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At least 19 recordsLinked to original sources

PubMed1992

A randomised double-blind study of high-dose intravenous prochlorperazine versus high-dose metoclopramide as antiemetics for cancer chemotherapy.

High-dose prochlorperazine 0.8 mg/kg administered intravenously 30 min pre and 7 h 30 min post the initial dose of emetogenic chemotherapy was compared to high-dose metoclopramide 2 mg/kg over 20 min every 2 h for five doses starting 30 min prior to chemotherapy in a randomised, double-blind, parallel subjects design study. On the prochlorperazine arm intravenous dextrose placebos every 2 h maintained blinding. Complete suppression of vomiting occurred in 42% on metoclopramide (53% with non-cisplatin regimens) and 36% on prochlorperazine (52% with non-cisplatin-containing regimens) while major responses (2 or less vomits) occurred in 58% on metoclopramide and 54% on prochlorperazine. In patients who vomited after cisplatin, prochlorperazine achieved a significantly shorter duration of vomiting, a median of 5 h compared to 15 h on metoclopramide (P = 0.03). The response rate to prochlorperazine for cisplatin-induced emesis between 12 and 24 h was significantly better than for metoclopramide (prochlorperazine = 0.02). Toxicities were equivalent except for significantly greater sedation and dry mouth on prochlorperazine. Extrapyramidal reactions were recorded equally on both arms but were only severe enough to stop treatment on metoclopramide. The metoclopramide regimen was five times as expensive as prochlorperazine. High-dose prochlorperazine is an active and cost-effective antiemetic.

Adolescent↗

PubMed1988

Effects of prochlorperazine on the function of integral membrane proteins.

We have studied the effects of prochlorperazine on the activities of UDP-glucuronosyltransferase and glucose-6-phosphatase (glucose-6-P'ase) in rat liver microsomes. The activity of UDP-glucuronosyltransferase was increased in a graded fashion by addition of prochlorperazine. Maximal stimulation occurred at 1 mg prochlorperazine to 2 mg microsomal protein, which resulted in a 6-fold increase in activity. However, with smaller concentrations of drug, there was a time-dependent increase in the activity of UDP-glucuronosyltransferase. Sensitivity of UDP-glucuronosyltransferase to activation by UDP-N-acetylglucosamine was lost after treatment of microsomes with prochlorperazine. These results indicate that prochlorperazine causes a profound reorganization of the interactions between lipids and enzyme since the activity and allosteric properties of UDP-glucuronosyltransferase are known to depend on interactions with lipids in a gel phase. Glucose-6-P'ase also was activated in a graded fashion by prochlorperazine; 1 mg of drug/2 mg microsomal protein resulted in a 60% increase in activity. The temperature-dependent instability of glucose-6-P'ase was increased by treatment of microsomes with prochlorperazine and could be prevented only partially by substrate. We conclude that prochlorperazine disrupts the structural organization between lipids and proteins in microsomal membranes, altering thereby the activity and regulation of at least two different integral membrane proteins.

Animals↗

PubMed1987

Preliminary studies of the pharmacokinetics and pharmacodynamics of prochlorperazine in healthy volunteers.

The pharmacokinetics and pharmacodynamics of prochlorperazine were studied in healthy volunteers using a recently developed h.p.l.c. assay. Eight subjects received 12.5 mg and 6.25 mg i.v. doses of prochlorperazine, a 25 mg oral dose and placebo in random order. Plasma half-life (t1/2) of prochlorperazine was 6.8 +/- 0.7 h and 6.9 +/- 0.8 h for the 12.5 mg and 6.25 mg i.v. doses respectively. Apparent volume of distribution and plasma clearance were high and the kinetics did not appear to be dose-related. Absorption of oral prochlorperazine appeared to be slow and bioavailability was very low. A metabolite, possibly prochlorperazine sulphoxide, was noted after oral dosing. Mild sedation was common after i.v. prochlorperazine, but cardiovascular effects were minimal. The main adverse effect was akathisia which was reported by five out of eight subjects after the higher i.v. dose. These results provide preliminary information on the pharmacokinetics of i.v. prochlorperazine which were previously unknown.

Administration, Oral↗

PubMed1992

Pharmacokinetics and safety of prochlorperazine in paediatric patients receiving cancer chemotherapy.

Nausea and vomiting are common clinical problems in patients receiving cancer chemotherapy. Metoclopramide is often used but frequently causes extrapyramidal reactions. As an alternative, prochlorperazine is prescribed but no data on its pharmacokinetics in paediatric patients are available to guide the choice of suitable dosages. The primary objective of this study was to evaluate the pharmacokinetics and safety of intravenous prochlorperazine in paediatric patients receiving cancer chemotherapy. Eleven patients (ages 1-9 years) who received high doses of cisplatin or cyclophosphamide were given three to four intermittent doses of 0.2 mg/kg prochlorperazine i.v. over a period of 6-9 h. Multiple blood samples were collected and prochlorperazine was quantified by a specific gas-liquid chromatographic method. The peak serum concentrations ranged from 402 to 5,608 ng/ml. The total clearance and elimination half-life ranged from 0.03 to 0.28 (mean: 0.12) litre/kg/h, and from 1.2 to 15.5 (mean: 5.6) h, respectively. No adverse effects were observed in our patients. Three patients had uncontrolled episodes of vomiting during prochlorperazine therapy. These data suggest: (i) that there was a substantial interpatient variability in prochlorperazine pharmacokinetics thus the dose requirement differed among patients; and (ii) that prochlorperazine appeared safe at the doses used but higher doses may be required to control nausea and vomiting in some paediatric patients receiving high-dose cisplatin or cyclophosphamide therapy.

Adolescent↗

PubMed1987

High doses of prochlorperazine for cisplatin-induced emesis. A prospective, random, dose-response study.

This study investigated the antiemetic properties of four different doses of prochlorperazine (10 mg, 20 mg, 30 mg, 40 mg) when given randomly to patients receiving four cycles of the same dose of cisplatin-based chemotherapy. Prochlorperazine was given to 71 patients by slow intravenous infusion 30 minutes before and 3 and 6 hours after the start of cisplatin chemotherapy. The higher doses of prochlorperazine proved to be effective in the control of cisplatin-induced emesis. For the 20 patients who completed all 4 study cycles of treatment, a relationship was discerned between the dose of prochlorperazine administered and the antiemetic effect. When all 71 patients were analyzed in terms of the results of the first cycle of chemotherapy, a significant dose-response effect was also found. Overall toxic reactions in 82 treatment cycles using either 30 mg or 40 mg of prochlorperazine were dystonia (1 patient), restlessness (2), hypotension (3), and drowsiness (12). This study demonstrates that higher-than-conventional doses of prochlorperazine have an impressive antinauseant effect with only moderate toxicity.

Adult↗

PubMed1986

The effects of combined morphine and prochlorperazine on ventilatory control in humans.

Recent studies have shown that the antiemetic neuroleptic drug, prochlorperazine, is a potent stimulant of the ventilatory response to hypoxia. To investigate whether or not this effect persisted in the presence of central depression of ventilatory drive, the effects on ventilatory control of morphine with and without prochlorperazine were studied in 12 normal humans. Measurement of resting ventilation and the ventilatory responses to progressive hypercapnia and to transient asphyxia were made before and 15 min after morphine (0.15 mg/kg) given intravenously. Prochlorperazine (12.5 mg) was then administered intravenously to 6 study subjects and saline to 6 control subjects. After a further 10 min, resting ventilation and chemoreceptor function were remeasured. After the administration of morphine, resting ventilation, the ventilatory response to hypercapnia, and the ventilatory response to asphyxia were all significantly decreased (p less than 0.01 in each case; mean effect in control and study group were, respectively, -16 and -17%, -50 and -32%, -46 and -55%). Administration of saline produced no significant additional changes in the 6 control subjects. By contrast, administration of prochlorperazine to the 6 study subjects markedly increased the ventilatory response to asphyxia to levels significantly greater than postmorphine values (p less than 0.005; 2.38 +/- 0.22 L . min-1 . % Sao2 versus 0.80 +/- 0.14 L . min-1; mean +/- SEM). Resting ventilation and ventilatory response to hypercapnia were not significantly affected by prochlorperazine. These results were not explained by differences in end-tidal PCO2 at which hypercapnic hypoxic tests were performed. It is concluded that prochlorperazine reverses the depression of the ventilatory response to asphyxia caused by morphine.

Adult↗

PubMed1985

A comparison of the antiemetic efficacy of prochlorperazine and metoclopramide for the treatment of cisplatin-induced emesis: a prospective, randomized, double-blind study.

This study compared high-dose metoclopramide and prochlorperazine for their antiemetic activities in the treatment of patients with solid tumors receiving cisplatin-based cancer chemotherapy, in a prospective, double-blind fashion. Sixty patients were entered in the study, and 28 patients on each regimen were evaluable. For regimen 1, metoclopramide was given intravenously (IV) over 15 minutes at a dose of 2 mg/kg 30 minutes before, 30 minutes after, and three hours after treatment with cisplatin. In regimen 2, prochlorperazine was given IV 30 minutes before and three hours after the cisplatin; a placebo was administered at 30 minutes after cisplatin. There was no statistically significant difference between the two regimens in their antiemetic efficacies during the first three hours. For emesis that occurred from three to 24 hours after administration of cisplatin, prochlorperazine was marginally superior. The median number of emeses in the metoclopramide regimen was 2.5 (range, 0 to 10+) compared to 1.0 (range, 0 to 10+) in the prochlorperazine regimen. This is not a significant difference. The overall incidence of adverse reactions was greater in the metoclopramide regimen, with drowsiness being the most common toxicity for both antiemetic programs. Thus, IV high-dose metoclopramide and prochlorperazine are similar and effective in the management of cisplatin-induced emesis. IV prochlorperazine at 20-mg dosage is surprisingly effective.

Adolescent↗

PubMed1988

A randomized trial of oral nabilone and prochlorperazine compared to intravenous metoclopramide and dexamethasone in the treatment of nausea and vomiting induced by chemotherapy regimens containing cisplatin or cisplatin analogues.

Eighty patients receiving their first course of chemotherapy with regimens containing cisplatin or cisplatin analogues entered this open crossover study comparing nabilone 2 mg and prochlorperazine 5 mg given orally every 12 h for four doses against metoclopramide 2 mg/kg loading dose intravenously (i.v.), then 3 mg/kg as an (i.v.) infusion over 8 h and dexamethasone 20 mg (i.v.) over 3-5 min at the time of chemotherapy. There was complete control of nausea and vomiting in 24 patients (32%) given metoclopramide and dexamethasone compared to 14 patients (19%) given nabilone and prochlorperazine. For the 70 patients who completed the crossover assessment of emesis on a linear analogue scale significantly favoured metoclopramide and dexamethasone (P = 0.02). However, there was no overall patient preference for the metoclopramide and dexamethasone combination (nabilone and prochlorperazine 31 vs. metoclopramide and dexamethasone 26; 13 no preference), because a significant proportion of the patients receiving the cisplatin analogue carboplatin preferred nabilone and prochlorperazine (16 vs. 5; 1 no preference; P = 0.013). For patients receiving cisplatin chemotherapy metoclopramide and dexamethasone remains the antiemetic of choice but for regimens containing carboplatin, nabilone and prochlorperazine is better tolerated and preferred by the patients.

Adolescent↗

PubMed1985

A cross-over comparison of nabilone and prochlorperazine for emesis induced by cancer chemotherapy.

An anti-emetic drug, nabilone, a synthetic cannabinoid, has been compared with prochlorperazine in 24 lung cancer patients receiving cancer chemotherapy. Each of the drugs studied was given orally every 12 hours, starting the night before chemotherapy, during one of two consecutive identical chemotherapy cycles in accordance with a double-blind cross-over random order assignment. Single doses were 2 mg of nabilone, or 15 mg of prochlorperazine. The chemotherapeutic regimens given included the following drugs in various combinations: cis-platinum, vincristine, cyclophosphamide, adriamycin, vindesine, and etoposide (VP16). Nabilone was significantly superior to prochlorperazine in the reduction of vomiting episodes. Side effects, mainly vertigo, were evident in nearly half of the patients after nabilone, and three patients were withdrawn from the study due to decreased coordination and hallucinations after nabilone. Side effects from prochlorperazine were limited to mild drowsiness in one patient. Two-thirds of the patients preferred nabilone to prochlorperazine. We conclude that nabilone is a moderately effective anti-emetic drug, but that the unpredictability of its side effects call for careful patient information, especially with elderly outpatients. We recommend that at least after the first dose of nabilone, the patient should be kept under close observation during 4 hours.

Administration, Oral↗

PubMed1990

Dronabinol and prochlorperazine alone and in combination as antiemetic agents for cancer chemotherapy.

Nineteen patients receiving cancer chemotherapy were randomized in a double-blind fashion to receive either (a) dronabinol, 10 mg plus placebo q.i.d.; (b) prochlorperazine, 10 mg plus placebo q.i.d.; or (c) dronabinol plus prochlorperazine, each 10 mg q.i.d. There were six evaluable patients in each of the two single-agent groups and five in the combination group. The median duration and severity per episode of nausea was significantly greater in the group receiving prochlorperazine alone versus the other two groups. The median duration per episode of vomiting was also significantly greater in the prochlorperazine group than in the other two groups. The proportion of patients vomiting was the same in all groups; however, only one patient in the combination group versus three each in the single-agent groups experienced nausea (p = NS). The majority of side effects were associated with the CNS, including somnolence, dizziness, and confusion. Side effects were somewhat more common in both groups receiving dronabinol, though they were not statistically different from the side effects in the group receiving prochlorperazine as a single agent. Efficacy, as measured by duration of nausea and vomiting and by severity of nausea, was significantly greater in both groups receiving dronabinol.

Adult↗

PubMed1992

Abortive headache therapy in the office with intravenous dihydroergotamine plus prochlorperazine.

Over two years, 92 patients were treated in the office for 146 severe headache episodes. Headaches were aborted using four different intravenous regimens containing 0.5 or 1 mg. of dihydroergotamine and 3.5, 5, or 10 mg. of prochlorperazine. The speed and rate of response were directly proportional to the prochlorperazine dose used. High prochlorperazine doses (10 mg.) aborted the most headaches (95%) in the shortest time, but caused more sedation and akathesia. Low doses (3.5 mg.) aborted less headaches (89%) and responses were delayed; but, on the other hand, sedation was minimal and akathesia mild and uncommon. Dihydroergotamine given alone caused intolerable side effects; but, when it was given with prochlorperazine, efficacy was enhanced and side effects were greatly reduced. Aborting headaches in the office can be reliably achieved with minimal side effects by administering an intravenous mixture containing 1 mg. of dihydroergotamine and 3.5 mg. of prochlorperazine.

Adolescent↗

PubMed1989

A dose finding study of prochlorperazine as an antiemetic for cancer chemotherapy.

This phase I study determined the maximum tolerated dose of prochlorperazine when used as an antiemetic prior to cytotoxic chemotherapy. Initially, cohorts of three patients were given prochlorperazine at escalating doses of 0.2, 0.4, 0.6, 0.8, 1.0 and 1.2 mg/kg as an intravenous infusion over 20 min. The maximum tolerated dose was 1.2 mg/kg. The dose-limiting toxicity was hypotension which was reversed by a fluid load. The other major toxicities were extrapyramidal reactions which were dose related. All patients at the 1.2 mg/kg dose reported restlessness while five of six were restless and two of six at 1.0 mg/kg had muscle spasms. Two of seven patients reported restlessness at the 0.8 mg/kg level. Sedation and dry mouth were reported at all dose levels but were more common at higher doses. Prochlorperazine in plasma was assayed by high performance liquid chromatography with electrochemical detection and pharmacokinetics were determined for three patients at the 1.0 mg/kg dose level. The average terminal elimination half life was 7.6 +/- 0.4 h, plasma clearance 27 +/- 5 ml/min/kg and volume of distribution 17.7 +/- 4.5 l/kg. The dose of prochlorperazine recommended for further studies of antiemetic efficacy is 0.8 mg/kg intravenously.

Antiemetics↗

PubMed1991

Dronabinol and prochlorperazine in combination for treatment of cancer chemotherapy-induced nausea and vomiting.

Dronabinol (Marinol, Roxane Laboratories, Columbus, OH) and prochlorperazine were tested alone and in combination in a randomized, double-blind, parallel group, multicenter study. Patients were randomized to receive either 1) dronabinol 10 mg every 6 hr plus placebo; 2) placebo plus prochlorperazine 10 mg every 6 hr; or 3) dronabinol and prochlorperazine, each 10 mg every 6 hr. Antiemetic treatment was begun 24 hr prior to and continued for 24 hr after the last dose of chemotherapy; all was given orally. Only 29% of patients in group 3 versus 47% in group 1 and 60% in group 2 experienced nausea after chemotherapy. In addition, the median duration per episode and severity of nausea were significantly less with combination therapy. Vomiting occurred after chemotherapy in 41%, 55%, and 35% of patients in groups 1, 2, and 3, respectively. The median duration per episode of vomiting was 1 min in group 3 versus two in group 1 and four in group 2. Side effects, primarily CNS, were more common in group 1 than in group 2; addition of prochlorperazine to dronabinol appeared to decrease the frequency of dysphoric effects seen with the latter agent. The combination was significantly more effective than was either single agent in controlling chemotherapy-induced nausea and vomiting.

Adult↗

PubMed1986

Effects of somatostatin, naloxone and prochlorperazine on the control of ventilation in man.

In seven normal subjects the ventilatory responses to progressive isocapnic hypoxia and hyperoxic hypercapnia were measured during rebreathing. During an infusion of somatostatin (10 nmol/min) the mean hypoxic response decreased by 66% (control: -1.6 SD 1.2 litres min-1 %-1 SaO2; somatostatin: -0.6 SD 0.7) but the mean hypercapnic response was unchanged (control: 2.0 SD 0.8 litre min-1 mmHg-1; somatostatin: 2.3 SD 1.2). There was no change in resting VO2 or VCO2 during somatostatin infusion. The opiate antagonist, naloxone (0.1 mg/kg, intravenously), caused little change in either response (mean hypoxic response: -1.7 SD 1.0 litre min-1 %-1 SaO2; mean hypercapnic response: 2.4 SD 0.9 litre min-1 mmHg-1). In five of the subjects the dopamine antagonist, prochlorperazine (10 mg, intravenously), increased the mean hypoxic response by 134% (control: -1.9 SD 1.4 litres min-1 %-1 SaO2; after prochlorperazine: -3.8 SD 1.6; P less than 0.05). The mean hypercapnic response after this drug was also increased (control: 2.1 SD 1.0 litre min-1 mmHg-1; after prochlorperazine: 3.1 SD 1.0) but this change did not achieve significance. The selective effect of somatostatin on the hypoxic response, suggestive of an action on the carotid body, was not inhibited by prior injection of either naloxone or prochlorperazine, and its mode of action remains to be found.

Adult↗

PubMed1987

Comparative effects of intravenously administered alizapride and prochlorperazine in cisplatin-induced emesis.

A randomized, double blind crossover trial compared the antiemetic effects of alizapride, a benzamide, and prochlorperazine, a phenothiazine, both administered intravenously to 32 patients treated with chemotherapy combinations containing cisplatin. The total dose of alizapride administered to each patient was 14 mg/kg, and of prochlorperazine .56 mg/kg, divided in five doses. Although alizapride resulted in complete protection against emesis in 31% of the patients during their first course of cisplatin therapy, 42% of those who received alizapride had five or more episodes of emesis. Although prochlorperazine was less effective in offering complete protection against emesis, only 15% of the patients receiving this drug vomited more than five times. The duration of emesis during prochlorperazine treatment was also significantly shorter than during alizapride therapy (p less than 0.02). Optimal dosage and pharmacokinetic distribution of both drugs should be investigated further.

Adult↗

PubMed1989

Randomized double-blind trial of intravenous prochlorperazine for the treatment of acute headache.

In a prospective, randomized, double-blind clinical trial, intravenous prochlorperazine edisylate (Compazine Edisylate) was compared with a placebo in the treatment of severe headaches. Eighty-two adult patients with vascular or tension-type headaches were identified at the time of presentation to one of three participating emergency departments. After the patient gave informed consent, a 2-mL intravenous injection of sterile saline solution or prochlorperazine edisylate (10 mg) was given to each patient at the time of randomization. The treatment groups were similar with regard to age, sex, and type and duration of headache. Within 60 minutes after injection, 74% (31/42) of those who received prochlorperazine had complete relief; 14% (6/42) of the patients had partial relief. Overall, there was complete or partial relief of pain in 88% (37/42) of the drug group and in 45% (18/40) of the placebo group. This difference was statistically significant using chi 2 analysis. Adverse effects were minimal; one patient experienced asymptomatic orthostatic hypotension. These results suggest that intravenous prochlorperazine is an effective treatment for patients with severe vascular or tension headaches who present to the emergency department.

Acute Disease↗

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↗