Related Experiment Video
Updated: Jul 27, 2026
19:16
The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis
Published on: March 17, 2010
[Protein binding of cephems in the elderly]
M Kuroyama1, S Motohashi, S Murase
1Department of Pharmacy, Kitasato University Hospital.
Nihon Ronen Igakkai Zasshi. Japanese Journal of Geriatrics
|November 1, 1992
Summary
Elderly individuals exhibit reduced protein binding of cephalosporins, increasing free drug levels. This may lead to enhanced drug effects and adverse reactions in older patients.
Area of Science:
- Pharmacology
- Geriatrics
- Biochemistry
Context:
- Serum protein binding influences drug efficacy and safety.
- Aging can alter physiological parameters affecting drug disposition.
- Cephalosporins are a class of widely used antibiotics.
Purpose:
- To investigate the impact of aging on the serum protein binding of 12 cephalosporins.
- To compare protein binding in young versus elderly healthy subjects.
- To explore potential reasons for age-related changes in cephalosporin binding.
Summary:
- Serum protein binding of 12 cephalosporins was evaluated in young and elderly healthy adults using equilibrium dialysis.
- Elderly subjects showed significantly lower protein binding for these cephalosporins compared to younger subjects.
- This reduction is potentially due to decreased serum albumin and altered fatty acid profiles in the elderly, leading to higher free drug concentrations.
Impact:
- The decreased protein binding in elderly individuals may result in increased pharmacological effects and a higher incidence of adverse reactions.
- Clinical consideration of age-related changes in protein binding is crucial for optimizing cephalosporin therapy in the elderly.
- Further research into age-specific dosing strategies for cephalosporins is warranted.
Related Concept Videos
01:29Drug Distribution: Plasma Protein Binding
Drugs predominantly attach to plasma proteins, with only a small percentage remaining unbound. The unbound portion can be calculated as one minus the bound fraction. Acidic drugs form large, inactive complexes by reversibly binding to plasma albumin, which prevents them from diffusing across biological barriers. These drug-protein complexes act as reservoirs for the drugs. As the concentration of unbound drugs decreases, these complexes quickly dissociate to release the free drug, maintaining...
01:22Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence
Generic intravenous (IV) drugs are considered bioequivalent to their branded counterparts due to their 100% bioavailability upon administration. However, variations in stability among different drug products can significantly influence their therapeutic performance, even if they are pharmaceutically equivalent.Cefuroxime, a prophylactic antimicrobial, is often used as a single-dose IV injection for patients undergoing coronary artery bypass grafting surgery. A 3 g dose typically provides...
01:22Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Absorption
As individuals age, their body's physiology evolves, affecting drug pharmacokinetics. The most apparent changes occur in the gastrointestinal tract, where an increase in gastric pH, a delay in gastric emptying, and a reduction in gastrointestinal motility are observed. Remarkably, these changes do not substantially modify the absorption of orally administered drugs, particularly those absorbed via passive diffusion.Transdermal drug delivery emerges as a highly viable method for older adults due...
01:18Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Metabolism
Geriatric patients show significant variation in how their bodies process medications, which can change how effective and safe treatments are. The liver is the primary organ where drug metabolism occurs, involving two main types of chemical reactions: phase I and II. Phase I metabolism is driven by the cytochrome P450 enzyme system, which includes key types such as CYP3A, CYP2D6, and CYP2C9. Research indicates that while aging doesn't notably alter the levels or activity of these enzymes, it...
01:18Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Excretion
In geriatric patients, renal physiology undergoes significant changes, including diminished renal blood flow and a lower glomerular filtration rate (GFR), leading to alterations in medication clearance. Drugs such as aminoglycoside antibiotics, lithium, and digoxin, which rely on glomerular filtration for removal from the body, particularly impact pharmacokinetics. These drugs tend to have slower clearance rates in older adults, necessitating careful dosage considerations.Evaluation of renal...
01:25Mechanism of Antibiotic Resistance in MRSA
Antibiotic resistance in bacteria arises when microorganisms evolve the ability to withstand drugs designed to kill them or inhibit their growth, rendering once-effective treatments useless. This phenomenon, driven by genetic change and selection under antibiotic exposure, poses a profound threat to modern medicine. Mechanisms include drug-inactivating enzymes (e.g., β-lactamases), efflux pumps that eject antibiotics, mutations altering antibiotic targets, decreased drug uptake, and acquisition...