Antivirals/retrovirals Flashcards
Purine/pyrimidine Analog which is the
DOF IN: HSV ENCEPHALITIS
ACYCLOVIR
Neuraminidase Inhibitors. Name them:
Oseltamivir, Zanamivir
Synthetic Guanosine analogue that is:
- Active against broad spectrum of RNA & DNA viruses (eg, RSV, HCV, Lassa fever)
- Commonly used in combination with interferon for the treatment of HCV
name the Antiviral
Ribavirin
Purine/pyrimidine Analogs
which drug is commonly used in combination with interferon for the treatment of HCV?
ribavirin
if you attempt to treat HBV or HIV (hepatic infections) with Lamivudine but have no luck what is drug you can use that you can use? pick one.
Interferon
Ganciclovir
Ribavarin
Entecavir
Cidofovir
Entecavir
(must monitor after discontinuation in case of exacerbation of severe hepatitis
whats the most common AE related to the Fusion inhibitor Enfuvirtide
Injection site-related rxs
The herpes antiviral drug which does NOT require phosphorylation to be active is indicated in the treatment of… name 3 things
What is the drug?
CMV
CMV retinitis (in immunocompromised patients)
Acyclovir-resistant HSV & CMV retinitis
Ganciclovir-resistant CMV & VZV
The drug is Foscarnet
list all the NRTI’s
ST. Z’ LEAD
Stavudine
Tenofovir
Zidovudine
Lamivudine
Emtricitabine
Abacavir
Didanosine
Herpes Simplex Labialis (cold sores) is treated with this drug and the AE associated with it is Mild erythema.
Penciclovir
which herpes antiviral DOES NOT require phosphylation to be active?
Foscarnet
Are protease inhibitors metabolized by CYP3A4 and P glycoprotein?
yes, extensively.
which antiviral….
prevents viral mRNA capping.
used to treat
- *1. RSV
2. HCV**
3.LASSA FEVER
Ribavirin
List the 5 Protease Inhibitors (PIs)
L’ D I N A
Lopinavir
Darunavir
Indinavir
Nelfinavir
Atazanavir
which vacciens are CI in pts with a CD4+ count of < 200?
LIVE VACCINES!
- MMR
- Varicella and • Zoster
Other vaccines may be administered without regard to the patient’s CD4+
which is the only ONCE daily PI’s
Atazanavir
Blocks viral membrane protein, M2 (H+ ion channel)
• Channel is required for fusion of viral with cell membrane to endosome (requirement for viral uncoating)
which drug is this?
the -tadines!
Amantadine
Rimantadine
name the antiviral with the following pattern of pharmodynamics & AE
- Oral, IV, & aerosolized
- Distribution significantly prolonged in RBC (16-40 days)
Adverse Effects
• Dose-dependent transient anemia (can bind to RBC)
Ribavirin
- GI discomfort, nausea (alleviated when taken with food)
- airway irritation (avoid in severe asthma, COPD)
match the drug with the AE of the following Neuramidase inhibitors.
options are: Oseltamivir & Zanamivir
- GI discomfort, nausea (alleviated when taken with food)=Oseltamivir
- airway irritation (avoid in severe asthma, COPD)=Zanamivir (side note, the med is inhaled/intranasal and is NOT orally active)
Upon exposure to HIV, healthcare personnel should immediately receive a postexposure prophylaxis regimen containing at least 3 antiretroviral drugs. what are the preffered 3 drugs in this regiment
Raltegravir (INSTI) + tenofovir (NRTI) + emtricitabine (NRTI)
Regimen is given for 28 days and can be stopped if source is shown to be HIV-negative.
Do NNRTI’s have in vitro activity against HIV 2?
NO.
from SGD.
the absorption of which protease inhibitor decreaes if take with a meal
INDINAVIR
main AE: hematuria, Rash, blurred vision, nephrolithiasis & hyperbilirubinemia
which class of drugs is being described? • Currently most popular antiretroviral class due to good side-effect profile and favorable effects on lipid metabolism
INSTI’s (integrease inhibitors)
Name that NNRTI
AE list: Rash, dizziness, headache, insomnia, difficulty concentrating, vivid dreams, nightmares, reductions in vitamin D levels, hyperlipidemia,
teratogenic (avoid in 1st trimester)
Substrate of CYP3A4
Inducer of CYP3A4 and 2B6
Efavirenz
Transient eye irritation, light intolerance & palpebral (eyelid) edema are the main AE for which Anti Herpes anti-viral?
Trifluridine (its an opthalmic ointment)
DOC for HSV Keratoconjunctivitis
does Acyclovir or Valacyclovir (its prodrug) have greater ORAL bioavailbility?
Valacyclovir
Val gives better ORAL.
What is an important toxicity common to all approved protease inhibitors?
the potential for metabolic drug interactions. Most of these drugs inhibit CYP3A4
- Effective against hepatitis B and HIV
- Triphosphate form inhibits HBV and HIV reverse
transcriptase
- Monophosphate form is incorporated into DNA (by HBV polymerase) resulting in chain termination
- Well tolerated (headache, dizziness, GI complaints)
Lamivudine
all Herpes antivirals Require phosphorylation by viral kinases and work by Inhibiting DNA polymerase /DNA synthesis. which is the only one that is phosphorylated by host cellular kinases only?
Cidofovir (does not require any viral enzymes)
Resistance to drug is acquired by Mutations in phosphotranferase (UL97), or viral DNA polymerase AND its the
DOC for: CMV retinitis & CMV prophylaxis in
immunocompromised
Ganciclovir
which NNRTI is CI in the first trimester if pregnancy
Efavirenz
The following class of antiretrovirals has the following AE:
hyperglycemia, insulin resistance and hyperlipidemia, in addition to altered body fat distribution. Buffalo hump, gynecomastia, and truncal obesity may occur with facial and peripheral lipodystrophy. They are also associated with parathesias, nausea, vomiting and diarrhea.
Protease Inhibitors
which Integrase inhibitor has the following drug interactions
Drug Interactions
• Rifampin, tipranavir & efavirenz may decrease its conc
• PPI’s may increases it conc
raltegraivr
side note. Can cause increases in creatine phosphokinases
What do Efavirenz and Nevirapine share in common in relation to the CYP P 450 system
Inducer of CYP3A4 and 2B6
Lets say an adult pt has Hep C, and you’ve tried interferon and ribavirin but no luck there. whats an alternative?
The -previrs!
Boceprevir, Telaprevir (Protease Inhibitors)
due to its poor intrinsic bioavailability, WHICH Protease inhibitor requires the avoidance of Enzyme inducers such as St. Johns worts andn Rifampin
this is a PREFFERED PI by the way
LOPINAVIR
which class of antiretrovirals is being being described
are more susceptible to high-level drug resistance than other classes because a single-amino acid change in the NNRTI-binding pocket renders the virus resistant to all available drugs in the class and this is their major disadvantage.
The NNRTIs
• ___________ form inhibits HBV and HIV reverse
transcriptase
• ___________form is incorporated into DNA (by HBV polymerase) resulting in chain termination
fill in the blank with with either “Monophosphate” or Triphosphate” in relation to which type of Lamivudine mechanism is being described.
• Triphosphate form inhibits HBV and HIV reverse
transcriptase
• Monophosphate form is incorporated into DNA (by HBV polymerase) resulting in chain termination
Prevents viral mRNA capping inhibition of RNA polymerase
Teratogenic (Cat X)
can bind to RBC and therefore causes transient dose dependent anemia
Ribavirin (guanosine analogue)
Do Amantadine or Rimantadine fit the following description?
- ________is widely distributed & crosses BBB and is not extensively metabolized & excreted into urine where it may accumulate
- ________ IS metabolized before elimination in urine
Amantadine (first blank)
Rimantadine (second blank)
• Major use is treatment of CMV-induced retinitis in HIV/AIDS
- NOT phosphorylated by viral kinases
- Requires activation by host cell kinases (no viral enzymes necessary!)
CIDOFOVIR
Name that NNRTI
Rash, fever, nausea, headache, severe hepatotoxicity, hepatic failure and death
Inducer of CYP3A4 and 2B6
Nevirapine
The following MOA belongs to which class or ANTIRETROVIRALS
competitively inhibit the action of the virus aspartyl protease. These drugs prevent proteolytic cleavage of HIV gag and pol polyproteins that include essential structural and enzymatic (reverse transcriptase, protease and integrase) components of the virus. This prevents the metamorphosis of HIV particles into their mature infectious form.
OVERALL, THEY PREVENT PROCESSING OF VIRAL PROTEINS, RESULTING IN THE PRODUCTION OF IMMATURE NON INFECTIOUS VIRAL PARTICLES
HIV protease inhibitors
Lopinavir
Darunavir
Indinavir
Nelfinavir
Atazanavir
Which purine/pyrimidine analogue (which is a Pyrophosphate analogue) does NOOOOTTTTTTT require phosphorylation?
FOSCARNET
which PI CANNOT be boosted by Ritonavir bc its metabolized by several CYPS and it also has a ton of CI’s and Generally well tolerated, diarrhea, nausea and flatulence are common
Nelfinavir
- Effective against HSV & ganciclovir resistant HSV
- Must be co-administered with probenecid (blocks renal tubular secretion)
name that drug.
CIDOFOVIR
which of the following are AE/CI are associated with Ganciclovir
a. Myelosuppressionb.
b. insomnia, dizziness, ataxia leading to hallucinations, seizures]
c. Severe dose-dependent neutropenia
d. Pregnancy (FDA Category C)
e. Flu-like (fever, chills, myalgias & GI disturbances)
f. Fatigue & mental depression
a. Myelosuppression
c. Severe dose-dependent neutropenia
d. Pregnancy (FDA Category C)
Zidovudine (thymdidne analogue) is an NRTI whose main AE is Bone suppression in pts with advnaced HIV diseae). When combined with_______ (antiviral), pt could get Neutropenia
Ganciclovir
- Used in combination with most protease inhibitors (not nelfinavir)
- Never used alone
____________________________________
- Used commonly in combination with the INSTI elvitegravir
- Also found in combination with darunavir and atazanavir (which are both PI’s)
- RITONAVIR
- COBICISTAT
Guanosine analogs.
Monophosphorylated by HSV/VZV thymidine kinase and not phosphorylated in uninfected cells
ACYCLOVIR
the following MOA is associated with which antiviral drug?
MOA
- Use innate immune response.
- DO NOT target viral gene products directly
- Inhibit RNA & DNA synthesis by activating / inducing protein expression that inhibit virus infection eg, PKR
Interferon
a. Neuraminidase Inhibitors [for Influenza A & B]
b. Inhibitors of Viral Uncoating [for Influenza A ONLY!!!]
c. Synthetic Guanosine Analog (inhibits RNA dep-RNA pol)-[for RSV, HCV, Lassa Fever]
- Amantadine, Rimantadine
- Ribavirin
- Oseltamivir, Zanamivir
match the desciption with the name of the dru
a. Neuraminidase Inhibitors [for Influenza A & B]
• Oseltamivir, Zanamivir
b. Inhibitors of Viral Uncoating [for Influenza A ONLY!!!]
• Amantadine, Rimantadine
c. Synthetic Guanosine Analog (inhibits RNA dep-RNA pol)-[for RSV, HCV, Lassa Fever]
• Ribavirin
List the 3 Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)
Nevirapine
Efavirenz
Rilpivirine
