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antiviral drug
Question | Answer |
---|---|
antiviral的機轉有幾個? | 主要有六個 |
請舉出antiviral的六個機轉 | 1. 防病毒與細胞表面的receptor結合 2. 防病毒pentrate到細胞裡面 3. 防uncoating產生(M2;ion channel blockers) 4. 防複製產生(polymerase inhibitors) 5. 防蛋白質外殼產生(protease inhibitor) 6. 防病毒從已感染細胞釋放(NA inhibitor) |
請舉例出 防病毒與細胞表面的receptor結合 的藥物 | arildone、enfurirtide(HIV)、docosanol(HSV)、palivizumab(RSV) |
請舉例出 防病毒pentrate到細胞裡面 的藥物 | enfuvirtide(T-20)(HBV、HCV) |
請舉例出 防uncoating產生 的藥物 (for influenza) | amantadine、rimantadine、(M2;ion channel blockers) |
請舉例出 防複製產生 的藥物 | NRTIs(HIV)、NNRTIs(HIV)、acyclovir(HSV)、foscarmet(CMV)、entecavir(HBV) |
請舉例出 防蛋白質外殼產生 的藥物 | saquinavir、ritanavir (protease inhibitor most for HIV) |
請舉例出 防病毒從已感染細胞釋放 的藥物 | zanamivir、oseltamivir(Neuramindase;NA inhibitor) |
anti-influenza 藥物 | (一)M2 Proton Channel Antagonists: Amantadine and Rimantadine. (二)Neuraminidase Inhibitors: Zanamivir and Oseltamivir |
anti-influenza 機轉點 | 1. uncoating 2. release |
anti-herpes | Acyclovir, Valacyclovir, Penciclovir, Famciclovir, Vidarabine, Docosanol - last two are topical. |
anti-Cytomegalovirus | Ganciclovir, Valganciclovir, Cidofovir, Foscarnet. |
anti-hepatitis B/C agents | Adefovir, Entacavir, Ribavirin, Interferon-alpha. |
against RSV | Ribavirin and Palivizumab. |
against genital warts(生殖器疣) | Imiquimod. |
What is the largest barrier towards developing anti-viral drugs as compared to anti-bacterial agents? | Viruses use host machinery to replicate. Thus, drugs are difficult to make that target just the viral proteins and/or mRNA. |
M2 Proton Channel Antagonists prevent the _________ virus from __________ in host acidic endosomes. | Influenza A, uncoating. |
True/False: M2 Proton Channel Antagonists target Influenza A and a number of other viruses. | This is false. It only targets Influenza A. |
True/False: The M2 Proton Channel is located in the endosome of the host cell. | This is false. It is located in the viral capsid. |
What are the mechanisms of resistance of amantadine and rimantadine? | Resistance primarily occurs in response to mutations in the transmembrane domain of the M2 proton channel. This is uncommon, however. |
Describe the adverse reactions to Amantadine and Rimantadine. | 1. Well tolerated. 2. Some GI and CNS problems - nervousness, loss of appetite. 3. CNS problems more common with Amantadine because it can cross the blood brain barrier. |
What are the therapeutic uses of Amantadine and Rimantadine? | 1. Prevention and treatment of influenza A. 2. Seasonal prophylaxis is ~70-90% effective against Influenza A. 3. Decreases duration of symptoms by 1-2 days. |
True/False: Neuraminidase Inhibitors target both Influenza A and B. | This is true. |
Both Zanamivir and Oseltamivir are synthetic and stable analogs of __________. | sialic Acid. |
Describe the mechanism of action of neuraminidase inhibitors? | 1. Egress from the cell involves binding of viral hemagglutinin with plasma membrane sialic acid. 2. These inhibitors bind neuraminidase and prevent cleavage of cellular sialic acid and release. |
What are the primary mechanisms of drug resistance to neuraminidase inhibitors? | Rare, but through mutations in either viral hemagglutinin or neuraminidase. Hemagglutinin mutations are cross-reactive for both neuraminidase inhibitors, while neuraminidase mutations are relatively agent-specific. |
Describe the adverse reactions of neuraminidase inhibitors. | 1. Zanamivir - well-tolerated, some wheezing and bronchospasms with asthma or COPD patients. 2. Oseltamivir - GI complaints. |
Both neuraminidase inhibitors are used to treat ___________. | Influenza A AND B. |
anti-HBV 的作用點 | 1. penetration:interferon 2. copy:entecavir |
anti-HBV 有哪6個主要治療藥物 | lamivudine(干安能)、entecavir(貝樂克)、 adefovir(干適能)、telbivudine(喜必福)、 tenofovir、Interferon-α |