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rifampin (Rifadin, Rimactane)

 

Classes: Antitubercular Agents

Dosing and uses of Rifadin, Rimactane (rifampin)

 

Adult dosage forms and strengths

capsule

  • 150mg
  • 300mg

injectable powder

  • 600mg

 

Tuberculosis

10 mg/kg/day PO or 10 mg/kg PO twice weekly (directly observed therapy [DOT]); not to exceed 600 mg/day

Dosing considerations

  • May be given in conjunction with isoniazid or with isoniazid and pyrazinamide
  • Rifampin dosage not to exceed 600 mg/day

 

Neisseria Meningitidis Carrier

600 mg q12hr for 2 days

 

Haemophilus Influenzae Type B Infection

Prophylaxis

600 mg/day PO/IV for 4 days

 

Pediatric dosage forms and strengths

capsule

  • 150mg
  • 300mg

injectable powder

  • 600mg

 

Tuberculosis

10-20 mg/kg/day IV/PO or 10-20 mg/kg PO twice weekly (DOT); not to exceed 600 mg/day

 

Neisseria Meningitidis Infection

Prophylaxis

≤1 month: 10 mg/kg/day PO divided q12hr for 2 days

>1 month: 20 mg/kg/day PO divided q12hr for 2 days; not to exceed 600 mg/day

 

Haemophilus Influenzae Type B Infection (Off-label)

Prophylaxis

≤1 month: 10 mg/kg/day PO for 4 days

>1 month: 20 mg/kg/day PO for 4 days; not to exceed 600 mg/day

 

Rifadin, Rimactane (rifampin) adverse (side) effects

1-10%

Elevated liver function test (LFT) results (up to 14%)

Rash (1-5%)

Epigastric distress (1-2%)

Anorexia (1-2%)

Nausea (1-2%)

Vomiting (1-2%)

Diarrhea (1-2%)

Cramps (1-2%)

Pseudomembranous colitis (1-2%)

Pancreatitis (1-2%)

 

Frequency not defined

Muscular weakness

Edema

Flushing

Ataxia

Impaired concentration

Fever

Fatigue

Headache

Numbness

Behavioral changes

Dizziness

 

Warnings

Contraindications

Hypersensitivity to rifamycins

Concomitant administration of live bacterial vaccines

Contraindicated in patients receiving ritonavir-boosted saquinavir, because of increased risk of severe hepatocellular toxicity

Contraindicated in patients receiving atazanavir, darunavir, fosamprenavir, saquinavir, or tipranavir, because rifampin may cause substantial decreases in plasma concentrations of these antiviral drugs, which may result in loss of antiviral efficacy or development of viral resistance

 

Cautions

May decrease the effectiveness of oral contraceptive pills (OCPs)

Do not administer parenteral preparation IM or SC

Patients on regimens of >600 mg once or twice weekly may experience adverse reactions, including flulike syndrome

History of diabetes mellitus (rifampin may make diabetes management more difficult)

Regimens of >600 mg once or twice weekly may cause leukemia, anemia, or thrombocytopenia

Discontinue therapy if patient develops any signs of hepatocellular damage, including hyperbilirubinemia

Prolonged use may result in bacterial or fungal superinfection

Use with caution in patients with liver impairment and porphyria

Not for use in meningococcal disease; may be suitable for short-term use in asymptomatic carriers

Use with caution in patients with history of alcoholism and patients receiving additional medications that may cause hepatotoxicity

Rifampin is not recommended for intermittent therapy; caution patient against intentional or accidental interruption of daily dosage regimen; rare renal hypersensitivity reactions have been reported when therapy was resumed in such cases

Rifampin has enzyme-inducing properties that can enhance metabolism of endogenous substrates, including adrenal hormones, thyroid hormones, and vitamin d

 

Pregnancy and lactation

Pregnancy category: C

Effects unknown; reported to cross placental barrier and appear in cord blood; increased congenital malformations, primarily spina bifida and cleft palate reported in offspring of rodents given oral doses of 150-250 mg/kg/day during pregnancy; case reports of postnatal hemorrhage in mother and infant when administered during last few weeks of pregnancy

Lactation: Drug enters breast milk

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Rifadin, Rimactane (rifampin)

Mechanism of action

Inhibits DNA-dependent RNA polymerase by binding to beta subunit, which in turn blocks RNA transcription; potent enzyme inducer

 

Absorption

PO well absorbed; food may delay or slightly reduce peak

Peak plasma time: PO, 2-4 hr

 

Distribution

Highly lipophilic; crosses blood-brain barrier well, and relative diffusion from blood into CSF is adequate, with or without inflammation (exceeds usual MICs)

Protein bound: 80%

 

Metabolism

Metabolized by liver; undergoes enterohepatic recirculation

 

Elimination

Half-life: 3-4 hr (prolonged in hepatic impairment); in end-stage renal disease, 1.8-11 hr

Excretion: Feces (60-65%) and urine (~30%) as unchanged drug

 

Administration

PO

Take on empty stomach

 

IV Compatibilities

Solution: D5W (at 1.2 g/L within 4 hours)

 

IV Incompatibilities

Solution: NS (may be used within 24 hours)

Additive: Minocycline

Y-Site: Diltiazem

 

IV Preparation

Add 10 mL of SWI to 600 mg of rifampin in viaL

Before administration, solution may be added to 500 mL of D5W or 100 mL of D5W

 

IV Administration

Prepare and administer within 4 hours

In 500 mL of D5W: Infuse within 3 hours

In 100 mL of D5W: Infuse within 30 minutes