Antivirals Flashcards
Drugs that affect (3):
Attachment and penetration
- Enfuviritide (HIV)
- Docosanol (HSV)
- Palivizumab (RSV)
- Maraviroc
Drugs that affect (2):
Uncoating
- Amantadine
- Rimantadine (Influenza)
Drugs that affect (5):
Synthesis of viral components
- NRTIs (HIV)
- NNRTIs (HIV)
- Acyclovir (HSV)
- Foscarnet (CMV)
- Entecavir (HBV)
Drug that affects (1):
Packaging and assembly of virus particle
- Protease inhibitors (HIV)
Drug that affects (1):
Release of virus
- Neuraminidase inhibitors (Influenza)
Virus attaches to specific receptors on host cell and becomes internalized
Attachment and penetration
Protein coat of the virus is dissolved by viral enzymes to liberate viral RNA or DNA
Uncoating
Virus takes over host cell nucleus and replicates its DNA or RNA, then makes proteins
Synthesis of viral components
Viral genome may be encapsulated by viral protein, multiple membranes, or no protein
Packaging and assembly of virus particle
Some viruses are released rapidly and kill the host cell; others are released slowly and allow the cell to survive
Release of virus
Herpes Drugs (4)
- Acyclovir (Zovirax)
- Valacyclovir (Valtrex)
- Famciclovir (Famvir)
- Docosanol (Abreva)
Acyclovir MOA (3)
- Guanosine analoge
- Activated by viral thymidine kinase
- Inhibits DNA synthesis by competing with dGTP
Acyclovir Admin and t 1/2
- Oral
- Topical
- IV
- Short half life, dose 3-4qd
Acyclovir Elimination
Kidney
- Decreased renal fxn will affect drug significantly
Prodrug of Acyclovir
Valacyclovir
- Higher biavail
- Food does NOT affect absorption
DOC Herpes
Acyclovir
Acyclovir Tx (3)
- Genital herpes, herpes keratitis, herpes zoster, herpes encephalitis, varicella zoster
- Prophylaxis in organ transplant
- Chronically to immunocomp
Acyclovir SE (3)
Well tolerated
- N/V, HA
- Nephrotoxic with high IV dose (hydrate)
- Somnolence/lethargy with Zidovudine in HIV pts
- Safe in pregnancy
Famciclovir (Famvir) / Penciclovir MOA and features
t 1/2, elimination
- Phosphorylated by viral thymidine kinase
- Similar to acyclovir
- Longer t 1/2
- Renal elimination
Docosanol MOA
- Inhibits viral fusion to cell membrane
Docosanol Tx
- OTC cold sores
CMV/Herpes Drugs (5)
- Ganciclovir
- Valganciclovir
- Cidofovir
- Foscarnet
- Fomvirsen
Ganciclovir & Valganciclovir MOA (3)
- Inhibits CMV DNA replication
- Activated by viral kinase in cells infected with herpes or CMV
- Less selective than acyclovir (more toxic)
Ganciclovir Admin
IV
Valganciclovir Admin
Oral
Ganciclovir & Valganciclovir Tx (3)
Tx or prophylaxis of CMV/Herpes
- Immunocomp
- Transplant pts
- CMV retinitis
Ganciclovir & Valganciclovir SE (5)
- Neutropenia, thrombocytopenia (mainly when high doses given IV, especially when combined with Zidovudine)
- Nausea, fever (most common)
- Rash
- Phlebitis
- Confusion, headache, seizures
- Abnormal liver function tests
Other drugs for CMV/Herpes that do NOT req activation (2)
- Cidofovir
- Foscarnet
Cidofovir Tx
- Resistant CMV/Herpes
Cidofovir SE
- Renal tox (use probenecid/hyrate)
Foscarnet MOA
- Inhibits DNA and RNA polymerase, reverse transcriptase
Foscarnet Admin
IV
Foscarnet Tx
- Resistant CMV/Herpes
Foscarnet SE (1)
- Renal toxicity
Fomvirsen MOA
- Antisense compound to viral mRNA
Fomvirsen Tx
- CMV retinitis (intraocular)
Fomviersen SE (2)
- Ocular inflammation
- Visual haze
Influenza Drugs (4)
- Oseltamivir
- Zanamivir
- Amantadine
- Rimantadine
Neuraminidase Inhibitors (2)
- Oseltamivir
- Zanamivir
Oseltamivir & Zanamivir MOA (2)
- Neuraminidase Inhibitors
- Block release of virus
Oseltamivir Tx (2)
- Influenza Type A and B
- Bird flu
Zanamivir Tx
- Influenza A and B
Oseltamivir Admin and SE
- Oral
- NAUSEA/VOMITING (take with food)
Zanamivir Admin and SE
- Inhaled or intranasal
- May worsen RESPIRATORY fxn in COPD
- Bronchospasm in asthmatics
Amantadine MOA
- Inhibits uncoating of virus
Amantadine Tx
- Influenza A tx and prophylaxis
Amantadine Elimination
- Renal
Amantadine SE (2)
- CNS HALLUCINATIONS
- N/V
- Rarely used
Rimantidine vs Amantadine SE
- Rimantidine does NOT enter CNS = NO hallucinations
RSV Drugs (2)
- Ribavirin
- Palivizumab
Ribavirin MOA (4)
- Purine analogue
- Becomes phosphorylated
- Inhibits viral RNA synthesis
- Inhibits RNA polymerase and synthesis of GTP
Ribavirin Tx (3)
- Active against many viruses
- RSV
- Hep C
Ribavirin Admin
- Aerosol (RSV)
- IV (Lassa, SARS)
- Oral
Ribavirin SE (4)
- Pulmonary, dyspnea
- Hypotension
- Anemia
- Depression, lethargy
- GI