HIV Medications: Antiretroviral Therapy Flashcards
- CD4 count should usually be:
- Name the opportunistic IFX and medication for Px with Landmark CD4 counts of:
-usually around 1000 cells/mm3
-
Name the categories of antiviral therapy (6).
- CCR5 antagonist
- fusion inhibitors
- NNRTI’s
- NRTI’s
- Integrase inhibitors
- Protease inhibitors
Atripla (three drugs tripled)
- combination
- interesting side effects
- regimen
- efavirenz, emtricitabine, tenofovir
- efavirenz causes night terror, CNS
- MID, empty stomach
Complera
- combination (3)
- contraindication (think of starting a new pt on therapy)
- rilpivirine*, emtricitabine, tenofovir
* not as effective with viral load over 100K, which many pts present with. Starts with Atripla
Stribild
- combination (*quad pill)
- interesting caveat
- elvitegravir, cobicstat, emtricitabine, tenofovir
* used for treatment naive patients (must be the first drug we use)
Combivir
- combination
- regmien
- lamivudine, zidovudine
- BID
Cobicistat (Tybost)
- how is this drug used?
- which CYP does it inhibit?
- which drugs does it potentiate?
- Boosts (Ty-boost) the activity of other drugs, part of the quad pill
- CYP3A
- enhances the effect of atazanavir or darunavir
Maraviroc (Selzentry)
- MOA
- indication
- adverse effects
- binds CCR5 receptor of CD4 cell (cell’s entry)
- restricted to HIV pts infected with CCR5 (M tropic) virus
- rash, ab pain, URIs, dizziness, MSK sxs
Enfuvirtide (Fuzeon)
- administration
- hallmark side effects
- MOA, what exactly does it bind to?
- subQ injection
- localized nodules at injection sites
- usually second or third line because of this
- Inhibits fusion by binding to BR1 in the gp41 subunit of the envelope glycoprotein
NNRTI’s
-name the drugs (there are 5)
- Delavirdine
- Efavirenz
- Etravirine
- Nevirapine
- Rilpivirine
NNRTI’s
- MOA
- Side Effects
- SJS highest incidence with which drug?
- which drug causes neuropsychiatric sxs?
- viral mechanism of resistance (think about stopping therapy)
- how to avoid resistance
- directly bind to reverse transcriptase
- RASH, transaminases
- SJS highest incidence with Nevirapine
- neuropsychiatric sxs with Efavirenz
- non-compliance leads to exclusive stay in the system because of their land half lives, this allows the virus to gain resistance to essentially a monotherapy
- use in combination
Name the NRTI’s (there are 7 of them)
-Most of these are nucleosides. Which is a nucleoTide?
- Abacavir
- Didanosine
- Emtricitabine
- Lamivudine
- Stavudine
- Tenofovir
- Zidovudine
- T-enofovir
Hallmark Side Effects for:
- Abacavir
- Didanosine
- Stavudine
- Zidovudine
- Abacavir causes hypersensitivity! Pre-screen the pt for HLA-b*5701
- Didanosine can cause peripheral neuropathy MI pancreatitis
- Stavudine also causes peripheral neuropathy
- myelosuppression, lipoatrophy and myopathy
Tenofovir
- What sets this guy apart from the rest of the NRTI’s
- adverse reactions (3)
- It is a nucleotide, so it has a slightly different mechanism
- lactic acidosis, decrease bone density, exacerbation of hepatitis
Integrase Inhibitors
- Members
- MOA
- Inidication
- Raltegravir, Elvitegravir, Dolutegravir
- no integration to host DNA
- anybody
Protease Inhibitors:
- MOA
- Which is “the booster of all booster?”
- hallmark side effects (endocrine type)
- indinavir special side effect
- inhibit HIV-1 protease
- Ritonavir, allows a lower pill burden
- hyperlipidemia, fat maldistribution, insulin resistance, osteonecrosis
- nephrolithiasis, increased SCR, pyuria, hydronephrosis
Post-exposure Px
-name 2
- raltegravir
- Truvada
PrEP
-Truvada
After starting therapy, how is the viral load used to monitor?
-The viral load is taken regularly and should be steadily decreasing.
Antiretroviral therapy is recommended for:
-pts. with a history of _____
-Which types of women?
-Persons with which type of infections?
There are different levels of recommendation depending on the pts CD4 count. (i.e. CD4 count 500
-AIDS defining illnesses
-Pregnant women
-Hepatitis B co-infection
CD4 500=Level BIII
Nevirapine has special considerations for females with CD4>250 and Males>400. Why?
-how do you decrease the side effects?
- Nevirapine causes severe liver toxicity, which outweighs the benefit unless the pt has lower numbers than these.
- two week dose escalation
Name the other booster beside Tybost.
Ritonavir
NRTIS: -MOA -Don't forget that these have a variable metabolism and renal excretion. Which of the following have an AUC effected by food? -Abacavir -Didanosine -Lamivudine -Zidovudine
- MOA: look like RNA and DNA nucleosides, get phosphorylated in the cell and incorporate into the chain to block reverse transcriptase
- Food effects: Didanosine and Zidovudine
Efavirenz
- class
- side effects
- NNRTI
- night terrors and teratogen