Exam 8: Antivirals Flashcards
Gamma Globulin Mechanism
Prevent attachment and penetration of viral particles
Gamma globulin adverse effects?
Systemic anaphylaxis
Pavilizumab
Monoclonal Antibody to RSV
Used in high risk infants by IV administration
Amantidine Mechanism
Blocks the M2 viral protein and causes buffering of the endosomal pH, preventing viral penetration and uncoating
Amantidine Uses (2)
- Influenza A Respiratory tract illness (Not effective against B)
- Also used as an Antiparkinsonian agent
What surface Antigens are used to type Influenza?
Hemagglutinin
Neuraminidase
(example: H1N1)
What is Neuraminidase important for?
A cleavage reaction required for release of virions from infected cells
What is Hemagglutinin important for?
Attachment of the virus to silica acid residues on the cell (important for penetration
Zanamivir mechanism
Inhibits neuraminidase of Influenza virus
Zanimivir uses
Influenza A and B
Oseltamivir Mechanism
Inhibits neuraminidase of Influenza virus
What is the difference between Zanamivir and Oseltamivir?
Oseltamivir can be taken orally and reaches places other than the respiratory tract.
Ribavirin Mechanism
Purine analog
Inhibits viral RNA synthesis
Ribavirin Uses (2)
- RSV in infants and young children
2. Chronic Hepatitis C (with IFN alpha)
Ribavirin Adverse Effects
Teratogenic
Pregnant healthcare workers should avoid caring for patients receiving aerosolized Ribavirin
Trifluridine Mechanism
Pyrimidine analog (Thymidine) Inhibits viral DNA synthesis
Trifluridine Uses
HSV1 and 2
Used topically for HSV keratoconjunctivitis or keratitis
Trifluridine Adverse Effects
Teratogenic
Acyclovir Mechanism
Purine Analog derived from Guanine
Must be phosphorylated to be active (done by Herpes’ intrinsic Tyrosine Kinase)
Inhibits viral DNA polymerase
How is Acyclovir selective?
It must be activated by a viral Tyrosine kinase.
Makes it non toxic to normal human cells
What is a problem with Acyclovir use?
Resistance is starting to occur.
Acyclovir uses
IV against Herpes viruses (all kinds of manifestations)
Topical agains mucocutaneous and keratitis caused by herpes
Also taken orally for VZV and herpes in the immunocompromised
Gancyclovir Uses
Cytomegalovirus retinitis
Gancyclovir Adverse effects (3)
- Teratogenic and carcinogenic
- Granulocytopenia, thrombocytopenia
- Myelosuppression
Foscarnet mechanism
Inhibits Viral DNA polymerase
Foscarnet use
used for cytomegalovirus retinitis in AIDS patients!
Foscarnet advise effect
Renal Toxicity
Name 3 Hep B drugs
Lamivudine
Tenofovir
Emtricitabine
Interferon Alpha Mechanism
Alarm Molecule
Signals neighboring cells to prepare to defend themselves form viral infection.
Cells produce enzymes that inhibit viral transcription, translation, protein processing, and virus maturation.
Interferon alpha uses
- Cutaneous warts
- Herpes keratoconjunctavitis
- Hepatitis B and C (+ribavirin)
- Also some cancers (bladder, karposi, hairy cell lymphoma)
Interferon alpha adverse effects
mild/moderate flu like syndrome muscle pain NV etc.
What are 5 nucleoside reverse transcriptase inhibitors?
Zidovudine Didanosine Lamivudine Abacavir Emtricitabine
Name 1 nucleotide reverse transcriptase inhibitor
Tenofovir
NucleoTide–Tenofovir
Name 1 non-nucleoside reverse transcriptase inhibitor
Efavirenz
Name 5 Protease Inhibitors
Ritonavir Indinavir Nelfinavir Lopinavir Atazanavir *** They all end in NAVIR
Zidovudine Mechanism
Nucleoside Reverse Transcriptase Inhibitor (causes chain termination, inhibition of viral replication)
Zidovudine Pharmacokinetics
Good CNS penetration
Zidovudine Adverse Effects (2)
- GI disturbances
2. Bone marrow Toxicity
What drug is used to prevent transmission of HIV from mother to child?
Zidovudine
What is a major use of Zidovudine?
To prevent transmission of HIV from mother to child
Didanosine Mehcanism
Nucleoside Reverse Transcriptase Inhibitor (causes chain termination, inhibition of viral replication)
Didanosine Adverse Effects (3)
- Peripheral Neuropathy
- Pancreatitis
- GI effects
Lamivudine Mechanism
Nucleoside Reverse Transcriptase Inhibitor (causes chain termination, inhibition of viral replication)
Lamivudine Advantage
Less toxic than other drugs
Also treats Hep B
Abacavir mechanism
Nucleoside Reverse Transcriptase Inhibitor (causes chain termination, inhibition of viral replication)
How do non nucleoside RTIs work?
they bind directly to the reverse transcriptase enzyme and inhibit its activity
Emtricitabine Mechanism
Nucleoside Reverse Transcriptase Inhibitor (causes chain termination, inhibition of viral replication)
Emtricitabine Adverse effect
Pigmentation of palms of hands and soles of feet
Tenofovir Mechanism
NucleoTide Reverse Transcriptase Inhibitor (causes chain termination, inhibition of viral replication)
Tenofovir use besides HIV
Hep B
What is a pharmacokinetic interaction with non nucleoside RTIs?
p450 metabolism
Efavirenz
Non nucleoside RTI
metabolized by p450
Cause headache, rash, insomnia
Also can cause neural tube defects
Adverse effects of Ritonavir
NVD
Paresthesias
Use of Ritonivir
Boost serum concentrate of other PIs
Adverse effect of Indinavir
Nephrolithiasis
Nelfinavir adverse effects
GI problems
What are the preferred PIs for naive patients?
Ritonavir boosted Atazanavir
What are the preferred NRTI treatments for naive patients? (2)
- Abacavir/Lamivudine
2. Emtricitabine/Tenofovir