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Topic Review
Chromatographic Techniques in Pharmaceutical Analysis
High-performance liquid chromatography (HPLC) is an incredibly universal tool, especially when combined with different detectors, such as UV-Visible spectroscopy, mass spectrometry (MS), and fluorescence detection for numerous active ingredients in different pharmaceutical formulations without interferences from other excipients. TLC, in combination with densitometry, is a very efficient tool for the determination of biologically active substances present in pharmaceutical preparations. In addition, TLC coupled to densitometry and mass spectrometry could be suitable for preliminary screening and determination of the biological activity (e.g., antioxidant properties, thin layer chromatography (TLC) by 2,2-diphenyl-1-picrylhydrazyl (DPPH) method) of plant materials. Gas chromatography, coupled with a mass spectrometer (GC-MS, GC-MS/MS), is of particular importance in the testing of any volatile substances, such as essential oils. LC, coupled to NMR and MS, is the best solution for identifying and studying the structure of unknown components from plant extracts, as well as degradation products (DPs). Thanks to size-exclusion chromatography, coupled to multi-angle light scattering, the quality control of biological pharmaceuticals is possible.
  • 5.5K
  • 26 Apr 2022
Topic Review
Oxadiazole
Nowadays, an increasing number of heterocyclic-based drugs found application in medicinal chemistry and, in particular, as anticancer agents. In this context, oxadiazoles—five-membered aromatic rings—emerged for their interesting biological properties
  • 5.0K
  • 29 Apr 2021
Topic Review
Natural Phenols
Phenols are widespread in nature, being the major components of several plants and essential oils. Natural phenols’ anti-microbial, anti-bacterial, anti-oxidant, pharmacological and nutritional properties are, nowadays, well established. Hence, given their peculiar biological role, numerous studies are currently ongoing to overcome their limitations, as well as to enhance their activity.
  • 4.9K
  • 29 Sep 2021
Topic Review
1,2,4-Triazoles
Compounds containing the 1,2,4-triazole ring in their structure are characterised by multidirectional biological activity.
  • 4.8K
  • 23 Aug 2021
Topic Review
Functionalization of Cyclodextrins
Cyclodextrins (CDs) are cyclic oligosaccharides bearing several glucopyranose residues connected by α-1,4 glycosidic bonds. Natural cyclodextrins contain six, seven, or eight glucopyranose units (α-, β- and γ-cyclodextrin, respectively) and are natural products, biodegradable, and generally lacking in toxicity. Cyclodextrins have toroidal shapes, with the smaller opening of the toroid (primary rim) corresponding to the C6-OH primary hydroxyls and the larger opening (secondary rim) to the C2-OH and C3-OH secondary hydroxyls. 
  • 4.7K
  • 17 Oct 2023
Topic Review
CYP3A4
CYP3A4 is a low specificity isoenzyme of the CYPs family, which contributes to the metabolism of approximately 50% of all marketed drugs. Induction or inhibition of CYP3A4 activity results in the varied oral bioavailability and unwanted drug-drug, drug-food, and drug-herb interactions.
  • 4.7K
  • 01 Sep 2021
Topic Review
Pharmaceutical Hydrates Analysis
This entry discusses a set of instrumental and computational methods that are used to characterize hydrated forms of APIs (active pharmaceutical ingredients). The focus has been put on highlighting advantages as well as on presenting some limitations of the selected analytical approaches. This has been performed in order to facilitate the choice of an appropriate method depending on the type of the structural feature that is to be analyzed, that is, degree of hydration, crystal structure and dynamics, and (de)hydration kinetics. The presented techniques include X-ray diffraction (single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD)), spectroscopic (solid state nuclear magnetic resonance spectroscopy (ssNMR), Fourier-transformed infrared spectroscopy (FT-IR), Raman spectroscopy), thermal (differential scanning calorimetry (DSC), thermogravimetric analysis (TGA)), gravimetric (dynamic vapour sorption (DVS)), and computational (molecular mechanics (MM), Quantum Mechanics (QM), molecular dynamics (MD)) methods. Further, the successful applications of the presented methods in the studies of hydrated APIs as well as studies on the excipients’ influence on these processes have been described in many examples.
  • 4.6K
  • 19 Oct 2020
Topic Review
Copper in the Human Body
Copper, an essential trace element found in the brain, liver, and kidneys, enables the body to form red blood cells, maintain bone health, and can help prevent cardiovascular disease and osteoporosis. Copper is also a key element in maintaining lung function as it plays a vital role in metabolic processes such as cellular respiration.
  • 4.5K
  • 26 Jan 2021
Topic Review
Pseudoephedrine
Pseudoephedrine (PSE) is a drug with a long history of medical use; it is helpful in treating symptoms of the common cold and flu, sinusitis, asthma, and bronchitis.
  • 4.4K
  • 29 Jun 2021
Topic Review
Papaverine and Its Mechanism of Action
Papaverine has been proven to be a high-value opioid alkaloid in the field of therapeutics either in solitude or in combination with other metabolites/molecules. Pharmacological research has revealed that papaverine demonstrates a variety of biological activities, including activity against erectile dysfunction, postoperative vasospasms, and pulmonary vasoconstriction, as well as antiviral, cardioprotective, anti-inflammatory, anticancer, neuroprotective, and gestational actions.
  • 4.2K
  • 07 Apr 2023
Topic Review
Acetylsalicylic Acid History and Structure
Aspirin (ASA, acetylsalicylic acid ATC code: N02BA01, DrugBank ID: DB00945, brand names: Arthritis Pain, Aspi-Cor, Aspirin 81, Aspirin-Low, Bayer Plus, Bufferin, Ecortin, Eciprin, Miniprin, Vazalore), is one of the first drugs to be obtained by synthesis. It is regarded as, being the most used drug with the longest lasting commercial success.
  • 4.2K
  • 06 Dec 2022
Topic Review
The Mechanisms of Clozapine-Induced Neutropenia
Despite its severe adverse effects, such as agranulocytosis, clozapine is the primary treatment for treatment-resistant schizophrenia. Clozapine is the gold standard for treatment-resistant schizophrenia. It was discovered over a half-century ago by researchers at Wander AG, a Swiss pharmaceutical company. After a decade, the use of clozapine began to fade away due to its alarming side effect but was re-introduced in the year 1989 for the treatment of refractory psychosis. Numerous comparative studies between clozapine and other antipsychotics have reported superior efficacy of clozapine in treatment-resistant schizophrenia.
  • 4.1K
  • 10 Nov 2021
Topic Review
Medicinal Value of Dandelion
The genus Taraxacum is part of the Asteraceae family of the Cichorioideae subfamily, Lactuceae tribe. This plant's geographical distribution is usually around the warm areas of the Northern Hemisphere and its users have been cherishing it for its curative properties since ancient times. Reports show that traditional medicine practitioners used Taraxacum officinale L. for treating dyspepsia, spleen, liver disorders, hepatitis, and anorexia. Aqueous extracts of dandelion were also used traditionally through Asia, Europe, and North America for treating different types of cancer like leukemia and breast cancer, even if their working mechanisms were unknown. The main reported components of dandelions consist of phenolic acids (chicoric, caffeic, and chlorogenic acids), terpenes (taraxacoside, ainslioside, taraxinic acid), and storage carbohydrates (inulin), which are thought to be accountable for the plant’s health-related properties. This entry is based on a literature review and highlights the beneficial and therapeutic action of dandelion extracts and their confirmed or hypothesized mechanism of action in diabetes, hepatic disorders, and cardiovascular disease, as indicated by the results of in vivo an in vitro studies, on cell lines, human and animal models.
  • 4.1K
  • 10 May 2021
Topic Review
Ketamine and Driving, Cognitive, and Motor Ability
Ketamine is a medication that has many medical purposes but also has been used illicitly by people for its dissociative properties. While driving under the influence of drugs, drivers are more likely to be involved in and cause more accidents than drivers who do not drive under the influence.  A study with ketamine and a ketamine-like medication, rapasitnel, showed that those who were given ketamine experienced more sleepiness and had decreased self-reported motivation and confidence in their driving abilities. Moreover, there seem to be significant differences in the acute versus persistent effects of ketamine, as well as the anesthetic versus subanesthetic doses, both in terms of effects and outcomes. These divergent effects complicate the clinical uses of ketamine, specifically involving driving, drowsiness, and cognitive abilities. 
  • 4.0K
  • 16 Mar 2023
Topic Review
Methotrexate
Methotrexate (MTX), a structural analogue of folic acid, that inhibits cell division (mainly in the S phase of the cell cycle) is commonly used for the treatment of many cancers as well for severe and resistant forms of autoimmune pathologies and inflammatory disorders. This paragraph of clinical overview presents state of knowledge with regards to different pathways of MTX active transport system, mechanisms of action and its applications as immunosuppressive drug and anticancer agent.  
  • 4.0K
  • 28 Oct 2020
Topic Review
Phospholipids
Phospholipids are unique and versatile molecules. They are of natural occurrence and the main components in cellular membranes. Arranged as a lipid bilayer, phospholipids play a significant role in the structure and functionality of biological membranes. They are amphiphilic and consist of a hydrophilic headgroup and a lipophilic/hydrophobic tail.
  • 4.0K
  • 04 Feb 2021
Topic Review
Food–Drug Interactions with Fruit Juices
Fruit juices contain a large number of phytochemicals that, in combination with certain drugs, can cause food–drug interactions that can be clinically significant and lead to adverse events. The mechanisms behind such interactions are in most cases related to phytochemical interference with the activity of cytochrome P450 metabolizing enzymes (CYPs) or drug transporters. Moreover, alterations in their activity can have a clinical relevance if systemic exposure to the drug is decreased or increased, meaning that the pharmacological drug effects are suboptimal, or the drug will cause toxicity. In general, the common pharmacokinetic parameters found to be altered in food–drug interactions regarding fruit juices are the area under the concentration–time curve, bioavailability, and maximum plasma concentration. In most cases, the results from the drug interaction studies with fruit juices provide only limited information due to the small number of subjects, which are also healthy volunteers. Moreover, drug interactions with fruit juices are challenging to predict due to the unknown amounts of the specific phytochemicals responsible for the interaction, as well as due to the inter-individual variability of drug metabolism, among others. Therefore, this work aims to raise awareness about possible pharmacological interactions with fruit juices. 
  • 4.0K
  • 29 May 2021
Topic Review
Pomegranate Juice for CYP3A4- and CYP2C9-Mediated Drugs Metabolism
The Punica granatum L. (pomegranate) fruit juice contains large amounts of polyphenols, mainly tannins such as ellagitannin, punicalagin, and punicalin, and flavonoids such as anthocyanins, flavan-3-ols, and flavonols. These constituents have high antioxidant, anti-inflammatory, anti-diabetic, anti-obesity, and anticancer activities. Because of these activities, many patients may consume pomegranate juice (PJ) with or without their doctor’s knowledge. This may raise any significant medication errors or benefits because of food-drug interactions that modulate the drug’s pharmacokinetics or pharmacodynamics. 
  • 4.0K
  • 18 May 2023
Topic Review
Plants as anti-inflammatory drugs
Plants represent the main source of molecules for the development of new drugs, which intensifies the interest of transnational industries in searching for substances obtained from plant sources, especially since the vast majority of species have not yet been studied chemically or biologically, particularly concerning anti-inflammatory action. Anti-inflammatory drugs can interfere in the pathophysiological process of inflammation, to minimize tissue damage and provide greater comfort to the patient. Therefore, it is important to note that due to the existence of a large number of species available for research, the successful development of new naturally occurring anti-inflammatory drugs depends mainly on a multidisciplinary effort to find new molecules. Although many review articles have been published in this regard, the majority presented the subject from a limited regional perspective.
  • 3.9K
  • 25 Aug 2020
Topic Review
Glutamatergic System in Depression
Major depressive disorder (MDD) is a heterogeneous neuropsychological disorder characterized by a combination of symptoms that negatively impact the productivity and well-being of inflicted patients, including impairments in cognition, emotional regulation, memory, motor function, motivation, and possible suicidal ideation. Glutamate is the major excitatory neurotransmitter in the central nervous system. It plays an important role in several physiological functions.
  • 3.9K
  • 11 May 2022
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