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At least 19 recordsLinked to original sources
PubMed1986

Irreversible binding with biological macromolecules and effects in bacterial mutagenicity tests of the radical cation of promethazine and photoactivated promethazine. Comparison with chlorpromazine.

The irreversible binding of the radical cation of promethazine (PMZ+.) to DNA and protein in vitro and bacterial macromolecules in situ has been studied. Binding experiments were performed with synthesized [35S] promethazine. The results are compared to those with the chlorpromazine radical cation (CPZ+.). Secondary reaction products which result from fission of the alkylamino side chain are involved in the macromolecular binding of PMZ+. Compared to CPZ+. the covalent DNA binding of PMZ+. is significantly less. A larger amount of PMZ+. binds to single-stranded DNA than to double-stranded DNA. The extent of binding to proteins and RNA is of the same order as that of CPZ+. Bacterial mutagenicity tests show that the low genotoxicity of PMZ+. is related to the low DNA binding. The bacterial cytotoxicity is possibly related to the covalent protein binding. Similar results have been obtained with photoactivated promethazine (PMZ) and chlorpromazine (CPZ). The role of radical cations in the photosensitization and metabolic activation of phenothiazine drugs is discussed.

Animals↗
PubMed1990

Magnesium sulfate and promethazine do not interact to cause hypotension in gravid ewes.

The purpose of this study was to determine whether magnesium sulfate and promethazine interact to cause hypotension in gravid ewes. Fifteen experiments were performed in five chronically instrumented animals between 125 and 130 days of timed gestation (term = 145 days). In one group of experiments each animal received magnesium sulfate (4 gm intravenous bolus followed by 4 gm/hr intravenous infusion) then promethazine (50 mg intravenously). In a second group each animal received magnesium sulfate then saline solution as a control. In a third group each animal received saline solution then promethazine. Infusion of magnesium sulfate increased the mean (+/- SEM) serum magnesium concentration to 5.7 +/- 0.6 and 6.6 +/- 0.6 mg/dl in the magnesium sulfate-promethazine and magnesium sulfate-saline solution groups, respectively. Magnesium sulfate slightly decreased maternal mean arterial pressure (p less than 0.05) and increased cardiac output (p less than 0.05) in both the magnesium sulfate-promethazine and magnesium sulfate-saline solution groups. Otherwise there were no significant changes in maternal mean arterial pressure or cardiac output in any group. Promethazine increased maternal heart rate (p = 0.0001) in both the magnesium sulfate-promethazine and saline solution-promethazine groups. Magnesium sulfate increased uterine blood flow (p less than 0.01) in both the magnesium sulfate-promethazine and magnesium sulfate-saline solution groups, but promethazine blunted the increase in uterine blood flow associated with magnesium sulfate. Similarly, magnesium sulfate decreased uterine vascular resistance (p less than 0.01) in both the magnesium sulfate-promethazine and magnesium sulfate-saline solution groups, but promethazine eliminated the decrease in uterine vascular resistance associated with magnesium sulfate. Maternal and fetal arterial blood gas and acid-base values did not change in any group, except that there was a small, near-significant decrease (p = 0.06) in fetal pH 10 minutes after promethazine was given in the magnesium sulfate-promethazine group. We conclude that magnesium sulfate and promethazine did not interact to cause maternal hypotension in normovolemic gravid ewes. However, promethazine increased maternal heart rate and blunted the increase in uterine blood flow associated with magnesium sulfate.

Animals↗
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↗
PubMed1991

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↗
PubMed1992

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↗
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↗
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↗
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↗
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↗
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↗
PubMed1992

Influence of promethazine on symptom-therapy scores for nausea during patient-controlled analgesia with morphine.

We assessed whether adding promethazine to the syringe containing morphine for patient-controlled analgesia (PCA) decreases nausea after gynecologic surgery. Patients were assigned randomly to receive PCA (morphine 1.5 mg, 6-min lockout interval) with or without promethazine (0.625 mg/PCA dose, providing an average of 17.6 mg/24 h). Assessments included a visual analogue scale (VAS) for nausea (0 = none, 10 = worst possible) at scheduled times, rescue therapy requirements, and a maximum symptom-therapy score that provided an aggregate assessment of nausea intensity, duration, and response to rescue therapy (0 = no nausea; 1 = mild; 2 = moderate, requiring droperidol; 3 = severe or persistent, requiring droperidol; 4 = requiring droperidol+transdermal scopolamine; 5 = unrelieved). Nausea scores on the visual analogue scale at 2, 6, 8, and 24 h and use of rescue droperidol identified no significant differences between the groups. However, symptom-therapy scores differed significantly, with median values of 0 and 2, respectively, for the promethazine-treated and control groups. We conclude that simultaneous titration of morphine and promethazine decreases nausea associated with PCA therapy; the difference may best be appreciated with use of the combined symptom-therapy score.

Adult↗
PubMed1991

[Potentiation by promethazine of hypotensive effects of adrenergic drugs on intraocular pressure].

Experiments including previous installations of promethazine (pipolphen) into the conjunctival sac followed by the topical administration of beta-adrenergic blocker timolol or a sympathomimetic drug isoptoepinal (adrenaline) have been performed on 24 rabbits (48 eyes). The substantial changes in the action mode of the mentioned drugs as the enhancement of their hypotensive effect on the intraocular pressure (IOP) have been demonstrated under the performance of the above mentioned procedure. When applied after promethazine instillations, timolol induced significantly increased outflow facility of the aqueous humor that was not usually noted in the cases of timolol topical instillations without a pretreatment of the eye with promethazine. The similar increased hypotensive effect on the IOP was noted for adrenaline when it has been used after promethazine treatment. The possible mechanisms underlying the changes in pharmacological activities of the investigated adrenergic drugs are discussed.

Adrenergic beta-Antagonists↗
PubMed1990

[Effects of promethazine on acupuncture analgesia].

Promethazine, one of histaminergic H1-receptor antagonist, was often used as an adjuvant drug prior to and during acupuncture anesthesia in clinics, However, its effects was not known clearly. By using potassium iontophoretic dolorimetry and stimulating unilateral "Hegu" and "Waiguan" points with electroacupuncture (EA) in 42 rabbits, we found that Promethazine could drop the pain threshold in small dosages (0.5 mg/kg, 1 mg/kg) and raise the pain threshold in relatively large dosages (2 mg/kg, 4 mg/kg). In different dosages (1 mg/kg, 2 mg/kg), promethazine could attenuate the analgesic effect of EA. It was suggested that promethazine should be used carefully in acupuncture anaesthesia.

Acupuncture Analgesia↗
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↗