Hepatitis B Treatment Overview

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Questions and Answers

What is the primary mechanism of action for integrase inhibitors?

  • They block viral protein synthesis.
  • They inhibit the incorporation of viral DNA with host DNA. (correct)
  • They enhance host immune response.
  • They prevent viral entry into host cells.

Which of the following adverse effects is associated with Amantadine?

  • Ataxia (correct)
  • Renal failure
  • Prolonged QT interval
  • Hepatotoxicity

Which drug is classified as a CYP450 inhibitor?

  • Dolutegravir
  • Ritonavir (correct)
  • Raltegravir
  • Amantadine

How is Rimantadine primarily metabolized and excreted?

<p>Metabolized by the liver and extensively excreted. (D)</p> Signup and view all the answers

What is a common side effect of drugs like Nelfinavir and Saquinavir?

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

What type of drug is Lamivudine categorized as?

<p>Nucleoside reverse transcriptase inhibitor (C)</p> Signup and view all the answers

Which side effect is commonly associated with Lamivudine?

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

What is the metabolism route for Adefovir dipivoxil?

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

How does Lamivudine disrupt viral replication?

<p>By terminating chain elongation (C)</p> Signup and view all the answers

What is the primary way Adefovir is excreted?

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

What is the half-life of Lamivudine?

<p>7 hours (A)</p> Signup and view all the answers

What is the mechanism of action of Lamivudine in treating HBV?

<p>Inhibition of DNA polymerase (C)</p> Signup and view all the answers

Which additional virus can Lamivudine be used to treat aside from HBV?

<p>HIV (B)</p> Signup and view all the answers

What is the primary function of NRTIs in treating viral infections?

<p>Inhibit reverse transcriptase (B)</p> Signup and view all the answers

Which of the following side effects is most commonly associated with the use of Zidovudine?

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

Which NRTI is known to cause nephrotoxicity?

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

What is the mechanism of action for NNRTIs in viral treatment?

<p>Allosteric inhibition of reverse transcriptase (C)</p> Signup and view all the answers

Which of the following is a common side effect of Efavirenz?

<p>CNS toxicity including mood changes (B)</p> Signup and view all the answers

What is an effect of using Protease Inhibitors?

<p>Cleavage of polyproteins (B)</p> Signup and view all the answers

Which drug is known for causing a teratogenic effect?

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

Which side effect is associated with Maraviroc?

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

What effect does Abacavir have on the body?

<p>Can lead to hepatic steatosis (D)</p> Signup and view all the answers

Which of the following best describes the effect of antiretroviral therapy on DNA synthesis?

<p>Terminates DNA formation from RNA (B)</p> Signup and view all the answers

What is the function of Velpatasvir in the treatment of HCV?

<p>Inhibits the NS5A protein (B)</p> Signup and view all the answers

In which patient population is weight-based ribavirin dosing recommended?

<p>Patients with decompensated cirrhosis (B)</p> Signup and view all the answers

Which enzyme is primarily involved in the metabolism of Velpatasvir?

<p>CYP2B6 (D)</p> Signup and view all the answers

What is a common adverse reaction associated with the use of HIV viral fusion inhibitors?

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

Sofosbuvir is primarily excreted through which route?

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

What mechanism of action does Maraviroc utilize in HIV treatment?

<p>Inhibits CCR5 binding (B)</p> Signup and view all the answers

What is true about Sofosbuvir as a prodrug?

<p>It is converted to an active metabolite (A)</p> Signup and view all the answers

What is the primary mechanism of action for Entecavir?

<p>Inhibiting reverse transcriptase (C)</p> Signup and view all the answers

Which drug is classified as a fixed-dose combination product for treating chronic HCV?

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

In HAART therapy, which combination is standard?

<p>2 NRTIs + 1 Integrase Inhibitor (C)</p> Signup and view all the answers

Which of the following represents a potential adverse reaction of NS5B polymerase inhibitors?

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

Which side effect is associated with the use of Mavyret?

<p>Angioedema (B)</p> Signup and view all the answers

What distinguishes Velpatasvir from Sofosbuvir in terms of excretion?

<p>Sofosbuvir is predominantly excreted in urine (D)</p> Signup and view all the answers

What is a significant contraindication for patients treated with Mavyret?

<p>Past HBV infection (A)</p> Signup and view all the answers

What is the excretion pathway for Glecaprevir?

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

Which statement about Pibrentasivir is true?

<p>It has no significant hepatic metabolism. (B)</p> Signup and view all the answers

What is one of the mechanisms of action of Sofosbuvir in treating HCV?

<p>Preventing RNA replication (C)</p> Signup and view all the answers

Which of the following side effects is not commonly associated with Entecavir?

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

How is Entecavir mainly metabolized in the body?

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

What is a primary characteristic of Epclusa?

<p>Contains Sofosbuvir and Velpatasvir (C)</p> Signup and view all the answers

Flashcards

Lamivudine MOA

Lamivudine is a nucleoside reverse transcriptase inhibitor, which interferes with viral DNA replication by incorporating itself into viral DNA, stopping elongation.

Lamivudine Classification

Cytosine analogue;Nucleoside reverse transcriptase inhibitor (NRTI)

Adefovir dipivoxil MOA

Adefovir dipivoxil, an adenosine nucleotide analog, interferes with viral DNA replication by being incorporated into viral DNA, similar to Lamivudine.

Adefovir dipivoxil Class

Adenosine nucleotide analog, used in the treatment of hepatitis B (HBV).

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Lamivudine Metabolism

Minimal metabolism, mainly intracellular by sulfotransferase, and excreted primarily unchanged in urine.

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Adefovir Dipivoxil Metabolism

Adefovir undergoes phosphorylation, then converted to its active form, and excreted in urine.

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Lamivudine Drug Form

100 mg orally, once daily.

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Adefovir Dipivoxil Drug Form

10 mg orally once daily.

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Entecavir MOA

Entecavir inhibits HBV DNA replication and transcription by targeting reverse transcriptase.

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Entecavir Route

Entecavir is taken orally, once a day, at 1 mg.

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Mavyret MOA

Mavyret acts as an HCV NS3/4A protease inhibitor and NS5A inhibitor, blocking HCV replication.

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Mavyret Drug Class

Mavyret is a fixed-dose combination of Glecaprevir and Pibrentasivir.

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Epclusa MOA

Epclusa inhibits HCV NS5A polymerase to interfere with HCV RNA replication.

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Mavyret Side Effects

Mavyret can cause liver failure, angioedema, and HBV reactivation.

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Epclusa Drug Class

Epclusa is a combination drug containing Sofosbuvir.

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Mavyret Excretion

Glecaprevir is primarily excreted in the feces, while Pibrentasivir is mostly excreted in the urine.

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Mavyret Indication

Mavyret treats chronic HCV infections (genotypes 1-6) without cirrhosis or Compensated cirrhosis (Child-Pugh A).

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Entecavir Excretion

Entecavir is excreted primarily through glomerular filtration and tubular secretion.

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Sofosbuvir MOA

Sofosbuvir inhibits HCV NS5B polymerase, stopping viral RNA replication.

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Velpatasvir MOA

Velpatasvir inhibits HCV NS5A protein, interfering with viral RNA functions.

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Sofosbuvir/Velpatasvir combination

A combination of Sofosbuvir and Velpatasvir used for hepatitis C.

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HCV genotypes 1-6

Different forms or versions of the hepatitis C virus.

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Decompensated cirrhosis

Advanced liver disease, requiring special caution in treatment.

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Viral fusion inhibitor

Drug that prevents the virus from entering host cells.

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Attachment coreceptor inhibitor

Drug that prevents the virus from binding to host cell receptors.

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HAART (Highly Active Antiretroviral Therapy)

A combination therapy used to treat HIV.

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Hepatitis C

Viral infection targeting the liver.

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Ribavirin dosing

Dosage of ribavirin adjusted based on patient's weight for effective hepatitis C treatment.

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CYP450 inhibitor

A drug that prevents the liver enzyme CYP450 from breaking down other drugs, leading to higher levels of those other drugs in the body.

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Integrase Inhibitors

Drugs that stop a virus from integrating its genetic material into the host cell's DNA, preventing viral replication.

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Rhabdomyolysis

A serious muscle breakdown caused by some antiviral drugs.

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Amantadine MOA

Amantadine is a dopamine-like medication that treats influenza infections.

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RSV Drug Admin

Amantadine and Rimantadine are taken orally, twice a day for 3-5 days, soon after infection symptoms start.

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NRTIs (ZDV)

Nucleoside reverse transcriptase inhibitors; these drugs trick the virus into incorporating them into its DNA, stopping its replication process.

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NNRTIs (-vir)

Non-nucleoside reverse transcriptase inhibitors; they bind to the enzyme, preventing it from working properly to form viral DNA.

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Protease Inhibitors (-navir)

These drugs stop the virus from producing complete viral proteins, hindering its ability to replicate.

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Mitochondrial toxicity

Side effect of some antiretroviral drugs that can damage mitochondria, the energy-producing parts of cells.

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Hepatotoxicity

Liver damage as a side effect of certain antiviral medications.

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Reverse Transcriptase

An enzyme that converts viral RNA into DNA, essential for viral replication.

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Zidovudine

A nucleoside reverse transcriptase inhibitor used in the treatment for HIV.

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Allosteric inhibitors

Drugs that bind to a site on an enzyme, causing a shape change and preventing it from properly functioning.

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Polyproteins

A single long protein that needs to be cut up into smaller proteins. These smaller proteins are then used to build new viruses

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Protease- cleaving Polyprotein

An enzyme that cuts a polyprotein to produce smaller proteins that are needed for constructing new viruses.

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Study Notes

Hepatitis B (HBV) Treatment

  • Lamivudine (DOC):
    • Classification: Cytosine analogue, Nucleoside reverse transcriptase and polymerase inhibitor
    • MOA: Turns into active metabolite (phosphorylation by host cell), incorporated into viral DNA, disrupting replication process.
    • Metabolism & Excretion: Minimal metabolism (intracellular by sulfotransferase). Excretion is primarily through urine (mainly unchanged). Half-life: 7 hours. CYP450 minimal.
    • Side Effects: Nausea, Vomiting, Nephrotoxicity.
  • Adefovir dipivoil:
    • Classification: Adenosine nucleotide analog.
    • MOA: Leads to termination of HBV DNA. Active form is incorporated into viral DNA, which disrupts the process of replication.
    • Metabolism & Excretion: Phosphorylation (prodrug), converted to active form. Excretion primarily through urine (45% unchanged). Half-life: 7 hours. CYP450 none.
    • Side Effects: HA
  • Entecavir (Baraclude):
    • Classification: Deoxyguanosine analog.
    • MOA: Inhibits reverse transcriptase, DNA replication, and transcription, Effective in Lamivudine-resistant HBV.
    • Metabolism & Excretion: Minimal metabolism. Excreted by glomerular filtration and tubular secretion.
    • Side Effects: HA, Fatigue, Nausea, Dizziness

Hepatitis C (HCV) Treatment

  • Mavyret (Pibrentasivir/Glecaprevir):
    • Classification: Fixed-dose combination, HCV NS3/4A protease inhibitor and HCV NS5A inhibitor.
    • MOA: Inhibits HCV NS3/4A protease (cleavage of HCV-encoded polyprotein) and HCV NS5A (essential for viral RNA replication and virion assembly).
    • Metabolism & Excretion: Glecaprevir: liver, partially CYP3A4. Pibrentasivir: none. Glecaprevir excretion is in feces. Pibrentasivir excretion is in urine.
    • Side Effects: Liver failure, Angioedema, HBV reactivation, HA, Nausea, Diarrhea
  • Epclusa:
    • Classification: Combination of Sofosbuvir (HCV NS5B inhibitor) and Velpatasvir (HCV NS5A inhibitor).
    • MOA: Sofosbuvir inhibits the HCV NS5B polymerase. Velpatasvir inhibits the HCV NS5A protein. NS5A polymerase inhibitors interact with viral and host proteins. NS5B polymerase inhibitors interferes with the viral RNA polymerase.
    • Metabolism & Excretion: Sofosbuvir: liver extensively, CYP450 none. Prodrug converted to active form. Velpatasvir: liver CTYP 2B6, 2C8, 3A4. Sofosbuvir excretion is in urine (80%). Velpatasvir excretion is in feces/bile (94%).
    • Side Effects: HA, Diarrhea, Rash, Bradycardia, HBV reactivation, Angioedema, Nausea, Vomiting.

HIV Treatment

  • Viral Fusion Inhibitors:
    • MOA: Inhibits entry of viral RNA into host cell.
    • Drugs: Enfuvirtide
  • Attachment Co-receptor Inhibitors:
    • MOA: Inhibits entry of viral RNA into host cell by blocking interaction of viral proteins with co-receptors.
    • Drug: Maraviroc
  • NRTIs (Nucleoside Reverse Transcriptase Inhibitors):
    • MOA: Inhibit reverse transcriptase, stopping viral DNA production.
    • Drugs: Zidovudine, Abacavir, Emtricitabine, Stavudine, Didanosine, Lamivudine, Tenofovir.
  • NNRTIs (Non-Nucleoside Reverse Transcriptase Inhibitors):
    • MOA: Bind to and alter reverse transcriptase enzyme, stopping viral DNA production.
    • Drugs: Nevirapine, Efavirenz, Etravirine, Delavirdine, Rilpivirine

Protease Inhibitors

  • MOA: Inhibit protease, stopping the cleavage of polyproteins.
    • Drugs: Atazanavir, Darunavir, Indinavir, Lopinavir, Nelfinavir, Saquinavir, Tipranavir, Ritonavir.

Integrase Inhibitors

  • MOA: Inhibit integrase, preventing the incorporation of viral DNA with the human DNA.
    • Drugs: Dolutegravir, Raltegravir, Elvitegravir.

Respiratory Syncytial Virus (RSV)

  • Amantadine:
    • MOA: Dopamine drugs.
    • Admin: 100mg PO BID x 3-5 days
    • Side Effects: Ataxia, Seizures, Dizziness
  • Rimantadine:
    • MOA: Inhibits Inosine 5-phosphate dehydrogenase, preventing the formation of guanine nucleotides and RNA synthesis.
    • Admin: Same dose as Amantadine.
    • Side Effects: GI intolerance, Prolonged QT interval, seizures. etc.
  • Ribavirin:
    • MOA: Inhibits Inosine 5-phosphate dehydrogenase.
    • Admin: Aerosol
    • Side Effects: Teratogenic, Hemolytic Anemia

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