Antivirals Flashcards

1
Q

Amantadine

A

Influenza

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2
Q

Oseltamivir

A

Influenza

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3
Q

Zanamivir

A

Influenza

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4
Q

Acyclovir

A

Herpes

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5
Q

Valacyclovir

A

Herpes

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6
Q

Ganciclovir

A

Herpes

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7
Q

Cidofovir w/ Probenicid

A

Herpes

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8
Q

Foscarnet

A

Herpes

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9
Q

INF Alpha

A

Viral Hepatitis

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10
Q

Ribavirin

A

Viral Hep

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11
Q

Simeprevir

A

Viral Hep

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12
Q

Sofosbuvir

A

Viral Hep

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13
Q

Entecavir

A

Viral Hep

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14
Q

Toxicity of Antivirals vs Antibacterials

A

Antivirals is harder because tough to inhibit protein synth without messing up cell protein synth
-Most =Nucleosides and prevent replication, others attack replicative enzymes

MAJORITY are VIRUSTATIC

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15
Q

RNA viruses

A

highly variable, undergo frequent mutation

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16
Q

What is most effective approach to prevent any viral infection?

A

VACCINATION

-high risk pops need addtional prophylaxis

17
Q

Amantadine

A
Non-Nucleoside
Mech: blocks Influenza A viral uncoating via M2 ion channel
          -NO EFFECT ON INFLUENZA B
Complete Resistance!!
PK=Oral
Adverse=well tolerated, some tremors
18
Q

Oseltamivir

A

Neuraminadase Inhibitor
Non-Nucleoside
Mech: Competitive inhibition with neuraminadase, blocks release of virus from infected cells
PK- Oral, metabolized in liver, excreted by kidney
Some resistance
USES: Treatment of Influenza A and B
-MUST BE GIVEN WITHIN 48 hrs of symptom onset to work
Adverse=well tolerated

19
Q

Zanamivir

A

Low oral biioavail

-Bronchospasm with asthma patients

20
Q

Acyclovir

A

Nucleoside Analog for HSV»>VZV

  • inserted into viral DNA by viral DNA poly causes chain term
  • Must be converted from acyclo-GMP to Acyclo-GTP by Thymidine Kinase
  • USES: Gental Herpes with symptoms
    - Herpetic Gingiostomatitis(ORAL LESIONS)
    - Prophalaxis in immunocompromised pts
  • HSV ENCEPHALITIS-present as seizures or temporal headache, CT
  • MUST USE MORE DRUG TO ACHIEVE THERAPEUTIC EFFECT IN VZV or CMV
21
Q

Valcyclovir

A

-prodrug that is rapidly converted to acyclovir by hepatic first pass metabolism

22
Q

Ganciclovir

A

ALL HERPES INFECTIONS, great against CMV
Nucleoside
Triphosphate form blocks viral DNA poly, chain terminated but not immediately
-Restricted Use due to toxicity, –>primarily used with

-Treatments: Mainly used in CMV retinitis in immunocomps,
and CMV prophylaxis in transplant pts
Adverse:Myelosuppression–>Neutropenia, Thrombocytopenia

23
Q

Cidofovir

A

NOT DEPENDENT ON TK Phoshorylation like Acyclovir
USED IN RESISTANT PTs
-Nucleoside action–>inhibits DNA poly
-Given IV
-GIVEN WITH PROBENICID to block OAT1 efflux
-Theapeutics:CMV retinitis in AIDS pts, alternative to ganciclovir
Adverse:MAJOR NEPHROTOXIC, probenicid reduces neph tox

24
Q

Foscarnet

A

POWERFUL SHIT, drug resistant HSV and CMV
Mech: Inhibits Viral DNA poly with 100 fold affinity over mammalian, Inhibits HIV reversetranscriptase,
-GIVEN IV
Treatment: CMV retinitis, RESISTANT strains in AIDS
Adverse: Nephrotox,

25
Q

Hepatitis C

A

RNA virus that does not integrate into human genome,
CURABLE
Acute infection can become chronic and becomes significant risk of morbitdity and mortality
Risks=IV drug use, Sexual, Needle Sticks

26
Q

Standard Hep C treatment

A

24-48 weeks of combination

RIBAVIRIN and INTERFERON ALPHA

27
Q

Ribavirin

A

Crucial Hep C and Pediatric hospital pneumonia bronchitis
NUCLEOSIDE analog
Mech of action=not clearly understood
Causes LETHAL mutations to RNA viruses
Oral dosing
Long Half life—>Hepatic Metabolism and renal excretion

Given for chronic Hep C-orally
Given for RSV and pneumonia- inhalation

Adverse: Hemolytic anemia

28
Q

Interferons

A

cytokines expressed in response to viral infection
INF alpha, beta, and gamma
–>INF alpha=only used clinically, INFalpha2A
BROAD SPECTRUM usage
non-pegylated= short acting
pegylated= Long acting, increased serum conc and prolonged action of drug ONCE PER WEEK DOSING, Inject

Uses: Hep C and Hep B–> usually given with other drugs

  • treat genital warts of HPV
  • Some cancers

Adverse Effects:Flu like symptoms in over 50% of pts
Depression
Neutropenia and Thrombocytopenia

29
Q

Simeprevir

A

Inhibits a viral protease necessary for maturation and release of viral protein

Given in combo with ribavirin and IFN

Adverse: Photosensitivity and rash; contraindicated during pregnancy; CYP3A4

30
Q

Sofosbuvir

A

RNA poly inhibitor
WELL TOLERATED
given with ribavirin/INF and/or simeprevir

31
Q

Hepatitis B

A

Integrates into host genome
VACCINATION is most effective approach
High risk of Fibrosis, cirrhosis, and hepatocellular carcinoma

Prolonged monotherapy =high risk of resistance
but risk relapse if treatment is stopped

TREAT=Pegylated IFN once a week for 48 weeks
and ENTECAVIR daily for 1year

32
Q

Entecavir

A
Nucleoside analog
FIRST LINE FOR CHRONIC HBV
inhibits DNA poly and terminates DNA chain sythesis
Oral dose
Well tolerated

Adverse: well tolerated
chance of lactic acidosis and Hepatomegaly