Hepatitis Pharmacology Flashcards
What is the specific treatment for hepatitis B?
- No specific treatment because it most often resolves spontaneoulsy
What are the goals of HBV therapies?
- Suppression of HBV DNA to undetectable levels
- Seroconversion of HBeAg (or more rarely, HBsAg) from positive to negative
- Reduction in elevated serum aminotransferase levels
What are the endpoints of HBV treatment?
- Improvement in necro-inflammatory disease
- A decreased risk of hepatocellular carcinoma and cirrhosis
- A decreased need for liver transplantation
What is Entecavir?
- A hepatitis B virus nucleoside analogue reverse transcriptase
What are the BB warnings for Entecavir?
- Severe acute exacerbations of hepatitis B
- Patients co-infected with HIV and HBV
- Lactic acidosis
- Hepatomegly
What are the indications of Entecavir?
- Indicated for the treatment of chronic hepatitis B virus infection in adults and children at least 2 years of age with evidence of active viral replication and either evidence of persistent elevations in serums aminotransferases or histologically active disease
What are some contraindications of Entecavir?
- None
What are some adverse reactions of Entecavir?
- In adults, most common are headache, fatigue, dizziness, and nausea
- Pediatric patient effects were consistent with those observed in adults
What is Tenofovir Disoproxil?
- A nucleotide analog HIV-1 reverse transcriptase inhibitor and an HBV reverse transcriptase inhibitor
What are the BB warnings for Tenofovir Disoproxil?
- Lactic acidosis/Severe hepatomegaly with steatosis
- Post treatment exacerbation of hepatitis
What are some indications of Tenofovir Disoproxil?
- Used in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients 2 years of age and older
- Used for the treatment of chronic hepatitis B in adults and pediatric patients 12 years of age and older
What are some warnings of Tenofovir Disoproxil?
- New onset or worsening renal impairment: Can include acute renal failure and Fanconi syndrome
What are some adverse reactions with Tenofovir Disoproxil?
- In HBV infected subjects with compensated liver disease: most common reaction was nausea
What is adefovir?
- Nucleotide analogue used for the treatment of chronic hepatitis B in patients 12 years of age or older
What are some contraindications of adefovir?
- In patients with previously demonstrated hypersensitivity to any of the components of the product
What are some warnings/precautions of adefovir?
- Nephrotoxicity: monitor renal function during therapy for all patients particularly those with pre-existing or other risks for renal impairment
- Severe acute exacerbations of hepatitis
What are some adverse reactions of adefovir?
- Most common is asthenia and increased creatinine in pre and post transplantation lamivudine-resistant liver disease patients
What are some drug interactions of adefovir?
- Coadministration with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of adefovir or the coadministered drug
What is lamivudine?
- Nucleoside analogue reverse transcriptase inhibitor
What are some BB warnings for lamivudine?
- Lactic acidosis
- Severe hepatomegaly
- Exacerbations of hepatitis B
- Different formulations
What are some indications of lamivudine?
- Used in combination with other antiretroviral agents for the treatment of HIV-1 infection
What are some contraindications of lamivudine?
- In patients with previous hypersensitivity reaction to lamivudine
What are some warnings and precautions of lamivudine?
- Co-infected HIV-1/HBV patients
- Emergence resistant HBV variants associated with lamivudine containing antiretroviral regimens has been reported. Monitor for treatment associated toxicities
- Pancreatitis: or other significant risk factors for pancreatitis. Discontinue treatment as clinically appropriate
What are some adverse reactions of lamivudine?
- The most common were headache, nausea, malaise and fatigue, nasal signs and symptoms, diarrhea, and cough
What is Telbivudine?
- Nucleoside analogue reverse transcriptase inhibitor
What are some BB warnings for telbivudine?
- Lactic acidosis
- Severe hepatomegaly with steatosis
- Severe acute exacerbations of hep B
What are some indications of telbivudine?
- Used for the treatment of chronic hepatitis B in adult patients with evidence of viral replication and either evidence of persistent elevations in serum aminotransferases or histologically active disease
What are some contraindications of telbivudine?
- Combination of telbivudine with PEGylated interferon alfa-2a: increased risk of peripheral neuropathy
What are some adverse reactions of telbivudine?
- Most common: Fatigue, increased creatine kinase, headache, cough, diarrhea, abdominal pain, nausea, arthralgia, pyrexia, rash, back pain, dizziness, myalgia, ALT increase, dyspepsia, insomnia, and abdominal distention
What is the BB warning of PEG interferon alfa-2a?
- Risk of serious disorders and ribavirin associated effects
What are the indications of PEG interferon alfa-2a?
- Treatment of chronic hepatitis C with compensated liver disease not previously treated with interferon alpha, in patients with histological evidence of cirrhosis and compensated liver disease
- Treatment of patients with chronic hepatitis B infection who have compensated and evidence of viral replication and liver inflammation
What are some contraindications of PEG interferon alfa-2a?
- Autoimmune hepatitis
- Hepatic decompensation in patients with cirrhosis
- Use in neonates/infant
What are some adverse reactions?
- Most common are fatigue/astehnia, pyrexia, myalgia, and headache
What is BB warning of PEG interferon alfa-2b?
- Can cause or aggravate fatal or life-threatening neuropsychiatric, autoimmune, ischemic, and infectious disorders
What are some indications of PEG interferon alfa-2b?
- Used for the treatment of chronic hepatitis C in patients 18 years or older with compensated liver disease who have a history of blood or blood-product exposure and/or are HCV antibody positive
What are some contraindications of PEG interferon alfa-2b?
- Hypersensitivity to interferon alpha or any component of the product
- Autoimmune hepatitis
- Decompensated liver disease
What are some adverse reactions of PEG interferon alfa-2b?
- Most frequently reported were “flu-like” symptoms, fever, headache, chills, nausea, and fatigue
What is the goal of HCV treatment?
- Viral eradication
What are some indications of Elbasvir/grazoprevir?
- A fixed dose combination product containing:
- Elbasvir, a hepatitis NS5A inhibitor
- Grazoprevir, an HCV NS3/4A protease inhibitor used in the treatment of HCV
What are some contraindications of Elbasvir/grazoprevir?
- Patients with moderate of severe hepatic impairment
What are some warnings and precautions of Elbasvir/grazoprevir?
- ALT elevations
What are some adverse reactions of Elbasvir/grazoprevir?
- Fatigue, headache, and nausea
What are some drug interactions of Elbasvir/grazoprevir?
- Co-administration with moderate CYP3A4 inducers is not recommended as they may decrease the plasma concentration of Elbasvir/grazoprevir
What is ledipasvir/sofosbuvir?
- A fixed dose combination of:
- Ledipasvir, a hep C NS5A inhibitor
- Sofosbuvir, an HCV nucleotide analog NS5B polymerase inhibitor
What are the indications of ledipasvir/sofosbuvir?
- Treatment of chronic hepatitis C infection in adults
What are the warnings of ledipasvir/sofosbuvir?
- Only recommended with some combination of ribavirin
What are some adverse reactions of ledipasvir/sofosbuvir?
- Fatigue and headache
What are some drug interactions of ledipasvir/sofosbuvir?
- Poly Glycoprotein inducers (St. John’s wort) may alter concentrations of ledipasvir and sofosbuvir»not recommended
What is velpatasvir/sofosbuvir?
- Fixed dose combination of:
- Sofosbuvir: A hepatitis C virus nucleotide analog NS5B polymerase inhibitor
- Velpatasvir: HCV NS5A inhibitor
What are the indications of velpatasvir/sofosbuvir?
- Treatment of adult patients with chronic HCV infection
- Without cirrhosis or with compensated cirrhosis
- With decompensated cirrhosis for use in combination with ribavirin
What are the contraindications of velpatasvir/sofosbuvir?
- Patients for whom ribavirin is contraindicated
What are some warnings of velpatasvir/sofosbuvir?
- Can potentiate bradycardia with amiodarone co-administration
- Caution also in patients receiving beta blockers or those with underlying cardiac comorbidities and/or advanced liver disease
What are some adverse reactions of velpatasvir/sofosbuvir?
- Headache and fatigue
What are some drug interactions of velpatasvir/sofosbuvir?
- PGP inducers and/or moderate to potent CYP inducers
- May decrease concentrations of sofosbuvir and/or velpatasvir
What are some BB warnings of ribivarin?
- Risk of serious disorders and ribavirin associated effects
- Birth defects and fetal death with ribavirin. Do not use in pregnancy and for 6 months after treatment
What are some indications of ribavirin?
- Nucleoside analogue indicated for the treatment of chronic hepatitis C virus infection in combination with interferon alfa-2a in patients 5 years and older with compensated liver disease not previously treated with interferon alpha and used in CHC patients co-infected with HIV
What are some contraindications of ribavirin?
- Pregnant women and men whose female partners are pregnant
- Hemnoglobinopathies
What are some adverse reactions of ribavirin?
- Most common adverse reactions are fatigue/asthenia, pyrexia, myalgia, and headache
What is boceprevir?
- NS3/4A protease inhibitor indicated for the treatment of chronic hepatitis C infection in combination with peginterferon alfa and ribavirin, in adults with compensated liver disease, including cirrhosis, who are previously untreated or who have failed previous interferon and ribavirin therapy
What are some contraindications of boceprevir?
- All contraindications to peginterferon alfa and ribavirin also apply since boceprevir must be administered with peginterferon alfa and ribavirin
What are some warnings of boceprevir?
- Use of boceprevir with ribavirin and peginterferon alfa:
- Ribavirin may cause birth defects and fetal death; avoid pregnancy in female patients and female partners of male patients
What are some adverse reactions of boceprevir?
- Fatigue
- Anemia
- Nausea
- Headache
- Dysgeusia
What does the ending “previr” mean?
- NS3/4A protease inhibitor
What does the ending “asvir” mean?
- NS5A inhibitor
What does the ending “buvir” mean?
- NS5B polymerase inhibitor
