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Pronunciation |
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(sef
a LEKS
in) |
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U.S. Brand
Names |
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Biocef; Keflex®;
Keftab® |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Apo®-Cephalex; Novo-Lexin;
Nu-Cephalex |
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Synonyms |
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Cephalexin Hydrochloride; Cephalexin Monohydrate |
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Pharmacological Index |
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Antibiotic, Cephalosporin (First Generation) |
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Use |
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Dental: An alternate antibiotic to treat orofacial infections in patients
allergic to penicillins; susceptible bacteria including aerobic gram-positive
bacteria and anaerobes. Also, an alternate antibiotic for prevention of
bacterial endocarditis; individuals allergic to amoxicillin (penicillins) may
receive cephalexin provided they have not had an immediate, local, or systemic
IgE-mediated anaphylactic allergic reaction to penicillin. Also, antibiotic for
premedication in patients not allergic to penicillin who may be at potential
increased risk of hematogenous total joint infection.
Medical: Treatment of susceptible bacterial infections, including those
caused by group A beta-hemolytic Streptococcus, Staphylococcus,
Klebsiella pneumoniae, E. coli, Proteus mirabilis, and
Shigella; predominantly used for lower respiratory tract, urinary tract,
skin and soft tissue, and bone and joint; prophylaxis against bacterial
endocarditis in high-risk patients undergoing surgical or dental procedures who
are allergic to penicillin |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to cephalexin, any component, or
cephalosporins |
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Warnings/Precautions |
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Modify dosage in patients with severe renal impairment, prolonged use may
result in superinfection; use with caution in patients with a history of
penicillin allergy, especially IgE-mediated reactions (eg, anaphylaxis,
urticaria); may cause antibiotic-associated colitis or colitis secondary to
C. difficile |
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Adverse
Reactions |
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1% to 10%: Gastrointestinal: Diarrhea
<1%: Dizziness, fatigue, headache, rash, urticaria, angioedema,
anaphylaxis, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson
syndrome, serum-sickness reaction, nausea, vomiting, dyspepsia, gastritis,
abdominal pain, pseudomembranous colitis, interstitial nephritis, agitation,
hallucinations, confusion, arthralgia, eosinophilia, neutropenia,
thrombocytopenia, anemia, increased transaminases, hepatitis, cholestasis
Other reactions with cephalosporins include anaphylaxis, vomiting,
agranulocytosis, colitis, pancytopenia, aplastic anemia, hemolytic anemia,
hemorrhage, prolonged PT, encephalopathy, asterixis, neuromuscular excitability,
seizures, superinfection |
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Overdosage/Toxicology |
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After acute overdose, most agents cause only nausea, vomiting, and diarrhea,
although neuromuscular hypersensitivity and seizures are possible, especially in
patients with renal insufficiency; many beta-lactam antibiotics have the
potential to cause neuromuscular hyperirritability or seizures
Hemodialysis may be helpful to aid in the removal of the drug from the blood
but not usually indicated, otherwise most treatment is supportive or symptom
directed following GI decontamination |
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Drug
Interactions |
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Increased effect: High-dose probenecid decreases clearance
Increased toxicity: Aminoglycosides increase nephrotoxic potential
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Stability |
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Refrigerate suspension after reconstitution; discard after 14
days |
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Mechanism of
Action |
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Inhibits bacterial cell wall synthesis by binding to one or more of the
penicillin-binding proteins (PBPs) which in turn inhibits the final
transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus
inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing
activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while
cell wall assembly is arrested. |
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Pharmacodynamics/Kinetics |
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Absorption: Delayed in young children; may be decreased up to 50% in neonates
Distribution: Widely distributed into most body tissues and fluids, including
gallbladder, liver, kidneys, bone, sputum, bile, and pleural and synovial
fluids; CSF penetration is poor; crosses placenta; appears in breast milk
Protein binding: 6% to 15%
Half-life: Neonates: 5 hours; Children 3-12 months: 2.5 hours; Adults:
0.5-1.2 hours (prolonged with renal impairment)
Time to peak serum concentration: Oral: Within 1 hour
Elimination: 80% to 100% of dose excreted as unchanged drug in urine within 8
hours |
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Usual Dosage |
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Oral:
Adults: 250-1000 mg every 6 hours; maximum: 4 g/day
Prophylaxis of bacterial endocarditis: 2 g 1 hour prior to the procedure
Dosing adjustment in renal impairment: Adults:
Clcr 10-40 mL/minute: 250-500 mg every 8-12 hours
Clcr <10 mL/minute: 250 mg every 12-24 hours
Hemodialysis: Moderately dialyzable (20% to 50%) |
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Dietary
Considerations |
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Food: Peak antibiotic serum concentration is lowered and delayed, but total
drug absorbed is not affected; take on an empty stomach. If GI distress, take
with food. |
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Monitoring
Parameters |
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With prolonged therapy monitor renal, hepatic, and hematologic function
periodically; monitor for signs of anaphylaxis during first
dose |
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Test
Interactions |
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Positive direct Coombs', false-positive urinary glucose test using cupric
sulfate (Benedict's solution, Clinitest®, Fehling's
solution), false-positive serum or urine creatinine with
Jaffé reaction, false-positive urinary proteins and
steroids |
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Mental Health: Effects
on Mental Status |
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May cause nervousness; case reports of euphoria, delusion, illusions, and
depersonalization with cephalosporins |
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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause neutropenia; use caution with clozapine and
carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take as directed, at regular intervals around-the-clock (with or without
food). Chilling oral suspension improves flavor (do not freeze). Complete full
course of medication, even if you feel better. Drink 2-3 L fluid/day. If
diarrhea occurs, yogurt or buttermilk may help. May cause false-positive test
with Clinitest®; use another form of testing. May
interfere with oral contraceptives; additional contraceptive measures are
necessary. Report severe, unresolved diarrhea; vaginal itching or drainage;
sores in mouth; blood, pus, or mucus in stool or urine; easy bleeding or
bruising; unusual fever or chills; rash; or respiratory difficulty.
Breast-feeding precautions: Consult prescriber if
breast-feeding. |
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Nursing
Implications |
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Administer around-the-clock rather than 4 times/day to promote less variation
in peak and trough serum levels |
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Dosage Forms |
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Capsule, as monohydrate: 250 mg, 500 mg
Powder for oral suspension, as monohydrate: 125 mg/5 mL (5 mL unit dose, 60
mL, 100 mL, 200 mL); 250 mg/5 mL (5 mL unit dose, 100 mL, 200 mL)
Suspension, oral, as monohydrate, pediatric: 100 mg/mL [5 mg/drop] (10 mL)
Tablet, as monohydrate: 250 mg, 500 mg, 1 g
Tablet, as hydrochloride: 500 mg |
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References |
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"Advisory Statement. Antibiotic Prophylaxis for Dental Patients With Total Joint Replacements. American Dental Association; American Academy of Orthopedic Surgeons,"
J Am Dent Assoc, 1997, 128(7):1004-8.
Dajani AS, Taubert KA, Wilson W, et al,
"Prevention of Bacterial Endocarditis Recommendations by the American Heart Association,"
JAMA 1997, 277(22):1794-801.
Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med,
1988, 318(7):419-26 and 318(8):490-500.
Saxon A, Beall GN, Rohr AS, et al,
"Immediate Hypersensitivity Reactions to Beta-Lactam Antibiotics," Ann Intern
Med, 1987, 107(2):204-15.
Smith GH, "Oral Cephalosporins in Perspective," DICP, 1990,
24(1):45-51. |
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