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| {{intro}} | | {{Short description|Overview of the medication Dasabuvir}} |
| Viekira Pak is a combination of oral antiviral agents that is used to treat chronic hepatitis C, genotype 1.
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| | '''Dasabuvir''' is an [[antiviral drug]] used in the treatment of [[hepatitis C]]. It is a non-nucleoside inhibitor of the [[hepatitis C virus]] (HCV) [[RNA polymerase]], specifically targeting the NS5B protein. Dasabuvir is commonly used in combination with other antiviral agents to enhance its efficacy in clearing the virus from the body. |
| This combination has been associated with a low rate of serum enzyme elevations during therapy, and has been reported to cause rare cases of clinically apparent liver injury with jaundice and may result in hepatic decompensation in some patients with preexisting cirrhosis.
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| | ==Mechanism of Action== |
| The hepatitis C virus is a small RNA virus that is a major cause of chronic hepatitis, cirrhosis and hepatocellular carcinoma in the United States as well as worldwide. Various approaches to antiviral therapy of chronic hepatitis C have been developed, starting in the 1980s with interferon alfa which was replaced in the 1990s by long acting forms of interferon (peginterferon), to which was added the oral nucleoside analogue, ribavirin. Between 2010 and 2015, several potent oral, direct acting anti-HCV agents were developed and combinations of these found to have marked activity against the virus, allowing for highly effective and well tolerated therapy without use of interferon and with treatment courses of 8, 12 or 24 weeks only.
| | Dasabuvir works by inhibiting the NS5B RNA-dependent RNA polymerase, an enzyme crucial for the replication of the hepatitis C virus. By binding to the polymerase, dasabuvir prevents the virus from replicating its RNA, thereby reducing the viral load in the patient's body. |
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| | ==Clinical Use== |
| [[Viekira Pak]] (vee kee' rah pak) is the commercial name for a combination of oral, direct acting antiviral agents used to treat chronic hepatitis C associated with HCV genotype 1. The hepatitis C virus (HCV) encodes several nonstructural (NS) polypeptides that are essential for its replication: NS3/4 that has protease and helicase activities, NS5A that is a membrane bound polypeptide that is essential in the creation of the replicative complex, and NS5B an HCV specific, RNA-dependent, RNA polymerase. These polypeptides are effective targets for antiviral therapy of hepatitis C. Viekira Pak is a combination paritaprevir (par’ i ta’ pre veer: formerly ABT-450) which is a potent HCV NS3/4 protease inhibitor, ombitasvir (om bit’ as veer: ABT-267) an NS5A replication complex inhibitor, and dasabuvir (da sa’ bue veer: ABT-333) a nonnucleoside HCV RNA polymerase [NS5B] inhibitor. Paritaprevir is metabolized by CYP 3A4 and is typically given in combination with low doses of ritonavir, an inhibitor of CYP 3A4, to achieve higher and more prolonged drug levels which allow for once daily dosing. In cell culture and in humans infected with HCV, each of the agents has potent activity against HCV, but development of antiviral resistance rapidly arises with continued exposure. The combination of several direct acting agents with different molecular targets allows for a sustained viral suppression while avoiding antiviral resistance. | | Dasabuvir is primarily used in combination with other antiviral medications, such as [[ombitasvir]], [[paritaprevir]], and [[ritonavir]], in a regimen known as the "3D regimen" or "Viekira Pak." This combination therapy is effective against genotype 1 of the hepatitis C virus, which is the most common genotype in many parts of the world. |
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| | ==Administration== |
| The combination of these three agents (and ritonavir) with and without ribavirin (an antiviral nucleoside analogue with activity against HCV) has been shown to be very effective in suppressing HCV replication in patients infected with HCV genotype 1, and to result in a sustained virological response (SVR) and eradication of HCV in more than 90% of patients when given for 12 weeks or more. | | Dasabuvir is administered orally, typically in the form of tablets. The dosage and duration of treatment depend on the specific combination regimen and the patient's genotype and liver function status. |
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| | ==Side Effects== |
| Viekira Pak was approved for use in the United States in 2015, the second all-oral antiviral combination to receive approval for chronic hepatitis C. It is available as two tablets, one being the fixed combination of ombitasvir (12.5 mg), paritaprevir (75 mg) and ritonavir (100 mg) which is given once daily, and the other being dasabuvir (250 mg) which is given twice daily with meals.
| | Common side effects of dasabuvir include fatigue, nausea, itching, and insomnia. More serious side effects can occur, especially when used in combination with other drugs, and may include liver dysfunction and allergic reactions. |
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| | ==Pharmacokinetics== |
| Ribavirin (if a part of the combination therapy as is recommended for genotype 1a and for patients with cirrhosis) is available in tablets of 200 mg and is given twice daily for a total dose of 1,000 mg (if body weight is <75 kg) or 1,200 mg (if body weight ≥75 kg). Current indications for Viekira Pak (the combination of dasabuvir, ombitasvir and paritaprevir with ritonavir: D-O-P/r) are limited to patients with HCV genotype 1. The combination of just ombitasvir and paritaprevir with ritonavir (O-P/r) is also available under the commercial name Technive and is approved for use in combination with ribavirin in patients with chronic hepatitis C, genotype 4, without cirrhosis. Side effects of Viekira Pak and Technive are uncommon, but are generally mild and can include nausea, itching, rash, cough and insomnia. When given with ribavirin, side effects are greater, but are largely due to the hemolysis, nasal congestion and skin reactions that are common with that agent.
| | Dasabuvir is metabolized in the liver and excreted primarily in the feces. Its pharmacokinetic profile is influenced by factors such as liver function and the presence of other medications. |
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| | ==Related pages== |
| | * [[Hepatitis C]] |
| | * [[Antiviral drug]] |
| | * [[RNA polymerase]] |
| | * [[NS5B protein]] |
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| | [[Category:Antiviral drugs]] |
| | [[Category:Hepatitis C treatments]] |
Overview of the medication Dasabuvir
Dasabuvir is an antiviral drug used in the treatment of hepatitis C. It is a non-nucleoside inhibitor of the hepatitis C virus (HCV) RNA polymerase, specifically targeting the NS5B protein. Dasabuvir is commonly used in combination with other antiviral agents to enhance its efficacy in clearing the virus from the body.
Mechanism of Action
Dasabuvir works by inhibiting the NS5B RNA-dependent RNA polymerase, an enzyme crucial for the replication of the hepatitis C virus. By binding to the polymerase, dasabuvir prevents the virus from replicating its RNA, thereby reducing the viral load in the patient's body.
Clinical Use
Dasabuvir is primarily used in combination with other antiviral medications, such as ombitasvir, paritaprevir, and ritonavir, in a regimen known as the "3D regimen" or "Viekira Pak." This combination therapy is effective against genotype 1 of the hepatitis C virus, which is the most common genotype in many parts of the world.
Administration
Dasabuvir is administered orally, typically in the form of tablets. The dosage and duration of treatment depend on the specific combination regimen and the patient's genotype and liver function status.
Side Effects
Common side effects of dasabuvir include fatigue, nausea, itching, and insomnia. More serious side effects can occur, especially when used in combination with other drugs, and may include liver dysfunction and allergic reactions.
Pharmacokinetics
Dasabuvir is metabolized in the liver and excreted primarily in the feces. Its pharmacokinetic profile is influenced by factors such as liver function and the presence of other medications.
Related pages
