Indications
Active tuberculosis or other mycobacterial diseases
(with at least one other drug).
Action
Inhibits the growth of mycobacteria. Therapeutic
Effects: Tuberculostatic effect against susceptible organisms.
Pharmacokinetics
Absorption: Rapidly and well absorbed (80%) from
the GI tract.
Distribution: Widely distributed; crosses bloodbrain
barrier in small amounts; crosses placenta and
enters breast milk.
Protein Binding: 20–30%.
Metabolism and Excretion: 50% metabolized by
the liver, 50% eliminated unchanged by the kidneys.
Half-life: 3.3 hr (increased in renal or hepatic impairment).
TIME/ACTION PROFILE (blood levels)
ROUTE ONSET PEAK DURATION
PO rapid 2–4 hr 24 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Optic neuritis.
Use Cautiously in: Renal and severe hepatic impairment
(dosage reduction required); OB: Although
safety not established, ethambutol has been used with
isoniazid in pregnant women without fetal adverse effects;
Lactation: Usually compatible with breast feeding
(AAP).
Adverse Reactions/Side Effects
CNS: confusion, dizziness, hallucinations, headache,
malaise. EENT: optic neuritis. GI: HEPATITIS, abdominal
pain, anorexia, nausea, vomiting.Metab: hyperuricemia.
MS: joint pain. Neuro: peripheral neuritis.
Resp: pulmonary infiltrates. Misc: anaphylactoid reactions,
fever.
Interactions
Drug-Drug: Neurotoxicity may beqwith other neurotoxic
agents. Aluminum hydroxide may decrease
absorption (space doses 4 hr apart).
Route/Dosage
PO (Adults and Children 13 yr): 15–25 mg/kg/
day (maximum 2.5 g/day) or 50 mg/kg (up to 2.5 g)
twice weekly or 25–30 mg/kg (up to 2.5 g) 3 times
weekly.
PO (Children 1 mo—13 yr): HIV negative—15–
20 mg/kg/day once daily (maximum: 1 g/day) or 50
mg/kg/dose twice weekly (maximum: 2.5 g/dose); HIVexposed/-
infected—15–25 mg/kg/day once daily
(maximum: 2.5 g/day); MAC, secondary prophylaxis,
or treatment in HIV-exposed/-infected—15–25 mg/
kg/day once daily (maximum: 2.5 g/day) with clarithromycin
(or azithromycin) with or without rifabutin;
Nontuberculous mycobacterial infection—15–25
mg/kg/day once daily (maximum: 2.5 g/day).
Availability (generic available)
Tablets: 100 mg, 400 mg.
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