Delving into the Latest Updates on Prochlorperazine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

2-Chloro-10-(3-(1-methyl-4-piperazinyl)propyl)-phenothiazine, 2-Chloro-10-(3-(4-methyl-1-piperazinyl)propyl)phenothiazine, 3-Chloro-10-(3-(1-methyl-4-piperazinyl)propyl)phenothiazine

+ [11]

Target

D2 receptor

Mechanism

D2 receptor antagonists(Dopamine D2 receptor antagonists)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Schizophrenia

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

GlaxoSmithKline, Inc.

Drug Highest PhaseWithdrawn

First Approval Date

US (26 Jan 1959),

Schizophrenia

Regulation-

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Structure

Molecular FormulaC20H24ClN3S

InChIKeyWIKYUJGCLQQFNW-UHFFFAOYSA-N

CAS Registry58-38-8

The purpose of this study is to determine if intranasal (IN) Ketorolac in combination with oral Prochlorperazine and Diphenhydramine is non-inferior to current migraine management which involves use of intravenous (IV) Ketorolac and oral adjuncts Prochlorperazine and diphenhydramine for reducing pain intensity in children with migraine headaches.
The investigators hypothesize that IN ketorolac combined with these oral adjuncts is non-inferior to IV ketorolac and oral adjuncts in reducing acute migraine headache pain by a minimum clinically significant difference within 60 minutes of administration.

Start Date01 Jan 2024

Sponsor / Collaborator

Washington University School of Medicine

[+1]

NCT05013437 / WithdrawnEarly Phase 1IIT

A Pilot Study to Assess Impact of Low Dose Melphalan on Disease Burden Measured by Next Generation Sequencing Before Autologous Hematopoietic Cell Transplant (AHCT) for Multiple Myeloma Patients

The purpose of this study is to see if Multiple Myeloma (MM) cells are sensitive to the chemotherapy used in transplant or not. The main chemotherapy agent utilized in stem cell transplant is melphalan. The study will utilize 1/10 of the dose used in transplant to study sensitivity of the tumor to melphalan. Melphalan is approved by the U.S. Food and Drug Administration (FDA) for transplant for MM patients.

Start Date01 Sep 2023

Sponsor / Collaborator-

CTRI/2023/06/054170 / Not yet recruitingPhase 2

Effectiveness of BioMin, NovaMin, Syzygium aromaticum, Strontium chloride hexahydrate & Potassium nitrate in hypersensitivity treatment: A Randomized Controlled Trial

Start Date30 Jun 2023

Sponsor / Collaborator

Institute of Crop Sciences

100 Clinical Results associated with Prochlorperazine

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100 Translational Medicine associated with Prochlorperazine

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100 Patents (Medical) associated with Prochlorperazine

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1,037

Literatures (Medical) associated with Prochlorperazine

01 Apr 2024·Biomaterials advances

Optimizing the fabrication of electrospun nanofibers of prochlorperazine for enhanced dissolution and permeation properties

Article

Author: Shafi, Hasham ; Jvus, Chakradhar ; Roy, Trisha ; Kawoosa, Shabnam ; Beigh, Mushtaq A ; Reddy, D V Siva ; Rashid, Rumaisa ; Bader, G N ; Sheikh, Faheem A ; Majeed, Shafquat ; Abdal-Hay, Abdalla ; Khan, Nisar Ahmad

Despite being an approved antiemetic for more than five decades, the clinical usefulness of prochlorperazine is limited by its low solubility and inconsistent absorption in the gastrointestinal tract, which presents challenges for nanotherapeutic interventions. Here, we report the preparation of a highly soluble and permeable nanofiber formulation of prochlorperazine using the Quality-by-Design approach. The final nanofiber formulation with drug entrapment of 88.02 ± 1.14 % was obtained at 20.0 kV, with a flow rate of 0.5 ml/h and tip-to-collector distance of 19.9 cm. Physio-mechanical properties, such as thickness (0.42 ± 0.02 mm), pH resistance (7.04 ± 0.08), folding endurance (54 ± 5), and tensile strength (0.244 ± 0.02 N.mm^-2), were appropriate for packaging and application to oromucosal surfaces. The content uniformity (93.48-106.63 %) and weight variation (<1.8 mg) of the optimal nanofiber formulation were within the permissible limits prescribed for orodispersible films. Microscopical investigations confirm a randomly deposited and dense network of woven nanofibers with an average diameter of 363 ± 5.66 nm. The drug particles were embedded homogeneously on the fiber in the nanoform (4.27 ± 1.34 nm). The spectral analysis using TEM-EDS shows diffraction peaks of sulfur and chlorine, the elemental constituents of prochlorperazine. The drug was amorphized in the nanofiber formulation, as led by the decline of the crystallinity index from 87.25 % to 7.93 % due to electrostatic destabilization and flash evaporation of the solvent. The enthalpy of fusion values of the drug in the nanofiber mat decreased significantly to 23.6 J/g compared to its pristine form, which exhibits a value of 260.7 J/g. The nanofibers were biocompatible with oral mucosal cells, and there were no signs of mucosal irritation compared to 1 % sodium lauryl sulfate. The fiber mats rapidly disintegrated within <1 s and released ≈91.49 ± 2.1 % of the drug within 2 min, almost 2-fold compared to the commercial Stemetil MD® tablets. Similarly, the cumulative amount of the drug permeated across the unit area of the oromucosal membrane was remarkably high (31.28 ± 1.30 μg) compared to 10.17 ± 1.11 μg and 13.10 ± 1.79 μg from the cast film and drug suspension. Our results revealed these nanofiber formulations have the potential to be fast-dissolving oromucosal delivery systems, which can result in enhanced bioavailability with an early onset of action due to rapid disintegration, dissolution, and permeation.

01 Feb 2024·Nanomedicine : nanotechnology, biology, and medicine

A PEGylated liposomal formulation of prochlorperazine that limits brain exposure but retains dynamin II activity: A potential adjuvant therapy for cancer patients receiving chemotherapeutic mAbs

Article

Author: Kaminskas, Lisa M ; Simpson, Fiona ; Minchin, Rodney F ; Subasic, Christopher N

Anti-cancer monoclonal antibodies often fail to provide therapeutic benefit in receptor-positive patients due to rapid endocytosis of antibody-bound cell surface receptors. High dose co-administration of prochlorperazine (PCZ) inhibits endocytosis and sensitises tumours to mAbs by inhibiting dynamin II but can also introduce neurological side effects. We examined the potential to use PEGylated liposomal formulations of PCZ (LPCZ) to retain the anti-cancer effects of PCZ, but limit brain uptake. Uncharged liposomes showed complete drug encapsulation and pH-dependent drug release, but cationic liposomes showed limited drug encapsulation and lacked pH-dependent drug release. Uncharged LPCZ showed comparable inhibition of EGFR internalisation to free PCZ in KJD cells. After IV administration to rats, LPCZ reduced the plasma clearance and brain uptake of PCZ compared to IV PCZ. The results suggest that LPCZ may offer some benefit over PCZ as an adjunct therapy in cancer patients receiving mAb treatment.

01 Jan 2024·Handbook of clinical neurology

Nonspecific analgesics, combination analgesics, and antiemetics

Review

Author: Pocora, Maria Magdalena ; Tassorelli, Cristina ; Martinelli, Daniele

The acute treatment of migraine attacks should provide rapid, effective, and long-lasting symptom relief, causing minimal adverse effects. For this purpose, there are several specific and nonspecific acute treatments. In this chapter, we focus on molecules not specifically designed for migraines, including anti-inflammatory not specific analgesics, such as acetaminophen, acetylsalicylic acid, and other non-steroidal anti-inflammatory drugs (or COX-2 inhibitors); antinausea medications like metoclopramide or prochlorperazine, which can alleviate sickness and vomiting associated with migraines, and may also have a direct painkiller effect; combinations of simple analgesics or association of a painkiller with caffeine. This stimulant can help enhance the pain-relieving effects of some headache medications and provide its own analgesic effect; physical approaches: applying cold packs or heating pads on the forehead or neck, can help relieve migraine pain; other classes with limited to no evidence to support their use, such as intravenous corticosteroids or antiepileptic drugs as sodium valproate. Finally, we will briefly mention opioids, barbiturates, or medical cannabis, bearing in mind that their use is not recommended by current guidelines.

18

News (Medical) associated with Prochlorperazine

26 Jun 2024

·www.biospace.com

Avenacy Announces Launch of Prochlorperazine Edisylate Injection, USP in the U.S. Market

Represents the Company’s eleventh product launch since inception in October 2023 SCHAUMBURG, Ill.--(BUSINESS WIRE)-- Avenacy, a specialty pharmaceutical company focused on supplying critical injectable medications, today announced it has launched Prochlorperazine Edisylate Injection, USP in the United States as a therapeutic generic equivalent for COMPAZINE® as approved by the U.S. Food and Drug Administration. Prochlorperazine Edisylate Injection, USP is indicated to control severe nausea and vomiting and for the treatment of schizophrenia. Prochlorperazine has not been shown effective in the management of behavioral complications in patients with mental retardation. This press release features multimedia. View the full release here: (Photo: Business Wire) Avenacy's Prochlorperazine Edisylate Injection, USP is available in 10 mg/2 mL (5 mg per mL) 10-pack multi-dose vials. In line with Avenacy’s mission to champion patient safety and streamline patient care, Prochlorperazine Edisylate Injection, USP will feature the Company’s highly differentiated packaging and labeling to support accurate medication selection. Avenacy will begin shipping Prochlorperazine Edisylate Injection, USP to wholesale partners this week. The Company is supported by a global network of development and contract manufacturing partners that have undergone successful FDA inspections based on cGMP-standards. Prochlorperazine Edisylate Injection, USP had U.S. sales of approximately $15 million for the twelve months ending in June 2023.1 Warning Increased Mortality in Elderly Patients with Dementia-Related Psychosis Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Analyses of seventeen placebo-controlled trials (modal duration of 10 weeks), largely in patients taking atypical antipsychotic drugs, revealed a risk of death in drug-treated patients of between 1.6 to 1.7 times the risk of death in placebo-treated patients. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was about 4.5%, compared to a rate of about 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotic drugs, treatment with conventional antipsychotic drugs may increase mortality. The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear. Prochlorperazine Edisylate Injection, USP is not approved for the treatment of patients with dementia-related psychosis (see WARNINGS). Please see link for Full Prescribing Information including the Boxed Warning. COMPAZINE® is a registered trademark of GlaxoSmithKline. 1Source: IQVIA About Avenacy Avenacy is a U.S.-based specialty pharmaceutical company focused on supplying critical injectable medications used to treat patients in various medically supervised settings, from acute care hospitals to outpatient clinics and physician offices. Through a rigorous and optimized selection process, the Company is building out a pipeline of high-quality FDA approved injectable products in order to ensure a resilient portfolio that can meet the needs of today’s dynamic drug supply chain. With an experienced team, commitment to quality and reliability, and product offerings intended to facilitate safe and efficient patient care, Avenacy strives to be a trusted partner for essential medications. Avenacy was launched in 2023 and is headquartered in Schaumburg, IL. For more information, please visit .

Drug ApprovalClinical Result

06 Jun 2024

·www.drugs.com

Several Drugs Linked to Risk for Aneurysmal Subarachnoid Hemorrhage

THURSDAY, June 6, 2024 -- Several commonly prescribed drugs are associated with aneurysmal subarachnoid hemorrhage (aSAH), according to a study published online June 5 in Neurology . Jos P. Kanning, from the University Medical Center Utrecht in the Netherlands, and colleagues conducted a drug-wide association study to examine the association between commonly prescribed drugs and aSAH incidence. Use of commonly prescribed drugs was examined across exposure windows (current, within three months; recent, three to 12 months; and past, >12 months). Exposure to 205 commonly prescribed drugs was investigated among 4,879 aSAH cases and 43,911 matched controls. The researchers found similar trends for lisinopril and amlodipine, with a decreased risk for aSAH in association with current use, while the risk for aSAH was increased with recent use. The risk for aSAH was reduced with current use of simvastatin, metformin, and tamsulosin. Increased aSAH risk was seen in association with current use of warfarin, venlafaxine, prochlorperazine, and co-codamol. "Future research should use a more hypothesis-driven approach to further investigate these associations and differentiate between drug class and specific drug substance effects," the authors write. "In addition, this research may help identify additional risk factors for aSAH, potentially leading to new pharmacologic therapy options for aneurysmal management." Abstract/Full Text Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

Clinical ResultClinical Study

06 Jun 2024

·www.drugs.com

Statins, Metformin Can Cut Odds for Brain Aneurysms

THURSDAY, June 6, 2024 -- Common drugs used to control cholesterol, blood sugar and high blood pressure might also lower a person’s risk of stroke , a new study finds. The researchers evaluated the risk of brain aneurysms that cause bleeding strokes in patients. For the study, they looked at the medical records for nearly 4,900 patients who had a bleeding stroke, and compared them against nearly 44,000 people who never had a brain aneurysm. They identified four specific drugs that appeared to lower the risk of a brain aneurysm, after accounting for other risk factors: “We urgently need new ways to prevent this type of stroke, which occurs at younger ages and with a higher death rate than other types of stroke,” said researcher Jos Peter Kanning , with the University Medical Center Utrecht in the Netherlands. “Our current surgical treatments for brain aneurysms have a risk of permanent disability and death that often outweighs the potential benefits, so preventing rupture with a noninvasive drug would be very beneficial,” Kanning added in a university news release. On the other hand, four drugs increased the risk of a bleeding stroke: the blood thinner warfarin , the antidepressant venlafaxine , the antipsychotic prochlorperazine , and the painkiller co-codamol . The findings, which were published June 5 in the journal Neurology, only show an association between these drugs and stroke risk, the researchers noted. “Future research is needed to investigate these associations and determine whether these drugs are effective in reducing the risk of hemorrhagic stroke,” Kanning said. “This work could also help us identify additional risk factors for subarachnoid hemorrhage, potentially leading to new therapies to manage aneurysms.” Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

100 Deals associated with Prochlorperazine

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External Link

KEGG	Wiki	ATC	Drug Bank
D00493	Prochlorperazine	N05AB04	DB00433

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Schizophrenia	US	GlaxoSmithKline, Inc.	26 Jan 1959

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03185130 (CTgov)	Phase 4	Headache	58	Prochlorperazine 0.15 mg/kg up to 10 mg IV+Normal Saline 5mL+Diphenhydramine 1 mg/kg up to 50 mg IV (Standard Treatment Arm)	aaaudumnlu(mnctkwycyx) = envywkyxzw sktbumxhgw (hgytapwuwc, bwdedrgcks - umcifoncxr) View more	-	06 Jun 2024
				Normal Saline 20mL/kg+Prochlorperazine 0.15 mg/kg up to 10 mg IV+Diphenhydramine 1 mg/kg up to 50 mg IV (Study Arm)	aaaudumnlu(mnctkwycyx) = jeiwbnoqfo sktbumxhgw (hgytapwuwc, yyaehllgyb - bzvprozgly) View more
NCT03435003 (CTgov)	Phase 4	Postoperative Nausea and Vomiting \| Vomiting	83	dexmedetomidine+Compazine+Total intravenous anesthesia+scopolamine transdermal+sugammadex+Reglan+Propofol+Fentanyl+Ondansetron+Aprepitant 80 mg Oral Capsule+Dexamethasone (Intervention Arm)	hxtojaygrf(kaopchlnjf) = wyfdsbbvkq aqclkkxfuu (vbdicumgtz, wbbxrgzrdn - qnauswskya) View more	-	14 Feb 2024
				Compazine+sugammadex+Reglan+Sevoflurane+Desflurane+Ondansetron+Dexamethasone (Control Arm)	hxtojaygrf(kaopchlnjf) = qvymntsyuc aqclkkxfuu (vbdicumgtz, xfyimlnohe - qgmvctpvvk) View more
CNS2023	Phase 1/2	Migraine Disorders	17	Normal Saline, Prochlorperazine, Ketorolac	fdgjthcree(wpezyekozq) = oreuzmnpmr tjpataunwl (qtghvsedkv ) View more	Positive	01 Oct 2023
NCT01629329 (CTgov)	Phase 4	Acute migraine	93	Aspirin, Acetaminophen, Caffeine pills (Aspirin, Acetaminophen, Caffeine Pills)	hjvrcrkqkm(ixymvxvkgg) = xhfyriqchu hpzrpbkqju (utkpwyajpx, mkhiwyulql - sbiklfacpv) View more	-	18 Mar 2020
				Prochlorperazine 10mg (Prochlorperazine 10mg)	hjvrcrkqkm(ixymvxvkgg) = xshnrpkawp hpzrpbkqju (utkpwyajpx, onasgkcuws - hkphwwikdx) View more
NCT02389829 (CTgov)	Phase 4	Acute migraine	127	Hydromorphone (Hydromorphone)	wmvmimzpoy(jvzevegrgl) = jzvpwlmezu gpvdxjwyxb (vecaeohhvk, ymboixxazr - bmyuasushv) View more	-	06 Jun 2018
				prochlorperazine+Diphenhydramine (Prochlorperazine)	wmvmimzpoy(jvzevegrgl) = frfpqhzcjv gpvdxjwyxb (vecaeohhvk, hvfuhxfvbe - uiulpmkrok) View more
NCT00422812 (CTgov)	Phase 2	Migraine With Aura	400	Inhaled Placebo (Inhaled Placebo)	ndijqsfajk(ljikjxfvmk) = menodhhqji jximiiwelx (odojjifbat, qxxhtoiqyg - zpwsiqucxy) View more	-	25 Jan 2018
				Prochlorperazine+Staccato (Inhaled PCZ 5 mg)	ndijqsfajk(ljikjxfvmk) = uvubbjpjxe jximiiwelx (odojjifbat, tsewuljwyt - zaypmpcygc) View more
NCT00590317 (CTgov)	Phase 2	Nausea \| Nausea and vomiting \| Vomiting	64	Prochlorperazine (Prochlorperazine)	kapdsivzej(cvdgxaywrd) = icmwofrhsy jiiuolbqks (crvfmfahvq, qnhsdttjoh - ntljnmawpq) View more	-	19 May 2014
				Ondansetron (Ondansetron)	kapdsivzej(cvdgxaywrd) = fbiixayqby jiiuolbqks (crvfmfahvq, pkjjngszvy - mrlccepqdg) View more
NCT00475085 (CTgov)	Phase 3	Nausea \| Delayed Nausea and Vomiting	1,021	prochlorperazine+placebo+granisetron hydrochloride+Dexamethasone (Arm II)	znqthfdifc(iibhdpwmvz) = hntdbyathu vnpvilfjno (fajqckyasv, npkgrynjhp - qoyhmidfmu) View more	-	03 Nov 2013
				placebo+palonosetron hydrochloride+aprepitant+Dexamethasone (Arm III)	znqthfdifc(iibhdpwmvz) = qphruoucbg vnpvilfjno (fajqckyasv, rfmpjncwmb - gtzicgiugn) View more
NCT02657031 \| NCT03185130 (Pubmed \| Ann Emerg Med)	Phase 4	Acute migraine	-	IV prochlorperazine with diphenhydramine	llxiczerxq(rtevljiwkr) = gumqgncntp dvknpgeqge (gjlyxasgpq )	Positive	01 Jul 2010
				subcutaneous sumatriptan	llxiczerxq(rtevljiwkr) = xrrvrjaivf dvknpgeqge (gjlyxasgpq )
ASCO2010	Not Applicable	Chemotherapy-induced nausea and vomiting	96	Prochlorperazine	iwjvxopvje(jardhtlgwi) = rpddihvwgg mrrngaqwwu (qqmvawyfwy )	-	20 May 2010
				5HT3 antagonists	iwjvxopvje(jardhtlgwi) = gnftfdmtmd mrrngaqwwu (qqmvawyfwy )