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29 Cards in this Set
- Front
- Back
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Protein Binding of Drugs |
a drug bound to protein forms a complex that is too large to cross cell membranes. |
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Reversible |
when a drug binds the protein with a weaker chemical bond |
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Irreversible |
chemical activation of the drug which then attaches to the protein macromolecules by covalent bonds |
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Albumin |
synthesized by the liver & responsible for reversible drug binding |
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Endogenous |
free fatty acids, bilirubin, various hormones (cortisone, aldosterone, thyroxine, tryptophan) |
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Exogenous |
weak acidic drugs, anionic drugs (aspirin, phenylbutazone, penicillins) |
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Electrostatic Bonds (Hydrophobic Bonds) |
binds weak acidic drugs |
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Histidine Arginine Lysine |
Basic Groups of ____________, ____________, and _____________ are responsible for binding acidic drugs |
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Tyrosine Aspartic Acid Glumatic Acid |
Acidic groups of ______________, ________________, and ______________ are responsible for binding basic drugs |
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Alpha, acid glycoproteins (orosomucoid) |
a globulin with low plasma concentration binds basic highly lipophilic drugs |
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Propranolol (Beta Blocker) Imipramine (Antidepressant) Lidocaine (Local anesthetic) |
drugs that bind basic highly lipophilic drugs |
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Lipoprotein |
marcomolecular complexes of lipids and proteins responsible for transport of plasma lipids & for the binding of drugs when the albumin sites become saturated |
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Low density Lipoprotein |
transport from the liver to the periphery; bad cholesterol |
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High denisity lipoprotein |
transport from the periphery to liver; good cholesterol |
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Erythrocytes |
have lipid membrane perforated by positively-charged aqueous channels of various diameters |
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Phenytoin Pentobarbital Amobarbital |
drugs that bind more with RBC than in Water |
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Molecular Filtration Ultracentrifugation Ultrafiltration Dialysis Sephadex-gel Filtration Electrophoresis Agar-plate test |
the extent of protein-bindings determined in-vitro by: |
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Drug Drug interactions Affinity of drug and protein Protein Patients pathophysiologic condition
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Factors affecting drug-protein binding |
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Drug |
physicochemical and total concentration of drug in the blood
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protein |
depends on the quantity (# of p) and quality (physicochemical nature) |
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affinity of drug and protein |
magnitude of association constant |
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drug interactions |
competition at binding sites |
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protein binding and apparent volume of distribution |
estimates the extent of drug distribution in the body |
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smaller |
drugs highly bound to plasma protein results in _____________ volume of distribution |
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increased |
increase in the percentage of drug bound to plasma results in ______________ elimination life |
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Hepatic metabolism |
Binding of drugs to plasma protein, reduced _____________________________. |
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Minimal |
If VD is large, the increase may be ______________ |
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rise |
If VD is small, it may significantly _______ in the free drug |
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0.15 mL/g |
important if the VD is less than ________ |
