Anti-Influenza Agents and Treatments
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Questions and Answers

What is the primary reason influenza A strains are significant in public health?

  • They can cause pandemics. (correct)
  • They are only found in birds.
  • They are resistant to antiviral drugs.
  • They have a low mutation rate.

Which influenza subtypes are currently circulating globally?

  • H2N2, H3N2, H5N1
  • H1N2, H5N1, H3N2
  • H1N1, H1N2, H3N2 (correct)
  • H1N1, H7N9, H5

Which of the following anti-influenza agents has a reported high level of resistance recently?

  • Peramivir
  • Zanamivir
  • Amantadine (correct)
  • Oseltamivir

How do neuraminidase inhibitors like oseltamivir and zanamivir function?

<p>They inhibit the release of new viruses. (C)</p> Signup and view all the answers

What distinguishes the function of adamantanes compared to neuraminidase inhibitors?

<p>They only act on influenza A viruses. (D)</p> Signup and view all the answers

What aspect of avian influenza viruses poses a risk to humans?

<p>Their ability to mutate rapidly. (B)</p> Signup and view all the answers

Which type of infection is treated with anti-influenza agents?

<p>Only severe influenza infections. (B)</p> Signup and view all the answers

What is true about the resistance levels of neuraminidase inhibitors?

<p>Neuraminidase inhibitors show a low level of resistance. (A)</p> Signup and view all the answers

Which of the following adverse effects are associated with zanamivir administration?

<p>Cough (C), Transient nasal and throat discomfort (D)</p> Signup and view all the answers

What is the main potential side effect of peramivir?

<p>Diarrhea (A)</p> Signup and view all the answers

Why is early treatment with peramivir considered optimal?

<p>It is less effective when started later (B)</p> Signup and view all the answers

Which statement about amantadine and rimantadine is true?

<p>Amantadine is less active than rimantadine (D)</p> Signup and view all the answers

What percentage of influenza B viruses tested retained susceptibility to oseltamivir and zanamivir?

<p>100% (D)</p> Signup and view all the answers

What is the primary route of elimination for peramivir?

<p>Kidney (C)</p> Signup and view all the answers

Which of the following statements is NOT true regarding the administration of zanamivir?

<p>It is recommended for patients with airway disease (B)</p> Signup and view all the answers

Which factor requires a dose adjustment for peramivir?

<p>Renal insufficiency (A)</p> Signup and view all the answers

What is the average concentration of rimantadine in nasal mucus compared to plasma?

<p>50% higher (D)</p> Signup and view all the answers

Which statement is true regarding the metabolism of rimantadine and amantadine?

<p>Rimantadine undergoes extensive metabolism before excretion. (C)</p> Signup and view all the answers

What is the likelihood that amantadine and rimantadine are effective in preventing clinical illness when initiated before exposure?

<p>70-90% protective (A)</p> Signup and view all the answers

What type of side effects are the most common with amantadine and rimantadine?

<p>Gastrointestinal and central nervous system (D)</p> Signup and view all the answers

In which patient population is there a requirement for dose reductions for amantadine and rimantadine?

<p>In the elderly and patients with renal insufficiency (A)</p> Signup and view all the answers

What serious side effects can occur due to alterations in dopamine neurotransmission?

<p>Marked behavioral changes and seizures (A)</p> Signup and view all the answers

What is a potential risk when amantadine is taken in overdose?

<p>Clinical manifestations of anticholinergic activity (C)</p> Signup and view all the answers

What major concern is related to amantadine and rimantadine during pregnancy?

<p>They are teratogenic and embryotoxic (A)</p> Signup and view all the answers

What is the peak replication period for the influenza virus after the onset of illness?

<p>24–72 hours (C)</p> Signup and view all the answers

How effective is once-daily prophylaxis with oseltamivir in preventing disease after exposure?

<p>70–90% (D)</p> Signup and view all the answers

What is the half-life of oseltamivir?

<p>6–10 hours (B)</p> Signup and view all the answers

What effect does probenecid have on oseltamivir excretion?

<p>Decreases renal clearance by 50% (B)</p> Signup and view all the answers

Which of the following is a common adverse effect associated with oseltamivir?

<p>Nausea (D)</p> Signup and view all the answers

What is the administration route of zanamivir?

<p>Inhalation (A)</p> Signup and view all the answers

Approximately what percentage of the zanamivir dose is absorbed and excreted in the urine?

<p>5–15% (C)</p> Signup and view all the answers

Which population is reported to have a higher incidence of neuropsychiatric events while using oseltamivir?

<p>Adolescents and adults in Japan (A)</p> Signup and view all the answers

Flashcards

What are H and N subtypes?

Viral proteins on the surface of influenza A viruses, used to classify the virus's subtype based on their structure. They are responsible for attaching to host cells.

Why is influenza A considered zoonotic?

Influenza A viruses can infect multiple animals, including birds, pigs, and humans. This allows the virus to spread more easily and create a reservoir of infection.

What makes influenza A a risk for pandemics?

The ability of a virus to spread efficiently from person to person through respiratory droplets. Influenza A viruses have a higher potential for pandemics due to their ability to circulate among humans.

How do neuraminidase inhibitors work?

Neuraminidase inhibitors are antiviral drugs that block the release of new viral particles from infected cells, preventing the spread of infection. They work against both influenza A and B viruses.

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How do adamantanes work?

Adamantanes are antiviral drugs that interfere with the uncoating process of influenza A viruses, preventing them from entering and infecting new cells. They are effective against influenza A only.

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What are some examples of adamantanes?

Amantadine and rimantadine are examples of adamantane drugs which have been highly affected by viral resistance, meaning they are less effective at fighting many influenza strains.

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Name two commonly prescribed neuraminidase inhibitors.

Oseltamivir and zanamivir are neuraminidase inhibitors, often prescribed for influenza treatment, particularly in high-risk individuals or for severe infections.

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Why is influenza virus classification important?

Influenza A and B viruses are classified by their core proteins and surface proteins. This classification helps track viral evolution and develop targeted treatments.

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What is oseltamivir?

Oseltamivir is a medicine that is used to treat and prevent influenza (flu). It is taken by mouth and works by blocking a protein called neuraminidase that the flu virus needs to spread.

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When is oseltamivir most effective?

Oseltamivir works best when started within 48 hours of the onset of flu symptoms. This is because the replication of the flu virus peaks at 24-72 hours after symptoms appear.

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How does oseltamivir get inside the body?

Oseltamivir is absorbed into the bloodstream and reaches various parts of the body, including the middle ear and sinus fluid. This allows it to target the flu virus in different areas of the body.

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What is the half-life of oseltamivir?

The active form of oseltamivir, called oseltamivir carboxylate, lasts in the body for about 6-10 hours. This means that it takes about 6-10 hours for the drug's concentration to decrease by half.

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How does kidney function impact oseltamivir dosing?

Oseltamivir can be adjusted for people with kidney problems because their bodies might not process the drug as quickly. The dosage might need to be changed based on their kidney function.

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What is zanamivir and how is it different from oseltamivir?

Zanamivir is another medicine for flu, but it is inhaled directly into the lungs instead of being taken by mouth. It works by targeting the flu virus in the respiratory tract.

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Why is zanamivir effective in the lungs?

Zanamivir reaches high concentrations in the lungs, making it effective in fighting the flu virus right at the site of infection. It's designed to stay in the lungs for a longer period of time, which is important for fighting the flu.

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How is zanamivir absorbed in the body?

Only a small amount of zanamivir is actually absorbed into the bloodstream. Most of it stays in the lungs, where it is needed to fight the flu.

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What is zanamivir?

Zanamivir is an antiviral medication used to treat influenza. It works by blocking a key protein called neuraminidase, which is essential for the influenza virus to spread within the body.

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What are some side effects of zanamivir?

Zanamivir can cause side effects like coughing, shortness of breath, and nasal and throat discomfort. However, these side effects are usually mild and temporary.

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Is zanamivir always effective?

Although zanamivir is generally effective against influenza, viral resistance has been observed. However, the majority of influenza strains remain susceptible to the drug.

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What is peramivir?

Peramivir is another antiviral medication effective against both influenza A and B. It is administered as a single intravenous dose.

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How is peramivir eliminated from the body?

Peramivir is primarily eliminated through the kidneys, so dose adjustments might be necessary in individuals with kidney problems.

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What are the potential risks of peramivir?

While peramivir generally has a good safety profile, diarrhea is a common side effect. In rare cases, it could lead to serious skin reactions or alterations in mental state.

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What are amantadine and rimantadine?

Amantadine and rimantadine belong to a class of drugs called adamantanes, which target a specific protein (M2) on influenza A viruses.

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How do amantadine and rimantadine work?

Amantadine and rimantadine inhibit the uncoating process of influenza A viruses, preventing them from releasing their genetic material and replicating.

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What are the limitations of adamantanes?

Amantadine and rimantadine are antiviral drugs that can prevent or shorten influenza A infections, but their effectiveness is limited due to frequent viral resistance.

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How do adamantane drugs work?

Amantadine and rimantadine work by interfering with the uncoating process of influenza A viruses, blocking them from entering host cells.

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How are amantadine and rimantadine metabolized?

Amantadine and rimantadine are excreted differently by the body. Amantadine is excreted unchanged, while rimantadine is metabolized before excretion.

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What are the side effects of adamantane drugs?

Both amantadine and rimantadine can cause adverse effects like nausea, nervousness, and insomnia. Serious side effects include behavior changes, hallucinations, and seizures.

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Who needs dosage adjustments for adamantanes?

Dose adjustments are necessary for patients with renal insufficiency, hepatic insufficiency, and older adults when using either amantadine or rimantadine.

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When are adamantanes effective against influenza?

Adamantanes are effective for influenza A but not influenza B. They can prevent clinical illness and shorten its duration if used before exposure.

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Are adamantane drugs safe during pregnancy?

Amantadine and rimantadine are teratogenic and embryotoxic, meaning they can harm a developing fetus. Birth defects have been reported after exposure during pregnancy.

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What factors increase the risk of serious side effects?

High plasma concentrations of amantadine or rimantadine can increase the risk of serious side effects, especially in patients with renal insufficiency, seizure disorders, or advanced age.

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Study Notes

Anti-Influenza Agents

  • Influenza strains are classified by core proteins (A, B, or C), origin (avian, swine), and geographic location.
  • Influenza A, causing pandemics, has 16 H (hemagglutinin) and 9 N (neuraminidase) subtypes.
  • Influenza B primarily infects humans, while influenza A infects diverse animals, including birds (reservoir).
  • Current circulating subtypes include H1N1, H1N2, and H3N2.
  • Avian subtypes (e.g., H5N1, H7N9) can mutate to high pathogenicity.
  • Human infection from avian strains is rare, limited, and sporadic.
  • Five anti-influenza drugs are approved: three neuraminidase inhibitors (oral oseltamivir, inhaled zanamivir, IV peramivir) and two adamantanes (amantadine, rimantadine).

Oseltamivir and Zanamivir

  • Oseltamivir and zanamivir are neuraminidase inhibitors.
  • They block influenza A and B virus release from infected cells.
  • They clump newly released viral particles to prevent spread.
  • Early administration (within 48 hours) is crucial.
  • Shortens symptom duration and viral shedding.
  • Modestly reduces viral titer.
  • Oral oseltamivir is a prodrug activated by hepatic esterases.
  • High oral bioavailability (~80%)
  • Low plasma protein binding
  • Excreted via glomerular filtration and tubular secretion.
  • Benecid reduces renal clearance.
  • Half-life: 6-10 hours
  • Side effects: nausea, vomiting, headache.
  • Inhaled zanamivir acts on respiratory tract.
  • High concentration in lungs.
  • Low systemic absorption.
  • Half-life: 2.8 hours
  • Side effects: cough, bronchospasm, nasal/throat discomfort.

Peramivir

  • Peramivir is a neuraminidase inhibitor.
  • Single 600 mg IV dose for uncomplicated influenza.
  • Early treatment (within 48 hours) is optimal.
  • Low protein-binding.
  • Eliminated primarily by the kidneys.
  • Half-life: ~20 hours
  • Side effects: diarrhea, rare serious skin reactions.
  • Potential risk of hallucinations, delirium, and abnormal behavior.

Amantadine and Rimantadine

  • Amantadine and rimantadine are adamantanes.
  • Block the M2 proton channel of influenza A virus.
  • Prevent virus uncoating.
  • Active only against influenza A, not B.
  • Rimantadine is more potent than amantadine.
  • Well absorbed; primarily excreted unchanged in urine.
  • Side effects: gastrointestinal, central nervous system (nervousness, concentration issues).
  • Potential for more serious side effects (behavioral changes, seizures) at high plasma concentrations.
  • High resistance rates, rendering them unlikely to be used.

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Description

This quiz covers key information about anti-influenza agents, including the classification of influenza strains and specific treatments like oseltamivir and zanamivir. Learn how these neuraminidase inhibitors work to block virus release and their importance in early treatment. Test your knowledge on current circulating subtypes and effective medications for the flu.

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