Neoplasia/Hematology - Pharmacology - Antiretrovirals; Antimalarials

Question 1

Name the three main categories of antiretrovirals used in combatting HIV infection.

Answer 1

NRTIs

NNRTIs

Protease inhibitors

Question 2

Name a few major categories of antiretrovirals used in combatting HIV infection besides NRTIs, NNRTIs, and protease inhibitors.

Answer 2

Entry inhibitors

Integrase inhibitors

Boosting agents

Question 3

What is the mechanism of action of NRTIs in combatting HIV infection?

Answer 3

Reverse transcriptase inhibition

Question 4

Name a few examples of nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs).

ATZ

Answer 4

Abacavir;

tenofovir;

zidovudine

Question 5

What is the hallmark toxicity of NRTIs?

Answer 5

Mitochondrial toxicity

Question 6

What is the mechanism of action of NNRTIs in combatting HIV infection?

Answer 6

Reverse transcriptase inhibition

Question 7

Name two commonly used NNRTIs.

ER

Answer 7

Efavirenz and rilpivirine

Question 8

Name a few of the various side effects seen with NNRTI use.

Answer 8

Teratogenicity (efavirenz);

rash and hepatotoxicity;

neurologic and psychiatric effects

Question 9

Name a few notable protease inhibitors used in HIV treatment.

AID

Answer 9

Atazanavir;

lopinavir;

darunavir

Question 10

True/False.

Protease inhibitors are often administered with a boosting agent in HIV treatment.

Answer 10

True.

Question 11

The protease inhibitors used in treating HIV infection work by blocking cleavage of what?

Answer 11

Gag-Pol polyproteins

Question 12

Name the medication class used in HIV treatment that result in the following side effects:

Insulin resistance, hyperglycemia, diabetes, hyperlipidemia, lipodystrophy, hepatotoxicity, bleeding in patients with hemophilia, and PR-interval prolongation

Answer 12

Protease inhibitors

Question 13

The names of the integrase inhibitors used in treating HIV infection end in what suffix?

Answer 13

-Gravir

E.g. raltegravir, dolutegravir, bictegravir

Question 14

True/False.

The side effects of integrase inhibitors (HIV treatment) include insomnia, dizziness, and even depression.

Answer 14

True.

Question 15

What is a leukocyte surface protein that can be blocked in order to prevent HIV entry?

Answer 15

CCR5

Question 16

What is an HIV envelope glycoprotein that can be blocked in order to prevent HIV fusion with the host cell?

Answer 16

gp41

Question 17

HIV entry into host cells can be blocked by blocking the early interaction of HIV via the ______ receptor on the host T_H cell and the ______ on the HIV envelope.

Answer 17

HIV entry into host cells can be blocked by blocking the early interaction of HIV via the CD4 receptor on the host T_H cell and the gp120 on the HIV envelope.

Question 18

Antiretroviral therapy side effects:

Abacavir — increased risk of _________ disease

Tenofovir — increased risk of _________ disease and _________

Tenofovir — decreases risk of HBV co-infection

Efavirenz — increases risk of psychiatric effects

Answer 18

Antiretroviral therapy side effects:

Abacavir — increased risk of cardiovascular disease

Tenofovir — increased risk of kidney disease and osteoporosis

Tenofovir — decreases risk of HBV co-infection

Efavirenz — increases risk of psychiatric effects

Question 19

Antiretroviral therapy side effects:

Abacavir — increased risk of cardiovascular disease

Tenofovir — increased risk of kidney disease and osteoporosis

_________ — decreases risk of HBV co-infection

_________ — increases risk of psychiatric effects

Answer 19

Antiretroviral therapy side effects:

Abacavir — increased risk of cardiovascular disease

Tenofovir — increased risk of kidney disease and osteoporosis

Tenofovir — decreases risk of HBV co-infection

Efavirenz — increases risk of psychiatric effects

Question 20

True/False.

ART adherence is highly important in those infected with HIV as poor adherence can lead to virologic failure.

Answer 20

True.

Question 21

Protease inhibitors and NNRTIs are metabolized by what system?

Protease inhibitors block what system?

Answer 21

The CP450 system;

the CP450 system

Question 22

True/False.

HIV typically shows little-to-no likelihood of developing resistance to ART.

Answer 22

False.

Some viral mutations result in a decreased susceptibility to antiretrovirals; however, several mutations are often needed for resistance to be clinically significant.

Question 23

HIV strains are most likely to become resistant to what medication class?

Answer 23

NNRTIs

Question 24

How are severe malarial infections treated?

Answer 24

IV artesunate

Question 25

P. _______ and P. _______ form dormant forms in _____cytes, thus eradication of BOTH the erythrocytic and hepatic parasites is required to cure these infections.

Answer 25

P. _ovale_ and P. _vivax_ form dormant forms in hepatocytes, thus eradication of BOTH the erythrocytic and hepatic parasites is required to cure these infections.

Question 26

P. ovale and P. vivax form dormant forms in hepatocytes, thus eradication of BOTH the __________ and __________ parasites is required to cure these infections.

Answer 26

P. ovale and P. vivax form dormant forms in hepatocytes, thus eradication of BOTH the erythrocytic and hepatic parasites is required to cure these infections.

Question 27

How should infection with chloroquine-sensitive malaria be treated?

Answer 27

Chloroquine (or Hydroxychloroquine)

(+ primaquine for P. ovale or P. vivax)

Question 28

What is the preferred treatment for chloroquine-resistant malaria?

Answer 28

Artemether + lumefantrine

(or atovaquone-proguanil)

(+ primaquine for P. vivax or P. ovale)

Question 29

What is the mechanism of action of artemisinins (e.g. artemether, artesunate)?

Answer 29

Free radical formation

Question 30

What is the mechanism of action of atovaquone and primaquone?

Answer 30

Disruption of electron transport

Question 31

What is the mechanism of action of proguanil?

Answer 31

Dihydrofolate reductase inhibition

Question 32

What is the mechanism of action of chloroquine, mefloquine, and hydroxychloroquine in treating malarial infections?

Answer 32

Prevents malarial usage of hemoglobin (not effective against liver stage)

Question 33

What medication inhibits mitochondrial electron transport and is useful against the hepatic stage of malarial infection?

Answer 33

Primaquine

Question 34

What medications that inhibit protein synthesis are used in treating malarial infections?

Answer 34

Tetracyclines;

clindamycin;

doxycycline

Question 35

Via what mechanism of action does pyrimethamine treat malarial infection?

Answer 35

Dihydrofolate reductase inhibition

Question 36

Mechanisms of chloroquine-resistance in malarial species:

Mutations of the __________ __________ transporter (PfCRT) as well as increased copies of the multidrug resistance protein-__ (PfMDR1) can result in resistance to chloroquine by reducing its concentration in the digestive food vacuole.

Answer 36

Mechanisms of chloroquine-resistance in malarial species:

Mutations of the chloroquine resistance transporter (PfCRT) as well as increased copies of the multidrug resistance protein-1 (PfMDR1) can result in resistance to chloroquine by reducing its concentration in the digestive food vacuole.

Question 37

________ and ________ commonly cause cinchonism (a combination of headache, tinnitus, high tone deafness, blurred vision, vertigo, nausea, vomiting and GI distress).

Postural hypotension can occur frequently. Prolongation of the ___ interval may occur, causing cardiac conduction disturbances and cardiac arrhythmias (Torsade de Pointes). Contraindicated in __________.

Answer 37

Quinine and quinidine commonly cause cinchonism (a combination of headache, tinnitus, high tone deafness, blurred vision, vertigo, nausea, vomiting and GI distress).

Postural hypotension can occur frequently. Prolongation of the QT interval may occur, causing cardiac conduction disturbances and cardiac arrhythmias (Torsade de Pointes). Contraindicated in pregnancy.

Question 38

Quinine and quinidine commonly cause _________ (a combination of headache, _________, high tone deafness, blurred vision, vertigo, nausea, vomiting and GI distress).

Postural hypotension can occur frequently. Prolongation of the QT interval may occur, causing cardiac conduction disturbances and cardiac arrhythmias (Torsade de Pointes). Contraindicated in pregnancy.

Answer 38

Quinine and quinidine commonly cause cinchonism (a combination of headache, tinnitus, high tone deafness, blurred vision, vertigo, nausea, vomiting and GI distress).

Postural hypotension can occur frequently. Prolongation of the QT interval may occur, causing cardiac conduction disturbances and cardiac arrhythmias (Torsade de Pointes). Contraindicated in pregnancy.

Question 39

Which antimalarial medication can cause a potentially fatal hemolytic anemia in patients with a G6PD deficiency?

Answer 39

Primaquine

Question 40

Patients should be screened for what disorder before being treated with primaquine?

Why?

Answer 40

G6PD deficiency;

potential for hemolytic anemia