| have REDUCED OVERALL DRUG CLEARANCE. | DRUGS highly bound to plasma protein |
| For a drug that is metabolized mainly by the
liver, binding to plasma proteins prevents the
drug from entering the__, resulting in
reduced drug metabolism by the liver. | HEPATOCYTES |
| 1 at LOW DRUG CONCENTRATIONS, most of the drug may be __
2 whereas at HIGH DRUG CONCENTRATIONS, the protein- binding sites may become __, with a consequent rapid increase in the __ | 1 bound to the protein
2 saturated, free drug concentrations |
| AMINO ACIDS THAT BINDS TO ACIDIC DRUGS | Histidine
Arginine
Lysine |
| AMINO ACIDS THAT BINDS TO BASIC DRUGS | Glutamic Acid
Aspartic Acid |
| PROTEIN BINDING IS DETERMINED BY: | 1 Dialysis
2 Ultracentrifugation
3 Ultrafiltration
4 Sephadex-gel filtration chromatography (resin)
5 Molecular filtration
6 Electrophoresis
7 Agar plate test
DUU SMEA |
| The Pharmacokinetic IMPORTANCE
OF PROTEIN BINDING | 1 Drug-protein binding INFLUENCES THE DISTRIBUTION EQUILIBRIUM OF THE DRUG
2 Plasma proteins EXERT A BUFFER and TRANSPORT FUNCTION in the DISTRIBUTION process
3 Only FREE and UNBOUND DRUG ACTS and can LEAVE the circulatory system and DIFFUSE INTO THE TISSUE |
| Pathological Conditions in which Plasma Concentration
of ∂1-ACIDGLYCOPROTEIN is increased | 1 Cancer
- Carcinoma, Leukemia, Lymphoma,
Malignant melanoma, myeloma
2 Inflammation
- Crohn’s disease, Inflammatory polyarthritis,
pneumonia, rheumatoid arthritis, ulcerative
colitis, systemic erythematosus
3 Myocardial Infarction Trauma
- Burns, extensive tissue damage, surgery,
transplantation |
