Drug Amoxicillin Research Articles

In silico ADME predictions and in vitro antibacterial evaluation of 2-hydroxy benzothiazole-based 1,3,4-oxadiazole derivatives.

In the present work, a library of fifteen 2-hydroxy benzothiazole-linked 1,3,4 -oxadiazole derivatives have been synthesized and confirmed using different analytical techniques. All of the synthesized compounds have been tested for antibacterial and in silico pharmacokinetic studies for the first time. From the ADME predictions, compound 4 showed the highest in silico absorption percentage (86.77%), while most of the compounds showed more than 70% absorption. All of the compounds comply with the Lipinski rule of 5, suggesting that the compounds possess good drug likeness properties upon administration. Furthermore, all of the compounds follow the Veber rule, indicating good bioavailability and good intestinal absorption. The antibacterial results exhibited excellent to moderate activity. Compounds 5 , 9 , 12 , 14 , 15 , 16 , and 17 were the most active compounds against the tested bacterial strains. Compound 14 showed comparable MIC 6.25 ±0.2 μg/disc to the standard drug amoxicillin against the tested Gram-positive bacterial strains. Compounds 5 , 14 , 17 exhibited MIC 12.5 ±0.8 μg/disc, which was comparable to the standard drug against E. faecalis . It can be concluded that the synthesized compound could be used as a lead molecule in the development of new antibacterial agents with high efficacy.

Amoxicillin Induced Steven Johnson’s Syndrome: A Case Report

Stevens-Johnson syndrome (SJS) is a very rare, potentially fatal skin reaction that is typically the result of reaction to the drug. In particular, SJS is characterized by extensive skin and mucous membrane lesions (i.e. mouth, nose, esophagus, anus, and genitalia), epidermis detachment, and acute skin blisters. In 95 % of case reports, drugs were found to be an important cause for the development of SJS. This story is a case of A 42 year old male hospitalized with rashes all over the body and fever, after oral consumption of Amoxicillin drug for sore throat. This case study discusses the possibility that serious hypersensitivity reactions with Amoxicillin can rarely occur and can be extremely harmful and life-threatening Menacing.
 Keywords: Toxic Epidermal Necrolysis, Stevens Johnson Syndrome, Adverse drug reaction, Nikolsky’s sign

Diffusion and Controlled Release in Physically Crosslinked Poly (Vinyl Alcohol)/Iota-Carrageenan Hydrogel Blends.

This paper reports the obtaining of poly (vinyl alcohol) and ι-carrageenan blend hydrogels by physical crosslinking (consecutive freeze–thaw cycles). The two polymers were completely miscible in the weight ratio interval used in this study, as determined by solution viscometry data. Strong interactions through hydrogen bonding and forming of mixed interpolymer crystalline domains were observed, which are responsible for the formation of stable drug release-tunable matrices. The release profiles of three model antibiotic drugs (amoxicillin, tetracycline hydrochloride, and gentamicin sulfate) were assessed in a pH interval between 3 and 7.3. They were found to be strongly dependent on the drug chemistry, mesh size of the hydrogels, swelling mechanism, and pH of the release medium. A decrease of up to 40% in the release rates and up to 10% in the diffusion coefficients of the model drugs was registered with the increase in ι-carrageenan content.

SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL STUDIES OF METAL(II) COMPLEXES WITH SCHIFF BASE DERIVED FROM 2-AMINOPHENOL AND 2-HYDROXY-6-METHOXY-3-QUINLINECARBOXALDEHYDE

Schiff base derived from 2-aminophenol and 2-hydroxy-6-methoxy-3-quinolinecarboxaldehyde and its Co(II) and Ni(II) complexes were synthesized and characterized by elemental analysis, melting point and decomposition temperature, molar conductivity, IR spectral analysis, AAS analysis, solubility test, and magnetic susceptibility. The FTIR spectral data of the Schiff base determined showed a band at 1622cm-1 which was assigned to the v(C=N), a feature of azomethine group. The same band was observed to shift to lower frequencies 1577 and 1599cm-1 in the complexes suggesting coordination of the Schiff base with the respective metal (II) ions. Molar conductance values 14.58 and 12.65Ω-1cm2mol-1show that the metal complexes were non-electrolytic in nature. The magnetic susceptibility of the complexes were determined and the gram magnetic susceptibility of the complexes were found to be positive, revealing that they are paramagnetic. The elemental analysis of the complexes for C, N and H determined suggested (1:1) metal to ligand ratio. The result of the antimicrobial studiesthat, the metal (II) complexes exhibited higher antibacterial and antifungal activity than the Schiff base but lower than the reference drugs Amoxicillin and Ketoconazole used as control in all cases.

Prediction of Drug Exposure in Critically Ill Encephalopathic Neonates Treated With Therapeutic Hypothermia Based on a Pooled Population Pharmacokinetic Analysis of Seven Drugs and Five Metabolites.

Drug dosing in encephalopathic neonates treated with therapeutic hypothermia is challenging; exposure is dependent on body size and maturation but can also be influenced by factors related to disease and treatment. A better understanding of underlying pharmacokinetic principles is essential to guide drug dosing in this population. The prospective multicenter cohort study PharmaCool was designed to investigate the pharmacokinetics of commonly used drugs in neonatal encephalopathy. In the present study, all data obtained in the PharmaCool study were combined to study the structural system specific effects of body size, maturation, recovery of organ function, and temperature on drug clearance using nonlinear mixed effects modeling. Data collected during the first 5 days of life from 192 neonates treated with therapeutic hypothermia were included. An integrated population pharmacokinetic model of seven drugs (morphine, midazolam, lidocaine, phenobarbital, amoxicillin, gentamicin, and benzylpenicillin) and five metabolites (morphine‐3‐glucuronide, morphine‐6‐glucuronide, 1‐hydroxymidazolam, hydroxymidazolam glucuronide, and monoethylglycylxylidide) was successfully developed based on previously developed models for the individual drugs. For all compounds, body size was related to clearance using allometric relationships and maturation was described with gestational age in a fixed sigmoidal Hill equation. Organ recovery after birth was incorporated using postnatal age. Clearance increased by 1.23%/hours of life (95% confidence interval (CI) 1.03–1.43) and by 0.54%/hours of life (95% CI 0.371–0.750) for high and intermediate clearance compounds, respectively. Therapeutic hypothermia reduced clearance of intermediate clearance compounds only, by 6.83%/°C (95% CI 5.16%/°C–8.34%/°C). This integrated model can be used to facilitate drug dosing and future pharmacokinetic studies in this population.

SYNTHESIS, ANTIBACTERIAL ACTIVITY AND DOCKING STUDIES OF BENZYL ALCOHOL DERIVATIVES

Benzyl alcohol derivatives were synthesized, and characterized using NMR and FTIR spectroscopic techniques. For the first time, the antibacterial activities of the synthesized compounds were examined using disc diffusion method by measuring the diameter of the zones of inhibition against Staphylococcus aureus and Pseudomonas aeruginosa. The results demonstrated that the activity was concentration dependant, and that the compounds were generally potent against P. aeruginosa. Only two of the compounds were active against S. aureus. In terms of broad spectrum activity, compound 2d (35 mm) was found to exhibit a promising efficacy which surpassed that of the standard drug (amoxicillin).The binding of compounds 2a-e to the glucosamine-6-phosphate synthase (GlcN-6-P) active-site revealed that all the synthesized compounds fitted into the GlcN-6-P active-site receptor cavity, exhibited potential hydrogen-bonding interactions with the proximal amino acid residues and aligned similar to amoxicillin. Interestingly, it has been found that the most active compound, 2d also appeared to have a relatively low binding energy (-52.8901 kcal/mol).

Amoxicillin-induced crystal nephropathy: A nationwide French pharmacovigilance databases study.

Amoxicillin (AMX)-induced crystal nephropathy (AICN) is a rarely reported adverse drug reaction (ADR) but its increase has been recently reported in the Paris area. Our aim was to investigate the incidence, characteristics and outcome of AICN in France. Retrospective analysis of all AICN cases reported to the French National Pharmacovigilance Database and the Marketing Authorization Holders Pharmacovigilance Database. AICN notification rate was compared to intravenous AMX and AMX-clavulanate sales. In total, 101 AICN cases were included. Intravenous AMX/AMX-clavulanate was prescribed as surgical prophylaxis (32 surgical patients) or to treat infection (69 medical patients). AKI KDIGO stage 3 was observed in 70 patients and 24/70 patients required renal replacement therapy and/or intensive care unit admission. The annual notification rate of AICN was increased by a factor of 13 since 2010 (6 [0;7] and 77 [24;111] cases per 100 000 patient-years of exposure, before and after 2010 respectively; P < .001). In surgical patients, the increase in AICN has been reported since 2010 and was mainly related to inadequate AMX administration. In medical patients, the increase in AICN was observed since 2014. After 2014, medical patients were older (67 [42;77] vs 74 years [64;84] respectively; P < .05) and were treated more frequently for endocarditis (0/20 vs 15/49 respectively; P < .01). A contributing factor was observed or suspected in 62 patients. AICN is a severe ADR that dramatically increased in France since 2010. Assessment of AICN contributing factors and AMX drug monitoring in patients receiving high dose of AMX could reduce the risk of AICN.

Spectrophotometric and Colorimetric Determination of Pharmaceutical by Oxidative Coupling Reaction: A Review

The expansion of the pharmaceuticals imparted a revolt in health human.These pharmaceuticals would avail their sake only if they are liberated from pollution and used in amount suitable. Create pharmaceuticals avail their purpose several instrumental and chemical way were developed at uniform period which are include in the determination of pharmaceuticals. A simple, selective and sensitive spectrophotometric way has been advanced for the quantitative determination of several antibiotic drugs The way was based on the reaction of coupling oxidative drug organic with reagent in thefound of oxidizing agent to give colored product the absorbance of which is observed at wavelengths. The reactions of the Oxidative coupling recently utilized for determination spectrophotometric of different drugs such as thiamine hydrochloride (THC), salbutamol, phenylephrine, folic acid, catecholamine and amoxicillin drugs.

Study of Molecular Interaction for Antibiotic Drug with Sugar Solutions at Different Temperature

The interactions of drug amoxicillin with maltose or galactose solutions with a variation of temperature have been discussed by taking in the volumetric and viscometric procedures. Physical properties [densities (ρ) and viscosities (η)] of amoxicillin (AMOX) aqueous solutions and aqueous solutions of two type saccharides (maltose and galactose 0.05m) have been measured at T = (298.15, 303.15 and 308.15) K under atmospheric pressure. The apparent molar volume (ϕv cm3mole-1) has been evaluated from density data and fitted to a Redlich-Mayer equation. The empirical parameters of the Mayer-Redlich equation and apparent molar volume at infinite dilution Ø°v were explicated in terms of interactions from type solute-solvent and solute–solute interactions. Transfer molar volume ΔtraØ°v for AMOX from water to aqueous maltose and galactose solutions were calculated to comprehend different interactions in the ternary solutions. Limiting apparent molar expansibility (Ø°E) and Hepler’s coefficient was also calculated to indicate the structure making ability of AMOX in the ternary solutions. Jones–Dole coefficient B and A have been calculated from viscosity data by employing the Jones–Dole equation. The free energy of activation of viscous flow per mole of the solute (Δμ°2*) and solvent (Δμ°1*) have been explained on the basis of the Eyring and Feakins equation.

Synthesis and evaluation of antibacterial and antioxidative activities of carbazole derivatives

Seven compounds were synthesized by known methods, and their antibacterial activity was evaluated against Bacillus subtilis and Escherichia coli using a disk diffusion method. Antioxidative activity was evaluated using free 1,1-diphenyl-2-picryl-hydrazyl radical scavenging assay and ferric reducing antioxidant power methods. The disk diffusion method revealed that 6 out of 7 tested compounds showed antibacterial activity against tested strains, they inhibited the growth of bacteria at various concentrations, from 31.25 to 250 μg/ml. 3-Cyano-9H-carbazole, 3-iodo-9Hcarbazole and 3,6-diiodo-9H-carbazole showed a stronger antibacterial activity against Bacillus subtilis compared to the reference drug amoxicillin. 1,3,6-Tribromo-9H-carbazole showed a stronger activity against Escherichia coli. All tested compounds showed a weak antioxidative activity by the 1,1-diphenyl-2-picryl-hydrazyl radical scavenging assay and ferric reducing antioxidant power assay methods.

Amoxicillin induced toxic epidermal necrolysis

Toxic epidermal necrolysis (TEN) is a rare life-threatening adverse drug reaction associated with mucocutaneous eruptions and peeling of skin (sloughing) mostly caused by drugs like sulphonamides, beta lactams, carbamazepine and non-steroidal anti-inflammatory drugs (NSAIDs). Amoxicillin is a broad spectrum, bactericidal, Beta-lactam antibiotic used in treatment of various infections. Here by we have reported the case of amoxicillin induced severe toxic epidermal necrolysis. A Patient admitted in the hospital with the symptoms of epidermal sloughing that resulted in bare dermis as he received Amoxicillin drug for his diagnosis of fever. After clear examination TEN was confirmed and suspected with the cause due to Amoxicillin. The drug was stopped and patient was treated with other drugs for symptomatic cure. The patient was recovered from his condition and improved significantly.

Determination of drug loading efficiency of nano capsules formed by the O/W emulsification of block copolymer

The self-assembly nature of pluronic triblock copolymers have been exploited by materials scientists in the field of drug delivery. We have used Pluronic P123 block copolymer to load an antibiotic drug Amoxicillin and have analyzed the drug loading efficiency. The amphiphilic nature and micellization of Pluronic P123block copolymer was efficiently utilized and the morphology of drug loaded block copolymer is analyzed in detail and correlated with the loading efficiency. Moreover this study also focuses on the antimicrobial activities of the amoxicillin loaded Pluronic P123block copolymer. It is seen that the micelle serve as excellent payloads for the delivery of the most common drug amoxicillin.

Synthesis and Characterization of Sintered Sr/Fe-Modified Hydroxyapatite Bioceramics for Bone Tissue Engineering Applications

In the current study, Sr/Fe co-substituted hydroxyapatite (HAp) bioceramics were prepared by the sonication-assisted aqueous chemical precipitation method followed by sintering at 1100 °C for bone tissue regeneration applications. The sintered bioceramics were analyzed for various structural and chemical properties through X-ray diffraction, scanning electron microscopy, and Fourier transform infrared spectroscopy, which confirmed the phase purity of HAp and Sr/Fe co-substitution into its lattice. The Vickers hardness measurement, high blood compatibility (less than 5% hemolysis), and ability to support the adhesion, proliferation, and osteogenic differentiation of human mesenchymal stem cells suggest the suitability of Sr/Fe:HAp bioceramics for bone implant applications. The physicochemical analysis revealed that the developed Sr/Fe:HAp bioceramics exhibited a polyphasic nature (HAp and βTCP) with almost identical structural morphology having a particle size less than 0.8 μm. The dielectric constant (ε') and dielectric loss (ε″) were potentially affected by the incorporated foreign ions together with the polyphasic nature of the material. The Sr/Fe co-substituted samples demonstrated extended drug (5-fluorouracil and amoxicillin) release profiles at the pH of physiological medium. The multifunctional properties of the developed HAp bioceramics enabled them to be an auspicious candidate for potential biomedical applications, including targeted drug-delivery applications, heating mediator in hyperthermia, and bone tissue repair implants.

Controlled release of amoxicillin and antioxidant potential of gold nanoparticles-xanthan gum/poly (Acrylic acid) biodegradable nanocomposite

In the present study, the green microwave assisted synthesis of gold nanoparticles imbedded in XG/Poly(AA) biodegradable nanocomposite for controlled delivery of amoxicillin has been reported. The evidence of in-situ synthesis of gold nanoparticles by plant extract of Nepeta leucophylla as reducing agent inside the polymer matrix, grafting of acrylic acid (AA) onto backbone XG, surface morphology, crystallinity, thermal properties and loading of amoxicillin inside the MW-AuNPs/XG/Poly(AA) nanocomposite are investigated using various characterization techniques, such as, UV–Vis, XRD, FTIR, TGA/DSC, FE-SEM, EDX, TEM, DLS and Nitrogen adsorption-desorption isotherms (BET studies). The biodegradation test of synthesized nanocomposite has been performed by soil burial method for 75 days. The evidence of biodegradability of MW-AuNPs/XG/Poly(AA) nanocomposite is confirmed by FTIR and FE-SEM micrographs. The release profiles of amoxicillin drug from synthesized nanocomposite has been investigated for different pH (2.4, 7.0 and 9.2) at 37°C using Korsmeyer–Peppas model. Here, the maximum drug loading efficiency is found to be about 85% and release of drug is large in basic medium as compare to acidic and neutral. It is expected that the present work may provide a noble method for synthesis of biodegradable nanocomposite with decent antioxidant potential for controlled release of amoxicillin.

Ion Exchange of Benzoate in Ni-Al-Benzoate Layered Double Hydroxide by Amoxicillin

AbstractThe Ni-Al-NO3 layered double hydroxide (LDH) compound has been intercalated with benzoate anion through an anion exchange process for amoxicillin drug adsorption. The purpose of this research is to synthesize Ni-Al-NO3, ion exchange with benzoate anion to form Ni-Al-Benzoate, and then applying it as an adsorbent of amoxicillin. The adsorption process was carried out using the batch technique. The materials synthesized in this study were characterized by Fourier Transform Infrared Spectroscopy (FT-IR), X-ray ray diffraction (XRD), and Thermogravimetric Analysis/Differential Thermal Analysis (TGA/DTA). The exchange of benzoate in Ni-Al-Benzoate LDH by amoxicillin was followed by UV-Vis spectrophotometry. The pH, LDH amount, and contact time are optimized. The adsorption of amoxicillin by Ni-Al-Benzoate is fit to the pseudo-second-order kinetics model, with an adsorption capacity of 40 mg/ g. The results showed that anion exchange was successfully carried out between benzoate anion and amoxicillin.

Removal of Pharmaceutical Amoxicillin drug by using (CNT) decorated Clay/ Fe2O3 Micro/Nanocomposite as effective adsorbent: Process optimization for ultrasound-assisted adsorption

Removal of Pharmaceutical Amoxicillin drug by using (CNT) decorated Clay/ Fe2O3 Micro/Nanocomposite as effective adsorbent: Process optimization for ultrasound-assisted adsorption

Colorimetric determination of Amoxicillin using 4-Aminoantipyrine and the effects of different parameters

The wide utilize of antibiotics has led to spreading of antibiotics resistance among bacterial populations and reducing the effectiveness of antibiotics. However, most of the administrated antibiotics enter the environmental matrixes through direct runoff and excretion of feces or urine as unchanged original drugs, active metabolites and/or degradation products. Amoxicillin is one of the most valuable and highly consumed antibiotics. Thus, amoxicillin removal from pharmaceutical wastes offers many economic and environmental benefits. Therefore, the aim of current study was to characterize an identification method for amoxicillin and to study the effects of different parameter such as order of addition, nature of the complex, temperature and effect of concentration and type of the base. A spectrophotometric, selective and sensitive method has been proposed for the determination of Amoxicillin. The method is based on the oxidation of potassium ferricyanide and coupling of the oxidized product with the reagent, 4- aminoantipyrine, to give intensely colored complex that absorbs light strongly in the spectral region of 509nm at room temperature. The results found that the order of addition, drug (Amoxicillin)- potassium ferricyanide –base-4- aminoantipyrine, gave highest absorbance and sensitivity, the best base was NaOH (0.1N) needful for developing the colored product and increase its stability. That complex, at 25°C, gave a preferable sensitivity and was selected for further use in this study. Under the proposed optimum conditions, Beer’s law was conform in the concentration range of ( 5-100 mg L−1). Good linearity (r2=0.9994). Calculation of standard error, limit of detection (LOD) (signal/noise = 3), accuracy and precision (RSD%) better than 1%. The utilized method seemed simple, rapid, reproducible and accurate. In addition, it is applicable for the assay of the drug under investigation in various dosage forms and the results are in very good concord with those obtained in previous studies.

Reviewing the Mechanistic Evidence Assessors E-Synthesis and EBM+: A Case Study of Amoxicillin and Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS).

Basic science has delivered unprecedented insights into intricate relationships on the smallest scales within well-controlled environments. Addressing pressing societal decision problems requires an understanding of systems on larger scales in real-world situations. To assess how well the evidence assessors E-Synthesis and EBM+ assess basic science findings to support medical decision making. We demonstrate the workings of E-Synthesis and EBM+ on a case study: the suspected causal connection between the widely-used drug amoxicillin (AMX) and the putative adverse drug reaction: Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS). We determine an increase in the probability that AMX can cause DRESS within the E-Synthesis approach and using the EBM+ standards assess the basic science findings as supporting the existence of a mechanism linking AMX and DRESS. While progress is made towards developing methodologies which allow the incorporation of basic science research in the decision making process for pressing societal questions, there is still considerable need for further developments. A continued dialogue between basic science researchers and methodologists, philosophers and statisticians seems to offer the best prospects for developing and evaluating continuously evolving methodologies.

Physico-chemical properties and antibacterial drug performance of amoxicillin from streets in Bamenda, Cameroon

Background: The advent of microbial drug resistance creates a concern about the quality of anti-infective drugs. The rise in some microbial resistance to therapy has urged us to investigate physico-chemical properties and antibacterial performance of amoxicillin from streets in Bamenda, Cameroon.Methods: Amoxicillin samples were purchased from street vendors in Bamenda. Cameroon. Visual inspection was done for defects and signs of discoloration, deterioration or other physical disfiguration. Weight uniformity test for each sample of antibiotic tablet was carried out. The time for drug disintegration for each sample of amoxicillin was evaluated. Microbial antibiotic susceptibility tests were done using both the agar disc diffusion and micro well broth dilution methods to check drug performance. Data analysis was done and comparison checked with Student-Newman-Keuls at p&lt;0.05.Results: The mean weight of amoxicillin drugs ranged from 632.00±11.5 to 748.06±17.9 mg. Tablets from Austria had a significant decrease in weight compared to those from Germany and Nigeria. This was similar with the capsules from India and China. Average disintegration varied significantly from as small as 2.2 to 14.4 minutes. All the amoxicillin samples were active against the tested bacteria with mean zones of inhibitions ranging from 8.33±0.57 to 39.33±0.57 mm. The MICs and MBCs values range from 1 to 64 µg/ml. For the same bacterium the growth inhibitory effects of the various drugs were not all similar.Conclusions: Some of the amoxicillin samples studied in this paper showed significant differences in their weights and performances (antibacterial activities). Probably the required amount of API was not respected.

Antimicrobial Activity of Substituted Benzopentathiepin-6-amines

A number of substituted benzopentathiepin-6-amines and their analogues without a polysulfur ring were synthesized and evaluated in vitro for antimicrobial activity against a panel of reference bacterial and fungal strains. Trifluoroacetamide 14 demonstrated high antibacterial activity against Staphylococcus aureus (MRSA strain) with a MIC of 4 μg/mL, which was four-fold higher than the activity of a reference drug amoxicillin. This compound was also most active against the Candida albicans fungus (MIC of 1 μg ml-1), whereas amide 17 containing a morpholine substituent was most active against the Cryptococcus neoformans fungus (MIC of 2 μg ml-1). These compounds have no hemolytic activity and are low cytotoxic. Replacement of the pentathiepine ring with 1,3-dithiolan-2-one or 1,3-dithiolane moieties leads to loss of antimicrobial activity. Based on the QSAR analysis and molecular docking data, bacterial DNA ligase might be one of the targets for the antibacterial activity of substituted benzopentathiepin-6-amines against S. aureus.