Drug Monograph

Cephalexin (Keflex)

cephalexin monohydrate

First-Generation Cephalosporin · Oral
Pharmacokinetic Profile
Half-Life
0.5–1.2 h (normal renal function)
Metabolism
None — excreted unchanged
Protein Binding
10–15%
Bioavailability
~90% (oral)
Volume of Distribution
~0.23 L/kg
Clinical Information
Drug Class
First-generation cephalosporin (beta-lactam)
Available Doses
250 mg, 500 mg, 750 mg capsules; 125 mg/5 mL, 250 mg/5 mL suspension
Route
Oral only
Renal Adjustment
Yes — required when CrCl <30 mL/min
Hepatic Adjustment
None required
Pregnancy
Compatible — no evidence of fetal harm in animal or epidemiologic studies
Lactation
Compatible — excreted in milk; RID <1%
Schedule
Prescription only (not scheduled)
Generic Available
Yes
Rx

Indications

IndicationApproved PopulationTherapy TypeStatus
Respiratory tract infections (S. pneumoniae, S. pyogenes)Adults & pediatric ≥1 yearMonotherapyFDA Approved
Otitis media (S. pneumoniae, H. influenzae, S. aureus, S. pyogenes, M. catarrhalis)Adults & pediatric ≥1 yearMonotherapyFDA Approved
Skin & skin structure infections (S. aureus [MSSA], S. pyogenes)Adults & pediatric ≥1 yearMonotherapyFDA Approved
Bone infections (S. aureus, P. mirabilis)Adults & pediatric ≥1 yearMonotherapy or step-downFDA Approved
Genitourinary tract infections including acute prostatitis (E. coli, P. mirabilis, K. pneumoniae)Adults & pediatric ≥1 yearMonotherapyFDA Approved

Cephalexin is a workhorse oral antibiotic with strong activity against gram-positive cocci (MSSA, streptococci) and selected gram-negative bacilli (E. coli, K. pneumoniae, P. mirabilis). It has no activity against MRSA, enterococci, Pseudomonas, or Acinetobacter. First-generation cephalosporins remain the preferred oral step-down from IV cefazolin for MSSA infections including osteomyelitis and septic arthritis, and cephalexin is one of the most commonly prescribed antibiotics in the United States.

Off-Label Uses

Infective endocarditis prophylaxis: AHA recommends cephalexin 2 g orally (adults) or 50 mg/kg (pediatric) as a single dose 30–60 minutes before dental procedures in penicillin-allergic patients (non-immediate hypersensitivity) with high-risk cardiac conditions. Evidence quality: High (AHA 2007 guideline).

Streptococcal pharyngitis (alternative): IDSA recommends a 10-day course of a first-generation cephalosporin (cephalexin 20 mg/kg BID, max 500 mg/dose) in penicillin-allergic patients without immediate-type hypersensitivity. Evidence quality: High.

Chronic suppressive therapy for prosthetic joint infections: IDSA recommends cephalexin 500 mg TID–QID as the preferred oral agent for chronic suppression of oxacillin-susceptible staphylococcal prosthetic joint infections. Evidence quality: Moderate.

Step-down from IV cefazolin (MSSA bacteremia, osteomyelitis): Commonly used as sequential oral therapy following initial IV cefazolin in pediatric and adult bone/joint infections. Evidence quality: High (PIDS/IDSA guidelines).

Dose

Dosing

Adult Dosing by Clinical Scenario

Clinical ScenarioStarting DoseMaintenance DoseMaximum DoseNotes
Uncomplicated cellulitis / impetigo (MSSA / GAS)500 mg QID500 mg QID4 g/day7–14 days; IDSA SSTI guideline recommendation
Impetigo may use 250 mg QID
Uncomplicated UTI250 mg Q6H500 mg Q12H4 g/day7–14 days; verify local E. coli susceptibility
500 mg BID shown equivalent to QID in ED study
Streptococcal pharyngitis (alternative to penicillin)500 mg BID500 mg BID1 g/day10 days minimum for GAS; IDSA guideline
Pediatric: 20 mg/kg BID (max 500 mg/dose)
Otitis media250 mg Q6H250 mg Q6H4 g/day7–14 days
Pediatric: 75–100 mg/kg/day in divided doses Q6H
Bone / joint infection — oral step-down500 mg QID500 mg QID4 g/dayTotal duration per clinical response; step-down from IV cefazolin
Higher doses (1 g QID) may be used in severe infections
Endocarditis prophylaxis (penicillin-allergic, non-immediate)2 g single doseN/A2 g30–60 min before dental procedure
AHA 2007; pediatric: 50 mg/kg (max 2 g)
Chronic suppression — prosthetic joint (MSSA)500 mg TID–QID500 mg TID–QID2 g/dayIndefinite; IDSA PJI guideline
Preferred for oxacillin-susceptible staphylococci

Renal Dose Adjustment (Adults & Pediatric ≥15 years)

CrCl (mL/min)Dosage RecommendationMaximum Daily DoseNotesSource
≥60No adjustment4 gStandard dosingFDA PI
30–59No adjustment1 g/dayCap maximum at 1 g/dayFDA PI
15–29250 mg Q8–12H750 mgMonitor renal functionFDA PI
5–14 (not on dialysis)250 mg Q24H250 mgSingle daily doseFDA PI
1–4 (not on dialysis)250 mg Q48–60H250 mgExtended interval dosingFDA PI
Clinical Pearl: Dosing Frequency

Cephalexin’s short half-life (~1 hour) traditionally mandated QID dosing for time-dependent killing. However, BID dosing (500 mg every 12 hours) is now endorsed for uncomplicated infections by the FDA PI and has demonstrated equivalent efficacy for UTIs in a published emergency department study. For serious infections such as osteomyelitis or deep-seated MSSA infections, QID dosing with higher total daily doses (up to 4 g) is preferred to maximise the time above MIC. The drug can be taken with or without food and absorption is not significantly affected by meals.

PK

Pharmacology

Mechanism of Action

Cephalexin is a bactericidal beta-lactam antibiotic that disrupts bacterial cell wall synthesis. It binds irreversibly to penicillin-binding proteins (PBPs), enzymes that catalyse the final transpeptidation step in peptidoglycan cross-linking. By blocking this essential reaction, cephalexin weakens the cell wall, rendering the bacterium vulnerable to osmotic pressure and ultimately resulting in cell lysis and death. The bactericidal effect is time-dependent, meaning clinical efficacy correlates with the proportion of the dosing interval during which free drug concentrations exceed the pathogen’s MIC (% fT > MIC). As a first-generation cephalosporin, cephalexin has excellent activity against gram-positive cocci including MSSA and streptococci, with more modest activity against selected gram-negative organisms. It is inherently inactive against MRSA due to the altered PBP2a target, and has no clinically useful activity against enterococci, Pseudomonas, or anaerobes.

ADME Profile

ParameterValueClinical Implication
Absorption~90% bioavailability; Tmax ~1 h; Cmax 9, 18, 32 mcg/mL at 250, 500, 1000 mg doses respectivelyRapid and nearly complete oral absorption; acid stable; food does not significantly affect total absorption
DistributionVd ~0.23 L/kg; 10–15% protein bound; distributes to kidney, liver, bone, respiratory tractLow protein binding allows high free drug concentrations; good penetration into bone supports use in osteomyelitis step-down therapy
MetabolismNo detectable hepatic metabolism; does not affect CYP450 enzymesVery low drug-drug interaction potential; no hepatic dose adjustment needed
Eliminationt½ 0.5–1.2 h; >90% excreted unchanged in urine within 8 h via glomerular filtration and tubular secretion; peak urine concentrations ~1000–5000 mcg/mLVery high urinary concentrations support efficacy in UTIs; short half-life requires multiple daily dosing; dose reduction needed when CrCl <30 mL/min
SE

Side Effects

Note on Incidence Data

The FDA prescribing information for cephalexin does not report specific percentage incidence rates for individual adverse reactions from pivotal trials. It lists reactions descriptively as “most frequent” or “have been reported.” The incidence estimates below are derived from published clinical literature and systematic reviews, supplemented by class-effect data from first-generation cephalosporin studies.

Most Frequent Very Common
Adverse EffectEstimated IncidenceClinical Note
Diarrhea2–5%Most frequently reported adverse reaction (FDA PI); distinguish from C. difficile if persistent or bloody
Nausea1–3%Usually self-limiting; taking with food may reduce GI intolerance
Dyspepsia / abdominal pain1–3%Grouped in FDA PI with nausea; resolves on completion of therapy
Vomiting1–2%More common in pediatric patients; ensure adequate hydration
Uncommon Common (Reported in Clinical Trials)
Adverse EffectEstimated IncidenceClinical Note
Vaginal candidiasis / genital pruritus<2%Class effect from disruption of normal flora; advise patients about symptoms
Dizziness / headache<2%Rarely treatment-limiting
Fatigue<1%May reflect underlying infection rather than drug effect
Rash / urticaria<2%Evaluate for hypersensitivity; discontinue if progressive
Elevated AST/ALT<1%Slight, transient elevations reported; usually not clinically significant
Eosinophilia<1%Typically transient; may reflect drug hypersensitivity
Serious Serious (Regardless of Frequency)
Adverse EffectEstimated FrequencyTypical OnsetRequired Action
Anaphylaxis / severe hypersensitivityRare (<0.1%)Minutes to hours after first doseDiscontinue immediately; epinephrine; emergency care; do not rechallenge
Stevens-Johnson syndrome / TENVery rare1–3 weeksDiscontinue immediately; dermatology referral; supportive care
Clostridioides difficile-associated diarrheaUncommonDuring or up to 2 months post-therapyTest for C. difficile toxin; discontinue cephalexin; treat with vancomycin or fidaxomicin
Drug-induced hemolytic anemia (positive Coombs’ test)RareDuring therapyDiscontinue; evaluate with direct Coombs’ test and hemolysis workup; transfuse if needed
SeizuresRare (primarily with renal impairment)Variable; risk increases with accumulationDiscontinue; anticonvulsant therapy if needed; dose-adjust for renal function
Interstitial nephritisVery rareDays to weeksDiscontinue; evaluate renal function; usually reversible
Neutropenia / thrombocytopeniaRareProlonged therapy (>2 weeks)Monitor CBC if therapy exceeds 14 days; discontinue if significant cytopenias develop
Discontinuation Discontinuation Rates
Overall
Low
Context: Cephalexin is generally well tolerated. The FDA PI does not report a specific discontinuation rate. Published data suggest discontinuation due to adverse effects is uncommon (<3%), with GI intolerance being the leading reason.
Leading Cause
GI Effects
Top reasons: Diarrhea, nausea, vomiting, abdominal discomfort
Management: Penicillin Allergy Cross-Reactivity

Cross-hypersensitivity between penicillins and cephalosporins occurs in up to 10% of patients with a documented penicillin allergy (FDA PI). This rate is higher for first-generation cephalosporins due to structural R1 side-chain similarity with aminopenicillins. Cephalexin shares an identical R1 side chain with ampicillin/amoxicillin, which is a key determinant of allergic cross-reactivity. Patients with a confirmed immediate-type (IgE-mediated) reaction to amoxicillin or ampicillin should not receive cephalexin. In patients with non-immediate penicillin allergy (e.g., delayed rash), cephalexin can generally be used with appropriate monitoring.

Int

Drug Interactions

Cephalexin undergoes no hepatic metabolism and does not affect CYP450 enzymes, giving it a very favourable drug interaction profile. The two clinically relevant interactions involve altered renal excretion (probenecid) and competition for renal tubular transport (metformin).

Moderate Probenecid
MechanismInhibits renal tubular secretion of cephalexin
EffectProlonged half-life (0.9 → 1.7 h) and elevated plasma concentrations; increased risk of dose-dependent toxicity
ManagementCo-administration not recommended (FDA PI)
FDA PI
Moderate Metformin
MechanismCompetition for renal tubular transport; cephalexin decreases metformin renal clearance by 14%
EffectMetformin Cmax increased ~34% and AUC increased ~24%; potential for hypoglycemia
ManagementMonitor blood glucose carefully; dose-adjust metformin if needed (FDA PI)
FDA PI
Minor Warfarin / Anticoagulants
MechanismCephalosporin class effect on vitamin K-dependent clotting factor synthesis
EffectPotentially prolonged prothrombin time, especially in patients with renal/hepatic impairment, poor nutrition, or prolonged therapy
ManagementMonitor PT/INR in at-risk patients; manage as indicated
FDA PI
Minor Urine Glucose Testing (Benedict’s / Fehling’s)
MechanismCephalexin interferes with copper-reduction urine glucose assays
EffectFalse-positive urine glucose result
ManagementUse glucose oxidase-based methods (e.g., Clinistix) during therapy
FDA PI
Mon

Monitoring

  • Renal Function Baseline; periodically in at-risk patients
    Routine
    Assess CrCl before initiating therapy, particularly in elderly patients. Dose adjustment required when CrCl falls below 30 mL/min. Monitor during therapy if renal impairment is present or develops.
  • Clinical Response 48–72 h after starting therapy
    Routine
    Evaluate for clinical improvement. Consider alternative antibiotics or broader coverage if no response within 48–72 hours. Obtain cultures if not already done.
  • GI Symptoms / Stool If diarrhea develops
    Trigger-based
    Test for C. difficile toxin if diarrhea is persistent, watery, or bloody, or if it develops during or up to 2 months after therapy.
  • CBC If therapy exceeds 14 days
    Trigger-based
    Monitor for neutropenia, thrombocytopenia, and eosinophilia during prolonged courses (e.g., osteomyelitis, chronic suppression).
  • Blood Glucose During concurrent metformin use
    Trigger-based
    Cephalexin increases metformin concentrations. Monitor glucose closely in diabetic patients and adjust metformin dose if needed.
  • PT/INR If on anticoagulants
    Trigger-based
    Monitor prothrombin time in patients on warfarin, especially those with renal or hepatic impairment, poor nutritional status, or receiving prolonged therapy.
CI

Contraindications & Cautions

Absolute Contraindications

  • Known hypersensitivity to cephalexin or any member of the cephalosporin class of antibacterial drugs

Relative Contraindications (Specialist Input Recommended)

  • Immediate-type (IgE-mediated) penicillin allergy (anaphylaxis, urticaria, angioedema) — cross-hypersensitivity may occur in up to 10% of penicillin-allergic patients; risk is higher with cephalexin specifically due to shared R1 side chain with aminopenicillins
  • MRSA infection — cephalexin has no activity against methicillin-resistant staphylococci; confirm susceptibility before initiating empiric therapy

Use with Caution

  • Renal impairment (CrCl <30 mL/min) — dose reduction required; risk of drug accumulation, seizures, and prolonged toxicity
  • Elderly patients — more likely to have impaired renal function; verify CrCl before dosing
  • History of GI disease, particularly colitis — increased susceptibility to C. difficile-associated diarrhea
  • Concurrent anticoagulant therapy — cephalosporins may prolong PT; monitor in patients with renal/hepatic impairment or poor nutritional status
  • Patients under 1 year of age — safety and effectiveness not established in this age group
FDA Class-Wide Safety Advisory Beta-Lactam Cross-Hypersensitivity

Cross-hypersensitivity among beta-lactam antibacterial drugs may occur in up to 10% of patients with a history of penicillin allergy. Before therapy with cephalexin is initiated, clinicians should inquire about previous hypersensitivity reactions to cephalosporins, penicillins, or other drugs. If an allergic reaction to cephalexin occurs, the drug should be discontinued immediately and appropriate treatment should be instituted (FDA PI, revised March 2026).

Pt

Patient Counselling

Purpose of Therapy

Cephalexin is a prescription antibiotic used to treat bacterial infections of the skin, bones, ears, respiratory tract, and urinary tract. It works by weakening and destroying the walls of bacteria. It is effective only against bacterial infections and will not treat viral illnesses such as the common cold or flu.

How to Take

Take cephalexin exactly as prescribed, typically every 6 or 12 hours depending on the infection. It may be taken with or without food; taking it with a meal or snack can help reduce stomach upset. Complete the full course of treatment even if you feel better, as stopping early may allow bacteria to survive and become resistant. Shake the liquid suspension well before each use, and keep it refrigerated (discard after 14 days).

Allergic Reactions
Tell patientAllergic reactions including rash, hives, or swelling can occur. If you have ever had an allergic reaction to penicillin, amoxicillin, or any antibiotic, inform your prescriber before starting cephalexin. Most patients with a mild previous penicillin allergy can safely take cephalexin, but this should be discussed with your prescriber first.
Call prescriberImmediately for any signs of difficulty breathing, facial or throat swelling, widespread rash or hives, or dizziness — these may indicate a serious allergic reaction requiring emergency care.
Diarrhea
Tell patientMild diarrhea is common with antibiotics and usually resolves when the course is completed. However, severe, watery, or bloody diarrhea — even weeks after finishing the course — can indicate a serious condition called C. difficile colitis. Do not take anti-diarrheal medication without consulting your prescriber.
Call prescriberIf diarrhea is severe, bloody, or persists for more than 2 days, or if it develops after finishing the antibiotic.
Diabetes and Metformin
Tell patientIf you take metformin for diabetes, cephalexin can increase metformin levels in your blood, which may raise the risk of low blood sugar. Monitor your blood sugar more frequently during the antibiotic course. Additionally, cephalexin may cause false-positive urine glucose tests if using older test methods.
Call prescriberIf you experience symptoms of low blood sugar (shakiness, sweating, confusion) or if your glucose readings are significantly different from usual.
Completing the Course
Tell patientIt is common to feel better before the antibiotic course is finished. However, stopping cephalexin early increases the risk that bacteria will survive and develop resistance, making the infection harder to treat in the future. Take every dose at the scheduled time.
Call prescriberIf symptoms do not improve within 3 days or worsen at any time during treatment.
Vaginal Yeast Infections
Tell patientAntibiotics can disrupt the normal balance of organisms in the body, sometimes leading to vaginal yeast infections. Symptoms include itching, discharge, and irritation. Over-the-counter antifungal treatments are usually effective.
Call prescriberIf symptoms are severe, recurrent, or if you are uncertain about the cause.
Ref

Sources

Regulatory (PI / SmPC)
  1. Keflex (cephalexin) for oral suspension prescribing information. Pragma Pharmaceuticals, LLC. Revised March 2026. FDA Label Primary source for all approved indications, dosing (including renal adjustment table), adverse reactions, drug interactions, and PK data cited in this monograph.
  2. Keflex (cephalexin) capsules prescribing information. Revised 2019. FDA Label Capsule formulation label with identical PK parameters and clinical information; confirms 250/500/750 mg capsule availability.
Key Clinical Trials / Reviews
  1. Kanan M, Atif S, Mohammed F, et al. A systematic review on the clinical pharmacokinetics of cephalexin in healthy and diseased populations. Antibiotics. 2023;12(9):1402. doi:10.3390/antibiotics12091402 Comprehensive PK systematic review confirming bioavailability (~90%), Vd (0.23 L/kg), half-life (0.5–1.2 h), and renal clearance parameters.
  2. Haynes AS, Wei Z, Anderson P, Scheetz MH, Parker SK, Fish DN. Cefadroxil and cephalexin pharmacokinetics and pharmacodynamics in children with musculoskeletal infections. Antimicrob Agents Chemother. 2024;68(5):e00182-24. doi:10.1128/aac.00182-24 Population PK study in pediatric bone/joint infections; provides Monte Carlo simulations for dosing optimisation and confirms 15% protein binding.
Guidelines
  1. Stevens DL, Bisno AL, Chambers HF, et al. Practice guidelines for the diagnosis and management of skin and soft tissue infections: 2014 update by the IDSA. Clin Infect Dis. 2014;59(2):e10-e52. doi:10.1093/cid/ciu296 IDSA guideline recommending cephalexin 500 mg QID for nonpurulent cellulitis and 250 mg QID for impetigo.
  2. Shulman ST, Bisno AL, Clegg HW, et al. Clinical practice guideline for the diagnosis and management of group A streptococcal pharyngitis: 2012 update by the IDSA. Clin Infect Dis. 2012;55(10):e86-e102. doi:10.1093/cid/cis629 IDSA guideline recommending first-generation cephalosporins as alternative to penicillin for GAS pharyngitis in non-immediate penicillin-allergic patients.
  3. Wilson W, Taubert KA, Gewitz M, et al. Prevention of infective endocarditis: guidelines from the American Heart Association. Circulation. 2007;116(15):1736-1754. doi:10.1161/CIRCULATIONAHA.106.183095 AHA guideline recommending cephalexin 2 g as single-dose endocarditis prophylaxis for penicillin-allergic patients without immediate-type hypersensitivity.
  4. Osmon DR, Berbari EF, Berendt AR, et al. Diagnosis and management of prosthetic joint infection: clinical practice guidelines by the IDSA. Clin Infect Dis. 2013;56(1):e1-e25. doi:10.1093/cid/cis803 IDSA PJI guideline recommending cephalexin as preferred oral agent for chronic suppression of oxacillin-susceptible staphylococcal prosthetic joint infections.
  5. Bradley JS, Byington CL, Shah SS, et al. The management of community-acquired pneumonia in infants and children older than 3 months of age: clinical practice guidelines by the PIDS and the IDSA. Clin Infect Dis. 2011;53(7):e25-e76. doi:10.1093/cid/cir531 PIDS/IDSA guideline recommending cephalexin as preferred step-down for community-acquired pneumonia caused by MSSA in children.
Mechanistic / Basic Science
  1. Tipper DJ. Mode of action of beta-lactam antibiotics. Pharmacol Ther. 1985;27(1):1-35. doi:10.1016/0163-7258(85)90062-2 Foundational review of beta-lactam mechanism of action through PBP binding and cell wall synthesis inhibition.
Pharmacokinetics / Special Populations
  1. Regamey C, Steinberg E, Kirby WMM. Pharmacokinetics of parenteral sodium cephalexin in comparison with cephalothin and cefazolin. Infection. 1977;5(3):173-180. doi:10.1007/BF01642232 Classic PK study confirming cephalexin half-life (0.9 h), renal clearance (252 mL/min/1.73 m²), and the effect of probenecid on half-life prolongation.
  2. Nightingale CH, Greene DS, Quintiliani R. Pharmacokinetics and clinical use of cephalosporin antibiotics. J Pharm Sci. 1975;64(12):1899-1926. doi:10.1002/jps.2600641203 Comprehensive review of cephalosporin PK including cephalexin; confirms protein binding (10–15%), urinary excretion (>90%), and tissue distribution.