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Questions and Answers
What are the main types of HIV drugs?
What are the main types of HIV drugs?
What does NRTI stand for?
What does NRTI stand for?
Nucleoside Reverse Transcriptase Inhibitors
NRTIs require phosphorylation to be active.
NRTIs require phosphorylation to be active.
True
What is the mechanism of action of NNRTIs?
What is the mechanism of action of NNRTIs?
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Monotherapy with PIs is contraindicated.
Monotherapy with PIs is contraindicated.
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Which of the following drugs is a CCR5 antagonist?
Which of the following drugs is a CCR5 antagonist?
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What are the two main mechanisms of resistance to NRTIs?
What are the two main mechanisms of resistance to NRTIs?
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Dual-NRTI pairs are a preferred backbone for combination therapy due to their minimal drug interactions.
Dual-NRTI pairs are a preferred backbone for combination therapy due to their minimal drug interactions.
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Which NRTI has the highest rate of lactic acidosis and hepatic steatosis?
Which NRTI has the highest rate of lactic acidosis and hepatic steatosis?
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What kind of analog is Abacavir?
What kind of analog is Abacavir?
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Abacavir is affected by food.
Abacavir is affected by food.
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What is a serious side effect associated with abacavir?
What is a serious side effect associated with abacavir?
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What type of analog is Tenofovir?
What type of analog is Tenofovir?
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Tenofovir requires three phosphorylations to be activated.
Tenofovir requires three phosphorylations to be activated.
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Food can increase the bioavailability of tenofovir.
Food can increase the bioavailability of tenofovir.
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What is the recommended regimen for pre-exposure prophylaxis?
What is the recommended regimen for pre-exposure prophylaxis?
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Which drugs suppress both HBV and HIV?
Which drugs suppress both HBV and HIV?
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What is the primary mutation associated with tenofovir resistance?
What is the primary mutation associated with tenofovir resistance?
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Which NRTI has the highest rate of lipodystrophy?
Which NRTI has the highest rate of lipodystrophy?
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What is the first FDA-approved ART?
What is the first FDA-approved ART?
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Zidovudine is poorly distributed in body fluids.
Zidovudine is poorly distributed in body fluids.
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Which drug should be avoided in combination with stavudine due to viral antagonism?
Which drug should be avoided in combination with stavudine due to viral antagonism?
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Didanosine should be taken with a meal.
Didanosine should be taken with a meal.
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What is the main side effect associated with stavudine?
What is the main side effect associated with stavudine?
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Stavudine is used as a first-line treatment for HIV.
Stavudine is used as a first-line treatment for HIV.
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What are the two first-generation NNRTIs?
What are the two first-generation NNRTIs?
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NNRTIs have a short half-life.
NNRTIs have a short half-life.
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NNRTIs are affected by food.
NNRTIs are affected by food.
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Which NNRTI is highly albumin bound?
Which NNRTI is highly albumin bound?
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Efavirenz is associated with an increased risk of Stevens-Johnson syndrome.
Efavirenz is associated with an increased risk of Stevens-Johnson syndrome.
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What is the main drug interaction associated with efavirenz?
What is the main drug interaction associated with efavirenz?
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Delavirdine has a better resistance profile than first-generation NNRTIs.
Delavirdine has a better resistance profile than first-generation NNRTIs.
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Rilpivirine is highly bound to plasma proteins.
Rilpivirine is highly bound to plasma proteins.
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Nevirapine is effective in preventing vertical transmission of HIV.
Nevirapine is effective in preventing vertical transmission of HIV.
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Which drug is NOT used as an ARV but is solely used as a booster for other PIs?
Which drug is NOT used as an ARV but is solely used as a booster for other PIs?
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Which PI has a higher risk of hepatotoxicity?
Which PI has a higher risk of hepatotoxicity?
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Atazanavir should be taken with a full meal.
Atazanavir should be taken with a full meal.
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Which PI is considered safe during pregnancy?
Which PI is considered safe during pregnancy?
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Darunavir is generally considered safe for patients with sulfonamide allergy.
Darunavir is generally considered safe for patients with sulfonamide allergy.
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What is the prodrug of amprenavir?
What is the prodrug of amprenavir?
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Food can decrease the absorption of fosamprenavir.
Food can decrease the absorption of fosamprenavir.
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Fosamprenavir is contraindicated in children.
Fosamprenavir is contraindicated in children.
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Study Notes
HIV Pharmacology Study Notes
- NRTIs (Nucleoside Reverse Transcriptase Inhibitors): Drugs that inhibit HIV reverse transcriptase. These drugs require phosphorylation to become active. Common examples include Abacavir (ABC), Didanosine (ddI), Emtricitabine (FTC), Lamivudine (3TC), Stavudine (d4T), Tenofovir (TDF), and Zidovudine (AZT, ZDV).
NNRTIs (Non-Nucleoside Reverse Transcriptase Inhibitors): These drugs bind directly to reverse transcriptase, inhibiting its function. They include Delavirdine (DLV), Efavirenz (EFV), Etravirine (ETR), Nevirapine (NVP), and Rilpivirine (RPV).
PIs (Protease Inhibitors): Inhibit HIV protease, which is essential for viral replication. Key examples are Atazanavir (ATV), Darunavir (DRV), Fosamprenavir (FPV), Indinavir (IDV), Lopinavir (LPV), Nelfinavir (NFV), Ritonavir (RTV), and Saquinavir (SQV). Ritonavir often used as a booster for other PIs.
Integrase Inhibitors: These drugs interfere with the integrase enzyme essential for HIV's integration into host DNA. Examples include Raltegravir (RAL), Elvitegravir (EVG), and Dolutegravir (DTG).
CCR5 Antagonist: Blocks CCR5 receptor, preventing HIV's entry into cells. An example is Maraviroc (MVC).
Fusion Inhibitors: Interfere with the fusion process required for HIV entry into cells. An example is Enfuvirtide (ENF, Fuzeon).
NRTI Mechanisms of Resistance: Mutations in the reverse transcriptase gene, such as M184V, L74V, D67N, and M41L, allow HIV to resist NRTI drugs. Pyrophosphorolysis can resume DNA synthesis.
Dual-NRTI Pairs: Combinations of 2 NRTIs are common for HIV treatment. Advantages include fewer interactions and established therapy. Disadvantages include rare reports of lactic acidosis and hepatic steatosis.
NRTI Adverse Effects: Common side effects include lactic acidosis, hepatic steatosis, and lipodystrophy. Stavudine has the highest incidence of lactic acidosis and lipodystrophy, while Tenofovir, Abacavir, Lamivudine, and Emtricitabine have lower incidence.
Abacavir (ABC): A guanosine analog. Not affected by food. Serious hypersensitivity reactions can occur, requiring HLA-B*5701 screening before use.
Tenofovir (TDF): A nucleotide analog; lower risk of metabolic side effects than some other NRTIs. Absorption increases after a high-fat meal. Often used in combination with emtricitabine.
Emtricitabine (FTC): A fluorinated analog of lamivudine. Unaffected by food. Recommended pre-exposure prophylaxis (PrEP) drug combination with tenofovir.
Lamivudine (3TC): A cytosine analog. Safe for mothers and infants. Well-tolerated but can cause darkened skin pigmentation.
Zidovudine (AZT, ZDV): A thymidine analog; first ART (antiretroviral therapy) approved. Commonly used in pregnancy. Significant side effects include bone marrow suppression (anemia, neutropenia, and macrocytosis).
Didanosine (ddI): A deoxyadenosine analog. Taken on an empty stomach. Side effects include peripheral neuropathy and pancreatitis.
Stavudine (d4T): A thymidine analog. High risk of peripheral neuropathy, lipoatrophy, and pancreatitis.
NNRTI Advantages and Disadvantages: Long half-lives, reduced metabolic toxicity (vs. PIs), and good potency. Disadvantages include rapid resistance development, cross-resistance among many NNRTIs.
NNRTI Adverse Effects: Rash (including severe reactions like Stevens-Johnson syndrome) and hepatotoxicity (especially with nevirapine).
Efavirenz (EFV): A long-acting NNRTI. Avoid high-fat meals. Central nervous system effects (drowsiness, insomnia) are possible.
Delavirdine (DLV): An older NNRTI. It has a high incidence of skin rash, erythema multiforme, and Stevens-Johnson syndrome. This drug is not used frequently.
Etravirine (ETR): A second-generation NNRTI that boasts a better resistance profile than first generation NNRTIs.
Rilpivirine (RPV): A second-generation NNRTI, commonly used. Associated with depression, insomnia, and headache.
Nevirapine (NVP): A lipophilic NNRTI. Good for preventing vertical transmission. Risks of rash and liver toxicity.
PIs Adverse Effects: Metabolic complications (fat redistribution, dyslipidemia, insulin resistance) and GI intolerance are common. Liver toxicity is also possible.
Ritonavir (RTV): A PI often used as a booster to increase the levels of other PIs. Potential for numerous drug interactions.
Atazanavir (ATV): Taken with a light meal due to absorption concerns in acidic environments. Avoid omeprazole for this reason. No dyslipidemia (a significant advantage).
Lopinavir (LPV): Taken with ritonavir to enhance drug levels, preventing resistance. Food dependant for higher absorption.
Darunavir (DRV): Used for patients resistant to other PIs. Fewer metabolic side effects than other PIs.
Fosamprenavir (FPV): A prodrug of amprenavir. Food affects absorption.
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Description
Explore the fundamental categories of HIV pharmacology in this quiz. Test your knowledge on NRTIs, NNRTIs, PIs, and Integrase Inhibitors, along with their mechanisms and key examples. This resource is essential for students studying virology or infectious diseases.
