Prochlorperazine
Overview
Description
Prochlorperazine is a phenothiazine derivative that is primarily used as an antipsychotic and antiemetic medication. It is commonly prescribed for the treatment of severe nausea and vomiting, schizophrenia, psychosis, and anxiety . This compound works by blocking dopamine receptors in the brain, which helps to alleviate symptoms associated with these conditions .
Mechanism of Action
Target of Action
Prochlorperazine, a phenothiazine derivative, primarily targets D2 dopamine receptors in the brain . These receptors are somatodendritic autoreceptors that play a crucial role in regulating dopamine release, synthesis, and neuron firing . This compound also blocks histaminergic, cholinergic, and noradrenergic receptors .
Mode of Action
This compound exerts its effects by blocking D2 dopamine receptors in the brain . This blockade inhibits the action of dopamine, a neurotransmitter that plays a significant role in behavior, cognition, and motor activity . By blocking these receptors, this compound can alleviate symptoms of conditions like schizophrenia and anxiety . It also depresses the chemoreceptor trigger zone, which contributes to its antiemetic (anti-nausea and vomiting) effects .
Biochemical Pathways
It’s known that the drug’s anti-dopaminergic effects play a significant role in its mechanism of action . By blocking D2 dopamine receptors, this compound disrupts dopamine signaling, which can affect various downstream pathways and processes .
Pharmacokinetics
The pharmacokinetics of this compound have been studied in both young and elderly subjects. After intravenous dosing, the terminal half-life of this compound was found to be 7.5 ± 1.8 hours . Oral bioavailability was low, at14.7 ± 1.5%
Result of Action
This compound’s action results in a variety of molecular and cellular effects. Its antipsychotic effects are primarily due to its ability to block D2 dopamine receptors, which can help alleviate symptoms of conditions like schizophrenia and anxiety . Additionally, its antiemetic effects are due to its ability to depress the chemoreceptor trigger zone . Some studies have also suggested that this compound may have anti-cancer activity .
Action Environment
The action, efficacy, and stability of this compound can be influenced by various environmental factors. For instance, the drug’s absorption, distribution, metabolism, and excretion can be affected by factors such as the patient’s age, health status, and the presence of other medications . .
Biochemical Analysis
Biochemical Properties
Prochlorperazine plays a significant role in biochemical reactions by interacting with various enzymes, proteins, and other biomolecules. It primarily inhibits D2 dopamine receptors in the brain, which leads to its antipsychotic and antiemetic effects . Additionally, this compound can interact with histamine, choline, and noradrenaline receptors, contributing to its broad pharmacological profile . These interactions are crucial for its therapeutic effects and side effects.
Cellular Effects
This compound affects various types of cells and cellular processes. It influences cell function by modulating cell signaling pathways, gene expression, and cellular metabolism. By blocking dopamine receptors, this compound reduces dopaminergic neurotransmission, which can alter gene expression related to dopamine signaling . This modulation can impact cellular metabolism and overall cell function, leading to its therapeutic and side effects.
Molecular Mechanism
The molecular mechanism of this compound involves its binding interactions with biomolecules, enzyme inhibition, and changes in gene expression. This compound binds to D2 dopamine receptors, inhibiting their activity and reducing dopaminergic neurotransmission . This inhibition can lead to changes in gene expression, particularly those genes involved in dopamine signaling pathways. Additionally, this compound can inhibit other receptors, such as histamine and choline receptors, contributing to its broad pharmacological effects .
Temporal Effects in Laboratory Settings
In laboratory settings, the effects of this compound can change over time. The stability and degradation of this compound are important factors that influence its long-term effects on cellular function. Studies have shown that this compound can degrade over time, leading to reduced efficacy . Long-term exposure to this compound can also result in changes in cellular function, such as alterations in receptor sensitivity and gene expression .
Dosage Effects in Animal Models
The effects of this compound vary with different dosages in animal models. At therapeutic doses, this compound effectively manages symptoms of nausea, vomiting, and psychosis . At higher doses, this compound can cause toxic or adverse effects, such as extrapyramidal symptoms and neuroleptic malignant syndrome . These threshold effects highlight the importance of careful dosage management in clinical settings.
Metabolic Pathways
This compound is involved in several metabolic pathways, including those mediated by cytochrome P450 enzymes . It undergoes extensive first-pass metabolism, leading to the formation of various metabolites, such as N-desmethyl this compound and this compound sulfoxide . These metabolic pathways can influence the drug’s efficacy and safety profile.
Transport and Distribution
This compound is transported and distributed within cells and tissues through various mechanisms. It can interact with transporters and binding proteins that facilitate its movement across cell membranes . The distribution of this compound within tissues can affect its localization and accumulation, influencing its therapeutic and side effects.
Subcellular Localization
The subcellular localization of this compound is crucial for its activity and function. This compound can be directed to specific compartments or organelles through targeting signals and post-translational modifications . This localization can impact its interactions with receptors and other biomolecules, ultimately influencing its pharmacological effects.
Preparation Methods
Synthetic Routes and Reaction Conditions: Prochlorperazine is synthesized through a multi-step chemical process. The synthesis typically involves the reaction of 2-chlorophenothiazine with 1-methyl-4-piperazine . The reaction conditions often include the use of solvents such as ethanol or methanol and catalysts to facilitate the reaction. The final product is purified through recrystallization or other purification techniques to obtain high-purity this compound.
Industrial Production Methods: In industrial settings, this compound is produced on a larger scale using similar synthetic routes. The process involves the use of large reactors and precise control of reaction conditions to ensure consistent quality and yield. The industrial production also includes rigorous quality control measures to ensure the safety and efficacy of the final product .
Chemical Reactions Analysis
Types of Reactions: Prochlorperazine undergoes various chemical reactions, including:
Oxidation: this compound can be oxidized to form sulfoxides and sulfones.
Reduction: Reduction reactions can convert this compound to its corresponding reduced forms.
Substitution: this compound can undergo substitution reactions, particularly at the chlorine atom on the phenothiazine ring.
Common Reagents and Conditions:
Oxidation: Common oxidizing agents include hydrogen peroxide and potassium permanganate.
Reduction: Reducing agents such as sodium borohydride and lithium aluminum hydride are used.
Substitution: Substitution reactions often involve nucleophiles such as amines or thiols.
Major Products Formed:
Oxidation: Sulfoxides and sulfones.
Reduction: Reduced forms of this compound.
Substitution: Various substituted phenothiazine derivatives.
Scientific Research Applications
Prochlorperazine has a wide range of scientific research applications:
Chemistry: Used as a model compound in studies of phenothiazine derivatives and their chemical properties.
Biology: Investigated for its effects on cellular processes and receptor interactions.
Medicine: Extensively studied for its therapeutic effects in treating nausea, vomiting, and psychiatric disorders.
Industry: Utilized in the development of new pharmaceutical formulations and drug delivery systems.
Comparison with Similar Compounds
Chlorpromazine: Another phenothiazine derivative with similar antipsychotic and antiemetic properties.
Promethazine: A phenothiazine derivative primarily used as an antihistamine and antiemetic.
Fluphenazine: A phenothiazine derivative used as an antipsychotic.
Comparison:
Prochlorperazine vs. Chlorpromazine: this compound has a higher potency in blocking dopamine receptors and is more effective in treating nausea and vomiting.
This compound vs. Promethazine: While both have antiemetic properties, this compound is more commonly used for its antipsychotic effects.
This compound vs. Fluphenazine: Fluphenazine is more potent as an antipsychotic, but this compound is preferred for its antiemetic properties.
This compound’s unique combination of antipsychotic and antiemetic effects makes it a valuable medication in both psychiatric and medical settings.
Properties
IUPAC Name |
2-chloro-10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine |
Source
|
|---|---|---|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
InChI |
InChI=1S/C20H24ClN3S/c1-22-11-13-23(14-12-22)9-4-10-24-17-5-2-3-6-19(17)25-20-8-7-16(21)15-18(20)24/h2-3,5-8,15H,4,9-14H2,1H3 |
Source
|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
InChI Key |
WIKYUJGCLQQFNW-UHFFFAOYSA-N |
Source
|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
Canonical SMILES |
CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl |
Source
|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
Molecular Formula |
C20H24ClN3S |
Source
|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
DSSTOX Substance ID |
DTXSID7023514 |
Source
|
| Record name | Prochlorperazine | |
| Source | EPA DSSTox | |
| URL | https://comptox.epa.gov/dashboard/DTXSID7023514 | |
| Description | DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology. | |
Molecular Weight |
373.9 g/mol |
Source
|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
Physical Description |
Solid |
Source
|
| Record name | Prochlorperazine | |
| Source | Human Metabolome Database (HMDB) | |
| URL | http://www.hmdb.ca/metabolites/HMDB0014577 | |
| Description | The Human Metabolome Database (HMDB) is a freely available electronic database containing detailed information about small molecule metabolites found in the human body. | |
| Explanation | HMDB is offered to the public as a freely available resource. Use and re-distribution of the data, in whole or in part, for commercial purposes requires explicit permission of the authors and explicit acknowledgment of the source material (HMDB) and the original publication (see the HMDB citing page). We ask that users who download significant portions of the database cite the HMDB paper in any resulting publications. | |
Solubility |
Freely soluble in alcohol, ether, chloroform, In water, 1.496X10-2 g/L (14.96 mg/L) at 24 °C, 1.10e-02 g/L |
Source
|
| Record name | Prochlorperazine | |
| Source | DrugBank | |
| URL | https://www.drugbank.ca/drugs/DB00433 | |
| Description | The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information. | |
| Explanation | Creative Common's Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/legalcode) | |
| Record name | Prochlorperazine | |
| Source | Hazardous Substances Data Bank (HSDB) | |
| URL | https://pubchem.ncbi.nlm.nih.gov/source/hsdb/3171 | |
| Description | The Hazardous Substances Data Bank (HSDB) is a toxicology database that focuses on the toxicology of potentially hazardous chemicals. It provides information on human exposure, industrial hygiene, emergency handling procedures, environmental fate, regulatory requirements, nanomaterials, and related areas. The information in HSDB has been assessed by a Scientific Review Panel. | |
| Record name | Prochlorperazine | |
| Source | Human Metabolome Database (HMDB) | |
| URL | http://www.hmdb.ca/metabolites/HMDB0014577 | |
| Description | The Human Metabolome Database (HMDB) is a freely available electronic database containing detailed information about small molecule metabolites found in the human body. | |
| Explanation | HMDB is offered to the public as a freely available resource. Use and re-distribution of the data, in whole or in part, for commercial purposes requires explicit permission of the authors and explicit acknowledgment of the source material (HMDB) and the original publication (see the HMDB citing page). We ask that users who download significant portions of the database cite the HMDB paper in any resulting publications. | |
Mechanism of Action |
The mechanism of action of prochlorperazine has not been fully determined, but may be primarily related to its anti-dopaminergic effects. Prochlorperazine blocks the D2 dopamine receptors in the brain, which are somatodendritic autoreceptors. Inhibition of D2 receptor signaling results in the blockade of postsynaptic dopamine receptors in the mesolimbic system and an increased dopamine turnover. Nausea and vomiting are proposed to arise from peripheral or central stimulation of serotonin type 3 (5-HT3) and dopamine type 2 receptors, the predominant receptors expressed at the chemoreceptor trigger zone (CTZ). Prochlorperazine exerts antiemetic effects and was shown to inhibit apomorphine-induced vomiting by blocking D2 dopamine receptors in the CTZ.., The principal pharmacologic effects of prochlorperazine are similar to those of chlorpromazine. Prochlorperazine has weak anticholinergic effects, moderate sedative effects, and strong extrapyramidal effects. Prochlorperazine has strong antiemetic activity., The development of phenothiazine derivatives as psychopharmacologic agents resulted from the observation that certain phenothiazine antihistaminic compounds produced sedation. In an attempt to enhance the sedative effects of these drugs, promethazine and chlorpromazine were synthesized. Chlorpromazine is the pharmacologic prototype of the phenothiazines. The pharmacology of phenothiazines is complex, and because of their actions on the central and autonomic nervous systems, the drugs affect many different sites in the body. Although the actions of the various phenothiazines are generally similar, these drugs differ both quantitatively and qualitatively in the extent to which they produce specific pharmacologic effects. /Phenothiazine General Statement/, In the CNS, phenothiazines act principally at the subcortical levels of the reticular formation, limbic system, and hypothalamus. Phenothiazines generally do not produce substantial cortical depression; however, there is minimal information on the specific effects of phenothiazines at the cortical level. Phenothiazines also act in the basal ganglia, exhibiting extrapyramidal effects. The precise mechanism(s) of action, including antipsychotic action, of phenothiazines has not been determined, but may be principally related to antidopaminergic effects of the drugs. There is evidence to indicate that phenothiazines antagonize dopamine-mediated neurotransmission at the synapses. There is also some evidence that phenothiazines may block postsynaptic dopamine receptor sites. However, it has not been determined whether the antipsychotic effect of the drugs is causally related to their antidopaminergic effects. Phenothiazines also have peripheral and/or central antagonistic activity against alpha-adrenergic, serotonergic, histaminic (H1-receptors), and muscarinic receptors. Phenothiazines also have some adrenergic activity, since they block the reuptake of monoamines at the presynaptic neuronal membrane, which tends to enhance neurotransmission. The effects of phenothiazines on the autonomic nervous system are complex and unpredictable because the drugs exhibit varying degrees of alpha-adrenergic blocking, muscarinic blocking, and adrenergic activity. The antipsychotic activity of phenothiazines may be related to any or all of these effects, but it has been suggested that the drugs' effects on dopamine are probably most important. It has also been suggested that effects of phenothiazines on other amines (eg, gamma-aminobutyric acid [GABA]) or peptides (eg, substance P, endorphins) may contribute to their antipsychotic effect. Further study is needed to determine the role of central neuronal receptor antagonism and of effects on biochemical mediators in the antipsychotic action of the phenothiazines and other antipsychotic agents. /Phenothiazine General Statement/, Although the exact mechanism(s) of action has not been conclusively determined, phenothiazines have an antiemetic effect. The antiemetic activity may be mediated via a direct effect of the drugs on the medullary chemoreceptor trigger zone (CTZ), apparently by blocking dopamine receptors in the CTZ. Phenothiazines inhibit the central and peripheral effects of apomorphine and ergot alkaloids. Phenothiazines generally do not inhibit emesis caused by the action of drugs at the nodose ganglion or by local action on the GI tract. /Phenothiazine General Statement/, For more Mechanism of Action (Complete) data for Prochlorperazine (15 total), please visit the HSDB record page. |
Source
|
| Record name | Prochlorperazine | |
| Source | DrugBank | |
| URL | https://www.drugbank.ca/drugs/DB00433 | |
| Description | The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information. | |
| Explanation | Creative Common's Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/legalcode) | |
| Record name | Prochlorperazine | |
| Source | Hazardous Substances Data Bank (HSDB) | |
| URL | https://pubchem.ncbi.nlm.nih.gov/source/hsdb/3171 | |
| Description | The Hazardous Substances Data Bank (HSDB) is a toxicology database that focuses on the toxicology of potentially hazardous chemicals. It provides information on human exposure, industrial hygiene, emergency handling procedures, environmental fate, regulatory requirements, nanomaterials, and related areas. The information in HSDB has been assessed by a Scientific Review Panel. | |
Color/Form |
Viscous liquid | |
CAS No. |
58-38-8 |
Source
|
| Record name | Prochlorperazine | |
| Source | CAS Common Chemistry | |
| URL | https://commonchemistry.cas.org/detail?cas_rn=58-38-8 | |
| Description | CAS Common Chemistry is an open community resource for accessing chemical information. Nearly 500,000 chemical substances from CAS REGISTRY cover areas of community interest, including common and frequently regulated chemicals, and those relevant to high school and undergraduate chemistry classes. This chemical information, curated by our expert scientists, is provided in alignment with our mission as a division of the American Chemical Society. | |
| Explanation | The data from CAS Common Chemistry is provided under a CC-BY-NC 4.0 license, unless otherwise stated. | |
| Record name | Prochlorperazine [USP:INN:BAN:JAN] | |
| Source | ChemIDplus | |
| URL | https://pubchem.ncbi.nlm.nih.gov/substance/?source=chemidplus&sourceid=0000058388 | |
| Description | ChemIDplus is a free, web search system that provides access to the structure and nomenclature authority files used for the identification of chemical substances cited in National Library of Medicine (NLM) databases, including the TOXNET system. | |
| Record name | Prochlorperazine | |
| Source | DrugBank | |
| URL | https://www.drugbank.ca/drugs/DB00433 | |
| Description | The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information. | |
| Explanation | Creative Common's Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/legalcode) | |
| Record name | Prochlorperazine | |
| Source | EPA DSSTox | |
| URL | https://comptox.epa.gov/dashboard/DTXSID7023514 | |
| Description | DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology. | |
| Record name | Prochlorperazine | |
| Source | European Chemicals Agency (ECHA) | |
| URL | https://echa.europa.eu/substance-information/-/substanceinfo/100.000.345 | |
| Description | The European Chemicals Agency (ECHA) is an agency of the European Union which is the driving force among regulatory authorities in implementing the EU's groundbreaking chemicals legislation for the benefit of human health and the environment as well as for innovation and competitiveness. | |
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| Record name | PROCHLORPERAZINE | |
| Source | FDA Global Substance Registration System (GSRS) | |
| URL | https://gsrs.ncats.nih.gov/ginas/app/beta/substances/YHP6YLT61T | |
| Description | The FDA Global Substance Registration System (GSRS) enables the efficient and accurate exchange of information on what substances are in regulated products. Instead of relying on names, which vary across regulatory domains, countries, and regions, the GSRS knowledge base makes it possible for substances to be defined by standardized, scientific descriptions. | |
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| Record name | Prochlorperazine | |
| Source | Hazardous Substances Data Bank (HSDB) | |
| URL | https://pubchem.ncbi.nlm.nih.gov/source/hsdb/3171 | |
| Description | The Hazardous Substances Data Bank (HSDB) is a toxicology database that focuses on the toxicology of potentially hazardous chemicals. It provides information on human exposure, industrial hygiene, emergency handling procedures, environmental fate, regulatory requirements, nanomaterials, and related areas. The information in HSDB has been assessed by a Scientific Review Panel. | |
| Record name | Prochlorperazine | |
| Source | Human Metabolome Database (HMDB) | |
| URL | http://www.hmdb.ca/metabolites/HMDB0014577 | |
| Description | The Human Metabolome Database (HMDB) is a freely available electronic database containing detailed information about small molecule metabolites found in the human body. | |
| Explanation | HMDB is offered to the public as a freely available resource. Use and re-distribution of the data, in whole or in part, for commercial purposes requires explicit permission of the authors and explicit acknowledgment of the source material (HMDB) and the original publication (see the HMDB citing page). We ask that users who download significant portions of the database cite the HMDB paper in any resulting publications. | |
Melting Point |
228 °C |
Source
|
| Record name | Prochlorperazine | |
| Source | DrugBank | |
| URL | https://www.drugbank.ca/drugs/DB00433 | |
| Description | The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information. | |
| Explanation | Creative Common's Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/legalcode) | |
| Record name | Prochlorperazine | |
| Source | Hazardous Substances Data Bank (HSDB) | |
| URL | https://pubchem.ncbi.nlm.nih.gov/source/hsdb/3171 | |
| Description | The Hazardous Substances Data Bank (HSDB) is a toxicology database that focuses on the toxicology of potentially hazardous chemicals. It provides information on human exposure, industrial hygiene, emergency handling procedures, environmental fate, regulatory requirements, nanomaterials, and related areas. The information in HSDB has been assessed by a Scientific Review Panel. | |
| Record name | Prochlorperazine | |
| Source | Human Metabolome Database (HMDB) | |
| URL | http://www.hmdb.ca/metabolites/HMDB0014577 | |
| Description | The Human Metabolome Database (HMDB) is a freely available electronic database containing detailed information about small molecule metabolites found in the human body. | |
| Explanation | HMDB is offered to the public as a freely available resource. Use and re-distribution of the data, in whole or in part, for commercial purposes requires explicit permission of the authors and explicit acknowledgment of the source material (HMDB) and the original publication (see the HMDB citing page). We ask that users who download significant portions of the database cite the HMDB paper in any resulting publications. | |
Retrosynthesis Analysis
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Strategy Settings
| Precursor scoring | Relevance Heuristic |
|---|---|
| Min. plausibility | 0.01 |
| Model | Template_relevance |
| Template Set | Pistachio/Bkms_metabolic/Pistachio_ringbreaker/Reaxys/Reaxys_biocatalysis |
| Top-N result to add to graph | 6 |
Feasible Synthetic Routes
Q1: What is the primary mechanism of action of prochlorperazine?
A1: this compound primarily acts as a dopamine D2 receptor antagonist. [] It binds to these receptors, primarily in the chemoreceptor trigger zone and, at higher doses, the nucleus of the solitary tract, blocking the action of dopamine. [, ] This blockade leads to its antiemetic effects by reducing nausea and vomiting. [, ]
Q2: How does this compound impact stimulus-secretion coupling in pancreatic beta cells?
A2: Research suggests that this compound inhibits the activation of calmodulin-dependent phosphodiesterase in pancreatic beta-cells. [] This inhibition disrupts calcium-dependent stimulus-secretion coupling, ultimately decreasing insulin release stimulated by various factors like glucose, leucine, and glibenclamide. []
Q3: Is there any available information on the molecular formula, weight, and spectroscopic data of this compound?
A3: While the provided research focuses on the pharmacological aspects of this compound, specific details about its molecular formula, weight, and spectroscopic data are not discussed. Refer to chemical databases or literature for this information.
Q4: What is known about the compatibility of this compound with other drugs in admixtures?
A4: Studies investigating the stability and compatibility of this compound admixtures have shown mixed results. While this compound is physically compatible with hydromorphone for up to seven days at temperatures up to 37°C, admixtures with dimenhydrinate are not recommended due to precipitation of 8-chlorotheophylline after 48 hours. [] Combining this compound with lorazepam is physically possible, but the mixture's shelf life is limited by lorazepam's stability, recommending an expiry date not exceeding 96 hours at 4°C. []
Q5: How does the route of administration affect the pharmacokinetic profile of this compound?
A5: Research suggests that buccal administration of this compound achieves significantly higher plasma concentrations compared to oral administration. [] Specifically, buccal administration results in more than double the plasma concentration with less than half the variability compared to oral tablets. [] This difference highlights the impact of first-pass metabolism on this compound bioavailability following oral administration.
Q6: Does the cytochrome P450 genotype influence the metabolism of this compound?
A6: A study investigating the influence of CYP2C19, CYP2D6, and CYP3A5 genotypes on this compound metabolism found no significant effect. [] While this compound undergoes extensive metabolism by cytochrome P450 enzymes, this particular research indicates that genetic variations in these enzymes do not significantly alter the plasma concentrations of this compound or its metabolites. []
Q7: How does this compound distribute in the body after aerosol administration?
A7: A study using a recirculatory pharmacokinetic model in dogs revealed that this compound administered as a thermally generated aerosol is rapidly absorbed and distributed, achieving peak left ventricular concentrations in less than 30 seconds. [] This rapid absorption resulted in plasma drug concentrations comparable to those achieved after a rapid intravenous infusion of the same dose. [] The bioavailability of the aerosol was determined to be greater than 80% of the emitted dose, highlighting its potential as an alternative to intravenous administration for drugs requiring rapid onset of action. []
Q8: Is this compound effective in preventing opioid-induced nausea and vomiting (OINV)?
A9: Research suggests that prophylactic administration of this compound, either as an injection or at the initiation of oral oxycodone treatment, is not effective in preventing OINV in patients with end-stage cancer. [, ] This finding challenges previous recommendations regarding the use of antiemetics for OINV management and highlights the need for further research to identify effective strategies for this patient population.
Q9: Can this compound be used to treat migraine headaches?
A10: Clinical trials have shown that intravenous this compound, particularly in combination with diphenhydramine, can effectively treat acute migraine headaches in the emergency department setting. [, ] In a randomized controlled trial, intravenous this compound plus diphenhydramine demonstrated superior headache relief compared to intravenous hydromorphone. [] This finding supports the use of this compound as a potential first-line treatment option for acute migraine, potentially reducing the reliance on opioids. []
Q10: How does this compound interact with melanin and what are the implications?
A11: this compound demonstrates a strong interaction with melanin, forming stable complexes. [] This interaction, characterized by two classes of independent binding sites, raises concerns about potential drug accumulation in pigmented tissues. [] Studies on normal human melanocytes exposed to this compound revealed concentration-dependent effects on cell viability, melanogenesis, and the cellular antioxidant defense system, suggesting a potential role of melanin and oxidative stress in the mechanism of this compound's side effects. []
Q11: What are the potential side effects associated with this compound use?
A12: While this Q&A focuses on the scientific aspects of this compound, it's important to acknowledge potential side effects. Research indicates that this compound can cause extrapyramidal symptoms (EPS), such as akathisia and dystonia, especially at higher doses or with prolonged use. [, , , , ] The co-administration of diphenhydramine with this compound is often employed to mitigate the risk of EPS. []
Q12: Are there any known interactions between this compound and other medications?
A13: While specific drug interactions are not extensively discussed in the provided research, this compound's action on dopamine receptors can lead to interactions with other drugs affecting the dopaminergic system. [] Additionally, its metabolism by cytochrome P450 enzymes raises the possibility of interactions with drugs that induce or inhibit these enzymes. [] Clinicians should consider potential drug interactions when prescribing this compound.
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Please be aware that all articles and product information presented on BenchChem are intended solely for informational purposes. The products available for purchase on BenchChem are specifically designed for in-vitro studies, which are conducted outside of living organisms. In-vitro studies, derived from the Latin term "in glass," involve experiments performed in controlled laboratory settings using cells or tissues. It is important to note that these products are not categorized as medicines or drugs, and they have not received approval from the FDA for the prevention, treatment, or cure of any medical condition, ailment, or disease. We must emphasize that any form of bodily introduction of these products into humans or animals is strictly prohibited by law. It is essential to adhere to these guidelines to ensure compliance with legal and ethical standards in research and experimentation.
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