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MICROBIO DRUGS > Viral Drugs > Flashcards

Viral Drugs Flashcards

1
Q

Enfuvirtide

A

HIV fusion inhibitor

  • binds to gp41 and prevents gp41 from refolding & bringing HIV and Tcell close enough to fuse
  • subcu 2x/day, $20,000/yr

(enFUvirtide blocks FUsion)

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2
Q

Maraviroc

A

HIV fusion inhibitor

  • blocks HIV entry by binding human CCR5 coreceptor
  • metabolized by p450s
  • Resistance due to mutant strains that use CXCR4 to gain entry
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3
Q

Emtricitabine

A

HIV NRTI (nucleoside RT inhibitor)

  • long 1/2 life, can be taken as pill 1x/day, no big drug metabolism interactions
  • fluorinated lamivudine analog

(emTRICitabine TRICks RT into terminating the nucleotide chain)

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4
Q

Tenofovir

A

HIV NRTI (nuceloside RT inhibitor)
- Syntehtic adenosine analog with a phosphate and protective groups (overcome rate-limiting P step)
- Little interaction with p450s
- Single dose per day or combo pill with emtricitabine (Truvada)
- used against HIV also
(Tenofovir is a nucleoTide RT inhibitor)

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5
Q

Truvada

A

HIV Fixed-dose NRTI combination drug, can be used as prophylaxis in sex workers and spouses of HIV+ pts

emTRICitabine and Tenofovir

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6
Q

Stribilid

A

HIV combination drug

ElviTEGravir (integrase inhibitor)/cobicistat (booster)/emTRICitabine/Tenofovir

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7
Q

Etravirine

A

HIV NNRTI

  • 2x/day pull
  • reserved for pts with resistance/failing other therapies

(eTRAVirine prevents the active domains of RT from TRAVeling).

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8
Q

Raltegravir

A

HIV integrase inhibitor

  • no p450 interaction
  • 2x/daily pill
  • used to be reserved now first-line therapy

(ralTEGravir - anti-inTEGrase)

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9
Q

Elvitegravir

A

HIV integrase inhibitor

  • Part of 4-drug combo Stribild (elviTEGravir/CObicstat/emTRICitabine/Tenofovir)
  • CObicstat acts to boost concentration of elviTEGravir

(ElviTEGravir - anti-inTEGrase, CObicstat COoperates)

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10
Q

Dolutegravir

A

HIV integrase inhibitor

  • does not require boosting
  • 1x/day pill not formulated yet
  • active in pts resistent to earlier integrate inhibitors

(DoluTEGravir inTEGrase inhibitor)

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11
Q

Atazanavir

A

HIV protease inhibitor
- processed by CYP3A4, toxic side effects reduce compliance, but 1x/day dose is better than predecessor drugs
(aTAZanavir –> think Taz likes to cleave everything in his path like a protease)

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12
Q

Darunavir

A

HIV protease inhibitor

  • works against isolates resistant to other PI’s
  • better tolerated than tipranavir
  • CYP3A inhibitor

(DARunavir = Tasmanian DARedevil –> protease inhibitor)

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13
Q

Tipranavir

A

HIV protease inhibitor

  • non-peptide structure is unique
  • increased efficacy in the face of other mutations
  • CYP3A iinhibitor

(tiPranavir Protease inhibitor)

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14
Q

Ritonavir

A

HIV protease inhibitor that also inhibits p450s so it is used as a booster in combination drugs with aTAZanavir and DARunavir protease inhibitors.

(RITonavir gets RIT of p450s)

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15
Q

Entecavir

A

currently recommended drug for Hep B, used with Tenofovir

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16
Q

Peg-interferon

A

HepB drug that is no longer prevalent due to adverse side effects; sometimes used in pregnancy because known to be safe for fetus

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17
Q

Rituximab

A

Preemptively put them on Hep B anti-viral therapy if they are on Rituximab or any other immune-compromising therapy. They would be on Rituximab if they needed to have their immune system suppressed (i.e. for transplant etc)

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18
Q

Acyclovir

A

Herpes, CMV nucleoside analog

  • prodrug, chain terminator
  • requires viral thymidine kinase for first phosphotase, making it less toxic to humans
  • oral, topical and IV, generally well tolerated orally
  • Resistance due to HSV-TK mutations and viral DNA polymerase
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19
Q

Cidofovir

A

Herpes, CMV nucleoside analog
- chain terminator, prodrug
- taken up by infected and non-infected cells
- first phosphate already present on the drug, 2 more added by host enzymes
- resistence due to viral DNA pol mutations
- long half-life (advantage)
- dose-dependant nephrotoxicity (disadvantage)
-

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20
Q

Foscarnet

A

Herpes, CMV

  • blocks viral DNA and RNA pol, directly blocks HIV RT
  • binds enzyme pocket, holds tri-P, prevents cleavage
  • specific for viral pol’s
  • activity remains against ganciclovir and cidofovir resistant strains
21
Q

Amantadine

A

Influenza viral entry inhibitor

  • bind the M2 viral channel protein, blocking the unseating process
  • resistance when M2 gets mutated
22
Q

Rimantidine

A

Influenza viral entry inhibitor

  • bind the M2 viral channel protein, blocking the unseating process
  • resistance when M2 gets mutated
23
Q

Zanamivir

A

Influenza viral exit inhibitor

  • viral neuramidase inhibitor prevents sialic residue cleavage, reduces viral escape from infected cells, preventing spread of virus to other cells
  • inhaler
24
Q

Oseltamivir

A

Influenza viral exit inhibitor

  • viral neuramidase inhibitor prevents sialic residue cleavage, reduces viral escape from infected cells, preventing spread of virus to other cells
  • H1N1 likely resistant
  • orally
25
Q

Interferons

A

HBV&HCV

  • human proteins with antiviral immunmodulating and anti proliferative actions by activating JAK/STAT pathway
  • horrible adverse effects (hepatotoxicity, neurotoxicity, autoimmune disorders, psych disorders, nephrotoxicity)
  • PEG increases its half-life from 2–>54 hours
  • reduces p450 metabolism of other drugs
  • never used alone, use with Ribavirin
26
Q

Telbivudine

A

HBV nuceloside analog

27
Q

Tenofovir ^^

A

HBV nucleoside analog

28
Q

Entecavir

A

HBV nucleoside analog

29
Q

Adefovir

A

HBV nucleoside analog

30
Q

Ribavirin

A

HCV nucleoside analog (looks like guanine)

  • used with IFN
  • tetratogenic in animals, keep away from pregnant women
  • aerosolized may cause conjunctivitis, wheezing, rash
31
Q

Sofosbuvir

A

HCV nucleoside analog

  • latest and greatest!
  • genotypes 1&4: use with PEG-IFN/RBV
  • genotypes 2&3: use with RBV - first all-oral therapy
  • SVR 90%
  • SVR 100% achieved with drugs still in development
  • 1st Phosphate included
  • no drug-drug interactions
  • resistance develops slowly
32
Q

Simiprevir

A

HCV protease inhibitor

  • recent drug
  • 80% SVR in all pts (naive or experienced w treatment)
  • once/day orally, lower side effects
33
Q

Famciclovir

A

HSV nucleoside analog (chain terminator)

- not good, mutagenic in animal models and should be avoided during pregnancy

34
Q

Ganciclovir

A

HSV nucleoside analog (chain terminator)

  • many adverse affects (teratogenic, carcinogenic, mutagenic)
  • HIV/immunocompromised pts need these drugs
35
Q

Trifluridine

A

Topical HSV drug, too toxic for anything other than ophthalmic use

36
Q

Vidarabine

A

Topical HSV drug, too toxic for anything other than ophthalmic use

37
Q

Teleprevir

A

HCV Protease Inhibitor

  • used with PEG-IFN/RBV
  • inhibit HCV NS3 serine protease
  • Taken with food multiple x/day
  • resistance develops quickly - don’t use alone!
38
Q

Boceprevir

A

HCV Protease Inhibitor

  • used with PEG-IFN/RBV
  • Taken with food multiple x/day
  • resistance develops quickly - don’t use alone!
39
Q

Daclatasvir

A

HCV
NS5A inhibitor - protein has no enzymatic function but inhibition blocks viral RNA replication and packaging
- binding pocket conserved: broad coverage

40
Q

Ledipasvir

A

HCV
NS5A inhibitor - protein has no enzymatic function but inhibition blocks viral RNA replication and packaging
- binding pocket conserved: broad coverage

41
Q

Entecavir

A

HBV nucleoside analog

  • prodrug
  • unique chain termination: entecavir gets incorporated, a few more bases are added before nucleic acid is so distorted the chain cannot finish
  • treat for life. expensive, ultimately resistance (2 mutations)
42
Q

Adefovir

A
  • prodrug, 1st phosphate included
  • effective after lamivudine resistance and entecavir cross resistance
  • reserved for when drug resistance occurs toward other drugs
43
Q

Telbivudine

A

HBV nucleoside analog

- lamivudine resistant strains are cross-resistant to telbivudine

44
Q

5-fluorocytosine

A

5FC, anti fungal drug
structural analog of cytosine that fungi convert to an analog of dTMP. Inhibits thymine synthesis and blocks fungal DNA synthesis.
Combo with amphotericin due to 5FC resistance

45
Q

Polyenes

A

Anti fungal - bind ergosterol in membrane, increase permeability, cause loss of small molecules from cell

46
Q

Amphotericin

A

anti fungal used for systemic or deep-seated infections, target ergosterol

47
Q

Nystatin

A

topical anti-fungal targets ergosterol

48
Q

Echinocandins

A

anti fungal

block cell-wall polysaccharide synthesis

49
Q

Pentamidine

A

Anti fungal, inhibits self splicing in pneumocystis carnii

selective for fungal because self splicing does not occur in humans

MICROBIO DRUGS (6 decks)

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