Pharmacodynamics of Propylthiouracil in Normal and Hyperthyroid Subjects After a Single Oral Dose

McMurry, James; Gilliland, Paul F.; Ratliff, Charles R.; Bourland, Philip D.

doi:10.1210/jcem-41-2-362

Cited by 30 publications

(12 citation statements)

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“…They also postulated that differences in absorption could account for their observation. Our results support the observations by McMurry et al [27] and Ringhand et al [18] of an increased rate of PTU absorption and increased peak serum concentrations in the same group of children during the HT state in comparison to the ET state ( fig. 1, 2).…”

Section: Discussionsupporting

confidence: 93%

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Pharmacokinetics of Propylthiouracil in Children and Adolescents with Graves’ Disease in the Hyperthyroid and Euthyroid States

Hoffman

Miceli²

1988

Dev Pharmacol Ther

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The pharmacokinetics of propylthiouracil (PTU) was studied in 7 patients having Graves' disease when they were hyperthyroid and then again when they were euthyroid. Two additional euthyroid patients were also studied. The t(1/2), K(e), K(a), apparent V(d), AUC and clearance were calculated. Serum T(3) and T(4) were also measured. PTU had an immediate effect in reducing T(3) levels. Although there were intraindividual variations, the mean PTU elimination half-time did not change from the hyperthyroid state (1.47 h) to the euthyroid state (1.53 h). The mean K(a) when hyperthyroid (2.12 h^–1) was significantly increased (p < 0.005) compared to when euthyroid (1.00 h^–1). The calculated kinetic information indicates that the disposition of PTU in children is similar to that reported in adults.

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Section: Discussionsupporting

confidence: 93%

“…McMurry et al [27] studied 8 normal and 7 HT adults. They showed that the HT sub jects had, on the average, higher peak PTU concentrations which decreased to normal after they became ET.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of Propylthiouracil in Children and Adolescents with Graves’ Disease in the Hyperthyroid and Euthyroid States

Hoffman

Miceli²

1988

Dev Pharmacol Ther

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“…Therefore, PTU may be the drug of choice for the treatment of pregnant or lactating women (5). As to the difference in pharmacokinetics, MMI is cleared from the circulation more slowly than PTU in both euthyroid and hyperthyroid individuals; the serum half-life is 3-6 h for MMI (13)(14)(15) and 1 h for PTU (10,16). The antithyroid effect, however, does not always parallel the circulating drug concentration, and more likely reflects accumulation and retention of the drug in the thyroid (17,18).…”

mentioning

confidence: 99%

Reevaluation of the Effects of Methylmercaptoimidazole and Propylthiouracil in Patients with Graves' Hyperthyroidism

Okamura

Ikenoue

Shiroozu

et al. 1987

The Journal of Clinical Endocrinology & Metabolism

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The effects of methylmercaptoimidazole (MMI) and propylthiouracil (PTU) were compared in patients with Graves' hyperthyroidism. Firstly, the duration of action of the drugs was studied by the perchlorate discharge test, which was performed 2, 12, or 24 h after administering a single dose of 15 mg MMI or 300 mg PTU. After 2 h, the 9 MMI-treated patients who were tested had marked discharge (mean +/- SD, 65.0 +/- 15.8%), as did the 6 patients treated with PTU (57.6 +/- 26.6%). The mean values for the percent discharge 12 and 24 h after drug administration were 34.9 +/- 31.9% (4 patients) and 36.5 +/- 26.9% (69 patients), respectively, in the MMI group and 19.1 +/- 11.7% (11 patients) and 8.6 +/- 10.5% (7 patients) in the PTU group, indicating that the effect of MMI lasted longer. Secondly, the clinical effects of long term administration of the drugs were compared in a different group of patients with Graves' hyperthyroidism. Within 5 weeks after the onset of treatment, 34 (52%) of 66 patients treated with MMI (10 mg, 3 times daily) were euthyroid, while only 1 of 17 patients treated with PTU (100 mg, 3 times daily) was euthyroid. The average time required to achieve euthyroidism, namely normal serum T3 and T4 levels, was significantly shorter in the MMI group [6.7 +/- 4.6 (+/-SD) weeks] than in the PTU group (16.8 +/- 13.7). In spite of the well known effect of PTU on the extrathyroidal conversion of iodothyronines, the serum T3 level normalized much faster with MMI than with PTU. These results indicate that in our patient population 15 mg MMI had a longer inhibitory effect on the organification of iodide than did 300 mg PTU, and that MMI was more rapidly effective in the treatment of Graves' hyperthyroidism.

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“…PTU is rapidly and almost completely absorbed after oral administration and cleared from the body with a terminal half-life in serum of about 1 h. No significant differences in these kinetic parameters were found between euthyroid and hyperthyroid subjects (Schuppan et al, 1973;Kampmann & Skovsted, 1975;McMurray et al, 1975).…”

Section: Introductionmentioning

confidence: 96%

“…The pharmacokinetics of propylthiouracil (PTU) in humans has recently been investigated in several studies (Schuppan et al, 1973;Kampmann & Skovsted, 1974;McMurray et al, 1975;Sitar & Hunninghake, 1975). PTU is rapidly and almost completely absorbed after oral administration and cleared from the body with a terminal half-life in serum of about 1 h. No significant differences in these kinetic parameters were found between euthyroid and hyperthyroid subjects (Schuppan et al, 1973;Kampmann & Skovsted, 1975;McMurray et al, 1975).…”

Section: Introductionmentioning

confidence: 99%

Correlation between antithyroid effect and serum concentrations of propylthiouracil in patients with hyperthyroidism.

Kampmann¹,

Jm²

1981

Brit J Clinical Pharma

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1 Correlation between the kinetics of propylthiouracil and its antithyroid effect was studied in 17 hyperthyroid patients. The serum concentration of propylthiouracil 1 h after an oral dose of 400 mg of hyperthyroid patients. The serum concentration of propylthiouracil 1 h after an oral dose of 400 mg of the drug was used as kinetic parameter as this concentration from the previous study was found to correlate significantly (r = 0.84, P less than 0.01) with the area under the serum concentration‐time curve. 2 After 3 weeks of treatment with 200 mg propylthiouracil three times daily the serum concentration of propylthiouracil was correlated to the decrease in various thyroid parameters such as total and free indexes of serum thyroxine, triiodothyronine and reverse triiodothyronine. 3 Significant correlations were found between the serum concentration of propylthiouracil and all the measured thyroid variables except reverse triiodothyronine. The highest degree of correlation was obtained between serum propylthiouracil and the percentage decrease in total and free indexes of triiodothyronine (r = 0.63 and 0.70, respectively, P less than 0.01). 4 It is suggested that a serum concentration of propylthiouracil above 4 to 5 micrograms/ml 1 h after an oral dose of 400 mg of the drug will secure a sufficient and rapid antithyroid effect during continuous therapy.

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Pharmacodynamics of Propylthiouracil in Normal and Hyperthyroid Subjects After a Single Oral Dose

Cited by 30 publications

References 1 publication

Pharmacokinetics of Propylthiouracil in Children and Adolescents with Graves’ Disease in the Hyperthyroid and Euthyroid States

Pharmacokinetics of Propylthiouracil in Children and Adolescents with Graves’ Disease in the Hyperthyroid and Euthyroid States

Reevaluation of the Effects of Methylmercaptoimidazole and Propylthiouracil in Patients with Graves' Hyperthyroidism

Correlation between antithyroid effect and serum concentrations of propylthiouracil in patients with hyperthyroidism.

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