Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Priftin: 150 mg [contains disodium edta, fd&c blue #2 aluminum lake]
Pharmacology
Mechanism of Action
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.
Pharmacokinetics/Pharmacodynamics
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
Metabolism
Hepatic; hydrolyzed by an esterase enzyme to form the active metabolite 25-desacetyl rifapentine
Excretion
Feces (70%); urine (17%, primarily as metabolites)
In pediatric patients 2 to 18 years of age, clearance decreases with increasing age.
Time to Peak
Serum: 3 to 10 hours
Half-Life Elimination
Rifapentine: ~17 hours; 25-desacetyl rifapentine: ~24 hours
Protein Binding
Rifapentine: ~98%, primarily to albumin; 25-desacetyl rifapentine: ~93%
Use: Labeled Indications
Tuberculosis, active: Treatment of active pulmonary tuberculosis caused by Mycobacterium tuberculosis in adults and children 12 years and older; must be used in combination with one or more antituberculosis drugs to which the isolate is susceptible.
Limitations of use: Rifapentine should not be used once weekly in the continuation phase regimen in combination with isoniazid in HIV-infected patients with active pulmonary tuberculosis because of a higher rate of failure and/or relapse with rifampin-resistant organisms. Rifapentine has not been studied as part of the initial phase treatment regimen in HIV-infected patients with active pulmonary tuberculosis.
Tuberculosis, latent infection: Treatment of latent tuberculosis infection caused by Mycobacterium tuberculosis, in combination with isoniazid, in adults and children 2 years and older at high risk of progression to tuberculosis disease. To identify candidates for latent tuberculosis infection treatment, refer to Centers for Disease Control and Prevention (CDC) guidelines for current recommendations.
Limitations of use: Rifapentine in combination with isoniazid is not recommended for individuals presumed to be exposed to rifamycin- or isoniazid-resistant M. tuberculosis.
Contraindications
Hypersensitivity to rifapentine, other rifamycins, or any component of the formulation
Dosage and Administration
Dosing: Adult
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:
Once-weekly regimen: Oral: Administer for 12 weeks in combination with isoniazid. Note: May be administered by DOT or as self-administered therapy. This regimen may only be used in patients who are not pregnant and/or not expecting to become pregnant; if used in HIV-infected patients, it may only be used in those receiving antiretroviral therapy (ART) with acceptable drug-drug interactions with rifapentine (CDC [Borisov 2018]).
25.1 to 32 kg: 600 mg once weekly
32.1 to 50 kg: 750 mg once weekly
>50 kg: 900 mg once weekly
Once-daily regimen (HIV-infected patients): Oral: Administer for 1 month in combination with isoniazid. Note: This regimen has been studied in HIV-infected patients living in regions with high tuberculosis prevalence or with evidence of latent tuberculosis infection (Swindells 2019), but is not yet widely recommended (Menzies 2019).
<35 kg: 300 mg once daily
35 to 45 kg: 450 mg once daily
>45 kg: 600 mg once daily
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Note: Rifapentine must always be used in conjunction with at least one other antituberculosis drug to which the isolate is susceptible.
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 (INH) 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 (LTBI): Note: For HIV-positive patients, including those with AIDS, rifapentine in combination with isoniazid is recommended if receiving HAART therapy 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 (SAT) at the clinician's discretion based on local practice, patient attributes/preferences, and other factors including risk for TB disease progression (CDC [Borisov 2018]) for 12 weeks (12 doses) in combination with isoniazid:
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
Administration
Oral: Administer with meals. For patients who cannot swallow tablets, the tablets may be crushed and added to a small amount of semi-solid food and consumed immediately.
Dietary Considerations
Take with food.
Storage
Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from excessive heat and humidity.
Drug Interactions
Abemaciclib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Abemaciclib. Avoid combination
Abiraterone Acetate: Rifapentine may decrease the serum concentration of Abiraterone Acetate. Monitor therapy
Alfentanil: Rifamycin Derivatives may decrease the serum concentration of Alfentanil. Management: Monitor closely for decreased alfentanil effectiveness. Increased alfentanil doses will likely be needed. Alternatively, changing from alfentanil to a different opioid anesthetic (e.g., sufentanil) may also be considered. Consider therapy modification
Antifungal Agents (Azole Derivatives, Systemic): May increase the serum concentration of Rifamycin Derivatives. Only rifabutin appears to be affected. Rifamycin Derivatives may decrease the serum concentration of Antifungal Agents (Azole Derivatives, Systemic). Management: Avoid these combinations when possible. Voriconazole and isavuconazonium are considered contraindicated. Consider therapy modification
Antihepaciviral Combination Products: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Antihepaciviral Combination Products. Avoid combination
Asunaprevir: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Asunaprevir. Avoid combination
Atovaquone: Rifamycin Derivatives may decrease the serum concentration of Atovaquone. Avoid combination
Avapritinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Avapritinib. Avoid combination
Axitinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Axitinib. Avoid combination
Barbiturates: Rifamycin Derivatives may increase the metabolism of Barbiturates. Monitor therapy
BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Avoid combination
BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Monitor therapy
Bedaquiline: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Bedaquiline. Avoid combination
Benzhydrocodone: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Benzhydrocodone. Specifically, the serum concentrations of hydrocodone may be reduced. Monitor therapy
Beta-Blockers: Rifamycin Derivatives may decrease the serum concentration of Beta-Blockers. Exceptions: Atenolol; Carteolol (Ophthalmic); Levobunolol; Metipranolol; Nadolol. Monitor therapy
Bictegravir: Rifapentine may decrease the serum concentration of Bictegravir. Avoid combination
Bosutinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Bosutinib. Avoid combination
Brigatinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Brigatinib. Management: Avoid concurrent use of brigatinib with moderate CYP3A4 inducers when possible. If combined, increase the daily dose of brigatinib in 30 mg increments after 7 days of treatment with the current brigatinib dose, up to maximum of twice the dose. Consider therapy modification
Cabozantinib: Rifapentine may decrease the serum concentration of Cabozantinib. Monitor therapy
Calcium Channel Blockers: Rifamycin Derivatives may decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers. Management: The labeling for some US and Canadian calcium channel blockers contraindicate use with rifampin, however recommendations vary. Consult appropriate labeling. Exceptions: Clevidipine. Consider therapy modification
Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Management: Avoid cholera vaccine in patients receiving systemic antibiotics, and within 14 days following the use of oral or parenteral antibiotics. Avoid combination
Clarithromycin: CYP3A4 Inducers (Moderate) may increase serum concentrations of the active metabolite(s) of Clarithromycin. CYP3A4 Inducers (Moderate) may decrease the serum concentration of Clarithromycin. Management: Consider alternative antimicrobial therapy for patients receiving a CYP3A inducer. Drugs that enhance the metabolism of clarithromycin into 14-hydroxyclarithromycin may alter the clinical activity of clarithromycin and impair its efficacy. Consider therapy modification
CloZAPine: CYP3A4 Inducers (Moderate) may decrease the serum concentration of CloZAPine. Monitor therapy
Cobicistat: Rifapentine may decrease the serum concentration of Cobicistat. Avoid combination
Cobimetinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Cobimetinib. Avoid combination
Codeine: CYP3A4 Inducers (Moderate) may decrease serum concentrations of the active metabolite(s) of Codeine. Monitor therapy
CycloSPORINE (Systemic): Rifamycin Derivatives may increase the metabolism of CycloSPORINE (Systemic). Consider therapy modification
CYP2C9 Substrates (High risk with Inducers): Rifapentine may decrease the serum concentration of CYP2C9 Substrates (High risk with Inducers). Monitor therapy
CYP3A4 Substrates (High risk with Inducers): CYP3A4 Inducers (Moderate) may decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Exceptions: Apixaban; Rivaroxaban. Monitor therapy
Daclatasvir: Rifapentine may decrease the serum concentration of Daclatasvir. Management: US labeling recommends increasing the daclatasvir dose to 90 mg once daily if used with rifapentine. Canadian labeling states that the combination of daclatasvir and rifapentine is contraindicated. Consider therapy modification
Dapsone (Systemic): Rifamycin Derivatives may decrease the serum concentration of Dapsone (Systemic). Monitor therapy
Darunavir: Rifapentine may decrease the serum concentration of Darunavir. Avoid combination
Dasabuvir: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Dasabuvir. Avoid combination
Deflazacort: CYP3A4 Inducers (Moderate) may decrease serum concentrations of the active metabolite(s) of Deflazacort. Avoid combination
Delavirdine: Rifamycin Derivatives may increase the metabolism of Delavirdine. Delavirdine may increase the serum concentration of Rifamycin Derivatives. Specifically, Rifabutin serum concentration may be increased. Avoid combination
Doravirine: Rifapentine may decrease the serum concentration of Doravirine. Avoid combination
Elbasvir: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Elbasvir. Avoid combination
Elexacaftor, Tezacaftor, and Ivacaftor: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Elexacaftor, Tezacaftor, and Ivacaftor. Monitor therapy
Elvitegravir: Rifapentine may decrease the serum concentration of Elvitegravir. Avoid combination
Encorafenib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Encorafenib. Avoid combination
Entrectinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Entrectinib. Avoid combination
Enzalutamide: Rifapentine may decrease the serum concentration of Enzalutamide. Monitor therapy
Erdafitinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Erdafitinib. Management: Dose modifications of erdafitinib may be required. See full monograph for details. Consider therapy modification
Erlotinib: Rifapentine may decrease the serum concentration of Erlotinib. Management: Avoid combination if possible. If combination must be used, increase erlotinib dose by 50 mg increments every 2 weeks as tolerated, to a maximum of 450 mg/day. Consider therapy modification
Estriol (Systemic): CYP3A4 Inducers (Moderate) may decrease the serum concentration of Estriol (Systemic). Monitor therapy
Estriol (Topical): CYP3A4 Inducers (Moderate) may decrease the serum concentration of Estriol (Topical). Monitor therapy
Estrogen Derivatives (Contraceptive): Rifamycin Derivatives may decrease the serum concentration of Estrogen Derivatives (Contraceptive). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal contraceptive is recommended. Consider therapy modification
Etravirine: Rifapentine may decrease the serum concentration of Etravirine. Avoid combination
Everolimus: Rifapentine may decrease the serum concentration of Everolimus. Monitor therapy
Fedratinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Fedratinib. Avoid combination
FentaNYL: CYP3A4 Inducers (Moderate) may decrease the serum concentration of FentaNYL. Monitor therapy
Flibanserin: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Flibanserin. Avoid combination
Glecaprevir and Pibrentasvir: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Glecaprevir and Pibrentasvir. Monitor therapy
Grazoprevir: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Grazoprevir. Avoid combination
GuanFACINE: CYP3A4 Inducers (Moderate) may decrease the serum concentration of GuanFACINE. Management: Increase the guanfacine dose by up to double when initiating guanfacine in a patient taking a moderate CYP3A4 inducer. Increase guanfacine dose gradually over 1 to 2 weeks if initiating a moderate CYP3A4 inducer in a patient already taking guanfacine. Consider therapy modification
HMG-CoA Reductase Inhibitors (Statins): Rifamycin Derivatives may decrease the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Management: Consider use of noninteracting antilipemic agents (note: pitavastatin concentrations may increase with rifamycin treatment). Monitor for altered HMG-CoA reductase inhibitor effects. Rifabutin and fluvastatin, or possibly pravastatin, may pose lower risk. Exceptions: Pitavastatin; Rosuvastatin. Consider therapy modification
HYDROcodone: CYP3A4 Inducers (Moderate) may decrease the serum concentration of HYDROcodone. Monitor therapy
Ibrutinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Ibrutinib. Monitor therapy
Ifosfamide: CYP3A4 Inducers (Moderate) may decrease serum concentrations of the active metabolite(s) of Ifosfamide. CYP3A4 Inducers (Moderate) may increase serum concentrations of the active metabolite(s) of Ifosfamide. Monitor therapy
Imatinib: Rifamycin Derivatives may decrease the serum concentration of Imatinib. Management: Avoid concurrent use of imatinib with the rifamycin derivatives when possible. If such a combination must be used, increase imatinib dose by at least 50% and monitor the patient's clinical response closely. Consider therapy modification
Indinavir: Rifapentine may decrease the serum concentration of Indinavir. Management: Consider avoiding the combination of indinavir and rifapentine whenever possible due to the risk for decreased indinavir concentrations, reduced efficacy, and development of resistance. If combined, monitor for indinavir treatment failure. Consider therapy modification
Irinotecan Products: Rifapentine may decrease serum concentrations of the active metabolite(s) of Irinotecan Products. Specifically, serum concentrations of SN-38 may be reduced. Rifapentine may decrease the serum concentration of Irinotecan Products. Monitor therapy
Isoniazid: Rifamycin Derivatives may enhance the hepatotoxic effect of Isoniazid. Even so, this is a frequently employed combination regimen. Monitor therapy
Istradefylline: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Istradefylline. Monitor therapy
Ivacaftor: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Ivacaftor. Monitor therapy
Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Monitor therapy
Ledipasvir: Rifapentine may decrease the serum concentration of Ledipasvir. Avoid combination
Lefamulin: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin with moderate CYP3A4 inducers unless the benefits outweigh the risks. Consider therapy modification
Lefamulin (Intravenous): CYP3A4 Inducers (Moderate) may decrease the serum concentration of Lefamulin (Intravenous). Management: Avoid concomitant use of lefamulin (intravenous) with moderate CYP3A4 inducers unless the benefits outweigh the risks. Consider therapy modification
Lemborexant: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Lemborexant. Avoid combination
Lorlatinib: CYP3A4 Inducers (Moderate) may enhance the hepatotoxic effect of Lorlatinib. CYP3A4 Inducers (Moderate) may decrease the serum concentration of Lorlatinib. Management: Avoid use of lorlatinib with moderate CYP3A4 inducers. If such a combination must be used, monitor AST, ALT, and bilirubin within 48 hours of starting the combination and at least three times within the first week of combined use. Consider therapy modification
Lumacaftor and Ivacaftor: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Lumacaftor and Ivacaftor. Monitor therapy
Lumateperone: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Lumateperone. Avoid combination
Lurasidone: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Lurasidone. Management: Monitor for decreased lurasidone effects if combined with moderate CYP3A4 inducers and consider increasing the lurasidone dose if coadministered with a moderate CYP3A4 inducer for 7 or more days. Consider therapy modification
Meperidine: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Meperidine. Monitor therapy
Methadone: Rifamycin Derivatives may decrease the serum concentration of Methadone. Management: Seek alternatives when possible. If used concomitantly, monitor closely for symptoms of methadone withdrawal upon rifamycin derivative initiation, and for excess sedation upon rifamycin derivative discontinuation. Consider therapy modification
Mirodenafil: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Mirodenafil. Monitor therapy
Mycophenolate: Rifamycin Derivatives may decrease the serum concentration of Mycophenolate. Specifically, rifamycin derivatives may decrease the concentration of the active metabolite mycophenolic acid. Avoid combination
Naldemedine: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Naldemedine. Monitor therapy
Neratinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Neratinib. Avoid combination
Nilotinib: Rifapentine may decrease the serum concentration of Nilotinib. Monitor therapy
Nisoldipine: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Nisoldipine. Avoid combination
Olaparib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Olaparib. Avoid combination
Palbociclib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Palbociclib. Management: The US label does not provide specific recommendations concerning use with moderate CYP3A4 inducers, but the Canadian label recommends avoiding use of moderate CYP3A4 inducers. Consider therapy modification
Perampanel: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Perampanel. Management: Increase the perampanel starting dose to 4 mg/day when perampanel is used concurrently with moderate and strong CYP3A4 inducers. Consider therapy modification
Pexidartinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Pexidartinib. Monitor therapy
Pimavanserin: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Pimavanserin. Avoid combination
Pitavastatin: Rifamycin Derivatives may increase the serum concentration of Pitavastatin. Management: Limit pitavastatin dose to a maximum of 2 mg/day with concurrent rifampin. Consider therapy modification
Pitolisant: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Pitolisant. Monitor therapy
Pretomanid: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Pretomanid. Avoid combination
Progestins (Contraceptive): Rifamycin Derivatives may decrease the serum concentration of Progestins (Contraceptive). Contraceptive failure is possible. Management: Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended. Consider therapy modification
QuiNIDine: Rifamycin Derivatives may decrease the serum concentration of QuiNIDine. Management: Consider alternatives to combination treatment with quinidine and rifampin due to large potential decreases in quinidine concentrations. Monitor for decreased quinidine concentrations/effects with initiation/dose increase of any rifamycin derivative. Consider therapy modification
Raltegravir: Rifapentine may increase the serum concentration of Raltegravir. Rifapentine may decrease the serum concentration of Raltegravir. Monitor therapy
Ranolazine: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Ranolazine. Avoid combination
Rilpivirine: Rifamycin Derivatives may decrease the serum concentration of Rilpivirine. Avoid combination
Rolapitant: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Rolapitant. Monitor therapy
RomiDEPsin: Rifapentine may decrease the serum concentration of RomiDEPsin. Monitor therapy
Simeprevir: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Simeprevir. Avoid combination
Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Consider therapy modification
Sofosbuvir: Rifapentine may decrease the serum concentration of Sofosbuvir. Avoid combination
Sonidegib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Sonidegib. Avoid combination
Tacrolimus (Systemic): Rifamycin Derivatives may decrease the serum concentration of Tacrolimus (Systemic). Management: Consider alternatives when possible. If these combination are used, monitor for reduced tacrolimus concentrations/effects following rifamycin initiation/dose increase, or increased concentrations/effects following rifamycin discontinuation/dose decrease. Consider therapy modification
Tamoxifen: Rifamycin Derivatives may increase the metabolism of Tamoxifen. Consider therapy modification
Tazemetostat: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Tazemetostat. Avoid combination
Temsirolimus: Rifamycin Derivatives may decrease the serum concentration of Temsirolimus. Rifamycins will likely cause an even greater decrease in the concentration of the active metabolite sirolimus. Management: Temsirolimus prescribing information recommends against coadministration with strong CYP3A4 inducers such as rifampin; however, if concurrent therapy is necessary, an increase in temsirolimus adult dose to 50 mg/week should be considered. Consider therapy modification
Tenofovir Alafenamide: Rifapentine may decrease the serum concentration of Tenofovir Alafenamide. Avoid combination
Tezacaftor and Ivacaftor: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Tezacaftor and Ivacaftor. Monitor therapy
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 3 days after cessation of antibacterial agents. Consider therapy modification
Ubrogepant: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 100 mg and second dose (if needed) of 100 mg when used with a moderate CYP3A4 inducer. Consider therapy modification
Upadacitinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Upadacitinib. Monitor therapy
Velpatasvir: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Velpatasvir. Avoid combination
Venetoclax: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Venetoclax. Avoid combination
VinCRIStine (Liposomal): Rifapentine may decrease the serum concentration of VinCRIStine (Liposomal). Monitor therapy
Vitamin K Antagonists (eg, warfarin): Rifamycin Derivatives may increase the metabolism of Vitamin K Antagonists. Monitor therapy
Voriconazole: May increase the serum concentration of Rifamycin Derivatives. Rifamycin Derivatives may decrease the serum concentration of Voriconazole. Avoid combination
Voxelotor: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Voxelotor. Management: Avoid concomitant use of voxelotor and moderate CYP3A4 inducers. If concomitant use is unavoidable, increase the voxelotor dose to 2,500 mg once daily. Consider therapy modification
Zanubrutinib: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Zanubrutinib. Avoid combination
Zidovudine: Rifamycin Derivatives may decrease the serum concentration of Zidovudine. Monitor therapy
Zolpidem: CYP3A4 Inducers (Moderate) may decrease the serum concentration of Zolpidem. Monitor therapy
Test Interactions
Rifampin has been shown to inhibit standard microbiological assays for serum folate and vitamin B12; this should be considered for rifapentine; therefore, alternative assay methods should be considered.
Adverse Reactions
Frequency may vary based on treatment phase; adverse reaction data is based on rifapentine combination therapy.
>10%:
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%)
1% to 10%:
Cardiovascular: Chest pain (3% to 6%), edema (1%)
Central nervous system: Pain (3% to 6%), headache (≤3%), dizziness (≤1%), fatigue (≤1%)
Dermatologic: Diaphoresis (2% to 5%), skin rash (3% to 4%), acne vulgaris (≤3%), pruritus (≤3%), maculopapular rash (≤2%)
Endocrine & metabolic: Hypoglycemia (5% to 10%), hyperglycemia (1% to 4%), increased nonprotein nitrogen (1% to 3%), gout (1%), hyperphosphatemia (1%)
Gastrointestinal: Anorexia (3% to 4%), nausea (≤3%), constipation (1% to 2%), dyspepsia (1% to 2%), abdominal pain (≤2%), diarrhea (≤2%), vomiting (≤2%), hemorrhoids (1%)
Genitourinary: Casts in urine (4% to 8%), cystitis (1%)
Hematologic & oncologic: Leukopenia (4% to 7%), thrombocytosis (≤6%), leukocytosis (2% to 3%), neutrophilia (1% to 3%), thrombocythemia (1% to 3%), polycythemia (≤2%), lymphadenopathy (≤1%)
Hepatic: Increased serum ALT (2% to 7%), increased serum AST (2% to 6%), hepatotoxicity (≤2%)
Hypersensitivity: Hypersensitivity reaction (≤4%; children & adolescents 1%)
Infection: Influenza (3% to 8%), herpes zoster (1%), infection (1%)
Neuromuscular & skeletal: Back pain (4% to 7%), arthralgia (≤4%), osteoarthrosis (1%), tremor (1%)
Ophthalmic: Conjunctivitis (≤3%)
Respiratory: Hemoptysis (2% to 8%), cough (3% to 6%), bronchitis (3%), pharyngitis (1% to 2%), epistaxis (1%), pleurisy (1%)
Miscellaneous: Accidental injury (1% to 5%), fever (≤1%)
<1%, postmarketing, and/or case reports: Ageusia, allergic skin reaction, alopecia, anaphylaxis, anxiety, asthma, azotemia, bronchial hyperactivity, bronchospasm, chills, confusion, convulsions, decreased appetite, depression, diabetes mellitus, disorientation, drowsiness, dyspnea, dysuria, enlargement of salivary glands, erythematous rash, esophagitis, facial edema, fungal infection, gastritis, hematoma, hepatitis, hepatomegaly, hyperbilirubinemia, hypercalcemia, hyperhidrosis, hyperkalemia, hyperlipidemia, increased blood urea nitrogen, increased serum alkaline phosphatase, jaundice, jitteriness, laryngeal edema, laryngitis, leukorrhea, lymphocytosis, myalgia, myasthenia, myositis, oropharyngeal pain, orthostatic hypotension, palpitations, pancreatitis, paresthesia, pericarditis, peripheral neuropathy, pneumonitis, pulmonary fibrosis, pulmonary tuberculosis (exacerbation), purpura, pyelonephritis, rhabdomyolysis, seizure, skin discoloration, suicidal ideation, syncope, tachycardia, thrombosis, urinary incontinence, urticaria, vaginal hemorrhage, vaginitis, viral infection, voice disorder, vulvovaginal candidiasis, vulvovaginal pruritus, weakness, weight gain, weight loss, xerostomia
Warnings/Precautions
Concerns related to adverse effects:
- Hypersensitivity reactions: Hypersensitivity reactions, including anaphylaxis, may occur. Discontinue therapy and administer supportive measures if hypersensitivity occurs.
- Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.
Disease-related concerns:
- Hepatic impairment: Patients with abnormal liver tests and/or liver disease should only be given rifapentine when absolutely necessary and under strict medical supervision. Monitoring of liver function tests (eg, serum transaminases) should be carried out prior to therapy and then every 2 to 4 weeks during therapy. Combination therapy should be discontinued if ALT is ≥5 times the upper limit of normal (ULN) even in the absence of liver dysfunction symptoms or ≥3 times ULN in the presence of symptoms (CDC 2012).
- Porphyria: Use is not recommended in patients with porphyria; exacerbation is possible due to enzyme-inducing properties.
Concurrent drug therapy issues:
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Special populations:
- HIV-seropositive patients: Use of rifapentine during the initial phase of treatment in HIV-seropositive patients has not been evaluated. Rifapentine should not be used during the continuation phase of treatment in HIV-seropositive patients; a higher rate of failure and/or relapse with rifampin-resistant organisms has been reported.
Dosage form specific issues:
- Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated with hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Zar 2007).
Other warnings/precautions:
- Appropriate use: Use with caution in patients with cavitary pulmonary lesions and/or positive sputum cultures after initial treatment phase and patients with bilateral pulmonary disease; higher relapse rates may occur in these patients.
- Compliance: Compliance with dosing regimen is absolutely necessary for successful drug therapy.
- Contact lenses: Remove soft contact lenses during therapy since permanent staining may occur.
- Red/orange discoloration: Urine, feces, saliva, sweat, tears, skin, teeth, tongue, and CSF may be discolored to red/orange. Advise patients with dentures that permanent staining of dentures may occur.
Monitoring Parameters
Patients with preexisting hepatic problems should have liver function tests monitored (eg, serum transaminases) prior to therapy and then every 2 to 4 weeks during therapy. In treatment of latent infection with rifapentine and isoniazid combination therapy, patients with HIV infection, liver disorders, immediate postpartum (≤ 3 months after delivery), or regular ethanol use should have liver function (at least alanine aminotransferase [ALT]) monitored prior to therapy and then at subsequent clinical visits whose baseline testing is abnormal or for others at risk for liver disease (CDC, 2012).
Pregnancy
Pregnancy Risk Factor
C
Pregnancy Considerations
Adverse events have been observed in animal reproduction studies. Information related to the use of rifapentine in pregnant women is limited. Postnatal hemorrhages have been reported in the infant and mother with rifampin (another rifamycin) administration during the last few weeks of pregnancy. Monitoring of the prothrombin time in the mother and neonate is recommended following exposure late in pregnancy; treatment with vitamin K may be needed.
Patient Education
What is this drug used for?
- It is used to treat TB (tuberculosis).
Frequently reported side effects of this drug
- Diarrhea
- Lack of appetite
- Joint pain
- Nausea
- Vomiting
- Body tissue or body fluid discoloration
- Denture discoloration
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Liver problems like dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin
- Abnormal heartbeat
- Severe loss of strength and energy
- Chills
- Sore throat
- Bruising
- Bleeding
- Chest pain
- Fast heartbeat
- Dizziness
- Passing out
- Flu-like symptoms
- Muscle pain
- Swollen glands
- Cough
- Eye redness
- Shortness of breath
• Clostridioides (formerly Clostridium) difficile (C. diff)-associated diarrhea like abdominal pain or cramps, severe diarrhea or watery stools, or bloody stools
- Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
