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How is cephalexin eliminated from the body? A Pharmacological Review

3 min read

Over 90% of a cephalexin dose is excreted unchanged in the urine within 8 hours, highlighting the kidney's critical role [1.3.1]. Understanding how is cephalexin eliminated from the body is crucial for safe and effective use, especially in certain patient populations.

Quick Summary

Cephalexin is eliminated almost entirely by the kidneys. It is not metabolized by the liver and is excreted unchanged in the urine through glomerular filtration and tubular secretion. Kidney health is the primary factor affecting its clearance rate.

Key Points

  • Primary Renal Elimination: Over 90% of cephalexin is eliminated unchanged by the kidneys within 8 hours of administration [1.3.1].

  • No Liver Metabolism: Cephalexin is not metabolized in the body, meaning the liver is not involved in its clearance [1.8.1, 1.8.5].

  • Dual Kidney Action: Elimination occurs through both glomerular filtration and active tubular secretion in the kidneys [1.2.3, 1.3.1].

  • Short Half-Life: In healthy adults, cephalexin has a short half-life of about 0.5 to 1.2 hours, requiring frequent dosing [1.4.2].

  • Renal Function is Key: Kidney impairment significantly prolongs the drug's half-life, necessitating dose adjustments to avoid toxicity [1.6.2, 1.7.5].

  • Drug Interactions: Probenecid can block renal excretion, increasing cephalexin levels in the blood [1.6.5, 1.9.4].

  • Age Affects Clearance: Both elderly patients and very young infants may have slower clearance rates due to differences in kidney function [1.2.3, 1.3.1].

In This Article

The Journey of Cephalexin Through the Body

Cephalexin, a first-generation cephalosporin antibiotic, is widely prescribed for various bacterial infections, from skin and soft tissue infections to those affecting the respiratory and urinary tracts [1.2.1, 1.10.3]. After oral administration, it is rapidly and almost completely absorbed from the gastrointestinal (GI) tract [1.2.3]. Unlike many other drugs, cephalexin is not metabolized or inactivated in the body [1.8.3, 1.8.5]. This means its chemical structure remains intact from absorption to elimination, a key feature of its pharmacokinetic profile [1.8.2].

The Primary Pathway: Renal Excretion

The fundamental answer to the question, 'How is cephalexin eliminated from the body?' lies with the kidneys. The body gets rid of cephalexin almost exclusively through renal excretion [1.4.2, 1.4.4]. Studies show that more than 90% of an administered dose is excreted unchanged in the urine within a period of 8 hours [1.3.1, 1.5.2]. This rapid and efficient clearance makes it particularly effective for treating urinary tract infections (UTIs), as high concentrations of the active drug are delivered directly to the site of infection [1.3.4, 1.3.5].

The process of renal excretion for cephalexin involves a two-part mechanism:

  1. Glomerular Filtration: As blood passes through the kidneys, the glomeruli act as filters. Small molecules like cephalexin are filtered from the blood into the urine [1.2.3, 1.3.1].
  2. Tubular Secretion: In addition to filtration, the kidney tubules actively secrete cephalexin from the blood into the urine [1.2.3, 1.3.1]. This active transport process, involving organic anion transporters (OATs), significantly contributes to the drug's rapid clearance [1.4.3, 1.9.4].

Because it does not undergo hepatic metabolism, the liver plays no significant role in its elimination [1.2.1, 1.8.1]. This is an important distinction from many other medications that are broken down by liver enzymes.

Half-Life and Clearance Rate

The elimination half-life of a drug is the time it takes for the concentration of the drug in the body to be reduced by half. In adults with normal kidney function, cephalexin has a very short half-life of approximately 0.5 to 1.2 hours [1.2.3, 1.4.2]. This short duration is why cephalexin typically requires frequent dosing, such as every 6 or 12 hours, to maintain therapeutic levels in the bloodstream needed to fight infection [1.7.2, 1.4.3]. Within about eight hours, more than 90% of a single dose has been cleared from the system of a healthy individual [1.5.1, 1.5.3].

Factors Influencing Cephalexin Elimination

Several factors can alter how quickly cephalexin is removed from the body. The most significant of these is renal function.

  • Renal Impairment: Since the kidneys are almost solely responsible for elimination, any impairment in their function dramatically affects clearance [1.6.2]. In patients with chronic kidney disease (CKD), the half-life of cephalexin is prolonged substantially. For example, in adults with a creatinine clearance below 13.5 mL/minute, the half-life can increase to as long as 7.7 to 13.9 hours [1.4.5]. This necessitates dosage adjustments—either reducing the dose or extending the interval between doses—to prevent the drug from accumulating to toxic levels [1.6.3, 1.7.5].
  • Age: Geriatric patients are more likely to have age-related decreases in renal function, even if not formally diagnosed with kidney disease [1.3.1]. Therefore, caution is often exercised when prescribing cephalexin to older adults, and renal function monitoring may be recommended [1.2.4, 1.6.1]. Conversely, elimination half-life is also longer in very young children, being about 5 hours in neonates and 2.5 hours in infants aged 3-12 months [1.2.3].
  • Drug Interactions: Certain medications can interfere with cephalexin's elimination. The most notable is probenecid, a drug used for gout. Probenecid competitively inhibits the tubular secretion of cephalexin in the kidneys, which blocks its primary excretion pathway [1.6.5, 1.9.4]. This leads to higher and more sustained blood concentrations of the antibiotic [1.9.1, 1.9.3]. Other medications like metformin can also interact, potentially leading to higher concentrations of metformin [1.6.5].
Feature Cephalexin Cefazolin (Injectable Cephalosporin)
Primary Route Oral Intravenous/Intramuscular
Metabolism Not metabolized [1.8.3] Not significantly metabolized
Elimination >90% renal (unchanged) [1.3.1] Primarily renal (unchanged)
Half-Life (Normal Renal Fx) 0.5 - 1.2 hours [1.4.5] 1.2 - 2.2 hours
Protein Binding Low (10-15%) [1.3.4, 1.8.5] High (approx. 85%)
Effect of Probenecid Delays excretion [1.6.5] Delays excretion

Conclusion

In summary, the elimination of cephalexin from the body is a rapid process managed almost entirely by the kidneys. The drug is filtered and secreted into the urine without being metabolized by the liver. Its short half-life necessitates multiple daily doses, and its clearance is highly dependent on the patient's renal function, age, and potential interactions with other drugs like probenecid. This renal-centric pathway makes monitoring kidney function a critical aspect of ensuring the safe and effective use of this common antibiotic. For further reading, you can consult authoritative sources like the National Library of Medicine's DailyMed.

Frequently Asked Questions

In individuals with normal kidney function, over 90% of a cephalexin dose is eliminated from the system in the urine within 8 hours [1.5.2, 1.5.3].

Cephalexin is eliminated by the kidneys, so the risk of toxicity may be greater in individuals with pre-existing impaired renal function [1.2.4]. For those with healthy kidneys, it is generally safe when taken as prescribed. Dose adjustments are necessary for patients with kidney disease [1.7.2].

No, cephalexin is not metabolized by the liver [1.2.1, 1.8.1]. It is excreted from the body in its original, unchanged form primarily through the kidneys.

Cephalexin has a very short elimination half-life, typically around 0.5 to 1.2 hours in healthy adults [1.4.5]. Frequent dosing (e.g., every 6 hours) is necessary to maintain a consistent concentration of the antibiotic in your body to effectively fight the infection [1.7.2].

Food can slightly delay the time it takes to reach peak concentration in the blood, but it does not change the total amount of the drug absorbed or its ultimate elimination from the body [1.2.3].

If you have impaired kidney function, cephalexin can stay in your body much longer, increasing the risk of side effects [1.6.2]. Your doctor will need to adjust your dose, typically by giving a smaller amount or increasing the time between doses [1.7.5].

Yes. The gout medication probenecid is known to block the kidney's ability to secrete cephalexin, which increases the antibiotic's concentration and prolongs its effect [1.9.4]. Metformin and zinc-containing products can also interact with cephalexin [1.6.5, 1.9.2].

References

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.