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Propylthiouracil powder (ptu), chemical name 6-propyl-2-thiouracil, is an organic compound with the chemical formula C7H10N2OS, CAS 51-52-5, and a melting point of approximately 222 225 ° C. The melting point refers to the temperature at which a substance transforms into a liquid state. It is generally a white crystalline solid. It can exist in the form of crystals or powders. Low solubility in water. It is relatively easy to dissolve in organic solvents such as ethanol, ether, and acetic acid. It is a thiouracil compound with pharmacological activity against hyperthyroidism. It works by inhibiting the synthesis of thyroid hormones. By inhibiting the peroxidase system in the thyroid gland, the iodization and condensation of tyrosine iodide in the thyroid gland are prevented, thereby inhibiting the synthesis of thyroid hormones.
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Chemical Formula |
C7H10N2OS |
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Exact Mass |
170 |
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Molecular Weight |
170 |
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m/z |
170 (100.0%), 171 (7.6%), 172 (4.5%) |
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Elemental Analysis |
C, 49.39; H, 5.92; N, 16.46; O, 9.40; S, 18.83 |
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Propylthiouracil (PTU), as a classic anti thyroid drug, plays an important role in the treatment of hyperthyroidism and its complications by inhibiting the core mechanism of thyroid hormone synthesis and release.
Basic treatment for hyperthyroidism
Long term control of mild to moderate hyperthyroidism
It is the preferred medication for patients with mild to moderate hyperthyroidism, especially for those with mild to moderate thyroid enlargement and slow disease progression. Its mechanism of action involves specific inhibition of thyroid peroxidase (TPO), blocking the oxidation of iodide to active iodine, thereby inhibiting tyrosine iodide and iodide tyrosine coupling, ultimately reducing the synthesis of thyroxine (T4) and triiodothyronine (T3).
Clinical studies have shown that standardized medication can restore normal serum thyroid stimulating hormone (TSH) levels in over 80% of patients, and significantly alleviate high metabolic symptoms such as palpitations, hand tremors, excessive sweating, and weight loss. Usually, continuous treatment is required for 12-18 months, and some patients may need to extend it to 24 months to achieve stable condition. During the treatment period, thyroid function should be monitored every 4-6 weeks, and the dosage should be dynamically adjusted based on TSH and free T4 (FT4) levels. The initial dosage is generally 100-300mg/d, divided into 3 oral doses, and the maintenance dosage is usually 50-150mg/d.
Targeted treatment for special types of hyperthyroidism
Hyperthyroidism during pregnancy: It is the preferred medication for early pregnancy (first 12 weeks) because its placental penetration rate is lower than that of methimazole, which can reduce the risk of fetal malformation. Treatment should maintain the lowest effective dose to keep maternal free T4 at the normal upper limit and avoid excessive suppression of thyroid function.
Adolescent hyperthyroidism: For patients in the growth and development stage, precise dosage adjustment (usually starting at a weight of 4mg/kg/day) is used to effectively control symptoms while minimizing interference with the thyroid pituitary hypothalamic axis, ensuring the needs of growth and development.
Elderly hyperthyroidism: Elderly patients with combined liver and kidney dysfunction can reduce the risk of drug accumulation by shortening the half-life (about 1.5 hours), and with liver and kidney function monitoring, individualized safe medication can be achieved.
Emergency rescue of thyroid crisis
Thyroid crisis is a serious complication of hyperthyroidism, characterized by high fever, tachycardia, vomiting, diarrhea, restlessness, and even coma, with a mortality rate of up to 10% -30%. Propylthiouracil plays a triple role in this scenario:
Rapid inhibition of hormone synthesis: By blocking TPO activity, the rate of thyroid hormone production is significantly reduced within 2-4 hours after medication.
Inhibition of peripheral T4 to T3 conversion: It is the only anti thyroid drug with 5 '- deiodinase inhibition effect, which can block the conversion of T4 to more active T3 in peripheral tissues, resulting in a 30% -50% decrease in serum T3 levels within 24 hours.
Synergistic stabilization of vital signs: When used in combination with beta blockers (such as propranolol) and glucocorticoids (such as dexamethasone), it can quickly control heart rate, body temperature, and central nervous system excitability symptoms.
The clinical rescue plan usually includes: oral or nasal feeding of 600-800mg/d propiconazole, once every 6 hours; Cooperate with iodine agents (such as Lugol's solution) to inhibit hormone release; Beta blockers control heart rate; Corticosteroids have anti-inflammatory and immunosuppressive effects. Standardized rescue can increase the survival rate of crisis patients to over 85%.
Preoperative preparation for thyroid surgery
1. Thyroid function optimization
Preoperative use of propylthiouracil can restore thyroid hormone levels to normal within 2-4 weeks, significantly reducing surgical risks
Reduce intraoperative bleeding: By inhibiting the expression of thyroid angiogenic factors, thyroid blood flow is reduced by 40% -60%.
Reducing the risk of nerve damage: Normalization of thyroid function can restore the sensitivity of the recurrent laryngeal nerve and reduce the incidence of intraoperative traction injury by 70%.
Preventing thyroid storm: Standardized preoperative preparation can reduce the incidence of intraoperative thyroid crisis from 5% to below 0.5%.
Usually used in conjunction with iodine agents (such as Lugol's solution), the medication time is generally 2-3 weeks, and the specific plan is formulated by the doctor according to the patient's condition.
2. Preoperative management of special cases
Giant goiter: Combined use of iodine can reduce thyroid volume by 20% -30% and lower the risk of tracheal compression.
Combined cardiovascular disease: By controlling the symptoms of hyperthyroidism, the patient's heart function classification (NYHA) can be improved by 1-2 levels, creating conditions for surgery.
Intolerance or allergy to methimazole: Some patients may experience rash or liver dysfunction after using methimazole, and can be replaced with propylthiouracil.
Propylthiouracil powder (PTU) is a drug widely used in thyroid therapy or treatment of hyperthyroidism, and various synthetic methods have been developed. This article will introduce some of the more important synthetic methods.
First, a relatively simple propylthiouracil ptu synthesis method is introduced. This method obtains ethanolylthiouracil through the reaction of thioaminoacyl chloride and isopropanol, and then obtains PTU through a vulcanization reaction.
Using thioaminoacyl chloride and isopropanol as raw materials, ethanolylthiouracil can be obtained through the following reaction:
SCl2 + 2C3H7OH + NH3 → C3H7NHCS2Cl + 3H2O
C3H7NHCS2Cl + NaOH → C3H7NHCS2Na + HCl
C3H7NHCS2Na + I2 → C3H7NHC(S)SCH2CH2OH + NaI
In this reaction, thioaminoacyl chloride reacts with isopropanol to form C3H7NHCS2Cl, which can be treated with alkali to generate C3H7NHCS2Na, and through a series of active hydrogen exchange reactions, ethanolylthiouracil is obtained.
After obtaining ethanolylthiouracil, PTU propylthiouracil can be obtained through sulfidation reaction. Vulcanization reactions use mercaptans or sulfites as vulcanizing agents to create a sulfur-sulfur bond in the molecule.
Here is one of the synthetic methods:
C3H7NHC(S)SCH2CH2OH + H2S → C3H7NHC(S)SCH3 + H2O
C3H7NHC(S)SCH3 + I2 → C7H8N2OS + HI
In this reaction, ethanolylthiouracil reacts with H2S to generate sulfurized ethanolylthiouracil, which is reacted with I2 to obtain PTU.
The method is a high-yield synthesis that treats nitrobenzene and acetone with tetrahydrofuran and up to 3% cesium chloride or zirconium chloride. The intermediates produced by the reaction were then reduced to the amino rings for the synthesis of PTU.
The synthesis starts with 5-sulfonyluracil. The two sulfuryl groups are reduced to thioether groups by chemical reduction and reduction with a unitary agent. Brunswick acid chloride (BzCl) was used to impose a third methylthio group, and finally acetone (Ac2O) for acylation.
In conclusion, PTU is a relatively simple drug to synthesize. Although there are a variety of synthetic methods, the ultimate goal is to combine the thioether group and the amino ring to generate PTU, a drug that requires a specific use.
Pharmacological effects
PTU belongs to the thiol methionine class, which is a drug that can inhibit the production of thyroid hormone by the thyroid gland. It reduces thyroid function by:
(1) Inhibition of thyroid peroxidase (thyroid peroxidase, TPO):
PTU can prevent the thyroid from synthesizing thyroid hormones by inhibiting the activity of TPO.
(2) Reduce the conversion of thyroid hormone precursors:
PTU can also reduce the synthesis of thyroxine, because it can reduce the conversion of thyroid hormone precursors, thereby inhibiting the synthesis of thyroid hormones.
Frequently Asked Questions
What is the drug propylthiouracil used for?
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Propylthiouracil is an anti-thyroid drug used to manage Graves disease and hyperthyroidism.
What is the most serious side effect of PTU?
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Serious side effects of propylthiouracil
fever.
painful or difficult urination.
shortness of breath.
sore throat.
sores, ulcers, or white spots on the lips or in the mouth.
swollen glands.
unusual bleeding or bruising.
unusual tiredness or weakness.
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What is the difference between carbimazole and propylthiouracil?
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Generally, carbimazole is the first choice treatment for hyperthyroidism. PTU is considered second-line therapy, to be used when a patient is unable to tolerate carbimazole, to treat hyperthyroidism in pregnancy or breast feeding, and when surgery or radioactive iodine therapy are not suitable.
Which is safer, PTU or methimazole?
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Conclusion. The study confirmed propylthiouracil is a safer alternative to methimazole for treating hyperthyroidism in pregnant women, and it is appropriate to treat maternal thyroid disease with PTU during the first trimester of pregnancy.
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