Pharmacology & Pharmacy

Journal Information
ISSN / EISSN : 2157-9423 / 2157-9431
Current Publisher: Scientific Research Publishing, Inc. (10.4236)
Total articles ≅ 635
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Latest articles in this journal

Michel Tagliati, Marianna Leopoulou, Jo Ann LeQuang, Charles E. Wollmuth, Joseph V. Pergolizzi, Kailyn Mitchell, Peter Magnusson
Pharmacology & Pharmacy, Volume 12, pp 10-24; doi:10.4236/pp.2021.121002

Introduction: The inflammatory mechanisms of COVID-19 suggest that corticosteroids may be beneficial, but their benefits must outweigh their potential risks. The RECOVERY trial results suggest that dexamethasone 6 mg/day (but not other steroids) may confer mortality benefits on ventilated COVID-19 patients. Methods: This is a narrative review of the literature about the use of ciclesonide and dexamethasone for COVID-19 patients. Literature is being created rapidly and this review is offered as a state-of-the-science narration. Results: The SARS-CoV-2 virus is an RNA virus whose RNA is transcribed via open reading frames, making its elimination difficult. Coronaviruses have evolved multiple strategies for proteolytic activation of the spike; viral replication occurs entirely in the cytoplasm. In this connection, the RNA-cleaving endoribonuclease (NSP-15 also known as EndoU) may play a key role by facilitating viral double-stranded RNA recognition by the host’s macrophages. Furthermore, the virus is able to undergo RNA recombination rapidly, enabling it to evade host immunity and develop drug resistance. Ciclesonide is an inhaled corticosteroid that reduces lung inflammation and blocks the activity of specific kinases which may explain its anti-inflammatory effect. Dexamethasone is known to reduce mortality in ventilated COVID-19 patients. Discussion: Systemic corticosteroids were used in previous coronavirus epidemics (SARS and MERS) and pulmonary histology of these patients is similar to those in COVID-19 patients. Acute respiratory distress syndrome is the main cause of death in most COVID-19 infections and steroids may be effective in addressing that condition, brought on by cytokine storm. However, it should be noted that inhaled steroids likely have a narrower window for effect than systemic regimens. Conclusion: Dexamethasone has been proven to confer mortality benefits on ventilated COVID-19 patients and may be used with inhaled ciclesonide, which has few side effects and can be locally metabolized. Further study is needed.
Sohel Rana, Maruf Hasan, Eshak Enan, Fatema-Tuz Zohora, A. T. M. Zafrul Azam
Pharmacology & Pharmacy, Volume 12, pp 25-41; doi:10.4236/pp.2021.121003

Coronavirus infectious disease 2019 (COVID-19) first reported in Wuhan, China, causes serious respiratory illnesses such as lung failure and pneumonia. Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) the pathogenic agent of COVID-19 has been confirmed as a novel coronavirus. WHO announced COVID-19 a global pandemic and now the whole world is eagerly waiting for vaccines and therapeutic treatment to get rid of this unstoppable coronavirus. As COVID-19 infection, a global threat creates unwanted human casualties and serious economic loss. To stop the ongoing uncontrolled situation researchers are racing to develop prevention and treatment strategies. Vaccines of different countries are in clinical and preclinical trials and the repurposed-drugs are providing to find out a positive result against COVID-19. The report is an analysis of published information focusing on treatment options including vaccination, drug-therapy, cytokines, therapeutic antibodies. Most of the vaccine’s development strategies and drugs target the surface structural spike glycoprotein or S-protein, the major inducer of pathogenic responses. Here, it is reviewed the features of SARS-CoV-2 and the global current status of therapeutic, and vaccine development for the prevention and effective treatment of COVID-19.
Yuka Miyachi, Chika Nakayama, Taeyuki Oshima
Pharmacology & Pharmacy, Volume 12, pp 55-62; doi:10.4236/pp.2021.122005

In recent years, consumers are becoming more health-conscious. Supplements are becoming popular as they can be purchased easily. In Japan, the “Food with Function Claims” system began in 2015; the market for supplements is expected to continue to expand. However, the use of some supplements has not been supported with sufficient scientific evidence; some products have even caused health problems. In addition, consumers may not be able to make correct decisions based on the information from the Internet. Unlike medicine, the instruction on the usage of supplements is not precise. Therefore, improving the quality of the information on the supplements will become more necessary in the future. This study aims to improve the quality of the information on supplements by surveying the disintegration and dissolution behavior of the carnitine-containing supplements and evaluated their quality. The products tested here were supplements containing commercial carnitine. Disintegration test and dissolution test were conducted according to the Japanese Pharmacopoeia. Carnitine was quantified by high-performance liquid chromatography. The disintegration tests revealed that the products had different disintegration times, varying from 35 to 100 minutes; some products took more than 5 hours to disintegrate. Thus, some products had a slow rise in their dissolution rate. These results suggest that the carnitine-containing supplements used in this study may affect the absorption process. Therefore, in the case of oral administration, the expected effect might not be achieved depending on the product.
Syed Ata Ur Rahman, Abdullah Alsaedi, Abdulelah Alhusayni, Abdulmalik Alqurshi, Sameh Ahmed, Yaser M. Alahmadi, Alaa Omer M. Abdullaal, Badr Ahmed A. Taher, El-Sayed E. Habib
Pharmacology & Pharmacy, Volume 12, pp 1-9; doi:10.4236/pp.2021.121001

Epilepsy is a chronic and the fourth most common neurological disorder which affects people of all age groups. Recently research and awareness on epilepsy-related deaths have rapidly grown over the past two decades. Many previous studies are attributed to the guidelines that apprise health care professionals in handling these deaths, but there is a relative scarcity of information accessible for clinicians and pharmacists who are responsible for manufacturing or preparing the extemporaneous anti-epileptic suspensions in the hospitals. Mostly in partial seizures, phenytoin is one of the first-choice drugs. In Saudi Arabian hospitals, the extemporaneous preparation of phenytoin suspension is common, but the hot climatic weather in Saudi Arabia possesses stability problems that should be tackled as the prepared suspension should pass all the stability tests to ensure uniform dosage of the extemporaneous formulation. In the current study, the commercial capsules were used to prepare the oral phenytoin sodium extemporaneous suspension. The physical, chemical and microbiological stability of phenytoin sodium suspension is analyzed at various temperatures.
Toshio Kurihara, Honami Kojima, Miyako Yoshida, Mizuho Oshio, Rino Kunikata, Haruka Nishikawa, Takahiro Uchida
Pharmacology & Pharmacy, Volume 12, pp 43-54; doi:10.4236/pp.2021.122004

The purpose of this study was to evaluate the palatability of dry syrups for pediatric use by human gustatory sensation testing and the artificial taste sensor. The bitterness intensities of dry syrups mixed with various beverages were also evaluated using the taste sensor. Twenty dry-syrup formulations of antibacterial and anti-allergic drugs containing bitter active ingredients, frequently used in pediatric medicine in Japan, were selected for testing. The main factors influencing palatability were determined by factor analysis of data from human gustatory sensation testing using the semantic differential method. It was shown that the bitterness intensity of dry syrups in water could be predicted by the artificial taste sensor. The influence of different beverages (orange juice, milk or cocoa) mixed with the dry syrups was evaluated using the artificial taste sensor. Taste and texture were found to be the principal factors influencing the palatability of dry syrups. While the bitterness intensities of some dry syrups were increased by mixing with orange juice, the bitterness intensities of most dry syrups were decreased by mixing with milk or cocoa. This suggests that one or more constituents of milk or cocoa may reduce the bitterness intensities of dry syrups.
Xianjun Long, Bo Liu, Zuren Peng, Ping Qiu, Xuechun Yang, Yuanxiang Yang, Meili Wang, Songmao Yin, Xingchu Gong
Pharmacology & Pharmacy, Volume 11, pp 188-195; doi:10.4236/pp.2020.118017

The change of drug quality of Yuxingcao injection after formulation is considered as one of the causes for adverse reactions. In this study, orthogonal experimental design was used to investigate the influencing factors on the pH stability of Yuxingcao injection. Two methods of accelerated tests were carried out in the experiments. The results showed that using Tween 80 as the solubilizer could significantly decrease the pH value of Yuxingcao injection after accelerated tests. There was no significant difference in the pH value after the accelerated tests when the other 6 factors varied, including the type of liquid processed, the dosage of activated carbon, heating temperature, reagents for pH adjustment, pH value range after adjustment, and sterilization conditions. In order to improve the quality stability of Yuxingcao injection, the quality of Tween 80 should be strictly controlled to minimize the change of pH value of Yuxingcao injection.
Moushumi Tabassoom Salam, Ashim Kumar, Akito Hata, Hiromu Kondo, Abdus Salam, Mir Imam Ibne Wahed, Rafiqul Islam Khan, Ranjan Kumar Barman
Pharmacology & Pharmacy, Volume 11, pp 159-173; doi:10.4236/pp.2020.118015

This investigation was undertaken to enhance the solubility and consequent antibacterial activity of cefuroxime axetil (CA), a β-lactamase-stable broad spectrum second generation cephalosporin through solid dispersion (SD) technique. For this purpose, CA loaded SDs (CSDs) were prepared by solvent evaporation method using different concentrations of microcrystalline cellulose (MCC) as carrier. The CSDs were characterized by in-vitro dissolution study, thermal analysis (DSC), crystallinity (PXRD), interactions (FTIR) and morphology (SEM). Among the formulations, CSD-2 showed the highest dissolution rate which was 2.59-fold higher than pure CA with a drug-carrier (CA: MCC) ratio of 1:3. Enhanced dissolution rate was attributed to conversion of drug from crystalline to amorphous state during preparation of SDs, which was validated by DSC, PXRD, FTIR and SEM analyses. Antibacterial activity of CSD-2 against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) showed 1.94- and 6.75-fold higher relative zone of inhibition (RZOI), respectively than pure CA. CSD-2 has been found to be the most effective optimized formulation in terms of both enhanced dissolution rate and antibacterial activity. Thus, it can be an effective alternative to conventional dosage forms of CA. However, further investigations are needed to validate its pharmacokinetic properties, in-vivo antibacterial efficacy and safety before recommending as a novel formulation
Froylán Ibarra-Velarde, Yolanda Vera-Montenegro, Yazmín Acala-Canto, Irene Cruz-Mendoza
Pharmacology & Pharmacy, Volume 11, pp 174-187; doi:10.4236/pp.2020.118016

The acaricidal efficiency of fipronil alone and fipronil + methoprene compared to commercial fipronil and commercial fipronil + methoprene, applied by the epicutaneous route (spot-on) in dogs naturally infested with ticks, was assessed. Thirty dogs infested with high loads of ticks were used. On day 0, the dogs were divided into 5 groups of 6 animals each. Each animal was duly identified for individual and group monitoring. Treatments were made based on body weight according to manufacturer’s instructions. Group 1 (G1) received 10.0% fipronil at a single dose of a pipette applied by epicutaneous route in the base of the neck. G2 received 10% fipronil + 10% methoprene in single application similarly to G1. G3 was treated with 9.8% commercial fipronil as before mentioned. G4 received commercial 9.8% fipronil + 9.8% methoprene applied as in previous groups. G5 served as an infected untreated control. Animals were examined by thumb tick counts on days 0 (Treatment day), 3, 7, 14, 21 and 28. Efficacy was measured as a percentage of tick reduction in the treated groups relative to the untreated control. Results indicated an overall efficacy of 88.2%, 93%, 90.4% and 99.3%, respectively. There was no significant statistical difference between the treated groups (P ly and in full development. It is concluded that the combined formulations of fipronil + methoprene compared to fipronil applied alone, showed an additive effect against Rhipicephalus sanguineus ticks in naturally infested dogs kept in captivity.
Baraa G. Alani, Ameer H. Alwash, Ismail T. Ibrahim
Pharmacology & Pharmacy, Volume 11, pp 251-281; doi:10.4236/pp.2020.1110022

Chloroquine (CQ) was and still considered as the most common agent in the treatment and prophylaxis of malaria, it also possesses many different pharmacological and biological activities that make it able to be used as a therapy or adjuvant therapy for many types of diseases. CQ exhibits anticancer activity alone or as adjuvants with other agents against many kinds of tumors. Its activities also were approved as an anti-inflammatory agent in rheumatoid and other autoimmune diseases like systemic lupus and rheumatic arthritis. Its’ important role in the improvement of many metabolic disorders like hypertension, hyperglycemia, and lipid profile disturbances was also established. CQ can act against different microbial infections such as many types of viruses, bacteria and fungus by different mechanisms of action. Furthermore, its dermatological role in the treatment of many skin diseases was demonstrated. Recently, CQ showed a very responsive role in curing and prevention of the covoid-19 virus. This review summarizes intensively the multiple therapeutic applications of CQ and discusses the possible mechanisms of action for these applications.
Jiuli Hu, Zhu Xiaoqin, Chanchan Hu, Rui Wang, Yanwu Zhao, Xiaoqin Zhu
Pharmacology & Pharmacy, Volume 11, pp 299-305; doi:10.4236/pp.2020.1111024

Introduction: The prevalence of Klebsiella pneumoniae has rapidly increased in recent years and the distribution differed greatly by region, We aimed to study the relationship between antibiotic resistance and K. pneumoniae, especially carbapenem-resistant Klebsiella pneumoniae (CRKP) in our tertiary hospitals from 2014 to 2018. Methodology: The antibiotic consumption data of K. pneumoniae were expressed as the defined daily dose (DDD) per 100 inpatient days (DDDs). K. pneumoniae which isolated from clinical samples in hospital between January 2014 and December 2018 were retrospectively analyzed, and the correlation between antibiotic resistance rate and antibiotic frequency was analyzed. Results: From 2014 to 2018, a total of 2295 strains of K. pneumoniae were isolated, with the detection rates of 8.2%, 9.2%, 11.9%, 13.4% and 14.0%. There were 423 strains of CRKP, with the detection rates of 7.5%, 5.8%, 17.8% 24.2% and 25.2% respectively. K. pneumoniae showed different degrees of resistance to antibiotics and showed an increasing trend year by year to carbapenems. The resistance rate of imipenem was 2.5%, 2.8%, 9.9%, 12.3%, 13.4%, and the resistance rate of meropenem was 2.0%, 3.0%, 8.8%, 12.6%, 12.7%, respectively. The resistance rate of most other drugs decreased. The DDDs values of cefoperazone/sulbactam, piperacillin-tazobactam and gentamicin showed a strong positive correlation with K. pneumoniae drug resistance rate (r > 0.8, P 0.05). Conclusions: The detection rate of K. pneumoniae and CRKP increased year by year, which was closely related to the dose of antibiotics. Strengthening the management of antimicrobial drugs and standardising the use of antimicrobial prescriptions were of great significance for delaying the emergence of drug-resistant bacteria.
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