Anti-viral drugs Flashcards

1
Q

DNA viruses

A
  • HSV, HBV
  • genome replication takes place in the cell nucleus
  • they are dependent on the host cell’s DNA and RNA synthesizing machinery
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2
Q

RNA viruses

A
  • HCV, influenza virus
  • replication usually takes place in the cytoplasm
  • use their own enzymes to replicate RNA and create copies of their genomes
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3
Q

RNA retroviruses

A
  • HIV

- integrate the DNA copy of viral RNA produced by reverse transcriptase into the host genome as a provirus

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4
Q

Which type of therapy has a greater clinical effectiveness?

A

Combination therapy

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5
Q

Viral replication

-steps

A
  1. Attachment of the virus to the receptors on the host cell surface
  2. Entry of the virus through the host cell membrane
  3. Uncoating of viral nucleic acid
  4. Synthesis of early regulatory proteins
  5. Synthesis of new viral RNA or DNA
  6. Integration into the nuclear genome
  7. Synthesis of late, structural proteins
  8. Assembly (maturation) of viral particles)
  9. Release from the cell
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6
Q

Drugs for herpes

  • names
  • mechanism of action
A

Acyclovir
Ganciclovir
Valaciclovir

-inhibits the synthesis of new viral DNA

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7
Q

Acyclovir

  • mechanism of action
  • pharmacokinetics
  • indications
A

-acts as a competitive substrate for DNA polymerase (inhibits synthesis) and chain termination after its incorporation into viral DNA

  • topica, oral, i/v, renal excretion
  • herpes simplex virus and varicella zoster virus
  • mucocutaneous and genital herpes lesions
  • prophylaxis in AIDS and in other immunocompromised patients
  • i/v: severe herpes disease
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8
Q

Acyclovir

  • effect on which phase of viral replication?
  • unwanted effects
  • in comparison to Valacyclovir?
A
    1. Synthesis of new viral DNA
  • nephrotoxicity
  • Valacyclovir has a longer duration of action
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9
Q

Gancyclovir

  • mechanism of action
  • pharmacokinetics
  • indications
A

-same as Acyclovir

  • i/v, penetrates well into tissues, renal elimination, oral bio-availability less than 10%
  • cytomegalovirus (HSV-5), HSV

-prophylaxis and treatment of cytomegalovirus infections in immunocompromised patients

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10
Q

Gancyclovir

  • unwanted effects
  • in comparison to Valganciclovir?
A
  • bone marrow depression (neutropenia)

- high oral bio-availability and decrease use of i/v gancilovir in CMV

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11
Q

Drugs for influenza

-names

A

Amantadine
Rimantadine
Oseltamivir
Zanamivir

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12
Q

Amantadine and Rimantadine

  • mechanism of action
  • indications
A
  • inhibit an early step in replication of the influenza A (but not influenza B) virus
  • prevent uncoating by binding to proton channel
  • used for prophylaxis, they have no effect if you are already sick
  • can reduce the duration of symptoms if given within 48h after contact
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13
Q

Amantadine and Rimantadine

  • effect on which phase of viral replication?
  • unwanted effects
A
    1. Uncoating of viral nucleic acid

- GI irritation, dizziness, ataxia, slurred speech

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14
Q

Oseltamivir and Zanamivir

  • mechanism of action
  • pharmacokinetics
  • indications
A

-inhibitors of neuraminidases produced by influenza A and B –> inhibit viral release from the cell

  • Oseltamivir: oral, Zanamivir: inhalation
  • should be used only if you already have symptoms
  • decrease the time to alleviation of influenza symptoms; are more effective if used within 24h after onset of symptoms
  • prophylatically decrease incident of influenza
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15
Q

Oseltamivir and Zanamivir

  • effect on which phase of viral replication?
  • unwanted effects
A
    1. release from the cell

- GI symptoms (Oseltamivir)m bronchospasms in asthmatic patients (zanamivir)

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16
Q

Drugs for HBV and HCV

-names

A
Interferon gama (PEGylated interferon) 
Ribavarin
17
Q
Interferon gama (PEGylated interferon) 
-mechanism of action
A
  • it is a cytokine –> increases formation of antiviral proteins (ribonuclease) –> degrades viral mRNA
  • promotes formation of natural killer cells that destroy infected lived cells
18
Q

Hepatitis C viral infection is treated with…

A

Protease + Polymerase inhibitors

19
Q

Interferon gama (PEGylated interferon)

  • pharmacokinetics
  • indications
A
  • intramuscular or subcutaneous infection, elimination via kidney
  • given once weekly

-chronic HCB/HBV - monotherapy or in combinations with ribavarin

20
Q

Interferon gama (PEGylated interferon)

  • unwanted effects
  • contraindications
A
  • bone marrow depression

- pregnancy

21
Q

Ribavirin

  • mechanism of action
  • effect on which phase of viral replication?
A
  • inhibits virus replication of DNA and RNA viruses
  • inhibits guanosine triphosphate formation –> prevents capping of viral mRNA and block RNA dependent RNA polymerases
    1. Synthesis of new viral RNA or DNA
22
Q

Ribavirin

  • pharmacokinetics
  • indications
A
  • oral (avoid antacids), i/v, aerosol, eliminated by the kidney
  • used in combination with interferon gamma in chronic HCV infection
23
Q

Ribavirin

  • unwanted effects
  • contraindications
A
  • hemolytic anemia, conjunctival and bronchial irritation (aerosol)
  • pregnancy
24
Q

Drugs for HIV

-name

A

Zidovudine

25
Q

Current approach to treatment of infection with HIV (4)

A
  • initiation of treatment with 3 or more anti-retroviral drugs
  • nucleoside reverse transcriptase inhibitors (NRTIs) together with inhibitors of HIV protease (PIs)
  • combinations of at least 3 drugs (2 reverse transcriptase inhibitors + 1 protease inhibitor)
  • change to new regimen if plasma viral concentration increases
26
Q

Zidovudine

-mechanism of action

A
  • Nucleoside Reverse Transcriptase inhibitor
  • competitively inhibit binding of natural nucleotides to the binding site of reverse transcriptase
  • act as chain terminators via their insertion into the growing DNA chain
  • resistance emerges rapidly when are used as single agents
27
Q

Zidovudine

  • effect on which phase of viral replication?
  • unwanted effects
A
    1. Synthesis of new viral RNA or DNA

- bone marrow suppression