Loprolol

Loprolol Uses, Dosage, Side Effects, Food Interaction and all others data.

Ombitasvir is a direct acting antiviral medication used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients . Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) such as Ombitasvir. Ombitasvir is an inhibitor of NS5A, a protein essential for viral replication and virion assembly . The barrier for develoment of resistance to NS5A inhibitors is lower than that of NS5B inhibitors, another class of DAAs .

In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) recommend Ombitasvir as a first line therapy option when used in combination with other antivirals for genotypes 1a, 1b, and 4 . Depending on the genotype, Ombitasvir is often used in combination with other antivirals such as Dasabuvir, Paritaprevir, Ritonavir, and Ribavirin with the intent to cure, or achieve a sustained virologic response (SVR), after 12 weeks of daily therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality . Treatment with direct acting antivirals such as Ombitasvir is associated with very minimal side effects, with the most common being headache and fatigue . Lack of significant side effects and short duration of therapy is a considerable advantage over older interferon-based regimens, which were limited by infusion site reactions, reduced blood count, and neuropsychiatric effects .

Ombutasvir first came on the market as a fixed-dose combination product with Dasabuvir, Paritaprevir, and Ritonavir as the FDA-approved product Viekira Pak. First approved in December 2014, Viekira Pak is indicated for the treatment of HCV genotype 1b without cirrhosis or with compensated cirrhosis, and when combined with Ribavirin for the treatment of HCV genotype 1a without cirrhosis or with compensated cirrhosis.

Paritaprevir is a direct acting antiviral medication used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients . Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) such as paritaprevir. As a newer generation and directly acting HCV antiviral, paritaprevir products have better Sustained Virological Response (SVR) rates, higher barriers to resistance, fewer side effects, and a reduced pill burden compared to older agents such as Boceprevir, Telaprevir, Peginterferon alfa-2a, Peginterferon alfa-2b, and Ribavirin. By combining multiple antiretroviral medications into fixed dose products, the viral lifecycle can be targeted at multiple stages while simultaneously reducing the risk of developing resistant viral strains . Within Canada and the United States, paritaprevir is currently available in three fixed dose products: Viekira Pak (FDA), Technivie (FDA and Health Canada), and Holkira Pak (Health Canada).

More specifically, paritaprevir prevents viral replication by inhibiting the NS3/4A serine protease of Hepatitis C Virus (HCV) . Following viral replication of HCV genetic material and translation into a single polypeptide, Nonstructural Protein 3 (NS3) and its activating cofactor Nonstructural Protein 4A (NS4A) are responsible for cleaving genetic material into the following structural and nonstructural proteins required for assembly into mature virus: NS3, NS4A, NS4B, NS5A, and NS5B . By inhibiting viral protease NS3/4A, paritaprevir therefore prevents viral replication and function.

In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) recommend Paritaprevir as a first line therapy option when used in combination with other antivirals for genotypes 1a, 1b, and 4. Depending on the genotype, Paritaprevir is often used in combination with other antivirals such as Ombitasvir, Dasabuvir, Ritonavir, and Ribavirin, with the intent to cure, or achieve a sustained virologic response (SVR), after 12 weeks of daily therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality . Treatment with direct acting antivirals such as paritaprevir is associated with very minimal side effects, with the most common being headache and fatigue . Lack of significant side effects and short duration of therapy is a considerable advantage over older interferon-based regimens, which were limited by infusion site reactions, reduced blood count, and neuropsychiatric effects .

Trade Name Loprolol
Generic ombitasvir + paritaprevir + ritonavir and dasabuvir
Weight 100mg
Type Tablet
Therapeutic Class
Manufacturer Ikapharmindo Putramas
Available Country Indonesia
Last Updated: September 19, 2023 at 7:00 am
Loprolol
Loprolol

Uses

Ombitasvir is a direct acting antiviral agent used in combination with other antiviral agents for the treatment of Hepatitis C Virus (HCV) infections.

When used in combination with Paritaprevir and Ritonavir (as the fixed dose product Technivie), Ombitasvir is indicated in combination with Ribavirin for the treatment of patients with genotype 4 chronic hepatitis C virus (HCV) infection without cirrhosis .

When used in combination with Paritaprevir, Ritonavir, and Dasabuvir (as the fixed dose product Viekira Pak), Ombitasvir is indicated for the treatment of HCV genotype 1b and ,when combined with Ribavirin, for the treatment of HCV genotype 1a

Paritaprevir is a direct acting antiviral agent used in combination with other antiviral agents for the treatment of Hepatitis C Virus (HCV) infections.

When used within the fixed-dose combination product with Ombitasvir, Dasabuvir, and Ritonavir as the FDA-approved product Viekira Pak, paritaprevir is indicated for the treatment of HCV genotype 1b without cirrhosis or with compensated cirrhosis, and when combined with Ribavirin for the treatment of HCV genotype 1a without cirrhosis or with compensated cirrhosis.

When used within the fixed-dose combination product with Ombitasvir and Ritonavir as the FDA- and Health Canada-approved product Technivie, paritaprevir is indicated in combination with Ribavirin for the treatment of patients with genotype 4 chronic hepatitis C virus (HCV) infection without cirrhosis or with compensated cirrhosis.

When used within the fixed-dose combination product with Ombitasvir, Dasabuvir, and Ritonavir as the Health Canada-approved, commercially available product Holkira Pak, paritaprevir is indicated for the treatment of HCV genotype 1b with or without cirrhosis, and when combined with Ribavirin for the treatment of HCV genotype 1a with or without cirrhosis.

Loprolol is also used to associated treatment for these conditions: Chronic hepatitis C genotype 1a, Chronic hepatitis C genotype 1b, Chronic hepatitis C genotype 4 without cirrhosisChronic hepatitis C genotype 1a with compensated cirrhosis, Chronic hepatitis C genotype 1a without cirrhosis, Chronic hepatitis C genotype 1b with compensated cirrhosis, Chronic hepatitis C genotype 1b without cirrhosis, Chronic hepatitis C genotype 4 without cirrhosis

How Loprolol works

Ombitasvir is an inhibitor of the HCV non-structural protein 5A. While the precise role of this protein is unknown, it is essential to viral replication and virion assembly . Potential modes of action of NS5A inhibitors like Elbasvir include blocking signaling interactions, redistribution of NS5A from the endoplasmic reticulum to the surface of lipid droplets, and modification of the HCV replication complex .

Paritaprevir is a potent inhibitor of the NS3/4A serine protease of Hepatitis C Virus (HCV) . Following viral replication of HCV genetic material and translation into a single polypeptide, Nonstructural Protein 3 (NS3) and its activating cofactor Nonstructural Protein 4A (NS4A) are responsible for cleaving it into the following structural and nonstructural proteins required for assembly into mature virus: NS3, NS4A, NS4B, NS5A, and NS5B. By inhibiting viral protease NS3/4A, paritaprevir therefore prevents viral replication and function.

Toxicity

The most common adverse effects of Viekira Pak either in combination with or without Ribavirin were pruritus, nausea, insomnia, and asthenia . The most common adverse effects of Technivie with or without Ribavirin were asthenia, fatigue, nausea, insomnia and pruritus .

Volume of Distribution

Ombitasvir has a volume of distribution at steady state of 173 liters .

Volume of distribution at steady state is approximately 103 L .

Elimination Route

Ombitasvir reaches peak plasma concentration 5 hours after administration . It has an absolute bioavailability of 48%. Taking ombitasvir with high or normal fat meals increases exposure by 1.76 or 1.82 fold respectively.

Tmax of approximately 4 to 5 hours with a maximum concentration (Cmax) of 194 ng/mL .

Half Life

Ombitasvir has a half life of elimination of 21-25 hours

5.5 hr

Clearance

Clearance of Ombitasvir has not been determined.

Elimination Route

Ombitasvir is mainly excreted in the feces (90.2%) with very little excreted in the urine (1.91%) . 87.8% and 0.03% of the dose excreted in the feces and urine respectively is present as the parent compound.

Following a single dose administration of 14C-paritaprevir co-dosed with 100 mg of ritonavir, approximately 88% of the radioactivity was recovered in feces with limited radioactivity (8.8%) in urine; unchanged paritaprevir accounted for 1.1% of the radioactivity in the feces and 0.05% in the urine .

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