A Comparison of the &lt;i&gt;in vitro&lt;/i&gt; Activities of Sulfamethoxazole and Sulfadiazine Combinations with Trimethoprim

Js, Kuipers

doi:10.1159/000237826

Cited by 5 publications

(1 citation statement)

References 7 publications

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“…Sulfametoxazole (SMX) is the SA most often used in a fixed combination with TMP. While sharing ba sically equal antibacterial properties with SMX [3], sulfadiazine (SDZ) is shown to be kinetically superior. It has better lipid solubility [2], lower binding to plasma pro teins [4] and lower metabolism [4,5], all of which favour more efficient tissue distri bution.…”

Section: Introductionmentioning

confidence: 99%

Trimethoprim and Sulfadiazine Penetration into Bile and Gallbladder in Acute Cholecystitis

et al. 1987

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The concentrations of trimethoprim (TMP) and sulfadiazine (SDZ) in serum, bile and gallbladder wall of 9 patients with acute cholecystitis were measured after b.i.d. treatment with 160 mg of TMP + 500 mg of SDZ. The samples were collected 2–4 h after the last dose. Mean TMP concentrations were 1.71 ± (SE) 0.51 μg/ml, 4.53 ± 5.26 μg/ml and 2.31 ± μg/g in serum, bile and gallbladder, respectively. Mean SDZ concentrations were 22.2 ± 14.9 μg/ml in serum, 9.37 ± 8.99 μg/ml in bile and 16.1. ± 10.1 μg/g in gallbladder. The average ratios of bile-serum and gallbladder-serum concentrations were 2.64 and 1.35 for TMP and 0.42 and 0.73 for SDZ. There was a significant correlation between serum and gallbladder concentrations of both TMP and SDZ. No correlation existed between serum and bile levels.

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Section: Introductionmentioning

confidence: 99%

Trimethoprim and Sulfadiazine Penetration into Bile and Gallbladder in Acute Cholecystitis

et al. 1987

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Some pharmacokinetic data of aditoprim and trimethoprim in healthy and tick‐borne fever infected dwarf goats

Knoppert¹,

Nijmeijer²,

Duin³

et al. 1988

Vet Pharm & Therapeutics

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Aditoprim (AP) is a new dihydrofolate reductase inhibitor, which is structurally related to trimethoprim (TMP). The pharmacokinetics of AP (10 mg/kg) and TMP (20 mg/kg) were assessed in healthy dwarf goats. Therapeutic efficacy against rickettsial infections was tested in tick-borne fever (TBF) infected goats. The animals were given TMP (n = 5) or AP (n = 5) by i.v. injection, and subsequently the drugs were administered orally (same groups, similar doses). Finally, both groups were infected with TBF and the i.v. experiment was repeated. Plasma concentration-time curves for both drugs followed first-order two-compartment decay. For TMP, mean t1/2 beta +/- SEM (h) was 0.84 +/- 0.06 (i.v. control) and 0.90 +/- 0.06 (i.v. infected), respectively, whereas for AP values of 8.00 +/- 0.31 (i.v. control) and 10.28 +/- 0.67 (i.v. infected) were obtained (P less than 0.05). Mean Vd beta +/- SEM values (l/kg) were 3.84 +/- 0.27 (i.v. control) and 4.07 +/- 0.85 (i.v. infected) for TMP (NS) and 7.02 +/- 0.63 vs 9.29 +/- 0.21 (P less than 0.05) for AP. After i.v. injection, rumen fluid concentrations of AP were significantly (P less than 0.05) higher and more persistent than those of TMP. For AP, the plasma and rumen fluid concentrations at 3 h were 1.20 +/- 0.06 micrograms/ml and 0.85 +/- 0.17 microgram/ml, respectively. After oral administration of TMP, Cmax in plasma was 0.12 +/- 0.01 microgram/ml and the maximum was reached after 1.2 +/- 0.16 h; systemic bioavailability (F) was 10.3% (relative to AUC i.v.). Oral treatment with AP resulted in a Cmax value of 0.21 +/- 0.02 microgram/ml with Tmax of 22.5 +/- 1.65 h and a F value of 71%. Based on WBC, serum ALP and rectal temperature responses, it was concluded that both TMP and AP were inactive against Ehrlichia phagocytophila.

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Trimethoprim, failure to penetrate intoPseudomonas aeruginosacells

Werner

Goeth

1984

FEMS Microbiology Letters

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Permeability mutants of Escherichia coli and Pseudomonas aeruginosa demonstrated a significantly higher susceptibility for trimethoprim (TMP). Although the target enzyme of this drug, dihydrofolic acid reductase, expressed about the same activity, it was comparably inhibited by TMP in permeability mutants and in wild‐type strains. The weak activity in wild‐type strains depends on the decreased uptake.

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A Comparison of the <i>in vitro</i> Activities of Sulfamethoxazole and Sulfadiazine Combinations with Trimethoprim

Cited by 5 publications

References 7 publications

Trimethoprim and Sulfadiazine Penetration into Bile and Gallbladder in Acute Cholecystitis

Trimethoprim and Sulfadiazine Penetration into Bile and Gallbladder in Acute Cholecystitis

Some pharmacokinetic data of aditoprim and trimethoprim in healthy and tick‐borne fever infected dwarf goats

Trimethoprim, failure to penetrate intoPseudomonas aeruginosacells

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