agents for atypical mycobacterium
Treatment of the following infections due to susceptible organisms:
Inhibits protein synthesis at the level of the 50S bacterial ribosome.
Bacteriostatic action against susceptible bacteria.Spectrum:
Active against the following gram-positive aerobic bacteria:
Active against these gram-negative aerobic bacteria:
Also active against:
Absorption: Rapidly absorbed (40%) after oral administration. IV administration results in complete bioavailability.
Distribution: Widely distributed to body tissues and fluids. Intracellular and tissue levels exceed those in serum; low CSF levels.
Protein Binding: 7–51%.
Metabolism and Excretion: Mostly excreted unchanged in bile; 4.5% excreted unchanged in urine.
Half-life: 11–14 hr after single dose; 2–4 days after several doses.
TIME/ACTION PROFILE (serum)
|PO||rapid||2.5–3.2 hr||24 hr|
|IV||rapid||end of infusion||24 hr|
Use Cautiously in:
CNS: dizziness, seizures, drowsiness, fatigue, headache
CV: TORSADES DE POINTES, chest pain, hypotension, palpitations, QT interval prolongation
Derm: ACUTE GENERALIZED EXANTHEMATOUS PUSTULOSIS, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS, photosensitivity, rash
F and E: hyperkalemia
GI: HEPATOTOXICITY, CLOSTRIDIOIDES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), abdominal pain, diarrhea, nausea, cholestatic jaundice, ↑ liver enzymes, dyspepsia, flatulence, melena, oral candidiasis, pyloric stenosis
GU: nephritis, vaginitis
Hemat: anemia, leukopenia, thrombocytopenia
Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Most Respiratory and Skin Infections
PO (Adults): 500 mg on 1st day, then 250 mg/day for 4 more days (total dose of 1.5 g); Acute bacterial sinusitis– 500 mg once daily for 3 days.
PO (Children ≥ 6 mo): Pneumonia/Pertussis– 10 mg/kg (not to exceed 500 mg/dose) on 1st day, then 5 mg/kg once daily (not to exceed 250 mg/dose) for 4 more days. Pharyngitis/tonsilitis– 12 mg/kg once daily for 5 days (not to exceed 500 mg/dose); Acute bacterial sinusitis– 10 mg/kg once daily for 3 days.
PO Neonates: Pertussis, treatment and post-exposure prophylaxis– 10 mg/kg once daily for 5 days.
PO (Children ≥6 mo): 30 mg/kg single dose (not to exceed 1500 mg/dose) or 10 mg/kg once daily (not to exceed 500 mg/dose) for 3 days or 10 mg/kg (not to exceed 500 mg/dose) on 1st day, then 5 mg/kg once daily (not to exceed 250 mg/dose) for 4 more days.
Acute Bacterial Exacerbations of Chronic Bronchitis
PO (Adults): 500 mg on 1st day, then 250 mg once daily for 4 more days (total dose of 1.5 g) or 500 mg once daily for 3 days.
IV PO (Adults): More severe– 500 mg IV every 24 hr for at least 2 doses, then 500 mg PO every 24 hr for a total of 7–10 days; Less severe– 500 mg PO, then 250 mg/day PO for 4 more days.
PO (Children >6 mo): 10 mg/kg on 1st day, then 5 mg/kg once daily for 4 more days.
Pelvic Inflammatory Disease
IV PO (Adults): 500 mg IV every 24 hr for 1–2 days, then 250 mg PO every 24 hr for a total of 7 days.
PO (Adults): 500 mg 1 hr before procedure.
PO Children: 15 mg/kg 1 hr before procedure.
Nongonococcal Urethritis, Cervicitis, Chancroid, Chlamydia
PO (Adults): Single 1-g dose.
PO Children: Chancroid: Single 20-mg/kg dose (not to exceed 1000 mg/dose). Urethritis or cervicitis: Single 10-mg/kg dose (not >1000 mg/dose).
PO (Adults): Single 2-g dose.
Prevention of Disseminated MAC Infection
PO (Adults): 1.2 g once weekly (alone or with rifabutin).
PO Children: 5 mg/kg once daily (not >250 mg/dose) or 20 mg/kg (not >1200 mg/dose) once weekly (alone or with rifabutin).
PO (Children ≥6 yrs, ≥40 kg): 500 mg every Monday, Wednesday, and Friday.
PO (Children ≥6 yrs, 25 kg to <40 kg): 250 mg every Monday, Wednesday, and Friday.
Powder for injection (requires reconstitution and dilution): 500 mg/vial
Powder for oral suspension (cherry and banana flavor) (requires reconstitution): 1 g/pkt
Generic: $72.45/3 pkts
Powder for oral suspension (cherry, creme de vanilla, and banana flavor) (requires reconstitution): 100 mg/5 mL, 200 mg/5 mL
Generic: 100 mg/5 mL $34.88/15 mL, 200 mg/5 mL $34.88/22.5 mL
Tablets: 250 mg, 500 mg, 600 mg
Generic: 250 mg $8.82/6, 500 mg $10.03/3, 600 mg $104.62/30
Lab Test Considerations:
May cause ↑ serum bilirubin, AST, ALT, LDH, and alkaline phosphatase concentrations.
Administer 1 hr before or 2 hr after meals.
Resolution of the signs and symptoms of infection. Length of time for complete resolution depends on the organism and site of infection.
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