Indications
Treatment of: Skin and skin structure infections, Otitis
media, Sinusitis, Respiratory infections, Genitourinary
infections. Endocarditis prophylaxis. Postexposure inhalational
anthrax prophylaxis. Management of ulcer
disease due to Helicobacter pylori. Unlabeled Use:
Lyme disease in children 8 yr.
Action
Binds to bacterial cell wall, causing cell death. Therapeutic
Effects: Bactericidal action; spectrum is
broader than penicillins. Spectrum: Active against:
Streptococci, Pneumococci, Enterococci, Haemophilus
influenzae, Escherichia coli, Proteus mirabilis,
Neisseria meningitidis, N. gonorrhoeae, Shigella,
Chlamydia trachomatis, Salmonella, Borrelia burgdorferi,
H. pylori.
Pharmacokinetics
Absorption: Well absorbed from duodenum (75–
90%). More resistant to acid inactivation than other
penicillins.
Distribution: Diffuses readily into most body tissues
and fluids. CSF penetration increased when meninges
are inflamed. Crosses placenta; enters breast milk in
small amounts.
Metabolism and Excretion: 70% excreted unchanged
in the urine; 30% metabolized by the liver.
Half-life: Neonates: 3.7 hr; Infants and Children: 1–
2 hr; Adults: 0.7–1.4 hr.
TIME/ACTION PROFILE (blood levels)
ROUTE ONSET PEAK DURATION
PO 30 min 1–2 hr 8–12 hr
Contraindications/Precautions A
Contraindicated in: Hypersensitivity to penicillins
(cross-sensitivity exists to cephalosporins and other
beta-lactams).
Use Cautiously in: Severe renal insufficiency (p
dose if CCr 30 mL/min); Infectious mononucleosis,
acute lymphocytic leukemia, or cytomegalovirus infection
(qrisk of rash); OB, Lactation: Has been used
safely.
Adverse Reactions/Side Effects
CNS: SEIZURES (high doses). GI: CLOSTRIDIUM DIFFICILE-
ASSOCIATED DIARRHEA (CDAD), diarrhea, nausea,
vomiting,qliver enzymes. Derm: rash, urticaria.
Hemat: blood dyscrasias. Misc: allergic reactions
including ANAPHYLAXIS, SERUM SICKNESS, superinfection.
Interactions
Drug-Drug: Probenecidprenal excretion andq
blood levels of amoxicillin—therapy may be combined
for this purpose. Mayqeffect of warfarin. Maypeffectiveness
of oral contraceptives. Allopurinol mayq
frequency of rash.
Route/Dosage
Most Infections
PO (Adults): 250–500 mg q 8 hr or 500–875 mg q
12 hr (not to exceed 2–3 g/day).
PO (Adults and Children 12 yr): Extended-release
tablets (for Strep throat)—775 mg once daily
for 10 days.
PO (Children 3 mo): 25–50 mg/kg/day in divided
doses q 8 hr or 25–50 mg/kg/day individual doses q
12 hr; Acute otitis media due to highly resistant
strains of S. pneumoniae—80–90 mg/kg/day divided
q 12 hr; Postexposure inhalational anthrax
prophylaxis—40 kg: 45 mg/kg/day in divided doses
q 8 hr; 40 k g: 500 mg q 8 hr.
PO (Infants 3 mo and neonates): 20–30 mg/kg/
day in divided doses q 12 hr.
H. Pylori
PO (Adults): Triple therapy—1000 mg amoxicillin
twice daily with lansoprazole 30 mg twice daily and clarithromycin
500 mg twice daily for 14 days or 1000 mg
amoxicillin twice daily with omeprazole 20 mg twice
daily and clarithromycin 500 mg twice daily for 14 days
or amoxicillin 1000 mg twice daily with esomeprazole
40 mg daily and clarithromycin 500 mg twice daily for
10 days. Dual therapy—1000 mg amoxicillin three
times daily with lansoprazole 30 mg three times daily
for 14 days.
Endocarditis Prophylaxis
PO (Adults): 2 g 1 hr prior to procedure.
PO (Children): 50 mg/kg 1 hr prior to procedure
(not to exceed adult dose).
Gonorrhea
PO (Adults and Children 40 kg): single 3 g dose.
PO (Children 2 yr and 40 kg): 50 mg/kg with
probenecid 25 mg/kg as a single dose.
Renal Impairment
PO (Adults CCr 10–30 mL/min): 250–500 mg q 12
hr.
Renal Impairment
PO (Adults CCr 10 mL/min): 250–500 mg q 24
hr.
Availability (generic available)
Chewable tablets (cherry, banana, peppermint
flavors): 125 mg, 200 mg, 250 mg, 400 mg. Cost: Generic—
250 mg $15.89/30. Tablets: 500 mg, 875 mg.
Cost: Generic—875 mg $9.53/30. Extended-release
tablets: 775 mg. Cost: $524.90/30. Capsules:
250 mg, 500 mg. Cost: Generic—250 mg $5.90/30,
500 mg $5.90/30. Suspension (pediatric drops)
(bubblegum flavor): 50 mg/mL. Powder for oral
suspension (strawberry [125 mg/5 mL] and bubblegum
[200 mg/5 mL, 250 mg/5 mL, 400 mg/5
mL] flavors): 125 mg/5 mL, 200 mg/5 mL, 250 mg/5
mL, 400 mg/5 mL. Cost: Generic—125 mg/5 mL
$4.11/150 mL, 200 mg/5 mL $6.84/75 mL, 250 mg/5
mL $6.09/100 mL, 400 mg/5 mL $7.33/75 mL. In
combination with: clarithromycin and lansoprazole
in a compliance package (Prevpac). See Appendix B.
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