Rifapentine (Priftin) - Complete Drug information

Rifapentine inhibits DNA-dependent RNA polymerase in susceptible strains of Mycobacterium tuberculosis. It is bactericidal against both intracellular and extracellular MTB organisms.

  • It is used in the treatment of active pulmonary tuberculosis caused by Mycobacterium tuberculosis in adults and children 12 years and older.

    • It should be used in combination with one or more anti-tuberculosis drugs to which the isolate is susceptible.

    • Rifapentine is not used once weekly in the continuation phase regimen in combination with isoniazid in HIV-infected patients with active pulmonary tuberculosis due to a higher rate of failure and/or relapse with rifampin-resistant organisms.

  • It is used in the treatment of latent tuberculosis infection caused by Mycobacterium tuberculosis, in combination with isoniazid, in adults and children 2 years and older who are at high risk of progression to tuberculosis disease.

    • Rifapentine is not recommended in combination with isoniazid for individuals presumed to be exposed to rifamycin- or isoniazid-resistant M. tuberculosis.

Rifapentine dose in Adults

Dose in the treatment of active Drug-susceptible Tuberculosis:

  • Initial phase:

    • 600 mg twice weekly is given (with an interval ≥72 hours between doses) by directly observed therapy (DOT) for 2 months as part of a multidrug regimen.
  • Continuation phase:

    • 600 mg once weekly is given by DOT for 4 months as part of a multidrug regimen.

 

  • drug-susceptible TB guidelines recommend against using once-weekly therapy.
  • Use should only be considered in rare situations in certain HIV-uninfected individuals with no cavitation on chest x-ray

Dosage in the treatment of latent Tuberculosis:

  • Once-weekly regimen:

    • Give for 12 weeks in combination with isoniazid.
    • It may be administered by DOT or as self-administered therapy.
    • This regimen can only be used in patients who are not pregnant and/or not expecting to become pregnant
    • If it is used in HIV-infected patients, then it may only be used in those receiving antiretroviral therapy (ART) with acceptable drug-drug interactions with rifapentine
      • 1 to 32 kg:

        • 600 mg once weekly is given
      • 1 to 50 kg:

        • 750 mg once weekly is given
      • >50 kg:

        • 900 mg once weekly is given
  • Once-daily regimen (HIV-infected patients):

  • Give for 1 month in combination with isoniazid.
    • <35 kg:

      • 300 mg once daily is given
    • 35 to 45 kg:

      • 450 mg once daily is given
    • >45 kg:

      • 600 mg once daily is given

Rifapentine dose in Childrens

  • Rifapentine should always be used in conjunction with at least one other antituberculosis drug to which the isolate is susceptible.

Rifapentine Dose in the treatment of active pulmonary Tuberculosis:

  • Children ≥12 years and Adolescents:

    • Initial phase:

      • 600 mg orally twice weekly is given (with an interval ≥72 hours between doses) by directly observed therapy (DOT) for 2 months.
      • The initial phase includes a 3- to 4 drug regimen.
    • Continuation phase:

      • 600 mg orally once weekly is given by DOT for 4 months in combination with isoniazid (INH) or another appropriate agent for susceptible organisms.
      • Drug susceptible TB guidelines recommend against using once-weekly therapy.
      • Use should only be considered in rare situations in certain HIV-uninfected individuals with no cavitation on chest x-ray

Dose in the treatment of Latent tuberculosis infection (LTBI):

  • For HIV-positive patients, including those with AIDS, rifapentine in combination with isoniazid is advised if receiving HAART therapy with acceptable drug-drug interactions with rifapentine when guided by experienced physicians.
  • Children ≥2 years and Adolescents:

  • Give 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  for 12 weeks (12 doses) in combination with isoniazid:
    • 10 to 14 kg:

      • 300 mg/dose once weekly is given
    • >14 to 25 kg:

      • 450 mg/dose once weekly is given
    • >25 to 32 kg:

      • 600 mg/dose once weekly is given
    • >32 to 50 kg:

      • 750 mg/dose once weekly is given
    • >50 kg:

      • 900 mg/dose once weekly is given

Pregnancy Risk Factor C

  • Animal reproduction studies have shown that adverse events can be observed.
  • Very little information is available on the use of rifapentine during pregnancy.
  • The mother and infant experienced postnatal hemorhages after rifampin (another form of rifamycin), was administered in the last few weeks.
  • After exposure late in pregnancy, monitoring of the mother's prothrombin time and the neonate is done. Vitamin K treatment may be required.

Rifapentine use during breastfeeding:

  • It is unknown if breast milk contains rifapentine or not.
  • The manufacturer suggests that the mother decide whether to stop breastfeeding or discontinue the drug because of the risk of serious side effects.
  • Rifapentine can discolor breast milk red-orange.

Rifapentine dose in Kidney disease:

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

Rifapentine dose in Liver disease:

  • There are no dosage adjustments given in the manufacturer’s labeling
  • use cautiously

Common Side Effects of Rifapentine Include:

  • Endocrine & Metabolic:

    • Hyperuricemia
  • Genitourinary:

    • Pyuria
    • Hematuria
    • Urinary Tract Infection
  • Hematologic & Oncologic:

    • Neutropenia
    • Lymphocytopenia
    • Anemia

Less Common Side Effects of Rifapentine Include:

  • Cardiovascular:

    • Chest Pain
    • Edema
  • Central Nervous System:

    • Pain
    • Headache
    • Dizziness
    • Fatigue
  • Dermatologic:

    • Diaphoresis
    • Skin Rash
    • Acne Vulgaris
    • Pruritus
    • Maculopapular Rash
  • Endocrine & Metabolic:

    • Hypoglycemia
    • Hyperglycemia
    • Increased Nonprotein Nitrogen
    • Gout
    • Hyperphosphatemia
  • Gastrointestinal:

    • Anorexia
    • Nausea
    • Constipation
    • Dyspepsia
    • Abdominal Pain
    • Diarrhea
    • Vomiting
    • Hemorrhoids
  • Genitourinary:

    • Casts In Urine
    • Cystitis
  • Hematologic & Oncologic:

    • Leukopenia
    • Thrombocytosis
    • Leukocytosis
    • Neutrophilia
    • Thrombocythemia
    • Polycythemia
    • Lymphadenopathy
  • Hepatic:

    • Increased Serum ALT
    • Increased Serum AST
    • Hepatotoxicity
  • Hypersensitivity:

    • Hypersensitivity Reaction
  • Infection:

    • Influenza
    • Herpes Zoster
    • Infection
  • Neuromuscular & Skeletal:

    • Back Pain
    • Arthralgia
    • Osteoarthrosis
    • Tremor
  • Ophthalmic:

    • Conjunctivitis
  • Respiratory:

    • Hemoptysis
    • Cough
    • Bronchitis
    • Pharyngitis
    • Epistaxis
    • Pleurisy
  • Miscellaneous:

    • Accidental Injury
    • Fever

Contraindication to Rifapentine Include:

  • Hypersensitivity to rifapentine or other rifamycins or any part thereof

Warnings and precautions

  • Hypersensitivity reactions

    • Hypersensitivity reactions (including anaphylaxis) might occur.
    • If hypersensitivity develops, stop therapy and take supportive measures.
  • Superinfection

    • Long-term use can lead to fungal and bacterial superinfections, such as C. difficile-associated diarrhea(CDAD) or pseudomembranous collitis.
    • CDAD was seen after more than two months of post-antibiotic treatment.
  • Hepatic impairment

    • Patients with liver disease or abnormal tests should not be given rifapentine unless absolutely necessary.
    • Before starting therapy, it is important to monitor liver function (eg, serum Transaminases) and every 2 to 4 week thereafter.
    • If ALT is greater than 5 times the upper limit normal (ULN), or more than 3 times ULN when there are symptoms, combination therapy should be discontinued.
  • Porphyria

    • Patients with porphyria should not use it; exacerbation can occur due to enzyme-inducing properties

Rifapentine: Drug Interaction

Risk Factor C (Monitor therapy)

Abiraterone Acetate

Rifapentine may decrease the serum concentration of Abiraterone Acetate.

Barbiturates

Rifamycin Derivatives may increase the metabolism of Barbiturates.

BCG Vaccine (Immunization)

Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization).

Benzhydrocodone

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Benzhydrocodone. Specifically, the serum concentrations of hydrocodone may be reduced.

Beta-Blockers

Rifamycin Derivatives may decrease the serum concentration of Beta-Blockers. Exceptions: Atenolol; Carteolol (Ophthalmic); Levobunolol; Metipranolol; Nadolol.

Cabozantinib

Rifapentine may decrease the serum concentration of Cabozantinib.

CloZAPine

CYP3A4 Inducers (Moderate) may decrease the serum concentration of CloZAPine.

Codeine

CYP3A4 Inducers (Moderate) may decrease serum concentrations of the active metabolite(s) of Codeine.

CYP2C9 Substrates (High risk with Inducers)

Rifapentine may decrease the serum concentration of CYP2C9 Substrates (High risk with Inducers).

CYP3A4 Substrates (High risk with Inducers)

CYP3A4 Inducers (Moderate) may decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Exceptions: Apixaban; Rivaroxaban.

Dapsone (Systemic)

Rifamycin Derivatives may decrease the serum concentration of Dapsone (Systemic).

Enzalutamide

Rifapentine may decrease the serum concentration of Enzalutamide.

Estriol (Systemic)

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Estriol (Systemic).

Estriol (Topical)

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Estriol (Topical).

Everolimus

Rifapentine may decrease the serum concentration of Everolimus.

FentaNYL

CYP3A4 Inducers (Moderate) may decrease the serum concentration of FentaNYL.

Glecaprevir and Pibrentasvir

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Glecaprevir and Pibrentasvir.

HYDROcodone

CYP3A4 Inducers (Moderate) may decrease the serum concentration of HYDROcodone.

Ibrutinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Ibrutinib.

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.

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.

Isoniazid

Rifamycin Derivatives may enhance the hepatotoxic effect of Isoniazid. Even so, this is a frequently employed combination regimen.

Lactobacillus and Estriol

Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol.

Mirodenafil

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Mirodenafil.

Naldemedine

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Naldemedine.

Nilotinib

Rifapentine may decrease the serum concentration of Nilotinib.

Pexidartinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Pexidartinib.

Pitolisant

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Pitolisant.

Raltegravir

Rifapentine may increase the serum concentration of Raltegravir. Rifapentine may decrease the serum concentration of Raltegravir.

Rolapitant

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Rolapitant.

RomiDEPsin

Rifapentine may decrease the serum concentration of RomiDEPsin.

Upadacitinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Upadacitinib.

VinCRIStine (Liposomal)

Rifapentine may decrease the serum concentration of VinCRIStine (Liposomal).

Vitamin K Antagonists (eg, warfarin)

Rifamycin Derivatives may increase the metabolism of Vitamin K Antagonists.

Zidovudine

Rifamycin Derivatives may decrease the serum concentration of Zidovudine.

Zolpidem

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Zolpidem.

Risk Factor D (Consider therapy modification)

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.

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.

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.

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.

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.

CycloSPORINE (Systemic)

Rifamycin Derivatives may increase the metabolism of CycloSPORINE (Systemic).

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.

Erdafitinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Erdafitinib. Management: Dose modifications of erdafitinib may be required. See full monograph for details.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

Meperidine

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Meperidine. Management: Consider increasing meperidine dose if concomitant use with moderate CYP3A4 inducers is required. Monitor for signs and symptoms of opioid withdrawal.

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.

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.

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.

Pitavastatin

Rifamycin Derivatives may increase the serum concentration of Pitavastatin. Management: Limit pitavastatin dose to a maximum of 2 mg/day with concurrent rifampin.

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.

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.

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.

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.

Tamoxifen

Rifamycin Derivatives may increase the metabolism of Tamoxifen.

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.

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.

Risk Factor X (Avoid combination)

Abemaciclib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Abemaciclib.

Antihepaciviral Combination Products

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Antihepaciviral Combination Products.

Asunaprevir

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Asunaprevir.

Atovaquone

Rifamycin Derivatives may decrease the serum concentration of Atovaquone.

Axitinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Axitinib.

BCG (Intravesical)

Antibiotics may diminish the therapeutic effect of BCG (Intravesical).

Bedaquiline

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Bedaquiline.

Bictegravir

Rifapentine may decrease the serum concentration of Bictegravir.

Bosutinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Bosutinib.

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.

Cobicistat

Rifapentine may decrease the serum concentration of Cobicistat.

Cobimetinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Cobimetinib.

Darunavir

Rifapentine may decrease the serum concentration of Darunavir.

Dasabuvir

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Dasabuvir.

Deflazacort

CYP3A4 Inducers (Moderate) may decrease serum concentrations of the active metabolite(s) of Deflazacort.

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.

Doravirine

Rifapentine may decrease the serum concentration of Doravirine.

Elbasvir

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Elbasvir.

Elvitegravir

Rifapentine may decrease the serum concentration of Elvitegravir.

Encorafenib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Encorafenib.

Entrectinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Entrectinib.

Etravirine

Rifapentine may decrease the serum concentration of Etravirine.

Fedratinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Fedratinib.

Flibanserin

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Flibanserin.

Grazoprevir

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Grazoprevir.

Ledipasvir

Rifapentine may decrease the serum concentration of Ledipasvir.

Mycophenolate

Rifamycin Derivatives may decrease the serum concentration of Mycophenolate. Specifically, rifamycin derivatives may decrease the concentration of the active metabolite mycophenolic acid.

Neratinib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Neratinib.

Nisoldipine

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Nisoldipine.

Olaparib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Olaparib.

Pimavanserin

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Pimavanserin.

Pretomanid

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Pretomanid.

Ranolazine

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Ranolazine.

Rilpivirine

Rifamycin Derivatives may decrease the serum concentration of Rilpivirine.

Simeprevir

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Simeprevir.

Sofosbuvir

Rifapentine may decrease the serum concentration of Sofosbuvir.

Sonidegib

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Sonidegib.

Tenofovir Alafenamide

Rifapentine may decrease the serum concentration of Tenofovir Alafenamide.

Velpatasvir

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Velpatasvir.

Venetoclax

CYP3A4 Inducers (Moderate) may decrease the serum concentration of Venetoclax.

Voriconazole

May increase the serum concentration of Rifamycin Derivatives. Rifamycin Derivatives may decrease the serum concentration of Voriconazole.

Monitor:

  • Patients with preexisting hepatic problems should have liver function tests monitored (eg, serum transaminases) before 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]) done prior to therapy and then at subsequent clinical visits whose baseline testing is abnormal or for others at risk for liver disease.

How to administer Rifapentine?

  • Give with meals.
  • For patients who cannot swallow tablets, the tablets can be crushed and added to a small amount of semi-solid food and consumed immediately.

Mechanism of action of Rifapentine:

  • It inhibits DNA-dependentRNA polymerase (MTB) in susceptible strains (but not in mammalian cell).
  • Rifapentine can be used to kill both intracellular as well as extracellular MTB bacteria.

Absorption:

  • High-fat meals increase AUC and C by 40% to 50%
  • In pediatric patients, crushing the tablet can result in 26% lower exposure than whole tablets.

Protein binding:

  • Rifapentine: almost 98% is bound to proteins, primarily to albumin
  • 25-desacetyl rifapentine: almost 93%

Metabolism:

  • Hepatic.
  • Hydrolyzed by an esterase enzyme to form the active metabolite 25desacetyl rifapentine

Bioavailability: 70%

Half-life elimination:

  • Rifapentine: almost 17 hours
  • 25-desacetyl rifapentine: almost 24 hours

Time to peak, serum: 3 - 10 hours

Excretion:  

  • From Feces (70%) & urine (17%, primarily as metabolites)
  • In pediatric patients 2 to 18 years of age, clearance usually decreases with increasing age.

International Brands of Rifapentine:

  • Priftin
  • Ming Jia Xin
  • Pentakoks
  • Rifapex

Rifapentine is not available in Pakistan.

Not Available in Pakistan.

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