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"This book gives an updated and expert overview of nuclear hormone receptors in drug metabolism and drug development and equips you with the interdisciplinary understanding of these receptors and how they can be regulated. Pharmaceutical researchers will find this extremely useful in developing drugs for cancer, heart disease, and diabetes treatment. This comprehensive resource collects scattered materials into one handy, informative volume."

"The book covers a broad spectrum of topics, ranging from pioneering research in the field of classical steroid hormones to very recently discovered orphan receptors and their modulators. State of the art technologies are also discussed in the individual chapters that help to develop a deeper insight into the biochemical and pharmacological principles underlying the biological function of nuclear receptors.Edited by two experts working at the pioneering pharmaceutical company and major global player in hormone-derived drugs, this handbook and reference systematically treats the drug development aspects of all human nuclear receptors, including recently characterized receptors such as PPAR, FXR and LXR. Authors from leading pharmaceutical companies around the world present examples and real-life data from their own work."

"Opening with a general introduction on chemokine function and chemokine receptor biology, the handbook goes on to cover the known implications of these signaling molecules in human diseases, such as cancer, neural disorders, and viral infection, including HIV/AIDS. The second half of the book systematically surveys current drug development efforts at targeting individual chemokine receptors, as well as other chemokine interaction partners. Contributions in the first part of the book are mainly from academia, whereas the second part contains up-to-date reports from the pharmaceutical industry."

"The essentials of drug metabolism vital to developing new therapeutic entities.Information on the metabolism and disposition of candidate drugs is a critical part of all aspects of the drug discovery and development process. Drug metabolism, as practiced in the pharmaceutical industry today, is a complex, multidisciplinary field that requires knowledge of sophisticated analytical technologies and expertise in mechanistic and kinetic enzymology, organic reaction mechanism, pharmacokinetic analysis, animal physiology, basic chemical toxicology, preclinical pharmacology, and molecular biology. With chapters contributed by experts in their specific areas, this reference covers :- Basic concepts of drug metabolism- The role of drug metabolism in the pharmaceutical industry- Analytical techniques in drug metabolism- Common experimental approaches and protocolsDrug metabolism in drug design and development emphasizes practical considerations such as the data needed, the experiments and analytical methods typically employed, and the interpretation and application of data. Chapters highlight facts, common protocols, detailed experimental designs, applications, and limitations of techniques."

"Proses invasi Plasmodium falciparum ke dalam sel darah merah merupakan tahapan penting pada infeksi malaria. Proses ini sangat kompleks melibatkan interaksi antara protein ligan pada permukaan merozoit parasit dengan reseptor permukaan pada sel darah merah inang. Reseptor sel darah merah yang digunakan pada saat invasi parasit P. falciparum diidentifikasi berdasarkan sensitivitasnya terhadap enzim neuraminidase (N), tripsin (T) dan kimotripsin (K). Penelitian ini dilakukan pada 69 darah pasien yang terinfeksi P. falciparum yang dikultur secara ex vivo secara langsung di laboratorium di Timika. Sel darah donor yang digunakan untuk uji invasi sebelumnya diberi perlakuan dengan 50 mU/ml neuraminidase, 1 mg/ml tripsin, atau 1 mg/ml kimotripsin. Kami mengidentifikasi 8 pola invasi parasit malaria dengan tipe terbanyak yang ditemukan adalah tipe A yang resistan terhadap ketiga perlakuan enzim (NrTrKr; 28,99%) dan tipe B (NsTsKr; 21,74%). Selain itu dilakukan pula analisis untuk mengetahui ekspresi relatif protein kelompok Duffy Binding Ligand (DBL) dan Reticulocytes Homolog (Rh) yang berperan pada proses invasi dengan mendeteksi ekspresi protein tersebut dari RNA yang disintesis menjadi cDNA yang diisolasi pada stadium schizon dari masing-masing isolat klinis. Protein kelompok DBL yang dianalisis adalah EBA-140, 175, 181 sedangkan dari kelompok Rh adalah Rh-1, 2a, dan 2b. Hasil analisis kuantitatif dengan real time reverse transcription PCR menunjukkan bahwa protein EBA-140, Rh-1 dan EBA-175 merupakan tiga protein ligan P. falciparum yang paling umum ditemukan pada isolat klinis parasit malaria di Timika, Papua. Variasi genetik sel darah merah seperti Southeast Asian Ovalocytosis (SAO), Gerbich negatif, dan varian hemoglobin (HbE) tidak ditemukan pengaruhnya pada proses invasi pada penelitian ini. Informasi yang dihasilkan pada penelitian ini diharapkan dapat menjadi masukkan untuk pengembangan vaksin malaria berbasis hambatan invasi parasit ke dalam sel darah merah.

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Plasmodium falciparum invasion is a complex process involving several parasite ligands and their receptors expressed on the red blood cell surface. We reported various receptors used by the parasite ligands during their invasion based on their sensitivity to neuraminidase (N), trypsin (T) or chymotrypsin (C). Most field isolates in Timika invaded red blood cells through type A receptor that was resistant to all enzyme treatments (NrTrCr; 28,99%) and type B that was sensitive to neuraminidase and trypsin (NsTsCr; 21,74%). The expression of two invasion ligands; Plasmodium falciparum Duffy binding ligand (PfDBL) and P. falciparum reticulocyte homolog (PfRh) were quantified from the schizonts stage of each isolate. We employed quantitative real-time reverse-transcription polymerase chain reaction (QRT-RT-PCR) to detect the expression of PfDBL family including EBA-140, EBA-175 and EBL-181 and PfRh genes such as Rh-1, Rh-2a, Rh-2b. We demonstrated thatEBA-140, Rh-1 and EBA-175 werethe major invasion ligands expressed in P. falciparum of Timikan isolates. The presence of red cell polymorphisms including the Southeast Asian Ovalocytosis (SAO), Gerbich negativity, and variant hemoglobin (HbE) as detected by PCR was not found to affect parasite invasion. The present study strengthens the support to include malaria invasion proteins into the development of malaria vaccine platform."

"A valuable reference tool for professionals involved in the industry, Drug Metabolism in Pharmaceuticals covers new tools such as LC-MS and LC-MS-NMR along with experimental aspects of drug metabolism. This work fills a gap in the literature by covering the concepts and applications of pharmaceutical research, development, and assessment from the point of view of drug metabolism. By providing both a solid conceptual understanding of the drug metabolism system, and a well illustrated, detailed demonstration and explanation of cutting edge tools and techniques."

"Explaining the assessment of potential drug compounds, this is an ideal introductory reference for those new to drug discovery. It includes sections on pharmacokinetics and drug metabolism, integration of pharmaceutical development, and predictive safety assessment. Topics include: cost analysis, drug transporters, cytochrome P-450 and drug-drug interactions, plasma protein binding, assessing stability, ways to optimize drug formulation, toxicology and toxicokinetics, and more. Readers will understand why absorption-distribution-metabolism-excretion-toxicology (ADMET) is key in drug development. "

"Drug Related Problem (DRPs) adalah kesalahan pengobatan yang mempengaruhi pada outcome klinis dari pasien. Jika tidak dikelola dengan baik, mengakibatkan dampak yang lebih luas dan serius bahkan sampai terjadi kejadian sentinel. Di Puskesmas Kecamatan Kalideres terdapat poli PTM yang melayani pasien dengan penyakit kronis seperti hipertensi, diabetes melitus tipe 2, hiperglikemia dan sebagainya. Pasien poli PTM ini biasa mendapat resep yang berisikan obat polifarmasi yang berisiko terjadi Drug Related Problems (DRPs). Oleh karena itu pada penulisan tugas khusus ini dilakukan pengidentifikasian jenis DRP yang terjadi pada pasien poli PTM di Puskesmas Kecamatan Kalideres pada periode April 2023. Metode yang digunakan adalah pengklasifikasi DRP berdasarkan Hepler-Strand dan kemudian direkomendasikan penyelesaian permasalahan berdasarkan literatur. DRPs menurut Hepler-Strand diklasifikasikan sebagai berikut: 1) Pemilihan obat yang tidak tepat; 2) Dosis Subterapeutik; 3) Kegagalan menerima obat; 4) Overdosis; 5) Reaksi obat yang merugikan; 6) Interaksi obat ; 7) Penggunaan obat tanpa indikasi dan; 8) Indikasi yang tidak diobati. Berdasarkan hasil validasi yang dilakukan dapat disimpulkan bahwa dari 5 resep pasien Poli PTM di Puskesmas Kecamatan Kalideres yang diindentifikasi DRPs, terdapat 1 resep yang tidak terdapat DRP dan 4 resep lainnya terdapat DRP. DRP yang didapat adalah terjadinya interaksi obat dan penggunaan obat tanpa indikasi.

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Drug Related Problems (DRPs) are medication errors that affect the clinical outcomes of patients. If not managed properly, it can have a wider and more serious impact and even lead to sentinel events. At the Kalideres Sub-district Health Center, there is a NCD clinic that serves patients with chronic diseases such as hypertension, type 2 diabetes mellitus, hyperglycemia and so on. These NCD poly patients usually receive prescriptions containing polypharmacy drugs that are at risk of Drug Related Problems (DRPs). Therefore, in this special assignment writing, the types of DRPs that occurred in Poly PTM patients at the Kalideres District Health Center in the April 2023 period were identified. The method used is DRP classification based on Hepler-Strand and then recommended problem solving based on the literature. DRPs according to Hepler-Strand are classified as follows: 1) Inappropriate drug selection; 2) Subtherapeutic dose; 3) Failure to receive the drug; 4) Overdose; 5) Adverse drug reactions; 6) Drug interactions; 7) Use of drugs without indications and; 8) Untreated indications. Based on the results of the validation carried out, it can be concluded that of the 5 prescriptions of PTM Poly patients at the Kalideres Subdistrict Health Center that DRPs were identified, there was 1 prescription that did not have DRPs and 4 other prescriptions had DRPs. DRPs obtained are the occurrence of drug interactions and the use of drugs without indications."

"Tuberkulosis (TBC) merupakan penyakit dengan risiko penularan yang tinggi. Ketidakpatuhan terhadap pengobatan menyebabkan respon pengobatan suboptimal sehingga muncul resistensi dan penularan penyakit terus menerus. Indonesia menempati urutan kedua sebagai negara yang memiliki jumlah kasus TBC terbesar setelah India (WHO, 2015). Reaksi obat tidak dikehendaki (ROTD) akibat penggunaan obat antituberkulosis (OAT) dapat mempengaruhi kepatuhan pasien. Tujuan penelitian ini adalah menilai pengaruh ROTD terhadap peningkatan risiko ketidakpatuhan berobat pada penderita TBC paru dewasa kategori I di RS Urip Sumoharjo Lampung. Desain penelitian yang digunakan adalah kasus kontrol dengan penggunaan data rekam medik. Kelompok kasus adalah pasien TBC paru dewasa kategori I yang tidak patuh dan ditandai dengan kejadian putus berobat, yaitu pasien TBC paru yang tidak memulai pengobatan atau menghentikan pengobatan selama dua bulan berturut-turut atau lebih. Kelompok kontrol adalah pasien dengan pengobatan lengkap dan dinyatakan sembuh. Populasi penelitian ini adalah seluruh rekam medik pasien TBC paru dewasa dengan umur ≥ 15 tahun kategori I yang berobat jalan di RS Urip Sumoharjo Lampung pada bulan Agustus 2013 s.d Juli 2015. Analisis data menggunakan uji chi square dan uji regresi logistik multivariat. Hasil penelitian menunjukkan bahwa pasien yang mengalami ROTD mempunyai risiko 2,143 kali untuk tidak patuh dibandingkan dengan pasien yang tidak mengalami ROTD setelah dikontrol oleh variabel pendidikan, penyakit penyerta, dan jenis OAT. Jenis OAT KDT merupakan faktor risiko terbesar bagi ketidakpatuhan pasien TBC paru dewasa kategori I. Pasien yang mendapatkan OAT jenis KDT berisiko sebesar 11,996 kali untuk tidak patuh dibandingkan dengan pasien TBC paru yang mendapatkan jenis OAT satuan setelah dikontrol oleh variabel ROTD, pendidikan, dan penyakit penyerta.

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Tuberculosis is a disease with a high risk of transmission. Poor adherence to treatment led to suboptimal response so it appears resistance and continuous transmission of the disease. In 2015 Indonesia ranks second of countries with the highest number of estimated incident tuberculosis cases after India. Adverse drug reactions of tuberculosis agents increase the risk of poor adherence. The objective of this study was to assess the risk of adult pulmonary TB patients non adherence caused by adverse drug reactions of antituberculosis agents at Urip Sumoharjo Hospital Lampung. This research is an observational study with design case control using data from medical record. Cases were defined as the pulmonary tuberculosis patients who didn?t begin treatment or stop their antituberculosis for 2 month or more. Controls were defined as the pulmonary tuberculosis patients with full treatment and were declared cured. The study population was all medical record of adult pulmonary tuberculosis patient age ≥ 15 years old with category I treatment at Urip Sumoharjo Hospital Lampung period august 2013 ? july 2015.. Data was analyzed by using chi square and multivariate logistic regression method. Result of this study showed that the patient who has adverse drug reactions of antituberculosis agent risk nonadherence 2,143 times higher than patient who has not adverse drug reactions of antituberculosis agent after controlled by educational variables, co-morbidities, and the type of OAT. Fixed dose combination of antituberculosis drug was the highest risk factor for patient non adherence. The patient who received fixed dose combination of antituberculosis drug risk nonadherence 11,996 times higher than patient who received separate antituberculosis drug after controlled by educational variables, co-morbidities, and adverse drug reactions."

"This volume presents a broad yet detailed review of current knowledge of muscarinic receptors. It describes the detailed insights that have been obtained on the structure, function, and cell biology of muscarinic receptors. This volume also describes physiological analyses of muscarinic receptors and their roles in regulating the function of the brain and of a variety of peripheral tissues. This volume shows how the study of muscarinic receptors continues to provide new and surprising insights not just to the cholinergic system but to the broad areas of neurobiology, cell biology, pharmacology, and therapeutics."