Ribavirin ADME

Stable Identifier
R-HSA-9755088
DOI
Type
Pathway
Species
Homo sapiens
Compartment
ReviewStatus
5/5
Locations in the PathwayBrowser
General
SVG |   | PPTX  | SBGN
Click the image above or here to open this pathway in the Pathway Browser

Ribavirin (RBV) is a synthetic nucleoside analog structurally related to guanine. It is given orally as part of the treatment of HCV infection, and by inhalation for the treatment of RSV infection. According to the WHO, ribavirin can also be used for the treatment of viral hemorrhagic fevers (WHO 2015).
RBV is administered orally in doses of 400 to 600 mg. It is highly soluble in water and a typical dose is dissolved completely over a wide range of acidities. RBV is rapidly absorbed into the circulation. After the oral administration of 600 mg radiolabeled ribavirin, approximately 61% of the drug was detected in the urine and 12% was detected in the feces. 17% of an administered dose was in unchanged form. RBV accumulates in human erythrocytes and remains in the body for weeks, with a halflife of >100 hours (Goodarzi et al, 2016). A consequence of the accumulation in erythrocytes is the well-known side effect of hemolytic anemia, which is reversible by cessation of administration (FDA label Rebetol, 2013).
Ribavirin is a prodrug. It is metabolized through two different paths: phosphorylation, yielding the active triphosphate (RBV-TP), and degradation via de-ribosylation and hydrolysis of the amide group. The GI tract, and not the liver, appears to be the major site of first-pass elimination (Dixit and Perelson, 2006).

Literature References
PubMed ID Title Journal Year
  HIGHLIGHTS OF PRESCRIBING INFORMATION

Food and Drug Administration, FDA

   
26952879 Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Ribavirin

Polli, JE, Mehta, MU, Langguth, P, Abrahamsson, B, Shah, VP, Goodarzi, N, Groot, DW, Cristofoletti, R, Dressman, JB, Barazesh Morgani, A

J Pharm Sci 2016
16501888 The metabolism, pharmacokinetics and mechanisms of antiviral activity of ribavirin against hepatitis C virus

Dixit, NM, Perelson, AS

Cell Mol Life Sci 2006
  World Health Organization model list of essential medicines: 21st list 2019. No. WHO/MVP/EMP/IAU/2019.06

World Health Organization, WHO

   
Participants
Participates
Orthologous Events
Cross References
PharmGKB
Authored
Reviewed
Created
Cite Us!