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36 Cards in this Set

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HIV drugs

What are the three major adverse effects of nucleoside analogs?
Nucleoside analogs:
1.lactic acidosis
2. pancreatitis
3. hepatic failure
HIV drugs

Six major nucleoside analogs:
NA "SAD TZ"

1. Stavudine: peripheral neuropathy, pancreatitis, lipodystrophy, preg C

2. Abacavir: fatal hypersensitivity reactions (never be rechallenged), pregC

3. Didanosine: peripheral neuoropathy, pancreatitis, take on empty stomach, preg B

4. Tenofovir: renal dysfunction, preg B

5. Zidovudine: headache, anemia (high MCV), neutropenia, take every 12 hrs, preg C
HIV drugs

What are the three non-nucleoside analogs?
NNRTI's

1. Efavirenz: 1st choice, CNS (insomnia, confusion, abnL dreams), take on an empty stomach, PREG D!!

2. Nevirapine: rash (very bad), hepatoxicity (necrosis), preg C (best of NNRTI's)

3. Atriplia: first drug that is triple therapy, preg D
HIV drugs
VIP

What four drugs have the least mitochondrial toxicity?
"TEAL" - nucleoside analogs

1. Tenofovin
2. Emtricitabin
3. Abacavir
4. Lamivudine
HIV drugs

Six major protease inhibitors (not including combo)?
PI's "FIN DAR"

1. Fosamprenavir: rash, increase lipids, increase LFT's
2. Indinavir: nephrothilasis (must drink alot of water), take every 8 hrs on empty stomach, increase LFT's
3. Nefinavir: (we don't boost) diarrhea, increase LFT, take with food

4. Darunavir: rash with sulfa moiety, take with ritonavir, only for treatment experienced
5. Atazanavir: indirect hyperbilirubinemia, prolonged PR interval, causes less lipid problems (give to those with high lipids)
6. Ritonavir: paresthesias, increase LFT's, drug interactions, it is a booster, take with food.
HIV drugs

What three drugs cause a rash?
1. Nevirapine (NNRTI)
2. Darunavir - sulfa moiety (PI)
3. Fosamprenavir (PI)
HIV drugs

What PI's are combined? (4 sets)
Set 1
Lopinavir + Ritonavir (no side effects other than increase LFT)

Set 2
Darunavir (rash/sulfa) + Ritonavir (paresthesias/drug interactions)

Set 3:
Saquinavir + Ritonavir

Set 4:
Tipranavir (tx experienced) + Ritonavir
HIV drugs

What drugs must you take on an empty stomach?
1. Indinavir (PI) - nephrolithiasis
2. Didanosine (NRTI) - periphreal neuropathy, pancreatitis

3. Efavirenz (NNRTI): CNS, abnL dreams, teratogenic
HIV drugs

What is the one fusion inhibitor?
Fusion inhibitor:

Enfuviritide: given subQ

Causes local injection site reactions (pain, erythema, induration)

Preg B
HIV drugs

Do any HIV drugs help the CD4 cells already infected?
NO!
HIV drugs

Do any of the NNRTI's require dosage adjustments in renal insufficiency?
NO (but Atripla should not be used in patients with a CrCl < 50ml/min
HIV drugs

What drugs are contraindicated when using Efavirenz?
Midazolam and triazolam
HIV drugs

Why does Nevirapine interact with other drugs?
Nevirapine (NNRTI - rash and hepatox)
Because it induces metabolism of other drugs
HIV drugs

What does Delavirdine do to other drugs?
It inhibits drug metabolism
HIV drugs

What does Efavirenz do to other drugs?
Efavirenz (NNRT - first choice, CNS and abnl dreams, teratogenic)
It can either promote or inhibit the metabolism of other drugs
HIV drugs

If a patient is on Rifampin along with either Nevirapine, Delaviridine, or Efavirenz - how must you change the drug concentrations? Why?
Rifampin induces p450 (decrease the drug available) -

Have to increase the dose all all three HIV medications
HIV drugs

What two drugs does Zidovudine interact with?
Zidovudine (NRTI - anemia, neutropenia, headache)

Interacts with:
1. Co-trimoxazole (bactrum)
2. Ganciclovir (for CMV)
HIV drugs

What nine drugs does Didanosine interact with?
Didanosine (NRTI, take on an empty stomach, peripheral neuropathy, pancreatitis from mito tox)

Interacts with:
Pentamidine
Ethanol
Stavudine
Dapsone
Ketoconazole, Itraconazole
Quinolones
Atazanvir, indinavir
HIV drugs

What two drugs are contraindicated with the use of any PI?
Midazolam and triazolam
HIV drugs

Should you use Rifampin with protease inhibitors?
No, renders them inactive
HIV drugs

Do we use Simvastatin and Lovastatin to combat hyperlipidemia in patients on PI's?

What can you use instead?
NO - Simvastatin and Lovastatin are contraindicated.

Can use instead: Atorvastatin or Pravastatin.
HIV drugs

What is the preferred regimen of NNRTI's, PI's, and NRTI's?
NNRTI: Efavirenz

PI: Either atazanivir, fosamprenavir, or lopinavir (all boosted with RITONAVIR)

NRTI:
tenofovir/emtricitabine
-or-
zidovudine/lamivudine
HIV drugs
VIP

What are all protease inhibitors associated with? (4)
Protease inhibitors:
1. development of hyperglycemia
2. fat maldistribution
3. lipid abnormalities
4. increase in bleeding episodes in patients with hemophilia.
HIV drugs

Regardless of antepartum ART regimen, what drug is recommended during the intrapartum period and for the newborn?
Zidovudine
HIV drugs

What is the treatment goal in HIV-infected pregnant women?
To reduce the HIV viral load to <1,000 copies/mL and prevent the transmission of HIV from mother to child
HIV drugs

In HIV infected pregnant women, when should Zidovudine be initiated to mom? When to the newborn?
Start mom on Zidovudine (NRTI, anemia, neutropenia, headache) - 14-34 wks gestation (and during labor)

Newborn: begin 8-12hrs after birth for the first 6wks of life.
HIV drugs

In an HIV patient receiving ARTs when should CD4 count be measured?
Measure: 2-8wks after starting therapy

Then every 3-4 mths
HIV drugs

What do most experts agress is the goal of therapy?
To maintain the virus load below the limits of detection (<50-80 copies/mL)
HIV drugs

When changing drugs how do you do it?
Do not change a single drug or add a single drug.

Instead use at least 3 new drugs and preferably an entire new regimen.
HIV drugs

Compare HIV infection to AIDS:
HIV: patient with a CD4 count of >200 cells and no signs of opportunistic infections

AIDS: patient with a CD4 count of <200 OR with an opportunistic infection OR AIDS indicator conditions (regardless of CD4 counts)
HIV drugs

What CD4 count is associated with the development of opportunistic infections?
CD4 < 500
HIV drugs
VIP

What are the two surrogate markers that are used to determine the indications for antiretroviral treatment and are used to monitor effectiveness of therapy?
CD4 cell count
&
Plasma HIV viral load
HIV drugs

What are two types of inhibitors of reverse transcriptase and how to they work?
Inhibitors of Reverse Transcriptase:
1. Nucleoside analogs (NRTI) - interfere with reverse trans to prevent further builidng of proviral DNA from RNA (incorporate into DNA to terminate chain elongation)
*require dosage adjustment in renal insuff (except acyclovir)

2. Non-nucleoside analogs (NNRTIs) - act as false nucleotides and bind adjacent active sites of reverse transcriptase inducing conformational changes that inactivate the enzyme. (combined with NRI and do NOT require a dosage adjustment in renal insufficiency)
HIV drugs

What NNRT should not be used in patients with a CrCl < 50?
Atripla
HIV drugs

MOA of inhibitors of HIV protease?
MOA of Protease inhibitors:

HIV protease is needed for processing and assembly of viral core and polymerase proteins to produce infectious virions.

Protease inhibitors bind reversibly to the active site of the protease enzyme to prevent the protease enzyme from cleaving the viral precursor proteins into funcitonal units and thus block viral maturation.
They decrease infected cell pool by halting production of infectious virions.

Do not require dosage adjustments in renal dysfunction but can in liver dysfunction
HIV drugs

MOA of fusion inhibitors?
Fusion inhibitors prevent the entry of HIV into suseptible cells by inhibiting the fusion of viral and cellular mechanisms.

Efuviritide does not require dosage adjustment in the presence of renal insufficiency.