Rifampin

— THERAPEUTIC CATEGORIES —
  • Bacterial infections
  • Tuberculosis
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Rifampin Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Rifampin 150mg, 300mg; caps.

    Pharmacological Class

    Rifamycin.

    See Also

      How Supplied

      Contact supplier

      Manufacturer

      Various generic manufacturers

      Mechanism of Action

      Rifampin inhibits DNA-dependent RNA polymerase activity in susceptible Mycobacterium tuberculosis organisms. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme.

      Rifampin Indications

      Indications

      Asymptomatic carriers of Neisseria meningitidis to eliminate meningococci from nasopharynx. Not for treatment of meningococcal infection.

      Rifampin Dosage and Administration

      Adult

      Give 1hr before or 2hrs after meals with water. 600mg twice daily for 2 days.

      Children

      Give 1hr before or 2hrs after meals with water. <1 month: 5mg/kg every 12hrs for 2 days. ≥1 month: 10mg/kg every 12hrs for 2 days; max 600mg per dose. Preparation of suspension: see full labeling.

      Rifampin Contraindications

      Contraindications

      Concomitant ritonavir-boosted saquinavir (increased risk of severe hepatotoxicity). Concomitant atazanavir, darunavir, fosamprenavir, saquinavir, tipranavir. Concomitant praziquantel. Concomitant lurasidone. Rifamycin hypersensitivity.

      Rifampin Boxed Warnings

      Not Applicable

      Rifampin Warnings/Precautions

      Warnings/Precautions

      Meningococcal: reserve rifampin for cases where high risk of meningococcal disease exists; confirm diagnosis. Not recommended for intermittent therapy (risk of rare renal hypersensitivity reactions). Monitor for hypersensitivity or severe cutaneous reactions (eg, SJS, TEN, DRESS); discontinue if occur. Monitor for signs of liver injury (esp. in prolonged treatment). If hepatic impaired: obtain LFTs at baseline, then every 2–4 weeks during therapy. Discontinue if signs of hepatic damage occur or worsen. Vitamin K-dependent coagulation disorders, bleeding; monitor. Pulmonary toxicity. Thrombotic microangiopathy (including thrombotic thrombocytopenic purpura, hemolytic uremia syndrome). Diabetes. May stain teeth, body secretions, contact lenses. IV: avoid extravasation. Elderly. Pregnancy. Nursing mothers: not recommended.

      Rifampin Pharmacokinetics

      Absorption

      Readily absorbed from the gastrointestinal tract. Absorption is reduced by about 30% when taken with food.

      Distribution

      Widely distributed throughout the body. Plasma protein bound: ~80%.

      Metabolism

      Rifampin undergoes progressive deacetylation.

      Elimination

      Renal (up to 30%). Half-life: ~3.35±0.66 hours (after a 600 mg oral dose); 5.08±2.45 hours (after a 900 mg dose).

      Rifampin Interactions

      Interactions

      See Contraindications. Discontinue rifampin 4 weeks before giving praziquantel; may be restarted one day after completing praziquantel treatment. Avoid concomitant zidovudine, indinavir, efavirenz, daclatasvir, simeprevir, sofosbuvir, telaprevir, halothane, quinine, ticagrelor, and alcohol. Concomitant hepatotoxic agents: may cause fatal liver dysfunction. Antagonizes oral or other hormonal contraceptives (consider nonhormonal methods), phenytoin, antiarrhythmics, tamoxifen, toremifene, haloperidol, azole antifungals (avoid 2 weeks before and during itraconazole), β-blockers, diazepam, zopiclone, zolpidem, CCBs, prednisolone, moxifloxacin, sulfonylureas, cyclosporine, oxycodone, morphine, ondansetron, simvastatin, rosiglitazone, nortriptyline, enalapril, chloramphenicol, clarithromycin, dapsone, doxycycline, irinotecan, levothyroxine, losartan, methadone, telithromycin, theophylline. Risk of bleeding with clopidogrel; do not use. Monitor warfarin, digoxin, tacrolimus; adjust dose as needed. May be potentiated by probenecid, cotrimoxazole. Concomitant atovaquone: not recommended. Separate dosing of antacids by at least 1hr. May cause false (+) urine tests for opiates. May inhibit assays for serum folate and Vit. B12 (consider alternative methods). Perform LFTs and use contrast media prior to morning dose.

      Rifampin Adverse Reactions

      Adverse Reactions

      GI disturbances, jaundice, headache, fever, drowsiness, fatigue, ataxia, dizziness, inability to concentrate, mental confusion, muscular weakness, pain in extremities, generalized numbness, visual disturbances, elevated BUN and serum uric acid, menstrual disturbances, urticaria, rash, edema; hepatotoxicity, hepatitis, abnormal LFTs, cholestasis, paradoxical drug reaction, interstitial lung disease; rare: blood dyscrasias, anaphylaxis.

      Rifampin Clinical Trials

      See Literature

      Rifampin Note

      Notes

      Formerly known under the brand name Rifadin.

      Rifampin Patient Counseling

      See Literature

      Rifampin Generic Name & Formulations

      Legal Class

      Rx

      General Description

      Rifampin 150mg, 300mg; caps.

      Pharmacological Class

      Rifamycin.

      See Also

      How Supplied

      Caps—contact supplier; Vials—1

      Manufacturer

      Various generic manufacturers

      Mechanism of Action

      Rifampin inhibits DNA-dependent RNA polymerase activity in susceptible Mycobacterium tuberculosis organisms. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme.

      Rifampin Indications

      Indications

      Susceptible tuberculosis, in combination with other antituberculars.

      Rifampin Dosage and Administration

      Adult

      10mg/kg once daily; max 600mg/day. Caps: give 1hr before or 2hrs after meals with water. IV: infuse over 30mins (100mL) or within 3hrs (500mL). Initial phase: treat for up to 2 months with isoniazid and pyrazinamide (streptomycin or ethambutol may be added as fourth drug if resistance to isoniazid exists). After initial phase, continue rifampin with isoniazid for at least 4 months; longer if sputum or culture remains (+), with resistant organisms, or HIV (+).

      Children

      10–20mg/kg once daily; max 600mg/day. Caps: give 1hr before or 2hrs after meals with water. IV: infuse over 30mins (100mL) or within 3hrs (500mL). Initial phase: treat for up to 2 months with isoniazid and pyrazinamide (streptomycin or ethambutol may be added as fourth drug if resistance to isoniazid exists). After initial phase, continue rifampin with isoniazid for at least 4 months; longer if sputum or culture remains (+), with resistant organisms, or HIV (+). Preparation of suspension: see full labeling.

      Rifampin Contraindications

      Contraindications

      Concomitant ritonavir-boosted saquinavir (increased risk of severe hepatotoxicity). Concomitant atazanavir, darunavir, fosamprenavir, saquinavir, tipranavir. Concomitant praziquantel. Concomitant lurasidone. Rifamycin hypersensitivity.

      Rifampin Boxed Warnings

      Not Applicable

      Rifampin Warnings/Precautions

      Warnings/Precautions

      Meningococcal: reserve rifampin for cases where high risk of meningococcal disease exists; confirm diagnosis. Not recommended for intermittent therapy (risk of rare renal hypersensitivity reactions). Monitor for hypersensitivity or severe cutaneous reactions (eg, SJS, TEN, DRESS); discontinue if occur. Monitor for signs of liver injury (esp. in prolonged treatment). If hepatic impaired: obtain LFTs at baseline, then every 2–4 weeks during therapy. Discontinue if signs of hepatic damage occur or worsen. Vitamin K-dependent coagulation disorders, bleeding; monitor. Pulmonary toxicity. Thrombotic microangiopathy (including thrombotic thrombocytopenic purpura, hemolytic uremia syndrome). Diabetes. May stain teeth, body secretions, contact lenses. IV: avoid extravasation. Elderly. Pregnancy. Nursing mothers: not recommended.

      Rifampin Pharmacokinetics

      Absorption

      Readily absorbed from the gastrointestinal tract. Absorption is reduced by about 30% when taken with food.

      Distribution

      Widely distributed throughout the body. Plasma protein bound: ~80%.

      Metabolism

      Rifampin undergoes progressive deacetylation.

      Elimination

      Renal (up to 30%). Half-life: ~3.35±0.66 hours (after a 600 mg oral dose); 5.08±2.45 hours (after a 900 mg dose).

      Rifampin Interactions

      Interactions

      See Contraindications. Discontinue rifampin 4 weeks before giving praziquantel; may be restarted one day after completing praziquantel treatment. Avoid concomitant zidovudine, indinavir, efavirenz, daclatasvir, simeprevir, sofosbuvir, telaprevir, halothane, quinine, ticagrelor, and alcohol. Concomitant hepatotoxic agents: may cause fatal liver dysfunction. Antagonizes oral or other hormonal contraceptives (consider nonhormonal methods), phenytoin, antiarrhythmics, tamoxifen, toremifene, haloperidol, azole antifungals (avoid 2 weeks before and during itraconazole), β-blockers, diazepam, zopiclone, zolpidem, CCBs, prednisolone, moxifloxacin, sulfonylureas, cyclosporine, oxycodone, morphine, ondansetron, simvastatin, rosiglitazone, nortriptyline, enalapril, chloramphenicol, clarithromycin, dapsone, doxycycline, irinotecan, levothyroxine, losartan, methadone, telithromycin, theophylline. Risk of bleeding with clopidogrel; do not use. Monitor warfarin, digoxin, tacrolimus; adjust dose as needed. May be potentiated by probenecid, cotrimoxazole. Concomitant atovaquone: not recommended. Separate dosing of antacids by at least 1hr. May cause false (+) urine tests for opiates. May inhibit assays for serum folate and Vit. B12 (consider alternative methods). Perform LFTs and use contrast media prior to morning dose.

      Rifampin Adverse Reactions

      Adverse Reactions

      GI disturbances, jaundice, headache, fever, drowsiness, fatigue, ataxia, dizziness, inability to concentrate, mental confusion, muscular weakness, pain in extremities, generalized numbness, visual disturbances, elevated BUN and serum uric acid, menstrual disturbances, urticaria, rash, edema; hepatotoxicity, hepatitis, abnormal LFTs, cholestasis, paradoxical drug reaction, interstitial lung disease; rare: blood dyscrasias, anaphylaxis.

      Rifampin Clinical Trials

      See Literature

      Rifampin Note

      Notes

      Formerly known under the brand name Rifadin.

      Rifampin Patient Counseling

      See Literature

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