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Antiretrovirals Flashcards

1
Q

NRTI’s

A

Zidovudine, Zalcitabine, Diadanosine, Stavudine, Abacavir, tenofovir, Lamivudien, emcitabine

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2
Q

NRTI’s MOA

A

substrate for RT, lack 3’OH group can’t elongate RNA

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3
Q

NRTI’s- what cells does it work in

A

Newly infected cells

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4
Q

NRTI- HIV1, 2 or both

A

Both

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5
Q

What is given to mother to prevent spread of HIV during child birth

A

NRIT

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6
Q

NRTI- AE

A

Lactic Acidosis (mtDNA interference), hepatic steatosis, N/V/D, fatigue, insomnia drugs with a d cause reversible, dose dependent peripheral neuropath

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7
Q

Zidovudine- abrev

A

AZT

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8
Q

Zidovudine- AE

A

Bone marrow suppression, malaise, myopathies, N/V, HA

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9
Q

Zidovudine- Contraindications

A

Don’t give to people with Ganciclovir, used to tx CMV

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10
Q

Zalcitabine- abrev

A

ddC

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11
Q

Zalcitabine- AE

A

peripheral neuropathy, pancreatitis

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12
Q

Didanosine- Abrev

A

ddl

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13
Q

Didanosine- AE

A

Pancreatitis- deadly Peripheral neuritis is common

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14
Q

Didanosine- meals

A

Do not take with meals, acid will destroy the drug

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15
Q

Stavudine- Abrev

A

d4t

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16
Q

Stavudine- AE

A

lipodystrophy- prevrent with pravastatin and atrovastatin peripheral nueropathy

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17
Q

Abacavir- abrev

A

ABC

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18
Q

Abacavir- AE

A

hypersensitivity rxn- deadly

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19
Q

Tenofovir- AE

A

nephrotoxic

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20
Q

Lamivudine, emtricitabine- AE

A

minimal toxicity, GI, HA

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21
Q

Emtricitabine- abrev

A

FTC

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22
Q

NRTI- MOR

A

3-4 AA mutations

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23
Q

NNRTI’s

A

Nevirapine, delavirdine, enfavirenz, etravirine, rilpirivine

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24
Q

NNRTI- MOA

A

non competitive antagonist of RT

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25
NNRTI- new or old cells?
New
26
NNRTI- HIV1, 2, or both
HIV 1
27
NNRTI- AE
Rash, hepatotoxicity
28
NNRTI- MOR
1 codon change- very common
29
NNRTI- T1/2
long
30
NNRTI- protein binding
high
31
NNRTI- metabolism
in the liver and high
32
Nevirapine- effect on CYP450
Inducer
33
Delvaridine- effect on CYP450
Inhibitor
34
Efavirenz- AE
Abnormal CNS effects- vivid dreams, insomnia, dizziness
35
Effavirenz- Food
don't take with fatty meals
36
Efavirenz- Contraindications
Pregnancy
37
Etravirine- - use
last line, NNRTI is have developed resistance to all the others
38
Riplirivine- AE
Severe rash, GI
39
Protease inhibitors
Indinavir, atazanavir, tipranavir, fosamprenavir, lopinavir, nelfinavir, ritonavir, saquinavir
40
PI- MOA
binds to active site of protease --> cant cleave the polyprotein
41
PI- new, old, both
both
42
PI- AE
hyperglycemia, dyslipidemia, lipodystrophy, osteoperosis, GI disturbances, redistribution of fat from face and extremities to waist
43
PI- resistance
4-5 Codon mutation
44
PI- lymphodystrophy
redistribution of fat from face and extremities to waist, HIV lymphodystrophy syndrome. Tx atrovastatin, provastatin
45
PI- liver enzymes
inhibitors or CYP3A4 --> lots of drug interactions
46
PI- metabolism
hepatic
47
PI- protein binding
high
48
PI- excretion
renal
49
PI- order of CYP3A4 interactions
Ritonavir- greatest squinavir- least
50
Indinavir- AE
Kidney stones, hyperbillirubinemia, alopecia
51
Atazanavir- AE
prolonged PR- messes up atria hyperbiirubinemia
52
Tipranavir-AE
Intracranial hemorrhage
53
Ritonavir- AE
largest inhibitor of CYP3A4 enzyme --> inhibits metabolism of other HIV drugs, so saves $
54
Fusion inhibitor
Enfuviritide- Fuzeon
55
Enfuviritide- MOA
binds to gp41 env protein and prevents fusion of HIV to cell
56
Enfuviritide- resistance
1 codon change, low barrier
57
Enfuviritide- HIV1,2, both
HIV1
58
Enfuviritide- usees
last ditch when all other drugs have failed
59
Enfuviritide- AE
Injection site rxns, N/D, fatigue, Neutropenia
60
Enfuviritide- admin
subcutaneous injection
61
Enfuviritide- protein binding
92%
62
Enfuviritide- metabolism
Proteloytic degridation, not hepatic metabolism
63
Agents for MDR HIV
Maraviroc, Raltegavir, Etravirine
64
Maraviroc- MOA
binds to CCR5, CCR5 antagonists, HIV can't bind
65
Maraviroc- AE
Major hepatotoxicity
66
Raltegavir- MOA
integrase inhibitor
67
Etravirine- uses
really an NNRTI that is used when other drugs have failed

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