Active pulmonary tuberculosis
Latent tuberculosis infection (LTBI)

Inhibits DNA-dependent RNA polymerase in susceptible strains of Mycobacterium tuberculosis (MTB) (but not in mammalian cells). Rifapentine is bactericidal against both intracellular and extracellular MTB organisms.

Absorption: High-fat meals increase AUC and Cmax by 40% to 50% In pediatric patients, crushing the tablet results in 26% lower exposure than whole tablets.
Distribution: Vd: ~70 L
Protein binding: Rifapentine: ~98%, primarily to albumin; 25-desacetyl rifapentine: ~93%
Metabolism: Hepatic; hydrolyzed by an esterase enzyme to form the active metabolite 25-desacetyl rifapentine
Bioavailability: 70%
Half-life elimination: Rifapentine: ~17 hours; 25-desacetyl rifapentine: ~24 hours
Time to peak, serum: 3 to 10 hours
Excretion: Feces (70%); urine (17%, primarily as metabolites)
In pediatric patients 2 to 18 years of age, clearance decreases with increasing age.

Hypersensitivity to rifapentine, other rifamycins, or any component of the formulation

C(FDA)

It is not known if rifapentine is present in breast milk. Because of the potential for serious adverse reactions in the breastfeeding infant, the manufacturer recommends a decision be made whether to discontinue breastfeeding or the drug, taking into account the importance of treatment to the mother. Rifapentine may discolor breast milk red-orange.

Endocrine & metabolic: Hyperuricemia (?32%; most likely due to pyrazinamide from initiation phase)
Genitourinary: Pyuria (11% to 22%), hematuria (10% to 18%), urinary tract infection (7% to 13%)
Hematologic & oncologic: Neutropenia (6% to 13%), lymphocytopenia (3% to 13%), anemia (2% to 11%)

Tuberculosis, active (drug-susceptible): Oral:
Initial phase: 600 mg twice weekly (with an interval ?72 hours between doses) by directly observed therapy (DOT) for 2 months as part of multidrug regimen.
Continuation phase: 600 mg once weekly by DOT for 4 months as part of a multidrug regimen. Note: Drug-susceptible TB guidelines recommend against once-weekly therapy; use should only be considered in rare situations in certain HIV-uninfected individuals with no cavitation on chest x-ray (Nahid 2016).
Tuberculosis, latent infection: Oral: Use once weekly for 12 weeks in combination with isoniazid.
25.1 to 32 kg: 600 mg
32.1 to 50 kg: 750 mg
>50 kg: 900 mg

Tuberculosis, treatment; active pulmonary infection: Children ?12 years and Adolescents:
Initial phase: Oral: 600 mg twice weekly (with an interval ?72 hours between doses) by directly observed therapy (DOT) for 2 months. Note: Initial phase should include a 3- to 4-drug regimen.
Continuation phase: Oral: 600 mg once weekly by DOT for 4 months in combination with isoniazid or another appropriate agent for susceptible organisms. Note: Drug-susceptible TB guidelines recommend against once-weekly therapy; use should only be considered in rare situations in certain HIV-uninfected individuals with no cavitation on chest x-ray (Nahid 2016).
Latent tuberculosis infection: Note: For HIV-positive patients, including those with AIDS, rifapentine in combination with isoniazid is recommended if receiving highly active antiretroviral therapy (HAART) with acceptable drug-drug interactions with rifapentine when guided by experienced clinicians (CDC [Borisov 2018]). Children ?2 years and Adolescents: Oral: Administer by DOT or self-administered therapy at the clinician's discretion based on local practice, patient attributes/preferences, and other factors, including risk for TB disease progression for 12 weeks (12 doses) in combination with isoniazid (CDC [Borisov 2018]):
10 to 14 kg: 300 mg/dose once weekly
>14 to 25 kg: 450 mg/dose once weekly
>25 to 32 kg: 600 mg/dose once weekly
>32 to 50 kg: 750 mg/dose once weekly
>50 kg: 900 mg/dose once weekly

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution. Pharmacokinetics in varying degrees of hepatic impairment were similar to those in healthy volunteers.