Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm I Final Review > Antiretroviral Drugs > Flashcards

Antiretroviral Drugs Flashcards

1
Q

Common opportunistic pathogens in HIV

A 
TB
CMV
Candidiasis
Cryptococcal meningitis
Toxoplasmosis
Cryptosporidiosis
Karposi’s sarcoma
Lymphoma
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

The four main classes of HIV drugs

A

Reverse transcriptase inhibitors (Nucleoside and Non-nucleoside)
Protease Inhibitors
Fusion Inhibitors
Integrate Inhibitors

Combinations decrease viral load and produce remission in some patients.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Goals for HIV treatment

A

Maintain a low viral load and a CD4+ count >200

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

A 
Zidovudine (AZT) - the first to be developed
First choice combo:
Emtricitabine
Tenofovir
Alternative combo:
Lamivudine
Abacavir
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

MOA for NRTIs

A

Nucleoside analogue, requires phosphorylation x3 (by HOST, not virus)
Incorporated into DNA, inhibits viral reverse transcriptase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Zidovudine (Retrovir,AZT)

A

Thymidine analogue
Oral, short acting (5x/day)
Good CNS penetration - useful for AIDS dementia
SAFE in pregnancy - decreases risk of transmission

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Zidovudine toxicity

A

Initial: CNS (HA, etc)
Lactic acidosis and hepatotoxicity (common for the class)
Myelosuppression (neutropenia, anemia)
• Use caution when BM compromised or combined with other myelosuppression game drugs
• Counteract with Epogen (RBC) or Neupogen (WBC)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

First line combo for HIV

A

Tenofovir and Emtricitabine
NRTIs
Major side effect = Flatulence (extreme)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Lamivudine

A

Cytosine analogue NRTI
Also inhibits Hep B polymerase (good combo for HepB coinfection - or as a HepB monotherapy)
Very well tolerated, SAFE in pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Huge caution for Abacavir (a NRTI)

A

Must screen for HLA-B-5701 —> hypersensitivity!!!

If they have rxn, must discontinue. NEVER restart —> Fatal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

General rule for NRTI side effects

A

Lactic acidosis and hepatotoxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

MOA for Non-Nucleotide Reverse Transcriptase Inhibitors

A

Bind DIRECTLY to inhibit viral reverse transcriptase. Do not require phosphorylation for activity
GREAT in combo with NRTIs because inhibiting at different points.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

First choice NNRTI

A

Efavirenz IF not pregnant! (Very teratogenic - category X)

Alt in pregnancy = Rilpivirine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Protease Inhibitors

A 
DarunAVIR
AtazanAVIR
RitonAVIR
SaquinAVIR
LopinAVIR
IndinAVIR
TipranAVIR

(Don’t try to add “abacavir” to this group)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

MOA for Protease Inhibitors

A

Bind to proteases (duh)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Common pharmacokinetics for protease inhibitors

A

Never use alone - always in combo with NRTIs
Metabolized by CYP3A4 - so can’t combine them with Inducers of of CYP3A4 like RIFAMPIN
• If treating for coinfection of TB, choose Isoniazid instead

17
Q

Why to be cautious with St. John’s Wort

A

Increases metabolism of protease inhibitors

18
Q

Common toxicities for Protease Inhibitors

A

Altered body fat distribution (buffalo hump, truncates obesity, and facial atrophy)
Insulin resistance —> hyperglycemia
Increases in serum cholesterol but DO NOT combine with statins!
Spontaneous bleeding in patients with hemophilia A or B

19
Q

Why is Ritonavir special amongst the protease inhibitors?

A

INHIBITS CYP3A4 - don’t relay on it as a solo PI, but give as a BOOST to protect other PIs from CYP metabolism
DO NOT combine it with saquinavir - QT
Contains ethanol, so don’t give it with metronidazole or cephalosporins

20
Q

DarunAVIR

A

DOC amongst the protease inhibitors

Can’t be given in patients with sulfa allergies b/c of sulfa moeity

21
Q

Atazenavir

A

Second choice to Darunavir

Less body fat redistribution but problem of increased bilirubin

22
Q

SaquinAVIR

A

Think QT - don’t give together with ritonavir

23
Q

LopinAVIR

A

ONLY given together with ritonavir to increase bioavailability

24
Q

IndinAVIR

A

Some cross resistance with ritonavir so beware

Big side effect = kidney stones and hyperbilirubinema (HYDRATE)

25
Q

TipranAVIR

A

Newer PI - non peptide
Drug of last choice - saving it for those who are treatment resistant
Increased risk for intracranial hemorrhage when given with ritonavir
Also has a sulfa moiety
Liver toxicity

26
Q

Fusion Inhibitors

A

Enfuvirtide (Fuzeon)
• Binds to gp41 to prevent conformation change required for membrane fusion
• For treatment resistant patients
Maraviroc
• Need to know tropism of patient receptor

27
Q

The only Parenteral antiretroviral agent

A

Enfuvirtide (Fuzeon)

28
Q

Antiretroviral that is only effective in patients with CCR5-tropic HIV infections

A

Maraviroc (because only inhibits that receptor - patients with CXCR4 receptors will not benefit)

29
Q

Dolutegravir

A

Integrase Inhibitor - blocks integrase enzyme needed for replication
DOC in combo with NRTIs in treatment-resistant patients from whom other drugs no longer working

Pharm I Final Review (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions