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Pharm Block 3 > Antivirals > Flashcards

Antivirals Flashcards

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
Q

Protease inhibitor - least toxic and easily develops resistance

A

Saquinavir

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26
Q

Protease inhibitor causing indirect hyperbilirubinemia

A

Atazanavir

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27
Q

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

28
Q

1st line for HAART

A

Lamivudine
+ NRTI (tenofivir, emtricitabine)
+ NNRTI (efavirenz, rilpivirine, etravirine)

29
Q

Boost regimen

A

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
Q

Viral co receptor antagonists - competes for binding at CCR5 co receptors (inhibits entry)

Not for CXCR4

Contra: end stage renal failure

31
Q

Binds gp41
Inhibits fusion of HIV to host CD4 cells
Causes local skin rxn, neutropenia, active against drug resistant HIV

A

Enfuvirtide

32
Q

Integrate inhibitor

Block HIV encoded integrate preventing integration of virus DNA into host chromosome

A

Raltegravir and other “gavir”

33
Q

Prototype, oral or IV

Guanosine nucleoside analog

34
Q

Inhibits viral DNA dependent polymerase
Triphosphate incorporates into replicating DNA - halting synthesis

Absence of thymidine kinase in a herpes strain confers resistance

35
Q

Treats serious HSV and VZV infection, neonatal infections

36
Q

ADR: dose dependent decrease GFR, interstitial nephritis crystalline nephropathy

37
Q

Metabolized to acyclovir
Improved bioavailability

DOC: herpes zoster

A

Valacyclovir

38
Q

Metabolized to peniclovir

To for shingles and VZV

A

Famuclovir

39
Q

Inhibits fusion between plasma membrane and HSV envelope

Topical, aliphatic alcohol

40
Q

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

A

Idoxuridine

Trifluridine

41
Q

Use for herpes simplex - keratojunctivitus
Vaccine virus keratitis
SE: ocular iirritation, edema of lids, photophobia

A

Trifluidine

42
Q

Converted to mono phosphate by virus encoded kinase UL97

Resistance: mutation in UL97 or DNA polymerase

A

Ganciclovir

43
Q

TX severe CMV

A

Ganciclovir

44
Q

ADR: high systemic toxicity - BM suppression, thrombocytopenia, increase crystalluria

A

Ganciclovir

45
Q

Does not require phosphorylation by viral kinase - active against ganciclovir and acyclovir resistant CMV, HSV, VZV

46
Q

Inhibits viral DNA and RNA poly and reverse transcriptase

47
Q

ADR: high toxicity- nephrotoxic, hypocalemia, hypomagnesium

48
Q

ADR: high systemic toxicity - BM depression (phosphorylated by host cell)

A

Trifluridine

49
Q

Phosphorylated by host cell (not viral kinase)

Active against acyclovir and ganciclovir resistant CMV, VZV, HSV

50
Q

ADR: nephrotoxicity, leading to proteinuria, azotemia, and metabolic acidosis

51
Q

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

A

Amantadine

Rimantadine

52
Q

Enzyme found on outer cell membrane of viral particles

A

Neuraminidase

53
Q

Inhibits neuramindase, prevents release of virions
Covers inf A, B and avian infuenza
Used within 36-48 hour of onset

A

Oseltamivir
Zanamivir
Peramivir

54
Q

immunomodulatory cytokines released from virus infected cells

interleukins upregulate their synthesis in infected cells

A

interferons

55
Q

treats hep B and C, kaposi sarcoma from HHV8, condyloma accuminata caused by HPV

A

interferon alpha

56
Q

may cause flu like syndrome, profound fatigue, myelosuppression with zidovudine, lupus

A

interferon alpha

57
Q

guanosine nucleoside analog
inhibit GTP and viral RNA syn.
inhibits RNA dependent RNA poly and capping of mRNA

58
Q

ADR: dose dependent hemolytic anemia, highly teratogenic

oral admin - HCV

indications: with interferon chronic hep C

Nebulized: RSV bronchiolitis

59
Q

inhibits the NS5B RNA polymerase

tx hep C

A

sofosabuvir

60
Q

NS3/4 protease inhibitors -

serine protease enzyme required for cleaving viral polypeptide into fxn units

A

simprevir

grazoprevir

61
Q

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

A

adefovir dipiroxil

62
Q

antibody to A antigen on RSV

A

palivizumab

63
Q 
NS5A inhibitor (Hep C1)
inhibits vira replication, assembly and release
A

ledipasvir

64
Q

provides cure for Hep C

A

ledipasvir + sofosabuvir alone or along with ribavirin and/or pedinterferons

65
Q

guanosine nucleoside
inhibits HBV DNA poly: base priming, reverse transcription of - strand and synthesis of + strand
treats hep B

A

entecavir

tenofovir
lamivudine

Pharm Block 3 (11 decks)

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