Daclatasvir
Indications
Daclatasvir is used for:
Chronic hepatitis C virus infection in adults.
Adult Dose
Hepatitis C
Indicated for use with sofosbuvir for chronic hepatitis C virus (HCV) genotypes 1 and 3 infection
Genotype 1
Without cirrhosis or with compensated (Child-Pugh A) cirrhosis: 60 mg (plus sofosbuvir 400 mg) PO qDay for 12 weeks
Decompensated (Child-Pugh B or C) cirrhosis or posttransplant: 60 mg (plus sofosbuvir 400 mg) PO qDay plus ribavirin for 12 weeks
Genotype 3
Without cirrhosis: 60 mg (plus sofosbuvir 400 mg) PO qDay for 12 weeks
Compensated (Child-Pugh A) or decompensated (Child-Pugh B or C) cirrhosis, or posttransplant: 60 mg (plus sofosbuvir 400 mg) PO qDay plus ribavirin for 12 weeks
Hepatic impairment (any degree): No dose adjustment required
Child Dose
Renal Dose
Renal impairment (any degree): No dose adjustment required
Administration
May be taken with or without food.
Contra Indications
Hypersensitivity. Co-administration w/ strong CYP3A4 inducers & P-gp eg phenytoin, carbamazepine, oxcarbazepine, phenobarb, rifampicin, rifabutin, rifapentine, systemic dexamethasone, St. John's wort.
Precautions
Patients w/ genotype 1 infection & compensated cirrhosis; receiving amiodarone; decompensated liver disease; prior exposure to a NS5A inhibitor; pre-, peri- or post-liver transplant or other organ transplant; HIV/HCV, HBV co-infected patients.
Rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. May impair ability to drive or operate machinery. Women of childbearing potential. Pregnancy & lactation. Childn & adolescents <18 yr.
Lactation
Unknown if distributed in human breast milk
Pregnancy-Lactation
Interactions
May lead to lower exposure & loss of efficacy w/ phenytoin, carbamazepine, oxcarbazepine, phenobarb, rifampicin, rifabutin, rifapentine, systemic dexamethasone & St. John's wort. Decreased plasma levels & therapeutic effect w/ strong or moderate CYP3A4 & P-gp inducers. Increased plasma levels w/ strong CYP3A4 inhibitors. May increase systemic exposure of P-gp, OATP, 1B1, OCT1 or BCRP substrates. Boceprevir, telaprevir, atazanavir/ritonavir, efavirenz, cobicistat-containing, clarithromycin, telithromycin, erythromycin, dabigatran, etexilate, posaconazole, voriconazole, amiodarone, digoxin, Ca channel blockers, HMG-CoA reductase inhibitors.
Adverse Effects
Side effects of Daclatasvir :
>10%
Headache (14%),Fatigue (14%)
1-10%
Nausea (8%),Diarrhea (5%),Elevated lipase, >3 x ULN (2%)
Mechanism of Action
Inhibits NS5A, a nonstructural protein encoded by HCV.
Binds to the N-terminus within domain 1 of NS5A, which may cause structural distortions that interfere with NS5A functions, and thereby inhibits both viral RNA replication and virion assembly.