药品详细
Propylthiouracil(丙基硫氧嘧啶)
化学结构式图
中文名
丙基硫氧嘧啶
英文名
Propylthiouracil
分子式
C7H10N2OS
化学名
6-propyl-2-sulfanylidene-1,2,3,4-tetrahydropyrimidin-4-one
分子量
Average: 170.232
Monoisotopic: 170.051383642
Monoisotopic: 170.051383642
CAS号
51-52-5
ATC分类
H03B Antithyroid preparations
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
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)
生产厂家
- Abbott laboratories pharmaceutical products div
- Actavis elizabeth llc
- Anabolic inc
- Dava pharmaceuticals inc
- Eli lilly and co
- Halsey drug co inc
- Impax laboratories inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- L perrigo co
- Lannett co inc
- Mutual pharmaceutical co inc
- Tablicaps inc
- Watson laboratories inc
- West ward pharmaceutical corp
封装厂家
- Actavis Group
- Avkare Incorporated
- Cardinal Health
- Comprehensive Consultant Services Inc.
- DAVA Pharmaceuticals
- Dispensing Solutions
- Heartland Repack Services LLC
- Kaiser Foundation Hospital
- Murfreesboro Pharmaceutical Nursing Supply
- Nucare Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Prepak Systems Inc.
- Remedy Repack
- Shanghai Multi Med Union Co. Ltd.
- Tya Pharmaceuticals
- Vangard Labs Inc.
- West-Ward Pharmaceuticals
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | Used to manage hyperthyroidism which is due to an overactive thyroid gland (Grave's disease). |
| Pharmacodynamics | 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. |
| Mechanism of action | Propylthiouracil binds to thyroid peroxidase and thereby inhibits the conversion of iodide to iodine. Thyroid peroxidase normally converts iodide to iodine (via hydrogen peroxide as a cofactor) and also catalyzes the incorporation of the resulting iodide molecule onto both the 3 and/or 5 positions of the phenol rings of tyrosines found in thyroglobulin. Thyroglobulin is degraded to produce thyroxine (T4) and tri-iodothyronine (T3), which are the main hormones produced by the thyroid gland. Therefore propylthiouracil effectively inhibits the production of new thyroid hormones. |
| Absorption | Well absorbed following oral administration. |
| Volume of distribution | Not Available |
| Protein binding | 82% |
| Metabolism |
Not Available
|
| Route of 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. |
| Half life | 2 hours |
| Clearance | Not Available |
| Toxicity | Oral, rat: LD50 = 1250 mg/kg. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | The anti-thyroid agent, propylthiouracil, may decrease the anticoagulant effect of acenocoumarol. |
| Anisindione | The anti-thyroid agent, propylthiouracil, may decrease the anticoagulant effect of anisindione. |
| Dicumarol | The anti-thyroid agent, propylthiouracil, may decrease the anticoagulant effect of dicumarol. |
| Digoxin | The antithyroid agent may increase the effect of digoxin. |
| Warfarin | Propylthiouracil may decrease the anticoagulant effect of warfarin. Monitor for changes in the therapeutic and adverse effects of warfarin if propylthiouracil is initiated, discontinued or dose changed. |
食物相互作用
- Take at the same time everyday.
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