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Pharmacology > Antiviral Agents > Flashcards

Antiviral Agents Flashcards

1
Q

acyclovir

A
  • herpesvirus
  • nucleoside analogue
  • MOA: activation by phosphorylation by viral thymidine kinase enzyme–> competitive inhibitor of DNA polymerase–> chain termination
  • use: genital and varicella zoster (oral); disseminated mucocutaneous, neonate infection, HSV encephalitis, VZV in immunocompromised (IV)
  • adverse effects: nausea, headache, diarrhea, nephrotoxicity (HYDRATE!)
  • resistance: mutation of thymidine kinase gene, cross-resistance w/ other antivirals
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2
Q

valacyclovir (Valtrex)

A
  • prodrug of acyclovir (metabolized in liver and intestines)
  • greater oral bioavailability
  • MOA: same as acyclovir–> inhibit DNA polymerase
  • use: primary/recurrent genital herpes, varicella in older children and adults, zoster, orolabial herpes
  • adverse effects: nausea, headache, vomiting, rash
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3
Q

foscarnet

A
  • analogue of pyrophosphate
  • MOA: binds site where pyrophosphate resides–> inhibits DNA polymerase
  • does NOT require prior phosphorylation
  • use: IV for HSV and VZV (resistant to acyclovir), CMV retinitis, CMV colitis, CMV esophagitis
  • adverse effects: renal impairment, changes in Ca phosphate K or Mg, avoid use w/ nephrotoxic drugs
  • resistance: rare, mutations in DNA polymerase
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4
Q

ganciclovir

A
  • herpes antiviral
  • acyclic guanosine analogue
  • MOA: phosphorylation by CMV UL97–> competitive inhibitor of viral DNA polymerase–> chain termination
  • use: (IV) CMV retinitis, colitis, pneumonitis, esophagitis, reduce risk of CMV in transplant pts
  • adverse effects: myelosuppression, CNS toxicity
  • resistance: mutation of UL97 gene, cross-resistance with other antivirals
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5
Q

valganciclovir

A
  • herpes antiviral
  • prodrug of ganciclovir (activated in liver and intestines)
  • MOA: same as ganciclovir (DNA polymerase inhibitor)
  • use: (oral) CMV retinitis (AIDS), prevention of CMV in transplant pts
  • adverse effects: myelosuppression, headache, nausea, diarrhea
  • resistance: UL97 mutation
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6
Q

trifluridien

A
  • fluorinated nucleoside
  • MOA: phosphorylated by cellular enzyme–> competitive inhibitor of thymidine
  • ocular admin
  • keratoconjunctivitis, recurrent epithelial keratitis (HSV-1 and 2)
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7
Q

oseltamivir (Tamiflu)

A
  • sialic acid analogue
  • MOA: activated by hepatic esterases–>binds active site of neuraminidase–> inhibits function–> inhibits spread of progeny virons through RT
  • use: >1yo with influenza A and B, chemoprophylaxis, 48 hrs w/in symptoms
  • adverse effects: nausea, vomiting, headache, diarrhea, rash
  • resistance: point mutations in hemagglutinin or neuraminidase
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8
Q

zanamivir

A
  • sialic acid analogue
  • MOA: activated by hepatic esterases–>binds active site of neuraminidase–> inhibits function–> inhibits spread of progeny virons through RT
  • use: 7 yo
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9
Q

peramivir

A
  • MOA: neuraminidase inhibitor
  • use: acute, influenza symptoms for no more than 48 hrs
  • IV admin
  • adverse effects: GI effects, rash, Steven Johnson syndrome, hyperglycemia, hypertension, delirium
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10
Q

amantadine

rimantadine

A
  • symmetric tricyclic amines
  • MOA: inhibit influenza A M2 protein–> inhibits necleocapsid release
  • use: Influenza A, w/in 48 hrs of symptoms
  • adverse effects: nausea, anorexia, neurological symptoms
  • resistance: high levels, aa substitution in M2
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11
Q

ribavirin

A
  • guanosine analogue
  • MOA: phosphorylated by cellular adenosine kinase–> interferes with synthesis of guanosine triphosphate–> inhibit viral mRNA capping–> inhibit RdRp of RSV and HCV
  • use: RSV bronchitis,combo therapy for HCV
  • aerosol admin (RSV), oral admin (HCV)
  • adverse effects: hemolytic anemia, depression, rash, cough, insomnia
  • contraindications: pregnancy, anemia, ischemic vascular disease, severe renal disease
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12
Q

paritaprevir

A
  • HCV protease inhibitor
  • MOA: inhibit HCV NS3/4A protease–> inhibit proteolysis cleavage of immature viral polypeptides into mature viral proteins
  • oral admin, combo w/ ombitasvir and ritonavir
  • use: chronic HCV
  • adverse effects: asthenia, fatigue, nausea, insomnia
  • resistance: NS3 gene substitituions
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13
Q

simeprevir

A
  • HCV protease inhibitor
  • MOA: inhibit HCV NS3/4A protease–> inhibit proteolysis cleavage of immature viral polypeptides into mature viral proteins
  • oral admin, combo w/ sofosbuvir, or ribavirin and pegylated interferon
  • use: chronic HCV (screen pts for NS3 Q80K polymorphism)
  • adverse effects: rash, pruritus, dyspena, nausea, myalgia
  • resistance: NS3 gene substitution
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14
Q

ledipasvir

A
  • nucleotide analogue HCV NS5A inhibitor
  • MOA: inhibit NS54 protein–> inhibit viral RNA replication and virion assembly
  • oral admin, combo w/ sofosbuvir
  • use: chronic HCV
  • adverse effects: diarrhea, fatigue, headache, hyperbilirubinemia, nausea, insomnia
  • resistance: NS5A gene substitution
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15
Q

ombitasvir

A
  • nucleotide analogue HCV NS5A inhibitor
  • MOA: inhibit NS54 protein–> inhibit viral RNA replication and virion assembly
  • oral admin, combo w/ paritaprevir and ritonavir
  • use: chronic HCV
  • adverse effects: asthenia, fatigue, nausea, insomnia
  • resistance: NS5A gene substitution
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16
Q

sofosbuvir

A
  • RNA polymerase inhibitor-nucleotide analogue
  • MOA: prodrug–> incorporated into RNA by RNA-dependent-RNA polymerase–> premature chain termination
  • oral admin, avoid coadmin w/ potent inducers of p-glycoprotein
  • use: chronic HCV, used in combo w/ ledipasvir (Harvoni)
  • adverse effects: anemia, fatigue, headache, insomnia, nausea, flu like symptoms
  • resistance: rapid–> monotherapy NOT recommended
17
Q

dasabuvir

A
  • RNA polymerase inhibitor, non-nucloside inhibitor
  • MOA: target palm domain of RNA by RNA-dependent-RNA polymerase–> halt viral life cycle
  • oral admin, combo w/ ombitasvir, paritaprevir, ritonavir
  • use: chronic HCV
  • adverse effects: fatigue, asthenia, insomnia
  • resistance: rapid–> monotherapy NOT recommended
18
Q

abacavir

A
  • nucleoside reverse transcriptase inhibitor (NRTIs), guanosine analogue
  • MOA: phosphorylated–> competitively inhibit reverse transcriptase enzyme
  • use: naive and experienced HIV, oral admin
  • adverse effects: allergic rxn (screen for HLA-B5707), rash, fever, nausea, vomiting, pancreatitis, cardiac events
  • lowers effects of methodone
  • resistance: mutation in HIV reverse transcriptase gene
19
Q

lamivudine

A
  • nucleoside reverse transcriptase inhibitor (NRTIs), cytosine analogue
  • MOA: phosphorylated–> competitively inhibit reverse transcriptase enzyme
  • use: naive and experienced HIV, oral admin, pregnant mothers and neonates, chronic HBV
  • adverse effects: least toxic antiretroviral, high doses–>GI and CNS
  • resistance: single base change
20
Q

emtricitabine

A
  • nucleoside reverse transcriptase inhibitor (NRTIs), fluorinated analogue of lamivudine
  • MOA: phosphorylated–> competitively inhibit reverse transcriptase enzyme
  • use: naive and experienced HIV, oral admin
  • contraindication: pregnant mothers and neonates, renal or hepatic failure
  • adverse effects: headache, nausea, diarrhea, rash, hyperpigmentation of palms and soles
  • resistance: single base change
21
Q

tenofovir

A
  • nucleoside reverse transcriptase inhibitor (NRTIs), adenosine analogue
  • MOA: phosphorylated–> competitively inhibit reverse transcriptase enzyme
  • oral admin., poorly soluble
  • use: naive and experienced HIV, reduces transmission, chronic HBV
  • adverse effects: GI discomfort, headache, asthenia, renal/bone toxicity, crosses placental (decreases fetal growth)
  • resistance: single codon change
22
Q

zidovudine (AZT)

A
  • nucleoside reverse transcriptase inhibitor (NRTIs), deoxythymidine analogue
  • MOA: phosphorylated–> competitively inhibit reverse transcriptase enzyme
  • use: naive and experienced HIV, oral admin, reduce vertical transmission, post exposure prophylaxis
  • adverse effects: myelosuppression, fatigue, malaise, nausea, headache, insomnia, asthenia, nail hyperpigmentation
  • resistance: multiple mutations in HIV reverse transcriptase gene
23
Q

efavirenz

A
  • non-nucleoside reverse transcriptase inhibitor (NNRTIs)
  • MOA: bind reverse transcriptase district from active site
  • do NOT require phosphorylation
  • NOT active against HIV-2
  • use: naive and experienced HIV
  • contraindicated: during pregnancy
  • adverse effects: CNS effects, rash, increased liver enzymes, headache, nausea, tertogenic, induces cytochrome P450
  • resistance: single base change
24
Q

nevirapine

A
  • non-nucleoside reverse transcriptase inhibitor (NNRTIs)
  • MOA: bind reverse transcriptase district from active site
  • do NOT require phosphorylation
  • NOT active against HIV-2
  • use: naive and experienced HIV, prevent vertical transmission
  • adverse effects: rash, hepatitis, nausea, headache
  • resistance: single base change
25
Q

atazanavir

A
  • protease inhibitor
  • MOA: mimic peptide targets–>inhibit HIV protease–> block maturation of virion particles after budding
  • oral admin, requires acid for absorption
  • use: naive and experienced HIV, 6yo
26
Q

ritonavir

A
  • protease inhibitor
  • MOA: mimic peptide targets–>inhibit HIV protease–> block maturation of virion particles after budding
  • oral admin
  • use: not used as sole PI in regimen, used as “booster” to increase half-life of ARV drugs
  • adverse effects: nausea, diarrhea, paresthesias, heptatis, lipodystrophy POTENT inhibitor of cytochrome P450
  • resistance: multiple mutations
27
Q

darunavir

A
  • protease inhibitor
  • MOA: mimic peptide targets–>inhibit HIV protease–> block maturation of virion particles after budding
  • oral admin, coadmin. w/ enhancers (ritonavir)
  • use: naive and experienced HIV
  • adverse effects: diarrhea, headache, nausea, rash, hyperlipidemia, increase liver enzymes and serum amylase
  • resistance: few
28
Q

maraviroc

A
  • CCR5 receptor antagonist
  • MOA: bind cellular CCR5 protein–> prevent interaction with gp120 envelop–> stop virion from entering cell
  • oral admin., substrate of CYP34A
  • use: CCR5 tropic HIV virus
  • adverse effect: cough, URT infection, postural hypotension, arthralgia, myalgia, allergic reaction, increased cardiac events
  • resistance: change in tropism or mutation in gp120
29
Q

enfuvirtide

A
  • fusion inhibitor
  • MOA: binds gp41 fusion protein–> prevent conformational change for fusion of viral envelop with plasma membrane–> prevent nucleocapsid from reaching interior cell
  • ONLY parenterally admin
  • use: experience HIV w/ evidence of HIV replication even w/ ARV tx
  • adverse effects: painful erythematous nodule at site of injection, insomnia, headache, allergy, eosinophilia
  • resistance: high requires multiple mutations in gp41 gene
30
Q

raltegravir

A
  • integrase inhibitor
  • MOA: inhibit integrase–> inhibit incorporation of linear HIV DNA into host genome–> prevent formation of provirus
  • oral admin
  • use: experienced and naive HIV
  • adverse effects: insomnia, headache, diarrhea, nausea, dizziness, fatigue, myopathy, rhabdomyolysis
  • resistance: single mutation in integrase gene
31
Q

elvitegravir

A
  • integrase inhibitor
  • MOA: inhibit integrase–> inhibit incorporation of linear HIV DNA into host genome–> prevent formation of provirus
  • oral admin, requires coadmin w/ ritonavir
  • use: experienced and naive HIV
  • adverse effects: nausea, diarrhea, elevation of lipase, headache, fatigue, insomnia, depression, rash
  • resistance: single mutation in integrase gene
32
Q

dolutegravir

A
  • integrase inhibitor
  • MOA: inhibit integrase–> inhibit incorporation of linear HIV DNA into host genome–> prevent formation of provirus
  • oral admin
  • use: HIV pts 12 yo
33
Q

ARV therapy

A
  • 1 PI (ritonavir boosted) + 2 NRTIs

- 1 II + 2 NRTIs

Pharmacology (34 decks)

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