Pharmacokinetics of tetroxoprim and sulphadiazine in various species

H, Vergin; Fritschi, E

doi:10.1093/jac/5.supplement_b.103

Cited by 11 publications

(7 citation statements)

References 4 publications

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“…The dis tribution coefficient of p = 24.0 for MTP (the determination was carried out in noctanol/phosphate buffer at pH 7.4) is 5.7 times larger than for TXP . Conversely, the different degrees of protein binding (MTP 80%, TXP 13%) seem to be hardly significant as far as CSF diffusion is concerned [Vergin and Fritschi, 1979].…”

Section: Discussionmentioning

confidence: 96%

“…The rate of penetration of the free, (i.e., not pro- tein-bound), diffusable, unionised drug molecules can be obtained graphically from the data following a single intrave nous injection [Brodie et al,I960], Figure 2 displays semilogarithmic plots of the dif ferences of drug concentrations (C) in plasma-water (pw) and CSF/pw concen tration (Cpw-Ccsf/Cpw) against time. Protein binding of TXP and MTP, as re ported in the literature, amounts to 13% [Vergin and Fritschi, 1979] and 80% [Brand, personal commun. ], respectively.…”

Section: Methodsmentioning

confidence: 99%

“…Benzylpyrimidines and their sulphadiazine (SDZ) combinations, i.e., metioprim (MTP), tetroxoprim (TXP) and tetroxoprim/sulphadiazine (TXP/SDZ) show potential antibacterial activity [By water efd\., 1979;77icnetal., 1982] and fa vourable extravascular diffusion [ Vergin and Ferber, 1980]. To assess the putative therapeutical value of these drugs in the treatment of human meningitis, knowl edge of CSF concentrations in laboratory animals is relevant.…”

Section: Introductionmentioning

confidence: 99%

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Diffusion of Metioprim, Tetroxoprim and Sulphadiazine in the Cerebrospinal Fluid of Dogs with Healthy Meninges and Dogs with Experimental Meningitis

H¹,

Bishop-Freudling²,

Foing

et al. 1984

Chemotherapy

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The diffusion of metioprim (MTP), tetroxoprim (TXP) and sulphadiazine (SDZ) in cerebrospinal fluid (CSF), following single intravenous doses and continuous infusions, was studied in dogs. The drugs penetrated well into the CSF of animals with and without experimental Staphylococcus aureus meningitis. In dogs with healthy meninges, the CSF bioavailability – expressed as the ratio of CSF/plasma area under the curve 0–5-hour values – following continuous infusion was determined to be 86.7% for MTP, 58.2% for TXP and 38.8% for SDZ. In infected animals, CSF availability following continuous infusion increases slightly to ratios of 96% (MTP), 70% (TXP) and 50% (SDZ). For all drugs, the concentrations reached in CSF were above the minimum inhibition concentrations for the majority of Enterobacteriaceae, indicating their potential value in the treatment of gram-negative bacillary meningitis.

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Section: Discussionmentioning

confidence: 96%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Diffusion of Metioprim, Tetroxoprim and Sulphadiazine in the Cerebrospinal Fluid of Dogs with Healthy Meninges and Dogs with Experimental Meningitis

H¹,

Bishop-Freudling²,

Foing

et al. 1984

Chemotherapy

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“…Data concerning the biliary excretion of unchanged TXP in laboratory animals is available from rats dosed with 10 mg/kg orally [8]. 0.5 h after administration of the drug, a dose-corrected maximum bile/serum ratio was found to be about 35.0 in this species.…”

Section: Discussionmentioning

confidence: 98%

“…However, the biotransformation patterns in rat and man are very different, being markedly demonstrated by the total renal excretion rates of unchanged mother substance. Usually, renal excretion of TXP in patients with intact kidney function is found to be 40-60% [6] after oral medica tion, whereas only 12-13% of intact TXP are excreted via the rat kidneys both after intravenous and oral dosing [8], Taking into account the TXP serum lev els in patients following a 200 mg dose of the drug (maximum: 4,/ig/ml) [8], from our results concentration factors between 6 and 8 can be calculated in bile. It would thus also be of interest to compare these data with the results of previous studies on tri methoprim (TMP) performed in T-tubedrained patients.…”

Section: Discussionmentioning

confidence: 99%

Biliary Excretion of Tetroxoprim in Man

H¹,

Luber²

1982

Chemotherapy

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The biliary excretion of tetroxoprim (TXP) was studied in 10 patients with T-tube drainage. A mean biliary peak of 32.56 ± 7.69 μg/ml was observed 2–3 h after a single oral dose of 200 mg. The biliary elimination rate constant (k_b) of TXP was found to be 0.056 (h^-1), indicating a longer elimination from the bile than from the central blood compartment. Taking into account the TXP serum levels, following the same oral dose as reported in the literature, concentration factors of 6–8 can be calculated in the bile.

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High performance liquid chromatographic analysis of tetroxoprim and sulphadiazine in serum and urine

Alkaysi

Salem

Badwan

1991

Biomedical Chromatography

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Quantitative determination of tetroxoprim and sulphadiazine in serum and urine was performed using reversed phase high performance liquid chromatography. Protein precipitation using 10% perchloric acid was utilized for purification of serum samples while urine samples were diluted prior to analysis. The mobile phase consisted of triethylammonium acetate buffer (85%), acetonitrile (12%) and methanol (3%), with a final pH of 4.2. The eluent was monitored at 280 nm. Benzoic acid was used as an internal standard. Standardization, validation and application of the method is described.

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Pharmacokinetics of tetroxoprim and sulphadiazine in various species

Cited by 11 publications

References 4 publications

Diffusion of Metioprim, Tetroxoprim and Sulphadiazine in the Cerebrospinal Fluid of Dogs with Healthy Meninges and Dogs with Experimental Meningitis

Diffusion of Metioprim, Tetroxoprim and Sulphadiazine in the Cerebrospinal Fluid of Dogs with Healthy Meninges and Dogs with Experimental Meningitis

Biliary Excretion of Tetroxoprim in Man

High performance liquid chromatographic analysis of tetroxoprim and sulphadiazine in serum and urine

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