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Unit 6 Pharm - MEEE > Antivirals I > Flashcards

Antivirals I Flashcards

1
Q

What are the five different classes of anti-retroviral therapy?

A
  1. Nucleoside Reverse Transcriptase Inhibitors (NRTI’s)
    • –Nucleotide RTI’s (tenofovir)
  2. Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI’s)
  3. Protease Inhibitors (PI’s)
  4. Entry Inhibitors: enfuvirtide; CCR5 antagonists
  5. Integrase Inhibitors
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2
Q

NRTIs include

A

Lamivudine = Emtricitabine

Tenofovir

Abacavir

Zivovudine (AZT)

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3
Q

Truvada is a combination of which two NRTIs

A

Tenofovir/Emcitrabine

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4
Q

Epzicom is a combination of which two NRTIs

A

Abacavir/Lamivudine

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5
Q

MOA of NRTIs

A

They act as DNA analogs that inhibit reverse transcriptase leading to viral chain termination

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6
Q

What are the side effects of Tenofovir?

A

Nephrotoxicity—Fanconi Syndrome

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7
Q

What are the side effects of Abacavir?

A

hypersensitivity reaction - send for HLA test first

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8
Q

What are the side effects of Lamivudine/emtricitabine?

A

very few side effects

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9
Q

What are the side effects of Zidovudine

A

anemia - not used anymore for long term use

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10
Q

What are the side effects of the NRTIs as a class?

A

lactic acidosis and GI upset

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11
Q

Which drugs are the Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)?

A

Efavirenz, EFV
Nevirapine, NVP
Rilpivirine, RPV
Etravirine

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12
Q

MOA of NNRTIs?

A

bind directly to the reverse transcriptase enzyme and causing direct enzyme inhibition

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13
Q

What are the common side effects of Efavirenz?

A

CNS symptoms!!
**vivid dreams
-drowsiness
Teratogenic

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14
Q

What are the common side effects of Nevirapine?

A

Rash

Hepatits including hepatic necrosis!!

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15
Q

What are the common side effects of Etravirine?

A

Rash

Increased LFT’s

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16
Q

What are the common side effects of Rilpivirine?

A

Rash

QT prolongation

17
Q 
Which drugs belong to the class of Protease Inhibitors?
"Navir tease a pro!"
A 
Ritonavir, RTV
Fosamprenavir, fAPV
Lopinavir/ritonavir, KAL
Atazanavir,  ATZ
Darunavir
18
Q

MOA of PI

A

Bind within active pocket of protease, causing conformational change inhibiting binding of virus. Without protease cleavage, virus cannot cleave protein chains and cause infection!

19
Q

Protease Inhibitors and Ritonavir Boosting

A

Mechanism P4503A4 inhibition in the liver and gut
Inhibition of P-glycoprotein transport
—So Ritonavir at low doses enhances blood levels of other PI’s when given together
—patients don’t have to take drugs as often
*Usually Lopinavir/Ritonavir known as Kaletra

20
Q

What are the adverse effects of PIs as a class?

A
  1. N/V/D
2. Metabolic Toxicities
Dyslipidemia
Hyperglycemia
Lipodystrophy
*Pt. predisposed to diabetes
21
Q

Which drug is considered an viral entry inhibitor?

A

Enfuvirtide/Maravaroc - it is given by Injection

a salvage drug when you have no other choice

22
Q

CCR5 Antagonists targets a receptor in humans and it is the only drug called?

A

Maravaroc - it inhibits the co-receptor on the humans from allowing the virus to gain entry into the CD4 T-cell

23
Q

Adverse effects of CCR5 Antagonists include

A

Hepatotoxicity – appears to be rare

Common: cough, fever, upper respiratory infections, rash, musculoskeletal symptoms, abdominal pain, and dizziness

24
Q

HIV-Integrase Inhibitors MOA

A

Inhibit viral integrase necessary for insertion of viral DNA into human genomic DNA

25
Q

Drugs in the Integrase Inhibitor class

A

Raltegravir
Elvitegravir
Dolutegravir

26
Q

Adverse side effects of Integrase Inhibitors?

A

Myopathy and rhabdomyolysis, elevated CK
Generally few adverse effects

Common: nausea, headache, diarrhea, pyrexia

27
Q

HAART Therapy uses 3 HIV agents from two different classes

A

the cocktail includes:
2 NRTIs + PI (± ritonavir boosting)

2 NRTIs + NNRTI

2 NRTIs + Integrase Inhibitor

28
Q

Resistance to HAART

A

Very important
Can quickly limit treatment options

Once resistance has develop to an antiretroviral agent it is permanent

Cross-resistance can occur within antiretroviral classes

Directly associated with adherence and attainment of virologic goals

Unit 6 Pharm - MEEE (12 decks)

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