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Pharmacology > Multi-Systems: Antiviral Agents > Flashcards

Multi-Systems: Antiviral Agents Flashcards

1
Q

(2) Anti-herpes-viral drugs that are Guanosine analogs that
inhibit Nucleic Acid Synthesis?

A

Acyclovir (HSV, VZV)

Ganciclovir (CMV)

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2
Q

Mechanism of Acyclovir and Ganciclovir?

A
  • Acts as a Chain terminator and Viral DNA Polymerase Inhibitor (HSV-enzyme required to activate)
  • Guanosine analog w/ Acyclic Sugar
  • Phosphorylated by Viral Thymidine Kinase
  • -> acylcoGMP –> acycloGTP
  • Valacyclovir + H2O –> Acyclovir + Valine
  • Valganciclovir + H2O –> Ganciclovir + Valine
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3
Q

Clinical use of Acyclovir and Ganciclovir?

A
  • Acyclovir
    • HSV-1, HSV-2
    • VZV
    • EBV
  • Ganciclovir
    • CMV
    • HHV-6, HHV-7
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4
Q

Resistance to Acyclovir and Ganciclover?

A
  • Deleted or Mutated - Viral Tyrosine Kinase
  • Resistant - Viral DNA Polymerase
  • No effect during latent infection because Viral Tyrosine Kinase is not expressed
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5
Q

Drugs that work on CMV?

A
  • Ganciclovir (Guanosine analog)
  • Foscarnet (Viral DNA polymerase inhibitor)
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6
Q

(2) Anti-herpes-viral, Viral DNA polymerase inhibitors that stop Nucleid Acid Synthesis?

A
  • Foscarnet (CMV)
  • Cidofovir (HSV* - Acyclovir resistant)
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7
Q

Mechanism of Foscarnet?

A
  • An inorganic pyrophospate analog that Inhibits Viral DNA polymerase w/out requireng activation via Phosphorylation by Viral Kinases.
  • Effective against resistant strains of HSV, VSV, and CMV
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8
Q

Clinical use of Foscarnet?

A
  • Acyclovir-resistant HSV and VZV
  • Ganciclovir-resistant CMV
    • ​Produces less Bone Marrow suppression than Ganciclovir
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9
Q

SEs of Foscarnet?

A
  • Nephrotoxicity
  • Foscarnet acts as a Potent Chelator of divalent Cations
  • -> decreased ionized Ca2+, Mg2+
  • -> Symptomatic Hypocalcemia w/ normal Serum Ca2+
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10
Q

Resistance to Foscarnet?

A
  • Foscarnet binds to the pyrophosphate binding site of the DNA polymerase
  • -> Mutations in DNA Polymerase that prevent binding
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11
Q

(2) Antiviral drugs that Block the
Influenza A M2 Protein Channel
–> Preventing Uncoating of Influenza virion
–> Req’d for Infection

A
  • Amantadine
  • Rimantadine
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12
Q

Mechanism of Amantadine and Rimantadine?

A
  • M2 channel conducts Protons from the Endosome into the Virion
  • -> Acidification of the Interior and Dissociation of the Matrix protein from Viral ribonucleoproteins (RNPs)
  • Amantadine / Rimantadine prevent Virion from fusing w/ the Endosomal membrane and stops from Releasing contents into Cytoplasm
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13
Q

Clinical use of Amantadine and Rimantadine?

A
  • Influenza A infections
  • No longer used though due to increased Resistance
  • Resistance arises rapidly via Single-point mutation of M2 protein
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14
Q

(1) Hepatitis Anti-viral, Guanine nucleotide Synthesis that Inhibits Nucleic Acid Synthesis?

A
  • Ribavirin
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15
Q

Mechanism of Ribavirin?

A
  • Guanosine analog that is Phosphorylated by Cellular enzymes
  • Inhibits Syn. of Guanine Nucleotides by competitively inhibiting Inosine Monophosphate Dehydrogenase
  • Inhibits IMP dehydrogenase
  • -> Impaired Purine synthesis
  • Inhibits Viral RNA polymerase and 5’ cap formation on mRNAs
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16
Q

Clinical use of Ribavirin?

A
  • Chronic HCV Infection (in combination w/ IFN-α)
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17
Q

SEs of Ribavirin?

A
  • Hemolytic anemia when administered IV
  • Severe Teratogenic
  • Oncogenic
  • Gonadotoxic
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18
Q

Small polypeptide (18 kd) that binds to a cellular receptor
and Induces a Antiviral Cellular State?

A
  • IFN-α
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19
Q

Mechanism of IFN-α?

A
  • Binds to Cellular Receptor and Induces a Antiviral Cellular State
    1. ​​Phosph. of EF 2 –> Inhibit Peptide Chain Initiation
    2. Ribonuclease Activation –> degrade Viral mRNA
    3. Phosphodiesterase exp –> degrade tRNAs
  • -> inhibit Peptide Chain Elongation
    1. Increase Natural killer cell lytic function
    2. Increase exp. of MHC Class I molecules
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20
Q

Clinical use of IFN-α?

A
  • Chronic Hepatitis B and Hepatitis C Infections
  • Anti-tumor effect on various cancers
    • Melanoma
    • Hairy cell leukemia
    • Kaposi’s Sarcoma
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21
Q

SEs of IFN-α?

A
  • Flu-like Symptoms
    • Fever
    • Myalgias
    • Malaise
  • Neutropenia
  • Thrombocytopenia
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22
Q

(2) Drugs that Reversibly Inhibit Neuraminidase (NA)
of Influenza A and B and impairs budding of Virions?

A
  • Zanamivir
  • Oseltamivir
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23
Q

SEs of Zanamivir and Oseltamivir?

A
  • Bronchospasm
  • Oseltamivir (Tamiflu) is a prodrug that is converted by the Liver to an Active neuraminidase Inhibitor after Oral Administartion
    • Used for Treatment and Prophylaxis of Influenza A and Influenza B Infections.
24
Q

Mechanism of Enfuvirtide?

A
  • Polypeptide Fusion inhibitor
  • Binds to the First Heptad-repeat (HR1) in the
  • *gp41** subunit of the HIV envelope glycoprotein and
  • *Prevents** the Conformational changes Req’d for the Fusion of Viral and Cellular membranes
  • HIV is prevented from establishing infection in the Target Cell.
25
Q

Clinical use of Enfuvirtide?

A
  • HIV infection
  • Salvage regimens to treat Multi-drug-resistant HIV
26
Q

(3) Drugs that are Fusion Inhibitors?

A
  1. Maraviroc (HIV - CCR5 as a co-receptor)
  2. Enfuvirtide (HIV - gp41 HRI region)
  3. Palivizumab (RSV)
27
Q

Mechanism of Maraviroc?

A
  • This entry inhibitor Binds to the CCR5 Receptor on
  • *Macrophages**, T cells, and Dendritic cells
  • Prevents HIV from using CCR5 as a co-Receptor
  • Blocks entry of CCR5-trophic HIV into cells
28
Q

Clinical use of Maraviroc?

A
  • HIV Infection
  • Primarly to salvage regiments of multi-drug-resistant HIV
  • Prior to intiation of Therapy, a Viral tropism assay should be done to Exclude CXCR4 or dual trophic HIV Infection
29
Q

SEs of Maraviroc?

A
  • Cardiovascular
    • Myocardial Ischemia
    • Myocardial Infarction
30
Q

Mechanism of Raltegravir?

A
  • An Integrase inhibitor that reversibly
  • *Inhibits HIV Integrase** –> Preventing the HIV genome from being inserted into the Host cell Chromosome.
31
Q

Clinical use of Raltegravir?

A
  • HiV infection
32
Q

(5) Drugs used for HSV?

A
  1. Acylovir
  2. Ganciclovir
  3. Foscarnet
  4. Cidofovit
  5. Trifluridine
33
Q

(1) Drug used for EBV?

A
  • Acyclovir - Oral Hairy Leukoplakia only
  • Anti-viral therapy is not indicated for **Infectious Mononucleosis
  • ->**They will break out in a Full-Body Head to Toe Rash
34
Q

(4) Drugs used for VZV?

A
  1. Acyclovir
  2. Ganciclovir
  3. Foscarnet
  4. Cidofovir
35
Q

(3) Drugs used for CMV?

A
  1. Ganciclovir
  2. Foscarnet
  3. Cidofovir
36
Q

(5) Drugs used for HBV?

A
  • Tenofovir
  • Entecavir
  • Telbivudine
  • Lamivudine
  • INF-α
37
Q

(2) Drugs used for Influenza A?

A
  • Zanamivir
  • Amantadine
38
Q

(1) Drug used for Influenza B?

A
  1. Zanamivir
39
Q

(1) Drug for RSV?

A
  • Ribavirin
40
Q

(2) Drugs for HCV?

A
  • Ribavirin
  • IFN-α
41
Q

(6) Drugs that Inhibit HIV’s Reverse Transcriptase (RT):
AZT (Azidothymidine) - ?

(Nucleoside RT Inhibitors - NRTIs)

“SEAL-DZ”

A
  • Stavudine (d4T)
  • Emtricitabine (FTC)
  • Abacavir (ABC)
  • Lamivudine (3TC)
  • Didanosine (ddl)
  • Zidovudine (ZDV) –> Used for general Porphylaxis and During Pregnancy to decrease risk of Fetal Transmission
42
Q

Mechanism of AZT?

A
  • Nuclear analog of Thymidine –> Phosphorylated by Cellular Enzymes –> Zidovudine Triphosphate
  • -> Inhibits HIV’s Reverse Transcriptase (RT)
  • NRTI’s lack the Hydroxyl group at 3’ Position req’d for addition of Further Nucleotides
  • -> Chain Termination when Incorporated into DNA
43
Q

Clinical use of AZT?

A
  • HIV-1 and HIV-2
  • Decrease incidence of Maternal-fetal HIV Transmission
    (w/ combination treatment)
  • Post-HIV exposure Prophylasix (needlestick, sexual)
44
Q

SEs of AZT?

A
  • Myelosuppression
  • Increased MCV –> used to verify compliance
  • **Mitochondrial toxicity
  • -> Lactic acidosis
  • -> Hepatic acidosis**
  • -> Peripheral Fat Wasting
45
Q

(3) Drugs that Inhibit HIV and HBV Reverse Transcriptase?
And acts as a Chain Terminator when
Incorporated into Viral DNA?

“CAdT”

A
  • Cidofovir
  • Adelovir Dipivoxil
  • Tenofovir (TDF)
46
Q

Mechanism of Tenofovir?

A
  • Nucleotide analog of Adenosine
  • Addition of Two more Phosphate groups by Cellular enzymes
  • -> Inhibitor of HIV and HBV Reverse Transcriptase
  • Also, acts as a Chain Terminator when incorporated into Viral DNA
47
Q

Clinical use of Tenovir?

A
  • HIV Infection
  • Chronic HBV infection
    • Including HBV strains resistant to Lamivudine
48
Q

SE of Tenovir?

A
  • Nephrotoxicity
    • Especially w/ Adefovir and Cidofovir
  • Nucleotide analogs (NOT nucleoside analogs) are actively secreted by and are Toxic to the PCVT (Kidney)
  • Co-administration of Probenecid decreases Toxicity (by preventing drug accumulation in Renal tubular cells) and Increases Serum Drug levels
  • Severe“Rebound” Heptatitis can occur upon discontinuation if HBV infection persists
  • CONTRAINDICATED: Pregnancy (development and Bone abnormalities)
49
Q

(4) Drugs that Inhibit HIV’s Reverse Transcriptase (RT)?

(Non-nucleoside Reverse Transcriptase Inhibitor - NNRTI)

“NEED”

A
  • Nevirapine
  • Efavirenz
  • Etravirine
  • Delaviradine
50
Q

Mechanism of NNRTI’s?

A
  • Binds w/ High Affinity to and Inhibits HIV’s Reverse Transcriptase (RT)
  • Does not require Phosphorylation to be active or complete w/ Nucleotides
  • HIV-2 RT is not inhibited
51
Q

Clinical use of NNRTI’s?

A
  • HIV-1
52
Q

SEs of NNRTI’s?

A
  • Neuropsychiatric effects
    • ​Feeling “Hung-over”
    • Bizarre and Vivid Dreams
  • CONTRAINDICATED - Pregnancy (Teratogenic)
53
Q

(9) Drugs that Inhibit the HIV Protease that is responsible for Cleaving the two polyprotein products of HIV mRNA?

(gag and gag-pol polyproteins)

“F-SALT-RIND”

A
  • Fosamprenavir
  • Saquinavir
  • Atazanavir
  • Lopinavir
  • Tipranavir
  • Ritonavir
  • Indinavir
  • Nelfinavir
  • Darunavir
54
Q

SEs of HIV protease inhibitors?

A
  • GI Distress
  • Lipodystrophy
    • Glucose Intolerance
    • Hyperlipidemia
  • Myocardial Infarction (small)
55
Q

What is special about Ritonavir?

A
  • Ritonavir is a PI that potentially inhibit CYP450
  • -> multiple drug interactions
  • Co-administered w/ other Protease Inhibitors give w/ Ritonavir to “Boost” their serum levels
56
Q

Used topically for HSV-1 and HSV-2 Eye Infections?

A
  • Trifluridine
    • Thymidine analog
    • Phosphorylated by both Viral and Cellular Thymidine Kinases
    • Breackage and Faulty protein production
    • Inhibits DNA Synthesis

Pharmacology (29 decks)

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