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ID S.Nance > Antiviral Drugs > Flashcards

Antiviral Drugs Flashcards

1
Q

Anti-herpes virus Agents

A 
Acyclovir
Valacyclovir
Ganciclovir
Valganciclovir
Cidofovir
Foscarnet
Trifluridine
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2
Q

Anti-herpes virus Agents: Acyclovir

A

Anti-Metabolites: inhibit host polymerases
HSV infections
Activation by Viral Thymidine Kinase
Manage, not cure*

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3
Q

Anti-herpes virus Agents: Valacyclovir

A

Anti-Metabolites
HSV infections
Prodrug; better oral bioavailability
Manage, not cure*

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4
Q

Anti-herpes virus Agents:

Ganciclovir

A

Anti-Metabolites
CMV infections
more toxic
Ph. By viral kinase

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5
Q

Anti-herpes virus Agents:

Valganciclovir

A

Anti-Metabolites
CMV infections
prodrug; better oral bioavailability
Ph. By viral kinase

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6
Q

Anti-herpes virus Agents:

Cidofovir

A

Competitive inhibitor of Viral DNA synthesis
CMV infections (CMV retinitis)
phosphorylated; for resistant strains
nucleotide
Nephrotoxicity + Tubular Secretion: Must be administered with Probenecid

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7
Q

Anti-herpes virus Agents:

Foscarnet

A

Direct inhibition of viral polymerases
HSV and CMV infections (Ganciclovir R CMV and Acyclovir R HSV, VZV)
phosphorylated; for resistant strains
A Pyrophosphate

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8
Q

Anti-herpes virus Agents:

Trifluridine

A

Competes with TTP
inhibits DNA synthesis
primary keratoconjunctivitis and recurrent epithelial keratitis caused by HSV I and II
Activated by Host Kinase (NO viral kinase is required)

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9
Q

Anti-HIV Agents

A

Reverse Transcriptase Inhibitors
Nucleoside Reverse Transcriptase Inhibitors
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
HIV Protease Inhibitors (“-navir”)
Fusion Inhibitor
Integrase Strand transfer Inhibitors (INSTI) (“-gravir”)
CCR5 Antagonist
HAART

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10
Q

Anti-HIV Agents
Nucleoside Reverse Transcriptase Inhibitors
Zidovudine/Azidothymidine (AZT)

A

Thymidine Analog; Substrate for/inhibitor of HIV RT
Inhibits stable infection of new cells
temporarily reduces morbidity/mortality from HIV; use in 3-4 multidrug cocktail
Resistance develops due to mutations in RT
Well absorbed from GI tract; rapidly metabolized and excreted; half-life = 1-3 hours
common, may be severe; bone marrow depression; toxicity enhanced by drugs that compete for glucuronidation (acetaminophen)

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11
Q

Anti-HIV Agents
Nucleoside Reverse Transcriptase Inhibitors
Lamivudine

A

Also used to Tx Hep B

Safe in Pregnant Women

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12
Q

Anti-HIV Agents
Nucleoside Reverse Transcriptase Inhibitors
Abacavir

A

HLA B5701

Metabolized by Alcohol Dehydrogenase

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13
Q

Anti-HIV Agents
Nucleoside Reverse Transcriptase Inhibitors
Tenofovir disproxil

A

used when you have resistance to other agents; Hep. B
Used in combo with Emtricitabine
Nucleotide

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14
Q

Anti-HIV Agents
Nucleoside Reverse Transcriptase Inhibitors
Emtricitabine

A

Flourinated Lamivudine, used with Tenofovir

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15
Q

Anti-HIV Agents
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
Nevirapine

A

Non-competitive RT inhibitor, binds near but not in active side
can be active against AZT-resistant HIV
Rapid emergence of resistance - used in combo therapy
CYP3A4 substrate and inducer
severe, possibly life-threatening skin rash- SJS

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16
Q

Anti-HIV Agents
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
Efavirenz

A

Non-competitive RT inhibitor, binds near but not in active side

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17
Q

Anti-HIV Agents
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
Etravirine

A

Non-competitive RT inhibitor, binds near but not in active side

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18
Q

Anti-HIV Agents
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
Rilpivirine

A

Non-competitive RT inhibitor, binds near but not in active side

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19
Q

Anti-HIV Agents
HIV Protease Inhibitors (“-navir”)
Saquinavir

A

Inhibits the action of HIV protease, which cleaves the translated polyprotein to yield active individual proteins
Prevent viral particle production - added, synergistic activity
DDIs; resistance develops slowly; use in combo with RT inhibitors
Extensive first-pass effect (CYP3A4)-Administered with a PK booster
altered body fat distribution, hyperlipidemia, insulin resistance (buffalo hump, gynecomastia, truncal obesity, facial wasting); Cushingoid effects

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20
Q

Anti-HIV Agents
HIV Protease Inhibitors (“-navir”)
Lopinavir

A

Prevent viral particle production - added, synergistic activity
DDIs; resistance develops slowly; use in combo with RT inhibitors
Extensive first-pass effect (CYP3A4)-Administered with a PK booster
altered body fat distribution, hyperlipidemia, insulin resistance (buffalo hump, gynecomastia, truncal obesity, facial wasting); Cushingoid effects

21
Q

Anti-HIV Agents
HIV Protease Inhibitors (“-navir”)
Ritonavir, Cobicistat

A

“Pharmacokinetic Booster” - inhibitor of CYP3A4 to enhace the actions of these drugs
Prevent viral particle production - added, synergistic activity
DDIs; resistance develops slowly; use in combo with RT inhibitors
Extensive first-pass effect (CYP3A4)-Administered with a PK booster
altered body fat distribution, hyperlipidemia, insulin resistance (buffalo hump, gynecomastia, truncal obesity, facial wasting); Cushingoid effects

22
Q

Anti-HIV Agents
HIV Protease Inhibitors (“-navir”)
Indinavir

A

Prevent viral particle production - added, synergistic activity
DDIs; resistance develops slowly; use in combo with RT inhibitors
Extensive first-pass effect (CYP3A4)-Administered with a PK booster
altered body fat distribution, hyperlipidemia, insulin resistance (buffalo hump, gynecomastia, truncal obesity, facial wasting); Cushingoid effects

23
Q

Anti-HIV Agents
HIV Protease Inhibitors (“-navir”)
Darunavir

A

Only Ad. With sub-therapeutic dose of Ritonavir
Prevent viral particle production - added, synergistic activity
DDIs; resistance develops slowly; use in combo with RT inhibitors
Extensive first-pass effect (CYP3A4)-Administered with a PK booster
altered body fat distribution, hyperlipidemia, insulin resistance (buffalo hump, gynecomastia, truncal obesity, facial wasting); Cushingoid effects

24
Q

Anti-HIV Agents
Fusion Inhibitor
Enfuvertide

A

interferes with the entry of HIV-1 into host cells by inhibiting the fusion of the virus and cell membranes
reserved for individuals who have advanced disease or show resistance to current HIV tx
cysts, nodules as site of inj

25
Q

Anti-HIV Agents
Integrase Strand transfer Inhibitors (INSTI) (“-gravir”)
Raltegravir

A

inhibits the catalyic activity of integrase
prevents integration of the proviral gene into human DNA
Metabolized by UGT1A1

26
Q

Anti-HIV Agents
Integrase Strand transfer Inhibitors (INSTI) (“-gravir”)
Elvitgravir

A

inhibits the catalyic activity of integrase

prevents integration of the proviral gene into human DNA

27
Q

Anti-HIV Agents
Integrase Strand transfer Inhibitors (INSTI) (“-gravir”)
Dolutgravir

A

inhibits the catalyic activity of integrase
prevents integration of the proviral gene into human DNA
-Eliminated via UGT1A1

28
Q

Anti-HIV Agents

CCR5 Antagonist

A

Maraviroc
Selectively and reversibly binds to the CCR5 coreceptors located on human CD4 cells; inhibits gp120 conformational change required for fusion/entry
used in combo with other agents in pts with evidence of HIV-1 strains resistant to multiple antiretroviral therapy

29
Q

Anti-HIV Agents

HAART

A

2 nucleoside reverse transcriptase inhibitors + either INSTI (-gravir), NNRTI, or PI (-navir) (with a pharmacokinetic booster-Ritonavir, Cobicistat)
pts are prone to opportunistic infections; numerous DDIs

30
Q

Anti-Opportunistic Infx in AIDS pts

For Pneumocystic jiroveci (PJP) infx

A

TMP/SMX

prevention/treatment

31
Q

Anti-Opportunistic Infx in AIDS pts

For MAC infx

A

Clarithromycin plus ethambutol

32
Q

Anti-Opportunistic Infx in AIDS pts

For Toxoplasmosis

A

Pyrimethamine/sulfadiazine plus folinic acid

33
Q

Anti-Opportunistic Infx in AIDS pts

For Cryptococcal meningitis

A

Amphotericin B/Flucytosine

34
Q

Anti-Opportunistic Infx in AIDS pts

For CMV

A

Ganciclovir (Valgancyclovir)

35
Q

Anti-Opportunistic Infx in AIDS pts

For Candidiasis

A

Fluconazole

36
Q

Anti-Opportunistic Infx in AIDS pts

For HSV

A

Acyclovir (Valacyclovir)

37
Q

Anti-Opportunistic Infx in AIDS pts

For Herpes Zoster

A

Acyclovir (Valacyclovir)

38
Q

Inhibitors of Viral Nucleic Acid Synthesis

A

Ribavirin
anti-metabolite; blocks GMP formation
Effective as aerosol for RSV Tx; tx of hepatitis C(+ Peg IFN)
human teratogen; dose-dep. myelosuppresion

39
Q

Influenza Drugs
Viral Neuraminidase Inhibitors (“-amivir”)
Oseltamivir

A

Inhibit viral NA
Prevents viral release, infection of additional cells
all common influenza (A, B and C) virus strains
oral; prodrug; activated in gut and liver
well-tolerated, some n/v

40
Q

Influenza Drugs
Viral Neuraminidase Inhibitors (“-amivir”)
Zanamivir

A

Inhibit viral NA
Prevents viral release, infection of additional cells
effective early in infection (before 2 days)
oral inhalation
bronchospasm in asthmatics

41
Q

Influenza Drugs
Viral Neuraminidase Inhibitors (“-amivir”)
Peramivir

A

Inhibit viral NA
Prevents viral release, infection of additional cells
tx of acute, uncomplicated influenza in adults who have been symptomatic <2 days
single IV dose

42
Q

Influenza Drugs
Inhibitors of Uncoating
Amantadine

A

Block viral uncoating by blocking M2 proton channel; disrupts endocytosis and viral disassembly
protects against and treats only Influenza A
give in first 48 hours of contact; oral
GI intolerance, CNS effects

43
Q

Influenza Drugs
Inhibitors of Uncoating
Rimantadine

A

Block viral uncoating by blocking M2 proton channel; disrupts endocytosis and viral disassembly
protects against and treats only Influenza A
give in first 48 hours of contact; oral
GI intolerance, CNS effects

44
Q

Hepatitis C Drugs

Peg-Interferon alpha

A

Standard of Care for HCV

45
Q

Hepatitis C Drugs

Ribavirin

A

inhibits RNA Polymerase

Standard of Care for HCV

46
Q

Hepatitis C Drugs

Sofosbuvir

A

nucleotide analog, inhibits an HCV RNA-dependent RNA polymerase
$$

47
Q

Hepatitis B Drugs

Lamivudine-NRTI

A

Anti-retroviral nucleoside/nucleotide analog polymerase inhibitors

48
Q

Hepatitis B Drugs

Tenofovir-NRTI

A

Anti-retroviral nucleoside/nucleotide analog polymerase inhibitors

ID S.Nance (20 decks)

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