Rifapentine inhibits DNA-dependent RNA polymerase in susceptible strains of Mycobacterium tuberculosis. It is bactericidal against both intracellular and extracellular MTB organisms.
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It is used in the treatment of active pulmonary tuberculosis caused by Mycobacterium tuberculosis in adults and children 12 years and older.
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It should be used in combination with one or more anti-tuberculosis drugs to which the isolate is susceptible.
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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.
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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.
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Rifapentine is not recommended in combination with isoniazid for individuals presumed to be exposed to rifamycin- or isoniazid-resistant M. tuberculosis.
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Rifapentine dose in Adults
Dose in the treatment of active Drug-susceptible Tuberculosis:
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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.
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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:
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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
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1 to 32 kg:
- 600 mg once weekly is given
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1 to 50 kg:
- 750 mg once weekly is given
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>50 kg:
- 900 mg once weekly is given
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Once-daily regimen (HIV-infected patients):
- Give for 1 month in combination with isoniazid.
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<35 kg:
- 300 mg once daily is given
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35 to 45 kg:
- 450 mg once daily is given
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>45 kg:
- 600 mg once daily is given
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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:
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Children ≥12 years and Adolescents:
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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.
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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
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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.
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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:
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10 to 14 kg:
- 300 mg/dose once weekly is given
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>14 to 25 kg:
- 450 mg/dose once weekly is given
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>25 to 32 kg:
- 600 mg/dose once weekly is given
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>32 to 50 kg:
- 750 mg/dose once weekly is given
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>50 kg:
- 900 mg/dose once weekly is given
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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:
- The manufacturer's labelling does not mention dosage modifications (has not been studied).
Rifapentine dose in Liver disease:
- The manufacturer's labelling does not mention dosage modifications.
- use cautiously
Common Side Effects of Rifapentine Include:
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Endocrine & Metabolic:
- Hyperuricemia
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Genitourinary:
- Pyuria
- Hematuria
- Urinary Tract Infection
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Hematologic & Oncologic:
- Neutropenia
- Lymphocytopenia
- Anemia
Less Common Side Effects of Rifapentine Include:
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Cardiovascular:
- Chest Pain
- Edema
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Central Nervous System:
- Pain
- Headache
- Dizziness
- Fatigue
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Dermatologic:
- Diaphoresis
- Skin Rash
- Acne Vulgaris
- Pruritus
- Maculopapular Rash
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Endocrine & Metabolic:
- Hypoglycemia
- Hyperglycemia
- Increased Nonprotein Nitrogen
- Gout
- Hyperphosphatemia
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Gastrointestinal:
- Anorexia
- Nausea
- Constipation
- Dyspepsia
- Abdominal Pain
- Diarrhea
- Vomiting
- Hemorrhoids
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Genitourinary:
- Casts In Urine
- Cystitis
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Hematologic & Oncologic:
- Leukopenia
- Thrombocytosis
- Leukocytosis
- Neutrophilia
- Thrombocythemia
- Polycythemia
- Lymphadenopathy
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Hepatic:
- Increased Serum ALT
- Increased Serum AST
- Hepatotoxicity
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Hypersensitivity:
- Hypersensitivity Reaction
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Infection:
- Influenza
- Herpes Zoster
- Infection
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Neuromuscular & Skeletal:
- Back Pain
- Arthralgia
- Osteoarthrosis
- Tremor
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Ophthalmic:
- Conjunctivitis
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Respiratory:
- Hemoptysis
- Cough
- Bronchitis
- Pharyngitis
- Epistaxis
- Pleurisy
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Miscellaneous:
- Accidental Injury
- Fever
Contraindication to Rifapentine Include:
- Hypersensitivity to rifapentine or other rifamycins or any part thereof
Warnings and precautions
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Hypersensitivity reactions
- Hypersensitivity reactions (including anaphylaxis) might occur.
- If hypersensitivity develops, stop therapy and take supportive measures.
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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.
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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.
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Porphyria
- Patients with porphyria should not use it; exacerbation can occur due to enzyme-inducing properties
Rifapentine: Drug Interaction
Abiraterone Acetate |
The serum content of abiraterone acetate may drop when using rifapentine. |
Barbiturates |
The metabolism of barbiturates may be accelerated by rifamycin derivatives. |
BCG Vaccine (Immunization) |
Antibiotics may reduce the BCG vaccine's therapeutic effect (Immunization). |
Benzhydrocodone |
CYP3A4 Inducers (Moderate) may lower the level of benzhydrocodone in the blood. More specifically, hydrocodone serum concentrations might be decreased. |
Beta-Blockers |
Rifamycin derivatives may lower the level of beta-blockers in the blood. Atenolol, Carteolol (Ophthalmic), Levobunolol, Metipranolol, and Nadolol are exceptions |
Cabozantinib |
Cabozantinib's serum levels may drop due to rifapentine. |
CloZAPine |
CloZAPine's serum levels may be lowered by moderate CYP3A4 inducers. |
Codeine |
The active metabolite(s) of codeine's serum concentrations may be lowered by CYP3A4 Inducers (Moderate). |
CYP2C9 Substrates (High risk with Inducers) |
The serum concentration of CYP2C9 Substrates may be reduced by rifapentine (High risk with Inducers). |
CYP3A4 Substrates (High risk with Inducers) |
The serum concentration of CYP3A4 Substrates may drop when taking CYP3A4 Inducers (Moderate) (High risk with Inducers). Apixaban and Rivaroxaban are exceptions. |
Dapsone (Systemic) |
Dapsone serum levels may be decreased by rifamycin derivatives (Systemic). |
Enzalutamide |
Enzalutamide's serum levels may drop due to rifapentine. |
Estriol (Systemic) |
Estriol serum levels may be decreased by moderately potent CYP3A4 inducers (Systemic). |
Estriol (Topical) |
Estriol serum levels may be decreased by moderately potent CYP3A4 inducers (Topical). |
Everolimus |
Rifapentine may lower the level of Everolimus in the blood. |
FentaNYL |
The serum concentration of FentaNYL may drop in response to CYP3A4 Inducers (Moderate). |
Glecaprevir and Pibrentasvir |
Glecaprevir and Pibrentasvir's serum concentrations may be affected by CYP3A4 Inducers (Moderate). |
HYDROcodone |
The serum levels of HYDROcodone may drop in response to CYP3A4 Inducers (Moderate). |
Ibrutinib |
Ibrutinib's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Ifosfamide |
The active metabolite(s) of ifosfamide may be present in lower serum quantities when CYP3A4 Inducers (Moderate) are present. The active metabolite(s) of ifosfamide may be present in higher serum concentrations when CYP3A4 Inducers (Moderate) are used. |
Irinotecan Products |
The serum levels of the active metabolite(s) of irinotecan products may drop when rifapentine is taken. Particularly, serum levels of SN-38 could be decreased. The serum concentration of rifapentine-containing products may drop. |
Isoniazid |
Isoniazid's hepatotoxic effects may be increased by derivatives of rifamycin. Even so, this combined regimen is often used. |
Lactobacillus and Estriol |
The therapeutic effects of Lactobacillus and Estriol may be reduced by antibiotics. |
Mirodenafil |
The serum concentration of Mirodenafil may be decreased by CYP3A4 Inducers (Moderate). |
Naldemedine |
The serum concentration of naldemedine may drop in response to CYP3A4 Inducers (Moderate). |
Nilotinib |
Nilotinib's serum levels may drop due to rifapentine. |
Pexidartinib |
Pexidartinib's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Pitolisant |
Pitolisant's serum levels may drop when taken with CYP3A4 Inducers (Moderate). |
Raltegravir |
Raltegravir's serum levels may rise in response to rifapentine. Raltegravir's serum levels may drop due to rifapentine. |
Rolapitant |
The serum concentration of Rolapitant may fall in response to CYP3A4 Inducers (Moderate). |
RomiDEPsin |
RomiDEPsin's serum levels may drop due to rifapentine. |
Upadacitinib |
Upadacitinib's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
VinCRIStine (Liposomal) |
VinCRIStine serum levels may be decreased by rifapentine (Liposomal). |
Vitamin K Antagonists (eg, warfarin) |
The metabolism of Vitamin K antagonists may be accelerated by rifamycin derivatives. |
Zidovudine |
Zidovudine serum concentrations may drop when using rifamycin derivatives. |
Zolpidem |
CYP3A4 Inducers (Moderate) may lower the level of zolpidem in the blood. |
Risk Factor D (Consider therapy modification) |
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Alfentanil |
Rifamycin derivatives may lower the level of alfentanil in the blood. Management: Keep an eye out for signs of diminished alfentanil efficacy. Alfentanil dosages will probably need to be increased. Alternative options include switching from alfentanil to another opioid anaesthetic (such as sufentanil). |
Antifungal Agents (Azole Derivatives, Systemic) |
Rifamycin derivatives' serum levels can rise. Rifabutin appears to be the only drug impacted. Rifamycin derivatives may lower the level of antifungal agents in the serum (Azole Derivatives, Systemic). Management: Whenever you can, stay away from these pairings. Isavuconazonium and voriconazole are regarded as contraindicated. |
Brigatinib |
The serum concentration of Brigatinib may fall in response to CYP3A4 Inducers (Moderate). Management: Whenever possible, avoid taking brigatinib at the same time as mild CYP3A4 inducers. After seven days of treatment with the current brigatinib dose, increase the daily dose in increments of 30 mg, up to a maximum of twice the dose. |
Calcium Channel Blockers |
Calcium Channel Blockers' serum levels may be reduced by rifamycin derivatives. This predominantly affects calcium channel blockers used orally. Management: Some calcium channel blockers are not recommended for use with rifampin according to their labelling in the US and Canada. |
Clarithromycin |
The active metabolite(s) of clarithromycin may be present in higher serum quantities when CYP3A4 Inducers (Moderate) are present. It is possible for CYP3A4 Inducers (Moderate) to lower the level of clarithromycin in the blood. If a patient is receiving a CYP3A inducer, other antimicrobial therapy should be considered. Drugs that speed up the conversion of 14-hydroxyclarithromycin from clarithromycin may change the clinical action of clarithromycin and reduce its effectiveness. |
CycloSPORINE (Systemic) |
CycloSPORINE metabolism may be increased by rifamycin derivatives (Systemic). |
Daclatasvir |
Rifapentine may lower the level of Daclatasvir in the serum. Management: If used with rifapentine, US labelling advises raising the dose of daclatasvir to 90 mg once daily. The combination of daclatasvir and rifapentine is contraindicated, according to Canadian labelling. |
Erdafitinib |
Erdafitinib's serum levels may be decreased by CYP3A4 Inducers (Moderate). Management: Erdafitinib dosage adjustments may be necessary. For information, see the entire monograph. |
Erlotinib |
Erlotinib's serum levels could drop due to rifapentine. Management: If at all possible, avoid combining. Erlotinib dosage should be increased, if necessary, in combinations, by 50 mg increments every two weeks, as tolerated, up to a daily maximum of 450 mg. |
Estrogen Derivatives (Contraceptive) |
Estrogen derivative serum levels may be reduced by rifamycin derivatives (Contraceptive). Failure with contraception is possible. Management: It is advised to use a complementary, nonhormonal method of birth control. |
GuanFACINE |
GuanFACINE serum levels may be decreased by CYP3A4 Inducers (Moderate). Treatment: When starting guanfacine in a patient receiving a moderate CYP3A4 inducer, increase the guanfacine dose by up to a factor of two. If starting a new treatment, gradually increase the dosage of guanfacine over 1 to 2 weeks. |
HMG-CoA Reductase Inhibitors (Statins) |
HMG-CoA Reductase Inhibitors' serum levels may drop when rifamycin derivatives are used (Statins). Management: Take into account using separate antilipemic medications (note: pitavastatin concentrations may increase with rifamycin treatment). Check for any changes in the effects of HMG-CoA reductase inhibitors. The risk may be lessened with rifabutin, fluvastatin, or pravastatin. Exceptions: Rosuvastatin and pitavastatin. |
Imatinib |
The serum concentration of imatinib may be lowered by rifamycin derivatives. Management: Whenever feasible, refrain from using imatinib and rifamycin derivatives together. If it is necessary to utilise such a combination, increase the imatinib dose by at least 50% and keep a careful eye on the patient's clinical reaction. |
Indinavir |
Indinavir's serum levels could drop due to rifapentine. Management: Because of the potential for lower indinavir concentrations, decreased efficacy, and the emergence of resistance, you should think about avoiding the combination of indinavir and rifapentine whenever you can. |
Lefamulin |
Lefamulin's serum levels may be decreased by CYP3A4 Inducers (Moderate). Management: Unless the advantages outweigh the hazards, avoid using lefamulin concurrently with mild CYP3A4 inducers. |
Lefamulin (Intravenous) |
Lefamulin serum levels may be decreased by moderate CYP3A4 inducers (Intravenous). Management: Lefamulin (intravenous) should not be used concurrently with moderate CYP3A4 inducers unless the advantages outweigh the dangers. |
Lorlatinib |
The hepatotoxic impact of lorlatinib may be enhanced by CYP3A4 Inducers (Moderate). Lorlatinib's serum levels may be decreased by CYP3A4 Inducers (Moderate). Avoid using lorlatinib in combination with mild CYP3A4 inducers. If such a mixture must be used, AST, ALT, and bilirubin levels should be checked within 48 hours after beginning the mixture and at least three times during the first week of use. |
Lurasidone |
Lurasidone's serum levels may be reduced by moderate CYP3A4 inducers. Management: If provided with moderate CYP3A4 inducers for seven or more days, watch for any diminished effects of the lurasidone and consider raising the dose. |
Meperidine |
Meperidine's serum levels may drop if you take CYP3A4 Inducers (Moderate). When using mild CYP3A4 inducers concurrently, the dose of meperidine may need to be increased. Keep an eye out for the effects of opioid withdrawal. |
Methadone |
The serum concentration of methadone may be lowered by derivatives of rifamycin. Management: When possible, look for alternatives. If administered concurrently, keep a close eye out for methadone withdrawal symptoms while starting the rifamycin derivative and for excessive sedation when stopping it. |
Palbociclib |
Palbociclib's serum levels may be decreased by moderate CYP3A4 inducers. Management: The Canadian label advises against using mild CYP3A4 inducers, however the US label makes no particular advice on their use. |
Perampanel |
The serum concentration of Perampanel may be decreased by CYP3A4 Inducers (Moderate). When using perampanel alongside strong and moderate CYP3A4 inducers, the beginning dose should be increased to 4 mg/day. |
Pitavastatin |
Pitavastatin's serum levels may rise as a result of rifamycin derivatives. Limit your intake of pitavastatin to no more than 2 mg per day when taking rifampin at the same time. |
Progestins (Contraceptive) |
Rifamycin derivatives may lower progesterone levels in the blood (Contraceptive). Failure with contraception is possible. Management: It is possible for contraceptives to fail. It is advised to use an alternative, nonhormonal method of birth control. |
QuiNIDine |
QuiNIDine serum levels may be lowered by rifamycin derivatives. Due to the potential for significant quinidine concentration declines, management should consider alternatives to quinidine and rifampin combination therapy. When starting or increasing the dosage of any rifamycin derivative, keep an eye out for any decreasing quinidine concentrations or effects. |
Sodium Picosulfate |
Antibiotics may reduce Sodium Picosulfate's therapeutic impact. Management: If a patient previously used or is currently using an antibiotic, think about utilising an alternative product for bowel cleansing prior to a colonoscopy. |
Tacrolimus (Systemic) |
Tacrolimus serum levels may be decreased by derivatives of rifamycin (Systemic). Management: When feasible, take into account alternatives. If this combination is used, keep an eye out for changes in tacrolimus concentrations or effects after starting or increasing the dose of rifamycin, or for changes in tacrolimus concentrations or effects after stopping or decreasing the dose of rifamycin. |
Tamoxifen |
The metabolism of Tamoxifen may be accelerated by rifamycin derivatives. |
Temsirolimus |
Temsirolimus serum levels may be lowered by rifamycin derivatives. The concentration of the active metabolite sirolimus will probably drop even further as a result of rifamycins. Treatment: The prescribing literature for temsirolimus warns against taking it with potent CYP3A4 inducers like rifampin; nonetheless, if concurrent therapy is required, an increase in the adult dose to 50 mg/week should be taken into consideration. |
Typhoid Vaccine |
The Typhoid Vaccine's therapeutic benefits may be reduced by antibiotics. The only strain impacted is the live attenuated Ty21a strain. Treatment: Patients receiving systemic antibacterial drugs should refrain from receiving the live attenuated typhoid vaccination (Ty21a). It is recommended to wait at least 3 days following the last dose of antibacterial medication before administering this vaccine. |
Risk Factor X (Avoid combination) |
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Abemaciclib |
Abemaciclib's serum levels may be reduced by moderate CYP3A4 inducers. |
Antihepaciviral Combination Products |
Antihepaciviral Combination Products' serum concentration may be decreased by CYP3A4 Inducers (Moderate). |
Asunaprevir |
Asunaprevir's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Atovaquone |
The serum levels of atovaquone may drop if rifamycin derivatives are consumed. |
Axitinib |
Axitinib's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
BCG (Intravesical) |
Antibiotics may lessen BCG's therapeutic effects (Intravesical). |
Bedaquiline |
Bedaquiline's serum levels may be lowered by moderately potent CYP3A4 inducers. |
Bictegravir |
Bictegravir's serum levels may drop due to rifapentine. |
Bosutinib |
Bosutinib's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Cholera Vaccine |
The therapeutic benefit of the cholera vaccine may be reduced by antibiotic use. Management: Cholera vaccine should not be administered to individuals taking systemic antibiotics or within 14 days after taking oral or parenteral antibiotics. |
Cobicistat |
Cobicistat's serum levels may drop if rifapentine is used. |
Cobimetinib |
Cobimetinib's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Darunavir |
Darunavir's serum levels may drop ifripentin is used. |
Dasabuvir |
Dasabuvir's serum levels may be decreased by moderate CYP3A4 inducers. |
Deflazacort |
The serum concentrations of the active metabolite(s) of Deflazacort may be lowered by CYP3A4 Inducers (Moderate). |
Delavirdine |
Delavirdine's metabolism may be accelerated by rifamycin derivatives. Rifamycin derivatives' serum levels may rise in response to delavirdine. Rifabutin serum concentration may rise specifically. |
Doravirine |
Doravirine's serum levels may drop if rifapentine is used. |
Elbasvir |
Elbasvir's serum levels may be reduced by moderate CYP3A4 inducing drugs. |
Elvitegravir |
Elvitegravir's serum levels could drop due to rifapentine. |
Encorafenib |
Encorafenib's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Entrectinib |
Entrectinib's serum levels may be lowered by moderately potent CYP3A4 inducers. |
Etravirine |
Rifapentine may lower the level of etravirine in the serum. |
Fedratinib |
Fedratinib's serum levels may be affected by CYP3A4 Inducers (Moderate). |
Flibanserin |
Flibanserin's serum levels may drop if CYP3A4 Inducers (Moderate) are taken. |
Grazoprevir |
The serum concentration of Grazoprevir may fall in response to CYP3A4 Inducers (Moderate). |
Ledipasvir |
Ledipasvir's serum levels may drop if rifapentine is used. |
Mycophenolate |
The serum levels of mycophenolate may be lowered by rifamycin derivatives. Particularly, the content of the active metabolite mycophenolic acid may be lowered by rifamycin derivatives. |
Neratinib |
Neratinib's serum levels may be reduced by CYP3A4 Inducers (Moderate). |
Nisoldipine |
The serum concentration of nisoldipine may fall in response to CYP3A4 Inducers (Moderate). |
Olaparib |
Olaparib's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Pimavanserin |
Pimavanserin's serum levels may be decreased by moderate CYP3A4 inducers. |
Pretomanid |
Pretomanid's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Ranolazine |
Ranolazine's serum levels may be reduced by moderate CYP3A4 inducers. |
Rilpivirine |
Rilpivirine's serum levels may drop if rifamycin derivatives are consumed. |
Simeprevir |
Simeprevir's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Sofosbuvir |
Sofosbuvir's serum levels may drop due to rifapentine. |
Sonidegib |
Sonidegib's serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Tenofovir Alafenamide |
Tenofovir Alafenamide's serum levels may drop due to rifapentine. |
Velpatasvir |
The serum concentration of Velpatasvir may fall in response to CYP3A4 Inducers (Moderate). |
Venetoclax |
Venetoclax serum levels may be decreased by CYP3A4 Inducers (Moderate). |
Voriconazole |
Rifamycin derivatives' serum levels can rise. Rifamycin derivatives may lower the level of voriconazole in the blood. |
Monitor:
- Liver function tests should be evaluated in patients with pre-existing hepatic issues both before and during treatment (e.g., serum transaminases).
- 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.
- Patients who are unable to take pills can crush them and mix them with a little amount of semi-solid food to be eaten right away.
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.