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Pharm Block 3 > Antivirals > Flashcards

Antivirals Flashcards

(65 cards)

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1
Q

1 step - Binds to CD4 receptor of CD4 + T cells

A

GP120

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2
Q

2 step - binds to CCR5/CXCR4 co receptor of T cells

A

GP120

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3
Q

3 step - binds to T cell membrane and causes fusion of virus and T cell followed by viral genome entry into the cell

A

GP41

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4
Q

Codes for p24 and p17 (core protein)

A

Gag

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5
Q

Reverse transcriptase, integrate, protease

A

Pol

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6
Q

Gp120, gp41 (entry)

A

Env

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7
Q

Competive inhibition of HIV 1 reverse transcriptase

A

NRTIs

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8
Q

Absent hydroxyl group at 3’
Inhibition of 3’-5’ PDE bond formation
Incorporation into growing viral DNA strand causes premature chain termination
Nucleosides needs phosphorylation by cellular enzymes to be activated
Mitochondrial toxicity

A

NRTIs

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9
Q

Less toxic
ADR - headache, nausea, neutropenia
Cytidine base

A

Lamivudine

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10
Q

No serious A/E: low affinity for human DNA polymerase
Fanconi like syndrome
Adenosine base

A

Tenofovir

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11
Q 
Used during pregnancy and breastfeeding to reduce vertical infection 
Tx and prophylaxis of HIV
Combined with NNRTI and PI
Can cause anemia
Tymidine base
A

Zidovudine

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12
Q

ADR acute pancreatitis and peripheral neuropathy

Tymidine base

A

Stavudine

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13
Q

ADR: acute pancreatitis, optic neuritis, diarrhea, peripheral neuropathy
Adenosine base

A

Didanosine

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14
Q

Hypersensitivity associated with HLA-B 57:01 allele
May cause delayed type 4 hypersensitivity ran
Guanosine base

A

Abacravir

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15
Q

Less toxic
SE: hyperpigmentation of palms and soles
Cytidine base

A

Emitricitabine

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16
Q

Bind directly and not phosphorylated by intracellular enzymes - resulting in allosteric inhibition preventing replication of DNA

Bind directly and allosteric inhibition of HIV reverse transcriptase

A

NNRTIs

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17
Q

SE: insomnia and nightmares, rash is freq. with all drugs - 1st 4wks Rx

A

NNRTIs - especially efavirenz

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18
Q

NNRTIs

A

Nevarapine
Elfavirenz
Delaviridine

Etravirine
Rilpivirine

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19
Q

Inhibit the aspartate protease protease in HIV

Inhibit cytochrome p450

A

Protease inhibitors “Navir”

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20
Q

Codes for production of HIV enzymes, resistance mechanism will be developed in varying genes

A

POL gene

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21
Q

SE: hyperglycemia in diabetes due to insulin resistance, lipodystrophy, paraesthesia, rash at therapeutic [ ]

A

Protease inhibitors

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22
Q

Need to process gag and pol polyproteins into mature HIV components

A

Aspartate protease

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23
Q

Protease inhibitor that may cause nephrolithiasis

A

Indinavir

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24
Q

Protease inhibitor has greatest cytochrome p450 inhibitory effect and boosts concentration of other protease inhibitors

A

Ritonavir

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25
Protease inhibitor - least toxic and easily develops resistance
Saquinavir
26
Protease inhibitor causing indirect hyperbilirubinemia
Atazanavir
27
Maximal suppression of HIV replication and increase px’s CD4 + T cell count Combo of PI or NNRTI with one or two NRTIs often recomm. Used to prolong life and delay sx’s
HAART
28
1st line for HAART
Lamivudine + NRTI (tenofivir, emtricitabine) + NNRTI (efavirenz, rilpivirine, etravirine)
29
Boost regimen
Co admin low dose ritonavir with other anti HIV drugs increase plasma [ ] of drugs Lopinavir is PI with low oral bioavailability Lopinavir + ritonavir increase antiretroviral effect Saquinavir + ritonavir - prolong QT
30
Viral co receptor antagonists - competes for binding at CCR5 co receptors (inhibits entry) Not for CXCR4 Contra: end stage renal failure
Maraviroc
31
Binds gp41 Inhibits fusion of HIV to host CD4 cells Causes local skin rxn, neutropenia, active against drug resistant HIV
Enfuvirtide
32
Integrate inhibitor | Block HIV encoded integrate preventing integration of virus DNA into host chromosome
Raltegravir and other “gavir”
33
Prototype, oral or IV | Guanosine nucleoside analog
Acyclovir
34
Inhibits viral DNA dependent polymerase Triphosphate incorporates into replicating DNA - halting synthesis Absence of thymidine kinase in a herpes strain confers resistance
Acyclovir
35
Treats serious HSV and VZV infection, neonatal infections
Acyclovir
36
ADR: dose dependent decrease GFR, interstitial nephritis crystalline nephropathy
Acyclovir
37
Metabolized to acyclovir Improved bioavailability DOC: herpes zoster
Valacyclovir
38
Metabolized to peniclovir | To for shingles and VZV
Famuclovir
39
Inhibits fusion between plasma membrane and HSV envelope | Topical, aliphatic alcohol
Docosanol
40
Thymidine analogs Get incorporated into DNA - faulty DNA formed - breaks down easily Faulty DNA - synthesis of wrong viral proteins - maturation of virus inhibited Only topical use
Idoxuridine | Trifluridine
41
Use for herpes simplex - keratojunctivitus Vaccine virus keratitis SE: ocular iirritation, edema of lids, photophobia
Trifluidine
42
Converted to mono phosphate by virus encoded kinase UL97 Resistance: mutation in UL97 or DNA polymerase
Ganciclovir
43
TX severe CMV
Ganciclovir
44
ADR: high systemic toxicity - BM suppression, thrombocytopenia, increase crystalluria
Ganciclovir
45
Does not require phosphorylation by viral kinase - active against ganciclovir and acyclovir resistant CMV, HSV, VZV
Foscarnet
46
Inhibits viral DNA and RNA poly and reverse transcriptase
Foscarnet
47
ADR: high toxicity- nephrotoxic, hypocalemia, hypomagnesium
Foscarnet
48
ADR: high systemic toxicity - BM depression (phosphorylated by host cell)
Trifluridine
49
Phosphorylated by host cell (not viral kinase) | Active against acyclovir and ganciclovir resistant CMV, VZV, HSV
Cidofovir
50
ADR: nephrotoxicity, leading to proteinuria, azotemia, and metabolic acidosis
Cidofovir
51
Only against inf A virus Blocks M2 proton ion ch of virus and inhibits uncoating of viral RNA ADR: insominia, seizures and arrhythmias at high doeses, livedo reticularis (venous swelling due to capillary thrombi) Contra- pregnancy
Amantadine | Rimantadine
52
Enzyme found on outer cell membrane of viral particles
Neuraminidase
53
Inhibits neuramindase, prevents release of virions Covers inf A, B and avian infuenza Used within 36-48 hour of onset
Oseltamivir Zanamivir Peramivir
54
immunomodulatory cytokines released from virus infected cells interleukins upregulate their synthesis in infected cells
interferons
55
treats hep B and C, kaposi sarcoma from HHV8, condyloma accuminata caused by HPV
interferon alpha
56
may cause flu like syndrome, profound fatigue, myelosuppression with zidovudine, lupus
interferon alpha
57
guanosine nucleoside analog inhibit GTP and viral RNA syn. inhibits RNA dependent RNA poly and capping of mRNA
ribavirin
58
ADR: dose dependent hemolytic anemia, highly teratogenic oral admin - HCV indications: with interferon chronic hep C Nebulized: RSV bronchiolitis
ribavirin
59
inhibits the NS5B RNA polymerase | tx hep C
sofosabuvir
60
NS3/4 protease inhibitors - | serine protease enzyme required for cleaving viral polypeptide into fxn units
simprevir | grazoprevir
61
pro drug, active against hep B inhibits HBV DNA poly, itself gets incorporated and terminates DNA chain ADR: sore throat, headache, weakness, AB pain, flu like syndrome, *nephrotoxicity and * lactic acidosis
adefovir dipiroxil
62
antibody to A antigen on RSV
palivizumab
63
``` NS5A inhibitor (Hep C1) inhibits vira replication, assembly and release ```
ledipasvir
64
provides cure for Hep C
ledipasvir + sofosabuvir alone or along with ribavirin and/or pedinterferons
65
guanosine nucleoside inhibits HBV DNA poly: base priming, reverse transcription of - strand and synthesis of + strand treats hep B
entecavir tenofovir lamivudine

Pharm Block 3 (11 decks)

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