|
This information has been developed and provided by an independent third-party source. Merck & Co., Inc. does not endorse and is not responsible for the accuracy of the content, or for practices or
standards of non-Merck sources.
Pronunciation
(rif AM pin)
Generic Available (U.S.)
Yes
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Management of active tuberculosis in combination with other agents; elimination of meningococci from the nasopharynx in asymptomatic carriers
Use: Unlabeled
Prophylaxis of Haemophilus influenzae type b infection; Legionella pneumonia; used in combination with other anti-infectives in the treatment of staphylococcal infections; treatment of M. leprae infections
Pregnancy Risk Factor
C
Pregnancy Considerations
Teratogenic effects have been reported in animal studies. Rifampin crosses the human placenta. Due to the risk of tuberculosis to the fetus, treatment is recommended when the probability of maternal disease is moderate to high. Postnatal hemorrhages have been reported in the infant and mother with isoniazid administration during the last few weeks of pregnancy.
Lactation
Enters breast milk/not recommended (AAP rates “compatible”; AAP 2001 update pending)
Breast-Feeding Considerations
The manufacturer does not recommend breast-feeding due to tumorigenicity observed in animal studies; however, the CDC does not consider rifampin a contraindication to breast-feeding.
Contraindications
Hypersensitivity to rifampin, any rifamycins, or any component of the formulation; concurrent use of amprenavir, saquinavir/ritonavir (possibly other protease inhibitors)
Warnings/Precautions
Concerns related to adverse effects:
• Flu-like syndrome: Regimens of >600 mg once or twice weekly have been associated with a high incidence of adverse reactions including a flu-like syndrome.
• Hematologic effects: May cause thrombocytopenia, leukopenia, or anemia with regimens >600 mg once or twice weekly.
• Hyperbilirubinemia: Discontinue therapy if this occurs in conjunction with clinical symptoms or any signs of significant hepatocellular damage develop.
• Hypersensitivity: Hypersensitivity reactions have occurred in patients taking >600 mg once or twice weekly.
• 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:
• Alcoholism: Use with caution in patients with a history of alcoholism (even if ethanol consumption is discontinued during therapy).
• Hepatic impairment: Use with caution in patients with liver impairment; dosage modification recommended.
• Meningococcal disease: Do not use for meningococcal disease, only for short-term treatment of asymptomatic carrier states.
• Porphyria: Use with caution in patients with porphyria; exacerbations have been reported due to enzyme-inducing properties.
Concurrent drug therapy issues:
• Medications associated with hepatotoxicity: Use with caution in patients receiving concurrent medications associated with hepatotoxicity.
Other warnings/precautions:
• Appropriate administration: Do not administer I.V. form via I.M. or SubQ routes; restart infusion at another site if extravasation occurs.
• Compliance: Monitor for compliance in patients on intermittent therapy.
• Contact lenses: Remove soft contact lenses during therapy since permanent staining may occur.
• Red/orange discoloration: Urine, feces, saliva, sweat, tears, and CSF may be discolored to red/orange.
Adverse Reactions
1% to 10%:
Dermatologic: Rash (1% to 5%)
Gastrointestinal (1% to 2%): Anorexia, cramps, diarrhea, epigastric distress, flatulence, heartburn, nausea, pseudomembranous colitis, pancreatitis, vomiting
Hepatic: LFTs increased (up to 14%)
Frequency not defined:
Cardiovascular: Edema, flushing
Central nervous system: Ataxia, behavioral changes, concentration impaired, confusion, dizziness, drowsiness, fatigue, fever, headache, numbness, psychosis
Dermatologic: Pemphigoid reaction, pruritus, urticaria
Endocrine & metabolic: Adrenal insufficiency, menstrual disorders
Hematologic: Agranulocytosis (rare), DIC, eosinophilia, hemoglobin decreased, hemolysis, hemolytic anemia, leukopenia, thrombocytopenia (especially with high-dose therapy)
Hepatic: Hepatitis (rare), jaundice
Neuromuscular & skeletal: Myalgia, osteomalacia, weakness
Ocular: Exudative conjunctivitis, visual changes
Renal: Acute renal failure, BUN increased, hemoglobinuria, hematuria, interstitial nephritis, uric acid increased
Miscellaneous: Flu-like syndrome
Metabolism/Transport Effects
Substrate of P-glycoprotein, SLCO1B1; Induces CYP1A2 (strong), CYP2A6 (strong), CYP2B6 (strong), CYP2C19 (strong), CYP2C8 (strong), CYP2C9 (strong), CYP3A4 (strong), P-glycoprotein
Drug Interactions
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. Risk D: Consider therapy modification
Amiodarone: Rifamycin Derivatives may increase the metabolism of Amiodarone. Risk C: Monitor therapy
Angiotensin II Receptor Blockers: Rifamycin Derivatives may increase the metabolism of Angiotensin II Receptor Blockers. Exceptions: Candesartan; Eprosartan; Olmesartan; Telmisartan; Valsartan. Risk C: Monitor therapy
Antidiabetic Agents (Thiazolidinedione): Rifampin may increase the metabolism of Antidiabetic Agents (Thiazolidinedione). Risk C: Monitor therapy
Antiemetics (5HT3 Antagonists): Rifamycin Derivatives may increase the metabolism of Antiemetics (5HT3 Antagonists). Exceptions: Dolasetron; Granisetron; Palonosetron. Risk C: Monitor therapy
Antifungal Agents (Azole Derivatives, Systemic): Rifamycin Derivatives may decrease the serum concentration of Antifungal Agents (Azole Derivatives, Systemic). Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Rifamycin Derivatives. Only rifabutin appears to be affected. Risk D: Consider therapy modification
Aprepitant: Rifamycin Derivatives may increase the metabolism of Aprepitant. Risk C: Monitor therapy
ARIPiprazole: CYP3A4 Inducers may decrease the serum concentration of ARIPiprazole. Management: Double aripiprazole dose when initiating concomitant therapy with a CYP3A4 inducer (e.g., carbamazepine). Monitor response and adjust aripiprazole dose as clinically indicated. If CYP3A4 inducer is discontinued, reduce aripiprazole dose to 10-15 mg/day. Risk D: Consider therapy modification
Atazanavir: Rifampin may decrease the serum concentration of Atazanavir. Risk X: Avoid combination
Atovaquone: Rifamycin Derivatives may decrease the serum concentration of Atovaquone. Risk D: Consider therapy modification
Axitinib: CYP3A4 Inducers (Strong) may decrease the serum concentration of Axitinib. Risk X: Avoid combination
Barbiturates: Rifamycin Derivatives may increase the metabolism of Barbiturates. Risk C: Monitor therapy
BCG: Antibiotics may diminish the therapeutic effect of BCG. Risk X: Avoid combination
Bendamustine: CYP1A2 Inducers (Strong) may decrease the serum concentration of Bendamustine. Concentrations of active metabolites may be increased. Risk C: Monitor therapy
Benzodiazepines (metabolized by oxidation): Rifamycin Derivatives may increase the metabolism of Benzodiazepines (metabolized by oxidation). Risk D: Consider therapy modification
Beta-Blockers: Rifamycin Derivatives may decrease the serum concentration of Beta-Blockers. Exceptions: Atenolol; Carteolol; Carteolol (Ophthalmic); Levobunolol; Metipranolol; Nadolol. Risk C: Monitor therapy
Boceprevir: Rifampin may decrease the serum concentration of Boceprevir. Risk X: Avoid combination
Bortezomib: CYP3A4 Inducers (Strong) may decrease the serum concentration of Bortezomib. Risk X: Avoid combination
Brentuximab Vedotin: CYP3A4 Inducers (Strong) may decrease the serum concentration of Brentuximab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be decreased. Risk C: Monitor therapy
BusPIRone: Rifamycin Derivatives may decrease the serum concentration of BusPIRone. Management: The degree to which rifampin alters buspirone concentrations warrants the consideration of an alternative to buspirone that is not metabolized by CYP3A4. If these agents are used together, buspirone dose adjustments may be needed. Risk D: Consider therapy modification
Calcium Channel Blockers: Rifamycin Derivatives may increase the metabolism of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers. Management: The labeling for some U.S. and Canadian calcium channel blockers contraindicate use with rifampin however recommendations vary. Consult appropriate labeling. Exceptions: Clevidipine. Risk D: Consider therapy modification
Caspofungin: Rifampin may decrease the serum concentration of Caspofungin. Management: Caspofungin prescribing information recommends using a dose of 70 mg daily in adults (or 70 mg/m2, up to a maximum of 70 mg, daily in pediatric patients) who are also receiving rifampin. Risk D: Consider therapy modification
Caspofungin: Inducers of Drug Clearance may decrease the serum concentration of Caspofungin. Management: Consider using an increased caspofungin dose of 70 mg daily in adults (or 70 mg/m2, up to a maximum of 70 mg, daily in pediatric patients) when coadministered with known inducers of drug clearance. Risk D: Consider therapy modification
Chloramphenicol: Rifampin may increase the metabolism of Chloramphenicol. Risk D: Consider therapy modification
Clopidogrel: Rifamycin Derivatives may enhance the therapeutic effect of Clopidogrel. Risk C: Monitor therapy
Contraceptives (Estrogens): Rifamycin Derivatives may decrease the serum concentration of Contraceptives (Estrogens). Contraceptive failure is possible. Management: Use of an alternative, nonhormonal contraceptive is recommended. Risk D: Consider therapy modification
Contraceptives (Progestins): Rifamycin Derivatives may decrease the serum concentration of Contraceptives (Progestins). Contraceptive failure is possible. Management: Contraceptive failure is possible. Use of an alternative, nonhormonal contraceptive is recommended. Risk D: Consider therapy modification
Corticosteroids (Systemic): Rifamycin Derivatives may increase the metabolism of Corticosteroids (Systemic). Risk C: Monitor therapy
CycloSPORINE: Rifamycin Derivatives may increase the metabolism of CycloSPORINE. Risk D: Consider therapy modification
CycloSPORINE (Systemic): Rifamycin Derivatives may increase the metabolism of CycloSPORINE (Systemic). Risk D: Consider therapy modification
CYP1A2 Substrates: CYP1A2 Inducers (Strong) may increase the metabolism of CYP1A2 Substrates. Risk C: Monitor therapy
CYP2A6 Substrates: CYP2A6 Inducers (Strong) may increase the metabolism of CYP2A6 Substrates. Risk C: Monitor therapy
CYP2B6 Substrates: CYP2B6 Inducers (Strong) may increase the metabolism of CYP2B6 Substrates. Risk C: Monitor therapy
CYP2C19 Substrates: CYP2C19 Inducers (Strong) may increase the metabolism of CYP2C19 Substrates. Risk C: Monitor therapy
CYP2C8 Substrates: CYP2C8 Inducers (Strong) may increase the metabolism of CYP2C8 Substrates. Risk C: Monitor therapy
CYP2C9 Substrates: CYP2C9 Inducers (Strong) may increase the metabolism of CYP2C9 Substrates. Risk C: Monitor therapy
CYP3A4 Substrates: CYP3A4 Inducers (Strong) may increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
Dabigatran Etexilate: P-glycoprotein/ABCB1 Inducers may decrease the serum concentration of Dabigatran Etexilate. Management: Avoid concurrent use of dabigatran with a p-glycoprotein inducer when possible. Closely monitor for decreased levels/effects of dabigatran if concomitantly administering a p-glycoprotein inducer, particularly strong inducers. Risk X: Avoid combination
Dapsone: Rifamycin Derivatives may increase the metabolism of Dapsone. Risk D: Consider therapy modification
Dapsone (Systemic): Rifamycin Derivatives may increase the metabolism of Dapsone (Systemic). Risk D: Consider therapy modification
Darunavir: Rifampin may decrease the serum concentration of Darunavir. Risk X: Avoid combination
Dasatinib: CYP3A4 Inducers (Strong) may decrease the serum concentration of Dasatinib. Management: Avoid when possible. If such a combination cannot be avoided, consider increasing dasatinib dose and monitor clinical response and toxicity closely. Risk D: Consider therapy modification
Deferasirox: Rifampin may decrease the serum concentration of Deferasirox. Management: Avoid combination when possible; if the combination must be used, consider an increase in initial deferasirox dose to 30 mg/kg, and monitor serum ferritin concentrations/clinical responses to guide further dosing. Risk D: Consider therapy modification
Delavirdine: May decrease the metabolism of Rifamycin Derivatives. Rifamycin Derivatives may increase the metabolism of Delavirdine. Risk D: Consider therapy modification
Diclofenac: CYP2C9 Inducers (Strong) may decrease the serum concentration of Diclofenac. Risk C: Monitor therapy
Disopyramide: Rifamycin Derivatives may decrease the serum concentration of Disopyramide. Risk C: Monitor therapy
Divalproex: Rifampin may decrease the serum concentration of Divalproex. Risk D: Consider therapy modification
Efavirenz: Rifampin may decrease the serum concentration of Efavirenz. Management: Increase efavirenz adult dose to 800 mg daily in patients weighing over 50 kg (per U.S. manufacturer; CDC sets this at 60 kg, and Canadian manufacturer recommends the dose increase regardless of weight). Avoid Atripla (efavirenz/emtricitabine/tenofovir). Risk D: Consider therapy modification
Eltrombopag: May increase the serum concentration of OATP1B1/SLCO1B1 Substrates. Management: According to eltrombopag prescribing information, consideration of a preventative dose reduction may be warranted. Risk D: Consider therapy modification
Erlotinib: Rifampin may increase the metabolism of Erlotinib. Risk D: Consider therapy modification
Esomeprazole: Rifampin may decrease the serum concentration of Esomeprazole. Risk X: Avoid combination
Etravirine: Rifamycin Derivatives may decrease the serum concentration of Etravirine. Risk X: Avoid combination
Exemestane: Rifampin may decrease the serum concentration of Exemestane. Management: Exemestane prescribing information recommends using an increased dose (50 mg/day) in patients receiving concurrent rifampin. Monitor patients closely for evidence of toxicity and/or inadequate clinical response. Risk D: Consider therapy modification
FentaNYL: Rifamycin Derivatives may decrease the serum concentration of FentaNYL. Risk C: Monitor therapy
Fexofenadine: Rifampin may decrease the serum concentration of Fexofenadine. Risk C: Monitor therapy
Fluconazole: May decrease the metabolism of Rifamycin Derivatives. This appears only affect rifabutin. Rifamycin Derivatives may increase the metabolism of Fluconazole. Risk C: Monitor therapy
Fosamprenavir: Rifampin may decrease the serum concentration of Fosamprenavir. Specifically, concentrations of amprenavir (active metabolite) may be decreased. Risk X: Avoid combination
Fosaprepitant: Rifampin may decrease the serum concentration of Fosaprepitant. More specifically, rifampin may decrease concentrations of the active metabolite aprepitant. Risk C: Monitor therapy
Fosphenytoin: Rifamycin Derivatives may decrease the serum concentration of Fosphenytoin. Risk C: Monitor therapy
Gefitinib: Rifamycin Derivatives may increase the metabolism of Gefitinib. Risk D: Consider therapy modification
GuanFACINE: CYP3A4 Inducers (Strong) may decrease the serum concentration of GuanFACINE. Management: Consider increasing the guanfacine dose (within the labeled dosage range) when such a combination is used. Risk D: Consider therapy modification
HMG-CoA Reductase Inhibitors: Rifamycin Derivatives may decrease the serum concentration of HMG-CoA Reductase Inhibitors. 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. Risk D: Consider therapy modification
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. Risk D: Consider therapy modification
Indinavir: Rifampin may decrease the serum concentration of Indinavir. Risk X: Avoid combination
Isoniazid: Rifamycin Derivatives may enhance the hepatotoxic effect of Isoniazid. Even so, this is a frequently employed combination regimen. Risk C: Monitor therapy
Ixabepilone: CYP3A4 Inducers (Strong) may decrease the serum concentration of Ixabepilone. Management: Avoid this combination whenever possible. If this combination must be used, a gradual increase in ixabepilone dose from 40 mg/m2 to 60 mg/m2 (given as a 4-hour infusion), as tolerated, should be considered. Risk D: Consider therapy modification
LamoTRIgine: Rifampin may increase the metabolism of LamoTRIgine. Risk C: Monitor therapy
Leflunomide: Rifampin may increase serum concentrations of the active metabolite(s) of Leflunomide. Risk C: Monitor therapy
Linagliptin: P-glycoprotein/ABCB1 Inducers may decrease the serum concentration of Linagliptin. Management: Strongly consider using an alternative to any strong P-glycoprotein inducer in patients who are being treated with linagliptin. If this combination is used, monitor patients closely for evidence of reduced linagliptin effectiveness. Risk D: Consider therapy modification
Lopinavir: Rifampin may enhance the adverse/toxic effect of Lopinavir. Specifically, the risk of hepatocellular toxicity may be increased. Rifampin may decrease the serum concentration of Lopinavir. Risk X: Avoid combination
Lurasidone: CYP3A4 Inducers (Strong) may decrease the serum concentration of Lurasidone. Risk X: Avoid combination
Macrolide Antibiotics: May decrease the metabolism of Rifamycin Derivatives. Exceptions: Azithromycin; Azithromycin (Systemic); Fidaxomicin; Spiramycin. Risk D: Consider therapy modification
Maraviroc: CYP3A4 Inducers (Strong) may decrease the serum concentration of Maraviroc. Management: Increase maraviroc adult dose to 600 mg twice daily when used with strong CYP3A4 inducers. This does not apply to patients also receiving strong CYP3A4 inhibitors. Do not use maraviroc with strong CYP3A4 inducers in patients with Clcr less than 30 mL/min. Risk D: Consider therapy modification
Methadone: Rifamycin Derivatives may decrease the serum concentration of Methadone. Risk C: Monitor therapy
Morphine (Systemic): Rifamycin Derivatives may decrease the serum concentration of Morphine (Systemic). Risk C: Monitor therapy
Morphine Sulfate: Rifamycin Derivatives may decrease the serum concentration of Morphine Sulfate. Risk C: 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. Risk X: Avoid combination
Nelfinavir: Rifampin may decrease the serum concentration of Nelfinavir. Risk X: Avoid combination
Nevirapine: Rifampin may decrease the serum concentration of Nevirapine. Risk D: Consider therapy modification
Omeprazole: Rifampin may decrease the serum concentration of Omeprazole. Risk X: Avoid combination
OxyCODONE: Rifampin may decrease the serum concentration of OxyCODONE. Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-glycoprotein/ABCB1 Substrates: P-glycoprotein/ABCB1 Inducers may decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Phenytoin: Rifamycin Derivatives may decrease the serum concentration of Phenytoin. Risk C: Monitor therapy
Pitavastatin: Rifamycin Derivatives may increase the serum concentration of Pitavastatin. Management: Limit pitavastatin dose to a maximum of 2 mg/day with concurrent rifampin. Risk D: Consider therapy modification
Prasugrel: Rifampin may diminish the antiplatelet effect of Prasugrel. Risk C: Monitor therapy
Praziquantel: CYP3A4 Inducers (Strong) may decrease the serum concentration of Praziquantel. Management: Avoid concomitant use of praziquantel with strong CYP3A4 inducers. Discontinue rifampin 4 weeks prior to initiation of praziquantel therapy. Rifampin may be resumed the day following praziquantel completion. Risk X: Avoid combination
Propafenone: Rifamycin Derivatives may decrease the serum concentration of Propafenone. Management: Monitor propafenone serum concentrations closely with rifamycin initiation/dose adjustments/discontinuation. Propafenone serum concentrations/therapeutic effects may decrease with rifamycins. Propafenone dose adjustments may be necessary. Risk D: Consider therapy modification
Pyrazinamide: May enhance the hepatotoxic effect of Rifampin. Severe (even fatal) liver injury has been reported in patients receiving these 2 drugs as a 2-month treatment regimen for latent TB infection. Risk D: 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. Risk D: Consider therapy modification
QuiNINE: Rifampin may decrease the serum concentration of QuiNINE. Risk X: Avoid combination
Raltegravir: Rifampin may decrease the serum concentration of Raltegravir. Management: Increase raltegravir dose to 800 mg twice daily (adult dose) when used concomitantly with rifampin. Risk D: Consider therapy modification
Ramelteon: Rifamycin Derivatives may increase the metabolism of Ramelteon. Risk C: Monitor therapy
Ranolazine: Rifampin may decrease the serum concentration of Ranolazine. Risk X: Avoid combination
Repaglinide: Rifamycin Derivatives may increase the metabolism of Repaglinide. Risk C: Monitor therapy
Rilpivirine: Rifamycin Derivatives may decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Ritonavir: Rifampin may decrease the serum concentration of Ritonavir. Risk X: Avoid combination
Roflumilast: Rifampin may decrease the serum concentration of Roflumilast. Management: Roflumilast U.S. prescribing information recommends against combining rifampin with roflumilast. The Canadian product monograph makes no such recommendation but notes that rifampin may reduce roflumilast therapeutic effects. Risk X: Avoid combination
Saquinavir: Rifampin may enhance the adverse/toxic effect of Saquinavir. Specifically, the risk of hepatocellular toxicity may be increased. Rifampin may decrease the serum concentration of Saquinavir. Risk X: Avoid combination
Sirolimus: Rifampin may increase the metabolism of Sirolimus. Risk D: Consider therapy modification
SORAfenib: CYP3A4 Inducers (Strong) may decrease the serum concentration of SORAfenib. Risk X: Avoid combination
Sulfonylureas: Rifampin may increase the metabolism of Sulfonylureas. Risk C: Monitor therapy
Tacrolimus: Rifamycin Derivatives may increase the metabolism of Tacrolimus. Risk D: Consider therapy modification
Tacrolimus (Systemic): Rifamycin Derivatives may increase the metabolism of Tacrolimus (Systemic). Risk D: Consider therapy modification
Tadalafil: CYP3A4 Inducers (Strong) may decrease the serum concentration of Tadalafil. Management: Erectile dysfunction: monitor for decreased effectiveness - no standard dose adjustments recommended. Avoid use of tadalafil for pulmonary arterial hypertension in patients receiving a strong CYP3A4 inducer. Risk D: Consider therapy modification
Tamoxifen: Rifamycin Derivatives may increase the metabolism of Tamoxifen. Risk D: Consider therapy modification
Telaprevir: Rifampin may decrease the serum concentration of Telaprevir. Risk X: 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. Risk D: Consider therapy modification
Terbinafine: Rifampin may decrease the serum concentration of Terbinafine. Risk C: Monitor therapy
Terbinafine (Systemic): Rifamycin Derivatives may increase the metabolism of Terbinafine (Systemic). Risk D: Consider therapy modification
Thyroid Products: Rifampin may decrease the serum concentration of Thyroid Products. Risk C: Monitor therapy
Ticagrelor: CYP3A4 Inducers (Strong) may decrease serum concentrations of the active metabolite(s) of Ticagrelor. CYP3A4 Inducers (Strong) may decrease the serum concentration of Ticagrelor. Risk X: Avoid combination
Tipranavir: Rifampin may decrease the serum concentration of Tipranavir. Risk X: Avoid combination
Toremifene: CYP3A4 Inducers (Strong) may decrease the serum concentration of Toremifene. Risk X: Avoid combination
Treprostinil: CYP2C8 Inducers (Strong) may decrease the serum concentration of Treprostinil. Risk C: 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 24 hours after cessation of antibacterial agents. Risk D: Consider therapy modification
Ulipristal: CYP3A4 Inducers (Strong) may decrease the serum concentration of Ulipristal. Risk C: Monitor therapy
Valproic Acid: Rifampin may decrease the serum concentration of Valproic Acid. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Rifamycin Derivatives may increase the metabolism of Vitamin K Antagonists. Risk C: Monitor therapy
Voriconazole: May increase the serum concentration of Rifamycin Derivatives. Rifamycin Derivatives may decrease the serum concentration of Voriconazole. Risk X: Avoid combination
Zaleplon: Rifamycin Derivatives may increase the metabolism of Zaleplon. Risk C: Monitor therapy
Zidovudine: Rifamycin Derivatives may decrease the serum concentration of Zidovudine. Risk C: Monitor therapy
Zolpidem: Rifamycin Derivatives may decrease the serum concentration of Zolpidem. Risk C: Monitor therapy
Zuclopenthixol: CYP3A4 Inducers (Strong) may decrease the serum concentration of Zuclopenthixol. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may increase risk of hepatotoxicity).
Food: Food decreases the extent of absorption; rifampin concentrations may be decreased if taken with food.
Herb/Nutraceutical: St John's wort may decrease rifampin levels.
Storage
Rifampin powder is reddish brown. Intact vials should be stored at room temperature and protected from excessive heat and light. Reconstituted vials are stable for 24 hours at room temperature.
Stability of parenteral admixture at room temperature (25°C) is 4 hours for D5W and 24 hours for NS.
Reconstitution
Reconstitute powder for injection with SWFI. Prior to injection, dilute in appropriate volume of compatible diluent (eg, 100 mL D5W).
Compatibility
Variable stability (consult detailed reference) in D5W, NS.
Y-site administration: Incompatible: Diltiazem.
Mechanism of Action
Inhibits bacterial RNA synthesis by binding to the beta subunit of DNA-dependent RNA polymerase, blocking RNA transcription
Pharmacodynamics/Kinetics
Duration: ≤24 hours
Absorption: Oral: Well absorbed; food may delay or slightly reduce peak
Distribution: Highly lipophilic; crosses blood-brain barrier well
Relative diffusion from blood into CSF: Adequate with or without inflammation (exceeds usual MICs)
CSF:blood level ratio: Inflamed meninges: 25%
Protein binding: 80%
Metabolism: Hepatic; undergoes enterohepatic recirculation
Half-life elimination: 3-4 hours; prolonged with hepatic impairment; End-stage renal disease: 1.8-11 hours
Time to peak, serum: Oral: 2-4 hours
Excretion: Feces (60% to 65%) and urine (~30%) as unchanged drug
Dosage
Usual dosage ranges: Oral, I.V.:
Infants and Children: 10-20 mg/kg/day as a single dose or in 2 divided doses; maximum: 600 mg/day
Adults: 600 mg once or twice daily
Indication-specific dosing: Oral, I.V.:
Endocarditis, prosthetic valve due to MRSA (unlabeled use): Adults: 300 mg every 8 hours for at least 6 weeks (combine with vancomycin for the entire duration of therapy and gentamicin for the first 2 weeks) (Liu, 2011)
H. influenzae
prophylaxis (unlabeled use):
Infants and Children: 20 mg/kg/day every 24 hours for 4 days, not to exceed 600 mg/dose
Adults: 600 mg every 24 hours for 4 days
Leprosy (unlabeled use): Adults:
Multibacillary: 600 mg once monthly for 24 months in combination with ofloxacin and minocycline
Paucibacillary: 600 mg once monthly for 6 months in combination with dapsone
Single lesion: 600 mg as a single dose in combination with ofloxacin 400 mg and minocycline 100 mg
Meningitis
(Pneumococcus
or
Staphylococcus)
(unlabeled use): Adults: 600 mg once daily
Note: Recommended only for organisms known to be rifampin-susceptible and highly penicillin- or cephalosporin-resistant. May be used in place of or in addition to vancomycin when dexamethasone therapy employed.
Meningococcal meningitis prophylaxis (unlabeled use):
Infants <1 month: 10 mg/kg/day in divided doses every 12 hours for 2 days
Infants ≥1 month and Children: 20 mg/kg/day in divided doses every 12 hours for 2 days (maximum: 600 mg/dose)
Adults: 600 mg every 12 hours for 2 days
Nasal carriers of
Staphylococcus aureus
(unlabeled use): Note: Must use in combination with at least one other systemic antistaphylococcal antibiotic. Not recommended as first-line drug for decolonization; evidence is weak for use in patients with recurrent infections (Liu, 2011).
Children: 15 mg/kg/day divided every 12 hours for 5-10 days in combination with other antibiotics
Adults: 600 mg/day for 5-10 days in combination with other antibiotics
Nontuberculous mycobacterium
(M. kansasii)
(unlabeled use): Adults: 10 mg/kg/day (maximum: 600 mg/day) for duration to include 12 months of culture-negative sputum; typically used in combination with ethambutol and isoniazid
Staphylococcus aureus
infections, adjunctive therapy (unlabeled use): Adults: 600 mg once daily or 300-450 mg every 12 hours with other antibiotics. Note: Must be used in combination with another antistaphylococcal antibiotic to avoid rapid development of resistance (Liu, 2011).
Tuberculosis, active: Note: A four-drug regimen (isoniazid, rifampin, pyrazinamide, and ethambutol) is preferred for the initial, empiric treatment of TB. When the drug susceptibility results are available, the regimen should be altered as appropriate.
Infants and Children <12 years:
Daily therapy: 10-20 mg/kg/day usually as a single dose (maximum: 600 mg/day)
Twice weekly directly observed therapy (DOT): 10-20 mg/kg (maximum: 600 mg)
Adults:
Daily therapy: 10 mg/kg/day (maximum: 600 mg/day)
Twice weekly directly observed therapy (DOT): 10 mg/kg (maximum: 600 mg); 3 times/week: 10 mg/kg (maximum: 600 mg)
Tuberculosis, latent infection (LTBI): As an alternative to isoniazid:
Children: 10-20 mg/kg/day (maximum: 600 mg/day) for 6 months
Adults: 10 mg/kg/day (maximum: 600 mg/day) for 4 months. Note: Combination with pyrazinamide should not generally be offered (MMWR, Aug 8, 2003).
Dosing adjustment in renal impairment: No dosage adjustment required in renal impairment.
Poorly dialyzed; no supplemental dose or dosage adjustment necessary, including patients on intermittent hemodialysis, peritoneal dialysis, or continuous renal replacement therapy (eg, CVVHD).
Dosing adjustment in hepatic impairment: Dose reductions may be necessary to reduce hepatotoxicity
Administration: Oral
Administer on an empty stomach with a glass of water (ie, 1 hour prior to, or 2 hours after meals or antacids) to increase total absorption (food may delay and reduce the amount of rifampin absorbed). The compounded oral suspension must be shaken well before using. May mix contents of capsule with applesauce or jelly.
Administration: I.M.
Do not administer I.M. or SubQ
Administration: I.V.
Administer I.V. preparation by slow I.V. infusion over 30 minutes to 3 hours at a final concentration not to exceed 6 mg/mL.
Administration: I.V. Detail
Avoid extravasation.
pH: 7.8-8.8
Monitoring Parameters
Periodic (baseline and every 2-4 weeks during therapy) monitoring of liver function (AST, ALT, bilirubin), CBC, mental status, sputum culture, chest x-ray 2-3 months into treatment
Test Interactions
May interfere with urine detection of opiates (false-positive); positive Coombs' reaction [direct], rifampin inhibits standard assay's ability to measure serum folate and B12; transient increase in LFTs and decreased biliary excretion of contrast media
Dietary Considerations
Rifampin should be taken on an empty stomach.
Patient Education
Rifampin may be prescribed in conjunction with other antibiotics; maintain dosing schedule as directed. Take rifampin on an empty stomach, 1 hour before or 2 hours after meals. Keep appointments for scheduled laboratory tests and chest x-rays. This medication will discolor urine, stool, saliva, tears, sweat, and other body fluids a red-brown color. Stains on contact lenses and clothing are permanent. Report persistent vomiting, diarrhea, rash, fever, chills, flu-like symptoms, or unusual bruising or bleeding.
Geriatric Considerations
Rifampin, in combination with isoniazid, is the foundation of tuberculosis treatment. Since most older patients acquired their Mycobacterium tuberculosis infection before effective chemotherapy was available, either a 9-month regimen of isoniazid and rifampin or a 6-month regimen of isoniazid and rifampin with pyrazinamide (the first 2 months) should be effective.
Anesthesia and Critical Care Concerns/Other Considerations
Clinical Pearls/Comments: Rifampin causes body secretions to turn orange and may stain contact lenses.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause drowsiness, dizziness, confusion, behavioral changes, or ataxia; report of cognitive disturbances, delusions, and hallucinations
Mental Health: Effects on Psychiatric Treatment
May cause leukopenia; use caution with clozapine and carbamazepine; rifampin is a potent hepatic enzyme inducer; monitor for altered clinical effects when used concurrently with psychotropics
Nursing: Physical Assessment/Monitoring
Concurrent use with rifampin may decrease levels/effects of multiple other drugs; analyze complete medical regimen. Infusion site must be monitored to prevent extravasation. Assess results of chest x-ray. Monitor for hypersensitivity reactions, hepatotoxicity, CNS changes, hematologic changes, visual disturbances, and gastrointestinal upset on a regular basis during therapy. Monitor patient compliance with treatment regimen.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, oral: 150 mg, 300 mg
Rifadin®: 150 mg, 300 mg
Injection, powder for reconstitution: 600 mg
Rifadin®: 600 mg
Pricing: U.S. (www.drugstore.com)
Capsules (Rifadin)
150 mg (60): $166.32
Capsules (Rifampin)
150 mg (60): $115.99
300 mg (30): $64.99
Extemporaneously Prepared
A rifampin 1% w/v suspension (10 mg/mL) may be made with capsules and one of four syrups (Syrup NF, simple syrup, Syrpalta® syrup, or raspberry syrup). Empty the contents of four 300 mg capsules or eight 150 mg capsules onto a piece of weighing paper. If necessary, crush contents to produce a fine powder. Transfer powder to a 4-ounce amber glass or plastic prescription bottle. Rinse paper and spatula with 20 mL of chosen syrup and add the rinse to bottle; shake vigorously. Add 100 mL syrup to the bottle and shake vigorously. Label "shake well". Stable for 4 weeks at room temperature or refrigerated.
A 25 mg/mL oral suspension may be made with capsules and cherry syrup concentrate diluted 1:4 with simple syrup, NF. Empty the contents of ten 300 mg capsules into a mortar and reduce to a fine powder. Add 20 mL of the vehicle and mix to a uniform paste; mix while adding the vehicle in incremental proportions to almost 120 mL; transfer to a calibrated bottle, rinse mortar with vehicle, and add quantity of vehicle sufficient to make 120 mL. Label "shake well" and "refrigerate". Stable for 28 days refrigerated (preferred) or at room temperature.
Nahata MC, Pai VB, and Hipple TF, Pediatric Drug Formulations, 5th ed, Cincinnati, OH: Harvey Whitney Books Co, 2004.
References
Acocella G, “Clinical Pharmacokinetics of Rifampicin,“ Clin Pharmacokinet, 1978, 3(2):108-27.
Advenier C, Gobert C, Houin G, et al, “Pharmacokinetic Studies of Rifampicin in the Elderly,” Ther Drug Monit, 1983, 5(1):61-5.
American Academy of Pediatrics Committee on Drugs, "Transfer of Drugs and Other Chemicals Into Human Milk," Pediatrics, 2001, 108(3):776-89.
American Academy of Pediatrics Committee on Infectious Diseases, “Chemotherapy for Tuberculosis in Infants and Children,” Pediatrics, 1992, 89(1):161-5.
American Academy of Pediatrics, “Pediatric Infections,“ Red Book®: 2006 Report of the Committee on Infectious Diseases, 27th ed, Pickering LK, ed, Elk Grove Village, IL: American Academy of Pediatrics, 2006, 530.
American Thoracic Society, “Targeted Tuberculin Testing and Treatment of Latent Tuberculosis Infection,” MMWR Recomm Rep, 2000, 49(RR-6):1-51.
Askgaard DS, Wilcke T, and Dossing M, “Hepatotoxicity Caused by the Combined Action of Isoniazid and Rifampin,” Thorax, 1995, 50(2):213-4.
Baddour LM, Wilson WR, Bayer AS, et al, “Infective Endocarditis. Diagnosis, Antimicrobial Therapy, and Management of Complications: A Statement for Healthcare Professionals From the Committee on Rheumatic Fever, Endocarditis, and Kawasaki Disease, Council on Cardiovascular Disease in the Young, and the Councils on Clinical Cardiology, Stroke, and Cardiovascular Surgery and Anesthesia, American Heart Association - Executive Summary: Endorsed by the Infectious Diseases Society of America,” Circulation, 2005, 111(23):3167-184.
Bass JB Jr, Farer LS, Hopewell PC, et al, “Treatment of Tuberculosis and Tuberculosis Infection in Adults and Children,” Am J Respir Crit Care Med, 1994, 149(5):1359-74.
Blumberg HM, Burman WJ, Chaisson RE, et al, “American Thoracic Society/Centers for Disease Control and Prevention/Infectious Diseases Society of America: Treatment of Tuberculosis,” Am J Respir Crit Care Med, 2003, 167(4):603-62.
Borcherding SM, Baciewicz AM, and Self TH, “Update on Rifampin Drug Interactions. II,” Arch Intern Med, 1992, 152(4):711-6.
Centers for Disease Control, “Update: Adverse Event Data and Revised American Thoracic Society/CDC Recommendations Against the Use of Rifampin and Pyrazinamide for Treatment of Latent Tuberculosis Infection - United States, 2003,” MMWR, 52(31);735-9. Available at http://www.cdc.gov/mmwr/preview/mmwrhtml/mm5231a4.htm
Daher R, Haidar JH, and Al-Amin H, “Rifampin Interference With Opiate Immunoassays,” Clin Chem, 2002, 48(1):203-4.
Davidson PT and Le HQ, “Drug Treatment of Tuberculosis - 1992,” Drugs, 1992, 43(5):651-73.
De Vriese AS, Robbrecht DL, Vanholder RC, et al, “Rifampicin-Associated Acute Renal Failure: Pathophysiologic, Immunologic, and Clinical Features,” Am J Kidney Dis, 1998, 31(1):108-15.
“Drugs for Tuberculosis,” Med Lett Drugs Ther, 1993, 35(908):99-101.
Furlan V, Perello L, Jacquemin E, et al, “Interactions Between FK506 and Rifampicin or Erythromycin in Pediatric Liver Recipients,” Transplantation, 1995, 59(8):1217-8.
Gould FK, Denning DW, Elliott TS, et al, “Guidelines for the Diagnosis and Antibiotic Treatment of Endocarditis in Adults: A Report of the Working Party of the British Society for Antimicrobial Chemotherapy,” J Antimicrob Chemother, 2012, 67(2):269-89.
Griffith DE, Aksamit T, Brown-Elliott BA, et al, “An Official ATS/IDSA Statement: Diagnosis, Treatment, and Prevention of Nontuberculous Mycobacterial Diseases,” Am J Respir Crit Care Med, 2007, 175(4):367-416.
Havlir DV and Barnes PF, “Tuberculosis in Patients With Human Immunodeficiency Virus Infection,” N Engl J Med, 1999, 340(5):367-73.
Herrera Trevilla P, Ortiz Jimenez E, Tena T, et al, “Presence of Rifampicin in Urine Causes Cross-Reactivity With Opiates Using the KIMS Method,” J Anal Toxicol, 1995, 19(3):200.
Holdiness MR, “A Review of the Redman Syndrome and Rifampicin Overdose,” Med Toxicol Adverse Drug Exp, 1989, 4(6):444-51.
Iseman MD, “Treatment of Multidrug-Resistant Tuberculosis,” N Engl J Med, 1993, 329(11):784-91.
Kindelan JM, Serrano I, Jurado R, et al, “Rifampin-Induced Severe Thrombocytopenia in a Patient With Pulmonary Tuberculosis,” Ann Pharmacother, 1994, 28(11):1304-5.
Liu C, Bayer A, Cosgrove SE, et al, “Clinical Practice Guidelines by the Infectious Diseases Society of America for the Treatment of Methicillin-Resistant Staphylococcus Aureus Infections in Adults and Children: Executive Summary,” Clin Infect Dis, 2011, 52(3):285-92.
Lundstrom TS and Sobel JD, “Vancomycin, Trimethoprim-Sulfamethoxazole, and Rifampin,” Infect Dis Clin North Am, 1995, 9(3):747-67.
Nahata MC, Morosco RS, and Hipple TF, “Effect of Preparation Method and Storage on Rifampin Concentration in Suspensions,” Ann Pharmacother, 1994, 28(2):182-5.
Noble A, “Antituberculous Therapy and Acute Liver Failure,” Lancet, 1995, 345(8953):867.
Orisakwe OE, Dioka CE, Orish CN, et al, “Charcoal and Rifampicin Pharmacokinetics,” Am J Therapeut, 1995, 68-70.
Plomp TA, Battista HJ, Unterdorfer H, et al, “A Case of Fatal Poisoning by Rifampicin,” Arch Toxicol, 1981, 48(4):245-52.
“Prevention and Treatment of Tuberculosis Among Patients Infected With Human Immunodeficiency Virus: Principles of Therapy and Revised Recommendations. Centers for Disease Control and Prevention,” MMWR Recomm Rep, 1998, 47(RR-20):1-58.
Starke JR, “Modern Approach to the Diagnosis and Treatment of Tuberculosis in Children,” Pediatr Clin North Am, 1988, 35(3):441-64.
Starke JR, “Multidrug Therapy for Tuberculosis in Children,” Pediatr Infect Dis J, 1990, 9(11):785-93.
“Treatment of Latent Tuberculosis Infection (LTBI), Last Updated: April 8, 2004.” Available at http://www.cdc.gov/nchstp/tb/pubs/tbfactsheets/250110.htm. Last accessed February 16, 2005.
Tunkel AR, Hartman BJ, Kaplan SL, et al, “Practice Guidelines for the Management of Bacterial Meningitis,” Clin Infect Dis, 2004, 39(9):1267-84.
Van Scoy RE and Wilkowske CJ, “Antituberculosis Agents,” Mayo Clin Proc, 1992, 67(2):179-87.
Vesely JJ, Pien FD, and Pien BC, “Rifampin, a Useful Drug for Nonmycobacterial Infections,” Pharmacotherapy, 1998, 18(2):345-57.
Walker-Renard P, “Pruritus Associated With Intravenous Rifampin,” Ann Pharmacother, 1995, 29(3):267-8.
Wong P, Bottoroff MB, Heritage RW, et al, “Acute Rifampin Overdose: A Pharmacokinetic Study and Review of the Literature,” J Pediatr, 1984, 104(5):781-3.
Yoshikawa TT, “Tuberculosis in Aging Adults,” J Am Geriatr Soc, 1992, 40(2):178-87.
International Brand Names
Lexi-Comp.com
Last full review/revision March 2012
|
