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Wiadomosci Lekarskie (Warsaw, Poland :... 2021Intensive studies on properties of synthetic compounds are simultaneously conducted with studies on the effectiveness and safety of drugs derived from natural compounds.... (Review)
Review
Intensive studies on properties of synthetic compounds are simultaneously conducted with studies on the effectiveness and safety of drugs derived from natural compounds. These drugs have been effectively used for years in dentistry, in treatment of inflammatory conditions of the oral cavity and in laryngology, in treatment of pharyngeal inflammatory conditions. The subject of this article is a compilation of studies conducted on medicinal products containing composed ethanolic extract as an active substance, and obtained from: chamomile capitulum (Matricaria recutita L.), oak bark (Quercus spp.), sage leaf (Salvia officinalis L.), arnica herb (Arnica spp.), calamus rhizome (Acorus calamus L.), peppermint herb (Mentha piperita L.), thyme herb (Thymus spp.) Preclinical studies confirmed that a particular tested plant extract exhibits antimicrobial (antibacterial, antifungal and antiprotozoal) as well as anti-inflammatory, immunomodulatory and astringent properties. Under clinical conditions, it was confirmed that drugs containing the analysed extract used in periodontology, in prevention and complex treatment of gingivitis, periodontitis as well as diseases of oral mucosa (but also the throat) of viral, bacterial, fungal and protozoal aetiology significantly improved the effectiveness of therapy, shortened the treatment and improved the patients' quality of life. The above preparations used in dental surgery contributed to faster tissue regeneration, more quickly relieved pain and swelling after a surgery or difficult dentition. Furthermore, drugs containing the above-mentioned extract can also be successfully used for oral cavity decontamination in the case of various diseases of teeth or the oral and pharyngeal mucosa. The tested composed herbal extract (CHE), applied in the form of a mouthwash and in the form for topical application with benzocaine content (CHEB), is a component of drugs which are great alternatives to widely used synthetic drugs. They are characterised with high effectiveness, comparable to that of synthetic agents, and a higher safety profile. Results of pharmacological and clinical studies justify their use in both prevention and treatment of inflammatory diseases of the gums, periodontium, oral cavity and pharynx.
Topics: Gingivitis; Humans; Mucous Membrane; Pharynx; Plant Extracts
PubMed: 34459780
DOI: No ID Found -
Brazilian Dental Journal 2015Although the use of injectable anesthesia prior to subgingival scaling and root planing (SRP) reduces pain, many patients report fear and prolonged numbness of adjacent... (Comparative Study)
Comparative Study Randomized Controlled Trial
Although the use of injectable anesthesia prior to subgingival scaling and root planing (SRP) reduces pain, many patients report fear and prolonged numbness of adjacent tissues. The aim of the present study was to compare the effects of a eutectic mixture containing 25 mg/g of lidocaine and 25 mg/g of prilocaine, injectable 2% lidocaine, topical 2% benzocaine and a placebo substance on reducing pain during SRP. In this randomized, split-mouth, masked clinical trial, thirty-two patients presenting more than two teeth with probing depth and clinical attachment level ≥ 5 mm in at least 4 sextants were randomly allocated to four groups: EMLA(r); injectable 2% lidocaine; topical 2% benzocaine and placebo. Pain and discomfort were measured using a visual analogue scale (VAS) and verbal scale (VS). Repeated-measures analysis of variance and Poisson regression were used for analysis. Patient satisfaction with the anesthesia was determined at the end of each treatment session. VAS and VS scores did not differ between injectable 2% lidocaine and EMLA (p > 0.05) and both substances showed significantly better pain control compared to 2% benzocaine and placebo (p < 0.05). 93.7% and 81.2% of the individuals were satisfied with the injectable anesthetic and EMLA, respectively (p = 0.158). Dissatisfaction with benzocaine and placebo was approximately 10 times greater than injectable anesthesia (p = 0.001). In conclusion, EMLA showed an equivalent effect on pain control when compared to the injectable anesthesia and performed better than 2% benzocaine in SRP. Thus, EMLA is a viable anesthetic option during scaling and root planning, despite the frequent need for second application.
Topics: Anesthesia, Dental; Anesthesia, Local; Anesthetics, Local; Benzocaine; Dental Scaling; Drug Combinations; Female; Gingivitis; Humans; Lidocaine; Lidocaine, Prilocaine Drug Combination; Male; Middle Aged; Pain Management; Pain Measurement; Patient Satisfaction; Prilocaine; Reproducibility of Results; Root Planing; Treatment Outcome
PubMed: 25672380
DOI: 10.1590/0103-6440201300131 -
Anesthesia Progress 2005A case is reported in which a patient developed methemoglobinemia-induced cyanosis while under general anesthesia during surgery for multiple fascial space infections....
A case is reported in which a patient developed methemoglobinemia-induced cyanosis while under general anesthesia during surgery for multiple fascial space infections. The cause of methemoglobinemia was 20% benzocaine spray used for local anesthesia before intubation. Acutely developing methemoglobinemia is infrequently encountered in clinical practice. When confronted with cyanosis in the absence of cardiac or pulmonary disease, one must seriously consider the diagnosis of methemoglobinemia. The etiology of methemoglobinemia, the causative agents, the diagnosis, and the emergency treatment required are discussed.
Topics: Abscess; Anesthetics, Local; Benzocaine; Cyanosis; Drainage; Enzyme Inhibitors; Female; Humans; Methemoglobinemia; Methylene Blue; Middle Aged; Neck; Peritonsillar Abscess; Pharyngeal Diseases
PubMed: 16596913
DOI: 10.2344/0003-3006(2005)52[136:BM]2.0.CO;2 -
Pharmaceutics Jan 2021The dissolution behavior of novel active pharmaceutical ingredients (API) is a crucial parameter in drug formulation since it frequently affects the drug release....
The dissolution behavior of novel active pharmaceutical ingredients (API) is a crucial parameter in drug formulation since it frequently affects the drug release. Generally, a distinction is made between surface-reaction- and diffusion-controlled drug release. Therefore, dissolution studies such as the intrinsic dissolution test defined in the pharmacopeia have been performed for many years. In order to overcome the disadvantages of the common intrinsic dissolution test, a new experimental setup was developed within this study. Specifically, a flow channel was designed and tested for measuring the mass transfer from a flat, solid surface dissolving into a fluid flowing over the surface with well-defined flow conditions. A mathematical model was developed that distinguishes between surface-reaction- and diffusion-limited drug release based on experimental data. Three different drugs-benzocaine, theophylline and griseofulvin-were used to investigate the mass flux during dissolution due to surface reaction, diffusion and convection kinetics. This new technique shows potential to be a valuable tool for the identification of formulation strategies.
PubMed: 33499428
DOI: 10.3390/pharmaceutics13020146 -
Canadian Medical Association Journal Oct 1981
Topics: Benzocaine; Humans; Infant; Male; Methemoglobinemia; Tooth Eruption
PubMed: 7306890
DOI: No ID Found -
Toxicology Jan 2018According to the new EU Medical Devices (MDR) legislation coming into effect in 2017, manufactures will have to comply with higher standards of quality and safety for...
According to the new EU Medical Devices (MDR) legislation coming into effect in 2017, manufactures will have to comply with higher standards of quality and safety for medical devices in order to meet common safety concerns regarding such products. Metal alloys are extensively used in dentistry and medicine (e.g. orthopedic surgery and cardiology) even though clinical experience suggests that many metals are sensitizers. The aim of this study was to further test the applicability domain of the in vitro reconstructed human epidermis (RhE) IL-18 assay developed to identify contact allergens and in doing so: i) determine whether different metal salts, representing leachables from metal alloys used in medical devices, could be correctly labelled and classified; and ii) assess the ability of different salts for the same metal to penetrate the skin stratum corneum. Twenty eight chemicals including 15 metal salts were topically exposed to RhE. Nickel, chrome, gold, palladium were each tested in two different salt forms, and titanium in 4 different salt forms. Metal salts were labelled (YES/NO) as sensitizer if a threshold of more than 5 fold IL18 release was reached. The in vitro estimation of expected sensitization induction level (potency) was assessed by interpolating in vitro EC50 and IL-18 SI2 with LLNA EC3 and human NOEL values from standard reference curves generated using DNCB (extreme) and benzocaine (weak). Metal salts, in contrast to other chemical sensitizers and with the exception of potassium dichromate (VI) and cobalt (II) chloride, were not identified as contact allergens since they only induced a small or no increase in IL-18 production. This finding was not related to a lack of stratum corneum skin penetration since EC50 values (decrease in metabolic activity; MTT assay) were obtained after topical RhE exposure to 8 of the 15 metal salts. For nickel, gold and palladium salts, differences in EC50 values between two salts for the same metal could not be attributed to differences in molarity or valency. For chrome salts the difference in EC50 values may be explained by different valencies (VI vs. III), but not by molarity. In general, metal salts were classified as weaker sensitizers than was indicated from in vivo LLNA EC3 and NOEL data. Our in vitro results show that metals are problematic chemicals to test, in line with the limited number of standardized human and animal studies, which are not currently considered adequate to predict systemic hypersensitivity or autoimmunity, and despite clinical experience, which clearly shows that many metals are indeed a risk to human health.
Topics: Allergens; Animal Testing Alternatives; Epidermis; Haptens; Humans; Infant, Newborn; Interleukin-18; Local Lymph Node Assay; Male; Metals; No-Observed-Adverse-Effect Level; Toxicity Tests
PubMed: 29079364
DOI: 10.1016/j.tox.2017.10.014 -
Proceedings of the National Academy of... Dec 2018Potency of drug action is usually determined by binding to a specific receptor site on target proteins. In contrast to this conventional paradigm, we show here that...
Potency of drug action is usually determined by binding to a specific receptor site on target proteins. In contrast to this conventional paradigm, we show here that potency of local anesthetics (LAs) and antiarrhythmic drugs (AADs) that block sodium channels is controlled by fenestrations that allow drug access to the receptor site directly from the membrane phase. Voltage-gated sodium channels initiate action potentials in nerve and cardiac muscle, where their hyperactivity causes pain and cardiac arrhythmia, respectively. LAs and AADs selectively block sodium channels in rapidly firing nerve and muscle cells to relieve these conditions. The structure of the ancestral bacterial sodium channel NaAb, which is also blocked by LAs and AADs, revealed fenestrations connecting the lipid phase of the membrane to the central cavity of the pore. We cocrystallized lidocaine and flecainide with NaAb, which revealed strong drug-dependent electron density in the central cavity of the pore. Mutation of the contact residue T206 greatly reduced drug potency, confirming this site as the receptor for LAs and AADs. Strikingly, mutations of the fenestration cap residue F203 changed fenestration size and had graded effects on resting-state block by flecainide, lidocaine, and benzocaine, the potencies of which were altered from 51- to 2.6-fold in order of their molecular size. These results show that conserved fenestrations in the pores of sodium channels are crucial pharmacologically and determine the level of resting-state block by widely used drugs. Fine-tuning drug access through fenestrations provides an unexpected avenue for structure-based design of ion-channel-blocking drugs.
Topics: Anesthetics, Local; Anti-Arrhythmia Agents; Bacteria; Cell Membrane; Crystallography, X-Ray; Ion Channel Gating; Lipid Bilayers; Membrane Potentials; Protein Conformation; Sodium; Sodium Channel Blockers; Voltage-Gated Sodium Channels
PubMed: 30518562
DOI: 10.1073/pnas.1814928115 -
Saudi Medical Journal Nov 2015To investigate the effectiveness of topical anesthetic, 20% benzocaine in relieving pain and stress in patients following deep cavity restoration and extraction of teeth...
OBJECTIVES
To investigate the effectiveness of topical anesthetic, 20% benzocaine in relieving pain and stress in patients following deep cavity restoration and extraction of teeth under local anesthesia (LA).
METHODS
A prospective clinical trial was conducted from October 2014 until April 2015 at Taibah University, Al Madinah Al Munawarah, Kingdom of Saudi Arabia. Forty-five patients were included in the 20% benzocaine group, and 46 in the normal saline group. Evaluation of the dental stress was made pre-operatively and immediately post-operative treatment using the visual analogue scale (VAS). Furthermore, discomfort of the injections were recorded by the patients after each treatment on standard 100 mm VAS, tagged at the endpoints with "no pain" (0 mm) and "unbearable pain" (100 mm).
RESULTS
There were statistically significant differences between the mean stress scores for patients in the benzocaine and normal saline groups post-operatively (p=0.002). There were significant differences between the mean pain scores for patients in the post buccal injection (p=0.001), post palatal injection (p=0.01), and the post inferior alveolar nerve block groups (p=0.02). Buccal, palatal, and inferior alveolar nerve block injections were more painful for patients in the normal saline group than the benzocaine group.
CONCLUSION
This investigation has demonstrated that post-operative stress associated with deep cavity restoration and dental extractions under LA can be reduced by the application of topical anesthetic (20% benzocaine) at the operative site for intra-oral injections.
Topics: Anesthetics, Local; Benzocaine; Dental Restoration, Permanent; Humans; Pain, Postoperative; Tooth Extraction
PubMed: 26593169
DOI: 10.15537/smj.2015.11.12274 -
Pharmaceutics May 2023The availability of sufficient amounts of form I of benzocaine has led to the investigation of its phase relationships with the other two existing forms, II and III,...
The availability of sufficient amounts of form I of benzocaine has led to the investigation of its phase relationships with the other two existing forms, II and III, using adiabatic calorimetry, powder X-ray diffraction, and high-pressure differential thermal analysis. The latter two forms were known to have an enantiotropic phase relationship in which form III is stable at low-temperatures and high-pressures, while form II is stable at room temperature with respect to form III. Using adiabatic calorimetry data, it can be concluded, that form I is the stable low-temperature, high-pressure form, which also happens to be the most stable form at room temperature; however, due to its persistence at room temperature, form II is still the most convenient polymorph to use in formulations. Form III presents a case of overall monotropy and does not possess any stability domain in the pressure-temperature phase diagram. Heat capacity data for benzocaine have been obtained by adiabatic calorimetry from 11 K to 369 K above its melting point, which can be used to compare to results from in silico crystal structure prediction.
PubMed: 37242790
DOI: 10.3390/pharmaceutics15051549 -
International Journal of Dentistry 2018To compare the effectiveness of the topical administration of benzocaine and EMLA on oral pain and tactile sensitivity.
OBJECTIVES
To compare the effectiveness of the topical administration of benzocaine and EMLA on oral pain and tactile sensitivity.
MATERIALS AND METHODS
A randomized, double-blind, split-mouth clinical trial was carried out with 20 volunteers. The sensorial and quantitative tests were applied before the contact with topical anesthetic and after the application.
RESULTS
In the superficial tactile perception test, when we compared each group singly, there were statistically significant values in the decrease of superficial tactile perception when compared to the moment prior to the application of anesthetic agents. For the sensitivity to mechanical pain, no statistical significant difference was observed at evaluated times. In the needle penetration test, in an intergroup analysis, we found a decrease in the pain sensitivity to needle penetration at 5 min (=0.053) and at 10 min (=0.019) after the contact of the anesthetic drug with the oral mucosa.
CONCLUSION
The application of topical anesthetic drugs reduces the discomfort associated with this procedure, mainly until the first 10 minutes. Only the needle penetration sensitivity test showed sufficient sensitivity to reveal a difference in the anesthetic effect between EMLA and benzocaine. This trial is registered with RBR-2N2GSW.
PubMed: 29593794
DOI: 10.1155/2018/7916274