A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534)
Indication
Used to manage hyperthyroidism which is due to an overactive thyroid gland (Grave's disease).
Pharmacology
Propylthiouracil is a thiourea antithyroid agent. Grave's disease is the most common cause of hyperthyroidism. It is an autoimmune disease where an individual's own antibodies attach to thyroid stimulating hormone receptors within cells of the thyroid gland and then trigger overproduction of thyroid hormone. The two thyroid hormones manufactured by the thyroid gland, thyroxine (T4) and triiodothyronine (T3), are formed by combining iodine and a protein called thyroglobulin with the assistance of an enzyme called peroxidase. PTU inhibits iodine and peroxidase from their normal interactions with thyroglobulin to form T4 and T3. This action decreases thyroid hormone production. PTU also interferes with the conversion of T4 to T3, and, since T3 is more potent than T4, this also reduces the activity of thyroid hormones. The actions and use of propylthiouracil are similar to those of methimazole.
Toxicity
Oral, rat: LD50 = 1250 mg/kg.
Affected Organisms
Humans and other mammals
Absorption
Well absorbed following oral administration.
Half Life
2 hours
Protein Binding
82%
Elimination
Propylthiouracil is readily absorbed and is extensively metabolized. Approximately 35% of the drug is excreted in the urine, in intact and conjugated forms, within 24 hours.
Research Area: Endocrinology , Biological Activity: Propylthiouracil is a thyroperoxidase and 5’-deiodinase inhibitor. It is a thioamide drug used to treat hyperthyroidism (including Graves’ disease) by decreasing the amount of thyroid hormone produced by the thyroid gland. It normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I-) to iodine (I0), facilitating iodine’s addition to tyrosine residues on the hormone precursor thyroglobulin. It also acts by inhibiting the enzyme 5’-deiodinase (tetraiodothyronine 5’ deiodinase), which converts T4 to the active form T3. [1]
包装 10, 25, 100 g in glass bottle Application 6-Propyl-2-thiouracil is a thyreostatic (thyroid hormone) agent that may be used as a reference material in thyreostatic drug separation and detection technologies such as capillary electrophoresis, HPLC, or gas chromatography.
A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group.
参考文献
PubChem文献
数据源提供
• http://en.wikipedia.org/wiki/Propylthiouracil
• Aboul-Enein, H.Y., et al.: Anal. Profiles Drug Subs., 6, 457 (1977)
• Cooper, D.S., et al.: N. Engl. J. Med., 311, 1353 (1977)
Eyeshields, full-face particle respirator type N100 (US), Gloves, respirator cartridge type N100 (US), type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges
有害性 (Xn)
有毒 (T)
