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At least 145 records · Page 8Linked to original sources
PubMed1996

Mood effects of zolpidem versus phenobarbital combined with promethazine in an anesthesiological setting.

Zolpidem, a new imidazo-pyridine hypnotic, acts like a benzodiazepine. Because of its short half-life, zolpidem plays a special role in the group of drugs suitable for anesthesiological premedication because of its sedative and anxiolytic effects. The study compared preanesthesiological treatment by zolpidem and phenobarbital in combination with promethazine in a clinical setting. In a double-blind randomized design, 304 patients awaiting different kinds of surgery were studied. For the assessment of emotional states, a multidimensional rating scale was administered. The study showed differing effects of zolpidem and phenobarbital, which could be demonstrated in the scales 'irritation', 'vulnerability', and 'aggression' and could therefore represent in domain hostility. In most of the other scales there were similar effects of phenobarbital and zolpidem. Assuming that phenobarbital is a potent sedative, the reported results confirm the results found by other authors, that zolpidem also acts as a sedative. The reported results describe promethazine as selectively deactivating. These results are in agreement with the findings of an experimental study which tested the acute effects of stress under promethazine.

Adolescent↗
PubMed2006

Influence of simulated weightlessness on the intramuscular and oral pharmacokinetics of promethazine in 12 human volunteers.

The National Aeronautics and Space Administration (NASA) recommends using promethazine to prevent and treat space motion sickness, but pharmacologic responses in space and on Earth are different. Twelve volunteers were given 50 mg promethazine orally or intramuscularly before and after 48 hours of bed rest to simulate weightlessness. The maximum measured plasma concentration (C(max)), time to C(max) (t(max)), and area under plasma concentration versus time curve from 0 to infinity (AUC(inf)) were determined, and the bioequivalence was tested between bed-rest and ambulatory status for the intramuscular and oral routes as well as between both routes for bed-rest and ambulatory position. Simulated weightlessness did not influence the ratio AUC(bed rest)/AUC(ambulatory) after intramuscular injection, whereas a significant increase (26%) in the ratio was seen after oral administration, probably because of a prolonged contact time between promethazine and the intestinal wall associated with an increase in the intestinal transit time. The AUC was 3-fold higher when the drug was administered by the intramuscular route during both positions. Thus, intramuscular administration could be a good alternative to the oral route.

Administration, Oral↗
PubMed1996

Electron microscopic demonstration of intracelluar promethazine accumulation sites by a precipitation technique: application to the cerebellar cortex of the mouse.

A method is described that allows electron microscopic identification of the phenothiazine neuroleptic promethazine after supravital intracardiac injection of high drug concentrations (greater than or equal to 3 %). The cerebellar cortex of the mouse was used for the investigation. This procedure is based on simultaneous fixation of drug and tissue by immersion in a paraformaldehyde-glutaraldehyde solution with the addition of phosphomolybdic acid. The electron microscopic investigation revealed that the drug could easily be identified as an electron-dense precipitate. Subpopulations of neurons exhibited a higher affinity for the drug than others, but no preference for any nerve cell type was detected. Closer study showed that promethazine accumulated primarily within the cytoplasm, where it was bound to the endoplasmic reticulum. Furthermore, promethazine storage was observed within mitochondria and vesicular structures. Drug binding was also seen in the regions of synapses but without any predilection for these structures. Because this precipitation technique also appears to be well-suited for the ultrastructural identification of other drugs, it offers multiple possibilities for application.

Animals↗
PubMed1997

A peroxidase-catalyzed sulfoxidation of promethazine.

Lactoperoxidase, when incubated with increasing amounts of promethazine (P) and promethazine sulfoxide (PO) catalyzes the formation of promethazine sulfoxide accompanied by oxygen consumption. An intermediate radical of PO can be detected by electron spin resonance (ESR). Catalase or superoxide dismutase do not inhibit the reaction while dopamine does. The lactoperoxidase-catalyzed formation of dopaminochrome in the presence of hydrogen peroxide is inhibited by P. Both P and PO inhibit acetyl- and butyrylcholinesterase. Purified enzymes were used throughout the study and horseradish peroxidase but not myeloperoxidase had an activity similar to that of lactoperoxidase.

Catalase↗
PubMedDate not supplied

Investigation of interaction of promethazine with cyclodextrins.

The effect of beta-CD and its substituted derivatives (DM-beta-CD and HP-beta-CD) on the solubility and photostability of promethazine was investigated in solution and in the solid state. The soluble complexes of protonated (pH = 6.8) and basic (pH = 10.8) forms of promethazine with CDs were studied using the spectral method. The influence of pH and CD complexation on photostability of PM in solution was followed. It was found that the photochemical decomposition of promethazine (PM) alone and in the presence of CD proceeds according to the first order reaction. It was also established that as well the presence of CD as the acidic medium of reaction increased the photostability of PM in solution. Formation of solid inclusion complexes of PM with CDs was evaluated using FT IR, 13C NMR and DSC methods. The results obtained indicate that independently of the complexation method in the solid state (kneading or heating), the presence of CD decreases the solubility of PM; the reason may be that the phenothiazine ring of PM did not enter into the cavity of beta-CD and its derivatives.

Cyclodextrins↗
PubMed2002

A comparison study between ketamine and ketamine-promethazine combination for oral sedation in pediatric dental patients.

This study compared the incidence of vomiting and the sedative effectiveness of ketamine to a ketamine-prornethazine combination in pediatric dental patients. Twenty-two patients with American Society of Anesthesiologists' classification I physical status who were between the ages of 21 and 43 months were randomly divided into 2 groups. The control group received 10 mg/kg of ketamine orally, whereas the experimental group received 10 mg/kg of ketamine and 1.1 mg/kg of promethazine orally. Nitrous oxide in oxygen was supplemented between 35 and 50%. Each patient received 1 or 2 quadrants of restoration by one operator. Heart rate, blood pressure, and oxygen saturation were monitored and recorded during the treatment. Crying, alertness, movement, and overall general behavior were rated using the scale by Houpt et al. A dentist-anesthesiologist conducted the vital sign monitoring and behavioral assessment. Ketamine combined with promethazine eliminated the incidence of vomiting. A 2 x 2 chi-square contingency table showed a statistical difference between the 2 groups at P < .05 (control group, 27%; experimental group, 0%). Ketamine alone yielded better sedations than the combined agents as shown by the Mann-Whitney U statistical analysis (P < .05). Ketamine and a ketamine-promethazine combination are effective in the sedation of pediatric dental patients.

Administration, Oral↗
PubMed1992

[Anodic stripping voltammetry of promethazine hydrochloride with Nafion coated glassy carbon electrode].

This paper reports the determination of promethazine hydrochloride with Nafion coated glassy carbon electrode by anodic stripping voltammetry. There is a linear relationship between the concentration and peak height in the range of 4 x 10(-8)-5 x 10(-5) mol/L and 8 x 10(-5)-1 x 10(-3) mol/L for promethazine hydrochloride. The raw material and tablets of promethazine hydrochloride have been analysed and good results were obtained.

Electrodes↗
PubMed1985

[Determination of aminophylline and promethazine in suppositories].

A method for the determination of theophylline and promethazine in suppositories is proposed which allows the determination of both components in a single suppositorium. The ingredients were extracted by hot water and addition of a little bit of sulfuric acid. Theophylline is determined potentiometrically without separation of promethazine by titrating the acid which is set free after addition of silver nitrate. Promethazine is separated by ether in alkaline medium, reextracted in HCl (0,1 mol/l) and determined colorimetrically. The precision of both methods is good. The results of the determination in the suppositories are given.

Aminophylline↗
PubMed1984

[Prevention of anaphylactoid reactions using intramuscular promethazine and cimetidine. Studies of a histamine infusion model].

The effect of combined intramuscular premedication with H1 + H2-receptor-antagonists on histamine-induced cardiovascular and cutaneous reactions was studied in 8 volunteers in a randomized placebo-controlled double-blind crossover trial and compared with premedication with H1-receptor antagonist alone and with the histamine-induced effects without premedication. As H1-receptor antagonist the volunteers received 0.5 mg/kg promethazine i.m. 45 min before the start of histamine infusion; as H2-receptor antagonist we used 400 mg cimetidine i.m. 120 min before application of histamine. While the premedication with promethazine alone could prevent histamine-induced tachycardia, fall of blood pressure and cutaneous reactions only partially, these reactions were almost completely prevented by combined premedication. Like intravenous application of H1 + H2-receptor antagonists shortly injected before induction of anesthesia, intramuscular premedication with promethazine and cimetidine can prevent anaphylactoid reactions. In contrast to intravenous application, the latter application is also effective in reducing the risk of acid aspiration syndrome and as a sedative.

Adult↗
PubMed1984

Hypothalamic-pituitary-adrenocortical function after the dexamethasone-promethazine adhesion regimen.

Dexamethasone and promethazine are widely used as an antiadhesion regimen in infertility surgery. A major argument against the routine use of dexamethasone has been the concern that suppression of the hypothalamic-pituitary-adrenal axis may result. To investigate this concern, 25 healthy women undergoing surgery for infertility were administered dexamethasone and promethazine preoperatively, intraoperatively, and postoperatively for 48 hours. Insulin hypoglycemia testing was performed on postoperative day 6. A normal rise in cortisol of at least 7 micrograms/dl was observed in 19 of 21 women. Two women failed to achieve this rise, despite adequate hypoglycemia. Short-term suppression of the hypothalamic-pituitary-adrenal axis may occur after administration of the dexamethasone-promethazine regimen. Patients receiving this regimen should be carefully supervised during the postoperative period.

Blood Glucose↗
PubMed1984

Poisoning from dermal absorption of promethazine.

Two cases in which dermal absorption of promethazine hydrochloride resulted in a toxic neurologic syndrome are reported. The symptoms included central nervous system depression, acute excitomotor manifestations, ataxia and visual hallucinations. In addition, peripheral anticholinergic effects occurred. These symptoms are comparable with those of oral, intramuscular and rectal overdose of promethazine. The demonstrated risks of the topical use of promethazine outweigh any benefits.

Administration, Topical↗
PubMed1982

Effects of promethazine on hemorrhagic shock in the dog.

The effects of pre- and post-treatment with promethazine, an antihistamine, in hemorrhage-shocked dogs were investigated. Survival to 6 hours was enhanced in the dogs given (IM administration) the H1-receptor antagonist at 1 hour before hemorrhage was induced when compared with survivals of saline-treated control dogs (3 of 5 dogs vs 1 of 5 dogs). Furthermore, 4 of 5 dogs given (IV administration) promethazine at 30 minutes after the initial hemorrhage survived. Promethazine treatment by either route increased mean arterial pressure among surviving dogs throughout the 6-hour experimental period.

Animals↗
PubMed1994

Premedication with Midazolam (Dormicum) compared with Promethazine, Droperidol and placebo in relieving anxiety using Beck's anxiety inventory.

In a randomized double-blind study, Midazolam (Dormicum) (7.5 mg) was compared with Promethazine (Phenergan) (25 mg), Droperidol (2.5 mg) and placebo as premedication for 98 pre-selected patients undergoing surgery. The anxiolytic effect of the above drugs was monitored by Beck's Anxiety Inventory. 83.3% of patients who received Midazolam had a decrease in their anxiety state compared to 55.6% for Promethazine, 12% for Droperidol and 25% for placebo. The study clearly proved that Midazolam is a better anxiolytic drug compared to Droperidol and Promethazine.

Adolescent↗
PubMed1997

Trypanocidal effects of promethazine.

Promethazine is currently used for its antipsychotic and ansiolytic effects. It is a phenothiazine with anticalmodulin action, not toxic for human beings at therapeutic doses. The present results show that promethazine has trypanocidal effect on both epimastigote and trypomastigote stages of T. cruzi; two hundred microM inhibited epimastigote growth in culture medium and 2 microM immobilized and killed bloodstream trypomastigotes. When promethazine (55 mg/Kg/day) was used as treatment of T. cruzi infected mice, it proved effective in reducing parasitemia and it increased the survival of treated animals. Ultrastructural studies suggest that the lethal effect of this phenothiazine is related to a detergent effect that disrupts T. cruzi cell membrane.

Animals↗
PubMed1996

Intramuscular ketamine is superior to meperidine, promethazine, and chlorpromazine for pediatric emergency department sedation.

OBJECTIVE: To compare ketamine hydrochloride (KET) with combined meperidine hydrochloride, promethazine hydrochloride, and chlorpromazine hydrochloride (MPC) for pediatric emergency department sedation with respect to onset, duration, and efficacy. DESIGN: Prospective, randomized, double-blind clinical trial. SETTING: Pediatric emergency department in an urban university hospital. PATIENTS: Convenience sample of 29 patients, 6 months to 6 years of age, requiring sedation for suturing, wound or burn debridement, or lumbar puncture. INTERVENTION: Children received intramuscular KET (4 mg/kg) with atropine sulfate (0.01 mg/kg) or MPC (meperidine hydrochloride 2 mg/kg, promethazine hydrochloride 1 mg/kg, chlorpromazine hydrochloride 1 mg/kg). Data collection included demographics, vital signs, and onset of sedation; procedural distress using the Observational Scale of Behavioral Distress; and time to recovery. The operator was questioned on satisfaction with the drug, and parents received follow-up to assess parental satisfaction. RESULTS: Of the 29 patients enrolled in the study, 2 were excluded for protocol violation, 15 received KET, and 12 received MPC. Demographics and baseline vital signs did not differ. Although patients in the 2 groups had a similar duration of sedation (KET, 82 min vs MPC, 97 min, P = .15), patients receiving KET had more rapid onset of sedation (3 min vs 18 min, P < .01) a shorter time to discharge (85 min vs 113 min, P 0 .01) and lower Observational Scale of Behavioral Distress scores (9.9 vs 19.2, P = .003). All 15 physicians using KET would request it again vs 5 of 12 (42%) of the physicians using MPC (P < .001). No serious adverse reactions occurred. There were no differences in parental satisfaction. CONCLUSION: Ketamine has a faster onset and results in more rapid discharge from the pediatric emergency department while providing for less patient distress during procedures. Ketamine is also associated with greater physician satisfaction than MPC.

Child↗
PubMedDate not supplied

Spectrofluorimetric determination of diethazine and promethazine in pharmaceutical preparations.

A simple, sensitive and accurate spectrofluorimetric method is described for the quantitative determination of diethazine and promethazine either in the pure form or in its pharmaceuticals. The method is based on the formation of red fluorescent product of these drugs with Au(III). A linear calibration graph is obtained over the range 0.05-100 p.p.m. of diethazine and promethazine.

Gold↗
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↗
PubMed1998

Bioavailability of intranasal promethazine dosage forms in dogs.

Intramuscular promethazine (PMZ) is used aboard the US Space Shuttle to ameliorate symptoms of space motion sickness. Bioavailability after an oral dose of PMZ during space flight is thought to be impaired because of gastrointestinal disturbances associated with weightlessness and space motion sickness. In an attempt to find an alternative dosage form for use in space, we evaluated two intranasal (i.n.) dosage forms of PMZ in dogs for absorption and bioavailability relative to that of an equivalent intramuscular dose. Promethazine (5 mg kg-1) was administered as two intranasal dosage forms and as an intramuscular (i.m.) dose to three dogs in a randomised cross-over design. Serial blood samples were taken and analysed for PMZ concentrations and the absorption and bioavailability of PMZ were calculated for the three dosage forms. PMZ absorption from the carboxymethyl cellulose microsphere i.n. dosage form was more rapid and complete than from the myverol cubic gel formulation or from an i.m. injection. Bioavailability of the microsphere formulation was also greater than that of the gel formulation (AUC 3009 vs 1727 ng h ml-1). The bioavailability of the two i.n. dosage forms (relative to that of the i.m. injection) were 94% (microsphere) and 54% (gel). The i.n. microsphere formulation of PMZ offers great promise as an effective non-invasive alternative for treating space motion sickness due to its rapid absorption and bioavailability equivalent to the i.m. dose.

Administration, Intranasal↗