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Infectous Disease > Pharmacology of AntiRETROvirals Dr. Lewis EXAM 4 > Flashcards

Pharmacology of AntiRETROvirals Dr. Lewis EXAM 4 Flashcards

1
Q

What is PEPFAR?

A

Presidents Emergency Plan for AIDS Relief

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2
Q

What is the CD4 cell count associated with AIDS?

A

< 200 cells/mm3

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3
Q

What does the CD4 count and the viral load imply?

A

CD4 count: how close to the end

Viral load: how fast does the disease progress (you may have a decent amount of CD4 cells, but it can decrease rapidly with a high viral load)

-> The viral load is the best marker for treatment response

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4
Q

What are the steps during the infection of HIV?

A

Free virus
1. Attachment
2. Fusion
3. Reverse Transcription
4. Integration
5. Assembly
6. Maturation

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5
Q

What are the proteins on the surface of an HIV cell that bind to CD4 cells?

A

-Glycoprotein 120 (outside) and 41(integrated part)
-binding to CD4 receptor and CCR5 and CXCR4 Co-receptor on CD4 cells

-patients infected with CCR5-HIV receiving a bone marrow transplant with CXCR4 CD4 cells may be cured

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6
Q

What are the NRTIs used to treat HIV?

A

Abacavir (ABC), Ziagen®
Didanosine (ddI), Videx ®

Emtricitabine (FTC), Emtriva®
Lamivudine (3TC), Epivir ®

Tenofovir disoproxil fumarate (TDF), Viread®
Tenofovir alefenadamide Vemlidy® (TAF)

Zidovudine (AZT, ZDV), Retrovir (not used in practice; NAPLEX)

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7
Q

Class Side Effects of NRTIs

A

-Lactic acidosis, Hepatic steatosis (fatty liver)
-Pancreatitis and peripheral neuropathy with the “D” drugs: Didanosine (ddI), stavudine [d4T], and zalcitabine [ddC]

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8
Q

How are the NRTIs eliminated?

A

-All renally -> needs renal adjustment
-EXCEPT Abacavir !!!!

-Didanosine needs to be taken 30 min before or 2h after a meal (NOT on Exam but NAPLEX)

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9
Q

What are the cytosine analogs used to treat HIV?

A

Emtricitabine (FTC), Emtriva® (has a Flourid atom)
-> associated with skin hyperpigmentation
Lamivudine (3TC), Epivir ® (no Flourid atom)

-similar in structure -> interchangeable
both work for HBV
-these are newer agents and well-tolerated

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10
Q

Which side effect is associated with Emtricitabine (FTC), Emtriva®?

A

Skin hyperpigmentation

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11
Q

Which NRTI is a Guanine analog?

A

Abacavir
-check for HLA-B5701 -> allergic reaction (fatal rash) !!!

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12
Q

Which antiviral drug is the only nucleotide?

A

Tenofovir
-adenosine analog
-2 formulations (TAF, TDF)
-works for HBV

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13
Q

How is TAF different from TDF?

A

Tenofovir (TFV) by itself will not get absorbed (acidic GI?)
->TDF is the TFV salt and is protected from the acid but releases the active drug TFV in the plasma (too early) and causes TOXICITY

->TAF is a prodrug with a longer half-life allowing the drug to stay stable until it reaches the HIV target cell

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14
Q

DDIs and side effects of TDF

A

-it lowers the concentration of atazanavir, so atazanavir has to be boosted

ADE: renal insufficiency, proximal tubulopathy, Fanconi syndrome, bone toxicity

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15
Q

DDIs and side effects of TAF

A

DDI: rifampin/rifabutin (CYP inducer), St. Johns Wort, tipranavir

ADE: the toxicity caused by TDF was decreased, and higher lipid levels than TDF during the study

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16
Q

Which side effect is associated with Zidovudine?
NAPLEX

A

-bone marrow suppression
-need to monitor complete blood count (CBC)

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17
Q

What are the NNRTIs used to treat HIV?

A

Efavirenz (EFV), Sustiva® (lot of toxicity)
Nevirapine (NVP), Viramune® -> Hepatoxicity
(suggested by the mother-to-baby-transmission guidelines)

Newer agents:
Etravirine, Intelence®
Rilpivirine, Edurant® -> needs an acidic environment, low efficacy at high viral dose
Doravirine, Pifeltro®

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18
Q

How are NNRTIs different from NRTIs?

A

-No activation (phosphorylation) required
-they bind allosterically
-they don’t compete with other nucleosides or nucleotides (cross-reactivity only between NNRTIs)

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19
Q

Class ADE for NNRTIs

A

-Rash
-GI
-Hepatoxicity:
CD4 count-dependent hepatoxicity (fatal) for nevirapine

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20
Q

What are the side effects associated with Efavirenz (Sustiva)?

A

-has the lowest rash incidence
-but causes confusion, impaired concentration, and vivid dreams, can’t give it to pt with a psychiatric history -> concentration goes up with food -> issues with abuse bc of the hallucinogenic property

-CYP3A4 inducer and inhibitor, CYP2C19 inhibitor

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21
Q

Which patient population should Efavirenz be avoided?

A

Women in the first trimester of pregnancy

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22
Q

Which patient population is appropriate for using
Etravirine (Intelence®)?

A

for treatment-experienced patients

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23
Q

What to look out for when administering Rilpivirine, Edurant®?

A

-must be given with a high-fat meal
-low oral bioavailability with antiacids (need acidic environment)
-less effective with high viral load

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24
Q

DDIs of Doravirine (Pifeltro®)?

A

-Contraindicated with strong 3A4 inducers

-Carbamazepine, phenobarbital, phenytoin, Rifampin and rifapentine, St. John’s Wort

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25
Q

Important Protease Inhibitor

A

Often used:
Darunavir, Prezista®
Atazanavir, Reyataz®

Pregnancy:
Lopinavir/Ritonavir, Kaletra®
Fosamprenavir, Lexiva®

Indinavir, Crixivan® - drink with plenty of water (NAPLEX)

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26
Q

What are the Classe ADEs of Protease Inhibitors?

A

-Lipodystrophy
-Hyperlipidemia
-Hyperglycemia
-Bleeding in hemophiliacs (genetic bleeding disorder) -> NAPLEX

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27
Q

What to look out for in Protease Inhibitors?

A

-all should be taken with food bc N/V: EXCEPT Indinavir !!!

-monitor LFT and CBC
-monitor blood glucose and lipids (bc of hyperglycemia and hyperlipidemia)

-DDI with CYP3A4 drugs

28
Q

In which patient population is Darunavir used?

A

-mostly treatment-experienced patients and pt infected with a virus carrying a PI mutation
-> Give BID instead of once a day
->BOOST with Ritonavir

-can cause a rash (higher with sulfa allergy)
-take with food, and avoid statins

29
Q

What is important when administering Protease inhibitors?

A

They have to be boosted with Ritonavir or Cobicistat

30
Q

Which Protease Inhibitor is different from the other and WHY?

A

Atazanavir
ADE different:
less hyperlipidemia, less metabolic ADEs
cause prolonged PR intervals, hyperbilirubinemia (fake sign of liver dysfunction, ATZ replaces bilirubin from the binding site causing accumulation -> yellowing, but the liver is OK)

31
Q

A patient is treated with TDF and atazanavir,
what has te taken care of?

A

TDF decreases ATZ -> so ATZ needs to be boosted

32
Q

Considerations about Raltegravir

A

-Integrase inhibitor
-when given with rifampin (CYP inducer) -> higher dose
-don’t give with Al-Mg hydroxide antacids, carbamazepine, phenobarbital, phenytoin

-a low barrier for resistance

33
Q

Considerations for Elvitegravir
ELIVS needs a friend

A

-taken with Cobicistat
-Limited to CrCl > 70
-Cobicistat may inhibit SCr secretion

-take with food
-Do not give with inhaled steroids (except
beclomethasone)
-Low drug levels during pregnancy

34
Q

Considerations for Dolutegravir

A

-can be used for RAL and ELV-resistant strains
-potent at any CD4 count or viral load
-no food requirement

-Absorption reduced by polycovalent cations
-dont give with dofetilide (antiarrhythmic)
-pregnancy test before starting

35
Q

Considerations for Bictegravir

A

-Coformulated with emtricitabine/TAF
-May be useful in a majority of INSTI-mutations

-not used when CrCl is <30 ml/min
-give 2hr before antacids
-don’t use it with dofetilide (similar to dolutegravir)

36
Q

How is Cabotegravir used?

A

Cabotegravir Apretude®
-used with Rilpivirine (NNRTI) for HIV treatment
-used for PrEP w/o Rilpivirine
-IM injection once monthly or once every other month !!!

37
Q

1st Entry Inhibitor

A

-Maraviroc, Selzentry®
-only works with CCR5-tropic virus -> Trofile assay
-ORAL

38
Q

How is the MOA of Entry inhibitors different from Fusion inhibitors?

A

-Entry inhibitor blocks the CCR5 Co-receptor on the target CD4 cell

-Fusion inhibitor blocks the Glycoprotein gp41 on the virus’s outer membrane

39
Q

Considerations for Enfuvirtide, Fuzeon®

A

-Fusion inhibitor
-Reserve for last salvage therapy
-injection site reaction (injection site can be only used once)

40
Q

How does Ibalizumab (Trogarzo) work?

A

-an antibody blocking the CD4 receptor
-for heavily treatment-experienced patient
-IV every 14 days

41
Q

Fostemsavir (Rukobia)

A

-Film-coated, extended-release tablet, Oral
-used for treatment-experienced patients infected with MDR-virus
-MOA: binds to gp120 and prevents attachment
-ADEs: QTc prolongation, acute liver injury

42
Q

What is the function of Metabolism inhibitors?

A

Ritonavir and Cobisistat
-used to BOOST antiviral agents
-Ritonavir with antiviral activity -> could contribute to resistance

43
Q

Combiproduct: Genvoya

A

Elvitegravir / Cobicistat / Emtricitabine / TAF

44
Q

Which product contains:
Elvitegravir / Cobicistat / Emtricitabine / TDF

A

Stribild

45
Q

Which product contains:
Abacavir / Dolutegravir / Lamivudine

A

Triumeq

46
Q

Combiporduct: Descovy

A

– Emtricitabine / TAF

47
Q

Which product contains:
Emtricitabine / TDF

A

Truvada

48
Q

What does Cabenuva contain?

A

Cabotegravir / rilpivirine

49
Q

How is chronic Hepatitis B defined?

A
  • defined as persistence of HBsAg > 6
    months

-further: Further classified by “e” antigen (HBeAg) status AND by whether there is liver necroinflammation

50
Q

How is hepatitis B treated?

A

-used to be treated with Interferons and Pegylated interferons
-then NRTIs
-now combination therapies

51
Q

MOA of Interferons

A

Activates the Janus Kinase-Signal Transducer and the JAK-STAT pathway (inhibited in auto-immune diseases)

52
Q

What is the purpose of Pegylated Interferons?

A

prolongs the half-life -> so it can be given less frequently

53
Q

What are the side effects of Interferons?

A

-Flu-like symptoms:
N/V, chills, headaches, Malaise
-Bone marrow suppression
-Neuropsychiatric disturbance

54
Q

Which drug is active against Hep B and HIV
and should not be co-administered?

A

Entecavir (Baraclude)
-not for treatment of HIV unless other HIV drugs are on board -> bc if treated for HepB alone HIV can develop resistance
-more potent than lamivudine

-take on an empty stomach (2hr space before or after food), avoid fatty meals

55
Q

Entecavir is considered an alternative to which drug and to treat which disease?

A

-lamivudine (3TC) and tenofovir to treat only HepB

56
Q

Which drug can be used in lamivudine and entecavir-resistant strains?

A

-Adefovir (HEPSERA)
-Less potent than lamivudine

-ADEs at higher doses: Nephrotoxicity, Falconi syndrome !!!

57
Q

Which step of the infection is blocked by Neuraminidase?

A

The releasing step

-Neuraminidase cleaves off the sialic acid residue on the host cell -> the newly formed virus can be released
-Blocking neuraminidase will result in failed budding of the virus

58
Q

Which steps are blocked by amantadine and rimantadine?

A

The viral uncoating step

59
Q

What are the side effects of Oseltamivir?

A

-rare cases of SJS and neuropsychiatric effects (personality change)
-requires renal adjustment

60
Q

Formulation of Anti-Influenza drugs

A

Osletamvir: Oral
Zanamivir: Inhaled
Peramivir: IV

61
Q

ADE of Zanamivir

A

Bronchospasm

works against mild Influenza A and B, and some avian influenza

62
Q

Peramivir

A

-given IV
-only FDA-approved for uncomplicated Influenza A/B
-20h half-life, single dose
-ADEs: Seizures, anticholinergic

63
Q
A
63
Q

What is Amantadine actually approved for

A

Anticholinergic
Class side effects: Seizueres, CNS, edema, anticholinergic (can’t see, can’t pee, can’t spit, can’t swallow)

Amantadine (SYMMETREL)
Rimantadine (FLUMADINE)
prevent uncoating of the virus

64
Q

Baloxavir (Xofluza)

A

First-in-class polymerase acidic (PA) endonuclease inhibitor
-viral RNA polymerase complex for viral transcription
-may have activity against oseltamivir-resistant strains

Infectous Disease (29 decks)

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