Block 3 materials (Antivirals) Flashcards

1
Q

Drugs that are Entry inhibitors?

A

Maraviroc (Attachment)

Enfuvirtide (Fusion)

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2
Q

Drugs that are Reverse transcriptase inhibitors?

A

NRTI’s
Abacavir (ABC)
Emtricitabine (FTC)
Lamivudine (3TC)
Tenofovir (TDF)
Zidovudine (ZDV,
formerly AZT)

NNRTI
Delavirdine
Efavirenz
Nevirapine

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3
Q

Drugs that are integrase inhibitors?

A

gravir suffix

Dolutegravir
Elvitegravir
Raltegravir
Bictegravir

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4
Q

Drugs that are protease inhibitors?

A

navir suffix

Atazanavir
Darunavir
Fosamprenavir
Indinavir
Lopinavir
Ritonavir
Saquinavir

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5
Q

Drugs that are nucleic acid synthesis inhibitors?

A

1) Guanosine analogs
- Acyclovir, etc (HSV, VZV)
- Ganciclovir (CMV)

2) Adenosine analog
- Remdesivir (SARS-CoV-2)

3) Endonuclease inhibitor
- Baloxavir (influenza virus)

4) Viral DNA polymerase
inhibitors
- Cidofovir &Foscarnet
(HSV* & CMV)

5) Guanine nucleotide synthesis
- Ribavirin (RSV, HCV

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6
Q

Drugs that inhibit progeny release?

A

Neuraminidase inhibitors
Oseltamivir & Zanamivir (Influenza A & B)

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7
Q

Oseltamivir & Zanamivir

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Neuraminidase inhibitors that prevent the release of viral progeny

Clinical uses:
Influenza A & B

Adverse effects:
1) Gi upset
2) Exacerbate COPD (Zanamivir)

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8
Q

MOA:
Neuraminidase inhibitors that prevent the release of viral progeny

Clinical uses:
Influenza A & B

Adverse effects:
1) Gi upset
2) Exacerbate COPD (Zanamivir)

A

Oseltamivir & Zanamivir

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9
Q

Baloxavir

MOA:

Clinical uses:

A

MOA:
Inhibits cap0snatching endonucleases to reduce viral replication

Clinical use:
Reduce the severity of influenza virus within 48hrs

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10
Q

MOA:
Inhibits cap0snatching endonucleases to reduce viral replication

Clinical use:
Reduce the severity of influenza virus within 48hrs

A

Baloxavir

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11
Q

Remdesivir

MOA:

Clinical uses:

A

MOA:
Adenosine analog that inhibits viral RNA-dependent RNA polymerase (reduce viral production)

Clinical use:
SARS-CoV-2 (covid)

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12
Q

MOA:
Adenosine analog that inhibits viral RNA-dependent RNA polymerase (reduce viral production)

Clinical use:
SARS-CoV-2 (covid)

A

Remdesivir

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13
Q

Acyclovir, Famciclovir, Valacyclovir

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

MOA:
Guanosine analogs that are phosphorylated by HSV/VZV thymidine kinase to inhibit viral DNA polymerase

Clinical use:
HSV & VZV

Adverse effects:
1) Obstructive crystalline nephropathy
2) Acute kidney injury (hydrate!)

Resistance:
Mutated thymidine kinase

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14
Q

MOA:
Guanosine analogs that are phosphorylated by HSV/VZV thymidine kinase to inhibit viral DNA polymerase

Clinical use:
HSV & VZV

Adverse effects:
1) Obstructive crystalline nephropathy
2) Acute kidney injury (hydrate!)

Resistance:
Mutated thymidine kinase

A

Acyclovir, Famciclovir, Valacyclovir

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15
Q

Ganciclovir

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

MOA:
Guanosine analog that is formed by CMV kinase to inhibit viral DNA polymerase to prevent viral replication

Clinical uses:
CMV (HIV/AIDS)

Adverse effects:
1) Bone marrow suppression (leukopenia, neutropenia, thrombocytopenia)
2) Nephrotoxicity

Resistance:
Mutated CMV viral kinase

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16
Q

MOA:
Guanosine analog that is formed by CMV kinase to inhibit viral DNA polymerase to prevent viral replication

Clinical uses:
CMV (HIV/AIDS)

Adverse effects:
1) Bone marrow suppression (leukopenia, neutropenia, thrombocytopenia)
2) Nephrotoxicity

Resistance:
Mutated CMV viral kinase

A

Ganciclovir

17
Q

What is the second option if a patient with CMV is resistant to ganciclovir?

A

Use Valganciclovir

18
Q

Foscarnet

MOA:

Clinical uses:

Adverse effects:

Resistance:

A

MOA:
Viral DNA/RNA polymerase inhibitor & HIV reverse transcriptase inhibitor that binds the pyrophosphate site to activate
(does NOT need kinases to be activated)

Clinical uses:
CMV retinitis (in HIV/AIDS)
Acyclovir-resistant HSV

Adverse effects:
1) Nephrotoxicity
2) Electrolyte abnormalities
3) Seizures
4) Genital ulcers

Resistance:
Mutated DNA polymerase

19
Q

MOA:
Viral DNA/RNA polymerase inhibitor & HIV reverse transcriptase inhibitor that binds the pyrophosphate site to activate
(does NOT need kinases to be activated)

Clinical uses:
CMV retinitis (in HIV/AIDS)
Acyclovir-resistant HSV

Adverse effects:
1) Nephrotoxicity
2) Electrolyte abnormalities
3) Seizures
4) Genital ulcers

Resistance:
Mutated DNA polymerase

A

Foscarnet

20
Q

Cidofovir

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Inhibits viral DNA polymerase (No viral kinases to activate it)

Clinical uses:
CMV retinitis (HIV/AIDS)
Acyclovir resistant HSV

Adverse effects:
Nephrotoxicity (give with probenecid & IV saline to reduce toxicity)

21
Q

MOA:
Inhibits viral DNA polymerase (No viral kinases to activate it)

Clinical uses:
CMV retinitis (HIV/AIDS)
Acyclovir resistant HSV

Adverse effects:
Nephrotoxicity (give with probenecid & IV saline to reduce toxicity)

A

Cidofovir

22
Q

NRTI’s

MOA:

Clinical uses:

Adverse effects:

“SEAL The DealZ”

A

Abacavir (ABC)
Emtricitabine (FTC)
Lamivudine (3TC)
Tenofovir (TDF) - nucleoTide
Zidovudine (ZDV)
Didanosine
Stavudine

MOA: HIV therapy (Nucleoside reverse transcriptase inhibitors)

Competitively inhibits nucleotide binding to reverse transcriptase & terminate DNA chain elongation (because they lack 3’‘OH)

Clinical uses:
HIV 1/2 therapy (HAART)
ZIDOVUDINE - safe to use in preggos

Adverse effects:
1) Bone marrow suppression
2) Peripheral neuropathy
3) Lactic acidosis (nucleoSides)
4) Anemia (zidovudine)
5) Hypersensitivity in people with HLA-B57 (abacavir)
6) Pancreatitis (Didanosine)

23
Q

Abacavir (ABC)
Emtricitabine (FTC)
Lamivudine (3TC)
Tenofovir (TDF) - nucleoTide
Zidovudine (ZDV)
Didanosine
Stavudine

MOA: HIV therapy (Nucleoside reverse transcriptase inhibitors)

Competitively inhibits nucleotide binding to reverse transcriptase & terminate DNA chain elongation (because they lack 3’‘OH)

Clinical uses:
HIV 1/2 therapy (HAART)
ZIDOVUDINE - safe to use in preggos

Adverse effects:
1) Bone marrow suppression
2) Peripheral neuropathy
3) Lactic acidosis (nucleoSides)
4) Anemia (zidovudine)
5) Hypersensitivity in people with HLA-B57 (abacavir)
6) Pancreatitis (Didanosine)

A

NRTI’s

24
Q

NNRTI’s

MOA:

Clinical uses:

Adverse effects:

A

Delavirdine
Efavirenz
Nevirapine

MOA: HIV 1 therapy (Non-nucleoside reverse transcriptase inhibitors)

Non-competitively binds HIV reverse transcriptase to inhibit viral DNA synthesis (does NOT need phosphorylation)

Clinical uses:
HIV 1

Adverse effects:
1) Rash (risk of SJS & toxic epidermal necrolysis)
2) Hepatotoxicity
3) Vivid dreams (Efavirenz)
4) Teratogenic

25
Q

Delavirdine
Efavirenz
Nevirapine

MOA: HIV 1 therapy (Non-nucleoside reverse transcriptase inhibitors)

Non-competitively binds HIV reverse transcriptase to inhibit viral DNA synthesis (does NOT need phosphorylation)

Clinical uses:
HIV 1

Adverse effects:
1) Rash (risk of SJS & toxic epidermal necrolysis)
2) Hepatotoxicity
3) Vivid dreams (Efavirenz)
4) Teratogenic

A

NNRTI’s

26
Q

Integrase inhibitors

MOA:

Clinical uses:

Adverse effects:

A

Bictegravir
Dolutegravir
Elvitegravir
Raltegravir

MOA:
Inhibits HIV genome integration into host cells chromosomes

Clinical uses:
HIV 1& 2 therapy (HAART)

Adverse effects:
1) Myosis/Myopathy (Elevated CK)

27
Q

Bictegravir
Dolutegravir
Elvitegravir
Raltegravir

MOA:
Inhibits HIV genome integration into host cells chromosomes

Clinical uses:
HIV 1& 2 therapy (HAART)

Adverse effects:
1) Myosis/Myopathy (Elevated CK)

A

Integrase inhibitors

28
Q

Protease Inhibitors

MOA:

Clinical uses:

Adverse effects:

A

Atazanavir
Darunavir
Lopinavir
Ritonavir

MOA:
Inhibit HIV-1 protease (pol gene) to prevent maturation of new viruses

Clinical uses:
HIV 1 & 2 therapy (HAART)

Adverse effects:
1) Hyperglycemia
2) GI upset
3) Lipodystrophy (Cushing’s like disease)
4) Inhibits CYP450 (Ritonavir)
5) Renal toxicity/Hematuria/Nephropathy/Thrombocytopenia (Indinavir)

AVOID Rifampin!

29
Q

Atazanavir
Darunavir
Lopinavir
Ritonavir

MOA:
Inhibit HIV-1 protease (pol gene) to prevent maturation of new viruses

Clinical uses:
HIV 1 & 2 therapy (HAART)

Adverse effects:
1) Hyperglycemia
2) GI upset
3) Lipodystrophy (Cushing’s like disease)
4) Inhibits CYP450 (Ritonavir)
5) Renal toxicity/Hematuria/Nephropathy/Thrombocytopenia (Indinavir)

AVOID Rifampin!

A

Protease Inhibitors

30
Q

Enfuvirtide

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Binds gp41 on the HIV envelope to inhibit fusion/entry

Clinical use:
HIV 1 therapy

Adverse effects:
1) Skin reaction at injection sites
2) Peripheral neuropathy

31
Q

MOA:
Binds gp41 on the HIV envelope to inhibit fusion/entry

Clinical use:
HIV 1 therapy

Adverse effects:
1) Skin reaction at injection sites
2) Peripheral neuropathy

A

Enfuvirtide

32
Q

Maraviroc

MOA:

Clinical uses:

Adverse effects:

A

MOA:
Binds CCR-5 on T cell/macrophages surfaces to prevent HIV envelop protein gp120 from docking/entry

Clinical use:
HIV 1 & 2 therapy

Adverse effect:
Hepatotoxicity

33
Q

MOA:
Binds CCR-5 on T cell/macrophages surfaces to prevent HIV envelop protein gp120 from docking/entry

Clinical use:
HIV 1 & 2 therapy

Adverse effect:
Hepatotoxicity

A

Maraviroc