繼續教育 Therapeutics of Clinical Drugs 臨床藥物治療學 (chemokinecoreceptors) CCR5 CXCR4 (CCR5) HIV-1 R5 (macrophage) M (M-tropic) (CXCR4) HIV X4 CD4+ T T (T-tro

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1 藥學雜誌 HIV 病毒及其相關治療藥物簡介中山醫學大學附設醫院藥劑科藥師廖文聰蕭如君中山醫學大學醫學系兼任講師蔡敏鈴摘要 (human Immunodeficiency Virus, HIV) (acquired immune deficiency syndrome, AIDS) HIV HIV HIV AIDS HAART acquired immune deficiency syndrome 壹前言 (lentivirus) T 4 (cluster of differentiation 4 receptors CD4)+ T CD4+ T 臨床HIV 藥物治療學3 gp 120 gp 41 (glycoprotein gp) gp 120 HIV-1 () 貳 HIV 病毒簡介一 HIV 病毒的基本結構 HIV RNA 70 Env 1 圖一 HIV-1 病毒的基本構造二病毒的趨向 (tropism) HIV CD4+ T gp 120 CD4+ T

2 繼續教育 Therapeutics of Clinical Drugs 臨床藥物治療學 (chemokinecoreceptors) CCR5 CXCR4 (CCR5) HIV-1 R5 (macrophage) M (M-tropic) (CXCR4) HIV X4 CD4+ T T (T-tropic) X4R5 (dual-tropic) CCR5-32 R5 三病毒的複製過程 HIV-1 gp 120 CD4 CCR5 gp 41 gp 41 () DNA HIV-1 (reverse transcriptase) (ribonuclease) RNA DNA (cdna) DNA-dependent DNA polymerase cdna DNA DNA DNA (integrase) DNA DNA B (nuclear factor kappa- 78 THE JOURNAL OF TAIWAN PHARMACY Vol.32 No.2 light-chain-enhancer of activated B cells NF- B)T T DNA mrna mrna (regulatory proteins) Tat Rev Tat Rev mrna ( full-length mrna) mrna (structural proteins) Gag Env Gag (budding) (budded virion) Gag (Gag-polyproteins) (protease) (matrix) (capsid) (nucleocapsid) () 2 圖二 HIV-1 病毒進入細胞過程

3 3 圖三 HIV-1 病毒複製過程及抗病毒藥物作用部位四病毒的遺傳變異 HIV-1 RNA (recombination) DNA (copy-choice) RNA 2 20 RNA 參抗 HIV-1 病毒藥物使用時機及注意事項 4 CD4 500 cells/ LCD4 > 500 cells/ L HIV 臨床藥物治療學 322 (nucleoside reverse-transcriptase inhibitors NRTI) (non-nucleoside reversetranscriptase inhibitors NNRTI) (protease inhibitors PI) 4,5 肆藥物簡介一 NRTI 類 DNA DNA HIV ( ) M184V 藥學雜誌

4 繼續教育 Therapeutics of Clinical Drugs 臨床藥物治療學 lamivudine zidovudine abacavir 表一 NRTI 類藥品資料 Zidovudine Lamivudine () (ZDV) (3TC) 500 mg 00 mg mg 300 mg g/dl g/dl 二 NNRTI 類 CYP450 Rilpivirine PH NNRTI 三 PI 類 gag-polyproteins 80 THE JOURNAL OF TAIWAN PHARMACY Vol.32 No.2 Tenofovir disoproxil fumarate (TDF) lamivudine () Abacavir (ABC) Didanosine (ddi) Retrovir 3TC Viread Ziagen Videx EC 300 mg mg 00 mg HLA-B* HIV-1 RNA 2. HLA-B* % 1% 0 4% mg mg mg NNRTI PI CYP3A4 四其他類 raltegravir 五複方 ( 一 )Kivexa Abacavir 00 mg + lamivudine 300 mg 40 kg CrCl 50 ml/min lamivudine abacavir

5 ( 二 )Truvada Tenofovir 300 mg + emtricitabine 200 mg CrCl50 ml/min ml/min 4830 ml/ min ( 三 )Combivir Zidovudin300 mg + lamivudine150 mg 30 kg CrCl 50 ml/min lamivudine ( 四 )Atripal Ttenofovir 300 mg + emtricitabine 200 mg + efavirenz 00 mg CrCl50 ml/min 表二 NNRTI 類藥品資料 () Nevirapine (NVP) Efavirenz (EFV) 臨床HIV 藥物治療學Darunavir (DRV) 322 Rilpivirine (RPV) Viramune Stocrit Edurant mg (2 ) CD4 CD4 250 cell/mm CD4400 cell/mm 3. HDL 表三 PI 類藥品資料 () Lopinavir/ritonavir (LPV/r) Atazanavir (ATV) 00 mg 25 mg 40% 50% 1. QTc ( EFV ) ,000 copies/ml RPV Ritonavir (RTV) Kaletra Reyataz Prezista Norvir mg/100 mg lopinavir mg/200 mg (1)300 mg Ritonavir 100 mg Ritonavir 400 mg (2) viread H2-blocker PPI 300 mg Ritonavir 100 mg ( H2-blocker H2-blocker 10 Reyataz H2- blocker 210 PPI 12 ) (3) stocrit 400 mg Ritonavir 100 mg Ritonavir (Darunavir CYP3A Ritonavir CYP3A Darunavir 14 ) mg Ritonavir 100 mg 2. DRV (V11I, V32I, L33F, I47V, I50V, I54L, I54M, T74P, L7V, I84V, L89V) 00 mg RTV (100 mg) 倂 12%-28% 300 mg 200 mg 1400 mg RTV ( ) RTV 100 mg-400 mg 藥學雜誌

6 繼續教育 Therapeutics of Clinical Drugs 臨床藥物治療學 P R QT 4. ( ) 5. 表四其它類藥品資料 Enfuvirtide Raltegravir () (ENF T-20) (RAL) 90 mg 3.1cc C24 HIV-1 gp THE JOURNAL OF TAIWAN PHARMACY Vol.32 No.2 2. (1)300 mg Ritonavir 100 mg (2) PPI stocrit (3) viread H2-blocker 400 mg Ritonavir 100 mg 2. PR Maraviroc (MVC) Fuzeon Isentress Celsentri DNA DNA HIV-1 CPK 3. DRV Darunavir10.3% (DRV sulfonamide Stevens-Johnson syndrome ) PR CCR5 HIV 300 mg CYP3A4150 mg CYP3A400 mg CCR5 HIV-1 gp120 CCR5 CCR5 HIV CCR5 伍結論 HIV copies/ml 4 HIV-1

7 藥學雜誌臨床HIV 藥物治療學Wen-Tsung Liau 1, Ju-Chun Shiao 1, Min-Ling Tsai 2 Department of Pharmacy, Chung Shan Medical University Hospital 1 Institude of Medicine, Chung Shan Medical University Introduction of Human Immunodeficiency Virus and Anti- Human Immunodeficiency Virus Drugs Abstract Acquired immune deficiency syndrome (AIDS) is caused by a virus called Human immunodeficiency virus (HIV) which infects the host and proceeds to replicate the virus and results in destroying immune system of the host. Here, we want to introduce to the readers about the basic concepts of HIV and the classification and characteristics of the anti-hiv drugs including "highly active anti-retroviral therapy"haart. 參考資料 : Monica Gandhi, M. D., M. P. H., and Rajesh T. Gandhi, M. D.: Single-Pill Combination Regimens for Treatment of HIV-1 Infection. N Engl J Med 2014; 371: Huldrych F. Gunthard, MD; Judith A. Aberg, MD; Joseph J. Eron, MD, et al: Antiretroviral Treatment of Adult HIV Infection 2014 Recommendations of the International Antiviral Society USA Panel. JAMA. 2014;312(4):

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