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Propylthiouracil
- indication:Used to manage hyperthyroidism which is due to an overactive thyroid gland (Grave's disease).
- pharmacologypharmacology:
- mechanism: 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.
- toxicity: Oral, rat: LD<sub>50</sub> = 1250 mg/kg.
- absorprion: Well absorbed following oral administration.
- halflife: 2 hours
- roouteelimination: 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.
- volumedistribution:
- clearance: