ANTIVIRALS Flashcards
(91 cards)
1
Q
4 Common Problems on Antivirals
A
- Resistance
- Ineffective (non-replicating virus)
- Limited spectrum
- -Static
RILS
2
Q
Enumerate the viral process.
A
- Attachment
- Entry
- Release
- Replication
- Assembly
- Release
AERRAR
3
Q
CHEMOPROPHYLAXIS INFLUENZA
For influenza A + Parkinson’s disease
A
Amantadine
(Symmetrel)
4
Q
CHEMOPROPHYLAXIS INFLUENZA
Adverse effect of Amantadine (Symmetrel)
A
Livedo Reticularis
Others: CNS anticholinergic effects - Anxiety, Insomnia, Seizures
5
Q
CHEMOPROPHYLAXIS INFLUENZA
MOA of amantadine
A
- Viral uncoating inhibition
- Viral assembly (Hemagglutinin processing)
6
Q
CHEMOPROPHYLAXIS INFLUENZA
Tricyclic amine compounds
A
Amantadine + Rimantadine
7
Q
CHEMOPROPHYLAXIS INFLUENZA
For influenza A at low concentrations
A
Amantadine + Rimantadine
8
Q
CHEMOPROPHYLAXIS INFLUENZA
Methylated amantadine but 4-10 times more active and cause GI problems
A
Rimantadine
9
Q
CHEMOPROPHYLAXIS INFLUENZA
Rimantadine causes ____ problems, while amantadine causes ____ effects.
A
- GI
- Anti-cholinergic
10
Q
NEURAMINIDASE INHIBITORS
Neuraminidase inhibitors are active against ____.
A
Influenza A and B
11
Q
NEURAMINIDASE INHIBITORS
Adverse effect of oseltamivir
A
Nausea & Vomiting
12
Q
NEURAMINIDASE INHIBITORS
Adverse effect of zanamivir
A
Bronchospasms
C/I: COPD and Asthma
13
Q
NEURAMINIDASE INHIBITORS
Neuraminidase inhibitors are ____ analogues.
A
Sialic acid
14
Q
NEURAMINIDASE INHIBITORS
MOA of oseltamivir and zanamivir
A
Prevents the release and spread of new virions
15
Q
NUCLEOSIDE ANALOGUES
Trifluridine
Identify the base.
A
Thymine
16
Q
NUCLEOSIDE ANALOGUES
Idoxuridine
Identify the base.
A
Thymine
17
Q
NUCLEOSIDE ANALOGUES
MOA of nucleoside analogs
A
Inhibiting viral replication
Act as antimetabolite
18
Q
NUCLEOSIDE ANALOGUES
Vidarabine
Identify the base.
A
Adenosine
19
Q
NUCLEOSIDE ANALOGUES
Acyclovir
Identify the base.
A
Guanosine
20
Q
NUCLEOSIDE ANALOGUES
Valacyclovir
Identify the base.
A
Guanosine
21
Q
NUCLEOSIDE ANALOGUES
Famciclovir
Identify the base.
A
Guanosine
22
Q
NUCLEOSIDE ANALOGUES
Penciclovir
Identify the base.
A
Guanosine
23
Q
NUCLEOSIDE ANALOGUES
Ganciclovir
Identify the base.
A
Guanosine
24
Q
NUCLEOSIDE ANALOGUES
Cidofovir
Identify the base.
A
Cytosine
25
# NUCLEOSIDE ANALOGUES
Ribavirin
| Identify the base.
Guanosine
26
# NUCLEOSIDE ANALOGUES
MOA of trifluridine and idoxuridine
1. Act as substrate
2. Viral DNA polymerase inhibition
27
# NUCLEOSIDE ANALOGUES
Non-selective tx for herpes simplex keratitis
Idoxuridine
28
# NUCLEOSIDE ANALOGUES
Tx for HSV (1 & 2) keratoconjunctivitis & recurrent epithelial keratitis
Trifluridine
29
# NUCLEOSIDE ANALOGUES
2’ epimer of natural adenosine
Vidarabine
(ara-A)
30
# NUCLEOSIDE ANALOGUES
Vidarabine source
Streptomyces antibioticus
31
# NUCLEOSIDE ANALOGUES
Alternative to Idoxuridine as 3% ointment for HSV keratitis
Vidarabine
32
# NUCLEOSIDE ANALOGUES
MOA of cytarabine
Blocks Deoxycytidine -> Replication inhibition
33
# NUCLEOSIDE ANALOGUES
Drug of choice for Herpes simplex virus (HSV)
Cytarabine
34
# NUCLEOSIDE ANALOGUES
Anti-cancer for burkitt lymphoma and myeloid & lymphatic leukemia
Cytarabine
35
# NUCLEOSIDE ANALOGUES
A Trisodium phosphonoformate - inorganic pyrophosphate analog
| Replaces the phosphate group
Foscarnet
36
# NUCLEOSIDE ANALOGUES
MOA of foscarnet
Viral DNA polymerase inhibition (Non-competitive)
37
# NUCLEOSIDE ANALOGUES
Prototype of anti-herpetic drug
Acyclovir
38
# NUCLEOSIDE ANALOGUES
MOA of acyclovir
Viral DNA polymerase inhibition
39
# NUCLEOSIDE ANALOGUES
Prodrug of acyclovir with better bioavailability
Valacyclovir
40
# NUCLEOSIDE ANALOGUES
Hydrolyzed to Penciclovir and has the greatest bioavailability
Famciclovir
41
# NUCLEOSIDE ANALOGUES
Used only topically whereas famciclovir can be administered orally
Penciclovir
42
# NUCLEOSIDE ANALOGUES
Drug of choice for Cytomegalovirus (CMV) retinitis
Ganciclovir
43
# NUCLEOSIDE ANALOGUES
Tx of herpes zoster (shingles) for immunocompromised patients
Valacyclovir
44
# NUCLEOSIDE ANALOGUES
Analogue of acyclovir with an additional hydroxymethyl group on the acyl side chain
Ganciclovir
45
# NUCLEOSIDE ANALOGUES
Topical tx of recurrent herpes labialis (cold sores)
Famciclovir/Penciclovir
46
# NUCLEOSIDE ANALOGUES
Drug of choice for Varicella zoster and chicken pox
Acyclovir and valacyclovir
47
# NUCLEOSIDE ANALOGUES
Tx of CMV retinitis in AIDS patients
Cidofovir
48
# NUCLEOSIDE ANALOGUES
2nd line drug for the tx of CMV retinitis in AIDS patients
| 1st line: Cidofovir
Foscarnet
49
# NUCLEOSIDE ANALOGUES
Adverse effects of Ribavirin
1. Anemia
2. Jaundice
50
# NUCLEOSIDE ANALOGUES
Drug of choice for RSV bronchiolitis, Pneumonia in hospitalized children, and Lassa fever
Ribavirin
51
# NUCLEOSIDE ANALOGUES
MOA of ribavirin
Interfere with viral transcription
52
# NUCLEOSIDE ANALOGUES
Phosphonic acid derivative that does not require phosphorylation
Cidofovir
53
# REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Reverse transcriptase converts viral RNA into a ____, ready for integration into the host chromosome
double-stranded DNA
54
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
It has high affinity for HIV RT than for human DNA polymerase
Zidovudine (AZT)
55
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Zidovudine (AZT) + ____ = Delayed AZT-resistant strains
Alpha Interferon
56
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Zidovudine (AZT) can be combined with ____ to overcome bone marrow toxicity.
| 3 drugs
1. Foscarnet
2. Zalcitabine (ddC)
3. Didanosine (ddI)
57
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Symptomatic HIV + Pneumocystis carinii pneumonia (PCP)
Zidovudine (AZT)
58
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
for Zidovudine (AZT) intolerant HIV infection
Didanosine (ddI)
59
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Zidovudine
(AZT)
| Nucleoside analog
Thymidine
60
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Stavudine
(D4T)
| Nucleoside analog
Thymidine
61
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Didanosine
(ddI)
| Nucleoside analog
Guanosine
62
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Lamivudine
(3TC)
| Nucleoside analog
Cytidine
63
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Zalcitabine
(ddC)
| Nucleoside analog
Cytosine
64
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Tenofovir
| Nucleoside analog
Adenine
65
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Zalcitabine (ddC) is combined with ____ for the tx of advance HIV infections.
Zidovudine
(AZT)
| ZZ
66
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Acid stable and well absorbed PO
Stavudine
(D4T)
67
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
Substitution of sulfur atom in place of a methylene group at the 3' of the ribose ring
Lamivudine
(3CT)
68
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
____ + Zidovudine (AZT) = increase CD4+ count
Lamivudine
(3CT)
69
# NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTIs)
HIV 1 + Hepatitis B
Tenofovir
70
MOA of pleconaril
Insert into pockets -> Interfere with virus + cell receptors
71
It targets a broad spectrum of small RNA viruses (picornaviruses)
Pleconaril
72
# ANTI-RETROVIRALS (ART)
It refers to the multidrug regimen for HIV infection
Highly Active Anti-Retroviral Therapy
(HAART)
73
# ANTI-RETROVIRALS (ART)
5 drug classes used in HAART
1. Protease inhibitors
2. Entry inhibitors
3. NRTIs
4. Integrase inhibitors
5. NNRTIs
| PENIN
74
# NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
MOA of NNRTIs
1. HIC-1 inhibition
2. Enzyme distortion
75
# NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
NNRTIs do not require bioactivation because they do not have ____.
Nucleosides
76
# NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
MOA of nevirapine (Viramune)
1. CYP450 -> Hydroxylated metabolites (inactive)
2. Hepatic recycling -> no DNA polymerase action
77
# NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
____ is an NNRTI readily absorbed after oral administration due to its cyclopropyl.
Nevirapine
(Viramune)
78
# NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
Pregnancy category of nevirapine (Viramune)
C
79
# NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
The risk of ____ during nevirapine (Viramune) therapy is greatest in the first 6 weeks.
| Other AE: Rashes, NV
Hepatitis
80
# NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
____ must be used with at least two additional antiretrovirals for HIV-1
| due to 98-99% protein bounding
1. Delavirdine (Rescriptor)
2. Efavirenz (Sustiva)
| MOA: same as nevirapine (Viramune)
81
# NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
Most common adverse effects of Efavirenz (Sustiva)
1. CNS changes
2. Rashes
3. Hepatotoxicity
82
# NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs)
NNRTI rashes can be severe and lead to ____ syndrome
Stevens-Johnson
83
# HIV PROTEASE INHIBITORS
Enzyme that cleaves gag-pro propeptides to yield active enzymes that function in the maturation & propagation of new virus
HIV Protease
84
# HIV PROTEASE INHIBITORS
HIV protease inhibitors can cause ____ and ____.
| ADRs
1. Dyslipidemia
2. Hyperglycemia
85
# HIV ENTRY INHIBITORS
This is also known as compound T20
Pentafuside
Enfuvirtide
86
# HIV ENTRY INHIBITORS
This inhibits the formation of the fusion component conformation of GP41
Pentafuside
Enfuvirtide
87
# CHEMOKINE RECEPTOR BINDERS
1st compound identified as a CXCR4-specific inhibitor but not CCR5
Compound AMD-3100
88
# CHEMOKINE RECEPTOR BINDERS
Exhibits high affinity for CCR5 coreceptors
Compound TAK-779
89
# CHEMOKINE RECEPTOR BINDERS
MOA of chemokine receptor binders
Prevents attachment to CCXR4 and CCR5 on the CD4's surface
90
# HAART
Foscarnet + Ganciclovir
| Indication
HSV1 and 2
91
# HAART
Trifluridine (TFT) / Acyclovir + Interferon
| Indication
Herpetic keratitis
