General

Pronunciation:
soe-fos-bue-vir


Trade Name(s)

  • Sovaldi

Ther. Class.
antivirals

Pharm. Class.
polymerase inhibitors

Indications

Treatment of chronic hepatitis C (CHC) infection (genotypes 1, 2, 3 and 4) in combination with ribavirin or ribavirin plus peginterferon alfa, including patients with hepatocellular carcinoma awaiting transplantation and those with HCV/HIV co-infection.

Action

Inhibits RNA-dependent RNA polymerase, resulting in inhibition of viral replication.

Therapeutic Effect(s):

Decreased HCV RNA levels with decreased severity and sequelae of HCV.

Pharmacokinetics

Absorption: Rapidly metabolized following absorption.

Distribution: Unknown.

Metabolism and Excretion: Extensively metabolized with much conversion to GS-461203, an active antiviral moiety, then converted GS-331007, which does not have antiviral activity. 80% excreted in urine mostly as GS-331007 (3.5% as unchanged drug), 14% excreted in feces, 2.5% excreted in expired air.

Half-life: Sofosbuvir– 0.4 hr; GS-331007– 27 hr.

TIME/ACTION PROFILE (blood levels)

ROUTEONSETPEAKDURATION
POunknown0.5–2 hr†24 hr
† Sofosbuvir (2–4 hr for GS-331007).

Contraindication/Precautions

Contraindicated in:

  • Contraindications for ribavirin and/or peginterferon alfa;
  • Severe renal impairment/end-stage renal disease;
  • Concurrent use of P-gp inducers, including rifampin and St. John's wort
  • OB: Pregnant women or men whose partners are pregnant (ribavirin may cause fetal harm)
  • Lactation:Discontinue sofosbuvir or discontinue breastfeeding.

Use Cautiously in:

  • Receiving immunosuppressant or chemotherapy medications (↑ risk of hepatitis B virus reactivation);
  • Rep: Women with childbearing potential and their male partners;
  • Pedi: Children <12 yr (safety and effectiveness not established).

Adverse Reactions/Side Effects

In combination with ribavirin

CNS: fatigue, headache, insomnia, irritability, weakness

GI: diarrhea, nausea

Derm: pruritus

MS: myalgia

Misc: chills, fever, hepatitis B virus reactivation

In combination with ribavirin and peginterferon alfa

CNS: fatigue, headache, insomnia, irritability, weakness

GI: diarrhea, nausea

Derm: rash, pruritus

Hemat: anemia

MS: myalgia

Misc: chills, fever, hepatitis B virus reactivation

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

  • Blood levels and effectiveness may be ↓ by concurrent use of carbamazepine , phenytoin , phenobarbital , oxcarbazepine , rifabutin , rifampin , rifapentine and tipranavir/ritonavir; avoid concurrent use.
  • Amiodarone may ↑ risk of symptomatic bradycardia when used with sofosbuvir and simeprevir; concurrent use not recommended; if amiodarone necessary, monitor patients in inpatient setting for first 48 hr of concomitant use and then monitor heart rate on outpatient basis for at least the first 2 wk of treatment (follow same monitoring procedure if discontinuing amiodarone immediately before initiation of sofosbuvir and simeprevir therapy)

Drug-Natural Products:

Blood levels and effectiveness may be ↓ by concurrent use of of P-gp inducers including St. John's wort ; avoid concurrent use.

Route/Dosage

PO: (Adults) Genotypes 1 or 4 (treatment-naïve without cirrhosis or with compensated cirrhosis [Child-Pugh A])– 400 mg once daily for 12 wk in combination with peginterferon alfa and ribavirin; Genotype 2 (treatment-naïve and treatment-experienced without cirrhosis or with compensated cirrhosis [Child-Pugh A])– 400 mg once daily for 12 wk in combination with ribavirin; Genotype 3 (treatment-naïve and treatment experienced without cirrhosis or with compensated cirrhosis [Child-Pugh A])– 400 mg once daily for 24 wk in combination with ribavirin; Patients with hepatocellular carcinoma awaiting liver transplantation– 400 mg once daily in combination with ribavirin for up to 48 wk or until transplantaion, whichever occurs first.

PO: (Children 12–17 yr or ≥35 kg): Genotype 2 (treatment-naïve and treatment-experienced without cirrhosis or with compensated cirrhosis [Child-Pugh A])– 400 mg once daily for 12 wk in combination with ribavirin; Genotype 3 (treatment-naïve and treatment experienced without cirrhosis or with compensated cirrhosis [Child-Pugh A])– 400 mg once daily for 24 wk in combination with ribavirin.

Availability

Tablets: 400 mg

Assessment

  • Monitor for signs and symptoms of chronic hepatitis C.
  • Monitor for signs and symptoms of hepatitis B reactivation (jaundice, dark urine, light colored stools, fatigue, weakness, loss of appetite, nausea, vomiting, stomach pain) during therapy.

Lab Test Considerations: A negative pregnancy test must be obtained immediately before beginning therapy and monthly thereafter.

  • Determine current or prior HBV infection by measuring hepatitis B surface antigen (HBsAg) and hepatitis B core antibody (anti-HBc) before initiating HCV therapy. In patients with HBV infection, monitor for clinical and laboratory signs of hepatitis flare or HBV reactivation (rapid ↑ in serum HBV DNA level) during HCV therapy and during post-therapy follow-up.
  • Monitor CBC periodically during therapy. If hemoglobin <10 g/dL in patients with no cardiac disease reduce ribavirin dose to 600 mg/day. If hemoglobin <8.5 g/dL, discontinue ribavirin. If ≥2 g/dL decrease in hemoglobin during any 4 wk treatment period in patient with history of stable cardiac disease, decrease ribavirin dose to 600 mg/day. If hemoglobin <12 g/dL despite 4 wk at reduced dose, discontinue ribavirin.
  • May cause pancytopenia and thrombocytopenia.
  • May cause ↑ bilirubin, creatine kinase, and serum lipase levels.

Potential Diagnoses

Implementation

  • Must be administered in conjunction with ribavirin or ribavirin plus peginterferon alfa. If ribavirin or ribavirin plus peginterferon alfa is/are discontinued, sofosbuvir must be discontinued.
  • PO: Administer once daily without regard to food.

Patient/Family Teaching

  • Instruct patient to take sofosbuvir with ribavirin or ribavirin plus pegainterferon alfa as directed. Take missed doses on same day on one day as soon as remembered; do not double doses. Advise patient to read Patient Information before starting and with each refill in case of changes.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. Johns Wort.
  • Rep: Advise female patients and male patients with female partners who are pregnant or may become pregnant to use effective contraception due to risks for birth defects and fetal death and avoid breastfeeding. Women and male partners must use 2 forms of non-hormonal contraception during and for at least 6 mo after discontinuation of therapy. Advise women who become pregnant to enroll in the Ribavirin Pregnancy Registry by calling 1-800-593-2214. For patients with HCV/HIV 1 co-infection taking antiretrovirals there is an Antiviral Pregnancy Registry at 1-800-258-4263.

Evaluation/Desired Outcomes

Decreased HCV RNA levels with decreased severity and sequelae of HCV.
  • Patients with genotype 1 and 4 chronic hepatitis C (CHC) should be treated with sofosbuvir, peginterferon alfa, and ribavirin for 12 wk.
  • Patients with genotype 2 CHC should be treated with sofosbuvir and ribavirin for 12 wk.
  • Patients with genotype 3 CHC should be treated with sofosbuvir and ribavirin for 24 wk.
  • Patients with hepatocellular cancer awaiting liver transplantation may be treated with sofosbuvir and ribavirin for up to 48 wk.
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TY - ELEC T1 - sofosbuvir ID - 110123 A1 - Quiring,Courtney, AU - Sanoski,Cynthia A, AU - Vallerand,April Hazard, BT - Davis's Drug Guide UR - https://nursing.unboundmedicine.com/nursingcentral/view/Davis-Drug-Guide/110123/all/sofosbuvir PB - F.A. Davis Company ET - 16 DB - Nursing Central DP - Unbound Medicine ER -