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Pharmacology (Fall) > Antivirals > Flashcards

Antivirals Flashcards

1
Q

What are the main drugs for HSV?

A
  • Acyclovir
  • Famciclovir
  • Docosanol
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2
Q

What are the main drugs for CMV?

A
  • Foscarnet
  • Ganciclovir
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3
Q

What are the main drugs for Influenza?

A
  • Amantadine
  • Rimantadine
  • Zanamivir
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4
Q

What are the drugs for HBV, HCV?

A
  • Interferon
  • Lamivudine (NRTI)
  • Boceprevir
  • Ribavarin
  • Sofosbuvir
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5
Q

What is Herpes Simplex Virus (HSV)?

A
  • Neurotropic
  • HSV-1 (cold sores), HSV-2 (genital herpes)
  • Chicken pox, singles (Varicella zoster - VZV), cytomegalovirus (CMV)
  • Close contact transmission
  • Latent infection
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6
Q

What does HSV effect?

A

lytic cycle in epithelial cells

viral progeny spread to sensory neurons

neurotrophic

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7
Q

What is Acyclovir (Zovirax)?

A

= drug for HSV

  • synthetic nucleoside analog
  • Viral thymidine kinase converts to acyclo-GMP
  • Acyclo-GTP inhibitor of viral DNA polymerase
  • Viral DNA chain termination
  • Tx for genital herpes, shingles, cold sores & chicken pox
  • oral or IV
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8
Q

What is Famciclovir?

A

= drug for HSV

  • prodrug of 6-deoxypenciclovir - 1st pass metabolism converts to penciclovir
  • active against HSV-1, HSV-2 & VZC
  • oral or topical
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9
Q

What is Docosanol?

A

= drug for HSV

  • inhibitor of fusion of HSV-1 virus with host cell.
  • Topical formulation.
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10
Q

What is CMV?

A
  • CMV major problem in immuno-compromised patients (organ transplantation).
  • Can lead to liver failure, colitis and retinitis (inflammation of retina).
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11
Q

What is Ganciclovir?

A

= drug for CMV

  • analog of acyclovir: x20-100 more effective against CMV;
  • targets virus specific protein kinase phospho-transferase UL97.
  • Intravenous.
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12
Q

What is Foscarnet?

A

= drug for CMV

  • reversible inhibitor of viral DNA/RNA polymerases;
  • CMV infection and resistant HSV;
    range of side effects (intravenous only)
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13
Q

What are the 3 drug targets for Influenza virus?

A
  1. Hemagglutin (Hag) binds to sailic acid sugars on cells
  2. Neuraminidase cleaves sailic residues to release virus
  3. M2 ion channel - proton channel that modulates pH & regulates uncoating
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14
Q

What are Neuraminidase Inhibitors?

A
  • Viral neuraminidase - glycoside hydrolase enzyme
  • Cleave glycosidic linkages on neuraminic (sailic) acid to release virus
  • Permits release of viral particle from host cell
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15
Q

What is Zanamivir?

A

= drug for Influenza (Neuraminidase Inhibitor)

  • effective prophylaxis and against spread of infection in flu A and B (b/c inhibits virus from leaving)
  • Problem - needs to be taken within 6-12 hr

(inhale)

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16
Q

What is Amantadine; Rimantadine?

A

= drugs for Influenza (Inhibitors of Viral Uncoating)

  • Block M2 channel
  • Prevent acidification of viral particle
  • Stop release of viral genome and uncoating
  • Early therapy effective against influenza A
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17
Q

What are Antiretrovirals?

A

denoting or relating to a class of drugs that inhibit the activity of retroviruses such as HIV

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18
Q

What are the main Antiretrovirals drugs?

A
  • NRTIs = AZT, abacavir, lamivudine, emtricitabine;
  • NNRTIs = efavirenz, nevirapine;
  • Protease inhibitors = atazanavir, ritonavir;
  • Fusion inhibitors = enfuvurtide, maravaroc;
  • DNA strand transfer inhibitors = raltegravir
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19
Q

What are the Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs)?

A
  • Zidovudine (AZT)
  • Abacavir
  • Lamivudine
  • Emtricitabine

= Antiretrovirals drugs

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20
Q

What are the Non Nucleoside/nucleotide reverse transcriptase inhibitors (NNRTIs)?

A
  • Efavirenz
  • Nevirapine

= Antiretrovirals drugs

21
Q

What are the Protease Inhibitors?

A
  • Atazanavir
  • Ritonavir

= Antiretrovirals drugs

22
Q

What are the Fusion Inhibitors? What are the Co-Receptor Inhibitors?

A

Fusion inhibitors
- Enfuvurtide

Co-receptor
- Maravaroc

= Antiretrovirals drugs

23
Q

What are the DNA Strand Transfer Inhibitors?

A
  • Raltegravir

= Antiretrovirals drugs

24
Q

What is Human Immunodeficiency Virus (HIV)?

A
  • Reverse transcriptase - error prone - drug resistance (why we need to make new drugs)
  • Latent ability - viral integrase enzyme (target for drugs)
  • AIDs
  • Blood/fluid transfer
  • Invades CD4+
  • Cell-mediated immunity lost
  • No cure (need highly active anti-retroviral therapy - HAART)
25
Q

What are the Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs)?

A
  • Analog of native ribosides - LACK 3’-hydroxyl leads to DNA CHAIN TERMINATION
26
Q

What is Zidovudine (AZT)?

A

= drug for HIV (a NRTI)

  • converted to triphosphate by cellular enzymes (that prevents DNA replication)
  • good tissue pen. across BBB (virus does get into CNS/brain)
  • toxic to bone marrow
  • inhibits DNA poly-gamma in mitochondria
  • often come off the drug due to: myopathy, neuropathy
27
Q

What is Abacavir?

A

= drug for HIV (a NRTI)

  • guanosine analogue; unaffected by food
  • avoid alcohol
  • RESISTENCE DEVELOPS SLOWLY!
  • hypersensitivity rxns can be severe
  • higher risk of MI
28
Q

What is Lamivudine?

A

= drug for HIV (a NRTI)

  • cytosine analogue; good bioavailability & unaffected by food
  • recommended in pregnant woman!
  • inhibits RT in HIV & HBV; does not inhibit mtDNA or bone marrow!
29
Q

What is Emtricitabine?

A

= drug for HIV (a NRTI)

  • fluor-derivative of lamivudine;
  • inhibits RT in HIV and HBV;
  • LONG INTRACELLULAR HALF-LIFE OF 39 hr makes once a day treatment feasible. !
  • Good bioavailability and unaffected by food.
  • ORAL formulation, with propylene glycol, CONTRAINDICATED in young children, pregnant women and renal/hepatic failure.
30
Q

What are the Non Nucleoside/nucleotide reverse transcriptase inhibitors (NNRTIs)?

A
  • Non-competitive inhibitors of HIV-1 reverse transcriptase
  • No activation required
  • No effect on bone marrow or mitochondrial DNA polymerase

(Efavirenz, Nevirapine)

31
Q

What is Efavirenz?

A

= drug for HIV (NNRTIs)

  • once daily treatment on an empty stomach.
  • Metabolized by CYP3A4 and CYP2B6. CNS side effects.
  • Some severe – e.g. psychosis.
  • Skin rash.
  • AVOID in pregnant women.
  • Induces CYP3A4.
32
Q

What is Nevirapine?

A

= drug for HIV (NNRTI)

  • good oral bioavailability and not food dependent.
  • Metabolized by CYP3A isoforms.
  • RECOMMENDED in pregnant women.
  • Severe rash can occur.
  • Liver toxicity.
  • Can induce CYP3A system.
33
Q

What are HIV Protease Inhibitors?

A
  • Reversible inhibitors of HIV aspartyl protease
  • Prevents proteolysis of viral polyprotein
  • 1000 fold higher affinity for HIV protease
  • Prevents maturation of viral particles
  • Non-infectious virus produced
  • Used in HAART

(Atazanavir, Ritonavir)

34
Q

What are the Pharmacokinetics for HIV Protease Inhibitors?

A
  • Poor oral bioavailability
  • Substrates for CYP3A4 isozyme of cyt p450
  • Substrates for P-glycoprotein multidrug efflux pump in endothelial cells of brain - restricts access to CNS
  • Bind to plasma proteins – alpha1 acid-glycoprotein

*Not easy to work with; have limitations, but can combine with other drugs

35
Q

What are the adverse effects of HIV Protease Inhibitors?

A
  • Parasthesia, nausea, vomiting, diarrhea
  • Diabetes phenotype
  • Fat redistribution

Resistance
- Mutations of HIV protease gene

36
Q

What are the specific drug toxicity issues with Atazanavir (HIV Protease Inhibitor)?

A
  • Nausea
  • Abdominal discomfort
  • Headache
  • Skin rash
37
Q

What are the specific drug toxicity issues with Ritonavir (HIV Protease Inhibitor)?

A
  • Diarrhea
  • Nausea
  • Taste perversion
  • Vomiting
  • Anemia
  • Increased hepatic enzymes
  • Increased triglycerides
  • Requires refrigeration; take with meals; chocolate milk improves the taste
38
Q

What are drug interactions for HIV Protease Inhibitors?

A

linked to inhibition of CYP isozymes

(Antiarrhythmics, Ergot Derivatives, Antimycobacterial drugs, Benzodiazepines, Barbiturates, Anticoagulants, Herbal Supplements)

39
Q

What is the HIV Integrase Inhibitors mech. of action?

A

?

40
Q

What is Raltegravir?

A

= HIV Integrase Strand Transfer Inhibitor

  • metabolized by UGT1A1.
  • Does not interact with Cyt p450 system.
  • Antacids should be used with caution.
  • Severe hypersensitivity and rash can occur.
41
Q

What is Enfuvirdie?

A

= drug for HIV (Viral Fusion Inhibitor)

  • HIV PROTEIN gp41 mediates cell fusion
  • 36 amino acid peptide binds to gp41
  • Given SC
  • Expensive!!!
  • SALVAGE THERAPY – for multidrug resistant HIV
42
Q

What is Maraviroc?

A

= drug for HIV (Co-receptor Inhibitor)

  • specifically binds to host CCR5 (V3 loop) – thus only effective against HIV-1 tropic for CCR5.
  • Contraindicated in renal impairment.
  • Caution required with hepatic problems.
  • Substrate for CYP3A4.
  • Resistance linked to mutations in gp120 protein.

(*most HIV is for CCR4, so this isn’t perfect)

43
Q

What is Hepatitis B Virus (HBV)?

A
  • most form Hepatitis, Cirrhosis, Carcinoma
  • dsDNA virus - but uses RT!!
  • Blood-blood transfer
  • Vaccine
  • Persistent infection - cccDNA
44
Q

What is Hepatitis C Virus?

A
  • (+)ssRNA virus
  • Difficult to detect symptoms
  • Blood-blood transmission
  • Tx in patients likely to exhibit Cirrhosis
45
Q

What is the Interferon Tx?

A
  • Chronic infection only
  • Interferon alpha 2a/2b
  • Raises cell resistance - ‘antiviral state’
  • Elevates MHC1
  • Increase p53

(normal immune response is to release interferon - to fight viral particles)

(increased antiviral cells - activate CD4+ to target these cells & lead to destruction of hepatitis & prevent spread & cirrhosis)

46
Q

What are the Anti-HBV drugs?

A
  • Use of nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs)
  • DNA chain termination
  • Lamivudine; tenofovir
  • Combined with interferon
47
Q

What is Ribavirin?

A

= Anti-HCV drug

  • Guanidine analogue - inhibits capping of viral mRNA and viral RNA-dependent RNA polymerase – also inhibits influenza/HIV-1.
  • Hemolytic anemia and range of other side effects.
  • Contraindicated in preganancy, kidney disease and vascular disease.

STANDARD THERAPY now ribavirin plus peginterferon alfa

48
Q

What are the Protease Inhibitors for Anti-HCV? What are the Polymerase inhibitors?

A

Inhibit NS3/4A protease that cleaves HCV-encoded poly-proteins. Numerous side effects and drug: drug interactions – CYP3A interactions. Contraindicated with statins and rifampin.

  • Boceprevir – combined with ribavirin and peginterferon
  • Telaprevir

Polymerase Inhibitor:
- Sofosbuvir - inhibits HCV NS5B RNA-dependent RNA polymerase. Combined with ribavirin and peginterferon alfa. Very expensive.

Pharmacology (Fall) (28 decks)

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