Felodipine
Overview
Description
Felodipine is a medication classified as a calcium channel blocker, primarily used to treat high blood pressure and stable angina . It was patented in 1978 and approved for medical use in 1988 . This compound works by relaxing blood vessels, which allows blood to flow more easily, thereby reducing the workload on the heart .
Scientific Research Applications
Felodipine has a wide range of scientific research applications. In pharmacology, it is used to study the effects of calcium channel blockers on blood pressure and heart rate . It is also used in drug-drug interaction modeling to predict how it interacts with other medications metabolized by CYP3A4 . In chemistry, this compound’s photostability and photodegradation are studied to understand its behavior under UV irradiation . Additionally, this compound is used in the development of solid lipid nanoparticles to enhance its oral bioavailability .
Mechanism of Action
Target of Action
Felodipine primarily targets vascular smooth muscle cells . It acts by stabilizing voltage-gated L-type calcium channels in their inactive conformation . These channels play a crucial role in the contraction of smooth muscle cells.
Mode of Action
This compound inhibits the influx of calcium ions in smooth muscle cells by binding to and stabilizing the inactive conformation of L-type calcium channels . This prevents calcium-dependent myocyte contraction and vasoconstriction . In addition to L-type calcium channels, this compound also binds to a number of calcium-binding proteins .
Biochemical Pathways
This compound’s action on L-type calcium channels leads to the relaxation of vascular smooth muscle and vasodilation . This results in a decrease in peripheral vascular resistance and blood pressure . The drug’s vasodilatory effects are thought to be brought about primarily through the inhibition of these channels .
Pharmacokinetics
This compound is rapidly and completely absorbed, but it undergoes extensive first-pass metabolism, resulting in a bioavailability of about 15% . It is metabolized by CYP3A4 , a major enzyme involved in drug metabolism . The peak plasma concentrations and area under the plasma concentration-time curve are linearly related to the dose .
Result of Action
The inhibition of calcium influx into vascular smooth muscle cells by this compound leads to the relaxation of these cells . This results in vasodilation, which increases the supply of blood and oxygen to the heart, reducing the heart’s workload .
Action Environment
Environmental factors can influence the action of this compound. For instance, the presence of CYP3A4 inhibitors can affect the metabolism and hence the bioavailability of this compound . Also, the drug’s environmental risk is considered low, with a Predicted Environmental Concentration (PEC) / Predicted No Effect Concentration (PNEC) ratio of 0.22 .
Safety and Hazards
Biochemical Analysis
Biochemical Properties
Felodipine: This compound acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation . By inhibiting the influx of calcium in smooth muscle cells, prevents calcium-dependent myocyte contraction and vasoconstriction . In addition to binding to L-type calcium channels, This compound binds to a number of calcium-binding proteins .
Cellular Effects
This compound: this compound has a significant impact on various types of cells and cellular processes. It prevents calcium-dependent myocyte contraction and vasoconstriction, thereby influencing cell function . This effect of can lead to a reduction in systemic vascular resistance and blood pressure .
Molecular Mechanism
This compound: This compound exerts its effects at the molecular level primarily through inhibition of voltage-gated L-type calcium channels . By binding directly to these inactive calcium channels, stabilizes their inactive conformation . This prevents the influx of calcium ions, which are necessary for muscle contraction, thereby causing vasodilation .
Temporal Effects in Laboratory Settings
In laboratory settings, the effects of this compound have been observed to change over time. For instance, in studies with spontaneously hypertensive rats, the reflexogenic increase in heart rate and plasma renin activity subsided within 3 to 5 hours of continuous This compound administration .
Dosage Effects in Animal Models
The effects of this compound have been observed to vary with different dosages in animal models. For example, in studies with spontaneously hypertensive rats, the plasma concentration required for a 20% reduction of mean arterial pressure was approximately 10 nmol .
Metabolic Pathways
This compound: This compound is metabolized by cytochrome P450 (CYP) 3A4 . This metabolic pathway involves the conversion of to dehydrothis compound .
Transport and Distribution
This compound is poorly soluble and undergoes extensive hepatic metabolism, leading to poor oral bioavailability . The development of solid lipid nanoparticles (SLNs) loading this compound has been shown to improve the oral bioavailability by enhancing absorption and reducing first-pass metabolism .
Subcellular Localization
The subcellular localization of this compound is primarily associated with its binding to L-type calcium channels, which are located in the cell membrane . By binding to these channels, This compound stabilizes them in their inactive conformation, preventing the influx of calcium ions into the cell .
Preparation Methods
Felodipine can be synthesized through various methods. One common method involves the dry granulation technique, where powder particles are made to adhere to each other without adding liquids . Another method involves wet granulation, where this compound is mixed with hydroxypropyl methylcellulose and a filler, wetted by a wetting agent, and then granulated . This method is suitable for industrial-scale production due to its high product yield and reduced production cost .
Chemical Reactions Analysis
Felodipine undergoes several types of chemical reactions, including oxidation, reduction, and substitution. It is metabolized by cytochrome P450 3A4, which means substances that inhibit or activate CYP3A4 can significantly affect the amount of this compound present . Common reagents that interact with this compound include cimetidine, erythromycin, itraconazole, and ketoconazole, which increase its availability, and phenytoin, carbamazepine, and rifampicin, which decrease its availability . The major products formed from these reactions are metabolites that are excreted through the renal system .
Comparison with Similar Compounds
Felodipine is part of the dihydropyridine class of calcium channel blockers, which also includes amlodipine, nifedipine, and nicardipine . Compared to these compounds, this compound is unique in its high selectivity for vascular smooth muscle over cardiac muscle . This selectivity makes it particularly effective in reducing peripheral vascular resistance without significantly affecting heart rate .
Properties
IUPAC Name |
5-O-ethyl 3-O-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate |
Source
|
|---|---|---|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
InChI |
InChI=1S/C18H19Cl2NO4/c1-5-25-18(23)14-10(3)21-9(2)13(17(22)24-4)15(14)11-7-6-8-12(19)16(11)20/h6-8,15,21H,5H2,1-4H3 |
Source
|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
InChI Key |
RZTAMFZIAATZDJ-UHFFFAOYSA-N |
Source
|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
Canonical SMILES |
CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C |
Source
|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
Molecular Formula |
C18H19Cl2NO4 |
Source
|
| Source | PubChem | |
| URL | https://pubchem.ncbi.nlm.nih.gov | |
| Description | Data deposited in or computed by PubChem | |
DSSTOX Substance ID |
DTXSID4023042 |
Source
|
| Record name | Felodipine | |
| Source | EPA DSSTox | |
| URL | https://comptox.epa.gov/dashboard/DTXSID4023042 | |
| Description | DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology. | |
Molecular Weight |
384.2 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 | Felodipine | |
| Source | Human Metabolome Database (HMDB) | |
| URL | http://www.hmdb.ca/metabolites/HMDB0015158 | |
| 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 |
7.15e-03 g/L |
Source
|
| Record name | Felodipine | |
| Source | DrugBank | |
| URL | https://www.drugbank.ca/drugs/DB01023 | |
| 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 | Felodipine | |
| Source | Human Metabolome Database (HMDB) | |
| URL | http://www.hmdb.ca/metabolites/HMDB0015158 | |
| 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 |
Felodipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through voltage-gated L-type calcium channels. It reversibly competes against nitrendipine and other DHP CCBs for DHP binding sites in vascular smooth muscle and cultured rabbit atrial cells. Calcium ions entering the cell through these channels bind to calmodulin. Calcium-bound calmodulin then binds to and activates myosin light chain kinase (MLCK). Activated MLCK catalyzes the phosphorylation of the regulatory light chain subunit of myosin, a key step in muscle contraction. Signal amplification is achieved by calcium-induced calcium release from the sarcoplasmic reticulum through ryanodine receptors. Inhibition of the initial influx of calcium decreases the contractile activity of arterial smooth muscle cells and results in vasodilation. The vasodilatory effects of felodipine result in an overall decrease in blood pressure. Felodipine may be used to treat mild to moderate essential hypertension. |
Source
|
| Record name | Felodipine | |
| Source | DrugBank | |
| URL | https://www.drugbank.ca/drugs/DB01023 | |
| 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) | |
CAS No. |
72509-76-3 |
Source
|
| Record name | Felodipine | |
| Source | CAS Common Chemistry | |
| URL | https://commonchemistry.cas.org/detail?cas_rn=72509-76-3 | |
| 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 | Felodipine [USAN:USP:INN:BAN] | |
| Source | ChemIDplus | |
| URL | https://pubchem.ncbi.nlm.nih.gov/substance/?source=chemidplus&sourceid=0072509763 | |
| 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 | Felodipine | |
| Source | DrugBank | |
| URL | https://www.drugbank.ca/drugs/DB01023 | |
| 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 | felodipine | |
| Source | DTP/NCI | |
| URL | https://dtp.cancer.gov/dtpstandard/servlet/dwindex?searchtype=NSC&outputformat=html&searchlist=760343 | |
| Description | The NCI Development Therapeutics Program (DTP) provides services and resources to the academic and private-sector research communities worldwide to facilitate the discovery and development of new cancer therapeutic agents. | |
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| Record name | Felodipine | |
| Source | EPA DSSTox | |
| URL | https://comptox.epa.gov/dashboard/DTXSID4023042 | |
| Description | DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology. | |
| Record name | 3,5-Pyridinedicarboxylic acid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, ethyl methyl ester (9CI) | |
| Source | European Chemicals Agency (ECHA) | |
| URL | https://echa.europa.eu/information-on-chemicals | |
| 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. | |
| Explanation | Use of the information, documents and data from the ECHA website is subject to the terms and conditions of this Legal Notice, and subject to other binding limitations provided for under applicable law, the information, documents and data made available on the ECHA website may be reproduced, distributed and/or used, totally or in part, for non-commercial purposes provided that ECHA is acknowledged as the source: "Source: European Chemicals Agency, http://echa.europa.eu/". Such acknowledgement must be included in each copy of the material. ECHA permits and encourages organisations and individuals to create links to the ECHA website under the following cumulative conditions: Links can only be made to webpages that provide a link to the Legal Notice page. | |
| Record name | FELODIPINE | |
| Source | FDA Global Substance Registration System (GSRS) | |
| URL | https://gsrs.ncats.nih.gov/ginas/app/beta/substances/OL961R6O2C | |
| 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. | |
| Explanation | Unless otherwise noted, the contents of the FDA website (www.fda.gov), both text and graphics, are not copyrighted. They are in the public domain and may be republished, reprinted and otherwise used freely by anyone without the need to obtain permission from FDA. Credit to the U.S. Food and Drug Administration as the source is appreciated but not required. | |
| Record name | Felodipine | |
| Source | Human Metabolome Database (HMDB) | |
| URL | http://www.hmdb.ca/metabolites/HMDB0015158 | |
| 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 |
145 °C |
Source
|
| Record name | Felodipine | |
| Source | DrugBank | |
| URL | https://www.drugbank.ca/drugs/DB01023 | |
| 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 | Felodipine | |
| Source | Human Metabolome Database (HMDB) | |
| URL | http://www.hmdb.ca/metabolites/HMDB0015158 | |
| 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
A: Felodipine is a dihydropyridine calcium channel blocker that selectively inhibits calcium influx into vascular smooth muscle cells by binding to L-type calcium channels. [] This inhibition leads to vasodilation, reducing peripheral vascular resistance and lowering blood pressure. []
A: Unlike some other calcium channel blockers, this compound, in clinically relevant doses, exhibits high selectivity for arteriolar smooth muscle and does not significantly impact cardiac contractility or conduction. []
A: this compound, at clinical doses, does not significantly affect venous smooth muscle, contributing to its lack of orthostatic hypotension as a side effect. []
A: this compound exhibits natriuretic/diuretic effects, counteracting the salt and water retention commonly observed with other potent vasodilators. [, ]
A: Clinical studies demonstrate that this compound is more effective in reducing blood pressure than several established antihypertensive drugs. []
ANone: The molecular formula of this compound is C18H19Cl2NO4, and its molecular weight is 384.25 g/mol.
A: Yes, a PBPK/PD parent–metabolite model of this compound and its metabolite dehydrothis compound has been developed for drug–drug interaction predictions. This model, developed in PK-Sim® and MoBi®, is based on 49 clinical studies and includes diastolic blood pressure and heart rate PD models. []
A: this compound exhibits low oral bioavailability (around 15%) primarily due to extensive first-pass metabolism. [, ]
ANone: Several strategies have been investigated to enhance this compound's solubility and dissolution, including:
- Solid dispersions: Formulations with polyethylene glycol (PEG 4000) and hydroxypropyl cellulose (HPC) have demonstrated significant improvements in this compound's solubility and dissolution rate. []
- Solid dispersion films: this compound incorporated into polyvinylpyrrolidone (PVP) K90 films prepared by solvent evaporation has shown promising results in enhancing dissolution characteristics. []
- Eudragit® RS100 nanoparticles: Nanoparticles formulated with Eudragit® RS100 using the solvent evaporation technique have demonstrated sustained release profiles and reduced burst release compared to pure this compound powder. []
- Eudragit® E-PHB polymeric microparticles: Microparticles containing this compound prepared with Eudragit® E blended with poly(3-hydroxybutyrate) (PHB) showed increased dissolution rates attributed to reduced drug crystallinity. []
- Cryomilling: Co-cryomilling this compound with polymers like hydroxypropyl methylcellulose (HPMC), HPMCAS, Soluplus® R, and PMMA has shown potential in creating amorphous solid dispersions with enhanced dissolution properties without using heat or solvents. []
A: this compound is primarily metabolized by the cytochrome P450 (CYP) 3A4 enzyme in the liver and intestine, leading to the formation of its main metabolite, dehydrothis compound. []
A: this compound undergoes extensive first-pass metabolism, resulting in low and variable oral bioavailability of approximately 15%. [, ]
A: The pharmacodynamic effect of this compound, particularly its antihypertensive action, directly correlates with its plasma concentration. []
A: Yes, coffee consumption can significantly reduce the antihypertensive effect of this compound. This interaction appears to be pharmacodynamic, as coffee doesn't affect this compound's bioavailability but rather induces a pressor effect that counteracts the drug's action. []
A: Yes, ethanol can enhance the hemodynamic effects of this compound, potentially leading to clinically relevant adverse effects, particularly postural hypotension. This interaction does not appear to be due to altered this compound bioavailability. []
A: this compound demonstrates a longer duration of action compared to other dihydropyridines like Nifedipine. In spontaneously hypertensive rats, this compound exhibited an effect lasting 4-6 hours in a steady state, while Nifedipine's effect lasted 1-2 hours. []
ANone: Several animal models have been utilized to study this compound, including:
- Spontaneously hypertensive rats (SHR): this compound demonstrated dose-dependent antihypertensive effects in SHR, proving more potent and longer-acting than Nifedipine. [, , , ]
- DOCA-salt and renal hypertensive (2K1C) rats: this compound exhibited superior antihypertensive effects compared to Nifedipine in these models, showing a greater reduction in blood pressure and longer duration of action. []
- Renal hypertensive (2K2C) dogs: this compound showed a stronger and more sustained antihypertensive effect than Nifedipine in this model. []
ANone: Numerous clinical trials have explored this compound's effectiveness in managing hypertension:
- Monotherapy: this compound, as monotherapy, effectively reduced blood pressure in patients with mild to moderate hypertension. A starting dose of 5 mg once daily was found to be appropriate. [, ]
- Combination therapy: this compound, in combination with beta-blockers, proved to be a suitable alternative to standard triple therapy and effectively managed hypertension in patients refractory to other treatments. [, , , , ]
- Elderly patients: this compound effectively reduced blood pressure in older adults with hypertension and was well-tolerated. Elderly patients appeared to require lower doses for blood pressure control compared to younger patients. [, ]
- Black African patients: this compound demonstrated superior efficacy and tolerability compared to Hydrochlorothiazide in Black African patients with mild to moderate hypertension. This compound achieved faster blood pressure control and had a lower incidence of side effects. []
- Comparison with other antihypertensive agents:
- Prazosin: this compound demonstrated superior blood pressure reduction compared to Prazosin when used as an add-on therapy to beta-blockers in patients with essential hypertension. [, ]
- Losartan: Once-daily administration of this compound ER was found to be as effective as Losartan in blood pressure reduction in Taiwanese patients with mild to moderate hypertension. []
- Aranidipine: Aranidipine (5-20 mg/d) and this compound (5-10 mg/d) showed similar efficacy and safety profiles in Chinese patients with mild-to-moderate essential hypertension. []
A: Yes, a study in hypercholesterolemic rabbits found that low-dose this compound inhibited intimal lesion formation, suggesting a potential anti-atherogenic effect. This effect was associated with improved endothelium-dependent relaxation and reduced endothelial adhesiveness, possibly mediated by increased nitric oxide activity. []
A: A study in patients with exercise-induced asthma showed that a single 10 mg dose of this compound significantly reduced the fall in FEV1 after exercise compared to placebo. This suggests a potential beneficial effect of this compound in exercise-induced bronchoconstriction. []
A: In a study using a pig model of myocardial ischemia and reperfusion, coronary venous retroinfusion of this compound before reperfusion significantly reduced myocardial infarct size and improved myocardial functional recovery compared to the control group. []
A: Researchers investigated the coronary venous retroinfusion of this compound to target drug delivery directly to the heart, achieving higher local concentrations and potentially minimizing systemic side effects. This approach proved successful in reducing myocardial infarct size and improving heart function recovery in a pig model. []
A: Researchers utilized fluorescence spectroscopy to study this compound's binding to calcium-binding proteins. This compound exhibits fluorescence, and its fluorescence intensity changes upon binding to these proteins in a calcium-dependent manner. This approach allowed researchers to determine binding affinities, calcium sensitivities, and allosteric interactions with other drugs. [, , ]
A: Solid dispersions of this compound in various carriers, such as PEG 4000/HPC, PVP K90, and Eudragit® E-PHB, have demonstrated significantly improved dissolution rates compared to pure this compound powder. This enhancement is attributed to factors like reduced particle size, increased drug wettability, and conversion to an amorphous state. [, , ]
ANone: Several factors contribute to the enhanced dissolution of this compound from solid dispersions:
- Reduced particle size: Solid dispersion techniques can reduce drug particle size, increasing surface area and facilitating faster dissolution. []
- Amorphous state: Converting crystalline this compound into an amorphous form in solid dispersions increases its solubility and dissolution rate due to the absence of a lattice energy barrier. [, ]
A: this compound is primarily metabolized by CYP3A4. [] As a sensitive substrate of this enzyme, this compound is susceptible to drug-drug interactions (DDIs) with CYP3A4 inhibitors and inducers. []
ANone: Several drugs have been identified to interact with this compound through CYP3A4 modulation, including:
A: this compound is considered one of the most potent dihydropyridines in relaxing coronary arteries. [] It exhibits high selectivity for arteriolar smooth muscle compared to other members of this class, resulting in fewer cardiac-related side effects. []
ANone: Several alternatives exist depending on the individual patient's needs and response to therapy:
- Angiotensin-converting enzyme (ACE) inhibitors: Drugs like Benazepril, Captopril, and Enalapril provide an alternative mechanism for lowering blood pressure. [, , ]
- Angiotensin II receptor blockers (ARBs): Losartan, Valsartan, and Irbesartan block the action of angiotensin II, a potent vasoconstrictor. [, , ]
- Thiazide diuretics: Hydrochlorothiazide and Chlorthalidone help lower blood pressure by reducing fluid volume. [, , ]
- Beta-blockers: Metoprolol, Atenolol, and Propranolol lower blood pressure by reducing heart rate and contractility. [, , , , , , ]
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