scholarly journals Vitamin Drug conjugate: a systematic review of pharmacological potential

2021 ◽  
Vol 101 (1) ◽  
pp. 27-52
Author(s):  
R.P. Bhole ◽  
◽  
Yogita Shinde ◽  
C.G. Bonde ◽  
R.D. Wavhale ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Side Effects ◽  
Viral Infections ◽  
Cytotoxic Agents ◽  
Tuberculosis Infection ◽  
New Approach ◽  
Drug Conjugate ◽  
Drug Selectivity ◽  
Life Threatening ◽  
Pharmacological Potential

Cancer is a chronic disease which can cause death. In traditional chemotherapycytotoxic drugs are used to kill proliferating cancer cells. The cytotoxic agent exhibits less specificity, less biological activity, causes sys-temic toxicity and undesirable side effects. Each year, about 1.8 million of the population are infected and die due to tuberculosis infection. An increase of drug resistance during the tuberculosis treatment is a significant concern. So, it is necessary to develop a new approach or therapies to resolve drug resistance, drug selectivity in tuberculosis infection and the reduction of the side effects of cytotoxic agents and anti-tubercular drugs. This review describes the newly emerging concept of «vitamin drug conjugate». Vitamin-drug conjugate is a specifically carried drug toward the target site, is one of the promising ways to treat chronic diseases like can-cer and tuberculosis and enhance the therapeutic outcome. The purpose of this review is to explore vitamin as a targeting moiety for new anticancer and anti-tubercular drug to overcome challenges, such as non-selectivity, systemic toxicity and multidrug resistance. This approach is beneficial in the treatment of life-threatening disease like cancer, tuberculosis and also in many viral infections.

scholarly journals A contemporary chemical entities infiltrating in the antimalarial therapy era: a comprehensive review

Folia Medica ◽  
2021 ◽  
Vol 63 (5) ◽  
pp. 637-646
Author(s):  
Sandip N. Badeliya ◽  
Pankaj P. Kapupara ◽  
Navneet F. Chauhan ◽  
Ishan I. Panchal
Keyword(s):  
Drug Resistance ◽  
Side Effects ◽  
Skin Color ◽  
Color Change ◽  
Blurred Vision ◽  
Artemisinin Derivatives ◽  
Antimalarial Agents ◽  
Reduced Body ◽  
Life Threatening ◽  
The Right

Malaria, a life-threatening disease, is caused by parasitic single-celled microorganisms. It is specifically transmitted by the anopheles female mosquito of the Plasmodium family. There are a lot of drugs available in the market to treat this life-challenging disease. Chloroquine, a cheaper molecule that is available worldwide, is one of them. Drug resistance has been observed with chloroquine as well as with some other quinine derivatives and with artemisinin derivatives in the southeast region of Asia in countries like Cambodia, Thailand, Myanmar, and Vietnam country since 1957. After 1970, the drug resistance has been further increased and it has been expanded in several localities of India. Also, antimalarial agents, particularly chloroquine, have so many side effects such as nausea, vomiting, blurred vision, abdominal cramps, diarrhea, headache, appetite loss, deprivation of hearing, skin color change, baldness, reduced body weight, and seizures. Furthermore, this drug cannot be given to pregnant women. Hence, it is the right time to design and develop newer antimalarial agents so that this kind of drug resistance, as well as side effects of the drugs, can be overcome.

scholarly journals Mechanisms of Pharmaceutical Therapy and Drug Resistance in Esophageal Cancer

2021 ◽  
Vol 9 ◽  
Author(s):  
Chengyi Mao ◽  
Xiaoxi Zeng ◽  
Chao Zhang ◽  
Yushang Yang ◽  
Xin Xiao ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Esophageal Cancer ◽  
Clinical Practice ◽  
Side Effects ◽  
Chemotherapy Regimen ◽  
Checkpoint Inhibitors ◽  
Molecular Therapy ◽  
Cytotoxic Agents ◽  
Therapy Regimen ◽  
Pharmaceutical Therapy

Pharmaceutical therapies are essential for esophageal cancer (EC). For the advanced EC, the neoadjuvant therapy regimen, including chemotherapy plus radiotherapy and/or immunotherapy, is effective to achieve clinical benefit, even pathological complete response. For the unresectable, recurrent, and metastatic EC, the pharmaceutical therapy is the limited effective regimen to alleviate the disease and prolong the progression-free survival and overall survival. In this review, we focus on the pharmaceutical applications in EC treatment including cytotoxic agents, molecular targeted antibodies, and immune checkpoint inhibitors (ICIs). The chemotherapy regimen is based on cytotoxic agents such as platinum-based complexes, fluorinated pyrimidines and taxenes. Although the cytotoxic agents have been developed in past decades, the standard chemotherapy regimen is still the cisplatin and 5-FU or paclitaxel because the derived drugs have no significant advantages of overcoming the shortcomings of side effects and drug resistance. The targeted molecular therapy is an essential supplement for chemotherapy; however, there are only a few targeted therapies available in clinical practice. Trastuzumab and ramucirumab are the only two molecular therapy drugs which are approved by the US Food and Drug Administration to treat advanced and/or metastatic EC. Although the targeted therapy usually achieves effective benefits in the early stage therapy of EC, the patients will always develop drug resistance during treatment. ICIs have had a significant impact on routine clinical practice in cancer treatment. The anti-programmed cell death-1 monoclonal antibodies pembrolizumab and nivolumab, as the ICIs, are recommended for advanced EC by several clinical trials. However, the significant issues of pharmaceutical treatment are still the dose-limiting side effects and primary or secondary drug resistance. These defects of pharmaceutical therapy restrain the clinical application and diminish the effectiveness of treatment.

Hybrid Compounds & Oxidative Stress Induced Apoptosis in Cancer Therapy

2020 ◽  
Vol 27 (13) ◽  
pp. 2118-2132 ◽  
Author(s):  
Aysegul Hanikoglu ◽  
Hakan Ozben ◽  
Ferhat Hanikoglu ◽  
Tomris Ozben
Keyword(s):  
Oxidative Stress ◽  
Drug Resistance ◽  
Side Effects ◽  
Cancer Therapy ◽  
Tumor Cells ◽  
Anticancer Drugs ◽  
Chemotherapeutic Agents ◽  
Oxidation Reactions ◽  
Hybrid Compounds ◽  
Induced Apoptosis

: Elevated Reactive Oxygen Species (ROS) generated by the conventional cancer therapies and the endogenous production of ROS have been observed in various types of cancers. In contrast to the harmful effects of oxidative stress in different pathologies other than cancer, ROS can speed anti-tumorigenic signaling and cause apoptosis of tumor cells via oxidative stress as demonstrated in several studies. The primary actions of antioxidants in cells are to provide a redox balance between reduction-oxidation reactions. Antioxidants in tumor cells can scavenge excess ROS, causing resistance to ROS induced apoptosis. Various chemotherapeutic drugs, in their clinical use, have evoked drug resistance and serious side effects. Consequently, drugs having single-targets are not able to provide an effective cancer therapy. Recently, developed hybrid anticancer drugs promise great therapeutic advantages due to their capacity to overcome the limitations encountered with conventional chemotherapeutic agents. Hybrid compounds have advantages in comparison to the single cancer drugs which have usually low solubility, adverse side effects, and drug resistance. This review addresses two important treatments strategies in cancer therapy: oxidative stress induced apoptosis and hybrid anticancer drugs.

Recent Advances in the Rational Drug Design Based on Multi-target Ligands

2020 ◽  
Vol 27 (28) ◽  
pp. 4720-4740 ◽  
Author(s):  
Ting Yang ◽  
Xin Sui ◽  
Bing Yu ◽  
Youqing Shen ◽  
Hailin Cong
Keyword(s):  
Drug Resistance ◽  
Clinical Practice ◽  
Side Effects ◽  
Drug Design ◽  
Rational Drug Design ◽  
Health Conditions ◽  
Pharmacokinetic Parameters ◽  
Single Target ◽  
Rational Drug ◽  
Huge Challenge

Multi-target drugs have gained considerable attention in the last decade owing to their advantages in the treatment of complex diseases and health conditions linked to drug resistance. Single-target drugs, although highly selective, may not necessarily have better efficacy or fewer side effects. Therefore, more attention is being paid to developing drugs that work on multiple targets at the same time, but developing such drugs is a huge challenge for medicinal chemists. Each target must have sufficient activity and have sufficiently characterized pharmacokinetic parameters. Multi-target drugs, which have long been known and effectively used in clinical practice, are briefly discussed in the present article. In addition, in this review, we will discuss the possible applications of multi-target ligands to guide the repositioning of prospective drugs.

Small Molecular Gemcitabine Prodrugs for Cancer Therapy

2020 ◽  
Vol 27 (33) ◽  
pp. 5562-5582 ◽  
Author(s):  
He Miao ◽  
Xuehong Chen ◽  
Yepeng Luan
Keyword(s):  
Drug Resistance ◽  
Side Effects ◽  
Anticancer Drug ◽  
Drug Stability ◽  
Effective Means ◽  
Active Form ◽  
Deoxycytidine Kinase ◽  
High Efficacy ◽  
Pyrimidine Nucleoside ◽  
Design And Synthesis

Gemcitabine as a pyrimidine nucleoside analog anticancer drug has high efficacy for a broad spectrum of solid tumors. Gemcitabine is activated within tumor cells by sequential phosphorylation carried out by deoxycytidine kinase to mono-, di-, and triphosphate nucleotides with the last one as the active form. But the instability, drug resistance and toxicity severely limited its utilization in clinics. In the field of medicinal chemistry, prodrugs have proven to be a very effective means for elevating drug stability and decrease undesirable side effects including the nucleoside anticancer drug such as gemcitabine. Many works have been accomplished in design and synthesis of gemcitabine prodrugs, majority of which were summarized in this review.

Cutaneous Adverse Events of Immune Checkpoint Inhibitors: A Summarized Overview

2019 ◽  
Vol 14 (1) ◽  
pp. 14-20 ◽  
Author(s):  
Kerasia-Maria Plachouri ◽  
Eleftheria Vryzaki ◽  
Sophia Georgiou
Keyword(s):  
Side Effects ◽  
Immune Checkpoint ◽  
Immune Checkpoint Inhibitors ◽  
Checkpoint Inhibitors ◽  
Skin Toxicity ◽  
Maculopapular Rash ◽  
Symptomatic Treatment ◽  
Stevens Johnson Syndrome ◽  
Life Threatening ◽  
Skin Side Effects

Background:The introduction of Immune Checkpoint Inhibitors in the recent years has resulted in high response rates and extended survival in patients with metastatic/advanced malignancies. Their mechanism of action is the indirect activation of cytotoxic T-cells through the blockade of inhibitory receptors of immunomodulatory pathways, such as cytotoxic T-lymphocyte-associated antigen-4 (CTLA-4), programmed cell death protein-1 (PD-1) and its ligand (PD-L1). Despite their impressive therapeutic results, they can also induce immune-related toxicity, affecting various organs, including the skin.Objective:To provide an updated summarized overview of the most common immune-mediated cutaneous side effects and their management.Method:English articles derived from the databases PubMed and SCOPUS and published between 2009 and 2018, were analyzed for this narrative review.Results:The most common adverse cutaneous reactions include maculopapular rash, lichenoid reactions, vitiligo and pruritus, with severity Grade 1 or 2. Less frequent but eventually life-threatening skin side effects, including Stevens-Johnson syndrome, Drug Reaction with Eosinophilia and Systemic Symptoms and Toxic Epidermal necrolysis, have also been reported.Conclusion:Basic knowledge of the Immune-Checkpoint-Inhibitors-induced skin toxicity is necessary in order to recognize these treatment-related complications. The most frequent skin side effects, such as maculopapular rash, vitiligo and pruritus, tend to subside under symptomatic treatment so that permanent discontinuation of therapy is not commonly necessary. In the case of life-threatening side effects, apart from the necessary symptomatic treatment, the immunotherapy should be permanently stopped. Information concerning the management of ICIs-mediated skin toxicity can be obtained from the literature as well as from the Summary of Product Characteristics of each agent.

scholarly journals Knowledge, attitude, and practice of pharmacy and medical students regarding self-medication, a study in Zabol University of Medical Sciences; Sistan and Baluchestan province in south-east of Iran

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Mahmoud Hashemzaei ◽  
Mahdi Afshari ◽  
Zahra Koohkan ◽  
Ali Bazi ◽  
Ramin Rezaee ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Medical Students ◽  
Side Effects ◽  
Drug Information ◽  
Significant Risk ◽  
Disease Recurrence ◽  
Medical Sciences ◽  
Self Medication ◽  
Attitude And Practice ◽  
Knowledge Attitude And Practice

Abstract Background Self-medication is defined as using medicinal products to treat the disorders or symptoms diagnosed by oneself. Although informed self-medication is one of the ways to reduce health care costs, inappropriate self-treatment can pose various risks including drug side effects, recurrence of symptoms, drug resistance, etc. The purpose of this study was to investigate the knowledge, attitude, and practice of pharmacy and medical students toward self-medication. Methods This study was conducted in Zabol University of Medical Sciences in 2018. Overall, 170 pharmacy and medical students were included. A three-part researcher-made questionnaire was designed to address the students’ knowledge, attitude, and practice. Statistical analysis was performed in SPSS 25 software. Results According to the results, 97 (57.1%) students had carried out self-medication within the past 6 months. Overall, the students self-medicated on average 4.2 ± 2.9 times per year. Self-medication was more common in male students (65.4%, P = 0.043). Cold was the most common ailment treated with self-medication (93.2%), and antibiotics (74.4%) were the most commonly used drugs. The primary information sources used by the students were their previous prescriptions (47.4%). Pharmacy students had a higher level of drug information (P < 0.001). There was a statistically significant association between the level of drug information and the tendency for self-medication (P = 0.005). Disease recurrence was the most common negative complication of self-medication. Conclusion There is a need to educate pharmacy and medical students regarding self-medication and its side effects. The high prevalence of self-medication and the overuse of antibiotics can pose a significant risk of drug resistance.

Proton Pump Inhibitors in 2021: Pros, Cons, and Everything in Between

2021 ◽  
pp. 263451612110217
Author(s):  
Joshua A. Sloan ◽  
Philip O. Katz
Keyword(s):  
Quality Of Life ◽  
Side Effects ◽  
Adverse Events ◽  
Proton Pump Inhibitors ◽  
Proton Pump ◽  
Drug Class ◽  
Life Threatening

The medical and lay literature has exploded with reports of adverse events associated with proton pump inhibitors over the last 10 to 15 years. The dissemination of these reports to patients and clinicians have created substantial concerns regarding what has been an exceptionally valuable drug class, dramatically improving patient quality of life, and in many cases preventing life threatening side effects of other medication. Patients are more frequently seeking to avoid these medications, and practitioners are reducing or discontinuing them to the patient’s detriment due to a misunderstanding of the data. This review will discuss the data regarding the most commonly publicized adverse events and attempt to put them in perspective.

Pharmacology Update: School Nurse Role and Emergency Medications for Treatment of Anaphylaxis

2021 ◽  
pp. 1942602X2110219
Author(s):  
Theresa A. Bingemann ◽  
Anil Nanda ◽  
Anne F. Russell
Keyword(s):  
Side Effects ◽  
School Personnel ◽  
Local Environment ◽  
School Nurses ◽  
First Line ◽  
Onset Of Action ◽  
Epinephrine Administration ◽  
Prompt Treatment ◽  
Nurse Role ◽  
Life Threatening

Anaphylaxis is a rapidly occurring allergic reaction that is potentially life threatening. Recognition of the early signs and prompt treatment of anaphylaxis is critical. School nurses are tasked with educating nonmedical school personnel on the recognition and treatment of anaphylaxis and emphasizing that epinephrine is the first line of treatment for anaphylaxis. Fortunately, there is now availability of multiple epinephrine administration devices. However, this also means that there are more devices that school nurses and nonmedical assistive personnel need to learn about to be able to administer in an emergency. Once epinephrine is administered, emergency medical services must be activated. Education regarding what to expect after the administration of epinephrine with respect to side effects and onset of action is also necessary. Though adjunctive medicines, such as antihistamines and inhalers, may also be administered after the injection of epinephrine, they should not be solely relied on in anaphylaxis. School nurses are uniquely situated for this role, as they understand the local environment in a school and can assess and reassess the needs of the faculty and staff.

Cellular uptake of drug loaded spider silk particles

2016 ◽  
Vol 4 (10) ◽  
pp. 1515-1523 ◽  
Author(s):  
Martina B. Schierling ◽  
Elena Doblhofer ◽  
Thomas Scheibel
Keyword(s):  
Drug Resistance ◽  
Side Effects ◽  
Cellular Uptake ◽  
Spider Silk ◽  
Medical Therapies

Medical therapies are often accompanied by not-wanted side-effects or, even worse, targeted cells can develop drug resistance leading to an ineffective treatment. Here, it was shown that drugs can be efficiently delivered into and released within cells when spider silk particles were used as a carrier.

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