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ethambutol (Myambutol)

 

Classes: Antitubercular Agents

Dosing and uses of Myambutol (ethambutol)

 

Adult dosage forms and strengths

tablet

  • 100mg
  • 400mg

 

Tuberculosis

Prescribing information

  • Initial TB treatment: 15 mg/kg PO qDay
  • Prior TB treatment: 25 mg/kg PO qDay; after 60 days, decrease to 15 mg/kg PO qDay

Daily administration

  • Guidelines from American Thoracic Society (ATS), Centers for Disease Control and Prevention (CDC), and the Infectious Diseases Society of America (IDSA)
  • 40-55 kg: 800 mg PO
  • 56-75 kg: 1.2 g PO
  • >75 kg: 1.6 g PO

Twice weekly administration

  • Guidelines from American Thoracic Society (ATS), Centers for Disease Control and Prevention (CDC), and the Infectious Diseases Society of America (IDSA)
  • 40-55 kg: 2 g PO
  • 56-75 kg: 2.8 g PO
  • >75 kg: 4 g PO

3x per week administration

  • Guidelines from American Thoracic Society (ATS), Centers for Disease Control and Prevention (CDC), and the Infectious Diseases Society of America (IDSA)
  • 40-55 kg: 1.2 g PO
  • 56-75 kg: 2 g PO
  • >75 kg: 2.4 g PO

 

Disseminated MAC (Off-label)

Treatment: 15 mg/kg PO qd

Prophylaxis: use same dose with other antibiotics

 

Pulmonary M. Avium Complex (MAC) without HIV (Off-label)

25 mg/kg PO qD; after 60 d, decrease to 15 mg/kg PO qd

 

Other Indications & Uses

Tuberculosis: intended to be used concomitantly with other anti-TB drugs; usually isoniazid initially; subsequently, use second-line anti-TB drugs

Off-label: MAC infections

 

Pediatric dosage forms and strengths

tablet

  • 100mg
  • 400mg

 

Tuberculosis

Prescribing information

  • Use not recommended in patients <13 years, but has been used in peds

ATS, CDC, and IDSA

  • Guidelines from American Thoracic Society (ATS), Centers for Disease Control and Prevention (CDC), and the Infectious Diseases Society of America (IDSA)
  • 15-20 mg/kg/day PO; not to exceed 1 g/day OR
  • 50 mg/kg PO 2x/week; not to exceed 2.5 g/dose

AAp

  • Guidelines from the American Academy of Pediatrics (AAP)
  • 15-25 mg/kg/day PO; not to exceed 1 g/day OR
  • 50 mg/kg PO 2x/week; not to exceed 2.5 g/dose

 

Disseminated MAC, Prophylaxis (Off-label)

As adult, 15 mg/kg PO qDay combined with other drugs; not to exceed 1 g/day

 

Myambutol (ethambutol) adverse (side) effects

Frequency not defined

Acute gout or hyperuricemia

Abdominal pain

Anaphylaxis

Anorexia

Confusion, disorientation

Fever

Headache

LFT abnormalities

Malaise

Nausea

Optic neuritis; symptoms may include decreased acuity, color blindness or visual defects (usually revrsible with discontinuation, though irreversible blindness has been reported)

Peripheral neuritis

Pruritis

Rash

Vomiting

 

Warnings

Contraindications

Optic neuritis

Hypersensitivity

 

Cautions

See pkg insert for complete dosage info

< 5 yo: may be difficult to monitor visual acuity

 

Pregnancy and lactation

Pregnancy category: B

Lactation: enters breast milk; use with caution (AAP Committee states "compatible with nursing")

 

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 Myambutol (ethambutol)

Mechanism of action

Interferes with metabolite production in Mycobacterium

 

Absorption

Bioavailability: ~80%

Peak Plasma Time: 2-4 hr

 

Distribution

Widely throughout body; concentrated in kidneys, lungs, saliva, and red blood cells

Relative diffusion from blood into CSF: Adequate with or without inflammation (exceeds usual MICs)

CSF:blood level ratio: 0% (normal meninges); 25% (inflamed meninges)

Protein binding: 20-30%

 

Metabolism

Hepatic (20%) to inactive metabolite

 

Elimination

Half-life elimination: 2.5-3.6 hr; 7-15 hr (end-stage renal disease)

Excretion: ~50% urine; ~20% feces as unchanged drug