A drug’s efficacy may be affected by the degree to which it binds to plasma proteins. In comparing two drugs that vary in plasma protein binding, but have otherwise similar properties, the drug with the ____________ fraction bound to plasma proteins will be more pharmacologically active, as only ____________ drug can leave the systemic circulation.
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In general, drugs that are highly bound to plasma proteins have increased overall drug clearance. For a drug that is metabolized mainly by the liver, binding to plasma proteins prevents the drug from entering the hepatocytes, resulting in increased drug metabolism by the liver. Protein-bound drugs act as larger molecules that cannot diffuse easily through the capillary membranes in the glomeruli, thereby preventing the biliary excretion of the drug. The elimination half-lives of some drugs, such as the cephalosporins, which are excreted mainly by renal excretion, are generally decreased when the percentage of drug bound to plasma proteins increases.
Suman K.
Drugs that are predominantly unionized (uncharged) at physiological pH (7.4) will have more extensive distribution when compared to drugs that are ionized (charged).
Supreeta N.
9. If a patient has a liver or kidney disease, the half-life period will generally be: (a) Longer; (b) zero; (c) shorter; (d) unaffected. 10. Which drug is most available for treatment? (a) Drug that is 100% protein bound (b) Drug that is 61-89% protein bound (c) Drug that is 30-61% protein bound (d) Drug that is <30% protein bound.
Adi S.
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