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Propylthiouracil | CAS No: 51-52-5 | GMP-certified suppliers
A medication that manages hyperthyroidism, particularly Graves’ disease, by reducing excessive thyroid hormone production to restore hormonal balance and improve clinical outcomes.
Therapeutic categories
Primary indications
- Used to manage hyperthyroidism which is due to an overactive thyroid gland (Grave's disease)
Product Snapshot
- Propylthiouracil is available in oral solid tablet and ophthalmic solution formulations
- It is primarily indicated for the management of hyperthyroidism related to overactive thyroid conditions such as Grave's disease
- The product holds approval status in both the US and Canadian regulatory markets
Clinical Overview
Pharmacodynamically, propylthiouracil reduces thyroid hormone levels by inhibiting thyroid peroxidase, the enzyme catalyzing iodide oxidation to iodine and the subsequent iodination of tyrosyl residues on thyroglobulin. This inhibition prevents the formation of the iodotyrosine precursors necessary for synthesis of T4 and T3. Additionally, propylthiouracil impairs the peripheral conversion of T4 to the more biologically active T3, thereby diminishing overall thyroid hormone activity. These dual effects distinguish propylthiouracil from other thioamides such as methimazole, which do not significantly inhibit peripheral deiodination.
Structurally, propylthiouracil belongs to the pyrimidone class of compounds, characterized by a pyrimidine ring bearing a ketone group. Its pharmacological profile includes classification as a thyroid hormone synthesis inhibitor and antithyroid agent, with noted involvement in hormonal modulation.
Key pharmacokinetic parameters include oral absorption with moderate bioavailability, hepatic metabolism, and renal excretion; however, detailed ADME profiles vary depending on formulation and patient factors.
Safety considerations are important in clinical use. Propylthiouracil has been associated with rare but severe side effects such as agranulocytosis, hepatotoxicity, and vasculitis. Monitoring of blood counts and liver function tests is recommended during therapy. Due to risk of hepatotoxicity, propylthiouracil is often reserved for specific clinical scenarios, such as during the first trimester of pregnancy or when patients are intolerant to alternative agents.
Notable brand names and usage contexts vary globally, but propylthiouracil remains an essential antithyroid agent in therapeutic arsenals for hyperthyroidism management.
From an API sourcing perspective, it is critical to ensure high purity and compliance with pharmacopeial standards given the compound’s narrow therapeutic index and potential for toxicity. Quality control should include rigorous testing for impurities, consistent batch characterization, and adherence to good manufacturing practices to support regulatory approvals and clinical safety.
Identification & chemistry
| Generic name | Propylthiouracil |
|---|---|
| Molecule type | Small molecule |
| CAS | 51-52-5 |
| UNII | 721M9407IY |
| DrugBank ID | DB00550 |
Pharmacology
| Summary | Propylthiouracil inhibits thyroid peroxidase, blocking the iodination of tyrosine residues in thyroglobulin and thereby reducing synthesis of thyroid hormones T4 and T3. It also decreases peripheral conversion of T4 to the more active T3. These effects collectively lower thyroid hormone levels, making propylthiouracil effective in managing hyperthyroidism associated with Graves' disease. |
|---|---|
| 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. |
| 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. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Thyroid peroxidase | Humans | inhibitor |
ADME / PK
| Absorption | Well absorbed following oral administration. |
|---|---|
| Half-life | 2 hours |
| Protein binding | 82% |
| 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. |
Formulation & handling
- Propylthiouracil is formulated primarily for oral and ophthalmic administration, including tablets and ophthalmic solutions.
- As a small molecule with moderate water solubility and LogP of 1.2, standard solid handling and formulation techniques apply.
- Consistent daily dosing timing is recommended to maintain stable plasma levels; no specific food sensitivity reported.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's primary patent protections expired in Canada and the US, leading to market entry of generic versions and increased competition. The product is currently in a mature phase with established presence in both markets. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Propylthiouracil includes multiple originator and generic pharmaceutical companies, reflecting a competitive supply chain. Branded products are primarily present in North American markets, specifically the US and Canada. The presence of numerous manufacturers and brand variants suggests that patent protections have likely expired, allowing for established generic competition. |
|---|
Safety
| Toxicity | Oral, rat: LD<sub>50</sub> = 1250 mg/kg. |
|---|
- Acute oral toxicity in rats shows an LD50 of 1250 mg/kg
- Handle with appropriate personal protective equipment to avoid ingestion and inhalation exposure
- Store in a well-ventilated area away from incompatible substances to prevent degradation
Propylthiouracil is a type of Thyreomimetics
Thyreomimetics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that mimic the actions of the thyroid hormones. These synthetic compounds are designed to interact with the thyroid hormone receptors and elicit similar effects as endogenous thyroid hormones, such as triiodothyronine (T3) and thyroxine (T4).
Thyroid hormones play a crucial role in regulating metabolism, growth, and development in the body. However, individuals with thyroid disorders, such as hypothyroidism or thyroid cancer, may have an impaired production of these hormones. Thyreomimetics offer a targeted therapeutic approach by acting as thyroid hormone agonists, stimulating the receptors and compensating for the deficiency.
These API subcategory drugs exhibit high selectivity and affinity for thyroid hormone receptors, ensuring minimal off-target effects. They are commonly used in the treatment of hypothyroidism, where the thyroid gland fails to produce adequate hormone levels. Thyreomimetics can help normalize metabolic processes and alleviate symptoms like fatigue, weight gain, and depression associated with hypothyroidism.
Furthermore, thyreomimetics are also employed in certain cases of thyroid cancer. By activating thyroid hormone receptors, they suppress the production of thyroid-stimulating hormone (TSH), which can promote tumor growth. This approach aids in the management of thyroid cancer by reducing TSH levels and inhibiting the proliferation of cancer cells.
In conclusion, thyreomimetics are a vital subcategory of pharmaceutical APIs used in the treatment of thyroid disorders. They act as synthetic thyroid hormone analogs, mimicking the effects of endogenous hormones and restoring normal physiological functions. With their targeted action and therapeutic benefits, thyreomimetics play a crucial role in improving the well-being of patients with thyroid-related conditions.
Propylthiouracil (Thyreomimetics), classified under Anti-Thyroid Agents
Anti-thyroid agents are a category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of thyroid disorders. These agents are specifically designed to target and inhibit the production or release of thyroid hormones in the body.
One commonly used anti-thyroid agent is propylthiouracil (PTU). PTU works by interfering with the synthesis of thyroid hormones within the thyroid gland, thereby reducing their production. Another widely used anti-thyroid agent is methimazole, which also acts by inhibiting thyroid hormone synthesis. These agents are typically prescribed for individuals with hyperthyroidism, a condition characterized by an overactive thyroid gland that produces an excessive amount of thyroid hormones.
Anti-thyroid agents are available in various forms, including tablets and solutions for oral administration. The dosage and duration of treatment may vary depending on the severity of the condition and individual patient factors.
It's important to note that anti-thyroid agents should be used under the guidance and supervision of a healthcare professional, as they may have potential side effects. These can include allergic reactions, liver toxicity, and blood disorders. Regular monitoring of thyroid function and liver function is typically recommended during treatment.
In summary, anti-thyroid agents are a class of pharmaceutical APIs used in the management of thyroid disorders. They work by inhibiting the production or release of thyroid hormones and are available in different formulations for oral administration. Proper medical guidance is essential for the safe and effective use of these agents.
Propylthiouracil API manufacturers & distributors
Compare qualified Propylthiouracil API suppliers worldwide. We currently have 4 companies offering Propylthiouracil API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Chemische Fabrik Berg | Producer | Germany | Germany | CoA, GMP, USDMF | 20 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Nantong Jinghua | Producer | China | China | CoA, GMP, WC | 12 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, USDMF | 764 products |
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