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Pharmacology II > Exam 3: Antivirals > Flashcards

Exam 3: Antivirals Flashcards

1
Q

Describe the mechanisms of Antivirals

A
  1. Alter uncaring of virus
    • virus uncoats to begin replication
    • drugs prohibit this phase, so cannot penetrate host
  2. Polymerase inhibitors
  3. Inhibit viral protein synthesis
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2
Q

What antiviral drugs are indicated for Influenza A?

A

amantadine (Symmetril)

rimantidine (Flumadine)

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3
Q

Mechanism of amantadine and rimantidine

A

Blocks uncaring of virus preventing penetration into host

- rimantidine is significantly more active than amantadine

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4
Q

Side effects of amantadine and rimantidine

A
  1. CNS stimulation
    • enhanced by antihistamines and caffeine
  2. Insomnia
  3. Grand Mal Seizures
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5
Q

Indications for Tamiflu

A

Influenza A or B

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6
Q

What drug is considered the classic prodrug?

A

Tamiflu

- hydrolyzed to active form

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7
Q

Action of Tamiflu

A

Neuraminidase inhibitor
- drug is an enzyme inhibitor that cleaves the budding viral progeny from its cellular envelope attachment point just prior to release

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8
Q

Indications for ribavirin (Rebetol, Virazole)

A

Treatment of respiratory syncytial virus

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9
Q

Mechanism of ribavirin

A

prevents synthesis of viral proteins encoded by viral mRNA

  • inhibits virus RNA polymerase
  • Disrupts transcription, translation or promotes degradation of viral RNA
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10
Q

Side effects of ribavirin

A

mutagenic
teratogenic
carcinogenic

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11
Q

Indications for trifluridine (Viroptic)

A

herpes simplex keratitis (in eye)

keratoconjunctivitis

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12
Q

Mechanism of trifluridine

A

interferes with viral replication by incorporating into viral DNA in place of thymidine, causing formation of defective proteins

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13
Q

What is the IV drug of choice for HSV encephalitis?

A

acyclovir (Zovirax)

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14
Q

Action of acyclovir (Zovirax)

A

Inhibits viral DNA polymerase preferentially (Cell cycle specific)

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15
Q

Indications for acyclovir

A

IV drug of choice for HSV encephalitis

- primary and recurrent herpes in immunocompromised patients

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16
Q

How often does acyclovir need to be used?

A

Every 3 hours, which is consistent with cycle phases of viruses

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17
Q

Indication of ganciclovir (Cytovene)

A 
human cytomegalovirus (CMV)
- treats CMV retinitis
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18
Q

Action of ganciclovir (Cytosine)

A

inhibits viral DNA synthesis

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19
Q

Which drugs are indicated to treat recurrent genital herpes

A

famciclovir and valacyclovir

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20
Q

T or F, famciclovir and valacyclovir are classic prodrugs

A

true

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21
Q

What are interferons?

A

a family of naturally occurring, inducible glycoproteins that interfere with the ability of viruses to infect cells
- antiviral, cytotoxic, immunomodulatory actions

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22
Q

3 types of interferons?

A

alpha
beta
gamma

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23
Q

How are interferons administered?

A

intralesionally
subcutaneously
IV

24
Q

Mechanism of Interferons

A

Not completely understood…
- Induction of host cell enzymes that inhibit viral RNA translation, ultimately leading to the degradation of viral mRNA and tRNA

25
Most common indications of Inteferons
Hepatitis B and C Multiple Sclerosis - Also used for some cancers
26
Adverse effects of Inteferons
1. Flu-like symptoms 2. bone marrow suppression 3. neurotoxicity 4. CNS effects 5. Severe fatigue 6. Severe weight loss 7. Autoimmune disorders 8. Cardiovascular 9. Oral
27
Name the new drugs for Hepatitis C
1. ledipasvir + sofosbuvir (Harvoni) 2. simeprevir (Olysio) 3. sofosbuvir (Sovaldi) 4. boceprevir (Victrelis) 5. telaprevir (Incivek)
28
What is the challenge with antiretrovirals
To kill the virus, host cells are often harmed | - Antivirals that alter viral replication processes are often toxic to host cells
29
Explain the mechanism of Antiretrovirals
- Inhibiting viral attachment and entry limits spread of virus within body - Alter genome replication = polymerase inhibitors - Immunization = provides antibodies against viral envelop proteins
30
Name the drug that was the first antiviral HIV agent that inhibits viral entry into host cells
enfuvirtide (Fuzeon)
31
Target of antiretrovirals for Retrovirsuses?
``` Reverse transcriptase (1st class to be used) - main enzyme used by virus to copy genome into DNA ```
32
3 primary classes of Antiretroviral drugs for HIV
1. Nucleoside reverse transcriptase inhibitors 2. Protease inhibitors 3. Nonnucleoside reverse transcriptase inhibitors
33
What are the drug concepts for HIV?
- Drugs target structural and functional differences between viral and human proteins - Treatment of HIV infection requires combination therapy = HAART (Highly Active AntiRetroviral Therapy) - "cocktails"
34
Define a typical cocktail
all of the primary classes of antiretroviral drugs 1. nucleoside reverse transcriptase inhibitor 2. non-nucleoside reverse transcriptase 3. protease inhibitors
35
When are antiretrovirals started in a patient?
when immunosuppression becomes pronounced | - CD4
36
What is a Triple Cocktail?
2 nucleoside reverse transcriptase inhibitors | 1 Protease inhibitor
37
Side effects of Antiretrovirals
1. Anemia (toxic to bone marrow and blood cells) 2. Leukopenia and granulocytopenia 3. Hepatotoxicity 4. Peripheral neuropathy 5. Pancreatitis
38
T or F, Nucleoside Reverse transcriptase inhibitors are not classified as prodrugs
False, | Must be biotransformed/bioactivated to work
39
Action of Nucleoside Reverse transcriptase inhibitors
Drug is integrated into DNA polymerase so that synthesis of viral DNA is terminated - Inhibits viral enzyme reverse transcriptase - ****Drugs have no effect on cells already containing HIV
40
T or F, Reverse transcriptase of HIV is 1100 times less susceptible to inhibition than are normal human cells making them harder to target
False, | 1100 times more susceptible
41
List the Nucleoside reverse transcriptase inhibitors
``` abacavir (Ziagen) (B) didanosine (Videx) emtricitabine (Emtriva) lamivudine (Epivir) stavudine (Zerit) zalcitabine (Hivid) (B) zidovudine (Retrovir) = AZT ```
42
Action of AZT
Inhibits HIV synthesis and reduces morbidity/mortality from AIDS and AIDS-related complex
43
Side effects of AZT
1. Very toxic = bone marrow depression 2. CNS effects 3. Nausea 4. Oral effects = altered taste, tongue edema, bleeding gingiva
44
What drugs have interactions that inhibit metabolism of AZT
NSAIDS | Aspirin
45
List the Non-nucleoside reverse transcriptase inhibitors
delavirdine (Rescriptor) efavirenz (Sustiva) etravirine (Intelence) nevirapine (Viramune)
46
Action of Non-nucleoside reverse transcriptase inhibitors
block reverse transcriptase | - Drugs inhibit the catalytic reaction of reverse transcriptase that is independent of nucleotide binding
47
T or F, Non-nucleoside reverse transcriptase inhibitors are classified as prodrugs
false, Do not require bioactivation
48
Action of Protease Inhibitors
Drugs suppress viral replication by inhibiting protease, the enzyme responsible for cleaving viral precursor peptides into infective virions - Prevents maturation of HIV-infected cells
49
What is the primary difference of protease inhibitors vs the other 2 classes of antiretrovirals
Interfere with the action of HIV-infected cells
50
List the Protease inhibitors
``` atazanavir (Reyataz) darunavir (Prezista) fosamprenavir (Lexiva) (B) indinavir (Crixivan) (B) nelfinavir (Viracept) ritonavir (Norvit) (B) saquinavir (Invirase) tipranavir (Aptivus) ```
51
Action of Nucleotide Reverse transcriptase inhibitors
Interferes with HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication
52
Name the Nucleotide Reverse Transcriptase inhibitor drug
tenofovir (Viread)
53
Action of Integrase Inhibitors
Inhibits integrase, the enzyme that helps to insert the viral cDNA strand produced by reverse transcriptase into the human genome - prevents integration of proviral gene into human DNA
54
Name the Integrase Inhibitor drugs
raltegravir (Isentress) | dolutegravir (Tivicay)
55
What is complera
A NEW combination drug used for initial treatment of HIV-infected individuals
56
Complera contains what 3 medications
emtricitabine rilpivirine tenofovir disoproxil fumarate

Pharmacology II (24 decks)

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