Select a medication above to begin.
Zepatier
elbasvir/ grazoprevir
Black Box Warnings .
Hepatitis B Reactivation
test all patients for currrent or prior HBV infection before starting tx; reported in HCV/HBV co-infected patients on or those who completed HCV direct-acting antiviral tx who were not on anti-HBV tx, including cases resulting in fulminant hepatitis, hepatic failure, and death; screen all patients for HBV infection before initial tx; monitor for hepatitis flare or signs/symptoms of HBV reactivation during tx and after D/C; initiate anti-HBV tx if needed
Adult Dosing .
Dosage forms: TAB: 50 mg/100 mg
hepatitis C infection, chronic
- [genotype 1]
- Dose: 1 tab PO qd x12wk or x16wk; Info: screen for NS5A polymorphism in patients with genotype 1a; duration depends on genotype subtype, prior tx; may give with ribavirin if tx-experienced; refer to AASLD/IDSA hepatitis C guidelines
- [genotype 4]
- Dose: 1 tab PO qd x12wk; Info: duration depends on prior tx; refer to AASLD/IDSA hepatitis C guidelines
renal dosing
- [see below]
- renal impairment: no adjustment
- HD: no adjustment; no supplement; PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B or C: contraindicated
Peds Dosing .
- Dosage forms: TAB: 50 mg/100 mg
chronic hepatitis C infection, genotype 1
- [12 yo and older, >30 kg]
- Dose: 1 tab PO qd x12wk or x16wk; Info: screen for NS5A polymorphism in patients with genotype 1a; duration depends on genotype subtype, prior tx; may give with ribavirin if tx-experienced
chronic hepatitis C infection, genotype 4
- [12 yo and older, >30 kg]
- Dose: 1 tab PO qd x12wk or x16wk; Info: duration depends on prior tx; may give with ribavirin if tx-experienced
renal dosing
- [see below]
- renal impairment: no adjustment
- HD: no adjustment; no supplement; PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B or C: contraindicated
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- hepatic impairment, Child-Pugh Class B-C
- hepatic decompensation history
- avoid: breastfeeding (patients with cracked nipple or bleeding nipple)
- caution: elderly patients
- caution: Asian patients (incr. risk of LFT abnormalities or hand-foot syndrome)
- caution: HBV carriers
- caution: HCV infection and HBV infection, concurrent
- caution: hepatic decompensation risk
- caution: hepatocellular carcinoma
- caution: alcohol abuse
- caution: immunosuppressed patients
- caution: diabetes mellitus
Drug Interactions .
Overview
elbasvir
direct-acting antiviral
- CYP3A4 substrate
- BCRP inhibitor
- caution advised with narrow therapeutic index drugs extensively metabolized in the liver; viral eradication may improve hepatic metabolic function, decr. levels, efficacy of concomitant drugs
- monitor glucose with drugs used for diabetes tx; viral eradication may change hepatic function, alter blood glucose control resulting in serious symptomatic hypoglycemia
grazoprevir
direct-acting antiviral
- CYP3A4 substrate
- OATP1B1 substrate
- OATP1B3 substrate
- CYP3A4 inhibitor, weak
- BCRP inhibitor
- caution advised with narrow therapeutic index drugs extensively metabolized in the liver; viral eradication may improve hepatic metabolic function, decr. levels, efficacy of concomitant drugs
- monitor glucose with drugs used for diabetes tx; viral eradication may change hepatic function, alter blood glucose control resulting in serious symptomatic hypoglycemia
Contraindicated
- apalutamide
- atazanavir
- belumosudil
- bempedoic acid
- butalbital
- carbamazepine
- cisapride
- clarithromycin
- clopidogrel
- cyclosporine
- darolutamide
- darunavir
- efavirenz
- elexacaftor/tezacaftor/ivacaftor
- eliglustat
- eltrombopag
- eluxadoline
- enasidenib
- encorafenib
- enzalutamide
- erythromycin
- fosphenytoin
- fostemsavir
- gemfibrozil
- glecaprevir
- irbesartan
- ivosidenib
- leflunomide
- leniolisib
- letermovir
- lopinavir/ritonavir
- lumacaftor/ivacaftor
- midostaurin
- mitotane
- pentobarbital
- phenobarbital
- phenytoin
- pibrentasvir
- primidone
- resmetirom
- rifabutin
- rifampin
- rilzabrutinib
- ritonavir
- sacubitril
- St. John's wort
- teriflunomide
- tipranavir
- vadadustat
- velpatasvir
- voclosporin
- voxilaprevir
Avoid/Use Alternative
- adagrasib
- alpelisib
- alprazolam
- bosentan
- ceftobiprole
- cenobamate
- ceritinib
- chloramphenicol
- cladribine oral
- cobicistat
- codeine
- colchicine
- dabrafenib
- etravirine
- fexinidazole
- fosamprenavir
- hydrocodone
- idelalisib
- itraconazole
- ketoconazole
- levoketoconazole
- lonafarnib
- lorlatinib
- mavacamten
- meperidine
- mifepristone
- mitapivat
- modafinil
- nafcillin
- nefazodone
- nelfinavir
- oxycodone
- pacritinib
- pazopanib
- pexidartinib
- pimozide
- posaconazole
- pralsetinib
- pretomanid
- propafenone
- repotrectinib
- ribociclib
- rifapentine
- simvastatin
- sotorasib
- topotecan
- tucatinib
- voriconazole
Monitor/Modify Tx
- abemaciclib
- acalabrutinib
- alfentanil
- amiodarone
- atorvastatin
- avanafil
- avapritinib
- brigatinib
- capivasertib
- clozapine
- disopyramide
- docetaxel
- dofetilide
- domperidone
- entrectinib
- eplerenone
- everolimus
- fedratinib
- felodipine
- fentanyl
- finerenone
- flibanserin
- fluvastatin
- gepirone
- ibrutinib
- ivabradine
- ixabepilone
- lapatinib
- lemborexant
- lomitapide
- lovastatin
- lumateperone
- lurasidone
- lurbinectedin
- methotrexate
- midazolam
- mobocertinib
- nifedipine
- nimodipine
- nisoldipine
- oliceridine
- pemigatinib
- quinidine (antiarrhythmic)
- red yeast rice
- riociguat
- rivaroxaban
- rosuvastatin
- selpercatinib
- sirolimus
- sirolimus albumin-bound
- sufentanil
- tacrolimus
- tadalafil
- talazoparib
- taletrectinib
- temsirolimus
- tenofovir alafenamide
- tenofovir disoproxil
- tolvaptan
- triazolam
- ubrogepant
- vardenafil
- venetoclax
- vinblastine
- vincristine
- vinorelbine
- warfarin
- zanubrutinib
Caution Advised
- aprepitant
- armodafinil
- artemether/lumefantrine
- avacopan
- belzutifan
- berotralstat
- bexarotene
- cariprazine
- ciprofloxacin
- clobazam
- clofazimine
- cobimetinib
- conivaptan
- crizotinib
- cyclophosphamide
- danazol
- danshen
- daridorexant
- dexamethasone
- dicloxacillin
- dihydroergotamine
- diltiazem
- dronedarone
- duvelisib
- echinacea
- elafibranor
- elagolix
- elinzanetant
- ergotamine
- eslicarbazepine acetate
- felbamate
- fluconazole
- garlic
- ginkgo
- ginseng, Asian
- glycerol phenylbutyrate
- grapefruit
- griseofulvin
- imatinib
- isavuconazonium
- lefamulin
- lenacapavir
- meropenem
- methylergonovine
- netupitant
- nevirapine
- nilotinib
- nirogacestat
- odevixibat
- olutasidenib
- omaveloxolone
- oxcarbazepine
- palovarotene
- perampanel
- pioglitazone
- roflumilast
- roflumilast topical
- rufinamide
- sarilumab
- seladelpar
- sirolimus topical
- stiripentol
- sulfasalazine
- sunvozertinib
- suzetrigine
- tazemetostat
- tecovirimat
- telotristat ethyl
- tocilizumab
- topiramate
- tovorafenib
- vaborbactam
- vamorolone
- vemurafenib
- verapamil
- vorasidenib
Adverse Reactions .
Serious Reactions
- HBV reactivation
- angioedema
- hepatic decompensation
- hepatic failure
Common Reactions
- fatigue
- headache
- nausea
- diarrhea
- insomnia
- abdominal pain
- ALT elevated
Safety/Monitoring .
Monitoring Parameters
CBC, hepatitis B serology including HBsAg, LFTs, pregnancy test at baseline; Cr at baseline, 4wk after tx start, then if clinically indicated; signs/symptoms of hepatic impairment during tx if pre-existing hepatic decompensation risk; signs/symptoms of hepatitis or HBV reactivation during tx and after D/C if current or prior HBV infection
Pregnancy/Lactation .
Pregnancy
Clinical Summary
elbasvir: weigh risk/benefit during pregnancy, consider delaying pregnancy until treatment completed; no human data available; no known risk of fetal harm based on animal data at 10x and 18x recommended human dose
grazoprevir: weigh risk/benefit during pregnancy, consider delaying pregnancy until treatment completed; no human data available; no known risk of fetal harm based on animal data at 41x and 78x recommended human dose
Lactation
Clinical Summary
elbasvir: avoid breastfeeding if nipples cracked or bleeding, otherwise may use while breastfeeding; no human data available, though risk of infant harm not expected based on drug properties; no human data available to assess effects on milk production
grazoprevir: avoid breastfeeding if nipples cracked or bleeding, otherwise may use while breastfeeding; no human data available, though risk of infant harm not expected based on drug properties; no human data available to assess effects on milk production
Pharmacology .
Metabolism: for elbasvir/grazoprevir: liver; CYP450: 3A substrate
Excretion: for elbasvir: feces >90%, urine <1%; Half-life: 24h; for grazoprevir: feces >90%, urine <1%; Half-life: 31h
Subclass: Hepatitis C (HCV)
Mechanism of Action
for elbasvir: inhibits non-structural protein 5A (NS5A), limiting viral replication (direct-acting antiviral); for grazoprevir: binds to active site of HCV protease (direct-acting antiviral)
Formulary .
No Formulary Selected
Join Now to View Patient Handouts!
Create a FREE epocrates Online account to access patient medication instructions. Your patients and caregivers will appreciate you printing these friendly handouts, available in English and Spanish. Each handout addresses common concerns such as how to take the medication, and possible side effects.
Current Members: Sign In.
Pill Pictures
Join Now to View Pill Pictures!
Create a FREE epocrates Online account to access full-color images of medications within the drug monograph.
Current Members: Sign In.