grazoprevir

Action and Spectrum

Actions and Spectrum: 

Action: 

grazoprevir is a medication used to treat hepatitis C (HCV) infection. It is an HCV NS3/4A protease inhibitor, which means it acts by inhibiting a specific enzyme involved in the replication of the hepatitis C virus. This action interferes with the virus’s ability to reproduce and spread in the body. 

Spectrum: 

The spectrum of grazoprevir is primarily focused on treating chronic hepatitis C virus (HCV) infection. It is effective against various genotypes of HCV, including genotype 1, one of the most common genotypes globally. The specific spectrum of activity can vary depending on the treatment regimen, as it is often combined with other antiviral medications, such as elbasvir. 

Drug Interaction

Adverse Reaction

Frequency not defined  

headache 

Insomnia 

Drowsiness 

Fatigue 

nausea 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: grazoprevir is contraindicated in patients with a known hypersensitivity or allergic reaction to the drug or any of its constituent elements. 

Concomitant Use of Certain Medications: There may be drug interactions between grazoprevir and other medications. Contraindications may exist when grazoprevir is used alongside specific drugs, so it is essential to consult with a healthcare provider to ensure compatibility with other medications. 

Severe Liver Impairment: grazoprevir’s use may be contraindicated in individuals with severe liver impairment. The degree of contraindication can vary based on the specific combination therapy being employed, so consultation with a healthcare professional is necessary. 

Pregnancy and Breastfeeding: As with many medications, the use of grazoprevir during pregnancy or breastfeeding is often not recommended. Consultation with a healthcare provider is crucial to weigh the potential risks and benefits on a case-by-case basis. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: grazoprevir is a medication used in the treatment of hepatitis C virus (HCV) infection 

Pharmacodynamics:  

grazoprevir is a direct-acting antiviral (DAA) agent, specifically classified as a protease inhibitor. It targets the non-structural protein 3/4A (NS3/4A) protease of the hepatitis C virus. By inhibiting this protease, grazoprevir interferes with the viral life cycle, preventing the production of infectious HCV particles. 

Pharmacokinetics: 

Absorption 

grazoprevir is well absorbed orally, with high bioavailability. It can be taken with or without food. 

Distribution 

It is primarily bound to plasma proteins, mainly albumin. 

Metabolism 

grazoprevir undergoes extensive hepatic metabolism, primarily via the cytochrome P450 (CYP) enzyme system. It is a substrate for CYP3A4 and CYP3A5. Concomitant use of strong CYP3A4 inducers or inhibitors may affect its metabolism and require dose adjustments. 

Excretion and Elimination 

grazoprevir is mainly excreted in the feces, with a smaller portion excreted in the urine. 

Adminstartion

Administration:  

The specific administration instructions for grazoprevir may vary depending on the patient’s individual condition, the presence of other medications, and the healthcare provider’s recommendations. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: grazoprevir 

Why do we use grazoprevir?  

grazoprevir is used to treat adults with chronic hepatitis C virus (HCV) infections, particularly those caused by HCV genotypes 1 and 4. It is used as part of a combination therapy along with other direct-acting antiviral drugs to achieve sustained virological response (SVR), which indicates the absence of detectable HCV in the blood and long-term cure.