The Binding of Sulfonamide Drugs by Plasma Proteins. A Factor in Determining the Distribution of Drugs in the Body

Davis, Bernard D.

doi:10.1172/jci101448

Cited by 139 publications

(53 citation statements)

References 22 publications

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“…(Table 1) suggesting that the disease, whether active or in remission, does not alter the saliva :plasma concentration relationships. The slope of approximately 0.5 is consistent with the reports on the plasma protein binding of sulphapyridine (Davies, 1943;Fischer & Klotz, 1979). Fifty per cent of the sulphonamide is unbound in the plasma and therefore only 50% of drug concentration is available to diffuse into the salivary glands.…”

Section: Saliva: Plasma Concentration Relationships For Sulphapyridinsupporting

confidence: 90%

Saliva: plasma concentration relationships for sulphapyridine following sulphasalazine administration to normal volunteers and patients with inflammatory bowel disease.

Day¹,

Houston²

1980

Brit J Clinical Pharma

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Section: Saliva: Plasma Concentration Relationships For Sulphapyridinsupporting

confidence: 90%

Saliva: plasma concentration relationships for sulphapyridine following sulphasalazine administration to normal volunteers and patients with inflammatory bowel disease.

Day¹,

Houston²

1980

Brit J Clinical Pharma

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“…Klotz, Urquhart & Weber (1950) reported that the extent of binding of penicillin decreased with increase in temperature and Scholtan & Schmid (1962 reported the binding of penicillin and tetracyclines to be lower at 37 than at 40 C. On the other hand, Wozniak (1960) reported binding of tetracycline to be slightly greater at 37 than at 2 to 50 C. In the case of sulphonamides, Davis (1943) reported binding to be little influenced by temperature. In the experiments reported here with two penicillins, binding was not significantly influenced by temperature in the range 4 to 370 C.…”

Section: Discussionmentioning

confidence: 99%

“…With regard to the effect of antibiotic concentration on the extent of binding, it is known that the proportion of unbound drug increases with increase in drug concentration (Davis, 1943;Goldstein, 1949). In the case of certain penicillins a significant difference in the extent of binding was reported by Scholtan & Schmid (1962) in a range of concentrations as low as 0.5 to 8.0 ug/ml.…”

Section: Discussionmentioning

confidence: 99%

The Binding of Antibiotics to Serum Proteins

Rolinson¹,

Sutherland²

1965

British Journal of Pharmacology and Chemotherapy

130

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The published work on the binding of antibiotics to serum proteins is extensive. Nevertheless, data are still incomplete in certain respects. For example, there is little information on the rate at which antibiotics are bound to the proteins and the rate at which this complex breaks down. Similarly, although the binding of antibiotics to serum proteins is known to be essentially reversible it is not certain whether there is any proportion of the drug which is bound irreversibly. On certain aspects, published data are available but are conflicting and some lack of agreement exists on the precise extent of binding of certain antibiotics, particularly of tetracyclines. There is also a general lack of comparative results on the extent of binding for related antibiotics obtained from experiments carried out by the same method.In the present paper, results are given for the effect of certain factors on the binding of penicillins and other antibiotics in serum and comparative data are also given for the extent of binding in human serum for all the penicillins at present in clinical use. METHODS Measurement of binding of antibiotics to serum proteinsThe extent of binding of penicillins and other antibiotics to the proteins of serum was measured by ultrafiltration through Visking viscose-cellulose dialysis tubing. Preliminary experiments indicated that there was no significant difference between the extent of binding in plasma obtained from heparinized blood and that in serum. The antibiotic present in the protein-free ultrafiltrate was measured by microbiological assay and this quantity represented the free, unbound, fraction of antibiotic in serum. The amount of antibiotic bound to protein was derived by subtracting the level of free antibiotic from the known total concentration in serum. Before comparative experiments were made to measure the extent to which different antibiotics were bound to the proteins of human serum, preliminary investigations were carried out into the effects of various experimental factors thought likely to influence the extent of binding. These included the effects of antibiotic concentration, nature of protein, temperature, individual variation, rate of binding and nature of binding. Ultrafiltraton techniquesSuitable lengths of Visking tubing (0.25 in. internal diameter) were knotted at one end and attached at the other to a manifold connected to compressed air. Serum samples were introduced into the tubing before connexion to the manifold and ultrafiltration was then carried out at room temperature at a positive pressure of 15 lb/in2. The ultrafiltrate was collected in a glass tube which closely surrounded the Visking sac. In most experiments the volume of serum used was 5 ml., and the volume of ultrafiltrate collected for assay was about 0.5 ml. In some experiments a volume of 10 to 12 ml. of serum was used which permitted an adequate sample of ultrafiltrate to be collected in about 7 min. ANTIBIOTICS AND SERUM PROTEINS 639Horse, sheep, rabbit, and calf sera were obtained as commercial samp...

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“…However, different degrees in vitro and in vivo of binding to proteins (especially to albumin) may also be of significance. Generally, the portion bound to protein is considered as inactive against bacteria (Davis, 1943;Tompsett, Shultz and McDermott, 1947;Quinn, 1964). The percentage binding of the penicillins to serum proteins increases from ampicillin through sodium methicillin and penicillin G to oxacillin (Tompsett and others, 1947;Bond, 1964;Rolinson, 1964;Kunin, 1966); 3-amino-adamantyl-l-penicillin is only slightly bound to serum proteins.…”

Section: -Amino-adamantyl-1-penicillinmentioning

confidence: 99%

A study of the relationships between the sensitivities of Neisseria gonorrhoeae to sodium penicillin G, four semi-synthetic penicillins, spiramycin, and fusidic acid.

Reyn¹,

Benzon²

1968

Sexually Transmitted Infections

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The Binding of Sulfonamide Drugs by Plasma Proteins. A Factor in Determining the Distribution of Drugs in the Body

Cited by 139 publications

References 22 publications

Saliva: plasma concentration relationships for sulphapyridine following sulphasalazine administration to normal volunteers and patients with inflammatory bowel disease.

Saliva: plasma concentration relationships for sulphapyridine following sulphasalazine administration to normal volunteers and patients with inflammatory bowel disease.

The Binding of Antibiotics to Serum Proteins

A study of the relationships between the sensitivities of Neisseria gonorrhoeae to sodium penicillin G, four semi-synthetic penicillins, spiramycin, and fusidic acid.

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