Chapter 99

Question 1

HIV
-What kind of virus is HIV?
-What kind of genetic material does it contain?

Answer 1

-Retrovirus
-RNA

Question 2

HIV
-What does it do in our bodies?

Answer 2

-It uses reverse transcriptase to convert RNA into DNA
-It then uses integrate to insert its DNA into ours

Question 3

HIV
-What are the target cells?
-What does HIV do?

Answer 3

-CD4 T cells (helper lymphocytes)
-It causes progressive immunodeficiency by destroying CD4T cells

Question 4

HIV
-How is it transmitted?

Answer 4

Through blood & body fluids

Question 5

HIV
-What are HIV drugs trying to do?

Answer 5

STOP HIV from replicating

Question 6

What are the 3 drug classes?

Answer 6

1. Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
2. Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
3. Protease Inhibitors

Question 7

What are the original drugs that are used to treat HIV?

Answer 7

NRTIs

Question 8

NRTIs
-What is the prototype of this class?

Answer 8

Zidovudine (Retrovir) (AZT)

Question 9

NRTIs: Mechanism of Action
-How does this inhibit HIV replication?
-Decribe the process once they enter the body (3)

Answer 9

-By suppressing synthesis of viral DNA
1. Once activated intracellularly, they compete for binding with reverse transcriptase
2. It will cause DNA strand termination
3. It stops continuous replication

Question 10

NRTIs: Adverse Effects
-What are the 4?

Answer 10

1. Lactic acid with hepatomegaly
2. Hepatic steatosis
3. Pancreatitis
4. Myopathy

Question 11

NRTIs: Adverse Effects
-What does lactic acidosis with hepatomegaly mean?

Answer 11

Build up of acids in the blood & large liver

Question 12

NRTIs: Adverse Effects
-What is hepatic steatosis?

Answer 12

Fat buildup in the liver

Question 13

NRTIs: Drug Interactions
-Describe them

Answer 13

There are very few since it is not broken down by P450 enzymes (liver enzymes)

Question 14

NNRTIs
-How do these differ from NRTIs?

Answer 14

In structure & mechanism of action

Question 15

NNRTIs
-Describe what these do to inhibit HIV replication

Answer 15

1. NNRTIs bind to the active center of reverse transcriptase
2. Cause direct inhibition of DNA replication (shut it off)

Question 16

NNRTIs
-Are they inactive as they are administered?

Answer 16

NO, they are active!

Question 17

NNRTIs
-What are the adverse effects that patients complain about most?

Answer 17

CNS effects –> dizziness, nightmares, vivid dreams, difficulty sleeping

Question 18

NNRTIs: Drug Interactions
-Can this be taken during pregnancy?

Answer 18

NO; it is teratogenic

Question 19

NNRTIs: Drug Interactions
-What are the drug interactions like?

Answer 19

There are MANY bc these are CYP450 inducers

Question 20

NNRTIs: Drugs
-What are the 5 drugs under this class? NEERD

Answer 20

1. Nevirapine (viramune)
2. Efavirenz (sustiva)
3. Etravirine (intelence)
4. Rilpivirine (edurant)
5. Doravirine (pifeltro)

Question 21

PROTEASE INHIBITORS
-These are among the (least/most) effective antiretroviral drugs

Answer 21

MOST

Question 22

PROTEASE INHIBITORS
-They are used in combination with _____
-Why?

Answer 22

-NRTIs
-To reduce viral load to an undetectable level

Question 23

PROTEASE INHIBITORS
-How does it inhibit HIV replication?

Answer 23

By blocking protease enzymes to prevent maturation of HIV

Question 24

PROTEASE INHIBITORS
-What is the challenge to protease inhibitors?

Answer 24

RESISTANCE; which is why multiple medications are used

Question 25

**PROTEASE INHIBITORS** -What are the 4 adverse effects?

Answer 25

1. Hyperglycemia/diabetes --> if severe enough 2. Lipodystrophy (fat distribution) 3. Hyperlipidemia 4. Decreased cardiac conduction velocity