Ballicules › Drugs › Propylthiouracil
What it is Thionamide inhibiting thyroid peroxidase and peripheral thyroid-hormone activation; hyperthyroidism.
Why this one Its peripheral conversion block makes it useful in thyroid storm, and it is preferred early in pregnancy.
What limits it Severe liver failure keeps it second-line otherwise; agranulocytosis demands urgent evaluation of fever or sore throat.
FDA-approved for
FDA label
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BOXED WARNING Severe liver injury and acute liver failure (some fatal, some requiring transplant) reported in adults and children; reserve for patients who cannot tolerate methimazole and in whom radioactive iodine or surgery are not appropriate.
FDA dosing Population Start Target Max
Hyperthyroidism Adults 300 mg/day divided q8h (TID) maintenance 100–150 mg/day 400 mg/day usual; occasionally 600–900 mg/day initially (severe)
Hyperthyroidism Pediatric ≥6y (rare; only when alternatives inappropriate) 50 mg/day, titrate upward
Renal Undefined
Hepatic Undefined
Instructions Give total daily dose in 3 equal doses at ~8-hour intervals Reserve for patients intolerant of methimazole or when RAI/surgery inappropriate
Cautions Severe hepatotoxicity / acute liver failure — monitor, warn patient Myelosuppression (agranulocytosis, granulopenia, aplastic anemia, thrombocytopenia) — report fever/infection ANCA-positive vasculitis with severe complications/death Lupus-like syndrome Serious hypersensitivity reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis) Hypoprothrombinemia and bleeding
Adverse reactions Liver injury (hepatitis, liver failure) Agranulocytosis/granulopenia/aplastic anemia Thrombocytopenia Drug fever Lupus-like syndrome ANCA-associated vasculitis Skin rash/urticaria Nausea/vomiting/epigastric distress Arthralgia Paresthesias Loss/perversion of taste
Pregnancy May be the preferred antithyroid agent during or just before the first trimester (methimazole teratogenicity); crosses placenta and can cause fetal goiter/cretinism — use lowest effective dose; given maternal hepatotoxicity risk, consider switching to methimazole for 2nd/3rd trimesters.
Lactation Undefined
⚠ BOXED WARNING
Severe liver injury and acute liver failure
Cost, est. cash $10–$300/month
Generic entry 2023
Classes and tags
Clinical profile
Therapeutic safety burden 4 / 4
Overdose danger 2 / 4
Weight-gain liability 0 / 4
Sedation liability 0 / 4
QT / Torsades 0 / 4
Direct muscarinic antagonism 0 / 4
Embryofetal risk 1 / 4
Legacy pregnancy category Unknown / historical label unavailable
Defining liability Potentially fatal hepatic failure and agranulocytosis; generally reserved for selected situations.
Mechanism of action: Propylthiouracil ballicule
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