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38 Cards in this Set

  • Front
  • Back
What are the pharmacological targets for parasites?
1. Unique Essential Enzymes found only in parasites
2. Enzymes indispensible only in parasites
3. Indispensible biochemical fxns common to both parasite and host, however w/ different pharmacological properties.
What form of the influenza virus infects humans only and what form infects all mammals?
Humans only: B
All mammals: A
What are the 5 agents used to treat Influenza A and respiratory viruses?
-Amantadine
-Oseltamivir
-Ribavirin
-Rimatadine
-Zanamivir
MOA of Amantadine?
Inhibits uncoating of viral RNA w/in the infected sell which prevents replication.
*Rimantadine is 4x's more potent)
ADE's of Amantadine?
-N/V
-CNS: Nervousness, Insomnia
MAO of Osteltamivir?
Is a Neuraminidase inhibitor, so it interferes with the release of prgency influenza virus from the infected cell to the new host.
*Prevents the spread of infection
What strain(s) or Influenza is Osteltamivir active against?
A & B
*Requires early administration to minimize replication.
What agents are availavle to treat HSV and VSV infections?
-Acyclovir
-Valacyclovir
-Famciclovir
-Penciclovir
-Docosanol
-Trifluridine
What viruses does acyclovir tx?
-HSV-1
-HSV-2
-VZV
What must happen for acyclovir to be activated?
-Must be phosphorylated (by thymidine kinase)
*active metabolite only accumulates in the infected cells
MOA of acyclovir?
Inhibits viral DNA synthesis by:
1. Competition w/ deoxyGTP for viral DNA polymerase, resulting in binding to the DNA templateas an irreversible complex.
2. Chain termination following incorporation into the viral DNA
What is acyclovir the DOC for?
-Herpes Simplex encephalitis
-Neonatal HSZ infection
-Serious HSV or VZV infections
What leads to acyclovir resistance?
-Alteration in viral thymidine kinase or DNA polymerase
*Cross resistance to Valacylovir, famciclovir, and ganciclovir
ADE's of acyclovir?
-Nausea
-Diarrhea
-HA
-If given IV: reversible renal dysfunction or neurologic toxicity (tremors, delirium, seizures)
What drug used to treat HSV is a diacetyl ester PRODRUG of 6-deoxypenciclovir?
Famciclovir
*After PO admission it is converted by 1st pass metabolisn to penciclovir.
What must happen for famciclovir to be activated?
Phosphorylation by thymidine kinase (same as acyclovir)
How is famciclovir's MOA similar to acyclovir?
-Competitive inhibition of viral DNA polymerase to block DNA synthesis, BUT it does not cause chain termination.
ADE's of Famciclovir?
-HA
-Diarhhea
-Nausea
What drug is the L-valyl ester of acyclovir?
-Valacylcolvir
*Rapidly converted to acyclovir after PO admin by intestinal and hepatic 1st pass metabolism
Compare the half lives of acyclovir and valacyclovir.
Acyclovir: 3 hrs
Valacyclovir: 30 mns
ADE's of Valacyclovir?
-N/V
-Rash
-Agitation
-Dizziness
-HA
-Liver enzyme elevation
-Anemia
*At high doses: Hallicinations and Seizures
What 4 agents are topical and tx HSV?
1. Acyclovir (IV and PO also)
2. Docosanol (Herpes labialis)
3. Penciclovir (Recurrent Herpes labialis
4. Trifluidine (Herpes keratitis, acyclovir-resistant HSV)
What is Foscarnet indicated for and how is it administered?
-Acyclovir-resistant HSV and VZV
-IV
Who is more susceptible to infection by CMV and what does CMV cause?
-Immunocomprimised individuals(AIDS or organ transplant)
-Causes:
1. Retinitis
2. Colitis
3. Esophagitis
4. CNS dz
5. Pneumonitis
*CMV can be passed to the fetus
What are the 4 main agents used to tx CMV?
1. Ganciclovir (IV,PO, intraocular implant)
2. Valganciclovir (PO only)
3. Foscarnet (IV only)
4. Cidofovir (active diphosphate)(IV only)
MOA of Foscarnet?
Direct inhibition of DNA polymerase, RNA polymerase, and HIV reverse transcriptase directly w/o requiring activation by phosphorylation.
*Is an inorganic pyrophosphate compound.
What agents are used to treat CMV retinitis?
1. Valganciclovir (PO)
2. Ganciclovir (IV, PO, Intraocular)
3. Foscarnet (IV)
4. Cidofovir (IV)
What agents are used for prophylaxis of CMV?
1. Valganciclovir (PO)
2. Ganciclovir (PO)
What cells does HIV infect?
1. T helper cells (CD4+)
2. Macrophages
3. Dendritic cells
What does HAART stand for?
Highly Active Anti-Retroviral Therapy
What are the 2 main categories of Antiretroviral Agents?
1. Nucleoside and Nucleotide Reverse Trancriptase Inhibitors (NRTI)
2. Nonnucleotide Reverse Trancriptase Inhibitors (NNRTI)
What is the only drug we talked about that is a Fusion Inhibitor used to treat HIV?
Enfuvirtide
What is the "Triple Treatment" of AIDS chemotherapy?
-2 inhibitors of HIV reverse transcriptase
-1 protease inhibitor
What is the most commonly used HAART drug combination?
-1 NRTI
-1 NNRTI
-1 Protease inhibitor
List some examples of Triple Treatment for HIV.
1. AZT(azidothymidine)+3TC (lamivudine)+Crixivan
2. AZT+d4T(stavudine)+Invirase
3. 3TC+NVP(nevirapine)+Norvir
4. d4T+DMP(efavirenz)+Viracept
5. ABV+DMP+Agenerase
What are the drugs that make up Combivir?
AZT+3TC
What are the drugs to tx Hepatitis B?
1. Lamivudine
2. Adefovir
3. Entecavir
4. Interferon Alfa 2b
What are the drugs to tx Hepatitis C?
1. Ribavirin
2. Interferon Alfa 2b
3. Interferon Alfa 2a