Look Up > Drugs > Cephalexin
Cephalexin
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(sef a LEKS in)

U.S. Brand Names
Biocef; Keflex®; Keftab®

Generic Available

Yes


Canadian Brand Names
Apo®-Cephalex; Novo-Lexin; Nu-Cephalex

Synonyms
Cephalexin Hydrochloride; Cephalexin Monohydrate

Pharmacological Index

Antibiotic, Cephalosporin (First Generation)


Use

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


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to cephalexin, any component, or cephalosporins


Warnings/Precautions

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


Adverse Reactions

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


Overdosage/Toxicology

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


Drug Interactions

Increased effect: High-dose probenecid decreases clearance

Increased toxicity: Aminoglycosides increase nephrotoxic potential


Stability

Refrigerate suspension after reconstitution; discard after 14 days


Mechanism of Action

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.


Pharmacodynamics/Kinetics

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


Usual Dosage

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%)


Dietary Considerations

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.


Monitoring Parameters

With prolonged therapy monitor renal, hepatic, and hematologic function periodically; monitor for signs of anaphylaxis during first dose


Test Interactions

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


Mental Health: Effects on Mental Status

May cause nervousness; case reports of euphoria, delusion, illusions, and depersonalization with cephalosporins


Mental Health: Effects on Psychiatric Treatment

May rarely cause neutropenia; use caution with clozapine and carbamazepine


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

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.


Nursing Implications

Administer around-the-clock rather than 4 times/day to promote less variation in peak and trough serum levels


Dosage Forms

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


References

"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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