Role andamp; future aspects of primaquine in malaria therapy

| Posted in: Science

Journal name: World Journal of Pharmaceutical Research
Original article title: Role & future aspects of primaquine in malaria therapy
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Original source:

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Author:

Pankaj Sharma and Dr. Mukul Tailang


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Role & future aspects of primaquine in malaria therapy

Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research

Doi: 10.20959/wjpr201611-7292


Summary of article contents:

Introduction

Malaria remains a significant global health challenge, especially in tropical and subtropical regions, impacting approximately 40% of the world’s population. Annually, it accounts for an estimated 300-500 million clinical cases and results in over one million deaths, predominantly among young children. Efforts to control the disease have historically included vaccine development, mosquito eradication, and drug discovery. Among the antimalarial agents, primaquine has gained attention, being the only drug licensed for the treatment of relapsing forms of malaria like those caused by Plasmodium vivax and P. ovale. However, its use is hindered by side effects and the potential for severe reactions in individuals with glucose-6-phosphate dehydrogenase deficiency (G6PD).

Nanomedicine in Primaquine Delivery

One promising approach to enhancing the effectiveness of primaquine therapy lies in the realm of nanomedicine. Development of nanomedicine drug-delivery systems, such as solid lipid nanoparticles (SLNs) and microemulsions, has shown to improve the bioavailability and therapeutic efficacy of primaquine. Research indicates that primaquine formulated in SLNs exhibited 20% greater effectiveness compared to conventional oral doses in animal studies. Moreover, these nanotechnology-based systems address the issues of rapid metabolism and toxicity commonly associated with primaquine, making a significant step forward in its therapeutic application.

Transdermal Drug Delivery System

Another innovative method proposed to enhance primaquine administration is the development of transdermal drug delivery systems. This method seeks to bypass the gastrointestinal side effects associated with oral formulations, such as nausea and abdominal cramps. Research suggests that a transdermal patch could sustain plasma concentrations of primaquine for extended periods, thus facilitating improved compliance and potentially reducing the required dosing frequency. Such systems aim to mitigate the adverse effects while maintaining therapeutic efficacy, presenting a viable alternative for both patients and healthcare providers.

Chemical Modifications and Derivatives

In addition to novel delivery mechanisms, exploring chemical derivatives of primaquine offers another pathway to enhance its effectiveness and reduce toxicity. Various peptide and amino acid derivatives have been synthesized, targeting metabolic pathways to minimize oxidative deamination. Approaches such as linking primaquine to carrier proteins or developing peptide derivatives encapsulated in biodegradable nanoparticles have demonstrated potential for improved pharmacokinetics and reduced side effects. These strategies aim to optimize the drug's stability and efficacy, marking a notable advancement in malaria therapy.

Conclusion

The global malaria crisis necessitates ongoing research and innovation in treatment strategies. Primaquine remains a crucial option for relapsing malaria despite its limitations. The exploration of nanomedicine, transdermal delivery systems, and chemical modifications represent significant opportunities to enhance primaquine's therapeutic impact, minimize adverse effects, and improve patient adherence to treatment regimens. Continued advancements in drug development and delivery systems are essential to combat malaria more effectively and save lives in endemic regions.

FAQ section (important questions/answers):

What is the significance of primaquine in malaria therapy?

Primaquine is crucial for treating relapsing malaria, particularly caused by Plasmodium vivax and P. ovale. It helps eliminate the liver stages of these parasites, preventing relapse and transmission of the disease.

What are the common side effects of primaquine?

Primaquine can cause nausea, vomiting, abdominal pain, and hemolytic anemia, especially in individuals with glucose-6-phosphate dehydrogenase deficiency (G6PD deficiency). These side effects restrict its use in specific populations, including pregnant women.

How can nanomedicine improve primaquine delivery?

Nanomedicine can enhance the therapeutic properties of primaquine through various drug-delivery systems, such as liposomes and nanoparticles. These systems can improve bioavailability and reduce side effects by ensuring more targeted delivery.

What are the dosing recommendations for primaquine?

For Plasmodium vivax, the recommended dose is 30 mg daily for 14 days. For P. ovale, the dose is 15 mg daily for the same duration, with concurrent monitoring for side effects.

Why is transdermal drug delivery considered for primaquine?

Transdermal delivery of primaquine may reduce gastrointestinal side effects and improve drug absorption. It allows for a controlled release, minimizing the frequency of doses and ensuring sustained therapeutic levels.

What future developments are anticipated for primaquine?

Future developments may include new formulations, such as transdermal patches or nanoparticles, to enhance delivery and reduce toxicity. Researchers are also exploring derivatives of primaquine to improve efficacy and minimize adverse effects.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Role andamp; future aspects of primaquine in malaria therapy”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.

1) Drug:
In the context of this article, 'drug' refers to primaquine, which is a crucial antimalarial medication used in the treatment of malaria, particularly in cases of relapsing malaria caused by Plasmodium vivax and P. ovale. The text discusses its pharmacological properties, dosage, mechanisms of action, and side effects.

2) Sharman (Sarma, Sharma, Sarman):
Pankaj Sharma is the corresponding author and one of the key researchers in this review article. His contributions encompass the exploration of primaquine's role in malaria therapy, as well as proposing future directions for drug delivery systems, emphasizing innovative approaches in pharmaceutical research.

3) Activity:
'Activity' in this text pertains to the antimalarial efficacy of primaquine and its derivatives. The article delves into various studies that document the effectiveness of primaquine in treating malaria, evaluating its ability to eliminate the malaria parasites and its safety profile in affected populations.

4) Transmission:
Transmission refers to the spread of malaria parasites from infected to non-infected individuals. The text highlights the use of primaquine in interrupting transmission, particularly in malaria elimination strategies, emphasizing its role in diminishing the infectivity of Plasmodium falciparum, especially in areas facing drug resistance.

5) Blood:
The term 'blood' is relevant in the context of malaria infection and the pharmacological effects of primaquine. The article discusses how primaquine targets the blood stages of malaria parasites and the implications of its use for individuals with certain blood disorders, including G6PD deficiency.

6) Life:
'Life' is relevant in the broader context of malaria's impact on health and mortality. The article mentions malaria as a life-threatening disease affecting millions globally, highlighting the urgent need for effective treatments like primaquine, which can save lives by preventing deaths from severe malaria episodes.

7) Toxicity:
Toxicity relates to the adverse effects associated with primaquine, which include nausea, vomiting, and gastrointestinal disturbances. The review discusses the challenges posed by primaquine's toxicity for certain populations, particularly those with glucose-6-phosphate dehydrogenase deficiency, emphasizing the need for better therapeutic formulations.

8) Gwalior:
Gwalior is a city in India where the research team is based, including the lead author, Pankaj Sharma. The mention of Gwalior connects the research to specific geographical and logistical contexts, providing insight into the local focus of malaria prevention and treatment efforts within India.

9) Science (Scientific):
'Science' refers to the systematic study of substance interactions, such as the pharmacological sciences that underpin the development and evaluation of primaquine. The article showcases the importance of scientific research in advancing malaria treatment and addressing pharmaceutical challenges associated with drug delivery.

10) Disease:
The term 'disease' refers specifically to malaria as a communicable and life-threatening illness caused by Plasmodium parasites. The article underlines the global burden of malaria and the necessity for effective treatments such as primaquine to mitigate the impact of this disease on public health.

11) Study (Studying):
'Study' refers to the research and systematic investigation presented in the article. This includes a review of existing literature on primaquine, its therapeutic applications, side effects, and future directions in malaria treatment. It emphasizes the need for continuous research to improve treatment outcomes.

12) Rheumatoid arthritis:
Rheumatoid arthritis is mentioned as a contraindication for primaquine use. The article highlights that individuals with this autoimmune condition may face increased risks when taking primaquine, illustrating the importance of considering patient-specific factors when prescribing antimalarial medications.

13) New Delhi:
New Delhi is the capital city of India and does not play a direct role in the article. However, the mention of Indian locations like New Delhi may suggest broader public health initiatives and research collaboration in malaria treatment strategies relevant to national health policies.

14) Pharmacological:
Pharmacological refers to the action of drugs within biological systems. The article discusses the pharmacological properties of primaquine, including its mechanism of action against malaria parasites and the implications of its use in terms of effectiveness and safety in treatment regimens.

15) Biodegradable:
'Biodegradable' is referenced in connection with drug delivery systems for primaquine. Innovations in nanomedicine and biodegradable carriers are explored as promising approaches to enhance the delivery and efficacy of primaquine while reducing its associated toxicity for patients.

16) Pharmacology:
Pharmacology encompasses the study of drugs and their interactions with living organisms. The article delves into the pharmacology of primaquine by discussing its mechanisms of action, dosage regimens, side effects, and effectiveness in treating malaria, highlighting the need for careful pharmacological considerations.

17) Chemotherapy:
'Chemotherapy' refers to the use of chemical substances to treat disease, in this instance, malaria. The article discusses primaquine as part of antimalarial chemotherapy, highlighting its role as a treatment for relapsing malaria and its inclusion in comprehensive malaria management strategies.

18) Meenakshi:
Meenakshi Bharkatiya is mentioned within the context of research contributions regarding drug formulations and studies. Her work, along with others, plays a role in advancing the understanding of drug delivery systems and improving treatment options for malaria, specifically with primaquine.

19) Bhatnagar:
Bhatnagar is mentioned as a contributor to research efforts in developing transdermal drug delivery systems and other formulations. This highlights the collaborative nature of scientific research aimed at improving drug therapies, specifically in relation to primaquine and malaria treatment advancements.

20) Medicine:
'Medicine' in this context refers to the field and practice of diagnosing and treating diseases. The article addresses how primaquine serves as a medicine for malaria, discussing therapeutic applications and the overall goal to improve malaria management using pharmacological advancements.

21) Vomiting:
Vomiting is cited as a significant side effect of primaquine administration. The article highlights the importance of addressing such adverse reactions in treatment plans and the necessity of developing improved formulations to reduce nausea and enhance patient compliance with malaria therapy.

22) Language:
'Language' in this context is indirectly related to the communication of scientific findings. The article underscores the importance of effectively articulating research results and medical knowledge in accessible language for healthcare professionals and communities, facilitating better understanding and implementation of malaria treatments.

23) Pregnant:
Pregnant women are specifically mentioned as a key group that should avoid primaquine due to its potential adverse effects. The article emphasizes the necessity of precautionary measures in prescribing antimalarial treatments, considering the unique health needs and risks associated with pregnancy.

24) Entering:
'Entering' may relate to the entrance of new methodologies or innovations in the field of malaria treatment, such as advancements in drug delivery systems. The review article discusses emerging strategies that researchers are exploring to enhance the efficacy of primaquine in combating malaria.

25) Kalluri:
Kalluri is mentioned in the context of discussing microchannel formation and its implications for drug delivery systems. This highlights the contributions of researchers like Kalluri in understanding skin permeation techniques relevant to transdermal delivery of drugs such as primaquine.

26) Channel:
'Channel' is relevant to the discussion surrounding transdermal drug delivery. The mention of channels and their formation is tied to the mechanisms through which drugs can be delivered effectively across the skin, which is particularly significant for minimizing side effects of primaquine.

27) Meeting:
The term 'meeting' refers to gatherings of experts for discussion, such as the CDC expert meeting on malaria chemoprophylaxis that is mentioned. These meetings facilitate collaboration among professionals, fostering shared knowledge and strategies for improving malaria treatment and prevention efforts globally.

28) Species:
'Species' pertains to the different types of malaria-causing parasites, notably Plasmodium vivax and Plasmodium falciparum. Understanding species differences is essential for targeted treatment planning, as response to primaquine and other drugs can vary based on the specific parasite involved.

29) Parisheka (Pariseka):
Parise is mentioned as a contributor to discussions about primaquine's use for malaria prevention, particularly in terms of its role in interrupting transmission. This indicates the collaborative efforts among researchers to enhance malaria control strategies and address challenges in malaria therapy.

30) Nausea:
Nausea is highlighted as a common side effect associated with primaquine treatment. The review emphasizes that managing nausea is crucial for treatment adherence, and there is a need for developing formulations that can effectively mitigate this side effect while maintaining therapeutic efficacy.

31) Bitter:
'Bitter' refers to the unpleasant taste associated with primaquine, which presents challenges for patient compliance. The article discusses various strategies for taste masking and drug formulation to improve the palatability of primaquine in order to enhance patient acceptance.

32) Powder:
Powder refers to the physical form of primaquine and related formulations. The article addresses drug formulation challenges, including whether primaquine can be effectively delivered in powdered form or if other delivery mechanisms like nanoparticles might be more effective.

33) Delhi:
Delhi, the capital of India, is mentioned in the context of the pharmaceutical and research activities occurring there. It denotes the location of research collaborations and could suggest wider public health strategies against malaria at a national level in areas like urban health management.

34) Banga (Bamga):
Banga is mentioned in relation to contributions to pharmaceutical formulations and drug delivery research. The mention signifies the collaboration within the scientific community aimed at evolving treatment protocols and enhancing the effectiveness of drugs like primaquine for malaria therapy.

35) Culli:
Culli appears as a name within the reference list, indicating contributions to this field of research, particularly concerning drug delivery systems. This highlights collaborative efforts aimed toward improving antimalarial therapy outcomes through innovative scientific approaches.

36) Death:
'Death' is relevant as it underscores the severe consequences of untreated malaria, which claims millions of lives annually. The article stresses the urgency of developing safe and effective treatments like primaquine to combat malaria and reduce mortality rates globally.

37) Dara:
Dara is referenced in the context of contributing to discussions about malaria treatment challenges. This name signifies collaborative research efforts aiming to improve malaria management strategies and enhance the effectiveness of treatments like primaquine.

38) Beta:
Beta refers to beta-cyclodextrin, which is mentioned as a method to mitigate the bitterness of primaquine. This highlights the importance of reformulating drugs to enhance patient compliance and reduce barriers to effective malaria treatment due to taste-related issues.

39) Food:
'Food' pertains to the recommendation of taking primaquine with food to enhance its absorption and reduce gastrointestinal side effects. This consideration emphasizes the importance of patient guidance in the administration of medications for improved therapeutic outcomes.

40) Pain:
Pain is mentioned in relation to the gastrointestinal side effects of primaquine. Addressing pain associated with medication intake is crucial for improving patient experience and ensuring adherence to malaria treatment regimens, showcasing the need for more tolerable drug formulations.

41) Salt (Salty):
'Salt' may refer generally to chemical compounds used in drug formulations. In the context of primaquine, discussions around salts could imply considerations for drug solubility and bioavailability, which are essential for ensuring effective delivery and therapeutic actions of antimalarial medications.

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