Brainscape's Knowledge GenomeTM

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


See full index

Pharmacology #1 > Antiretroviral Drugs- (NRTI's) > Flashcards

Antiretroviral Drugs- (NRTI's) Flashcards

1
Q

Current anti-retroviral drugs for treatment of HIV are:

A

1) nucleoside reverse transcriptase inhibitors (NRTIs)
2) Nucleotide inhibitors
3) non-nucleoside reverse transcriptase inhibitors (NNRTIs)
4) Protease inhibitors
5) Fusion inhibitors
7) Integrase inhibitors

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

Why should monotherapy of anti-retrovirals by avoided?

A

Increased risk of resistance

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

What is HAART?

A

Combination therapy (Highly active anti-retroviral therapy)

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

What must be monitored in HAART?

A

viral load and CD4 cell count in case of development of resistance

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

In HIV diagnosis, you should look for what?

A

Abs against virus, not virus species

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

What are Nuclease Transcriptase Inhibitors (NRTI)?

A

Nucleoside analogs that inhibit viral reverse trancriptase (RT) and also cause chain termination during viral DNA synthesis.

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

NRTI’s MOA?

A

Require intra-cytoplasmic activation by phosphorylation by cellular enzymes including TK to the triphosphates

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

Name the 6Nuclease Transcriptase Inhibitors (NRTI):

A

1) Zidovudine
2) Didanosine
3) Lamuvudine (SULFUR RING, HEP B ALSO)
4) Zalcitabine
5) Stavudine
6) Abacavir

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

Zidovudine is a…

A

deoxythymidine analog that contains an azido group on the 3’ carbon of the dideoxyribose pentose sugar

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

Ziduvudine bioavailability?

A

Good oral bio, tissue dist and cns distribution (60-65% in cerebrospinal fluid compared to plasma) (35% plasma protein bound)

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

ZIduvudine undergoes what kindof elimination?

A

hepatic glucuroniation and renal elimination (glom filtration and tubular secretion)

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

Ziduvudine has increased toxicity due to?

A

Renal and hepatic insufficiency

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

What drug reduces the rate of clinical disease progression and prolongs survival in HIV infected patients?

A

Ziduvudine (AZT)

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

What drug reduces viral transmission of HIV to the fetus in pregnant women and what dosage forms?

A

1) Oral AZT during pregnancy
2) IV during labor
3) syrup to the new born

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

Ziduvudine resistance may be due to?

A

mutations in the pol gene, withdrawal of AZT may permit reversion to susceptible wild type strain

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

Adverse effects of Ziduvudine:

A

myelosuppression- causing anemia, neutropenia, GI intolerance, headache, and insomnia, but may resolve.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

AZT co-admin with other myelosuppressive drugs may cause what?

A

increased hematoxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What other myelosuppresive therapies when co-admin’d with AZT may cause hematoxicity?

A

1) Ganciclovir
2) Ribavirin
3) other cytotoxic agents

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Didanosine is what analog?

A

a deoxyadenosine analog

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

How should didanosine be taken and why?

A

It should be taken on an empty stomach bc it is unstable at a low pH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Resistance to didanosine is due to?

A

RT mutation at 74 and may confer cross resistance to abacavir, lamivudine, and zalcitabine.

22
Q

Adverse effects of didanosine?

A

1) Dose dependent pancreatitis

23
Q

Didanosine is contraindicated in?

A

cases of alcoholism and hypertriglyceridemia due to the AE pancreatitis

24
Q

Patients on high dose therapy of didanosine may require what monitoring?

A

periodic retinal examination

25
Q

Didanosine may reduce GI absorbtion of what drugs and why?

A

FQ’s and tetracyclines due to CHELATION so must be admin’d 2 hours apart

26
Q

How does ganciclovir affect didanosine and vice versa?

A

Increases AUC

27
Q

What drug causes decreased serum of didanosine?

A

Methadone

28
Q

Lamvudine is a what analog?

A

deoxy-cytosine analong

29
Q

Why is Lamivudine best used in combo therapy?

A

bc M184V mutation causes high levels of resistance to 3TC, and reduced susceptibility to abacavir, didanosine, and zalcitabine

30
Q

Lamivudine is synergistic with what drugs?

A

1) Zidovudine

2) Stavudine

31
Q

What is combivir?

A

Lamvudine + Zidovudine

32
Q

Trizivir

A

Avacavir + Lamvudine + Zidovudine

33
Q

Why is combivir beneficial?

A

Bc the m184V mutation that increases resistance to lamvudine also increases susceptibility to zidovudine

34
Q

Lamivudine is also effective against what?

A

HBV (Hep B)

35
Q

What increases AUC of lamivudine?

A

Bactrim

36
Q

Emtricitabine is what analog?

A

a flourinated analog of lamivudine

37
Q

Emtricitabine has cross resistance with what drug?

A

lamivudine

38
Q

Zalcitabine is what analog

A

cytosine

39
Q

Zalcitabine absorbtion is decreased by?

A

food and antacids, >80% oral bioavailability

40
Q

Adverse effects of Zalcitabine?

A

Pancreatitis
Dose dependent neuropathy
Oral or esophageal ulceration

41
Q

Zalcitabine is CI’d with what drugs?

A

Neuropathy inducing drugs

1) stavudine
2) didanosine
3) isoniazid

42
Q

What decreases renal clearance of Zalcitabine?

A

ampho B
foscarnet
aminoglycosides

43
Q

What increases plasma drug concentrations of Zalcitabine?

A

Probenecid and cimetidine

44
Q

Stavudine is what analog?

A

thymidine analog

45
Q

Stavudine oral bioavail?

A

86%

46
Q

Stavudine potential adverse effects?

A

Dose related peripheral sensory neuropathy
pancreatitis
arthralgias
elevation of serum aminotransferase

47
Q

Zidovudine reduces the phosphorylation of what drug? *

A

Stavudine, so not used together

48
Q

Abacavir is what analog?

A

guanosine analog

49
Q

Abacavir undergoes what metabolism and by what enzymes?

A

hepatic- alcohol dehydrogenase and glucuronosyl-transferase and renal elimn.

50
Q

What effect will alcohol have on abacavir?

A

it will decrease metabolism of abacavir- so increase levels in serum

51
Q

Adverse reactions of Abacavir?

A

hypersensitivity rxns (could be fatal) -rash, n/v/d, fatigue, ha

Pharmacology #1 (15 decks)

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