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Results for “Promethazine”

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At least 19 recordsLinked to original sources

PubMed1975

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↗

PubMed1978

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↗

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↗

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↗

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↗

PubMedDate not supplied

Morphine and promethazine as intravenous premedicants.

Two hundred seventy patients received morphine 5 mg or 10 mg alone or with promethazine 6.25 mg, 12.5 mg, or 25 mg. Promethazine 25 mg alone also was studied. All drugs were given intravenously. Anxiety relief, sedation, patient acceptance, lack of recall, and side effects were the variables examined. Promethazine improved relief of anxiety, sedation, and patient acceptance when added to morphine. Doses of promethazine larger than 12.5 mg intravenously failed to improve these effects. Memory remained unaffected by any of the drugs.

Adolescent↗

PubMed1979

Prolonged kidney allograft survival with promethazine.

The effects of promethazine hydrochloride have been investigated in a rabbit kidney allograft model. The drug was ineffective on its own, but if added to a protocol that induced partial suppression of rejection in 50% of recipients, its effect was dramatic. Allograft survival was prolonged from a control mean of 10.3 days to a mean of 26.3 days. One animal survived 2 1/2 months, and no other drug than promethazine was given after day 6. Promethazine and 6-methylprednisolone alone also prolonged allograft survival, but the results were significantly better if the recipient had been exposed to donor blood before grafting. The results suggest that promethazine is a useful adjuvant immunosuppressive drug. It could be beneficial in man.

Adjuvants, Immunologic↗

PubMed1976

Effects of intravenous meperidine and meperidine with promethazine on uterine activity and fetal heart rate during labor.

A prospective study of the effects of the i.v. injection of 75 mg meperidine, alone or combined with 25 mg promethazine, was conducted by continuous and direct monitoring of the fetus and of intrauterine pressure. The study was carried out in 16 primiparas and 24 multiparas in active spontaneous labor with cervical dilatation of 3 to 4 cm. Administration of meperidine and of meperidine with promethazine was associated with an increase in uterine activity of 31 to 45% (Montevideo units), respectively. The most marked effects were on the amplitude of the uterine contractions. There was no significant change in uterine tone. A tetanic response was recorded in two patients who vomited after the administration of meperidine with promethazine and was followed by slowing of the fetal heart rate. In no other cases were there significant changes in fetal heart rate. Except for the latter two patients, no adverse effect of meperidine or of meperidine with promethazine on the fetal heart rate was noted. The condition of the newborns at birth was excellent in all but three cases, in two of which maternal amniotic infection and high fever were present.

Female↗

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↗

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↗

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↗

PubMed1978

Oxidative degradation of pharmaceutically important phenothiazines I: Isolation and identification of oxidation products of promethazine.

The thermal degradation of promethazine in water in the presence of oxygen was studied. After degradation, the products were isolated by TLC. Identification was carried out by comparison of the isolated compounds with reference compounds. Melting points, spectral data, and polarographic and chromatographic behavior were compared. The following products were identified: 10-methylphenothiazine, phenothiazine, 3H-phenothiazine-3-one, phenothiazine 5-oxide, promethazine 5-oxide, 7-hydroxy-3H-phenothiazine-3-one, acetaldehyde, formaldehyde, and dimethylamine.

Chemical Phenomena↗

PubMed1976

Possible effect of maternal promethazine therapy on neonatal immunologic functions.

The effect of the administration of promethazine in the treatment of erythroblastosis fetalis was studied in four maternal-fetal pairs. The three infants exposed for a prolonged period of time had decreased neonatal number and function of T cells, and abnormal specific humoral immune responses. The possible role of promethazine in the induction of fetal immunoincompetence is discussed.

Antibodies↗

PubMed1977

Selective inhibition of Bacillus subtilis sporulation by acridine orange and promethazine.

Two structurally similar compounds were found to inhibit sporulation in Bacillus subtilis 168. A dye, acridine orange, and an antischizophrenic drug, promethazine, blocked spore formation at concentrations subinhibitory to vegetative growth, while allowing synthesis of serine protease, antibiotic, and certain catabolite-repressed enzymes. The sporulation process was sensitive to promethazine through T2, whereas acridine orange was inhibitory until T4. The drug-treated cells were able to support the replication of phages phie and phi29, although the lytic cycles were altered slightly. The selective inhibition of sporulation by these compounds may be related to the affinity of some sporulation-specific genes to intercalating compounds.

Acridines↗

PubMed1978

Butorphanol and promethazine as pre-anaesthetic medication.

An open evaluation of a combination of butorphanol (1 or 2 mg), promethazine (25 or 50 mg) and atropine (0.5 mg) in 109 adult consenting patients was carried out to determine their safety and efficacy for preanaesthetic medication. All patients were kept under direct surveillance from before intramuscular medication until they were in satisfactory condition post-operatively for discharge from the recovery room. The medications employed did not disturb the blood pressure, pulse rate or respiration rate in any of the patients. None complained of nausea or dizziness while only one was slightly excited. Sedation was rated as satisfactory in 97 per cent, and 90 per cent were free of apprehension. In addition, global evaluation of the premedication by the investigator was rated good to excellent in 99 per cent of the patients. On the basis of these observations, the combination of butorphanol with promethazine and atropine appears safe and useful for pre-anaesthetic medication.

Adolescent↗

PubMed1976

The effect of promethazine hydrochloride on bilirubin metabolism in the rat.

The effect of 21 days of promethazine-HC1 administration on hepatic bilirubin metabolism and transport was studied in adult rats. A significant increase in mean cumulative hepatic bilirubin uptake (84.5 +/- 7.6 (SE) mug/100 g/min in controls vs. 110.0 +/- 4.3 in treated rats), mean hepatic glucuronide conjugation (1,330 +/- 86 (SE) mug bilirubin conjugated/g liver/40 min in controls vs. 1.713 +/- 61 in treated rats), and mean maximal hepatic excretion (47.2 +/- 4.9 (SE) mug/100 g/min vs. 63.5 +/- 2.7) was observed in treated animals. Mean total liver weight and total hepatic protein also increased significantly. These observations suggest that promethazine is an inducer of protein and enzyme synthesis in rat liver and is capable of significantly stimulating the three major steps in hepatic disposal of bilirubin.

Animals↗

PubMed1979

Control of radiation-induced emesis with promethazine, cimetidine, thiethylperazine, or naloxone.

Promethazine (2 mg/kg), cimetidine (4 mg/kg), thiethylperazine (0.86 mg/kg), and naloxone (0.08 mg/kg) were each evaluated for their ability to increase the threshold of radiation-induced emesis in the dog. Each dog was fed a can of dog food (ca 0.4 kg) and then injected IM with the appropriate drug 1 hour before being irradiated by a 60Co teletherapy unit. The total radiation dose given an individual dog was determined by an up-and-down exposure schedule. Dogs were then observed continuously for 10 hours while the number, time of onset, and duration of each emetic episode were monitored. The dose of radiation causing emesis in 50% (ED50 +/- SEM) of control dogs was 170 +/- 38.5 rad. The ED50 +/- SEM was increased to 402 +/- 18.6 rad by promethazine, to 331 +/- 27.3 rad by cimetidine, and to 320 +/- 38.5 rad by thiethylperazine. This increased tolerance was significant at P less than 0.05 for each drug. The ED50 for naloxone was 262.5 +/- 92.9 rad, which was not a statistically significant increase in threshold.

Animals↗

PubMed1978

In vitro and in vivo effects of promethazine (Phenergan) on drug metabolism.

Prolongation effects of promethazine on the pentobarbital sleeping time are not due to interactions of this drug with cytochrome P-450 or cytochrome c reductase or inhibition of drug metabolism because pentobarbital plasma levels in promethazine treated animals before awakening are not different than in controls. Results suggest additive effects of both drugs on the central nervous system. Those interactions do however play a role during in vitro studies.

Animals↗