions as a multifactorial construct, the study shows no different effects of benzodiazepines or benzodiazepin-like drugs on preoperative mood. No differences were also found on comparing these drugs with placebo. However, a better quality of sleep was seen under zolpidem and dipotassium clorazepate compared with placebo. The study shows that a combination with promethazine is recommended, because promethazine has a selective deactivating effect. The study stresses the significance of multidimensional rating scales for the measurement of emotions before anaesthesia.

Adult↗
PubMed2004

The effect of promethazine on postoperative pain: a comparison of preoperative, postoperative, and placebo administration in patients following total abdominal hysterectomy.

BACKGROUND: Histamine receptors are involved in the development of inflammatory pain and hyperalgesia, and the use of antihistamines is advocated as an alternative for pain therapy and treatment of postoperative nausea and vomiting. We investigated the influence of timing of promethazine administration on postoperative pain outcomes. METHODS: Ninety female patients undergoing total abdominal hysterectomy were randomly divided into three groups. All individuals received infusions of promethazine and normal saline before anaesthesia induction, and postoperatively the Pre group received promethazine 0.1 mg kg(-1) before anaesthesia and saline postoperatively, and the Post group received saline before anaesthesia and promethazine 0.1 mg kg(-1) postoperatively, while the Control group received two equivalent volumes of saline. Patients were treated using patient-controlled intravenous analgesia (PCA). The primary endpoint was pain intensity and morphine consumption. The secondary endpoint was postoperative nausea and vomiting. RESULTS: Postoperative morphine usage was significantly lower in the Pre group (24.1 +/- 3.9 mg) relative to the Post (30.0 +/- 4.6 mg) and Control groups (32.1 +/- 4.8 mg) during the first 24 h postoperatively (P<0.05). The number and incidence of patients suffering from postoperative nausea in the first 24 h was six (21%), seven (23%), and 15 (47%) in the Pre, Post, and Control groups, respectively (P<0.05). The number and incidence of patients vomiting in the first 24 h was three (10%), two (7%), and 10 (32%) in the Pre, Post, and Control groups, respectively (P<0.05). The number of patients asking for rescue antiemetic in the first 24 h was one (3%), two (7%), and seven (22%) in the Pre, Post, and Control groups, respectively (P<0.05). CONCLUSIONS: Our results suggest that preoperative administration of promethazine 0.1 mg kg(-1) reduces postoperative morphine consumption compared with postoperative and placebo administration, and that use of promethazine reduces PONV and the number of patients asking for rescue antiemetic in the first 24 h after surgery when compared with placebo.

Adult↗
PubMed1985

Comparison of the antiemetics metoclopramide and promethazine in labour.

A double blind trial was conducted in 477 mothers in labour to compare the antiemetics metoclopramide 10 mg and promethazine 25 mg and placebo when added to the first dose of pethidine. Metoclopramide and promethazine were equally effective, and both better than placebo, in reducing the incidence of nausea and vomiting after the administration of pethidine. Seventy seven per cent of mothers were drowsy, and 8% slept in the hour after the pethidine injection, with no difference between the groups. The sedative effect was more persistent in the promethazine group, 66% of whom were still drowsy after delivery. One third of the mothers in each group needed further analgesia, with 77% of these ultimately requesting an epidural. The reduction in pain half an hour and one hour after pethidine, assessed by a visual analogue scale, were, respectively, 22% and 22% for placebo; 26% and 23% for metoclopramide; 13% and 9% for promethazine. Analgesia after metoclopramide was significantly better than that after promethazine in terms of pain score, duration of first injection, and need for Entonox. Metoclopramide is therefore to be preferred to promethazine as an antiemetic in labour.

Clinical Trials as Topic↗
PubMed1978

Effect of promethazine on human polymorphonuclear chemiluminescence.

The effect of promethazine on the metabolic responsiveness of human polymorphonuclear leukocytes to opsonized zymosan was evaluated by chemiluminescence (CL) assay under the following situations: (1) preincubation of granulocytes with promethazine; (2) simultaneous addition of zymosan and promethazine, and (3) addition of promethazine after initiation of phagocytosis and CL. The presence of promethazine inhibited light emission in all cases. The data suggest that promethazine interferes with the generation and/or subsequent activity of those reactive forms of oxygen which contribute to CL.

Granulocytes↗
PubMedDate not supplied

Effects of promethazine on the energy metabolism of normoxic and hypoxic rat brain.

The metabolic effects of intraperitoneal administration of promethazine on normoxic, hypoxemic and hypoxemic-oligemic rat brain were assessed by measurement of the cerebral contents of energy phosphates, and selected glycolytic-citric acid cycle intermediates. In normoxic brain promethazine (25-100 mg/kg-1) was associated with unaltered adenylates, increased glucose and aspartate and decreased pyruvate, lactate and malate; a pattern which was compatible with cerebral metabolic depression. Hypoxemic animals receiving either saline or promethazine (25 mg/kg-1) showed equivalent decreases in ATP and increases in lactate which indicated that promethazine had no significant effect on the metabolism of the acutely hypoxic brain. In animals exposed to hypoxemia plus right carotid artery occlusion (oligemia) the promethazine treated group (25 mg/kg-1) showed significantly lower ATP and higher AMP contents which suggested an adverse effect on the metabolism of the acutely hypoxic-oligemic brain. It is concluded that promethazine does not beneficially alter the energy metabolism of the acutely hypoxic or hypoxic-oligemic brain.

Adenine Nucleotides↗
PubMedDate not supplied

Efficacy of promethazine suppositories dispensed to outpatient surgical patients.

Postoperative nausea and vomiting frequently complicate outpatient anesthesia and surgery. The duration of treatment for this complication must occasionally extend beyond discharge from the hospital. In this study, we evaluated the commonly used anti-emetic promethazine for its efficacy in the post-discharge period. Adult outpatient surgical patients who had excessive postoperative nausea and vomiting in the recovery room, or who were at risk for postoperative nausea and vomiting following discharge were given two promethazine suppositories (25 mg) for home use. All patients were contacted by our recovery room nurses on the first business day after their surgery and questioned as to their use of the suppositories and, if used, their efficacy. We found that 55 percent of patients given promethazine suppositories for home use had nausea and vomiting in the post-discharge period. Of the patients given promethazine, 89 percent used the suppositories. All of these patients reported improvement in their symptoms following use of the suppositories. None reported adverse effects from the promethazine suppositories. In conclusion, we found promethazine suppositories to be an inexpensive and efficacious treatment for nausea and vomiting in adult outpatient surgical patients following discharge from the hospital. Side-effects were minimal, and our patients voiced no complaints about this mode of therapy. We recommend this therapy for treatment of nausea and vomiting after hospital discharge following adult outpatient surgery.

Aged↗
PubMed2000

Promethazine as a motion sickness treatment: impact on human performance and mood states.

PURPOSE: Intramuscular (i.m.) injections of promethazine in 25 mg or 50 mg dosages are commonly used to treat space motion sickness in astronauts. The present study examined the effects of i.m. injections of promethazine on performance, mood states, and motion sickness in humans. METHODS: Subjects were 12 men, mean age 36 + 3.1, who participated in 1 training day and 3 treatment conditions: a 25-mg injection of promethazine, a 50-mg injection of promethazine, and a placebo injection of sterile saline. Each condition, scheduled at 7-d intervals, required an 8-10-h day in which subjects were tested on 12 performance tasks, and were given a rotating chair motion sickness test. On the training day subjects were trained on each task to establish stability and proficiency. Treatment conditions were counterbalanced and a double-blind procedure was used to administer the medication or placebo. RESULTS: Statistically significant decrements in performance were observed for both dosages of promethazine as compared with the placebo. Performance decrements were associated with mean blood alcohol dose equivalency levels of 0.085% for 25 mg and 0.137% for 50 mg doses. Mood scale results showed significant changes in individual subjective experiences with maximum deterioration in the arousal state and fatigue level. Only the 25-mg dosage significantly increased motion sickness tolerance when compared with the placebo. CONCLUSIONS: These data suggest that effective doses of promethazine currently used to counteract motion sickness in astronauts may significantly impair task components of their operational performance.

Adult↗
PubMed1990

Should promethazine in liquid form be available without prescription?

Promethazine, available by prescription only since its introduction in 1946, has been widely used for pediatric patients because of its antihistaminic, antiemetic, and sedative properties. Recently, it's makers have sought Federal Drug Administration approval to introduce two liquid over the counter allergy/cold/cough products containing promethazine as an active ingredient. Although millions of doses have been administered, promethazine use has not been free of risk. Promethazine has been reported to cause significant sedation, agitation, hallucinations, seizures, dystonic reactions, and possibly apparent life-threatening events or sudden infant death syndrome. The impact of these relatively uncommon adverse reactions on children would be minimal if parents would use over the counter promethazine only for appropriate indications and only in children greater than 2 years of age. However, according to results of research evaluating the use of various over the counter medications by families for their children, promethazine will be used inappropriately. Both its over the counter status, implying a certain margin of safety, and its formulation as a syrup, providing ease of administration, should increase its use in all age groups including that by children less than 2 years of age who may be most vulnerable to the adverse reactions associated with the drug's use.

Chemistry, Pharmaceutical↗
PubMed1984

Liquid chromatographic analysis of promethazine and its major metabolites in human postmortem material.

A method is described for the determination of promethazine and some of its major metabolites in postmortem specimens by enzymic digestion followed by high-pressure liquid chromatography of the extracts using a cyano-bonded (mu-Bondapak-CN) silica column packing and a mobile phase consisting of methanol, water, and n-octylamine (adjusted to pH 8). The system will separate and quantitate promethazine sulphoxide, desmonomethyl promethazine, didesmethyl promethazine, and promethazine. Pericyazine (2-cyano-10-[3-(4- hydroxypiperidino )propyl] phenothiazine) was used as internal standard. The parent drug and metabolites were extracted from a enzyme digested tissue homogenates with ethyl acetate using a simple, single micro-extraction procedure. The method was applied to four cases of fatal poisoning involving promethazine ingestion.

Adult↗
PubMed1993

Treatment efficacy of intramuscular promethazine for space motion sickness.

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.

Female↗
PubMed1975

Prevention of peritoneal adhesions in the rat. The effects of dexamethasone, methylprednisolone, promethazine, and human fibrinolysin.

Peritoneal adhesions were created in rats by brisk scrubbing of the terminal part of the ileum. Adhesions were graded by total number and the presence of small bowel obstruction. Adhesion prophylaxis was evaluated using dexamethasone, methylprednisolone sodium succinate, promethazine hydrochloride, and human fibrinolysin (Thrombolysin) in various combinations, doses, and routes of administration. Methylprednisolone and dexamethasone, depending on the route of administration, modified the total number of adhesions but did not modify their severity when compared to control animals. Promethazine by itself modified peritoneal adhesions in the rat. Used together, methylprednisolone and promethazine also modified adhesions, but were not substantially better than the combination of dexamethasone and promethazine. Methylprednisolone, promethazine, and human fibrinolyzin, when used in combination intraperitoneally, virtually eliminated adhesion formation.

Animals↗
PubMedDate not supplied

Rotary pursuit, a measure of human performance, and plasma concentrations of promethazine.

Promethazine in doses of 50 mg has demonstrated detrimental effects upon the performance of visual tasks. The purpose of the study was to examine the relationship between the blood concentration levels of promethazine and two human performance tasks. Fifteen paid healthy male volunteers completed a randomized five-way crossover design which included a 25 mg and 50 mg dose of the innovator dosage form, a 50 mg dose of a generic dosage form, a 50 mg solution dosage form, and a placebo. Serial blood samples were obtained in addition to performance measures of rotary pursuit and a simple force choice reaction time. Analysis of the forced choice reaction depicted a mild relationship with the blood concentration levels of promethazine. However, the measures of rotary pursuit, a more sensitive determinant of human motor performance, proved to be more related to both the promethazine blood concentration and the inherent learning which was confounded in the experiment. The degree of impaired pursuit performance and reaction time differences could be defined in terms of a linear relationship to the promethazine concentration.

Humans↗
PubMed1982

High-pressure liquid chromatographic determination of promethazine plasma levels in the dog after oral, intramuscular, and intravenous dosage.

Plasma levels of promethazine were determined using a high-pressure liquid chromatographic procedure incorporating a fixed wavelength (254 nm) UV detector, following single 50-mg intravenous, intramuscular, and oral doses to two male dogs. Initial plasma promethazine concentrations following intravenous doses were 556 and 535 ng/ml in the two dogs. The subsequent decline in drug levels were satisfactorily described by a triexponential function. Peak promethazine levels of 76 and 64 ng/ml were obtained 0.5 hr following intramuscular doses. Peak levels for the oral doses were 10.6 and 11.0 ng/ml occurring 2 hr after dosing. The apparent biological half-life of promethazine, obtained from only 2-3 data points, varied from 8.5 to 27.7 hr. Areas under the promethazine plasma curves, compared to values obtained from intravenous doses between 0 and 24 hr, indicated that systemic availability of intact drug was 55-73% following intramuscular injection and 8.3-9.5% following oral administration.

Administration, Oral↗
PubMed1983

Thermal and photolytic degradation studies of promethazine hydrochloride: a stability-indicating assay.

A stability-indicating GLC method for the analysis of promethazine hydrochloride in polyethylene glycol delivery systems is reported. This method is capable of distinguishing the intact drug from its thermal and photodegradation products. A linear relationship between peak height ratio (promethazine-promazine) and promethazine concentration is found up to a concentration of 600 micrograms/ml. Kinetic studies were performed to determine the photolytic and thermal degradation rates of promethazine hydrochloride as a function of pH. The activation energies at pH 2.98, 3.94, and 5.12 were obtained from linear Arrhenius plots and were found to be 6601, 5888, 5570 cal/mole, respectively. The first-order rate constant increased with increasing pH. The photolytic degradation of promethazine hydrochloride does not follow simple first-order kinetics.

Chromatography, Gas↗
PubMed1987

Bioequivalence and pharmacokinetic profile of promethazine hydrochloride suppositories in humans.

A bioequivalence study of promethazine hydrochloride (10-[2-(dimethylamino)propyl]-phenothiazine monohydrochloride) was conducted in 20 male human subjects with the purpose of comparing, under blind condition, the human serum levels of promethazine in three different formulations. The formulations tested were a 50-mg promethazine hydrochloride polyethylene glycol suppository, a 50-mg promethazine hydrochloride cocoa butter-white wax suppository, and a 50-mg oral dose of promethazine hydrochloride syrup. Each subject received single doses of each of the three formulations on each of three different days on a crossover basis. From the measured serum levels, estimates of the bioavailability parameters (area under the serum concentration versus time curve, time-to-peak serum concentration, and peak serum concentration) were obtained by least-squares digital computer fitting. Also, a one-compartment pharmacokinetic open model with two consecutive first-order input steps is proposed. Statistical analysis of the results was performed by using a linear multiple regression approach for the analysis of variance. No significant differences between the syrup and the polyethylene glycol suppositories were obtained (p greater than 0.05) for the above three bioavailability parameters. However, the polyethylene glycol suppositories provided statistically higher peak serum concentration, shorter time-to-peak serum concentration, and larger area under the serum concentration versus time curve than the cocoa butter-white wax suppositories.

Adult↗
PubMed2000

Promethazine oxidation by redox mediation in peroxidase reactions.

The effect of promethazine on peroxidase-catalyzed oxidation of 3,3', 5,5'-tetramethylbenzidine was investigated at pH 5.4. Promethazine dose dependently introduced a lag in the appearance of tetramethylbenzidine charge-transfer complex monitored at 652 nm. Increasing concentrations of tetramethylbenzidine however decreased the lag period proportional to the tetramethylbenzidine concentration. Addition of promethazine to preformed charge transfer complex caused rapid bleaching of the blue-colored complex. Titration of promethazine with the yellow-colored diimine gave rise to the blue charge-transfer complex and the complete reduction of the species to the colorless parent amine compound. The available evidence suggests that promethazine is oxidized via redox mediation by tetramethylbenzidine peroxidase-oxidized products.

Benzidines↗