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From Flashcardlet > pharmacology 3.3A Anti-virals > Flashcards

pharmacology 3.3A Anti-virals Flashcards

0
Q

Interferon alfa

A

Blocks viral penetration to host cell membrane

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1
Q

Doc Mara En Pal

Doconasol
Maraviroc
Enfuviride
Palivizumab

A

Blocks viral attachment and entry

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2
Q

A-man Ri-man

Amantadine
Rimantadine

A

Blocks viral uncoating

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3
Q

N,NN,FAE

NRTI
NNRTI
Foscarnet
Acyclovir
Entecavir
A

Blocks viral nucleic acid synthesis

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4
Q

Protease inhibitors (ritonavir,indinavir)

A

Blocks late protein synthesis and processing

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5
Q

Neuraminidase inhibitors (zanamivir, oseltamivir)

A

Blocks viral release/exit from host cell

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6
Q

Acyclovir
Valacyclovir
Famciclovir

A

Tx for HSV and VZV

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7
Q

Famciclovir and valacyclovir

A

Superior Tx for Herpes Zoster

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8
Q

Acyclovir
Panciclovir
Ganciclovir

A

Phosphorylated by virus’ thymidine kinase

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9
Q

Trifluridine

Cidofovir

A

Prevents host kinase phosphorylation

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10
Q

Foscarnet

A

Prevents competitive inhibition of viral DNA polymerase -> inhibition of viral DNA synthesis

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11
Q

Acyclovir

A

Acyclic guanosine derivative

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12
Q

Acyclovir

A

Both a substrate and an inhibitor of viral DNA Polymerase (chain termination because lacks 3’-OH)

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13
Q

Acyclovir

A

HSV: decreases viral shedding in genital herpes

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14
Q

Acyclovir

A

ADR:
Crystalluria (maintain full hydration)
Neurotoxicity
NOT hematotoxic

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15
Q

Valacyclovir and Famciclovir

A 
Prodrug
Lesser post herpetic neuralgia
Tx for HSV infections
High bioavailability
High CSF advantage
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16
Q

Valacyclovir

A

Improved acyclovir

Lesser pst herpetic neuralgia

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17
Q

Famciclovir

A

Does NOT cause chain termination because has 3’-OH

Prodrug of penciclovir

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18
Q

Doconazole

A

Topical cream

Inhibits viral entry and attachment to host cell

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19
Q

Trifluridine

A

Effect on 2nd phase phosphorylation

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20
Q

Ganciclovir
Foscarnet
Cidofovir

A

Against CMV

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21
Q

Ganciclovir

A

1st phosphorylation viral-specific via phosphotransferase
May cause chain termination
Inhibits viral DNA polymerase
IV,Oral, Intraocular implant

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22
Q

Ganciclovir

A

ADR:
Dose-limiting hematotoxicity
Crystalluria (maintain hydration)
Seizures in intraocular implant form

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23
Q

Foscarnet

A

Not an antimetabolite
Inhibits viral DNA and RNA polymerases and HIV reverse transcriptase without initial phosphorylation by viral enzyme
Does NOT cause chain termination

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24
Q

Foscarnet

A

ADR:
Dose-limiting nephrotoxicity with acute tubular necrosis
Hypocalcemia (electrolyte imbalance)

Avoid:
Pentamidine (more pronounced hypocalcemia)
Amphotericin B and aminoglycosides (nephrotoxic)

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25
Q

Cidofovir

A

Cytosine nucleotide analog

Independent of viral enzyme phosphorylation

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26
Q 
NRTI
NNRTI
PI: protease inhibitors
Fi: fusion inhibitors
HAART

Azidothymidine (AZT)

A

Anti retroviral agents

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27
Q

NRTI (nucleoside/nucleotide reverse transcriptase inhibitor)

A

Competitively inhibits HIV-1 reverse transcriptase

Incorporated into DNA causing chain termination

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28
Q

NRTI

A 
ADR:
Mitochondrial toxicity (DNA Polymerase Gamma)
Lipid metabolism disorders
Lactic acidosis
Hepatic steatosis
29
Q

Aba Did Ten LES ZaZi

Abacavir
Didanosine (ddl)
Tenofovir
Lamivudine (3TC)
Emtricitabine (FTC)
Stavudine (d4T)
Zalcitabine (ddC)
Zidovudine (AZT analog)
A

NRTIs

30
Q

Didanosine (ddl)

A

Guanosine analog
ADR:
Pancreatitis

31
Q

Lamivudine (3TC)

A

Cytosine analog

32
Q

Emtricitabine

A

Fluorinated analog of lamivudine

33
Q

Stavudine (d4T)

A

Thymidine analog
ADR:
Peripheral neuropathy
Myelosuppresion (<AZT)

34
Q

Zidovudine

A 
Deoxythymidine analog
Azidothymidine prototype
ADR:
Macrocytic anemia
High toxicity with acetaminophen, ASA, cimetidine, probenecid, sulfonamide (AZT prototype)
Dose-limiting hematotoxicity
Severe peripheral neuropathy
35
Q

Tenofovir

A

Acyclic adenosine phosphate analog

36
Q

Zalcitabine (ddC)

A

Cytosine analog
Administered 1-2 hours after an antacid
ADR:
Pancreatitis

37
Q

NNRTI (non nucleoside/nucleotide reverse transcriptase inhibitor

A

Binds directly to HIV-1 reverse transcriptase (RNA to DNA)
Blocks RNA and DNA-dependent DNA polymerase
Does not compete with nucleoside nor require phoshorylation
Metabolism via CYP450

38
Q

DEEN

Delaviridine
Efavirenz
Nevirapine
Etravirine

A

NNRTIs

39
Q 
Designer drug (knowledge of aspartate protease)
Bind to a unique dipeptide on enzyme
Prevents production of final structural proteins
A

Protease inhibitors

40
Q

Protease inhibitors

A

Fat redistribution causes cushingoid appearance

Insulin resistance, bleeding tendencies, substrate and inhibitors of CYP3A4 isozyme

41
Q

Ritonavir

A

Protease inhibitor

42
Q

Ritonavir

A

Increases effect of dronabinol (medical marijuana), erythromycin, ketocnazole, and rifampin
ADR:
Nausea, diarrhea, paresthesia, hepatitis

43
Q

Indinavir

A

Protease inhibitor with lesser side effects

44
Q

FLAIN STAR

Fosamprenavir
Lopinavir
Amprenavir
Indinavir
Nelfinavir

Saquinavir
Tipranavir
Atazanavir
Ritonavir

A

Protease inhibitors

45
Q

Entry/fusion inhibitors

A

Binds to gp41 subunit of envelope glycoprotein (halts conformational changes) to block viral entry into the cell

46
Q

Enfuvirtide

A

The only fusion inhibitor given SQ

Resistance occurs due to gp41 codon mutations

47
Q

Maraviroc

A

Prevents fusion of virus to cell membrane by binding to CCR5 (chemokine receptor necessary for entrance of HIV into CD4+ cells. Substrate of CYP3A4)

48
Q

Raltegravir

A

Integrase strand inhibitor

49
Q

Raltegravir

A

Pyrimidine analog that binds viral enzyme integrase

50
Q

HAART (highly active anti-retroviral)

A

ABC triple therapy

51
Q

HAART

A

Decreases viral DNA
Reverse decline in CD4+ cells
Decrease opportunistic infections

52
Q

Thymidine analogs:
Azidothymidine (AZT)
Stavudine (d4T)

A

Group A in HAART

53
Q

Z DEAL

Zalcitabine (ddl)
Didanosine (ddc)
Emtricitanine 
Abacavir
Lamivudine (3TC)
A

Group B of HAART

54
Q

Pi: indinavir or ritonavir
NNRTI: efavirenz or nevirapine

A

Group C of HAART

55
Q

E-RAIL

Interferon alfa-2B
Lamivudine (3TC)
Adefovir
Entecavir
Ribavirin
A

Anti hepatitis agents

56
Q

Interferon alfa-2B

A

Host cytokine with complex anti viral immunomodulatory and antiproliferative properties

Binds to specific cell membrane receptors w/c induces intracellular signals

Inhibits viral:
Penetration
Translation
Transcription
Protein processing, maturation, and release

Increased expression of MHC antigens

Augments proliferation and survival of cytotoxic T cells

57
Q

Interferon alfa -2B

A

Used for:
chronic hepatitis C
Hepatitis B Virus (HBV)

58
Q

Lamivudine

A

Causes chain termination by inhibiting nucleoside of HIV reverse transcriptase and HBV DNA polymerase by competing with deoxycytidine triphosphate for viral DNA incorporation

Longer intracellular half life in HBV than HIV infected cells

Lower dosages and les frequent administration

SAFELY ADMINISTERED TO PATIENTS WITH COMPENSATED LIVER DISEASE

Cross resistance between lamivudine and entricitabin

Tx for CHRONIC HEPATITIS B

59
Q

Adefovir

A

An acyclic phosphonated adenine nucleotide analog
No HBV resistance
Causes chain termination after incorporation into viral DNA by competitively inhibiting HBV DNA polymerase
Suppresses HBV replication and improves live histology and fibrosis
Tx for chronic hepatitis B

ADR:
Dose dependent nephrototxicity
Lactic acidosis
Severe hepatotoxicity

60
Q

Entecavir

A

Guanosine nucleoside analog
No resistance despite 48weeks of use

Competitively inhibits all three functions of HBV DNA polymerase:
Base priming
Reverse transcription of negative strand
Synthesis of positive strand of HBV DNA
100% bioavailability on empty stomach
61
Q

Ribavirin

A

Inhibits guanosine triphosphate formation
Prevents capping of viral mRNA
Blocks RNA-dependent DNA polymerase

62
Q

Ribavirin

A

Indication: chronic HEPATITIS C

Contraindication:
Uncorrected anemia
End-stage renal failure
Ischemic vascular disease in pregnancy

ADR:
Dose dependent haemolytic anemia
Insomnia
Pruritus
Aerosol forms: conjunctival and bronchial irritation, teratogenic
63
Q

Amantadine and rimantadine

Zanamivir and oseltamivir

A

Agents against influenza A

64
Q

Amantadine and rimantadine

A

Drug resistant influenza A virus mutants infect CONTACTS of patients in treatment

65
Q

Rimantadine

A

Longer half life than amantadine

No dosage adjustment required in renal failure patients

66
Q

Amantadine and rimantadine

A

Blocks M2 proton ion channel of virus
Inhibit uncoating with host
Prevent replication

Permits acidification of viral core
Activates viral RNA reverse transcriptase

Reduce flu symptoms if given within 48hours of contact

ADR:
GIT irritation
Dizziness
Ataxia and slurred speech

67
Q

Zanamivir and Osetalmivir

A

Analogs of sialic acid
Neuraminidase inhibitors (prevent viral release, prevent viral spread)
Has activity for both influenza A and B

68
Q

Zanamivir

A

Inhalational for Tx of Influenza A and B

69
Q

Oseltamivir

A

Tx for influenza A and B
Taken orally
Activated in the gut and liver
ADR: GIT symptoms

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