Yes

Antibiotic, Miscellaneous; Antitubercular Agent

Management of active tuberculosis in combination with other agents; eliminate meningococci from asymptomatic carriers; prophylaxis of Haemophilus influenzae type b infection; used in combination with other anti-infectives in the treatment of staphylococcal infections

C

Clinical effects on the fetus: Teratogenicity has occurred in rodents given many times the adult human dose

Hypersensitivity to any rifamycins or any component

Use with caution and modify dosage in patients with liver impairment; observe for hyperbilirubinemia; discontinue therapy if this in conjunction with clinical symptoms or any signs of significant hepatocellular damage develop; since rifampin has enzyme-inducing properties, porphyria exacerbation is possible; use with caution in patients with porphyria; do not use for meningococcal disease, only for short-term treatment of asymptomatic carrier states

Percentage unknown: Flushing, edema headache, drowsiness, dizziness, confusion, numbness, behavioral changes, pruritus, urticaria, pemphigoid reaction, eosinophilia, leukopenia, hemolysis, hemolytic anemia, thrombocytopenia (especially with high-dose therapy), hepatitis (rare), ataxia, myalgia, weakness, osteomalacia, visual changes, exudative conjunctivitis

1% to 10%:

Dermatologic: Rash (1% to 5%)

Gastrointestinal: (1% to 2%): Epigastric distress, anorexia, nausea, vomiting, diarrhea, cramps, pseudomembranous colitis, pancreatitis

Hepatic: Increased LFTs (up to 14%)

Symptoms of overdose include nausea, vomiting, hepatotoxicity

Treatment is supportive; lavage with activated charcoal is preferred to ipecac as emesis is frequently present with overdose; hemodialysis will remove rifampin, its effect on outcome is unknown

CYP3A3/4 enzyme substrate; CYP1A2, 2C9, 2C18, 2C19, 2D6, 3A3/4, and 3A5-7 enzyme inducer

Coadministration with INH or halothane may result in additive hepatotoxicity; probenecid and co-trimoxazole may increase rifampin levels while antacids may decrease its absorption

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

Inhibits bacterial RNA synthesis by binding to the beta subunit of DNA-dependent RNA polymerase, blocking RNA transcription

Absorption: Oral: Well absorbed

Time to peak serum concentration: Oral: 2-4 hours and persisting for up to 24 hours; food may delay or slightly reduce

Distribution: Crosses the blood-brain barrier well

Relative diffusion of antimicrobial agents from blood into cerebrospinal fluid (CSF): Adequate with or without inflammation (exceeds usual MICs)

Ratio of CSF to blood level (%): Inflamed meninges: 25

Protein binding: 80%

Metabolism: Highly lipophilic; metabolized in the liver, undergoes enterohepatic recycling

Half-life: 3-4 hours, prolonged with hepatic impairment

End-stage renal disease: 1.8-11 hours

Elimination: Undergoes enterohepatic recycling; principally excreted unchanged in the feces (60% to 65%) and urine (~30%); excreted unchanged: 15% to 30%; plasma rifampin concentrations are not significantly affected by hemodialysis or peritoneal dialysis

Oral (I.V. infusion dose is the same as for the oral route):

Note: A four-drug regimen (isoniazid, rifampin, pyrazinamide, and either streptomycin or 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)

Directly observed therapy (DOT): Twice weekly: 10-20 mg/kg (maximum: 600 mg); 3 times/week: 10-20 mg/kg (maximum: 600 mg)

Adults:

Daily therapy: 10 mg/kg/day (maximum: 600 mg/day)

Directly observed therapy (DOT): Twice weekly: 10 mg/kg (maximum: 600 mg); 3 times/week: 10 mg/kg (maximum: 600 mg)

H. influenzae prophylaxis:

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

Meningococcal prophylaxis:

<1 month: 10 mg/kg/day in divided doses every 12 hours for 2 days

Infants and Children: 20 mg/kg/day in divided doses every 12 hours for 2 days

Adults: 600 mg every 12 hours for 2 days

Nasal carriers of Staphylococcus aureus:

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

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

Dosing adjustment in hepatic impairment: Dose reductions may be necessary to reduce hepatotoxicity

Food: Rifampin is best taken on an empty stomach since food decreases the extent of absorption

Periodic (baseline and every 2-4 weeks during therapy) monitoring of liver function (AST, ALT, bilirubin BSD), CBC; hepatic status and mental status, sputum culture, chest x-ray 2-3 months into treatment

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

May cause drowsiness, dizziness, confusion, behavioral changes, or ataxia; report of cognitive disturbances, delusions, and hallucinations

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

No information available to require special precautions

No effects or complications reported

Take per recommended schedule. Complete full course of therapy; do not skip doses. Take on an empty stomach (1 hour before or 2 hours after meals). Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Will discolor urine, stool, saliva, tears, sweat, and other body fluids red-brown. Stains on clothing or contact lenses are permanent. Report persistent vomiting; fever, chill, or flu-like symptoms; unusual bruising or bleeding; or other persistent adverse effects. Pregnancy precautions: Inform prescriber if you are or intend to be pregnant or if you are using oral contraceptives (rifampin may effect the effectiveness of certain oral contraceptives).

The compounded oral suspension must be shaken well before using; may mix contents of capsule with applesauce or jelly; 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

Capsule: 150 mg, 300 mg

Injection: 600 mg

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

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

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