Module 9 14 Antivirals Flashcards
Question
Answer
What is the primary focus of this chapter regarding antiviral drugs?
This chapter discusses antiviral drugs used to treat infections caused by viruses other than human immunodeficiency virus (HIV).
Where can you find information on the specific antiviral drugs for non-HIV infections?
Information on antiviral drugs for non-HIV infections is available in Table 80.1.
What does this section provide information about?
This section lists various antiviral drugs and their spectrum of activity against specific viruses.
Why are antiviral drugs more specific compared to antibiotics?
Antiviral drugs are more specific because they are designed to target particular viruses, whereas antibiotics are used to treat various bacterial infections.
How are the antiviral drugs categorized in this list?
Antiviral drugs are categorized based on the associated viral infections they are designed to treat.
What are HSV and VZV, and what group of viruses do they belong to?
HSV stands for Herpes Simplex Virus, and VZV stands for Varicella Zoster Virus. They belong to the herpesvirus group.
What infections are caused by HSV in the body?
HSV causes infections in various body sites, including the genitalia, mouth, face, and others.
What diseases are associated with VZV, and what is herpes zoster?
VZV is responsible for causing varicella (chickenpox) and herpes zoster (shingles). Herpes zoster is a painful condition resulting from the reactivation of dormant VZV in sensory nerve roots.
Who is primarily affected by varicella, and what kind of disease is it?
Varicella (chickenpox) primarily affects children and is a contagious viral disease.
In which chapters can you find more detailed information on these conditions?
More detailed information on these conditions can be found in Chapter 55 for varicella and Chapter 82 for genital herpes.
What is Acyclovir, and what types of viral infections is it commonly used to treat?
Acyclovir (Zovirax) is a medication used to treat infections caused by Herpes Simplex Virus (HSV) and Varicella Zoster Virus (VZV).
How can Acyclovir be administered for treatment?
Acyclovir can be administered topically, orally, and intravenously depending on the type and location of the viral infection.
Are serious side effects associated with Acyclovir?
Serious side effects from Acyclovir are uncommon.
Which viral family is Acyclovir effective against, and name some specific viruses within this family?
Acyclovir is effective against viruses in the herpesvirus family, including herpes simplex viruses (HSV), varicella zoster virus (VZV), and cytomegalovirus (CMV).
Among the viruses treated with Acyclovir, which one is the most sensitive to the drug?
Herpes simplex viruses (HSV) are the most sensitive to Acyclovir.
How does the sensitivity to Acyclovir vary among the different viruses in the herpesvirus family?
Varicella zoster virus (VZV) is moderately sensitive, while most strains of cytomegalovirus (CMV) are resistant to Acyclovir.
How does Acyclovir inhibit viral replication?
Acyclovir inhibits viral replication by suppressing the synthesis of viral DNA.
What is the initial step required for Acyclovir to become active against herpesviruses?
Acyclovir must be converted to acyclo-guanosine monophosphate (GMP) by the viral enzyme thymidine kinase.
How does acyclo-GMP exert its antiviral effects?
Acyclo-GMP is further converted to acyclo-guanosine triphosphate (GTP), which directly inhibits viral DNA synthesis.
Why are herpes simplex viruses (HSVs) highly sensitive to Acyclovir?
HSVs are sensitive to Acyclovir because the drug is a better substrate for thymidine kinase produced by HSVs compared to mammalian thymidine kinase, leading to preferential activation in HSV-infected cells.
Why is cytomegalovirus (CMV) inherently resistant to Acyclovir?
CMV is resistant to Acyclovir because the drug is a poor substrate for the thymidine kinase produced by CMV, resulting in limited drug activation.
How can herpesviruses develop resistance to acyclovir?
Herpesviruses can develop resistance to Acyclovir through three mechanisms: (1) decreased production of thymidine kinase, (2) alteration of thymidine kinase to prevent the conversion of Acyclovir to its active form, acyclo-GMP, and (3) modification of viral DNA polymerase to reduce sensitivity to inhibition.
What is the most common mechanism of resistance to acyclovir?
Thymidine kinase deficiency is the most common mechanism of resistance to Acyclovir.
Is resistance to acyclovir common in individuals with a healthy immune system?
Resistance to acyclovir is rare in individuals with a healthy immune system.
In which patient populations is resistance to acyclovir more commonly observed?
Resistance to acyclovir is more commonly observed in transplant recipients and patients with AIDS.
What alternative treatments are used for lesions caused by acyclovir-resistant herpesviruses?
Intravenous drugs like foscarnet or cidofovir are used to treat lesions caused by acyclovir-resistant herpesviruses.
Which herpes simplex virus (HSV) type is usually responsible for herpes infections of the face and oropharynx?
Herpes infections of the face and oropharynx are typically caused by HSV type 2 (HSV-2).
What is the treatment option for primary herpes infections of the gums and mouth in immunocompetent patients?
In immunocompetent patients, oral acyclovir can be used to treat primary infections of the gums and mouth.
How can oral acyclovir be used to prevent recurrent herpes labialis (cold sores)?
Oral acyclovir can be taken prophylactically to prevent episodes of recurrent herpes labialis (cold sores).
Is there a highly effective treatment for active herpes labialis?
No, there is no truly effective treatment for active herpes labialis.
What is the recommended treatment for severe mucocutaneous herpes infections in immunocompromised patients?
For severe mucocutaneous herpes infections in immunocompromised patients, intravenous acyclovir is the treatment of choice.
What is the recommended treatment for herpes zoster (shingles) in older adults?
High doses of oral acyclovir are effective for herpes zoster (shingles) in older adults.
Is oral acyclovir effective for varicella (chickenpox), and for which age groups?
Oral acyclovir is effective for varicella (chickenpox) in children, adolescents, and adults, as long as dosing is initiated early (within 24 hours of rash onset).
What is the preferred treatment for VZV infection in immunocompromised individuals?
Intravenous acyclovir is the treatment of choice for VZV infection in immunocompromised individuals.
Where can you find detailed information about the characteristics and treatment of genital HSV (herpes simplex virus) infection?
Detailed information about genital HSV infection can be found in Chapter 82.
In what forms can acyclovir be administered?
Acyclovir can be administered topically, orally, and intravenously.
What is the oral bioavailability of acyclovir?
The oral bioavailability of acyclovir is low, ranging from 15% to 30%.
Is there significant absorption of acyclovir through the skin when topically applied?
No, there is no significant absorption of acyclovir when applied topically.
What is the half-life of acyclovir in individuals with normal kidney function?
In individuals with normal kidney function, acyclovir has a half-life of 2.5 hours.
How does renal impairment affect the half-life of acyclovir?
Renal impairment can prolong the half-life of acyclovir, reaching 20 hours in patients with anuria.
What should be done with acyclovir dosages in patients with kidney disease?
Dosages of acyclovir should be reduced in patients with kidney disease.
What is the peak time for Valacyclovir (Valtrex) after administration?
The peak time for Valacyclovir is 1.5 hours.
What is the protein binding percentage for Acyclovir (Sitavig, Zovirax)?
The protein binding for Acyclovir is 9%-33%.
How is Acyclovir (Sitavig, Zovirax) metabolized?
Acyclovir is metabolized by cellular enzymes.
What is the half-life of Famciclovir (Famvir)?
The half-life of Famciclovir is 2-4 hours.
In which organs is Famciclovir eliminated?
Famciclovir is eliminated in the urine (73%) and feces (25%).
Is there any metabolism involved in the processing of Foscarnet (Foscavir)?
No, there is no metabolism involved in the processing of Foscarnet.
How is Valacyclovir (Valtrex) metabolized?
Valacyclovir is converted in the liver to acyclovir, which is then processed by cellular enzymes.
What are some common side effects associated with Acyclovir?
Common side effects of Acyclovir include nausea, vomiting, diarrhea, headache, and vertigo.
Is renal impairment associated with the use of Acyclovir?
No, renal impairment has not been reported with the use of Acyclovir.
What is one of the potential side effects of topical Acyclovir?
Topical Acyclovir may cause transient local burning or stinging.
Is Acyclovir considered safe for use during pregnancy?
Yes, oral Acyclovir is safe during pregnancy and can be used to suppress recurrent genital herpes near term in pregnant individuals.
What is the potential risk associated with intravenous (IV) Acyclovir?
IV Acyclovir can potentially cause renal failure.
Who is at increased risk of renal failure due to IV Acyclovir?
Patients with preexisting renal disease and dehydration are at an increased risk of experiencing this adverse effect.
What should patients be informed about regarding the use of Acyclovir?
Patients should be informed that Acyclovir only decreases symptoms of viral infections; it does not eliminate the virus and does not produce a cure.
What precaution should patients take when applying topical Acyclovir?
Patients should apply topical Acyclovir with a finger cot or rubber glove to prevent viral transfer to other body sites or other people.
What should patients be told about any transient local burning or stinging they may experience when using topical Acyclovir?
Patients should be told that transient local burning or stinging may occur when applying topical Acyclovir, but this is considered a normal reaction and not a cause for concern.
What is the recommended dosage of Acyclovir for orolabial HSV (herpes simplex virus)?
For orolabial HSV, the dosage of Acyclovir is to apply cream five times daily for 4 days when used topically.
How should Acyclovir be dosed for Varicella in children over 40 kg?
The dosage information for Acyclovir for Varicella in children over 40 kg is not provided.
At what age is Acyclovir approved for use in children?
Acyclovir is approved for children as young as 3 months of age.
What is the recommended age for using Valacyclovir in children?
Valacyclovir is approved for children 2 years of age.
Why is Foscarnet not recommended during pregnancy?
Foscarnet is not recommended during pregnancy because it has caused abnormal development of tooth enamel in animal studies.
For pregnant women, did epidemiologic reviews find a significant increase in abnormal outcomes with acyclovir, famciclovir, and valacyclovir use?
No, epidemiologic reviews did not find a significant increase in abnormal outcomes for pregnant women using acyclovir, famciclovir, and valacyclovir.
What are the breastfeeding recommendations for women taking systemic drugs for HSV and VZV?
Women taking systemic drugs for HSV and VZV are recommended to avoid breastfeeding due to the potential for serious adverse events in infants.
Why should older adults with renal impairment be cautious when taking acyclovir and valacyclovir?
Older adults with renal impairment should be cautious when taking acyclovir and valacyclovir because they are at greater risk for adverse CNS effects.
What is Acyclovir used for?
Acyclovir is used for HSV (Herpes Simplex Virus) infections.
Which drug is used for Cytomegalovirus (CMV) infections?
Ganciclovir is used for CMV (Cytomegalovirus) infections.
Name a nucleoside analog used for hepatitis.
Lamivudine is a nucleoside analog used for hepatitis.
What is the purpose of Simeprevir in hepatitis treatment?
Simeprevir is a protease inhibitor used for hepatitis.
Which drug is an NS5A inhibitor used for hepatitis?
Daclatasvir is an NS5A inhibitor used for hepatitis.
What is the function of Sofosbuvir in hepatitis treatment?
Sofosbuvir is an NS5B inhibitor used for hepatitis.
What type of drug is Peginterferon alfa-2a, and what is its use?
Peginterferon alfa-2a is an interferon used for hepatitis.
What is the purpose of the influenza vaccine?
The influenza vaccine is used to prevent influenza.
What is the role of Oseltamivir in influenza treatment?
Oseltamivir is a neuraminidase inhibitor used for influenza.
Which drug acts as an endonuclease inhibitor for influenza?
Baloxavir marboxil is an endonuclease inhibitor used for influenza.
What is the function of Palivizumab, and for which viral infection is it used as prophylaxis?
Palivizumab is a monoclonal antibody used for prophylaxis of Respiratory Syncytial Virus (RSV) infection.
What is Valacyclovir?
Valacyclovir is a prodrug form of acyclovir.
How does the effective bioavailability of acyclovir change when taking Valacyclovir orally?
Valacyclovir increases the effective bioavailability of acyclovir to about 55%.
What conditions is Valacyclovir approved for managing?
Valacyclovir is approved for managing:Herpes labialis (cold sores). Varicella (chickenpox). Herpes zoster infection (shingles). Herpes simplex genitalis (genital herpes).
In what situations is Valacyclovir sometimes used off-label?
Valacyclovir is sometimes used off-label for the prophylaxis of HSV (Herpes Simplex Virus), VZV (Varicella Zoster Virus), and CMV (Cytomegalovirus) infections in patients with cancer.
What is another use of Valacyclovir in cancer patients?
Valacyclovir is sometimes used to treat cancer-related HSV and VZV infections.
What syndrome has been observed in immunocompromised patients during clinical research on valacyclovir?
Clinical research has revealed the occurrence of a syndrome known as thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS).
Is TTP/HUS generally observed in immunocompetent patients?
No, TTP/HUS has not been observed in immunocompetent patients.
Why has the US Food and Drug Administration (FDA) not approved the use of valacyclovir in most immunocompromised patients?
The FDA has not approved valacyclovir for most immunocompromised patients due to the risk of TTP/HUS, except for chronic suppressive therapy for recurrent genital herpes in HIV-infected patients.
Despite FDA recommendations, are there increasing recommendations in the literature for valacyclovir use in immunocompromised patients?
Yes, there are increasing recommendations in the literature for valacyclovir use in immunocompromised patients, but caution is advised.
In clinical trials, what dose of valacyclovir was associated with the occurrence of TTP/HUS in immunocompromised patients?
TTP/HUS occurred in clinical trials when immunocompromised patients were receiving high doses of 8 g/day of valacyclovir.
What are some common side effects associated with valacyclovir, aside from TTP/HUS?
Common side effects of valacyclovir include nausea, vomiting, diarrhea, headache, and vertigo.
What is famciclovir, and how does it work?
Famciclovir is a prodrug of penciclovir, which inhibits viral DNA replication. It undergoes enzymatic conversion to penciclovir, and then to penciclovir triphosphate, its active form.
What is the role of penciclovir triphosphate in viral infections?
Penciclovir triphosphate inhibits viral DNA polymerase, preventing the replication of viral DNA.
How is the formation of penciclovir triphosphate facilitated within infected cells?
Formation of penciclovir triphosphate requires the action of viral thymidine kinase, limiting its effects to infected cells while sparing most host cells.
Against which viruses is penciclovir active in vitro?
Penciclovir exhibits in vitro activity against HSV type 1 (HSV-1), HSV-2, and VZV.
For what medical conditions is famciclovir approved for treatment?
Famciclovir is approved for the treatment of acute herpes zoster (shingles) and herpes simplex genitalis (genital herpes).
Does famciclovir reduce the incidence of postherpetic neuralgia in patients with herpes zoster?
No, famciclovir does not reduce the incidence of postherpetic neuralgia, but it can decrease its duration.
Is famciclovir well-tolerated by patients?
Yes, famciclovir is generally well tolerated.
What are the common side effects associated with famciclovir use?
Common side effects include headache and nausea and were reported by more than 10% of subjects in clinical trials.
Under what circumstances can acute renal failure occur due to famciclovir use?
Acute renal failure can occur when higher than recommended doses of famciclovir are administered.
How many topical drugs are used for the treatment of recurrent herpes labialis?
There are three topical drugs available.
Name two of the topical drugs used for treating herpes labialis.
Two of the drugs used for treating herpes labialis are penciclovir and docosanol.
What is the third drug used for treating herpes labialis?
The third drug used for treating herpes labialis is acyclovir.
What is penciclovir (Denavir) used to treat?
Penciclovir (Denavir) is used to treat recurrent herpes labialis, commonly known as cold sores.
Which types of herpes simplex viruses (HSV) is penciclovir effective against?
Penciclovir is effective against HSV-1 and HSV-2.
How does penciclovir work to suppress viral replication?
Penciclovir works by inhibiting the DNA polymerase enzyme responsible for viral DNA synthesis.