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antiviral therapy Flashcards

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1
Q

Hepatitis C therapy - drugs

A
  1. Interferons - α
  2. ribavirin
  3. Simeprevir
  4. Sofosbuvir
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2
Q

Ribavirin - mechanism of action

A

inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophophate dehydrogenase

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3
Q

Ribavirin inhibits synthesis of …. by

A
  • guanine nucleotides

- competitively inhibiting inosine monophophate dehydrogenase

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4
Q

Ribavirin - clinical use

A
  1. Chronic HCV

2. RSV (palivizumab is preferred in children)

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5
Q

Ribavirin - toxicity

A
  1. hemolytic anemia

2. severe teratogen

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6
Q

Simeprevir - mechanism of action

A

HCV protease inhibitor

prevents viral replication

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7
Q

Simeprevir - clinical use

A

Chronic HCV in combination with ledipasvir (NS5A inhibitor)

DO NOT USE AS MONOTHERPAY

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8
Q

Simeprevir - toxicity

A
  1. photosensitivity reaction

2. rash

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9
Q

Sofosbuvir - mechanism of action

A

inhibitis HCV RNA-dependent RNA polymerase acting as a chain terminator

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10
Q

Sofosbuvir - clinical use

A

Chronic HCV in combination with ribavirin +/- peginterferon alfa
DO NOT USE AS MONOTHERAPY

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11
Q

Sofosbuvir - side effects

A

fatique
headache
nausea

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12
Q

HIV therpay regimen

A

Highly active antiretrovial therapy (HAART)

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13
Q

HIV therpay - groups of drugs

A
  1. protease inhibitors
  2. Nucleoside Reverse Transcriptase Inhibitor (NRTI)
  3. Non-nucleoside reverse transcriptase inhibitors (NNRTI)
  4. Integrase inhibitors
  5. Fusion inhibitors
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14
Q

HAART - when to start

A

often initiated at the time of HIV diagnosis

strongeest indication for patients presenting with AIDS-defining illness, low CD4 (under 5 hundreds), or high viral load

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15
Q

HAART regimen consist of

A

2NRTIs (Nucleoside Reverse Transcriptase Inhibitor) and 1 of the following: NNRT1 (Non-nucleoside reverse transcriptase inhibitors) or protease inhibitor or integrase inhibitor

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16
Q

Protease inhibitors - drugs

A

-NAVIR

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17
Q

HIV-1 Protease in encoded by

A

pol gene

18
Q

HIV-1 Protease - function

A

assembly of virions depend on HIV-1 protease, which cleaves the polypeptide products of HIV mrna into theri functional parts

19
Q

HIV Protease inhibitors - mechanism of action

A

inhibit HIV-protease –> prevents maturation of new viruses

20
Q

HIV Protease inhibitors - toxicity

A
  1. hyperglycemia
  2. GI tolerance (nausea, vomiting)
  3. Lipodystrophy (Cushing-like syndrome)
  4. Nephropathy (indinavir)
  5. hematuria (indinavir)
  6. inhibit cytochrome P-450 (ritonavir)
21
Q

HIV protease inhibitors with antimycobacterial drugs

A

Rifampin (a potent CYP/UGT inducer) contraindicated with proteae inhibitors because it can decrease protease inhibitor concentration

22
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) - mechansim of action

A

Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (Lack of OH group

23
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) - drugs

A
  1. Abacavir (ABC)
  2. Didanosine (ddl)
  3. Emtricitabine (FTC)
  4. Lamivudine (3TC)
  5. Stavudine (d4T)
  6. Tenofovir (TDF)
  7. Zidovudine (ZDV, formerly AZT)
24
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) - structure

A

Tenofovir –> nucleotide

the others –> nucleosides and need to be phosphorylated to be active

25
Q

Zidovudine - special clinical use

A

general prophylaxis and during pregnancy to decrease risk of fetal transmission

26
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) - side effects

A
  1. Bone marrow suppression
  2. peripheral neuropathy
  3. lactic acidosis (nucleosides)
  4. anemia (ZDV)
  5. pancreatitis (didanosine)
27
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) - pancreatitis is caused by

A

didanosine

28
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) - anemia is caused by

A

ZDV

29
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) - lactic acidosis is caused by

A

nucleosides

30
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) - how to prevent side effects

A

bone marrow suppression –> granulocyte colony stimulating factor (G-CSF) and erytrhopoietin)

31
Q

Non-nucleoside reverse transcriptase inhibitors (NNRTI) - drugs

A
  1. Delavirdine
  2. Efavirenz
  3. Nevirapine
32
Q

Non-nucleoside reverse transcriptase inhibitors (NNRTI) - drugs and mechanism of action

A
  1. Delavirdine 2. Efavirenz 3. Nevirapine
    Bind to reverse transcriptase at site different from NRTIs. Do not require phosphorylation to be active or compete with nucleotide
33
Q

Non-nucleoside reverse transcriptase inhibitors (NNRTI) - toxicity

A
  1. rash
  2. hepatotoxicity
  3. vivid dreams (efavirenz)
  4. CNS sympoms (efavirenz)
  5. contraindicated in pregnancy (Delavirdine and efavirenz)
34
Q

Non-nucleoside reverse transcriptase inhibitors (NNRTI) - which drugs are contraindicated in pregnancy

A

Delavirdine and efavirenz

35
Q

HIV - integrase inhibitors - drugs?

A
  1. raltegravir
  2. Elvitegravir
  3. Dolutegravir
36
Q

integrase inhibitors - mechanism of action

A

inhibits HIV genone integration into host cell chromosome by REVERSIBLY inhibiting HIV integrase

37
Q

integrase inhibitors - toxicity

A

increased creatine kinase

38
Q

HIV - fusion inhibitors - drugs

A
  1. Enfuvirtide

2. Maraviroc

39
Q

HIV - fusion inhibitors - drugs and mechanism of action

A
  1. Enfuvirtide –> Binds gp41, inhibiting viral entry

2. Maraviroc –> Binds CCR-5 on surface of T cells/monocytes, inhibiting interaction with gp120

40
Q

HIV - fusion inhibitors - toxicity

A

skin reaction on injection sites (Enfuvirtide)

41
Q

Abacavir - special characteristic of using

A

contraindicated if patients has HLA-B*5701 mutation

Microbiology (25 decks)

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