Neoplasia/Hematology - Pharmacology - Antiretrovirals; Antimalarials Flashcards
Name the three main categories of antiretrovirals used in combatting HIV infection.
NRTIs
NNRTIs
Protease inhibitors
Name a few major categories of antiretrovirals used in combatting HIV infection besides NRTIs, NNRTIs, and protease inhibitors.
Entry inhibitors
Integrase inhibitors
Boosting agents
What is the mechanism of action of NRTIs in combatting HIV infection?
Reverse transcriptase inhibition
Name a few examples of nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs).
ATZ
Abacavir;
tenofovir;
zidovudine
What is the hallmark toxicity of NRTIs?
Mitochondrial toxicity
What is the mechanism of action of NNRTIs in combatting HIV infection?
Reverse transcriptase inhibition
Name two commonly used NNRTIs.
ER
Efavirenz and rilpivirine
Name a few of the various side effects seen with NNRTI use.
Teratogenicity (efavirenz);
rash and hepatotoxicity;
neurologic and psychiatric effects
Name a few notable protease inhibitors used in HIV treatment.
AID
Atazanavir;
lopinavir;
darunavir
True/False.
Protease inhibitors are often administered with a boosting agent in HIV treatment.
True.
The protease inhibitors used in treating HIV infection work by blocking cleavage of what?
Gag-Pol polyproteins
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
Protease inhibitors
The names of the integrase inhibitors used in treating HIV infection end in what suffix?
-Gravir
E.g. raltegravir, dolutegravir, bictegravir
True/False.
The side effects of integrase inhibitors (HIV treatment) include insomnia, dizziness, and even depression.
True.
What is a leukocyte surface protein that can be blocked in order to prevent HIV entry?
CCR5
What is an HIV envelope glycoprotein that can be blocked in order to prevent HIV fusion with the host cell?
gp41
HIV entry into host cells can be blocked by blocking the early interaction of HIV via the ______ receptor on the host TH cell and the ______ on the HIV envelope.
HIV entry into host cells can be blocked by blocking the early interaction of HIV via the CD4 receptor on the host TH cell and the gp120 on the HIV envelope.
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
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
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
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
True/False.
ART adherence is highly important in those infected with HIV as poor adherence can lead to virologic failure.
True.
Protease inhibitors and NNRTIs are metabolized by what system?
Protease inhibitors block what system?
The CP450 system;
the CP450 system
True/False.
HIV typically shows little-to-no likelihood of developing resistance to ART.
False.
Some viral mutations result in a decreased susceptibility to antiretrovirals; however, several mutations are often needed for resistance to be clinically significant.
HIV strains are most likely to become resistant to what medication class?
NNRTIs
How are severe malarial infections treated?
IV artesunate
P. _______ and P. _______ form dormant forms in _____cytes, thus eradication of BOTH the erythrocytic and hepatic parasites is required to cure these infections.
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.
P. ovale and P. vivax form dormant forms in hepatocytes, thus eradication of BOTH the __________ and __________ parasites is required to cure these infections.
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.
How should infection with chloroquine-sensitive malaria be treated?
Chloroquine (or Hydroxychloroquine)
(+ primaquine for P. ovale or P. vivax)
What is the preferred treatment for chloroquine-resistant malaria?
Artemether + lumefantrine
(or atovaquone-proguanil)
(+ primaquine for P. vivax or P. ovale)
What is the mechanism of action of artemisinins (e.g. artemether, artesunate)?
Free radical formation
What is the mechanism of action of atovaquone and primaquone?
Disruption of electron transport
What is the mechanism of action of proguanil?
Dihydrofolate reductase inhibition
What is the mechanism of action of chloroquine, mefloquine, and hydroxychloroquine in treating malarial infections?
Prevents malarial usage of hemoglobin (not effective against liver stage)
What medication inhibits mitochondrial electron transport and is useful against the hepatic stage of malarial infection?
Primaquine
What medications that inhibit protein synthesis are used in treating malarial infections?
Tetracyclines;
clindamycin;
doxycycline
Via what mechanism of action does pyrimethamine treat malarial infection?
Dihydrofolate reductase inhibition
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.
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.
________ 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 __________.
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.
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.
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.
Which antimalarial medication can cause a potentially fatal hemolytic anemia in patients with a G6PD deficiency?
Primaquine
Patients should be screened for what disorder before being treated with primaquine?
Why?
G6PD deficiency;
potential for hemolytic anemia
