Dosing and uses of Emtriva (emtricitabine)
Adult dosage forms and strengths
capsule
- 200mg
oral solution
- 10mg/mL
HIV Infection
Capsule: 200 mg PO qDay
Oral Solution: 240 mg PO qDay
Renal Impairment
CrCl 50 mL/min or more: capsule 200 mg PO qDay; oral solution: 240 mg PO qDay
CrCl 30-49 mL/min: capsule 200 mg PO q48hr; oral solution: 120 mg PO qDay
CrCl 15-29 mL/min: capsule 200 mg PO q72hr; oral solution: 80 mg PO qDay
CrCl <15 mL/min: capsule 200 mg PO q96hr; oral solution: 60 mg PO qDay
Administration on day of hemodialysis: Administer after dialysis
Pediatric dosage forms and strengths
capsule
- 200mg
oral solution
- 10mg/mL
HIV Infection
<3 months
- Oral solution: 3 mg/kg PO qDay
>3 months
- Oral solution: 6 mg/kg PO qDay, no more than 240 mg
- Capsules (if >33 kg): 200 mg (1 capsule) PO qDay
Renal Impairment
Reduce dose and/or increase dosing intervaL
Emtriva (emtricitabine) adverse (side) effects
Frequencies based on combination treatment
>10%
Diarrhea (21-25%)
Dizziness (21-25%)
Headache (21-25%)
Insomnia (21-25%)
Rash (21-25%)
Asthenia (16-20%)
Nausea (16-20%)
Rhinitis (16-20%)
Abdominal pain (11-15%)
Abnormal dreams (11-15%)
Incr CK (11-15%)
Incr cough (11-15%)
Neuritis (11-15%)
Paresthesia (11-15%)
1-10%
Depressive symptoms (6-10%)
Dyspepsia (6-10%)
Vomiting (6-10%)
Incr triglycerides (6-10%)
Myalgia (6-10%)
<1%
Lactic acidosis/severe
Hepatomegaly with steatosis, including fatal cases; post treatment exacerbation of Hepatitis B
Warnings
Black box warnings
Lactic acidosis and severe hepatomegaly with steatosis (including fatal cases) reported with use of nucleoside analogues alone or in combination with other antiretrovirals
Not FDA approved for treatment of chronic hepatitis B virus (HBV) infection, and the safety and efficacy of this drug have not been established in patients co-infected with HBV and HIV
Contraindications
Hypersensitivity
Cautions
(All NRTIs): Risk of potentially fatal lactic acidosis & severe hepatomegaly with steatosis when used alone or in combination with other antiretrovirals
Risk of immune reconstitution syndrome if used in combination w/ other antiretroviral drugs
Should not be coadministered with combination antiretroviral agents containing emtricitabine
Pregnancy and lactation
Pregnancy category: B
Lactation: It is not known whether emtricitabine is excreted in milk. It should not be administered to nursing mothers. The CDC advises HIV-infected women not to breast-feed to avoid postnatal transmission of HIV.
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Emtriva (emtricitabine)
Mechanism of action
Nucleoside Reverse Transcriptase Inhibitor (NRTI); cytosine analog phosphorylated to emtricitabine 5'-triphosphate caucing inhibition of HIV and RNA dependent DNA polymerase
Pharmacokinetics
Bioavailability: 93%
Protein Bound: <4%
Metabolism: Oxidation
Dialyzable: 30% removed by hemodialysis
Excretion: Urine (86%); feces (14%)
Half-Life: 10 hr
Peak PlasmaTime: 1-2 hr
Concentration: 1.8±0.7 mcg/m
LAUC: 10±3.1 hr.mcg/mL
