emtricitabine (em-tri-

 Indications

HIV infection (with other antiretrovirals).

Action

Phosphorylated intracellularly where it inhibits HIV reverse

transcriptase, resulting in viral DNA chain termination.

Therapeutic Effects: Slowed progression of

HIV infection and decreased occurrence of sequelae.

Increases CD4 cell counts and decreases viral load.

Pharmacokinetics

Absorption: Rapidly and extensively absorbed; 93%

bioavailable.

Distribution: Unknown.

Metabolism and Excretion: Some metabolism,

86% renally excreted, 14% fecal excretion.

Half-life: 10 hr.

TIME/ACTION PROFILE (blood levels†)

ROUTE ONSET PEAK DURATION

PO rapid 1–2 hr 24 hr

†Normal renal function.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Concurrent

use of antiretroviral combination products containing

emtricitabine or lamivudine-containing products; Lactation:

Breast feeding not recommended in HIV-infected

patients.

Use Cautiously in: Hepatitis B infection (may exacerbate

following discontinuation); Renal impairment;

OB: Use only if clearly needed; Geri: May be atqrisk

for adverse effects.

Adverse Reactions/Side Effects

CNS: dizziness, headache, insomnia, weakness, depression,

nightmares. GI: abdominal pain, diarrhea,

nausea, SEVERE HEPATOMEGALY WITH STEATOSIS, dyspepsia,

vomiting. Derm: rash, skin discoloration. F and

E: LACTIC ACIDOSIS. MS: arthralgia, myalgia. Neuro:

neuropathy, paresthesia. Resp: cough, rhinitis. Misc:

immune reconstitution syndrome.

Interactions

Drug-Drug: None noted.

Route/Dosage

PO (Adults 18 yr): 200 mg once daily.

Renal Impairment

PO (Adults 18 yr): CCr 30–49 mL/min—200 mg

every 48 hr; CCr 15–29 mL/min—200 mg every 72

hr; CCr 15 mL/min—200 mg every 96 hr.

Availability

Capsules: 200 mg. Oral solution (cotton candy flavor):

10 mg/mL. In combination with: efavirenz

and tenofovir (Atripla); tenofovir (Truvada); rilpivirine

and tenofovir (Complera); elvitegravir, cobicistat, and

tenofovir (Stribild). See Appendix B.