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Clinical Pharm Exam 3 > Antiviral > Flashcards

Antiviral Flashcards

(98 cards)

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1
Q

Influenza

A

Amantidine
Rimantidine
Oseltamivir
Zanamivir

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2
Q

Amantidine MOA:

A

Inhibit uncoating of the viral RNA within infected host cells, preventing replication

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3
Q

Rimantidine MOA

A

Inhibit uncoating of the viral RNA within infected host cells, preventing replication

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4
Q

Oseltamivir MOA

A

Inhibit neuraminidase of influenza a and b; preventing the release of virons from the host cell and prevents entry into the cell

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5
Q

Zanamivir MOA

A

Inhibit neuraminidase of influenza a and b; preventing the release of virons from the host cell and prevents entry into the cell

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6
Q

Amantidine

A

Crosses BBB –> parkinson’s Disease
Pregnancy category C
CDC DOES NOT recommend use

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7
Q

Rimantidine

A

Pregnancy category C

CDC DOES NOT recommend use

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8
Q

Oseltamivir

A

Pro drug, oral
Indicated: prevention and treatment of Influenza A and B
BEGIN within 2 days of onset (renally dosed)
Pregnancy category C

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9
Q

Zanamivir

A

Oral inhalation
Indicated: prevention and treatment of Influenza A and B
Avoid in Dairy allergy - contains milk protein
Pregnancy category C

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10
Q

Nucleoside analogs MOA

A

synthetic analogs of purines or pyrimidines that inhibit the viral replication through
competitive inhibition of DNA polymerase
incorporation and termination of viral DNA chain
inactivation of viral DNA polymerase

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11
Q

Trifluridine

A

Pyrimidine analogs
Ophthalmic solution
Indications Ocular HSV
Refrigerate

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12
Q

Cidofovir

A

Pyrimidine analogs
IV formulation ONLY
Indication CMV infections, HSC activity (systemic, organs, meningitis)
Renally Toxic –> HYDRATE prior to therapy

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13
Q

Acyclovir

A

Guannine Analogs
ONLY effective against activiely replicating virus
Indications HSV and VZV
Oral, IV (renally toxic), topical
Poor bioavailability –> multiple dosing/day (5X)
Pregnancy category B
Monitor renal function

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14
Q

Valacyclovir

A

Prodrug of acyclovir
Better bioavailability
Indications HSV and VZV
Oral formulation only (1 x day)

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15
Q

Famciclovir

A 
Prodrug of penciclovir
guanine analog
Inhibits viral DNA polymerase
Better bioavailability
Indications: prevention and treatment of HSV and VZV
Pregnancy category B
Oral agent
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16
Q

Penicilovir

A

Guanine analog
Inhibits viral DNA polymerase
Topical formulation ONLY
Indication: treatment of HSV infections (Herpes labialis and facialis)

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17
Q

Ganciclovir

A

Guanine analog
Indications: treatment and prevention of CMV infection
IV formulation renally toxic –> HYDRATE
Monitor: CBC w/ diff, LFTs, Renal function, serum electrolytes
Pregnancy category: C

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18
Q

Valganciclovir

A 
prodrug of ganciclovir
Oral table take with food
renally excreted
Indications: Prevention and treatment of CMV infections
Monitor CBC w/ diff, renal function
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19
Q

Foscarnet

A

Inorganic pyrophosphate analog
inhibits viral-specific DNA polymerases and reverse transcriptase at the pyrophosphate binding site –> preventing DNA synthesis
Indications: prevention and treatment of CMV, treatment of refractory HSV and VZV
Monitor: chem 10 (renal function and electrolyte loss), CBC w/ diff (bone marrow suppression), EKG (AV block, ST wave changes)
Pregnancy category C

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20
Q

HAV Vaccines

A

Vaqta
Havrix
Twinrix

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21
Q

Vaqta

A

HAV only
Indications >12months of age
2 doses series - 1st dose then 2nd dose 6-18 months later

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22
Q

Havrix

A

HAV only
Indications >12 months
2 dose series - 1st dose then 2nd dose 6-12 months later

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23
Q

Twinrix

A

HAV/HBV combination
Indicated >18y/o
3 dose series - 1st dose, then 2nd dose @ 1month, then 3rd dose @ 6months

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24
Q

HBV Agents

A 
Adefovir
Entecavir
Lamivudine
Interferon/peg-interferon
Tenofovir
Telbivudine
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25
Interferon MOA
signaling proteins that are released by host cell in response to pathogens; triggering protective defense mechanisms within the immune system. Interfere with viral replication and activate natural killer cells and macrophages
26
Peg-Interferon
SQ once weekly ADEs: Anemias (cbc w/ diff), infections (CXR), arrhythmias (ekg), LFTs, Hypothyrodism (TSH), psych changes (moods), renal function REFRACTORY HBV
27
Interferon
IV, IM, SQ once daily for 16 weeks ADE:Anemias (cbc w/ diff), infections (CXR), arrhythmias (ekg), LFTs, Hypothyrodism (TSH), psych changes (moods) REFRACTORY HBV
28
Adefovir
Adenosine analog prodrug metabolixed by cellular kinases preventing DNA synthesis Indications HBV, effective against Lamivudine- resistant HBV Renally dosed when CrCl<50ml.min Monitor: Renal function, LFTs, HBV labs (viral load and serologies NO CO INFECTION COVERAGE DO NOT USE WITH TENOFOVIR
29
Entecavir
inhibit HBV reverse transcriptase --> suppressing DNA replication (weak toward HIV) Co-infectioon, lamivudine resistance on tenofovir Renally dosed when CrC<50ml/min Monitor: Renal function, LFTs, T.bili, Blood glucose
30
Lamivudine
nucleoside reverse transcriptase inhibitor Resistance via M184V and M184I mutations Indications: HIV-1, HIV-2: 300mg po 1xday HBV: 100mg po 1xday Well tolerated (mostly GI/HA) Monitor: Blood glucose, CBC with diff, HIV VL/CD4 count
31
Telbivudine
``` MOA: inhibits DNA polymerase --> preventing DNA replication Thymidine analog Renally dosed when CrCl<50ml/mn ADE: LFTs TOO EXPENSIVE ```
32
NS5B Polymerase Inhibitor MOA
Nucleoside/nucleotide analogs that incorporate into HCV RNA leading to chain termination --> stop HCV replication
33
NS3/4A Protease Inhibitor MOA
Inhibits the cleavage of polyproteins into nonstructural proteins that are essential in HCV replication Lower barrier of resistance Q80K
34
NS5A Inhibitor MOA
Inhibits the phosphorylation of proteins required for HCV RNA replication --> preventing HCV RNA replication * need to do genetic resistance testing
35
Non-Nucleoside NS5B palm Polymerase Inhibitor MOA
Inhibits the activity of the NS5B to inhibit HCV RNA replication
36
NS5B Polymerase Inhibitor Agents
Sofosbuvir
37
NS3/4A Protease Inhibitor Agents
``` Glecaprevir Grazoprevir Paritaprevir Simeprvir Voxilaprevir ```
38
NS5A Inhibitors Agents
``` Daclatasvir Elbasvir Ledipasvir Ombitasvir Pibrentasvir Velpatasvir ```
39
Non-Nucleoside NS5B palm Polymerase Inhibitor Agents
Dasabuvir
40
3A4 PK Booster Agents
Ritonavir
41
Sofosbuvir
``` NS5B RNA nucleotide polymerase inhibitor for Genotype 1,2,3,4 Pro drug Pangenotypic No CYP Interactions Substrate of pgp efflux pump and BCRP *Tenofovir --> Increase renal toxicity associated with Tenofovir Pregnancy: Sofosbuvir ONLY - Category B otherwise Category X ```
42
Sofosbuvir/Ledipasvir (Harvoni)
Ledipasvir - NS5A inhibitor metabolism via oxidation - no DDI via CYP elimination via pgp efflux pump and BCRP ADE: Asthenia, Hyperbilirubinemia, fatigue/headache, GI effects, No hepatic dosing, No renal dosing - caution CrCl<30ml/min DDI: acid suppressants, Tenofovir --> nephrotoxicity, Amiodarone --> Symptomatic bradycardia
43
Velpatasvir/Sofosbuvir (Epclusa)
``` NEW GOLD Standard in HCV management Velpatasvir NS5A inhibitor Pangenotypic for genotype 1-6 metabolized CYP 2B6, 2C8, 3A4 Eliminated via feces ``` ADE: anemia, GI, Headache, Fatigue, no hepatic dosing, no renal dosing - caution in GFR<30ml/min LOTS OF DDI
44
Voxilaprevir/Velpatasvir/Sofosbuvir (Vosevi)
Voxilaprevir NS3/4A protease Inhibitor via CYP3A4 --> DDI Significant DDI with acid suppressants (Antacid, H2Blockers, PPIs) Renal issues: do not use when GFR<30ml/min ADE: headache, fatigue, GI, Rash, Depression, Elevated lipase, CPK, t. bili
45
Elbasvir/Grazoprevir (Zepatier)
Elbasvir - NS5A Inhibitor Grazoprevir - NS3/4A Protease Inhibitor ADE: GI, Fatigue, headache, Anemia, elevated LFTs, Hyperbilirubinemia, No renal or hepatic dosing LOTS OF DDI
46
Viekira Pak
Paritaprevir (NS3/4A protease inhibitory) - Metabolism 3A4 - MAJOR DDIs Ritonavir (CYP3A4 Booster) Ombitasvir (NS5A Inhibitor) - Metabolized via hydrolysis + Dasabuvir (non-nucleoside NS5B palm polymerase inhibitor - Metabolism via 2C8, 3A4 (possible DDIs) Must be taken eith food No renal or hepatic dosing ADE: GI, rash, LFTs TO COMPLICATED
47
Viekira XR
Genotype 1a and 1b Paritaprevir/ritonavir/Ombitasvir/Dasabuvir Must be taken with food - cannot be chewed, crushed, or split TOO MANY DDI ADE: GI, rash, LFTs 3 pills once a day
48
Simeprevir
NS3/4A Protease Inhibitor for Genotype 1 ONLY - Q80K resistance mutation --> reduction in efficacy based on SVR - more effective in 1b Metabolized via 3A4 & 1A2 --> interactions Take with food Sulfonamide Allergy ADE: Rash, LFTs, GI, Hyperbilirubinemia MUST BE GIVEN WITH Sofosbuvir
49
Daclatavir
NS5A Inhibitor Indications: HCV genotype 3 Must be co-administered with Sofosbuvir Metabolism - CYP3A4 - substrate --> DDI Co-administered with 3A4 inhibitor --> reduce to 30mg QD Co-administered with 3A4 inducer --> increase to 90mg QD ADE: Anemia, Fatigue, GI effects, Headache
50
Glecaprevir/Pibrentasvir (Mavyret)
``` Glecaprevir - NS3/4A Protease Inhibitor Pibrentasvir - NS5A Inhibitor Pangenotypic for genotypes 1-6 Dose: 3 tablet once daily with food Glecaprevir: CYP3A4, eliminated pgp efflux pumps Pibrentasvir: Biliary-fecal route ``` No renal dosing ADE: Headache, Fatigue, GI, Elevated t.bili
51
Pef-Interferon + Ribavirin
Refractory HCV
52
Ribavirin
MOA: Increase mutation frequency and inhibits HCV polymerase activity Indications: in combination with PEG-IFN therapy ADE: pruritus, weight loss, GI symptoms, Neutropenia, Headache, Insomnia, Fatigue, Fever BBW: hemolytic anemia + Teratogenicity
53
Recommendations for patients with CKD stage 1, 2, or 3
``` Daclatasvir Elbasvir/Grazoprevir Glecaprevir/Pibrentasvir Ledipasvir/Sofosbuvir Sofosbuvir/Velpatasvir Simeprevir Sofosbuvir/Velpatasvir/Voxilaprevir Sofosbuvir ```
54
Recommendations for patients with CKD stage 4 or 5 (GFR<30ml/min)
Elbasvir/Grazoprevir | Glecaprevir/Pibrentasvir
55
When to initiate HIV Therapy
any time end organ damage, pregnant, co-infection (HBV/HCV) | DO NOT INITIATE THERAPY IF PATIENT IS NOT READY or WILLING
56
What to initiate
Integrase inhibitor based Antiretroviral therapy: - Raltegravir + Emtricitabine/Tenofovir DF or Tenofovir AF - Elvitegravir/c/TDF/Emtricitabine - Elvitegravir/c/TAF/Emtricitabine - Dolutegravir + Emtricitabine/Tenofovir DF or Tenofovir AF - Dolutugravir/abacavir/lamivudine HLA-B5701 negative
57
Under special conditions
Darunavir/Ritonavir or Darunavir/c + TDF/Emtricitabine or TAF/Emtricitabine or Abacavir/Lamivudine - epzicom if HLA-B5701 negative Atazanavir/ritonavir or Atazanavir/c + TDF/Emtricitabine or TAF/Emtricitabine or Abacavir/Lamivudine Raltegravir + Abacavir/Lamivudine (baseline HIV VL <100K copies/ml) inferior to truvada/descovy
58
Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs)
``` Abacavir Didanosine Emtricitabine Lamivudine Stavudine Tenofovir - TDF - TAF Zidovudine ``` MOA: competitively inhibits of HIV-1 reverse transcriptase ``` Renally dosed (except Abacavir) Mitochondrial toxicity - due to inhibition of mitochondrial DNA polymerase - lactic acidosis and hepatic steatosis - lipoatrophy --> fat wasting extremities, buttocks, face ```
59
Truvada
Emtricitabine/Tenofovir DF
60
Dsescovy
Emtricitabine/Tenofovir AF
61
Epzicom
Abacavir/Lamivudine
62
Combivir
Zidovudine/Lamivudine
63
Abacavir
ADE: Rash, CVD risk DO NOT USE baseline HIV VL >100K copies/ml Testing for HLA-B5701 allele before initiation of abacavir is recommended to identify the patients with an increased risk of an abacavir associated hypersensitivity reaction
64
Didanosine
ADE: Weight-dosed, pancreatitis, peripheral neuropathy
65
Emtricitabine
ADE: Hyperpigmentation, well tolerated Active against HBV
66
Lamivudine
ADE: well tolerated, headache Also reactive against HBV infections Rapidly selects for mutation - M184V
67
Stavudine
ADE: weight-dosed, pancreatitis, peripheral neuropathy
68
Tenofovir
TDF - nephrotoxicity, osteomalacia | TAF - Safer, no kidney or bone mineral density
69
Zidovudine
ADE: bone marrow suppression (anemias, RBC, WBC, platelets) High level resistance is generally seen
70
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
``` 1st Generation: - Efavirenz - Nevirapine 2nd Generation: - Etravirine - Rilpivirine ``` MOA: binds noncompetitively to allosteric site baseline genotypic resistance testing is recommended resistance occurs rapidly with monotherapy and results from single mutation - lowest genetic barrier resistance - MOST COMMON MUTATION = K103N (resistant to efavirenz & nevirapine)
71
Efavirenz
1st generation NNRTI take on empty stomach (take at bed) ADE: CNS effects - somnolence, fatigue, psych changes, SI/SA - rash, LFTs Metabolized by CYP3A4; induces and inhibits CYP3A4 Pregnancy category: D
72
Nevirapine
1st generation NNRTI DO NOT USE: in female with CD4 > 350cells/mm3; males with CD4 >400cells/mm3 Metavolized by CYP3A4; Induced CYP3A4 ADE: rash, liver toxicity
73
Etravirine
2nd generation NNRTI Active against K103N virus Metabolized by CYP3A4; Induces and Inhibits CYP3A4\ ADE: rash, LFTs, minor CNS effects
74
Rilpivirine
2nd generation NNRTI active against K103N virus Must be taken with food; 900kcals (bad for diabetic, heart disease, obese) Metabolized by CYP3A4; substrate ADE: rash, LFTs, CNS effects Do not use: baseline HIV VL > 100K copies/ml
75
Complera
Rilpivirine/TDF/Emtricitabine
76
Odefsey
Rilpivirine/TAF/Emtricitabine
77
Protease Inhibitors Agents
``` Atazanavir Fosamprenavir Darunavir Indinavir Lopinavir/ritonavir Nelfinavir Ritonavir Saquinavir Tipranavir ```
78
Protease Inhibitors
MOA: Inhibit the activation of immature proteins --> block the GAG-POL region within protease to inhibit the cleavage of proteins Class Effects: Rash, LFTs, Increases Blood glucose (DM), Increases TG and LDL, Lipodystrophy (central adiposity), Increases CVD risk All PIs are metabolized by CYP3A4 (most are potent CYP3A4 inhibitors) High genetic barrier to resistance (difficult to become resistance)
79
Ritonavir
Most 3A4 Potent inhibitor ADE: GI DO NOT give with nelfinavir Active against HIV --> as a booster
80
Atazanavir
ADE: PR interval prolongation, Hyperbilirubinemia GI neutral Lipid neutral
81
Darunavir
MUST co-admin w/ ritonavir Sulfonamide --> cautious with sulfa allergy GI neutral Lipid neutral
82
Fosamprenavir
Sulfonamide --> cautious with Sulfa allergy | ADE: GI
83
Indinavir
Nephrolithiasis, hyperbilirubinemia
84
Lopinavir
ADE: GI
85
Saquinavir
ADE: GI, CVD risk
86
Tipranavir
Only CYP3A4 inducer MUST Co-admin w/ ritonavir Sulfonamide --> cautious with sulfa allergy ADE: Intracranial hemorrhage
87
Cobicistat
Similar to ritonavir --> used as 3A4 booster ONLY with atazanavir and darunavir NO HIV Activity DDI/Contraindications = ritonavir ADE: renal impaitment (don't use with TDF when CrCl<70ml/min)
88
Evotaz
Atazanavir/Cobicistat | 1 tablet + 2 NRTIs
89
Prezcobix
Darunavir/Cobicistat | 1 tablet + 2 NRTIs
90
Fusion Inhibitor
Enfuvirtide ONLY SQ MOA: inhibits gp41 and prevents the fusion of HIV to CD4 cell surface ADE: injection site reaction, GI
91
Entry inhibitor
Maraviroc MOA: inhibits HIV co-receptor CCR5-tropic HIV-1 infection MUST test for co-receptor tropism prior to using With inhibitor: decrease dose With inducer: increase dose ADE: LFTs, Rash, Pyrexia, orthostasis
92
Integrase Inhibitors
Raltegravir Elvitegravir Dolutegravir Bictegravir/TAF/Emtricitabine
93
Raltegravir
MOA: Blocks the catalytic activity of the HIV-encoded integrase, thus preventing integration of virus DNA into the host Metabolized by glucuronidation and does not interact with the CYP450 system Eliminated via pgp efflux pumps Resistance: virologic failure has been uncommon in vitro resistance requires only a single point mutation at codons 148 or 155 ADE: rash, LFTs, Increase CPK, pyrexia
94
Quad Pill
Elvitegravir/COBI/TDF/Emtricitabine MOA: Blocks the catalytic activity of the HIV-encoded integrase, thus preventing integration of virus DNA into the host 3A4 Substrate, glucuronidation CrCl > 70ml/min Treatment naive patients ADE: new or worsening renal function, bone mineral density losses, GI TOO MANY C/I and DDI
95
Genvoya
Elvitegravir/COBI/TAD/Emtricitabine MOA: Blocks the catalytic activity of the HIV-encoded integrase, thus preventing integration of virus DNA into the host Safe in pt with CrCl > 30
96
Dolutegravir
MOA: Blocks the catalytic activity of the HIV-encoded integrase, thus preventing integration of virus DNA into the host Metabolism: UGT-1A1, 3A4 ADE: Hypersensitivity reaction, LFTs (especially in HBV or HCV co-infections), Insomnia, Hyperglycemia (>125mg/dl), hypertriglyceridemia DDI: Polyvalent cations (Mg, Al, Fe, Ca) Space 2hrs before or 6hrs after cations
97
Bictegravir/TAF/Emtricitabine
``` Integrase Inhibitor Treatment naive and as SWITCH regimen Renal issues CrCl<30ml/min Metabolism Glucuronidation and Via CYP3A4 ADE: GI & Headache ```
98
SWITCH regimen
a pt on an effective HIV regimen & able to maintain viral suppression for at least 6 months & looking for simple regimen

Clinical Pharm Exam 3 (5 decks)

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