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PubMed1987

Nabilone versus prochlorperazine for control of cancer chemotherapy-induced emesis in children: a double-blind, crossover trial.

In a randomized, double-blind, crossover trial, nabilone was compared to prochlorperazine for control of cancer chemotherapy-induced emesis in 30 children 3.5 to 17.8 years of age. All subjects received two consecutive identical cycles of chemotherapy with the trial antiemetics given in accordance to a body weight-based dosage schedule beginning eight to 12 hours before treatment. The overall rate of improvement of retching and emesis was 70% during the nabilone and 30% during the prochlorperazine treatment cycles (P = .003, chi 2 test). On completion of the trial, 66% of the children stated that they preferred nabilone, 17% preferred prochlorperazine, and 17% had no preference (P = .015, chi 2 test). Major side effects (dizziness, drowsiness, and mood alteration) were more common (11% v 3%) during the nabilone treatment cycles. CNS side effects appeared to be dose related and were most likely to occur when the nabilone dosage exceeded 60 micrograms/kg/d, but individual tolerance to nabilone varied considerably. Lower dosages of nabilone were associated with equivalent efficacy and no major side effects. Nabilone appears to be a safe, effective, and well-tolerated antiemetic drug for children receiving cancer chemotherapy. Although major side effects may occur at higher dosages, nabilone is preferable to prochlorperazine because of improved efficacy.

Adolescent↗
PubMed1986

Extrapyramidal reactions to prochlorperazine and haloperidol in the United Kingdom.

The epidemiology of extrapyramidal reactions to prochlorperazine and haloperidol in the United Kingdom has been studied using reports in the Adverse Reactions Register of the Committee on the Safety of Medicines (CSM) and from general practitioner prescribing data. Between 1967 and 1982 there were an estimated 37.0 million prescriptions for prochlorperazine and 3.2 million for haloperidol; in this time there were 104 reports of adverse reactions to prochlorperazine and 62 to haloperidol. The predominant extrapyramidal reaction reported was dystonia-dyskinesia (99 reports for prochlorperazine and 47 for haloperidol). The remaining reactions reported were of Parkinsonism. Dystonia-dyskinesia usually occurred within three days of commencing treatment, and for both drugs the incidence, expressed per million prescriptions, varied significantly with age, the highest incidence being in patients under 20 years. Thus young patients appear at particular risk of acute extrapyramidal reactions to dopamine receptor antagonists.

Adolescent↗
PubMedDate not supplied

Antiemetic efficacy of prochlorperazine, haloperidol, and droperidol in cisplatin-induced emesis.

The antiemetic efficacy of haloperidol, droperidol, and prochlorperazine in preventing cisplatin-induced emesis was evaluated. Twenty-seven patients receiving 51 courses of cisplatin chemotherapy randomly received antiemetic treatment with prochlorperazine (6 mg/sq m), droperidol (1 mg/sq m), or haloperidol (1 mg/sq m) in a double-blind crossover study. Antiemetics were given by intramuscular injection one hour before beginning cisplatin and every three hours thereafter for a total of six doses. The number of emetic episodes, volume of emesis, and duration of the emetic episodes were monitored by oncology nurses. There were no significant differences in the median number of emetic episodes among antiemetic treatments: 3.5 for prochlorperazine, 4.0 for haloperidol, and 3.0 for droperidol. There were also no significant differences among the antiemetics in the median volume of emesis or the median duration of the emetic episodes. At the doses used in this study, the antiemetic efficacy of prochlorperazine, droperidol, and haloperidol appear to be comparable for patients receiving cisplatin chemotherapy.

Aged↗
PubMed1980

Antiemetic effect of tetrahydrocannabinol. Compared with placebo and prochlorperazine in chemotherapy-associated nausea and emesis.

Fifty-five patients harboring a variety of neoplasms and previously found to have severe nausea or emesis from antitumor drugs were given antiemetic prophylaxis in a double-blind, randomized, crossover fashion. Tetrahydrocannabinol (THC), prochlorperazine, and placebo were compared. Nausea was absent in 40 of 55 patients receiving THC, eight of 55 patients receiving prochlorperazine, and five of 55 in the placebo group. The antiemetic effect of THC appeared to be more efficacious for cyclophosphamide, fluorouracil, and doxorubicin hydrochloride, and less so for mechlorethamine hydrochloride and the nitrosureas. Tetrahydrocannabinol appears to offer significant control of nausea in most patients and exceeding by far that provided by prochlorperazine.

Adult↗
PubMed1995

The cationic lipid stearylamine reduces the permeability of the cationic drugs verapamil and prochlorperazine to lipid bilayers: implications for drug delivery.

The therapeutic activity of a wide variety of drugs is significantly improved when their longevity in the circulation is extended by encapsulation in liposomes. To improve the retention of cationic drugs in liposomes, we have investigated the effect of the cationic lipid stearylamine on the permeability of the calcium channel blocker verapamil and the antipsychotic drug prochlorperazine, both of which are also multidrug resistance modulators. Both drugs were efficiently incorporated into liposomes composed of DSPC/cholesterol that possessed a transmembrane pH gradient (inside acidic). However, the efflux of the loaded drugs was relatively rapid (i.e., 50% of the encapsulated verapamil was released after 4 h at 37 degrees C), despite the presence of a 3 unit pH gradient (pHi = 4.0, pHo = 7.5). Drug retention within the liposomes was improved by increasing the magnitude of the transmembrane pH gradient to approx. 5 units (pHi = 2.0, pHo = 7.5). Further improvements in drug retention were achieved by the addition of 10 mol% of the cationic lipid stearylamine in the DSPC/cholesterol liposomes. The combination of the 5 unit pH gradient and stearylamine resulted in increases of the retention of verapamil and prochlorperazine by approx. 20- and 5-fold, respectively. Calculation of the permeability coefficients for the charged (cationic) and neutral forms of the drugs indicated that the neutral forms of both drugs were approx. 10(4)-fold more permeable than were the cationic forms of the drugs. Further, the presence of stearylamine reduced the permeability coefficient for the cationic species of the drugs by approximately an order of magnitude, but had no effect on the neutral species of the drugs. The efflux curves observed for both verapamil and prochlorperazine could be mathematically modeled by assuming that the primary influence of stearylamine was on the development of a positive surface charge density on the inner monolayer of the liposome. Taken in sum, these results indicate that stearylamine is effective at decreasing the leakage of cationic drugs from liposomes, and may prove to be a valuable component of liposomal drug formulations.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1992

A randomised trial of dexamethasone, lorazepam and prochlorperazine for emesis in patients receiving chemotherapy.

To define further the place of dexamethasone in antiemetic combinations, lorazepam, prochlorperazine and placebo (LP) were compared with lorazepam, prochlorperazine and dexamethasone (DLP) in a randomised, double-blind, crossover study. Both patient and observer assessments were documented in 84 patients receiving both cisplatin and non-cisplatin chemotherapy. The addition of dexamethasone significantly reduced the severity of nausea (P = 0.002) and vomiting (P less than 0.0001), duration of nausea (P = 0.01) and vomiting (P = 0.002) and the number of vomiting episodes (P = 0.003). DLP was the superior regimen in subsets of patients receiving cisplatin and the non-cisplatin chemotherapy. The improvements produced by the dexamethasone regimen were large and of major benefit to our patients. Patients documented significantly improved tolerance to chemotherapy with DLP courses (P = 0.0006). Overall, significantly more patients preferred DLP (P less than 0.0001). Patient assessments produced results similar to observer assessments but gave a broader understanding of their experience. The addition of dexamethasone to prochlorperazine and lorazepam significantly improved our patients' experience while receiving chemotherapy.

Adult↗
PubMed1984

Intravenous prochlorperazine for the rapid control of vomiting in the emergency department.

In this study, 40 patients whose active vomiting stemmed from various causes were given 2.5 mg of prochlorperazine by slow intravenous push. If no response was observed within 20 minutes, the dosage was repeated. Of 35 patients, 32 responded to doses of 2.5 to 5.0 mg. Three patients experienced no relief of vomiting while in the emergency department, after a total of 5 mg each, in divided doses. These three patients had received morphine sulphate for acute myocardial infarctions. The mean time to cessation of vomiting was 8.5 minutes, versus 35 minutes for a similar group receiving intramuscular prochlorperazine. This difference was statistically significant using analysis of variance (P less than .05). None experienced extrapyramidal reactions, or developed hypotension. We concluded that 2.5 mg of intravenous prochlorperazine given over one minute is an effective, safe treatment for the control of vomiting in the emergency department, until the etiology of the nausea and vomiting is determined and treated specifically. Further double-blind, controlled studies are warranted.

Adolescent↗
PubMed1996

Tardive dyskinesia as a result of long-term prochlorperazine use.

Prochlorperazine is a centrally acting dopamine receptor antagonist that is most commonly used for the treatment of nausea and vomiting. Like many dopamine antagonists, prochlorperazine has the ability to induce extrapyramidal reactions in susceptible patients. Rarely, however, have cases of tardive dyskinesia been caused by the long-term use of this agent. We report the case of a patient who used prochlorperazine for a prolonged period and, during hospital admission, was found to have a new movement disorder. Alternative antiemetics that do not pose a risk of movement disorders, such as ondansetron and granisetron, are readily available and are efficacious.

Antiemetics↗
PubMed1991

The effects of two anti-vertigo drugs (betahistine and prochlorperazine) on driving skills.

1. The effects of betahistine 72 mg three times daily, prochlorperazine 5 mg three times daily and placebo taken for 3 days before testing were compared on two actual driving tasks (weaving and gap estimation) and two psychomotor tasks (reaction time and kinetic visual acuity) in normal subjects in a double-blind prospectively randomised cross-over study. 2. The psychomotor effects of betahistine could not be distinguished from those of placebo. 3. Prochlorperazine impaired driving performance causing increased carelessness and slowing on the weaving test. 4. There was little subjective appreciation of impairment whilst taking prochlorperazine.

Adult↗
PubMed2005

The antipsychotic and antiemetic drug prochlorperazine delays the ventricular repolarization of the in situ canine heart.

Electropharmacological effect of the antipsychotic and antiemetic drug prochlorperazine was assessed using the halothane-anesthetized in vivo canine model (n = 5). Up to 10 times higher than the clinically relevant doses of prochlorperazine (< or = 3 mg/kg, i.v.) did not induce cardiohemodynamic collapse in the model. Meanwhile, clinically relevant to supratherapeutic doses (0.3 - 3 mg/kg, i.v.) prolonged the ventricular repolarization period in a dose-related and reverse-use dependent manner that could become proarrhythmic substrates. Thus, caution has to be paid on the use of prochlorperazine particularly for patients with risks of the elevated plasma drug concentration, compromised cardiac repolarization, and/or frequent ventricular premature beats.

Action Potentials↗
PubMed2001

Tolerability and effectiveness of prochlorperazine for intractable migraine in children.

OBJECTIVE: To study the effectiveness of prochlorperazine in aborting severe, intractable migraines in children. STUDY DESIGN: Patients for this study were drawn from the population seen and evaluated in the Headache Center at Cincinnati Children's Hospital Medical Center. All patients were diagnosed with migraine headache by both clinical and International Headache Society criteria. The effectiveness of intravenous prochlorperazine in 20 consecutive patients referred to the emergency department for severe, prolonged migraines was retrospectively reviewed. RESULTS: Patients evaluated in this study presented with a mean headache severity of 8.4 on a 0- to 10-point scale and an average duration of 54 hours. At 1 hour, 90% of the patients reported feeling better with 50% becoming pain-free. A 50% or greater reduction in severity occurred in 75% of patients at 1 hour and in 95% at 3 hours. At 3 hours, 95% of the patients reported feeling better, and 60% were pain-free. Only 1 patient failed to respond to prochlorperazine. CONCLUSION: Prochlorperzaine was shown to be highly effective in aborting intractable migraines in children. It was well tolerated with no significant side effects. Additional large, double-blinded, randomized, placebo-controlled studies are needed to further investigate its effectiveness.

Adolescent↗
PubMed1979

Delta-9-tetrahydrocannabinol as an antiemetic for patients receiving cancer chemotherapy. A comparison with prochlorperazine and a placebo.

The antiemetic activity and side-effects of delta-9-tetrahydrocannabinol (THC) were evaluated in 116 patients (median age 61 years) receiving combined 5-fluorouracil and semustine (methyl CCNU) therapy for gastrointestinal carcinoma. In a double-blind study, patients were randomized to receive THC, 15 mg orally three times a day, prochlorperazine, 10 mg orally three times a day, or placebo. The THC had superior antiemetic activity in comparison to placebo, but it showed no advantage over prochlorperazine. Central nervous system side-effects, however, were significantly more frequent and more severe with THC. With the dosage and schedule we used, and in our patient population of largely elderly adults, THC therapy resulted in an overall more unpleasant treatment experience than that noted with prochlorperazine or placebo. Although THC may have a role in preventing nausea and vomiting associated with cancer chemotherapy, this role must be more clearly defined before THC can be recommended for general use.

Adult↗
PubMedDate not supplied

Comparison of metoclopramide, prochlorperazine and placebo in prevention of postoperative nausea and vomiting (PONV) following tonsillectomy in young adults.

BACKGROUND: Postoperative nausea and vomiting following anaesthesia and surgery are common and can create considerable problems regarding management of patients and outcome of the surgical procedure. METHODS: This study evaluates and compares the efficacy and safety of the metochlopramide to that of prochlorperazine in the prevention of postoperative nausea and vomiting after tonsillectomy in young adult patients. 150 patients, of either sex, undergoing tonsillectomy under the same anaesthetic technique were studied in a randomized, double blind, placebo controlled manner. Either metoclopramide 0.1-0.2 mg kg(-1), prochlorperazine 0.1-0.2 mg kg(-1) or 5% Dextose and normal saline (5% D/N.S) (2ml) as placebo was injected intravenously 10 minutes before induction of general anaesthesia. Episodes of nausea, retching/vomiting, adverse events, vital signs, the need for rescue antiemetic drug (metoclopramide 0.1-0.2 mg kg(-1) IV) were recorded until four hours from the end of the surgical procedure. RESULTS: The overall frequency of PONV was 18%, 16%, and 24% in group A (metoclopramide), B (prochlorperazine) and C (placebo) respectively. The need for rescue antiemetic was 2%, 8% and 12% in Prochloperazine group, metoclopramide group and control group respectively. These differences did not reach statistical significance (P>0.05). During the study period 82%, 84% and 76% of patients in group A, B and C respectively were found free from postoperative nausea and vomiting, and no adverse events related to either of the test medication were noted in any patient. CONCLUSION: It is concluded that the differences in the results of occurrence of PONV in the experimental group and control group are not statistically significant. However either Prochloperazine 0.1 - 0.2 mg kg(-1) or metoclopramide 0.1 - 0.2 mg kg(-1) can be safely administered as Prophylactic antiemetic till the availability of more efficacious and safe antiemetic drugs.

Adolescent↗
PubMedDate not supplied

Buccal prochlorperazine as an antiemetic for day care surgery.

This study compares the antiemetic effect of prochlorperazine in a buccal preparation with a control group as a preoperatively administered antiemetic. Fifty-two female day care patients undergoing gynaecological surgery or breast biopsy were studied. Patients were randomly allocated to two groups. Patients in group one received no antiemetic, while those in group two received 6mg buccal prochlorperazine one hour before surgery. Nausea was assessed with a visual nausea scoring system and interview similar to those used in previous series. Assessment times were before surgery and at one, four and 24 hours after surgery. Patient demographics and type of surgery were similar for the groups. The incidence of postoperative nausea and vomiting for the groups one and two was 57.7% and 15.4% respectively, p < 0.05. Most of the patients who experienced nausea in group one and two (86.7% and 50%) gave it a score less than five, indicating mild nausea. The majority of patients did not require treatment for postoperative nausea. The postoperative antiemetic and narcotic requirements were similar in the two groups. This study demonstrates that prochlorperazine at the dose used is effective in preventing postoperative nausea in the patient population studied.

Administration, Oral↗
PubMed1979

Comparison of droperidol, haloperidol and prochlorperazine as postoperative anti-emetics.

The results of this study demonstrate that prochlorperazine, haloperidol and droperidol are all effective post-operative anti-emetic compounds when compared to saline but vary in onset of activity and duration of action. Haloperidol has the shortest onset of action, being effective within 30 minutes of intravenous administration. Prochlorperazine has an intermediate onset of action and droperidol is the slowest of the three compounds but the only one to provide significant anti-emesis 4-24 hours following administration. Our data suggest that a combination of haloperidol and droperidol may be more effective as an anti-emetic than any one of the compounds used alone.

Droperidol↗
PubMed1985

Attenuation of cyclophosphamide-induced taste aversions in mice by prochlorperazine, delta 9-tetrahydrocannabinol, nabilone and levonantradol.

A series of experiments were performed with adult CD-1 male mice to evaluate the antiemetic effects of several compounds using the conditioned taste aversion procedure. The antiemetics were administered IP immediately prior to a 30-min conditioning trial in which a novel tasting solution (0.3% saccharin) was presented to the subjects. The emetics, apomorphine and the cancer chemotherapeutic drug cyclophosphamide, were given IP immediately after the conditioning trial at doses that induced taste aversions. Three days later the mice received a two bottle preference test (saccharin vs. water) and the percent saccharin consumed of the total fluid intake was calculated. Doses of the phenothiazine antiemetic prochlorperazine (1 and 3 mg/kg) attenuated the aversions produced by 0.3 and 1.0 mg/kg apomorphine. Doses of drugs currently approved or under clinical investigation as antiemetics in conjunction with cancer chemotherapy, i.e., prochlorperazine (1.0 mg/kg), delta 9-tetrahydrocannabinol (0.3 and 1.0 mg/kg) and nabilone (0.01 and 0.03 mg/kg), significantly attenuated the taste aversions induced by cyclophosphamide. Levonantradol at doses of 0.03 and 0.06 mg/kg, however, did not attenuate cyclophosphamide-induced taste aversions. Conditioned taste aversions produced by emetic drugs warrants investigation as a model for evaluating potential antiemetics.

Animals↗
PubMed1987

Intravenous prochlorperazine for the rapid control of nausea and vomiting in acute myocardial infarction: a clinical observation.

Sixteen patients with acute myocardial infarctions who were either vomiting or nauseated were given an intravenous injection of prochlorperazine. All patients obtained relief with exception of one patient who was in acute renal failure. No patient developed symptomatic hypotension. Intravenous prochlorperazine in the dose of 2.5 mg is a rapid, effective, and safe method to relieve vomiting and nausea in patients who have sustained an acute myocardial infarction.

Aged↗
PubMed2004

Diphenhydramine in the treatment of akathisia induced by prochlorperazine.

Dopamine D(2) antagonists are known to induce akathisia, the emergency management of which remains undetermined. We sought to evaluate the effectiveness of diphenhydramine in the treatment of akathisia induced by 10 mg intravenous prochlorperazine. This prospective, open-label, uncontrolled study evaluated a cohort of akathisic adult Emergency Department patients who were participating in a series of three studies of acute akathisia at an academic medical center. Each subject received intravenous diphenhydramine, with akathisia measurements (graded from 0-17 points) performed just before and 30 min after infusion. Mean scores were calculated using descriptive statistical analyses. The effect of treatment was evaluated using the paired t-test. For the 87 akathisic patients, the mean score before treatment was 9.8 +/- 3.6, and after treatment was 1.2 +/- 2.6, a mean reduction of 8.5 +/- 3.8 (95% confidence interval [CI], 7.8 to 9.4; p < 0.0001). In conclusion, intravenous diphenhydramine rapidly reduces signs and symptoms of acute akathisia induced by prochlorperazine.

Adolescent↗