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Medication Safety Issues

Sound-alike/look-alike issues:

Rifadin® may be confused with Rifater®, Ritalin®

Rifampin may be confused with ribavirin, rifabutin, Rifamate®, rifapentine, rifaximin

Pronunciation

(rif AM pin)

U.S. Brand Names

• Rifadin®

Index Terms

• Rifampicin

Generic Available

Yes

Canadian Brand Names

• Rifadin®
• Rofact™

Pharmacologic Category

• Antibiotic, Miscellaneous
• Antitubercular Agent

Pharmacologic Category Synonyms

• Tuberculosis Treatment Agent

Use: Labeled Indications

Management of active tuberculosis in combination with other agents; elimination of meningococci from the nasopharynx in asymptomatic carriers

Use: Unlabeled/Investigational

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 bee 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”)

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

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

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%)

Metabolism/Transport Effects

Induces CYP1A2 (strong), 2A6 (strong), 2B6 (strong), 2C8 (strong), 2C9 (strong), 2C19 (strong), 3A4 (strong)

Drug Interactions

Alfentanil: Rifamycin Derivatives may increase the metabolism of Alfentanil. 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): 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). Exceptions: Miconazole. Risk D: Consider therapy modification

Aprepitant: Rifamycin Derivatives may increase the metabolism of Aprepitant. Risk C: Monitor therapy

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

Barbiturates: Rifamycin Derivatives may increase the metabolism of Barbiturates. Risk C: Monitor therapy

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; Levobunolol; Metipranolol; Nadolol. Risk C: Monitor therapy

BusPIRone: Rifamycin Derivatives may increase the metabolism of BusPIRone. 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. 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 70mg daily in adults (or 70mg/m², up to a maximum of 70mg, 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 70mg daily in adults (or 70mg/m², up to a maximum of 70mg, 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

Contraceptive (Progestins): Rifamycin Derivatives may decrease the serum concentration of Contraceptive (Progestins). Contraceptive failure is possible. 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

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 (High risk): CYP2C8 Inducers (Highly Effective) may increase the metabolism of CYP2C8 Substrates (High risk). Risk C: Monitor therapy

CYP2C9 Substrates (High risk): CYP2C9 Inducers (Highly Effective) may increase the metabolism of CYP2C9 Substrates (High risk). Risk C: Monitor therapy

CYP3A4 Substrates: CYP3A4 Inducers (Strong) may increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy

Dabigatran Etexilate: P-Glycoprotein Inducers may decrease the serum concentration of Dabigatran Etexilate. Risk C: Monitor therapy

Dapsone: Rifamycin Derivatives may increase the metabolism of Dapsone. Risk D: Consider therapy modification

Deferasirox: Rifampin may decrease the serum concentration of Deferasirox. Management: Increase deferasirox dose and increase monitoring of serum ferritin concentrations when using deferasirox with rifampin or other potent enzyme inducers. Doses greater than 40mg/kg are not recommended. 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

Disopyramide: Rifamycin Derivatives may increase the metabolism of Disopyramide. Risk D: Consider therapy modification

Dronedarone: CYP3A4 Inducers (Strong) may decrease the serum concentration of Dronedarone. Risk X: Avoid combination

Efavirenz: Rifampin may decrease the serum concentration of Efavirenz. Management: Efavirenz dose adjustment (to 800mg daily) may be required, particularly for patients weighing more than 60kg. Risk C: Monitor therapy

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

Etravirine: Rifamycin Derivatives may decrease the serum concentration of Etravirine. Risk X: Avoid combination

Everolimus: CYP3A4 Inducers (Strong) may decrease the serum concentration of Everolimus. Management: Everolimus prescribing information recommends avoiding concurrent use of strong CYP3A4 inducers, but if strong CYP3A4 inducers cannot be avoided, consider gradually (in 5mg increments) increasing the everolimus dose from 10mg/day to 20mg/day. Risk X: Avoid combination

Exemestane: Rifampin may increase the metabolism of Exemestane. 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

Fosaprepitant: Rifampin may decrease the serum concentration of Fosaprepitant. More specifically, rifampin may decrease concentrations of the active metabolite aprepitant. Risk C: Monitor therapy

Gadoxetate: Rifampin may increase the serum concentration of Gadoxetate. Additionally, rifampin may interfere with the hepatic uptake of gadoxetate (and consequently, inhibit both hepatic contrast enhancement and biliary excretion of gadoxetate). Risk C: Monitor therapy

Gefitinib: Rifamycin Derivatives may increase the metabolism of Gefitinib. Risk D: Consider therapy modification

HMG-CoA Reductase Inhibitors: Rifamycin Derivatives may increase the metabolism of HMG-CoA Reductase Inhibitors. Exceptions: Rosuvastatin. Risk D: Consider therapy modification

Imatinib: Rifamycin Derivatives may increase the metabolism of Imatinib. Risk D: Consider therapy modification

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

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

Macrolide Antibiotics: May decrease the metabolism of Rifamycin Derivatives. Exceptions: Azithromycin; Dirithromycin [Off Market]; Spiramycin. Risk D: Consider therapy modification

Maraviroc: CYP3A4 Inducers (Strong) may decrease the serum concentration of Maraviroc. Management: Maraviroc adult dose should be increased to 600 mg twice daily when used with strong CYP3A4 inducers. This recommendation only applies in the absence of a concurrent strong CYP3A4 inhibitor (e.g., most protease inhibitors). Risk D: Consider therapy modification

Methadone: Rifamycin Derivatives may increase the metabolism of Methadone. 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

Nevirapine: Rifampin may decrease the serum concentration of Nevirapine. Risk D: Consider therapy modification

Nilotinib: CYP3A4 Inducers (Strong) may decrease the serum concentration of Nilotinib. Risk X: Avoid combination

Oral Contraceptive (Estrogens): Rifamycin Derivatives may decrease the serum concentration of Oral Contraceptive (Estrogens). Contraceptive failure is possible. Risk D: Consider therapy modification

P-Glycoprotein Inducers: May decrease the serum concentration of P-Glycoprotein 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 Inhibitors: May increase the serum concentration of P-Glycoprotein 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 Substrates: P-Glycoprotein Inducers may decrease the serum concentration of P-Glycoprotein 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 increase the metabolism of Phenytoin. Risk D: Consider therapy modification

Prasugrel: Rifampin may diminish the antiplatelet effect of Prasugrel. Risk C: Monitor therapy

Praziquantel: Rifampin may decrease the serum concentration of Praziquantel. Risk X: Avoid combination

Propafenone: Rifamycin Derivatives may increase the metabolism of Propafenone. Risk D: Consider therapy modification

Protease Inhibitors: May decrease the metabolism of Rifamycin Derivatives. Specifically rifabutin. Rifamycin Derivatives may decrease the serum concentration of Protease Inhibitors. Rifampin administration should be avoided. Dosage adjustments with both rifabutin and the protease inhibitors are necessary if used together. Management: Avoid using rifampin with protease inhibitors. Rifabutin and protease inhibitor dose adjustments will likely be required when using rifabutin together with protease inhibitors; consult specific protease inhibitor(s) prescribing information. 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 increase the metabolism of QuiNIDine. 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 800mg twice daily 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

Saxagliptin: CYP3A4 Inducers may decrease the serum concentration of Saxagliptin. Risk C: Monitor therapy

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 D: Consider therapy modification

Sulfonylureas: Rifampin may increase the metabolism of Sulfonylureas. Risk C: Monitor therapy

Sunitinib: Rifamycin Derivatives may increase the metabolism of Sunitinib. Risk D: Consider therapy modification

Tacrolimus: Rifamycin Derivatives may increase the metabolism of Tacrolimus. 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 C: Monitor therapy

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 dose to 50 mg/week should be considered. Risk D: Consider therapy modification

Terbinafine: Rifamycin Derivatives may increase the metabolism of Terbinafine. Risk D: Consider therapy modification

Thyroid Products: Rifampin may decrease the serum concentration of Thyroid Products. Risk C: Monitor therapy

Tocainide: Rifamycin Derivatives may increase the metabolism of Tocainide. Risk C: Monitor therapy

Tolvaptan: CYP3A4 Inducers (Strong) may decrease the serum concentration of Tolvaptan. Management: If concurrent use is necessary, increased doses of tolvaptan (with close monitoring for toxicity and clinical response) may be needed. Risk X: Avoid combination

Treprostinil: CYP2C8 Inducers (Highly Effective) 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. Risk D: Consider therapy modification

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 increase the metabolism of Zidovudine. Risk D: Consider therapy modification

Zolpidem: Rifamycin Derivatives may increase the metabolism of Zolpidem. 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.

Compatibility when admixed: Incompatible: Minocycline.

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.:

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): 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.

Infants and Children: 20 mg/kg/day as a single dose or in 2 divided doses; maximum: 600 mg/day

Adults: 600 mg once daily

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):

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

Synergy for Staphylococcus aureus infections (unlabeled use): Adults: 300-600 mg twice daily with other antibiotics

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 hepatic impairment: Dose reductions may be necessary to reduce hepatotoxicity

Hemodialysis or peritoneal dialysis: Plasma rifampin concentrations are not significantly affected by hemodialysis or peritoneal dialysis.

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 once daily 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; hepatic status and mental status, sputum culture, chest x-ray 2-3 months into treatment

Test Interactions

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

Do not take any new medication during therapy without consulting prescriber. Rifampin may be prescribed in conjunction with another medication; maintain dosing schedule of both drugs as directed. Take rifampin on an empty stomach, 1 hour before or 2 hours after meals. It is extremely important that you complete full course of therapy and do not skip doses. Keep appointments for scheduled laboratory tests and chest x-rays. This medication will discolor urine, stool, saliva, tears, sweat, and other body fluid a red-brown color. Stains on contact lenses and clothing are permanent. Report persistent vomiting or diarrhea; rash; fever, chills, or flu-like symptoms; unusual bruising or bleeding; or other persistent adverse effects. Pregnancy precaution: Inform prescriber if you are or intend to become pregnant. This drug may interfere with effectiveness of oral/systemic contraceptives; consult prescriber for alternative contraceptive measures.

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

Assess potential for interactions with other pharmacological agents patient may be taking (eg, concurrent use with rifampin may decrease levels/effects of multiple other drugs, including some oral contraceptives, anticoagulants, hypoglycemics, and beta-blockers). See Administration for infusion specifics; infusion site must be monitored to prevent extravasation. Assess results of periodic laboratory tests and chest x-ray, therapeutic effectiveness, and adverse reactions (eg, hypersensitivity reactions, hepatotoxicity, CNS changes, hematologic changes, visual disturbances, and gastrointestinal upset) on a regular basis during therapy. Monitor patient compliance with treatment regimen. Teach patient proper use, possible side effects/appropriate interventions, and adverse symptoms to report.

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule: 150 mg, 300 mg

Injection, powder for reconstitution: 600 mg

Pricing: U.S. (www.drugstore.com)

Capsules (Rifadin)

150 mg (60): $148.99

Capsules (Rifampin)

300 mg (30): $64.99

Extemporaneously Prepared

For pediatric and adult patients with difficulty swallowing or where lower doses are needed, the package insert lists an extemporaneous liquid suspension as follows:

Rifampin 1% w/v suspension (10 mg/mL) can be compounded using one of four syrups (Syrup NF, simple syrup, Syrpalta® syrup, or raspberry syrup)

Empty 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 blend to a 4 oz amber glass or plastic prescription bottle

Rinse paper and spatula with 20 mL of syrup and add the rinse to bottle; shake vigorously

Add 100 mL of syrup to the bottle and shake vigorously

This compounding procedure results in a 1% w/v suspension containing 10 mg rifampin/mL; stability studies indicate suspension is stable at room temperature (25°C ± 3°C) or in refrigerator (2°C to 8°C) for 4 weeks; shake well prior to administration

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 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.

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International Brand Names

• Arficin (HR)
• Diabacil (ES)
• Dinoldin (ES)
• Eremfat (DE)
• Fenampicin (ES)
• Fimizina (ES)
• Manorifcin (TH)
• Medifam (PH)
• Oxitrin (PY)
• Prolung (ID)
• Ramicin (ID)
• Rifabiotic (ID)
• Rifacilin (IN)
• Rifadex (EC)
• Rifadin (AE, AR, AU, BF, BH, BJ, CI, CY, CZ, EG, ET, GB, GH, GM, GN, GR, HK, IE, IL, IQ, IR, IT, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MX, NE, NG, NL, OM, PH, PK, PT, QA, SA, SC, SD, SE, SL, SN, SY, TN, TW, TZ, UG, YE, ZA, ZM, ZW)
• Rifadine (BE, FR, LU)
• Rifagen (ES)
• Rifaldin (BR, CN, ES)
• Rifaldin[inj.] (ES)
• Rifamax (PH)
• Rifamcin (TH)
• Rifamed (HU)
• Rifampicin Labatec (CH)
• Rifampicyna (PL)
• Rifampin (KP)
• Rifapiam (IT)
• Rifapin (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE)
• Rifaprodin (ES)
• Rifarad (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IL, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TN, TZ, UG, YE, ZA, ZM, ZW)
• Rifarm (FI)
• Rifasynt (HK, MY)
• Rifodex (KP)
• Rifoldin (AT)
• Rifoldine (CH)
• Rifonilo (ES)
• Riforal (ES)
• Rimactan (AT, BG, CH, CO, DK, ES, FR, HR, IT, LU, MX, NL, NO, PE, SE, UY, VE)
• Rimactane (BB, BF, BJ, BM, BS, BZ, CI, ET, GB, GH, GM, GN, GY, HK, ID, IL, IN, JM, KE, LR, MA, ML, MR, MU, MW, MY, NE, NG, SC, SD, SL, SN, SR, TH, TN, TT, TZ, UG, ZA, ZM, ZW)
• Rimactan[inj.] (CH)
• Rimafed (PH)
• Rimapen (FI)
• Rimecin (TH)
• Rimpacin (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IL, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TN, TZ, UG, YE, ZA, ZM, ZW)
• Rimpin (IN)
• Rimycin (AU)
• Ripin (TW)
• Tubocin (HU)
• Tugaldin (ES)

Lexi-Comp.com

Last full review/revision September 2009

Content last modified September 2009