Prochlorperazine — A Review of the Literature since 1956<sup>*</sup>

Lapierre, Jean; Amin, Mansour; Hattangadi, Sunder

doi:10.1177/070674376901400307

Cited by 8 publications

(2 citation statements)

References 57 publications

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“…However, recent literature found conflicting results as a single therapeutic approach, with either an efficacy similar to that of NSAIDs [ 90 ], or no difference of intravenous metoclopramide compared to saline [ 91 ]. Prochlorperazine is a phenothiazine antipsychotic with antagonizing effect of dopamine D 2 receptors, similar to chlorpromazine [ 87 , 92 ] and might be the most effective intravenous antiemetic, which also has a higher risk of extrapyramidal adverse events [ 93 ]. Chlorpromazine is also an effective option to consider for the treatment of nausea in emergency settings [ 94 ].…”

Section: Nausea and Vomitingmentioning

confidence: 99%

Pathophysiology and Therapy of Associated Features of Migraine

Villar-Martínez

Goadsby

2022

Cells

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Migraine is a complex and debilitating disorder that is broadly recognised by its characteristic headache. However, given the wide array of clinical presentations in migraineurs, the headache might not represent the main troublesome symptom and it can even go unnoticed. Understanding migraines exclusively as a pain process is simplistic and certainly hinders management. We describe the mechanisms behind some of the most disabling associated symptoms of migraine, including the relationship between the central and peripheral processes that take part in nausea, osmophobia, phonophobia, vertigo and allodynia. The rationale for the efficacy of the current therapeutic arsenal is also depicted in this article. The associated symptoms to migraine, apart from the painful component, are frequent, under-recognised and can be more deleterious than the headache itself. The clinical anamnesis of a headache patient should enquire about the associated symptoms, and treatment should be considered and individualised. Acknowledging the associated symptoms as a fundamental part of migraine has permitted a deeper and more coherent comprehension of the pathophysiology of migraine.

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Section: Nausea and Vomitingmentioning

confidence: 99%

Pathophysiology and Therapy of Associated Features of Migraine

Villar-Martínez

Goadsby

2022

Cells

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“…Prochlorperazine [2-chloro-10-(3-(1-methyl-piperazinyl) propyl) phenothiazine] (PCZ) was introduced into medical practice in 1956 and is widely used in the prevention and symptomatic control of nausea, vomiting, vestibular and psychiatric disorders (Lapierre et al, 1969). Despite its use for more than three decades, very little is known of its human pharmacology, since early studies in the pre-regulatory era were principally designed to establish efficacy.…”

Section: Introductionmentioning

confidence: 99%

Clinical pharmacology of prochlorperazine in healthy young males.

Isah,

Rawlins,

Bateman

1991

Brit J Clinical Pharma

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1. The pharmacokinetics and pharmacodynamics of prochlorperazine (PCZ) have been studied in healthy young males following single 12.5 mg i.v. and 50 mg oral doses, and during repeated doses (25 mg twice daily) for 14 days. 2. Oral bioavailability was low and an N‐desmethyl metabolite was detected. Plasma clearance was high (0.98 1 kg‐1 h) and the volume of distribution was large (12.9 1 kg‐1) after i.v. dosing. 3. The terminal elimination half‐life of PCZ was 9 +/‐ 1 h and 8 +/‐ 2 h after i.v. and single oral dosing, respectively. The urinary recoveries of drug and metabolite were low. 4. Accumulation of PCZ and its metabolite occurred following repeated dosing. The half‐life at the end of 14 days therapy was 18 +/‐ 4 h. 5. Postural tachycardia, decreased salivary flow, impaired psychomotor function and a diminished level of arousal were observed after intravenous PCZ. Similar effects, but of lower magnitude were observed after single oral doses. During chronic dosing postural tachycardia and antihistaminic effects were observed, the latter not being observed after single doses. 6. After single intravenous dosing the maximal drug effects occurred 2‐4 h after peak plasma drug concentrations for all measures except for plasma prolactin and self‐scored restlessness 7. An antagonist action at dopamine (D2), muscarinic‐cholinergic and alpha‐adrenoceptors is postulated after single doses, with antihistaminic effects during chronic dosing, possibly indicating the presence of an active metabolite.

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

Carr

Blayney

Goldberg

et al. 1987

Cancer

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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.

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Prochlorperazine — A Review of the Literature since 1956^*

Abstract: The pertinent literature on prochlorperazine has been reviewed. Prochlorperazine appears to be a useful drug in maintaining psychiatric patients in the community, following discharge from the mental hospital.

Cited by 8 publications

References 57 publications

Pathophysiology and Therapy of Associated Features of Migraine

Pathophysiology and Therapy of Associated Features of Migraine

Clinical pharmacology of prochlorperazine in healthy young males.

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

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Prochlorperazine — A Review of the Literature since 1956*

Abstract: The pertinent literature on prochlorperazine has been reviewed. Prochlorperazine appears to be a useful drug in maintaining psychiatric patients in the community, following discharge from the mental hospital.

Cited by 8 publications

References 57 publications

Pathophysiology and Therapy of Associated Features of Migraine

Pathophysiology and Therapy of Associated Features of Migraine

Clinical pharmacology of prochlorperazine in healthy young males.

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

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Prochlorperazine — A Review of the Literature since 1956^*