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PubMed1978

Oxidative degradation pharmaceutically important phenothiazines II: Quantitative determination of promethazine and some degradation products.

Methods for the determination of promethazine and several degradation products, which can be used in kinetic studies, were developed. All determinations were carried out after isolation of the compounds by TLC. Promethazine was determined by oxidation with vanadyl sulfate in an acidic medium. The method was suitable for approximately 3 mg of the compound. 3H-Phenothiazine-3-one was determined spectrophotometrically at 492 nm in acetone. The compound could be determined in amounts of 30-40 microgram. Promethazine 5-oxide was determined spectrophotometrically using the acid dye method; 100-200 microgram could be determined. 7-Hydroxy-3H-phenothiazine-3-one could be determined spectrophotometrically at 600 nm after extraction of the other compounds from the solution. The medium had to be alkaline and contain water in a fixed ratio. The method was suitable for 15-30 microgram of the compound.

Chromatography, Thin Layer↗
PubMed1983

Spectrophotometric promethazine hydrochloride determination using bromcresol green.

A spectrophotometric method was developed for determining promethazine hydrochloride (I) complexed with bromcresol green and then extracted with chloroform. The complex in chloroform showed maximum absorption at 415 nm and obeyed Beer's law over 1.2-8.5 micrograms/ml. The complex molar absorptivity was 1.93 X 10(4) M. Complex formation and extraction were complete and quantitative over pH 2.7-2.8. The promethazine hydrochloride-bromcresol green molar ratio was 1:1. Excipients, coloring matter, flavoring agents, and other substances likely to be present in promethazine preparations did not interfere in the determination. Direct determination in tablet, syrup, and injection preparations were carried out satisfactorily.

Bromcresol Green↗
PubMed1987

Promethazine, scopolamine and cinnarizine: comparative time course of psychological performance effects.

Single oral doses of promethazine (12.5 mg, 25 mg), scopolamine (0.6 mg), and cinnarizine (30 mg), were compared in a double-blind, placebo controlled trial. Twelve normal volunteers undertook a battery of psychological performance tests and a feeling state questionnaire, before drug administration, and at 2-h intervals after. Promethazine and cinnarizine significantly impaired psychomotor performance, information processing and feelings of alertness. With promethazine these reductions were maximal 3-4 h post-drug, with performance returning near to baseline 8-9 h post-drug. With cinnarizine these impairments were maximal 5-6 h post-drug, and performance remained depressed 8-9 h post-drug. Scopolamine significantly reduced feelings of alertness, and memory task performance; the overall performance effects were most evident 1-4 h post-drug.

Adolescent↗
PubMed1977

Does promethazine (Atosil) influence the human's early acoustically evoked potentials in the same way as the late potential N1?

In a former investigation the effect of promethazine (Atosil) on the late acoustically evoked potential component N1 was examined. Now the cochlear and the brain-stem potentials were registered by the earlobe-vertex pick-up with i.m. application of 0.8 mg/kg (body weight) promethazine. There was no influence of promethazine either on the compound action potential (NAP) or on the brain-stem potentials (Pot. II-V), but sedation improves significantly the signal-to-noise ratio, therefore we sedate all patients when registering the five early acoustically evoked potentials.

Acoustic Stimulation↗
PubMed1985

Degradation products of the promethazine radical cation.

The degradation products of the promethazine radical cation, generated from promethazine with horseradish peroxidase/H2O2, have been investigated. Several products have been identified which resulted from fission of the bond between the two ethanamine carbon atoms of the N10 side chain. The main product (approx. 90%) was identified as 10-formyl-5-oxophenothiazine. The likely structure of three minor products was also elucidated. The degradation of the promethazine radical cation is different from that of radical cations derived from the propanamine side chain containing phenothiazine drugs.

Cations↗
PubMed1976

Effects of the H1-antagonist promethazine and the H2-antagonist burimamide on chronotropic, inotropic and coronary vascular responses to histamine in isolated perfused guinea-pig hearts.

On guinea-pig atria part of the inotropic response to histamine is attributable to a concomitant increase of the frequency [7]. Since the chronotropic effect of histamine is mediated by a stimulation of H2-receptors a direct interaction of histamine with H1-receptors a direct interaction of histamine with H1-receptors mediating the inotropic response on heart may be overlooked. For this reason the ability of the H1-antagonist promethazine and the H2-antagonist burimamide to inhibit the positive chronotropic, inotropic and coronary vascular responses to histamine was determined in spontaneously beating and electrically driven perfused guinea-pig hearts. (1) Burimamide produced a competitive blockade of the positive chrono- and inotropic responses to histamine. (2) On the other hand, promethazine in concentrations that had no effect on cardiac function by itself, proved to be ineffective against the positive chrono- and inotropic responses produced by histamine on spontaneously beating and electrically driven heart preparations. (3) The predominant coronary vasodilation observed after infusion with histamine was competitively antagonized by promethazine and burimamide. This blockade was not attributable to an interaction with myocardial H2-receptors mediating increases in heart rate and contractility and was, therefore, direct in nature. (4) Based upon the present study and former investigations [7] the following distribution of different histamine receptors in the guinea-pig heart does exist: H1-receptors are present in the atrial muscle and the coronary vascular bed. H2-receptors are located in the sinus node, the ventricular myocardium and the coronary vessels.

Animals↗
PubMed1982

Meperidine-promethazine combination and learning function of mice and of their progeny.

Twenty mice aged three to four months and trained to find food in a six compartment maze after a 24 hour fast, were divided into two equal groups. For just over one month the group which had received intraperitoneal meperidine 3 microgram.g-1 and promethazine 1.66 microgram.g-1 performed significantly slower than the group which had received intraperitoneal physiological saline. Because of this marked effect, it was decided to investigate the action of the drug combination on brain development and to assess whether it produced permanent retardation in learning function. The dams of a second group of 12 mice were, therefore, given either the same dose of drug combination or saline. At the age of seven weeks, the six pups born to dams which had received intramuscular saline and the six born to dams which were given intramuscular promethazine with meperidine performed equally well in a series of tests conducted in a T maze and in the six compartment maze after a 24 hour fast. In the T maze they had to distinguish between the presence of food provided in diminishing amounts or no food. In the six compartment maze they were tested with multiple maze pattern sequences. Meperidine and promethazine given during early labor does not permanently affect the learning function of the progeny of mice.

Aging↗
PubMedDate not supplied

A comparison of papaveretum-promethazine with morphine-ondansetron for patient-controlled analgesia.

BACKGROUND: Patient-controlled analgesia (PCA) with intravenous morphine is commonplace. Antiemetics are often added to reduce side-effects. In our institution an unusual combination of papaveretum-promethazine is in use. AIMS: We set out to compare this combination with a more commonly used one (morphine-ondansetron) by auditing the records of our pain-control team assessing analgesia and control of side-effects. METHODS: The records of two groups of 100 consecutive patients were studied. Pain scores were recorded 24 hours post-operatively on a scale of zero to ten. Also recorded were sedation scores, pruritus, emesis, and usage of breakthrough analgesia. The groups contained the work of a variety of anaesthetists and surgeons, though the majority were orthopaedic cases. All results were recorded by one pain-control nurse, using the same question, over a nine-month period. RESULTS: Sedation scores were identical, while side-effects were few and similar in both groups. The use of breakthrough analgesia was also similar. However, the median pain-score of zero in the papaveretum group was significantly lower than that of two in the morphine group, (p < 0.001, Mann-Whitney U). CONCLUSION: Papaveretum-promethazine appeared to be effective for PCA. This combination is also much less expensive than morphine-ondansetron. A previously described synergistic interaction between promethazine and opiates may be a factor in its success. Further evaluation of these drugs in PCA is warranted.

Analgesia, Patient-Controlled↗
PubMed1993

Rapid, sensitive high-performance liquid chromatographic method for the quantification of promethazine in human serum with electrochemical detection.

A method of analysis has been developed to quantify promethazine in human serum with a sensitivity that was suitable for bioavailability studies following a 50.0-mg rectal dose. The limit of quantification from 1.0 ml of serum for promethazine using electrochemical detection was 0.200 ng/ml. At this concentration, the total coefficient of variation obtained from seven replicates over the course of three days of validation was 7.53%. The amount of serum required, the ease of sample preparation and the precision of the method at the limit of quantification demonstrated an improvement over previous assays. A validation study was completed that included an evaluation of recovery, ruggedness, linearity of response, accuracy, precision, sensitivity, stability and selectivity. The method was then used to determine promethazine serum levels in a 36-subject bioavailability study following a 50.0-mg suppository dose.

Chromatography, High Pressure Liquid↗
PubMed1986

Effect on bone ash weights of long-term treatment of mice with oral promethazine HCl.

Ten and 18-month-old female B6D2F1 mice were given promethazine HCl in their drinking water (2.0-4.0 mg/dl and 1.0 mg/dl, respectively) and age, sex and weight matched controls were given acidified tap water. The surviving mice were killed when they were 30.5 months old and femur, ilium and sacrum ash weights were determined. It was found that promethazine HCl effectively prevented age-related mineral loss at the higher does level. There was no evidence of excess morbidity or mortality among the mice given promethazine.

Aging↗
PubMed1986

Age-related osteopenia in the mouse: effects of an H1 blocker, a phenothiazine, and promethazine.

Mature and old B6AF1 and B6D2F1 mice were given acidified tap water or promethazine HCl (a phenothiazine with H1 receptor blocking activity), chlorpheniramine (an H1 blocker) or trifluoperazine (a phenothiazine with no H1 blocking activity) in their drinking water, and the effects of these agents on bone mineral content were assessed by intermittently measuring the 24-h whole body retention of Tc 99m methylene diphosphonate (Tc 99m MDP, an indicator of bone metabolism) and at the end of the studies by determining ash weights of femur, ilium and sacrum. It was found that 24-h retention of Tc 99m MDP was elevated in old mice as it is in old osteopenic humans, that promethazine but not chlorpheniramine or trifluoperazine inhibited bone loss in aging mice, and that there was a correlation between decrease in retention of Tc 99m MDP and decreased bone loss. These preliminary results suggest that the ability of promethazine to inhibit age-related bone loss may not be mediated through its action as an H1 blocker or as a phenothiazine. However, more agents of each type need to be tested before this point can be established.

Age Factors↗
PubMed1994

Quantification of chlorprothixene, levomepromazine and promethazine in human serum using high-performance liquid chromatography with coulometric electrochemical detection.

Isocratic reversed-phase high-performance liquid chromatography with coulometric electrochemical detection was optimised to quantify the neuroleptic drugs chloroprothixene, levomepromazine, and promethazine in human serum. The method involves extraction of the neuroleptic drugs in n-heptane-isoamylalcohol from the alkalinized serum, followed by chromatographic separation on a Nucleosil CN column with acetonitrile-pyridine-sodium acetate buffer as the mobile phase. The extraction recovery was > 85% for each neuroleptic drug. The sensitivity and selectivity required for pharmacokinetic studies was obtained with a dual coulometric analytical cell operating in the oxidative screen mode. The lower limit of detection in human serum for chlorprothixene, levomepromazine, and promethazine, was 0.5, 0.2 and 0.1 ng/ml, respectively. A linear relationship (r2 > 0.99) was obtained between the concentrations of each neuroleptic drug and the detector signal. The accuracy of the quality control samples was +/- 7% for each neuroleptic drug with a precision within 9.5%, 8.1% and 13.5% for chlorprothixene, levomepromazine, and promethazine, respectively. The neuroleptic drugs were stable in acetonitrile and human serum for at least six months when stored at -20 degrees C. This method is applicable to analyze a large number of serum samples for pharmacokinetic studies of the neuroleptic drugs.

Chlorprothixene↗
PubMed1992

Spectrophotometric determination of promethazine by flow injection analysis and oxidation by CeIV.

A flow injection analysis (FIA) procedure is proposed for the determination of promethazine. The sample solution is directly injected into the carrier-reagent stream which comprises a solution of ceric ions in a sulphuric acid medium. The absorbance at 514 nm from the red colour developed by the oxidation of promethazine is measured. Effects of foreign substances have been investigated and the procedure has been applied to the determination of promethazine in a pharmaceutical formulation (tablets).

Cerium↗
PubMed1980

The effect of dexamethasone and promethazine administration on adhesion formation, tubal function, and ultrastructure following microsurgical anastomosis of rabbit oviducts.

In a controlled study, 24 rabbits underwent bilateral division and immediate microsurgical anastomosis of the oviducts. Dexamethasone and promethazine were administered to 13 rabbits in a dose and route of administration similar to those used in clinical practice. Eleven control rabbits received a saline vehicle. Morbidity and mortality were encountered only in the dexamethasone and promethazine-treated group. Dexamethasone and promethazine did not appear to influence the formation of intraluminal and peritubal adhesions, histology, ultrastructure, patency, implantation, or pregnancy rates. The presence of intraluminal adhesions, as seen by scanning electron microscopy, was associated with relatively more efficient tubal function as measured by the ability of the oviducts to convey ova to intrauterine implantation sites. Collagen accumulation in the muscularis, as demonstrated by trichrome staining, was associated with relatively decreased tubal function.

Animals↗
PubMed1994

Response of a promethazine-induced coma to flumazenil.

We report the first case of a patient in a promethazine-induced coma responding to treatment with flumazenil. A literature search conducted to determine the mechanism behind the antagonism of this overdose showed that promethazine interacts with receptors in the central nervous system. Sedative effects may, in fact, be mediated through the benzodiazepine receptor. We concluded that flumazenil can antagonize the sedative effects of promethazine at these receptors to return the patient to a wakeful state.

Aged↗
PubMed1985

Determination of promethazine in human plasma by automated high-performance liquid chromatography with electrochemical detection and by gas chromatography-mass spectrometry.

A highly specific and sensitive method using automated high-performance liquid chromatography with electrochemical detection (HPLC-ED) and a method using gas chromatography-mass spectrometry (GC-MS) have been developed for the quantitative determination of promethazine in plasma. The lowest detectable concentration by HPLC-ED is 0.1 ng/ml of plasma and by GC-MS 0.5 ng/ml of plasma. The HPLC-ED method incorporates a valve switching unit to prevent all of the electroactive impurities from entering the electrode compartment, thus maintaining the sensitivity of the detector for the analyses of large numbers of samples. The GC-MS method incorporates the highly specific selected-ion monitoring technique. Plasmas derived from healthy subjects each given a single 50-mg oral dose of promethazine were analyzed by both HPLC-ED and GC-MS. The two methods compare favorably with a correlation coefficient of 0.92 and a slope of 1.059. While both methods are suitable for studying single-dose pharmacokinetics of promethazine, the automated HPLC-ED method has a decided advantage in being more sensitive and suitable for unattended overnight analyses of the large number of samples encountered in pharmacokinetic studies. The specificity of the HPLC-ED method is demonstrated by comparison to the GC-MS analysis of biological samples.

Chromatography, High Pressure Liquid↗
PubMed1994

Lorazepam-enhancement of the antiemetic efficacy of dexamethasone and promethazine. A placebo-controlled study.

This investigation was designed with the objective of improving on currently available antiemetic regimens to counteract the disabling side effects of cancer chemotherapy. The combination of lorazepam, dexamethasone, and promethazine was compared with dexamethasone and promethazine without lorazepam in a double-blind crossover study. The initial study population consisted of 92 women (most with breast cancer) and 7 men; all received moderately or highly emetogenic chemotherapy. Complete data for both periods of therapy were available for 73 of these patients. Crossover analysis showed a highly significant effect of lorazepam in reducing the severity of nausea (p = .003); the severity of vomiting was also reduced, but less dramatically (p = .051). The frequency of all degrees of nausea and vomiting was less with lorazepam, but the difference was not statistically significant. It is concluded that lorazepam added to dexamethasone and promethazine provides an effective regimen for counteracting the emetic side effects of cancer chemotherapy.

Adult↗
PubMed1983

Determinants of systemic availability of promethazine in rabbits.

Promethazine blood concentration-time curves have been determined in 7 rabbits following intravenous, oral and hepatic portal vein administration of promethazine. This phenothiazine has a large volume of distribution and a high metabolic clearance resulting in low blood concentrations particularly when the oral route is used. Analysis of the areas under the blood concentration-time curves indicates that hepatic first-pass metabolism is the major determinant of promethazine's low oral availability. Absorption from the gastrointestinal tract is essentially complete in most rabbits and the contribution of metabolism by the intestinal mucosa is minimal. The present findings are compared with the literature on other phenothiazines.

Animals↗